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‫م‬2011 ‫دليل أدوية مستشفى االمير عبد الرحمن المركزي سكاكا‬

DRUG FORMULARY HOSPITAL

Table of contents

1. GIT DRUGS
 01.01 – ANTIACID
 01.02 – ANTISPASMODIC
 01.03 – MOTILITY STIMULANTS
 01.04 – ULCER - HEALING DRUGS
 01.05 – ANTIIDIARRHEAL DRUGS
 01.06 – DRUGS FOR INFLAMMATORY BOWEL DISEASE
 01.07 – LAXATIVES
 01.08 – ANTIFLATULENT
 01.09 – HEMORRHOID PREPARATIONS
 01.10 – DRUGS AFFECTING INTESTINAL SECRETIONS

2. CARDIOVASCULAR DRUGS
 02.01 – POSITIVE INTROPIC DRUGS
 02.02 – DIURETICS
 02.03 – ANTIARRHYTHMIC DRUGS
 02.04 – BETA – ADRENOCEPTER BLOCKING DRUGS
 02.05 – ANTIHYPERTENSIVE DRUGS
 02.06 –NO3,CA-CHANNEL BLOCKERS&P. VASODILATOR
 02.07 – SYMPATHOMIMETICS
 02.08 – ANTICOAGULANTS AND PROTAMINE
 02.09 – ANTIPLATELET DRUGS
 02.10 – FIBRINOLYTIC DRUGS
 02.11 – ANTIFIBROLYTIC DRUGS AND HEMOSTATICS
 02.12 – LIPID – LOWERING DRUGS
 02.13 – LOCAL SCLEROSANTS

3. RESPIRATORY DRUGS
 03.01 – BRONCHODILATORS
 03.02 – CORTICOSTEROIDS
 03.04 – ANTIHISTAMINES &ALLERGIC EMERGENCIES
 03.05 – PULMONARY SURFACTANTS
 03.06 – COUGH SUPPRESSANTS ,EXPECT.&DECONGESTANTS

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4. CNS DRUGS
 04.01 – HYPNOTICS & ANXIOLYTICS
 04.02 – ANTIPSYCHOTIC & ANTIMANIC DRUGS
 04.03 – ANTIDEPRESSANT DRUGS
 04.04 – CNS STIMULANTS
 04.05 – DRUGS USED IN NAUSEA & VERTIGO
 04.06 – ANALGESICS
 04.07 – ANTIEPILEPTICS
 04.08 – DRUGS USED IN PARKISONISM &RELATED DISORDERS

5. DRUGS USED IN THE TREATMENT OF INFECTIONS


 05.01 – ANTIBACTERIAL DRUGS
 05.02 – ANTIFUNGAL DRUGS
 05.03 – ANTIVIRAL DRUGS
 05.04 – ANTIPROTOZOAL DRUGS
 05.05 – ANTHELMINTICS

6. ENDOCRINE DRUGS
 06.01 – DRUGS USED IN DIABETES
 06.02 – THYROID & ANTITHYROID DRUGS
 06.03 – CORTICOSTEROIDS
 06.04 – HYPOTHALAMIC,PITUIT. HORM.&ANTIESTEROGENS
 06.05 – DRUGS AFFECTING BONE METABOLISM

DRUGS AFFECTING NUTRITION AND BLOOD .07


 07.01 – ANEMIAS & SOME OTHER BLOOD DISORDERS
 07.02 – FLUIDS & ELECTROLYTES
 07.05 – VITAMINS
 07.06 – METABOLIC DISORDERS

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MUSCULOSKELETAL&JOINT DISEASES .08
 08.01 – DRUGS USED IN RHEUMATIC DISEASES & GOUT
 08.02 – DRUGS USED IN NEUROMUSCULAR DISORDES
 08.03 – DRUGS FOR THE RELIEF OF SOFT TISSUE INFLAMM.

DRUGS ACTING ON THE EYE .09


 09.01 – ANTIINFECTIVE EYE PREPARATIONS
 09.02 – ANTIINFLAMMATORY PREPARATIONS
 09.03 – MYDRIATICS & CYCLOPLEGICS
 09.04 – TREATMENT OF GLAUCOMA
 09.05 – LOCAL ANESTHETICS
 09.06 – MISCELLANEOUS OPTHALMIC PREPARATIONS

EAR , NOSE &OROPHARYNEX DRUGS .10


 10.01 – DRUGS ACTING ON THE EAR
 10.02 – DREUGS ACTING ON THE NOSE
 10.03 – DRUGS ACTING ON THE OROPHARYNEX

DRUGS ACTING ON THE SKIN .11


 11.01– TOPICAL CORTICOSTEROIDS
 11.02 – PREPARATIONS FOR ECZEMA & PSORIASIS
 11.03– ANTIINFECTIVE SKIN PREPARATIONS

IMMUNOLOGIC PRODUCTS AND VACCINES .12

 14.01 – VACCINES & ANTISERA


 14.02 – IMMUNOGLOBULINS
 14.03 – ANTIVENOMS

DRUGS USED IN ANESTHESIA .13

 15.01 – GENERAL ANESTHESIA


 15.02 – LOCAL ANETHESIA

ANTIDOTES .14

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GIT DRUGS

 01.01 – ANTIACID

Generic Name Dosage Form brand


name
Al&Mg Hydroxide Tablets moxal
Al&Mg Hydroxide Suspension

MOA Aluminum &Mg hydroxide is used to treat the symptoms


of increased stomach acid in conditions such as heartburn, acid
reflux, acid indigestion, sour stomach, and stomach ulcers

Aluminum can decrease the effects of many other medicines by


binding to them ,Store aluminum hydroxide at room temperature
away from moisture and heat

Aluminum hydroxide may cause side effects.

constipation and loss of appetite diarrhea

Dose 1-2 tab chewed every 2-4 hrs

C.I hypophosphatemia

FDA PREGNANCY C

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 01.02 – ANTISPASMODIC

Hyocine Tablets 10mg/tab buscopane


Butylbromide

Hyocine Suppository 10mg/supp scopinal


Butylbromide

Hyocine Injection 20mg/amp spasmopan


Butylbromide

Mebeverine Tablets 135- DUSPATALIN


Hcl 200mg

Hyocine Butylbromide :

MOA :peripheral anti cholinergic

USES: This medication is used to relieve bladder or intestinal


spasms.

HOW TO USE: Take as directed. The usual maximum number of


tablets per day is 6. Swallow tablets whole with a glass of water.
Take at least one hour before antacids or certain anti-diarrhea
drugs (e.g., kaolin-pectin type).

SIDE EFFECTS: Constipation, dry mouth, trouble urinating, or


nausea could occur. If these continue or are bothersome, notify
your doctor promptly. Very unlikely but report: rash, itching,
swelling of the hands or feet, trouble breathing, increased pulse,
dizziness, diarrhea, vision problems, eye pain.

PRECAUTIONS: glaucoma or other eye problems, heart disease,


enlarged prostate (males), allergies, stomach or intestinal diseases.

FDA PREGRANCY C

Mebeverine Hcl

MOA musculotropic antispasmodic drug without atropic side-


effects whose major therapeutic role is in the treatment of irritable
bowel syndrome.

indicated for treatment of gastrointestinal spasm secondary to


organic disorder Irritable bowel syndrome.
- Chronic irritable colon.
- Spastic colitis.

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 Dose 135mg 3 times daily 20 min before meals
60 mg 3 times daily (children)
 Precautions: should be used with caution during pregnancy and lactation

 01.04 – ULCER - HEALING DRUGS


a-H2- RECEPTOR ANTAGONIST

Ranitidine Tablets 150 mg Zantac

Ranitidine Hcl Injection 50mg

MOA Ranitidine is in a group of drugs called histamine-2


blockers. Ranitidine works by reducing the amount of acid your
stomach produces.

USES Ranitidine is used to treat and prevent ulcers in the


stomach and intestines. It also treats conditions in which the
stomach produces too much acid, such as Zollinger-Ellison
syndrome. Ranitidine also treats gastroesophageal reflux disease
(GERD) and other conditions in which acid backs up from the
stomach into the esophagus, causing heartburn. Long term use
may cause vit b12 difficiency

DOSE 50mg / 6-8 hrs (not exceed 400 mg /d ) iv or im

maintains oral dose 150 mg at night ph .k : up to 50% of oral


dose is absorbed

b-PROTON PUMP INHIBITORS

Omeprazole or Capsule 20mg losec


Lansoprazole or30mg/cap
40mg vial* Proton
Omeprazole Sodium or* Injection* 40mg vial* risk

Pantoprazole Sodium* Injection*

20 mg nexium
esomeprasole tab

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MOA irreversible bloking system of H+/K+ ATP ase

Indication to treat and prevent ulcers in the stomach and


intestines. It also treats conditions in which the stomach produces
too much acid, such as Zollinger-Ellison syndrome. Ranitidine
also treats gastroesophageal reflux disease (GERD) and other
conditions in which acid backs up from the stomach into the
esophagus, causing heartburn.

Omeprasole enhance the effect of warfarin &diazepam .

FDA CATEGORY C

01.05 – ANTIIDIARRHEAL DRUGS

Generic Name Dosage Remarks Trade


Form name
Loperamide Hcl Capsule 2mg/caps imodum

MOA Slows intestinal motility, affects water and electrolyte


movement through intestine, inhibits peristalsis, reduces daily fecal
volume, increases viscosity and bulk density of stool, diminishes
loss of fluid and electrolytes Control and symptomatic relief of acute
nonspecific or chronic diarrhea; reduction in volume of ileostomy
output.
DOSE INITIAL DOSE 4 MG FOLLOWED BY 2 MG AFTER
EACH LOOSE STOOL TO MAX. OF 16 MG DAILY

01.06 – DRUGS FOR INFLAMMAORY BOWEL DISEASE

Sulfasalazine Tablets 500mg/tabs SALAZOPYRIN

 Sulfasalazine affects a substance in the body that causes


inflammation, tissue damage, and diarrhea.

 Sulfasalazine is used to treat moderate to severe ulcerative colitis.


It is also used to treat rheumatoid arthritis in children and adults

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who have received other arthritis medications without successful
treatment of symptoms.

 Sulfasalazine dose MD 500mg /3times /d

 01.07 – LAXATIVES

Bulk – sachet 270 mg fybogel


forming
laxative
Stimulant Tablets 5mg/tab dulcolax
Bisacodyl
Bisacodyl Pediatric 5mg/suppository
Supp.
Bisacodyl Adult Supp. 10mg/suppository
Glycerin 900mg glycerin
Adult
Suppository
Senna Tablets 5-10mg/tab laxal
(sennosides)
OSMOTICLAXATIVES
Osmotic Syrup 2- duphelac
Lactulose 250 4g/5ml
ml
Phosphate 100- fleet
Enema Enema 150ml

Definition : Laxatives are products that promote bowel movements.

Description: Laxatives may be grouped by mechanism of action.

Stimulant and irritant laxatives increase the peristaltic movement of


the intestine. Examples include cascara and bisadocyl (Dulcolax.)
Castor oil works in a similar fashion.

Bulk producing laxatives increase the volume of the stool, and will
both soften the stool and stimulate intestinal motility. Psyillium
(Metamucil, Konsil) and methylcellulose (Citrucel) are examples
of this type. The overall effect is similar to that of eating high-fiber
foods, and this class of laxative is most suitable for regular use.

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Mineral oil is an emollient laxative. It acts by retarding intestinal
absorption of fecal water, thereby softening the stool.

The hyperosmotic laxatives are glycerin and lactulose (Chronulac,


Duphalac), both of which act by holding water within the intestine.
Lactulose may also increase peristaltic action of the intestine

Precautions

Short-term use of laxatives is generally safe except in cases of


appendicitis, fecal impaction, or intestinal obstruction. Lactulose is
composed of two sugar molecules, galactose and fructose, and
should not be administered to patients who require a low-galactose
diet.

Chronic use of laxatives may result in fluid and electrolyte


imbalances, steatorrhea, osteomalacia, diarrhea, cathartic colon,
and liver disease. Excessive intake of mineral oil may cause
impaired absorption of oil soluble vitamins.

Lactulose and magnesium sulfate are pregnancy category B.


Casanthranol,

Interactions

Mineral oil and docusate should not be used in combination.


Docusate is an emulsifying agent that will increase the absorption
of mineral oil.

Bisacodyl tablets are enteric coated, and so should not be used in


combination with antacids. The antacids will cause premature
rupture of the enteric coating.

laxative

 Bulk-producing agents
 Lubricants
 Osmotics
 Irritants

Bulking agents
 Site of Action: Small and large intestine
 Onset of Action: 12 - 72 hours
 Examples: fibocyt

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 Bulk-producing agents cause the stool to be bulkier and to retain
more water, They should be taken with plenty of water. Bulk-
producing agents have the gentlest of effects among laxatives and
can be taken just for maintaining regular bowel movements.

Lubricants / Emollient
 Site of Action: Colon
 Onset of Action: 6 - 8 hours

These simply make the stool slippery, so that it slides through the
intestine more easily.

mineral oil, which also retards colonic absorption of water,


softening the stool. Mineral oil may decrease the absorption of fat-
soluble vitamins and some minerals.

Hydrating agents (osmotics)

These cause the intestines to hold more water within, softening the
stool. There are two principal types, saline and hyperosmotic.

Saline
 Site of Action: Small and large intestine
 Onset of Action: 0.5 - 6 hours
 Examples: Dibasic sodium phosphate, magnesium citrate,
magnesium hydroxide (Milk of magnesia), magnesium sulfate
(which is Epsom salt) , monobasic sodium phosphate, sodium
biphosphate.

Saline laxatives attract and retain water in the intestinal lumen,


increasing intraluminal pressure and thus softening the stool. They
will also cause

the release of cholecystokinin, which stimulates the digestion of fat


and protein. Saline laxatives may alter a patient's fluid and
electrolyte balance.

Hyperosmotic agents
 Site of Action: Colon
 Onset of Action: 0.5 - 3 hours
 Examples: Glycerin suppositories, and Lactulose .

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Lactulose works by the osmotic effect, which retains water in the
colon, lowering the pH and increasing colonic peristalsis.
Lactulose is also indicated in Portal-systemic encephalopathy.
Glycerin suppositories work mostly by hyperosmotic action

Stimulant / Irritant

 Site of Action :Colon

Examples
Onset of Action Laxative Name

 Bisacodyl tablets (Dulcolax) (laxal)


6 - 10 hours
 Senna (Ex-lax)

2 - 6 hours  Castor oil


 Bisacodyl suppository
15 min - 1 hour

These stimulate peristaltic action and can be dangerous under


certain circumstances. Long term use can lead to 'cathartic colon'.
Stimulant laxatives act on the intestinal mucosa, or nerve plexus;
they also alter water and electrolyte secretion. They are the most
severe among laxatives and should be used only in extreme
conditions. Castor oil may be preferred when more complete
evacuation is required.

Castor oil
 Site of Action

Small intestine

Castor oil acts directly on intestinal mucosa or nerve plexus and


alters water and electrolyte secretion. It is converted into ricinoleic
acid (the active component) in the gut.

Uses

Chronic constipation. Chronic immobility.


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Side effects

Laxative abuse is potentially serious since it can lead to

 intestinal paralysis,
 Irritable Bowel Syndrome (IBS)

 pancreatitis,

 renal failure

antispasmodic

Hyoscyamine, is a chemical compound, a tropane alkaloid. It is


the levorotary isomer to atropine

Pharmacology

Hyoscyamine ( buscopane, scoplamine )is an anticholinergic,


specifically an antimuscarinic, working by blocking the action of
acetylcholine at parasympathetic sites in smooth muscle, secretory
glands and the CNS; increases cardiac output, dries secretions, and
.antagonizes serotonin

Uses

Hyoscyamine is used to provide symptomatic relief to various


gastrointestinal disorders including spasms, peptic ulcers,
irritable bowel syndrome, pancreatitis, colic and cystitis. It has
also been used to relieve some heart problems, control some of
the symptoms of Parkinson's disease, as well as for control of
respiratory secretions in palliative care.

Side effects

Side effects include dry mouth and throat, eye pain, blurred vision,
restlessness, dizziness, arrythmia, flushing, faintness. An overdose
will cause headache, nausea, vomiting and CNS symptoms
including disorientation, hallucinations, euphoria, short term
memory loss and possible coma in extreme cases.

 01.08 – ANTIFLATULENT

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Generic Dosage strength Brand
Name Form name
Simethicone Tablet 60mg/tab

It is a mixture of polydimethylsiloxane and silica gel.

Simethicone allows gas bubbles in the stomach and intestines to


come together more easily, which allows for easier passage of gas.

Simethicone is used to relieve painful pressure caused by excess gas


in the stomach and intestines.

FDA pregnancy category C. This medication may be harmful to an


unborn baby. Simethicone works best if you take it after meals and
at bedtime. The chewable tablet must be chewed before
swallowing. Store simethicone at room temperature away from
moisture, light, and heat.

Dose / Capsules or tablets:

Adults and teenagers: 60 to 125 milligrams (mg) four times a day,


after meals and at bedtime. No more than 500 mg should be taken
in twenty-four hours.
 Chewable tablets:

Adults and teenagers: 40 to 125 mg four times a day, after meals and
at bedtime or the dose may be 150 mg three times a day, after
meals. No more than 500 mg should be taken in twenty-four hours.

01.09 – HEMORRHOID PREPARATIONS


SOOTHING PREPARATIONS WITH CORTICOSTEROIDS
Hemorrhoidal Soothing Tube 30g/Tube
Ointment
Hemorrhoidal Soothing Supp.
Supp.*

reparation H Ointment relieves both internal and external


hemorrhoidal symptoms. It is effective at shrinking swollen
hemorrhoidal tissues and gives prompt soothing relief from painful
burning, itching and discomfort.
Apply to the affected area up to 4 times daily, especially at night, in
the morning and after each bowel movement. For Intrarectal Use:
Before applying, remove protective cover from applicator. Attach
applicator
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 01.11

Ursodeoxycholic Tablet* 300 mg* ursodiol


Acid

MOA Ursodiol, also known as ursodeoxycholic acid and the


abbreviation UDCA, is one of the secondary bile acids, which
are metabolic byproducts of intestinal bacteria.

02. CARDIOVASCULAR DRUGS

 02.01 – POSITIVE INTROPIC DRUGS

Digoxin Tablet 125microgram/tab lanoxin


Digoxin Tablet 250microgram/tab
Digoxin Injection 100microgram/inj
Digoxin Injection 500microgram/inj

 MOA Digoxin increases the force of contraction of the


muscle of the heart by inhibiting the activity of an enzyme
(ATPase) that controls movement of calcium, sodium and
potassium into heart muscle.
 PRESCRIBED FOR: Digoxin is used for mild to moderate
congestive heart failure and for treating an abnormal heart
rhythm called atrial fibrillation.
DOSING: Digoxin may be taken with or without food. Digoxin is
primarily eliminated by the kidneys; therefore, the dose of
digoxin should be reduced in patients with kidney dysfunction.
Digoxin blood levels are used for adjusting doses in order to
avoid toxicity. The usual starting dose is 0.0625-0.25 mg daily
depending on age and kidney function. The dose may be
increased every two weeks to achieve the desired response.
INTERACTIONS: Drugs such as verapamil (Isoptin, Isoptin SR),
quinidine (Quinaglute, Quinide), amiodarone (Cordarone),
indomethacin (Indocin, Indocin-SR), alprazolam (Xanax, Xanax
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XR, Niravam), spironolactone (Aldactone), and itraconazole
(Sporanox) can increase digoxin levels and the risk of toxicity.

 02.02 – DIURETICS

a-THIAZIDES & RELATED DIURETICS


Chlorthalidone Tablet 50mg/tab
Hydrochlorothiazid Tablet 25mg/tab Esidrix
e
Indapamide Tablet 2.5mg/tab natrilix

MOA The members of this class of diuretics are derived from


benzothiadiazine. They inhibit Na+/Cl- reabsorption from the
distal convoluted tubules in the kidneys by blocking the thiazide-
sensitive Na+-Cl- symporter. Thiazides also cause loss of
potassium and an increase in serum uric acid
Indications

Thiazides are often used to treat hypertension, although they are


also used to treat congestive heart failure and symptomatic edema.

Side effects include hypokalemia, increased serum cholesterol,


triglyceride, impaired glucose tolerance, diabetes mellitus and
impotence.

b-LOOP DIURETICS

Furosemide Tablet 40mg/tab lasix


Furosemide Injection 20mg/amp
Furosemide Injection 250mg/amp, vial
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Furosemide is a potent diuretic (water pill) that is used to
eliminate water and salt from the body

DOSING: The usual starting oral dose for treatment of edema in


adults is 20-80 mg as a single dose. The same dose or an increased
dose may be administered 6-8 hours later. Doses may be increased
20-40 mg every 6-8 hours until the desired effect occurs. The
effective dose may be administered once or twice daily. Some
patients may require 600 mg daily. The starting oral dose for
children is 2 mg/kg. The starting dose may be increased by 1-2
mg/kg every 6 hours until the desired effect is achieved. Doses
greater than 6 mg/kg are not recommended. The recommended
dose for treating hypertension is 40 mg twice daily.

DRUG INTERACTIONS: Administration of furosemide with


aminoglycoside antibiotics (for example, gentamicin) or
[ethacrynic acid (Edecrin) - another diuretic] may cause hearing
damage. Furosemide competes with aspirin for elimination in the
urine by the kidneys. Concomitant use of furosemide and aspirin
may, therefore, lead to high blood levels of aspirin and aspirin
toxicity

c-POTASSIUM-SPARING DIURETICS & COMBINED DIURETICS

Spironolactone Tablet 25mg/tab Aldactone

(spironolactone) is indicated in the management of:

Primary hyperaldosteronism for:

Establishing the diagnosis of primary hyperaldosteronism by


therapeutic trial.
Short-term preoperative treatment of patients with primary
hyperaldosteronism.
Long-term maintenance therapy for patients with discrete
aldosterone-producing adrenal adenomas who are judged to be poor
operative risks or who decline surgery.
Long-term maintenance therapy for patients with bilateral micro or
macronodular adrenal hyperplasia (idiopathic hyperaldosteronism).

Edematous conditions for patients with:

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Congestive heart failure: For the management of edema and sodium
retention when the patient is only partially responsive to, or is
intolerant of, other therapeutic measures. Aldactone is also indicated
for patients with congestive heart failure taking digitalis when other
therapies are considered inappropriate.
Cirrhosis of the liver accompanied by edema and/or ascites:
Aldosterone levels may be exceptionally high in this condition.
Aldactone is indicated for maintenance therapy together with bed
rest and the restriction of fluid and sodium.
The nephrotic syndrome: For nephrotic patients when treatment of
the underlying disease, restriction of fluid and sodium intake, and
the use of other diuretics do not provide an adequate response.

Essential hypertension

Usually in combination with other drugs, Aldactone is indicated for patients


who cannot be treated adequately with other agents or for whom
other agents are considered inappropriate.

Hypokalemia

For the treatment of patients with hypokalemia when other measures are
considered inappropriate or inadequate. Aldactone is also indicated
for the prophylaxis of hypokalemia in patients taking digitalis when
other measures are considered inadequate or inappropriate.

PRECAUTIONS: Dependent edema in pregnancy, resulting from restriction


of venous return by the expanded uterus,

 02.03 – ANTIARRHYTHMIC DRUGS

a-SUPRAVENTRICULAR ARRHYTHMIAS
Adenosine for inj Injection
ection 6mg/vial adenocore

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MOA Adenosine injection slows conduction time through the A-
V node, can interrupt the reentry pathways through the A-V node,
and can restore normal sinus rhythm in patients with paroxysmal
supraventricular tachycardia (PSVT), including PSVT associated
withWolff-Parkinson-White Syndrome

Adenosine is antagonized competitively by methylxanthines such


as caffeine and theophylline, and potentiated by blockers of
nucleoside transport such as dipyridamole. Adenosine is not
blocked by atropine
PHK
The half-life of Adenosine injection is less than 10 seconds.
adverse effects are generally rapidly self-limiting. Treatment of
any prolonged adverse effects should be individualized and be
directed toward the specific effect. Methylxanthines, such as
caffeine and theophylline, are competitive antagonists of
Adenosine

b-SUPRAVENTRICULAR &VENTRICULAR ARRHYTHMIAS


Amiodarone Hcl Tablet
200mg/tab cordaron
Amiodarone Hcl for Injection
injection 150mg/amp amrinon
Quinidine Sulphate or Tablet
Bisulphate 200or250mg/tab

Amiodarone HCl is a member of a new class of antiarrhythmic


drugs with predominantly Class IIIThe antiarrhythmic effect of
Amiodarone may be due to at least two major properties: 1) a
prolongation of the myocardial cell-action potential duration and
refractory period and 2) noncompetitive α- and β-adrenergic
inhibition
PHK
Following oral administration in man, Amiodarone is slowly and
variably absorbed. The bioavailability of Amiodarone is
approximately 50%, but has varied between 35 and 65% in
various studies. Maximum plasma concentrations are attained 3
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to 7 hours after a single dose. Despite this, the onset of action
may occur in 2 to 3 days, but more commonly takes 1 to 3 weeks,
even with loading doses. Plasma concentrations with chronic
dosing at 100 to 600 mg
FDA pregnancy category D.

SIDE EFFECT wheezing, cough, chest pain, trouble breathing,


coughing up blood;
blurred vision, headache or pain behind your eyes, sometimes
with vomiting;
feeling short of breath, even with mild exertion, swelling, rapid
weight gain;

weight loss, thinning hair, feeling too hot or too cold, increased
sweating, irregular menstrual periods, swelling in your neck
(goiter); numbness, burningAn oral loading dose is typically a
total of 10 grams, divided over one to two weeks but there are
many other dosing regimens. Once an individual is loaded, a
typical maintenance dose of amiodarone is 100 or 200 mg either
once or twice daily.

DOSE

An intravenous loading dose is typically 300 mg in 20-30cc D5W


for cardiac arrest. The loading infusion for dysrhythmias is
typically 150 mg in a 100cc bag of D5W given over 10 minutes.
Both can be followed by a 360 mg slow infusion over 6 hours
then a maintenance infusion of 540 mg over 18 hours.

c-VENTRICULAR ARRHYTHMIAS
Lidocaine Hcl 1% Injection
or2% 100mg/amp
Lidocaine Hcl 2% Injection
100mg/pre.syringe
Mexiletine Hcl Injection
250mg/amp

Pharmacology - Lidocaine is considered to be a class IB


(membrane-stabilizing) antidysrhythmic agent. It is thought that

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lidocaine acts by combining with fast sodium channels when
inactive which inhibits recovery after repolarization
A potent local anesthetic and antiarrhythmic agent, lidocaine HCl
occurs as a white, odorless, slightly bitter tasting,
Storage/Stability/Compatibility - Lidocaine for injection should
be stored at temperatures less than 40°C and preferably between
15-30°C; avoid freezing.
 
Lidocaine is compatible with most commonly used IV infusion
solutions, including D5W, lactated Ringer’s, saline, and
combinations of these. It is also reportedly physically compatible
with: aminophylline, bretylium tosylate, calcium chlo-
ride/gluceptate/gluconate, carbenicillin disodium, chloramphenicol
sodium succinate, chlorothiazide sodium, cimetidine HCl,
dexamethasone sodium phosphate, digoxin, diphenhydramine HCl,
dobutamine HCl, ephedrine sulfate, erythromycin lactobionate,
glycopyrrolate, heparin sodium, hydrocortisone sodium succinate,
hydroxyzine HCl, insulin (regular), mephentermine sulfate,
metaraminol bitartrate, methicillin sodium, metoclopramide HCl,
nitrofurantoin sodium, oxytetracycline HCl, penicillin G
potassium, pentobarbital sodium, phenylephrine HCl, potassium
chloride, procainamide HCl, prochlorperazine edisylate, promazine
HCl, sodium bicarbonate, sodium lactate Lidocaine may not be
compatible with

dopamine, epinephrine, isoproterenol or norepinephrine as these


require low pH’s for stability.

Lidocaine is reportedly incompatible with: ampicillin sodium,


cefazolin sodium,

methohexital sodium, or phenytoin sodium. Compatibility is


dependent upon factors such as pH, concentration, temperature,
and diluents used and it is suggested to consult specialized
references for more specific information.
Pharmacokinetics - Lidocaine is not effective orally as it has a
high first-pass effect. If very high oral doses are given, toxic
symptoms occur (due to active metabolites?) before therapeutic
levels can be reached. Following a therapeutic IV bolus dose, the
onset of action is generally within 2 minutes and has a duration of
action of 10-20 minutes.

 
20
Adverse Effects/Warnings - At usual doses and if the serum level
remains within the proposed therapeutic range (1 - 5
micrograms/ml), serious adverse reactions are quite rare. The most
common adverse effects reported are dose  related (serum level)
and mild. CNS signs include drowsiness, depression, ataxia,
muscle tremors, etc. Nausea and vomiting may occur, but are
usually transient. Adverse cardiac effects generally only occur at
high plasma concentrations and are usually associated with PR and
QRS interval prolongation and QT interval shortening. Lidocaine
may increase ventricular rates if used in patients with atrial
fibrillation. If an IV bolus is given too rapidly, hypotension may
occur.
 
MEXILETINE

Mechanism of Action
Mexiletine hydrochloride is a local anesthetic, antiarrhythmic agent,
structurally similar to lidocaine, but orally active. In animal
studies, Mexiletine has been shown to be effective in the
suppression of induced ventricular arrhythmias, including those
induced by glycoside toxicity and coronary artery ligation.
Mexiletine, like lidocaine, inhibits the inward sodium current, thus
reducing the rate of rise of the action potential

02.04 – BETA – ADRENOCEPTER BLOCKING DRUGS

Propranolol Hcl Tablet 10mg/tab inderal


Propranolol Hcl Injection 1mg/amp
Atenolol Tablet 50mg/tab tenormin
Labetolol Hcl Tablet 100mg/tab trandate
Carvedilol OR Tablet 6.25 mg
BisoprololFummarate

Carvedilol OR Tablet 25 mg
BisoprololFummarate
Metoprolol tatrate* Score Tablet* 50mg/score tab* lopresor

21
Propranolol is used to treat tremors, angina (chest pain),
hypertension (high blood pressure), heart rhythm disorders, and
other heart or circulatory conditions. It is also used to treat or
prevent heart attack, and to reduce the severity and frequency of
migraine headaches . side effects may include:nausea, vomiting,
diarrhea, constipation, stomach cramps; decreased sex drive,
impotence, or difficulty having an orgasm; sleep problems
(insomnia); or tired feeling.

Atenolol (Tenormin) is a selective β1 receptor antagonist, a drug belonging to the group of beta
blockers (sometimes written β-blockers), a class of drugs used primarily in cardiovascular
diseases. Introduced in 1976, atenolol was developed as a replacement for propranolol in the
treatment of hypertension. The chemical works by slowing down the heart and reducing its
workload. Unlike propranolol, atenolol does not pass through the blood-brain barrier thus avoiding
various central nervous system side effects.

Indications

Atenolol can be used to treat cardiovascular diseases and conditions such as hypertension,
coronary heart disease, arrhythmias, angina (chest pain) and to treat and reduce the risk of heart
complications following myocardial infarction (heart attack). It is also used to treat the symptoms
of Graves Disease, until antithyroid medication can take effect.

Due to its hydrophilic properties, the drug is less suitable in migraine prophylaxis compared to
propranolol, because, for this indication, atenolol would have to reach the brain in high
concentrations.

Pharmacokinetic data
 tcmax = 2 to 4 hours after oral dosing (time elapsed before maximal concentration in the blood plasma
is reached)
 The mean elimination halflife is 6 hours. However, the action of the usual oral dose of 25 to 100 mg
lasts over a period of 24 hours.
 Atenolol is a hydrophilic drug. The concentration found in brain tissue is approximately 15% of the
plasma concentration only. The drug crosses the placenta barrier freely. In the milk of breastfeeding
mothers, approximately 3 times the plasma concentrations are measured.
 Atenolol is almost exclusively eliminated renally and is well removable by dialysis. A compromised
liver function does not lead to higher peak-activity and/or a longer halflife with possible
accumulation

Contraindications
 bradycardia
 cardiogenic shock
 asthma (may cause broncho-constriction), although unlikely as atenolol is cardioselective
 symptomatic hypotension (blood pressure of less than 90/60 mm Hg with dizziness, vertigo etc.)
 angina of the Prinzmetal type (vasospastic angina)
 metabolic acidosis (a severe condition with a more acidic blood than normal)
 severe disorders in peripheral arterial circulation
 AV-Blockage of second and third degree (a particular form of arrhythmia)
22
 acutely decompensated congestive heart failure (symptoms may be fluid retention with peripheral
edema and/or abdominal fluid retention (ascites), and/or lung edema)
 sick sinus syndrome (a particular form of arrhythmia)
 hypersensitivity and/or allergy to atenolol
 pheochromocytoma (a rare type of tumor of the adrenal glands)

Side effects include:

 indigestion, constipation
 dry mouth
 dizziness or faintness (especially cases of orthostatic hypotension)
 cold extremities
 hair loss
 impotence
 rhinitis
 depression
 confusion
 insomnia, nightmares
 fatigue, weakness or lack of energy

labetalol is a mixed alpha/beta adrenergic antagonist, which is used to treat high blood pressure

Indications

It has a particular indication in the treatment of pregnancy-induced hypertension which is


commonly associated with pre-eclampsia.[6]

It is also used to treat chronic and acute hypertension of pheochromocytoma and hypertensive
crisis.[4]

Administration

Labetalol is available in 100, 200, and 300 mg tablets and intravenously (only as Trandate) in
5 mg/ml solution. Adults taking tablets usually start with 100 mg twice daily, with a maximum of
2.4 g/day. In cases of emergency dosage might be higher. IV doses are usually started at 20 mg
over 2 minutes. Additional doses of 40 mg, then 80 mg may be administered every ten minutes as
needed. Additional 80 mg doses can be given to a total maximum dose of 300 mg. Additionally,
labetalol can be administered by IV infusion at a rate of 2 mg/minute, with a maximum dose of
300 mg.

Side effects

Side effects may include:

 Drowsiness
 Fatigue
 Weakness
 Difficulty sleeping
 Diminished sexual function
 Scalp tingling which passes after time.
 Drug eruption similar to lichen planus[7]
 A rare but potentially lethal side effect is respiratory distress.

23
Contraindications

Labetalol has relative contraindications for use in patients with asthma, congestive heart failure,
any degree of heart block, bradycardia, or those in cardiogenic shock.

Carvedilol is a non-selective beta blocker/alpha-1 blocker indicated in the treatment of mild to


moderate congestive heart failure (CHF)

Pharmacology

Carvedilol is both a beta blocker (β1, β2) and alpha blocker (α1):.

Relative to other beta blockers, carvedilol has minimal inverse agonist activity.[4] This suggests
that carvedilol has a reduced negative chronotropic and inotropic effect compared to other beta
blockers, which may decrease its potential to worsen symptoms of heart failure. However, to date
this theoretical benefit has not been established in clinical trials, and the current version of the
ACC/AHA guidelines on congestive heart failure management does not give preference to
carvedilol over other beta-blockers.

Side effects

The most common side effects include dizziness, fatigue, hypotension, diarrhea, asthenia,
bradycardia, and weight gain

Clinical use

Carvedilol is indicated in the management of congestive heart failure (CHF), as an adjunct to


conventional treatments (ACE inhibitors and diuretics). The use of carvedilol has been shown to
provide additional morbidity and mortality benefits in CHF.[9] Carvedilol (Coreg) is available at the
following doses 3.125 mg (smallest), followed by 6.25 mg, 12.5 mg, and 25 mg white tablets.

02.05 – ANTIHYPERTENSIVE DRUGS

a-VASODILATOR ANTIHYPERTENSIVE DRUGS


Diazoxide Injection 300mg/amp
Hydralazine Hcl Tablet 25mg/tab apresoline
Hydralazine Hcl Injection 20mg/amp Apresoline
Sodium Nitoprusside Injection 50mg/vialor
amp

DIAZOXIDE helps to reduce blood pressure in an emergency


situation. It is not for regular use in the reduction of blood
pressure. may interact with this medicine

24
• diuretics
• medicines for high blood pressure
• warfarin

It is used as a vasodilator in the treatment of acute hypertension.

It is also used in diabetes, to decrease the secretion of insulin in


disease states such as insulinoma (a tumor producing insulin).

Uses:

S.E allergic reactions like skin rash, itching or hives, swelling


of the face, lips, or tongue
• chest pain, palpitations
• confusion
• feeling faint or lightheaded, falls
• trembling, restlessness
• unusual swelling or sudden weight gain
• unusual bleeding or bruising
• unusually weak or tired

hydralasine is a direct-acting smooth muscle relaxant used to


treat hypertension by acting as a vasodilator primarily in arteries
and arterioles. By relaxing vascular smooth muscle, vasodilators
act to decrease peripheral resistance, thereby lowering blood
pressure Hydralazine is not used as a primary drug for treating
hypertension because it elicits a reflex sympathetic stimulation of
the heart (the baroreceptor reflex).

The sympathetic stimulation may increase heart rate and cardiac


output, and may cause angina pectoris or myocardial infarction.[1]
Hydralazine may also increase plasma renin concentration,
resulting in fluid retention. In order to prevent these undesirable
side effects, hydralazine is generally prescribed in combination
with a beta-blocker (e.g., propranolol) and a diuretic

Hydralazine is used to treat severe hypertension, but again, it is


not a first line therapy for essential hypertension. However,
hydralazine is the first line therapy for hypertension in
pregnancy, with methyldopa. Common side effects include:

 Diarrhea
 Compensatory tachycardia due to baroreceptor reflex
 Headache
 Loss of appetite
 Nausea or vomiting
 Depression
25
 Drug induse lupus erthromatosis

There are 38 known medications to cause DIL but there are three
that report the highest number of cases: hydralazine,
procainamide, and isoniazid

Na nitroprussied :This salt serves as a source of nitric oxide, a


potent peripheral vasodilator that affects both arterioles and
venules (venules more than arterioles). Sodium nitroprusside is
often administered intravenously to patients who are
experiencing a hypertensive emergency. Nitroprusside is light-
sensitive, and breaks down in sunlight, producing cyanide.

MOA: Its mechanism of action appears to be liberation of nitric


oxide (NO), which causes relaxation of vascular smooth muscle.
Nitroprusside also releases cyanide ions which are converted in
the liver to thiocyanate by the enzyme rhodanase, a reaction
which requires a sulfur donor such as thiosulfate. Alternatively,
cyanide may react with methemoglobin to form
cyanomethemoglobin. Thiocyanate is then excreted by the
kidney. In the absence of sufficient thiosulfate, cyanide ions can
quickly reach toxic levels. The half-life of nitroprusside is 1-2
minutes although thiocyanate has an excretion half life of several
days. The duration of treatment should not exceed 72 hours and
thiocyanate plasma concentrations should be monitored.

b-CENTRALLY ACTING ANTIHYPERTENSIVE DRUGS


Methyldopa Tablet 250 mg/tab aldomet

Methyl dopa is a centrally-acting adrenergic antihypertensive


medication

.MOA Methyldopa, in its active metabolite form, is a central


alpha-2 receptor agonist. Using methyldopa leads to alpha-2
receptor-negative feedback to sympathetic nervous system (SNS)
(centrally and peripherally), allowing peripheral sympathetic
nervous system tone to decrease. Such activity leads to a
decrease in total peripheral resistance (TPR) and cardiac output.

26
c-ALPHA – ADRENOCEPTOR BLOCKING DRUGS
Prazosin Hcl Tablet 1mg/tab miniprees
Prazosin Hcl Tablet 5mg/tab Minipress,

Prazosin is a sympatholytic drug used to treat high blood


pressure (hypertension). It belongs to the class of alpha-
adrenergic blockers, which lower blood pressure by relaxing
blood vessels. Specifically, prazosin is selective for the alpha-1
receptors on vascular smooth muscle. These receptors are
responsible for the vasoconstrictive action of norepinephrine
USES: hypertension or prostatic hyperplasia,

d-ANGIOTENSIN – CONVERTING ENZYME INHIBITORS


Captopril Tablet 25mg/tab capotine
Enalapril or Lisinopril Tablet 10mg/tab Zestril Renetic

Captopril's main uses are based on its vasodilation and inhibition of some renal function activities.
These benefits are most clearly seen in the following conditions:

1) Hypertension

2) Cardiac conditions such as post myocardial infarction and congestive heart failure

3) Preservation of kidney function in diabetic nephropathy

It has also been investigated for use in the treatment of cancer.

Adverse effects of captopril include cough due to increase in the plasma levels of bradykinin, angioedema,
agranulocytosis, proteinuria, hyperkalemia, taste alteration, teratogenicity, postural hypotension, acute renal
failure and leukopenia

Lisinopril :is a drug of the angiotensin converting enzyme (ACE) inhibitor class that is primarily used in
treatment of hypertension, congestive heart failure, heart attacks and also in preventing renal and retinal
complications of diabetes. It has been compared with omapatrilat which is of similar function.
Lisinopril does not undergo metabolism and is excreted unchanged entirely in the urine.

Adverse effects

Side effects, some or all of which are serious and require immediate medical attention, include:

 Chills, infection
27
 Dark urine, decreased urination (oliguria)
 Difficulty swallowing or breathing (signs of angioedema), allergic reaction (anaphylaxis)
 Hoarseness
 Itching
 Rapid weight gain, stomach pain
 Yellowing of skin or eyes (jaundice)
 Abdominal pain, bloating, vomiting
 Chest pain or tightness, dizziness, lightheadedness, fainting (syncope)

e–NITRATES,CA. - CHANNEL BLOCKERS&P. VASODILATORS

NITRATES
Nitroglycerin Transdermal 10mg/24-hour
Nitroglycerin Injection 50mg/vialor amp
Isosorbide Sublingual Tablet 5mg/subling. tab isordil
Dinitrate
Isosorbide Tablet 10mg/ tab
Dinitrate
Isosorbide Sust.ReleaseTablet 20mg/ s.r.tab isomak
Dinitrate

NITROGLYCERIN is a type of vasodilator. It relaxes blood


vessels, increasing the blood and oxygen supply to your heart. This
medicine is used to relieve chest pain caused by angina. It is also
used to prevent chest pain before activities like climbing stairs,
going outdoors in cold weather, or sexual activity.

USES: This medication is a nitrate used to relieve and prevent


chest pain (angina). Nitroglycerin relaxes blood vessels allowing
more blood to flow through. This reduces the workload on the
heart and improves blood flow to the heart.

HOW TO USE: At the first sign of chest pain, sit down and place
one tablet under the tongue or between your cheek and gum
allowing it to dissolve. The drug is absorbed directly through the
lining of the mouth SIDE EFFECTS: Burning or tingling under
the tongue, headache, dizziness, flushing, or restlessness may
occur. If any of these effects persist or worsen, notify your doctor
or pharmacist promptly. To minimize dizziness and
lightheadedness, get up slowly when rising from a seated or lying
position. Tell your doctor immediately if any of these serious side
effects occur: blurred vision, dry mouth, nausea, pale skin, rapid
heartbeat. Headache

Isosorbide dinitrate:
28
Uses

It is more useful in preventing angina attacks than reversing them once they have
commenced. It may be given as a tablet for the treatment of an angina attack.

CA. - CHANNEL BLOCKERS


Tablet 60mg/ tab Tildiem
Diltiazem Hcl
Nifidipine 20mg/ tab Adalat ret.
Retard Tablet

Verapamil Hcl Tablet 40mg/ tab Isoptien


Verapamil Hcl Tablet 80mg/ tab
Verapamil Hcl Injection 5mg/ amp

Diltiazem :Potent vasodilator of coronary vessels.

Vasodilator of peripheral vessels. This reduces peripheral resistance and afterload.

Negative inotropic effect. Diltiazem causes a modest decrease in heart muscle contractility and
reduces myocardium oxygen consumption.

Negative chronotropic effect. Diltiazem causes a modest lowering of heart rate. This effect is due
to slowing of the SA (sinoatrial) node. It results in reduced myocardium oxygen consumption.

Negative dromotropic effect. By slowing conduction through the AV (atrioventricular) node,


diltiazem increases the time needed for each beat. This results in reduced myocardium oxygen
consumption by the body.

Indications

Angina:

 Stable angina (exercise-induced) . Diltiazem increases coronary blood flow and decreases
myocardial oxygen consumption, secondary to decreased peripheral resistance, heart rate, and
contractility.[4][5]

 Variant angina. Diltiazem is effective due to its direct effects on coronary dilation.

 Unstable angina (preinfarction, crescendo). Diltiazem may be particularly effective if the underlying
mechanism is vasospasm.

Drug interactions

Beta-blockers

29
Intravenous diltiazem should be used with caution with beta-blockers, because while the
combination is most therauputically beneficial, there are rare instances of dysrhythmia and AV
node block.[9]

Quinidine

Quinidine should not be used concurrently with calcium channel blockers because of reduced
clearance of both drugs and potential pharmacodynamic effects at the SA and AV nodes.

Nifedipine is used to treat high blood pressure and to control angina (chest pain). Nifedipine is
in a class of medications called calcium-channel blockers. It works by relaxing the blood vessels
so the heart does not have to pump as hard. It also increases the supply of blood and oxygen to
the heart.

Nifedipine comes as a capsule and an extended-release (long-acting) tablet to take by mouth. The
capsule is usually taken three or four times a day. The extended-release tablet should be taken
once daily on an empty stomach, either 1 hour before or 2 hours after a meal. Take nifedipine at
around the same time(s) every day. Follow the directions on your prescription label carefully, and
ask your doctor or pharmacist to explain any part you do not understand. Take nifedipine exactly
as directed. Do not take more or less of it or take it more often than prescribed by your doctor.

Swallow the extended-release tablets whole; do not split, chew, or crush them.

Nifedipine may cause side effects. Tell your doctor if any of these symptoms are severe
or do not go away:
 headache
 nausea
 dizziness or lightheadedness
 flushing (feeling of warmth)
 heartburn
 fast heartbeat
 muscle cramps
 constipation
 cough
 decreased sexual ability

Symptoms of overdose may include:


 dizziness
 fast heartbeat
 flushing (feeling of warmth)
 nervousness
 nausea
 vomiting
 swelling of the hands, feet, ankles, or lower legs
 blurred vision
 fainting

30
Verapamil is a calcium ion influx inhibitor (slow-channel blocker or calcium
ion antagonist) available for oral administration in film-coated tablets
containing 40 mg, 80 mg,

Indicated for the treatment of the following:

Angina

1. Angina at rest including:


-Vasospastic (Prinzmetal's variant) angina
-Unstable (crescendo, pre-infarction) angina
2. Chronic stable angina (classic effort-associated angina)

Arrhythmias

1. In association with digitalis for the control of ventricular rate at


rest and during stress in patients with chronic atrial flutter
and/or atrial fibrillation (see WARNINGS: Accessory bypass
tract)
2. Prophylaxis of repetitive paroxysmal supraventricular
tachycardia

Essential hypertension

Dose the usual dos e is 80 mg to 120 mg three times a day.


However, 40 mg three times a day

f-PERIPHERAL VASODILATORS
75mg/cap stugron
Cinnarazine Capsule 5mg/tab
Tablet*
Amlodipine Besilate*
Pentoxifylline Tablet 400mg/ tab trental
Pentoxifylline Injection 300mg/ amp

Cinnarizine

Mechanism Of Action:
Binds to the Histamine H1 receptor and to muscarinic
acetylcholine receptors. Cinnarizine also inhibits contractions of
vascular smooth muscle cells by blocking L type calcium channels.
Cinnarizine has also been implicated in binding to dopamine D2
receptors.

31
Stugeron tablets contain the active ingredient cinnarizine, which is
a type of medicine called an antihistamine
Cinnarizine is used to control travel sickness and the symptoms of
inner ear disorders such as Meniere's disease.
Competitive antagonists at histamine H1 receptors may be divided
into first (sedating) and second (non-sedating) generation agents.
Some, such as Cinnarizine also block muscarinic acetylcholine
receptors and are used as anti-emetic agents. Cinnarizine through
its calcium channel blocking ability also inhibits stimulation of the
vestibular system. For the treatment of vertigo/meniere's disease,
nausea and vomiting, motion sickness and also useful for
vestibular symptoms of other origins.

used for

Preventing and treating motion sickness

 Relieving nausea, vomiting, attacks of dizziness or spinning


sensations (vertigo) and sensations of ringing or other noise in the
ears (tinnitus) associated with Meniere's disease and other middle
ear disorders.

Pentoxifyline : Pentoxifylline improves blood flow through peripheral blood vessels and therefore
helps with blood circulation in the arms and legs (e.g. intermittent claudication), and the brain (hence its use
in vascular dementia).

MOA : Pentoxifylline has also been used to treat nausea and headaches in the mountains (altitude sickness),
competitive nonselective phosphodiesterase inhibitor [4] which raises intracellular cAMP, activates PKA,
inhibits TNF-alpha [5][6] and leukotriene [7] synthesis, and reduces inflammation and innate immunity [7] and

In addition, pentoxifylline improves red blood cell deformability, reduces blood viscosity and
decreases the potential for platelet aggregation and thrombus formation. [8]

Drug interaction

Co-administration of pentoxifylline and sodium thiopental causes death by acute pulmonary


edema in rats.[9]

02.07 – SYMPATHOMIMETICS

a-INTROPIC SYMPATHOMIMETICS
Injection 250mg/vialor dobutrex
Dobutamine Hcl amp

32
Injection 200mg/vialor
Dopamine Hcl amp
Isoprenaline Hcl Injection 200mic.gm/ Isuprel® 
amp

Dobutamine is indicated when parenteral therapy is necessary


for inotropic support in the short-term treatment of adults with
cardiac decompensation due to depressed contractility resulting
either from organic heart disease or from cardiac surgical
procedures. Experience with intravenous dobutamine in
controlled trials does not extend beyond 48 hours of repeated
boluses and/or continuous infusions. Do not add dobutamine to
5% Sodium Bicarbonate Injection or to any other strongly
alkaline solution. Because of potential physical incompatibilities,
it is recommended that dobutamine not be mixed with other
drugs in the same solution.

Preparation and Stability – At the time of administration,


dobutamine must be further diluted in an IV container to at least
a 50 mL solution using one of the following intravenous
solutions as a diluent: 5% Dextrose Injection, 5% Dextrose and
0.45% Sodium Chloride Injection, 5% Dextrose and 0.9%
Sodium Chloride Injection, 10% Dextrose Injection, Isolyte®M
with 5% Dextrose Injection, Lactated Ringer's Injection, 5%
Dextrose in Lactated Ringer's Injection, Normosol®-M in D5-W,
20% Osmitrol® in Water for Injection, 0.9% Sodium Chloride
Injection, or Sodium Lactate Injection. Intravenous solutions
should be used within 24 hours.

Recommended Dosage – Infusion of dobutamine should be


started at a low rate (0.5 to 1.0 mcg/kg/min) and titrated at
intervals of a few minutes, guided by the patient's response,
including systemic blood pressure, urine flow, frequency of
ectopic activity, heart rate and (whenever possible)
measurements of cardiac output, central venous pressure, and/or
pulmonary capillary wedge pressure..

S.E Increased Heart Rate, Blood Pressure, and Ventricular


Ectopic Activity.
33
Dopamine :This medication is used to treat heart conditions. The medication provides
additional pumping strength by stimulating the heart muscle. In some patients it
is used for improving kidney blood supply. This drug is given by injection
through a vein (larger arm vein is preferred) in an IV solution. The dilution and
amount of medication given depend on the condition treated and how much
fluid can be safely given. Follow all doctor and pharmacist instructions exactly.
If MAO inhibitors (see Drug Interactions) have been used within the past 2-3
weeks, the starting dose of this drug should be no more than one-tenth of the
usual dose. The contents of the IV solution should be examined for
discoloration or particles before use. Solutions darker than slightly yellow or
containing particles should be discarded. The infusion rate of this drug should
be slowly reduced before stopping. Other IV solutions may be needed to
prevent low blood pressure.

SIDE EFFECTS: Nausea, vomiting or headache may occur. If these persist or


worsen, notify your doctor. Report promptly: any irregular or rapid heartbeat,
chest pain, dizziness, trouble breathing. Unlikely but report promptly: any major
change in the amount of urine, unusually cool skin, rapid change in skin color,
painful arms or legs. If you notice other effects not listed above, contact your
doctor or pharmacist.

PRECAUTIONS: Before using this drug, tell your doctor your medical history,
including: any allergies (especially drug allergies), blood vessel disease,
pheochromocytoma, irregular heartbeats (arrhythmias). Leakage of the IV
solution into the tissue around the vein is to be avoided. Swelling or pain at the
injection site must be promptly reported. Caution is advised when using this
drug in the elderly because they may be more sensitive to the effects of the
drug. This medication should be used only when clearly needed during
pregnancy. Discuss the risks and benefits with your doctor. It is not known
whether this drug is excreted into breast milk. Because of the potential risk to
the infant, breast-feeding while using this drug is not recommended. Consult
your doctor before breast-feeding.

DRUG INTERACTIONS: Tell your doctor of all nonprescription and


prescription medication you may use, especially: MAO inhibitors (e.g.,
furazolidone, linezolid, phenelzine, selegiline, tranylcypromine), beta-
blockers (e.g., metoprolol, propranolol), alpha-blockers (e.g., prazosin,
doxazosin, terazosin), anesthetics (e.g., halothane or cyclopropane),
phenytoin. Do not add this drug to IV solutions containing sodium
bicarbonate or other alkaline solutions, oxidizing agents or IV iron products
since this drug will be inactivated. Do not start or stop any medicine without
doctor or pharmacist approval.

OVERDOSE: If overdose is suspected, contact your local poison control


center or emergency room immediately. US residents can call the US
national poison hotline at 1-800-222-1222. Canadian residents should call
their local poison control center directly.

NOTES: Frequent blood and urine tests and heart monitoring are performed
with use of this medication.

MISSED DOSE: Not applicable. This drug is given continuously until


therapy is completed.

STORAGE: Store at room temperature between 59 and 86 degrees F (15-


30 degrees C) away from light and moisture. This medication is stable for a
34
minimum of 24 hours after it is diluted into the IV solution. Follow all
instructions for proper storage/use. Consult the pharmacist.

Isoproterenol is a synthetic beta1 and beta2 adrenergic agonist


that has no appreciable alpha activity at therapeutic doses. It is
thought that isoproterenol’s adrenergic activity is a result of
stimulating cyclic-AMP production. Its primary actions are
increased inotropism and chronotropism, relaxation of bronchial
smooth muscle and peripheral vasodilitation. Isoproterenol may
also increase perfusion to skeletal muscle (at the expense of vital
organs in shock). Isoproterenol will also inhibit the antigen-
mediated release of histamine and slow releasing substance of
anaphylaxis (SRS-A).
 

Uses/Indications - as adjunctive therapy in shock or heart failure


(limited use because of increases in heart rate and ventricular
arrhythmogenicity).
 
Pharmacokinetics - Isoproterenol is rapidly inactivated by the
GI tract and metabolized by the liver after oral administration.
Intravenous administration result in immediate effects, but only
persist for a few minutes after discontinuation.. Isoproterenol is
metabolized in the liver and other tissues by catechol-O-
methyltransferase (COMT) to a weakly active metabolite.
 
 
Adverse Effects/Warnings - Isoproterenol can cause
tachycardia, anxiety, tremors, excitability, headache, weakness
and vomiting.
Drug Interactions - Do not use with other sympathomimetic
amines (e.g., epinephrine) because of additive effects and
toxicity. Propranolol (or other beta-blockers) may antagonize
isoproterenol’s cardiac, bronchodilating, and vasodilating effects
by blocking the beta effects of isoproterenol. When isoproterenol
is used with potassium depleting diuretics (e.g., furosemide) or
other drugs that affect cardiac rhythm, there is an increased
chance of arrhythmias occurring.
Dosgeform:
Isoproterenol for Injection 1:5000 solution (0.2 mg/ml) in 1 & 5 ml
amps (Winthrop Pharm.); Generic; (Rx)
 
Isoproterenol sublingual or rectal Glossets 10 mg, 15 mg;
Isuprel® Glossets (Winthrop); (Rx)
35
 
Isoproterenol is also available in aerosol or solution form for oral
inhalation.

b-VASOCONSTRICTOR SYMPATHOMIMETICS
Injection 4mg/ amp
Noradrenaline

Injection 100mic.gm/ ml
Adrenaline1 :10,000
10ml/pre.sy.
Injection** 10mg/ amp**
Phenylepherine

Noradrenaline is a hormone and a neurotransmitter; it is


secreted by the adrenal medulla as a hormone into the blood, and
as a neurotransmitter from neurons.
Uses ;in depression ,vassopressor , Attention-deficit/hyperactivity
disorder
S.E : tissue hypoxia ,

Adrenaline : is a hormone naturally secreted by the medulla (inner portion) of the


adrenal gland, which are situated just above the kidneys. This hormone is secreted
along with noradrenaline (norepinephrine) to bring about the “flight or fight” response
in times of stress, exercise, and response to low blood sugar. It prepares the body for
strenuous activity or life-threatening situations. Increased secretion caused by fear or
anger results in increased heart rate, and glycogen in the liver is broken down to
glucose. The hormone was first extracted from the adrenal gland of animals in 1901,
and first synthesized in 1904.

In medicine adrenaline is used to treat:

• Anaphylaxis
• Cardiac arrest – stimulates the heart
• Asthma — acts as a bronchodilator (opens up the airways)
• Glaucoma — when applied topically to the eyes it decreases intra-ocular pressure
• Dental analgesia — added to local anaesthetic to reduce bleeding

Actions of Adrenaline

• Increased metabolism
• Cardiac stimulant & Increased heart rate
• Increased blood pressure
• Increased mental activity
• Increased blood flow to muscles
• Constriction of blood vessels (vasoconstriction)

36
Side Effects of Adrenaline

• Anxiety (transient), Fear & Tremor


• Cold fingers and toes and dry mouth (due to vasoconstriction)
• Headaches
• Pallor (“white as a sheet”) — also due to vasoconstriction
• Cardiac arrhythmias, Angina, and excessive rise in blood pressure
• Intracerebral bleeding leading to strokes
• Hyperventilation

Contraindications

Adrenaline may be administered in life-threatening anaphylactic reactions, even when


the following relative contraindications are present:

• Coronary artery disease


• Uncontrolled hypertension
• Serious ventricular arrhythmias (life-threatening abnormal heart rhythm)
• Second stage of labour

Interactions

• Sympathomimetics like ventolin & isoprenaline cause additive effects


• Beta-blockers antagonize therapeutic effects of adrenaline
• Digitalis potentiates the proarrhythmic effects of adrenaline
• Phenothiazine causes a paradoxical decrease in blood pressure
• Monoamine oxidase inhibitors (MOAIs) potentiate the cardiovascular effects of
adrenaline

Use of Adrenaline in Pregnancy

Classified as Pregnancy Category A: Adrenaline has been given to a large number of


pregnant women and women of child-bearing age without any proven increase in the
frequency of malformations or other direct or indirect harmful effects on the foetus
having been observed.

Precautions

Use with caution in elderly and patients that have:

• Hyperthyroidism
• Diabetes
• Hypertension
• Cardiovascular disease (angina, arrhythmias)
• Stroke
• Prostatic enlargement

Rapid intravenous infusion can cause death from cerebrovascular hemorrhage or


cardiac arrhythmias.

Dosage & Administration in Anaphylaxis

Adult
37
Adrenaline 1:1000, 0.3 to 0.5 mL (0.3-0.5mg), administered slowly. The dose may
be repeated every 10 minutes if necessary. In severe reactions the dose can be
increased to 1mL. The intramuscular route is better than the subcutaneous route.
Adrenaline 1:1000 should never be injected intravenously.

Children up to 12 years of age

Adrenaline 1:1000, 0.01ml / Kg (minimum 0.1ml 1:1000).

Phenylephrine is an α1-adrenergic receptor agonist used


primarily as a decongestant, as an agent to dilate the pupil, and to
increase blood pressure. Phenylephrine has recently been marketed
as a substitute for pseudoephedrine
 1 Uses
o .1 Decongestant
o .2 Mydriatic It is often used in combination with tropicamide
o .3 Vasopressor

side-effect of phenylephrine is hypertension

2. ANTICOAGULANTS AND PROTAMINE

4000U/4500U/syringe* clexan
Enoxaparin Injection*
5,000U/amp
Heparin Calcium Subcut.Injectio
n
25,000U/vial
Heparin Sodium Injection
Tablet 1,2,5 mg/ tab cumadine
Warfarin Sodium
50mg/amp
Protamine Sulphate Injection
20.000U/vial* inoohep
Tinzaparin Sodium* Injection*

38
Heparin and its derivatives (enoxaparin, dalteparin, tinzaparin) are
effective at preventing deep-vein thromboses and pulmonary emboli in
patients at risk

Heparin binds to the enzyme inhibitor antithrombin (AT)


causing a conformational change that results in its activation
through an increase in the flexibility of its reactive site loop.

Indecation :

Acute coronary syndrome, e.g., NSTEMI

 Atrial fibrillation
 Deep-vein thrombosis and pulmonary embolism
 Cardiopulmonary bypass for heart surgery.

 – ANTIPLATELET DRUGS

Tablet 75 – 100 mg/ tab ASPICARD


Aspirin
Tablet 75 or250mg/ tab PLAVIX
Clopidrogel or
Ticlopidine
Aspirin (acetylsalicylic acid). Pain reliever/fever reducer
Uses

 headache
 menstrual pain
 minor pain of arthritis
 muscle pain
 pain and fever of colds
 toothache

adults and children 12 years and over: take 1 or 2 tablets every 4 hours
or 3 tablets every 6 hours, not to exceed 12 tablets in 24 hours

WARNING Reye’s syndrome: Children and teenagers should not


use this medicine for chicken pox or flu symptoms

clopidogrel bisulfate) is an inhibitor of ADP-induced platelet


aggregation acting by direct inhibition of adenosine diphosphate

39
(ADP) binding to its receptor and of the subsequent ADP-mediated
activation of the glycoprotein GPIIb/IIIa complex

INDECATION : Recent MI, Recent Stroke or Established Peripheral


Arterial Disease

The recommended daily dose of Plavix is 75 mg once daily. Plavix


may be initiated with or without a loading dose (300 mg)

02.10 – FIBRINOLYTIC DRUGS

50mg/ vial
Alteplase Injection
250,000 U /
Streptokinase for Injection vial
injection
750,000 U /
Streptokinase for Injection vial
injection

Tissue plasminogen activator (abbreviated tPA or PLAT) is a


protein involved in the breakdown of blood clots. Specifically, it
is a serine protease (EC 3.4.21.68) found on endothelial cells, the
cells that line the blood vessels. As an enzyme, it catalyzes the
conversion of plasminogen to plasmin, the major enzyme
responsible for clot breakdown. Because it works on the clotting
system, tPA is used in clinical medicine to treat stroke
Treatment should only be initiated within 3 hours after the onset
of stroke symptoms

Streptokinase (SK), a protein secreted by several species of streptococci


can bind and activate human plasminogen. SK is used as an effective and
inexpensive clot-dissolving medication in some cases of myocardial
infarction (heart attack)[2] and pulmonary embolism.[3]. Streptokinase
belongs to a group of medications known as fibrinolytics, and complexes of
streptokinase with human plasminogen can hydrolytically activate other
unbound plasminogen by activating through bond cleavage to produce
plasmin. There are three domains to Streptokinase, denoted α (residues 1–
150), β (residues 151–287), and γ (residues 288–414).

40
 02.11 – ANTIFIBROLYTIC DRUGS AND HEMOSTATICS

Aminocaproic Acid Injection 500mg/or4g/amp,vial Amicar

Factor Vlll Fraction Injection 250U/ vial


(Human
antihemophilic
fraction)
Factor Vlll Fraction ( Injection 1000U/ vial
Human
antihemophilic
fraction )

Aminocaproic acid (also known as Amicar, ε-amino caproic acid, ε-Ahx, or 6-aminohexanoic
acid) is a derivative and analogue of the amino acid lysine, which makes it an effective inhibitor
for enzymes that bind that particular residue. Such enzymes include proteolytic enzymes like
plasmin, the enzyme responsible for fibrinolysis.
Aminocaproic acid is used to treat excessive postoperative bleeding, especially after procedures in
which a great amount of bleeding is indicated, such as cardiac surgery. It can be given orally or
intravenously>

Side effects

Its side effects include nausea, vomiting, and chronic mild fevers (99 degrees to 100 degrees).
When used long-term (for approx. 6 to 12 months) there is a risk of the inflammation of one's
internal organs, especially the appendix (appendicitis) and liver, as well as failure of the liver and
cyanosis. It almost always causes generalised myalgia and fibromyalgia. In some cases,
successive organ failure can occur after long-term usage. However, the main risk associated with
aminocaproic acid is the increased risk for thrombosis because of the inhibition of fibrinolysis.

Factor VIII also known as antihaemophilic factor A or AHF is a


plasma protein that participates in the intrinsic pathway of
blood coagulation.

Factor VIII circulates in the blood plasma in an extreme low


concentration in the form of a non-covalent complex of two
proteins Factor VIII:C is absent or defective in individuals
suffering from the bleeding disorder Haemophilia A affecting
about 5 out of 100.000 persons.

41
Factor VIII:C is absent or defective in individuals suffering from
the bleeding disorder Haemophilia A affecting about 5 out of
100.000 persons.

 02.12 – LIPID – LOWERING DRUGS

4g/ sachet
Cholestyramine Sachet
600mg tab LOPIDO
Gemfibrozil Tablet
10mg ZOCOR
Simvastatin Tablet or20mg/tab

CHOLESTYRAMINE
which sequester bile acid
fibrates decrease fatty acid and triglyceride levels by stimulating the
.peroxisomal β-oxidation pathway

Gemfibrozil helps reduce cholesterol and triglycerides (fatty acids) in the blood.
High levels of these types of fat in the blood are associated with an increased
risk of atherosclerosis (clogged arteries).

Gemfibrozil is used to treat very high cholesterol and triglyceride levels in people
with pancreatitis.

Gemfibrozil is also used to lower the risk of stroke, heart attack, or other heart
complications in people with high cholesterol and triglycerides who have not
been helped by other treatment methods.

Gemfibrozil is usually taken twice daily, 30 minutes before breakfast and dinner.

The statins inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG-


CoA) reductase and, thereby, suppress cholesterol biosynthesis

42
RESPIRATORY DRUGS

03.01 – BRONCHODILATORS

SELECTIVE BETA2- ADRENOCEPTOR STIMULANT


Salbutamol Tablet 4 mg/tab ventolin
Salbutamol 100- Syrup 2 mg/5ml
150ml/bottle
Salbutamol Inhaler 100micgm/inhalat.
200metered inhalation
Salbutamol 0.5 %for Solution 20 ml/bottle
nebulization

Salbutamol (INN) or albuterol is a short-acting β2-adrenergic


receptor agonist used for the relief of bronchospasm in
conditions such as asthma and chronic obstructive pulmonary
disease.

Also in Tocolytics are medications used to suppress premature


labor

The most common side effects are of fine tremor, nervousness,


headache, muscle cramps, dry mouth, and palpitation

ANTIMUSCARINIC
Inhaler 20micgm/inhalat. atrovent
Ipratropium Br
Ipratropium Solution 2 ml/vial
Bromide0.025%neb.

MOA It acts by blocking muscarinic receptors in the lung,


inhibiting bronchoconstriction and mucus secretion. It is a non-
selective muscarinic antagonist, and does not diffuse into the
blood, which prevents systemic side-effects. Ipratropium is a
derivative of atropine[3] but is a quaternary amine and therefore
does not cross the blood-brain barrier, which prevents central side-
effects (anticholinergic syndrome). Ipratropium is considered a
short-acting bronchodilator.;

USES It is administered by inhalation for the treatment of


obstructive lung diseases. And asthma.
43
S.E. dry mouth and sedation have been reported.

THEOPHYLLINE
Theophylline Sus.Re.Tab.or 250- QUIBRONE
Anhydrous Cap 300mg/tab/cap
Theophylline 100- Syrup 40-60 mg/5ml
200ml/bottle
Aminophylline Injection 250mg/amp

MOA: Theophylline, also known as dimethylxanthine, is a


methylxanthine drug used in therapy for respiratory diseases
such as COPD or asthma The main mechanism of action of
theophylline is that of adenosine receptor antagonism.
Theophylline is a non-specific inhibition of phosphodiesterase
enzymes, producing an increase in intracellular cyclic AMP

PHK

Bioavailability is 100%. However, taking the drug late in the


evening may slow the absorption process, without affecting the
bioavailability. Taking the drug after a meal high in fat content
will also s The use of theophylline is complicated by the fact
that it interacts with various drugs, chiefly cimetidine and
phenytoin, and that it has a narrow therapeutic index, so its use
must be monitored to avoid toxicity. It can also cause nausea,
diarrhea, increase in heart rate, arrhythmias, and CNS excitation
(headaches, insomnia, irritability, dizziness and
lightheadedness) [9][10]. Its toxicity is increased by erythromycin,
cimetidine, and fluoroquinolones, such as "cipro"
(ciprofloxacin). It can reach toxic levels when taken with fatty
meals, an effect called dose dumping.[11 low down the
absorption process, without affecting the bioavailability.

44
 03.02 – CORTICOSTEROIDS
Beclomethasone Inhaler 50mic.gm/inhalation becotide
Dipropionate
Beclomethasone Inhaler 100micgm/inhalation
Dippropionate or

BECLOMETHASON :is a potent glucocorticoid steroid. In the


form of an inhaler
it is used for the prophylaxis of asthma , sinusitis and in rihnitis
it is used to treat severe inflammatory skin disorders (e.g.
eczema) but is generally
avoided in the treatment of psoriasis due to the risk of rebound
on withdrawal.
S.E: Occasionally it may cause a cough upon inhalation.
Deposition on the
tongue and throat may promote oral candidiasis which appears as
a white coating
 03.03 – ANTIHISTAMINES &ALLERGIC EMERGENCIES
NONSEDATIVE ANTIHISTAMINES
Cetirizine or Tablet
loratidine 10mg/tab Zyrtic

Loratadine is an antihistamine drug used to treat allergies, and


marketed for its non-sedating properties

Indications

Loratadine is indicated for the symptomatic relief of allergy such


as hay fever (allergic rhinitis), urticaria (hives), and other skin
allergies.For allergic rhinitis (hay fever), loratadine is effective for
both nasal and eye symptoms: sneezing, runny nose, itchy or
burning eyes.

Mechanism of action

Loratadine is a tricyclic antihistamine, which selectively


antagonizes peripheral histamine H1-receptors. Histamine is
responsible for many features of allergic reactions.

Loratadine has a long-lasting effect and does not normally cause


drowsiness because it does not readily enter the CNS

SEDATIVE ANTIHISTAMINES
Chlorpheniramine Tablet 4mg/tab histop
Maleate
Diphenhydramine Syrup 12.5mg/5ml
45
Hcl 100ml
Promethazine Hcl Tablet 25mg/tab
Promethazine Hcl Syrup 5mg/5ml
100ml
Promethazine Hcl Injection 25mg/amp phenargan

Chlorpheniramine : is a first-generation alkylamine antihistamine used in the prevention of the


symptoms of allergic conditions such as rhinitis and urticaria. Its sedative effects are relatively
weak compared to other first-generation antihistamines.

Diphenhydramie is a first generation antihistamine mainly used to treat allergies. Like most other
first generation antihistamines, the drug also has a powerful hypnotic effect, and for this reason is
often used as a nonprescription sleep aid and a mild anxiolytic. The drug also acts as an antiemetic.
Diphenhydramine works by blocking the effect of histamine at H1 receptor sites. This results in
effects such as the increase of vascular smooth muscle contraction, thus reducing the redness,
hyperthermia and edema that occurs during an inflammatory reaction. In addition, by blocking the
H1 receptor on peripheral nociceptors, diphenhydramine decreases their sensitization and
consequently reduces itching that is associated with an allergic reaction, making it a popular choice
for treatment of the symptoms of allergic rhinitis, hives, motion sickness, and insect bites and
stings. It is also the reason many opioid users combine diphenhydramine (or other antihistamines)
to counteract the histamine-induced itching which is a common side effect of opioids

Common use and dosage

As an antihistamine, the recommended dose for adults is 25–50 mg diphenhydramine every four
to six hours.

Side effects

Like many other first-generation antihistamines, diphenhydramine can cause strong sedation, due
to H1 receptor antagonism. As such, diphenhydramine has also been used as an anxiolytic
because of this side effect. It is also a potent anticholinergic agent, leading to the side effects of
dry mouth and throat, increased heart rate, pupil dilation, urinary retention, constipation, and, at
high doses, hallucinations or delirium. Further side effects include motor impairment (ataxia),
flushed skin, blurred vision at nearpoint owing to lack of accommodation (cycloplegia), abnormal
sensitivity to bright light (photophobia), difficulty concentrating, short-term memory loss, visual
disturbances, irregular breathing, dizziness, irritability, itchy skin, confusion, decreased body
temperature (generally in the hands and/or feet), erectile dysfunction, and excitability

Promethazine is a first-generation H1 receptor antagonist of the phenothiazine chemical class


used medically as an antihistamine antiemetic. It has a strong sedative effect and in some
countries is prescribed for insomnia when benzodiazepines are contraindicated

Indications
 As a sedative.[3]
 For preoperative sedation and to counteract postnarcotic nausea.[3]
 As antiallergic medication to combat hay fever (allergic rhinitis), etc. To treat allergic reactions it
can be given alone or in combination with oral decongestants like pseudoephedrine.[3]
 As an adjunct treatment for anaphylactoid conditions (IM/IV route preferred).[3]
 Together with codeine or dextromethorphan against cough.
 As a motion sickness or seasickness remedy when used with Ephedrine or Pseudoephedrine.[3]

46
 03.06 – COUGH SUPPRESSANTS ,
EXPECT. & DECONGESTANTS
Dextromethorphan Hbr 60- Syrup 15mg/5ml
100 ml
Diphenhydramine Hcl, Syrup
Ammonium Chloride &
Sodium citrate about 100ml
bottle
Pseudoephedrine Tablet
&Antihistamine orCapsule
Pseudoephedrine Syrup 60 – 100
&Antihistamine ml /bottle

The primary use of dextromethorphan is as a cough suppressant, for the


temporary relief of cough caused by minor throat and bronchial
irritation
Dextromethorphan is rapidly absorbed from the gastrointestinal tract
and
converted into an active metabolite, dextrorphan, within 15 to 60
minutes of ingestion The average dosage necessary for effective
antitussive
therapy is between 10 mg and 45 mg, depending on the individual.
The duration of action after oral administration is approximately
three to eight hours for dextromethorphan-hydrobromide,

Side-effects of dextromethorphan use can include:

 body rash/itching
 nausea
 drowsiness
 dizziness
 fever
 vomiting
 blurred vision
 dilated pupils
 sweating

04-CNS DRUGS

 04.01 – HYPNOTICS & ANXIOLYTICS

Diazepam Tablet 5mg/tab


Diazepam Injection 10mg/amp
47
Alprazolam Tablet 250micr-
gm/tab
Alprazolam Tablet 500micr-
gm/tab

Diazepam is a benzodiazepine. It affects chemicals in the


brain that may become unbalanced and cause anxiety.
Diazepam is used for the management of anxiety disorders or
for the short-term relief of symptoms of anxiety. Diazepam
may also be used to relieve agitation, shakiness, and
hallucinations during alcohol withdrawal and relieve certain
types of muscle spasms. It may also be used to treat seizures,
insomnia, and other

Alprazolam : Alprazolam (trade name Xanax, among others) is


a potent short-acting drug of the benzodiazepine class. It is
primarily used to treat moderate to severe anxiety disorders (e.g.,
social anxiety disorder) and panic attacks, and is used as an
adjunctive treatment for anxiety associated with moderate
depression. It is available in an instant release and an extended-
release (Xanax XR) preparation, both of which are available under
several generic names. Alprazolam possesses anxiolytic, sedative,
hypnotic, anticonvulsant, and muscle relaxant properties.

Alprazolam has a fast onset of symptom relief (within the first


week). It is the most commonly misused benzodiazepine; however,
the majority of prescribed users do not develop a substance use
disorder.[4][5] Tolerance to the therapeutic effects of alprazolam is
controversial with one view being that alprazolam is ineffective with
long term use[6] and the other view being that tolerance to the
therapeutic effects does not occur.[7] A physical dependence
commonly occurs as a result of alprazolam treatment, typified by a
withdrawal and rebound symptoms necessitating a gradual
reduction in dosage to minimize withdrawal effects when
discontinuing.[4] Withdrawal symptoms similar in character to those
noted with sedative-hypnotics such as alcohol have occurred
following discontinuance of benzodiazepines, including alprazolam.
The symptoms can range from mild dysphoria and insomnia to a
major syndrome that may include anxiety, abdominal pain, muscle
cramps, vomiting, depression, sweating, tremors and in rare cases
seizures, suicidal ideation or suicide itself.

side-effects that may occur are as follows:

 Drowsiness, dizziness, lightheadedness, fatigue, unsteadiness and impaired


coordination, vertigo[29][30]
 Skin rash, respiratory depression, constipation[29][30]
 Disinhibition[31]
 Suicidal ideation (rare)[32][33]
 Urinary retention (infrequent)[34]
 Hallucinations (rare)[35]
48
 Ataxia, slurred speech[36]
 Short-term memory loss and impairment of memory functions, particular the
memory that the user experienced during the time of intoxication[37]
 Anterograde amnesia[38] and concentration problems
 Change in libido[39]
 Dry mouth (infrequent)[40]

 04.02 – ANTIPSYCHOTIC & ANTIMANIC DRUGS

ANTIPSYCHOTIC
Chlorpromazine Hcl Injection 25mg/amp
Haloperidol Tablet 1.5mg/tab
Haloperidol Injection 5mg/amp
Haloperidol Decanoate Injection 50mg/amp
Sulpiride Capsule or 50mg/cap
Tablet or tab

Chlorpromazine is a typical antipsychotic Chlorpromazine


works on a variety of receptors in the central nervous system,
producing anticholinergic, antidopaminergic, antihistaminic,
and weak antiadrenergic effects .

Indications

Chlorpromazine is classified as a low-potency typical antipsychotic and in the


past was used in the treatment of both acute and chronic psychoses,
including schizophrenia and the manic phase of bipolar disorder as well as
amphetamine-induced psychoses. Low-potency antipsychotics have more
anticholinergic side effects such as dry mouth, sedation and constipation, and
lower rates of extrapyramidal side effects, while high-potency antipsychotics
(such as haloperidol) have the reverse profile.

The use of chlorpromazine and other typical antipsychotics has been largely
replaced by newer generation of atypical antipsychotics which are generally
better tolerated. Recent global review of data supports its effectiveness as an
antipsychotic.

Chlorpromazine has also been used in porphyria and as part of tetanus


treatment. It still is recommended for short term management of severe
anxiety and aggressive episodes. Resistant and severe hiccups, severe
nausea/emesis and preanesthetic conditioning are other uses.

Adverse effects

The main side effects of chlorpromazine are due to its anticholinergic


properties; these effects overshadow and counteract, to some extent, the
extrapyramidal side effects typical of many early generation antipsychotics.
These include sedation, slurred speech, dry mouth, constipation, urinary
retention and possible lowering of seizure threshold. Appetite may be
increased with resultant weight gain, and Glucose tolerance may be impaired.
49
[21]
It lowers blood pressure with accompanying dizziness. [14] Chlorpromazine,
which has sedating effects, will increase sleep time when given at high doses
or when first administered, although tolerance usually develops. [22] Sleep
cycles or REM sleep is not altered by antipsychotics.[

Dosage and administration

A wide range is covered from 25 mg oral or intramuscular for mild sedation,
every 8 hours, up to 100 mg every 6 hours for severely ill patients. [17] Initial
doses should be low and be increased gradually. It is recommended that
most of the daily dose is given at bedtime for maximum hypnotic activity and
minimal daytime sedation and hypotension. In the US there are controlled
release forms of chlorpromazine (e.g. 300 mg). After the individual dose is
well established, such a CR capsule can be given with the evening meal as a
single dose, covering the next 24 hours. It is often administered in acute
settings as a syrup, which has a faster onset of action than tablets

Haloperidol is a typical antipsychotic. It is in the butyrophenone class of


antipsychotic medications and has pharmacological effects similar to the
phenothiazines.

Haloperidol is an older antipsychotic used in the treatment of schizophrenia


and, more acutely, in the treatment of acute psychotic states and delirium. A
long-acting decanoate ester is used as a long acting injection given every 4
weeks to people with schizophrenia or related illnesses who have a poor
compliance with medication and suffer frequent relapses of illness, or to
overcome the drawbacks inherent to its orally administered counterpart that
burst dosage increases risk or intensity of side effects. In some countries this
can be involuntary under Community Treatment Orders.

Pharmacology

Haloperidol is an antipsychotic and butyrophenone. Due to its strong central


antidopaminergic action, it is classified as a highly potent neuroleptic. It is
approximately 50 times more potent than chlorpromazine (sold under the
brand name Thorazine, among others) on a weight basis (50 mg
chlorpromazine is equivalent to 1 mg haloperidol). Haloperidol possesses a
strong activity against delusions and hallucinations, most likely due to an
effective dopaminergic receptor blockage in the mesocortex and the limbic
system of the brain. It blocks the dopaminergic action in the nigrostriatal
pathways, which is the probable reason for the high frequency of
extrapyramidal-motoric side effects (dystonias, akathisia,
pseudoparkinsonism). It has minor antihistaminic and anticholinergic
properties, therefore cardiovascular and anticholinergic side effects such as
hypotension, dry mouth, constipation, etc., are seen quite infrequently,
compared with less potent neuroleptics such as chlorpromazine. Haloperidol
also has sedative properties and displays a strong action against
psychomotor agitation due to a specific action in the limbic system. However,
in some cases haloperidol may worsen psychomotor agitation via its potent
dopamine receptor antagonism. Dopamine receptor antagonism, notably of
the D2 receptor subtype, can cause akathisia, psychomotor agitation, anxiety,
and restlessness, which may worsen the condition of some patients.

50
Sulpiride: is an anti-psychotic drug used mainly in the
treatment of psychosis (e.g. schizophrenia) and depression.
Sulpiride is a selective antagonist at postsynaptic D2-receptors.

Pharmacokinetics

Sulpiride is absorbed slowly from the GI-Tract. Its oral


bioavailability is only 25 to 35% with marked interindividual
differences. The peak plasma concentration is reached 4.5 hours
after oral dosing. The usual half-life is 6 to 8 hours. Ninety-two
percent is excreted unchanged in the urine. Sulpiride is usually
given in 2 or 3 divided doses.

Uses and dosage


 Productive psychosis: treatment with rather high doses—in
excess of 600 mg daily.
 Long-term Treatment of negative (unproductive) psychosis: in
moderate doses (approx. 600 mg daily)
 Treatment of depression and vertigo: in low to moderate doses
(50 to 200 mg daily)
 Levosulpiride has been promoted as a gastrointestinal prokinitic
agent

 04.03 – ANTIDEPRESSANT DRUGS

TRICYCLIC & RELATED DRUGS


Amitriptyline Hcl Tablet 10mg/tab
Imipramine Hcl Table 10mg/ta
t b
Imipramine Hcl Tablet 25mg/tab

indicated for the treatment of clinical depression, neuropathic


pain, nocturnal enuresis, and ADHD, but they have also been
used successfully for headache (including migraine
headache), anxiety, insomnia, smoking cessation and
Attention-deficit/hyperactivity disorder
Tricyclics with greater anti-muscarinic action(amitryptyline,
imipramine)

51
 04.05 – DRUGS USED IN NAUSEA & VERTIGO

ANTIHISTAMINES
Betahistine Tablet* 4mg/tab* Betaserc

Metoclopramide Hcl Tablet 10mg/tab


Metoclopramide Hcl Injection 10mg/amp plasil
Metoclopramide Hcl Suppository 10mg/suppository

Metoclopramide is a "prokinetic" drug that stimulates the


muscles of the gastrointestinal tract including the muscles of the
lower esophageal sphincter, stomach, and small intestine by
interacting with receptors for acetylcholine and dopamine on
gastrointestinal muscles and nerves

The anti-emetic action of metoclopramide is due to its


antagonist activity at D2 receptors in the chemoreceptor trigger
zone (CTZ) in the central nervous system (CNS)—this action
prevents nausea and vomiting triggered by most stimuli. At
higher doses, 5-HT3 antagonist activity may also contribute to
the anti-emetic effect.

The prokinetic activity of metoclopramide is mediated by


muscarinic

USES: Metoclopramide is used to relieve certain stomach-and-


esophagus problems such as diabetic gastroparesis and
gastroesophageal reflux disorder (GERD).

OTHER USES: This medication may also be used to prevent


nausea and vomiting caused by other medications. It may be
used for other purposes as determined by your doctor

SIDE EFFECTS: Nausea, diarrhea, headache, dizziness,


drowsiness, dry mouth, restlessness or sleeplessness may
occurand galactoria

metoclopramide has sometimes been used to stimulate


lactation. It can also be used in the treatment of migraines

SPECIFIC 5-HT3 SEROTONIN ANTAGONIST

Ondansetron Tablet 4mg/tab zofran

Ondansetron Injection 4mg/amp

52
MOA ondansetron is a serotonin 5-HT3 receptor
antagonist used mainly as an antiemetic to treat nausea and
vomiting following chemotherapy. Its effects are thought to
be on both peripheral and central nerves. Ondansetron reduces
the activity of the vagus nerve, which activates the vomiting
center in the medulla oblongata, and also blocks serotonin
receptors in the chemoreceptor trigger zone. It has little effect
on vomiting caused by motion sickness, and does not have
any effect on dopamine receptors or muscarinic receptors
USES
The clinical effect of ondansetron (and other drugs from the
same group) can be potentiated by combining it with
dexamethasone
Ondansetron lowers the cravings for alcohol, especially in
early-onset alcoholics

Irritable Bowel Syndrome

Odansetron blocks the 5-HT3 receptor in the enteric nervous


system, and thereby reduces colonic contractions, sensory
perception, and motility

side effects. Constipation, dizziness and headache are the


most commonly reported side effects associated with its use.

 04.06 – ANALGESICS

NONOPIOID ANALGESICS
Aspirin Tablet 500mg/tab
Paracetamol Tablet 500mg/tab
Paracetamol 100ml/bottle Liquid 120mg/5ml
Paracetamol Suppository 125 mg/supp.
Paracetamol Suppository 500 -.
Paracetamol Solution for 10mg /ml
infusion

Aspirin: also known as acetylsalicylic acid is a salicylate drug, often used as


an analgesic to relieve minor aches and pains, as an antipyretic to reduce
fever, and as an anti-inflammatory medication. Aspirin also has an antiplatelet
effect by inhibiting the production of thromboxane, which under normal
circumstances binds platelet molecules together to repair damaged blood
53
vessels. This is why aspirin is used in long-term, low doses to prevent heart
attacks, strokes, and blood clot formation in people at high risk for developing
blood clots.[1] It has also been established that low doses of aspirin may be
given immediately after a heart attack to reduce the risk of another heart attack
or of the death of cardiac tissue.

The main undesirable side effects of aspirin are gastrointestinal ulcers,


stomach bleeding, and tinnitus, especially in higher doses. In children and
adolescents, aspirin is no longer used to control flu-like symptoms or the
symptoms of chickenpox or other viral illnesses, because of the risk of Reye's
syndrome

Paracetamol It is commonly used for the relief of fever, headaches, and other
minor aches and pains, and is a major ingredient in numerous cold and flu
remedies. In combination with non-steroidal anti-inflammatory drugs (NSAIDs)
and opioid analgesics, paracetamol is used also in the management of more
severe pain (such as postoperative pain).

MOA : Paracetamol is usually classified along with nonsteroidal antiinflammatory


drugs (NSAID), but is not considered one. Like all drugs of this class, its main
mechanism of action is the inhibition of cyclooxygenase (COX), an enzyme
responsible for the production of prostaglandins, which are important mediators of
inflammation, pain and fever. Therefore, all NSAIDs are said to possess anti-
inflammatory, analgesic (anti-pain), and antipyretic (anti-fever) properties. The
specific actions of each NSAID drug depends upon their pharmacological
properties, distribution and metabolism.

OPIOID ANALGESICS
Morhine Sulphate Injection 10mg/amp
Pethidine Hcl Injection 50mg/amp
Pethidine Hcl Injection 100mg/amp

MORPHIN is a highly potent opiate analgesic psychoactive drug, is the principal


active ingredient in Papaver somniferum (opium poppy, or simply opium), is
considered to be the prototypical opioid.

Indication : Morphine can be used as an analgesic in hospital settings to relieve:

o pain in myocardial infarction


o pain in sickle cell crisis
o pain associated with surgical conditions, pre- and postoperatively
54
o pain associated with trauma
o severe chronic pain, eg., cancer
o pain from kidney stones (renal colic, ureterolithiasis)
o severe back pain

Pethidine or Meperidine Pethidine is indicated for the treatment of moderate to severe


pain, and is delivered as its hydrochloride salt in tablets, as a syrup, or by
intramuscular or intravenous injection

ANTIMIGRAINE DRUGS
Ergotamine Tartarate Tablet 1mg/tab
Tramadol Hydrochloride* Capsule* 50 mg /cap*

Ergotamine It possesses structural similarity to several neurotransmitters, and


has biological activity as a vasoconstrictor. It is used medicinally for
treatment of acute migraine attacks (sometimes in combination with caffeine),
and to induce childbirth and prevent post-partum haemorrhage.

Ergotamine is a precursor of LSD and produces vasoconstriction peripherally as


well as damages the peripheral epithelium. In high doses ergotamine is
conducive to vascular stasis, thrombosis and gangrene. It can increase uterine
contractivity and occasionally is used therapeutically immediately post-partum to
decrease uterine bleeding. Ergotamine continues to be prescribed for migraines.
Contraindications include: atherosclerosis, Buerger's syndrome, coronary artery
disease, hepatic disease, pregnancy, pruritus, Raynaud's syndrome, and renal
disease.

Tramadol is a centrally acting analgesic, used for treating moderate to severe


pain

Tramadol is used to treat moderate to moderately severe pain and most types of
neuralgia, including trigeminal neuralgia MOA it is believed to work through
modulation of the noradrenergic and serotonergic systems in addition to its mild
agonism of the μ-opioid receptor. The contribution of non-opioid activity is

demonstrated by the fact that the analgesic effect of tramadol is not fully
antagonised by the μ-opioid receptor antagonist naloxone.

 04.07 – ANTIEPILEPTICS

Carbamazipne Tablet 200mg/tab


Lamotrigine Tablet 25mg/tab
Lamotrigine Tablet 100mg/tab
Phenobarbital Tablet 30mg/tab
55
Phenobarbital Tablet 100mg/tab
Phenobarbital Injection 40mg/amp
Phenytoin Sodium Tablet or Capsule 100mg/tablet or cap

Sodium Valproate Tablet 200mg/tab


Sodium Valproate Tablet 500mg/tab
Slow release
Gabapentin Capsule 300mg/cap
Topiramate * Tablet* 25mg/tab*

Carbamazepine (CBZ) is an anticonvulsant and mood


stabilizing drug used primarily in the treatment of epilepsy and
bipolar disorder, as well as trigeminal neuralgia. Common
adverse effects include drowsiness, headaches and migraines
MOA : Voltage-gated sodium channels are the molecular pores
that allow brain cells (neurons) to generate action potentials, the
electrical events that allow neurons to communicate over long
distances. After the sodium channels open to start the action
potential, they inactivate, essentially closing the channel.
Carbamazepine stabilizes the inactivated state of sodium
channels, meaning that fewer of these channels are available to
open, making brain cells less excitable
PHK: it induces the expression of the hepatic microsomal
enzyme system CYP3A4, which metabolizes carbamazepine
itself

topiramate exerts its anticonvulsant and migraine prophylaxis


effects are unknown;

Vigabatrin is an antiepileptic drug that inhibits the catabolism of gamma-


aminobutyric acid (GABA) by irreversibly inhibiting GABA transaminase.
It is an analog of GABA, but it is not a receptor agonist

vigabatrin is approved for use as an adjunctive treatment (with other


drugs) in treatment resistant epilepsy, complex partial seizures,
secondary generalized seizures, and for monotherapy use in infantile
spasms in West syndrome. Pharmacokinetics:
Vigabatrin is rapidly absorbed following oral administration and peak plasma
concentrations are reached within 2 hours. Vigabatrin is widely distributed
with an apparent volume of distribution slightly greater than total body water.
The primary route of elimination is via the kidney, with little metabolic
transformation occurring. Following a single dose, approximately 70% is
excreted in the urine as unchanged drug within the first 24 hours post-dose.
The plasma elimination half-life is approximately 5 to 8 hours in young adults
and 12 to 13 hours in the elderly. In renal impairment the elimination is
prolonged and the rate of renal clearance is directly related to creatinine
clearance (see Precautions and Dosage). Vigabatrin does not induce the
hepatic cytochrome P450 system nor is it extensively metabolized or plasma-
protein bound. Administration of vigabatrin with food slightly reduces the
rate, but not the extent of absorption.

56
Precautions

Patients with a History of Psychosis:


Behavioral disturbances such as aggression and psychotic episodes
have been reported following initiation of vigabatrin therapy. A history
of abnormal behavior or psychosis appears to be a predisposing
factor for such reactions, therefore treatment in such patients should
be initiated cautiously at low doses and with frequent monitoring.

Geriatrics and Patients with Renal Impairment:


Vigabatrin is eliminated via the kidney and caution should be
exercised when administering the drug to elderly patients and to
patients with renal impairment (see Dosage).

Patients with Myoclonic Seizures:


As with other antiepileptic drugs, some patients may experience an
increase in seizure frequency with vigabatrin. Patients with myoclonic
seizures may be particularly liable to this effect.

Discontinuation of Therapy:
As with other antiepileptic drugs, abrupt discontinuation may lead to
rebound seizures. If a patient is to be withdrawn from vigabatrin
treatment, it is recommended that this be done gradually by reducing
the dose over a 2 to 4 week period if possible.

Drug Interactions:
A gradual reduction of about 20% in plasma phenytoin concentration
has been observed following add-on therapy with vigabatrin. The
mechanism

04.08 – DRUGS USED IN PARKISONISM &RELATED


DISORDERS

DOPAMINERGIC DRUGS
Carbidopa + Levodopa Tablet 10mg + sinemet
100mg/tab

The combination of carbidopa and levodopa is used to treat Parkinson's disease

SINEMET is indicated for the treatment of Parkinson's disease and


syndrome. It is useful in relieving many of the symptoms of parkinsonism,
57
particularly rigidity and bradykinesia. SINEMET frequently is helpful in the
management of tremor, dysphagia, sialorrhoea, and postural instability
associated with Parkinson's disease and syndrome. The optimum daily dosage
of SINEMET must be determined by careful titration in each patient. SINEMET
tablets are available in a 1:4 ratio of carbidopa to levodopa (SINEMET 25/100)
as well as a 1:10 ratio (SINEMET 25/250). Tablets of the two ratios may be
given separately or combined as needed to provide the optimum dosage.

Each tablet of SINEMET is designed to divide in half with minimal pressure.

05. DRUGS USED IN THE TREATMENT OF


INFECTIONS
β-lactam antibiotics work by inhibiting the formation of
peptidoglycan cross-links in the bacterial cell wall. The β-lactam
moiety (functional group) of penicillin binds to the enzyme (DD-
transpeptidase) that links the peptidoglycan molecules in bacteria,
which weakens the cell wall of the bacterium (in other words, the
antibiotic causes cytolysis or death due to osmotic pressure). In
addition, the build-up of peptidoglycan precursors triggers the
activation of bacterial cell wall hydrolases and autolysins, which
further digest the bacteria's existing peptidoglycan. The term
“penicillin” is often used in the generic sense to refer to one of the
narrow-spectrum penicillins, in particular, benzylpenicillin
(penicillin G).

Other types include:

 Penicillin V
 Procaine benzylpenicillin
 Benzathine benzylpenicillin

Adverse effects

Common adverse drug reactions (≥1% of patients) associated


with use of the penicillins include diarrhea, hypersensitivity,
nausea, rash, neurotoxicity urticaria, and/or superinfection
(including candidiasis). Infrequent adverse effects (0.1–1% of
patients) include fever, vomiting, erythema, dermatitis,
angioedema, seizures (especially in epileptics), and/or
pseudomembranous colitis.

Cephalosporins are indicated for the prophylaxis and treatment of


infections caused by bacteria susceptible to this particular form of
antibiotic. First-generation cephalosporins are predominantly active
against Gram-positive bacteria, and successive generations have
58
increased activity against Gram-negative bacteria (albeit often with
reduced activity against Gram-positive organisms).

Adverse effects

Common adverse drug reactions (ADRs) (≥1% of patients)


associated with the cephalosporin therapy include: diarrhea, nausea,
rash, electrolyte disturbances, and/or pain and inflammation at
injection site. Infrequent ADRs (0.1–1% of patients) include: vomiting,
headache, dizziness, oral and vaginal candidiasis,
pseudomembranous colitis, superinfection, eosinophilia, and/or fever.

Cefalexin (cephalexin; Keflex)

Cefazolin (cephazolin; Ancef, Kefzol)

Cefradine (cephradine; Velosef)

Second generation

The second-generation cephalosporins have a greater Gram-


negative spectrum while retaining some activity against Gram-
positive cocci. They are also more resistant to beta-lactamase.

Cefaclor (Ceclor, Distaclor, Keflor, Raniclor)

Cefuroxime (Zinnat, Zinacef)

Cefoxitin (mofixine)

Third generation

Third-generation cephalosporins have a broad spectrum of activity


and further increased activity against Gram-negative organisms.
Some members of this group (in particular, those available in an oral
formulation, and those with anti-pseudomonal activity) have
decreased activity against Gram-positive organisms. They may be
particularly useful in treating hospital-acquired infections, although
increasing levels of extended-spectrum beta-lactamases are
reducing the clinical utility of this class of antibiotics. They are also
able to penetrate the CNS, making them useful against meningitis
caused by pneumococci, meningococci, H. influenzae, and
susceptible E. coli, Klebsiella, and penicillin-resistant N.
gonorrhoeae.

Cefotaxime (Claforan)

Ceftriaxone (Rocephin)

Third-generation cephalosporins with antipseudomonal activity

Ceftriaxone (rosiphine)

59
Ceftazidime (Fortum, Fortaz)

Fourth generation

Fourth-generation cephalosporins are extended-spectrum agents


with similar activity against Gram-positive organisms as first-
generation cephalosporins. They also have a greater resistance to
beta-lactamases than the third-generation cephalosporins. Many can
cross the blood-brain barrier and are effective in meningitis. They are
also used against Pseudomonas aeruginosa.

Cefepime (Maxipime)

06. ENDOCRINE DRUGS

06.01 – DRUGS USED IN DIABETES

INSULIN
Human Soluble Insulin(Regular) Injection 1000U /10ml/vial
Human Isophane Insulin ( NPH) Injection 1000U /10ml/vial
Insulin Glargine Injection 1000U /10ml/vial
Biphasic Isophane Human Insulin Inj. (30S+70 Is.) 1000U /10ml/vial
Insulin Lispro(r DNA Origin ) or Vial 100 I.U /vial
Insulin Aspart

Insulin human injection 100 IU/mL.

HUMULIN R (Regular)
(also called soluble insulin injection) is a sterile, clear colourless aqueous solution of human
insulin (rbe) adjusted to a pH range of 7.0 to 7.8. HUMULIN R is a short-acting insulin preparation.

HUMULIN NPH
(also called isophane insulin injection) is a sterile suspension of a white, crystalline precipitate of
isophane human insulin (rbe) in an isotonic phosphate buffer adjusted to a pH range of 6.9 to 7.5.
HUMULIN N is an intermediate-acting insulin preparation.

HUMULIN 30/70
(also called biphasic isophane insulin injection) is a mixture of human insulin (70% isophane
human insulin (rbe), 30% soluble human insulin (rbe)) adjusted to a pH range of 6.9 to 7.5.
HUMULIN Mixture 70/30 is an intermediate acting insulin preparation.

60
ORAL HYPOGLYCEMIC AGENTS
Glibenclamide Tablet 5mg/tab
Gliclazide Tablet 80mg/tab
Glipizide Tablet 5mg/tab
Metformin Hcl Tablet 500mg/tab

Metformin hydrochloride is a biguanide oral hypoglycaemic agent. Its mode of action is thought to
be multifactoral and includes delayed uptake of glucose from the intestinal tract, increased
peripheral glucose utilisation mediated by increased insulin sensitivity and inhibition of increased
hepatic and renal gluconeogenesis.

The administration of metformin HCl results in improved glucose assimilation and reduced levels
of plasma cholesterol, triglycerides and prebetalipoproteins. Weight may also be reduced.

Pharmacokinetics

The degree of absorption of metformin HCl after oral administration is only about 50-60%, and it is
thought that the percentage absorbed from the gastrointestinal tract may decrease as the dose
increases. Absorption may be affected by food.

The peak concentration after a 500mg dose of metformin HCl has been measured as
approximately 1µg/mL between 2-2.5h. After a 850mg dose it is approximately 1.8µg/mL at about
3 hours. Metformin HCl is not significantly bound to plasma protein and is excreted almost
unchanged in the urine. Reports indicate that elimination may be biphasic.

Indications

Metformin hydrochloride is a biguanide hypoglycaemic agent and is used in diet-failed, non-


insulin-dependent diabetes mellitus, especially if overweight. It may be used alone as initial
therapy or, in sulphonylurea failures either alone or in combination with a sulphonylurea.

Metformin may also be used as adjuvant therapy in insulin-dependent diabetic patients who are
usually obese and not well controlled by insulin.

Dose: Adults: Metformin HCl tablets should be taken in divided doses with meals. Initially either
500mg three times a day or 850mg twice daily.

DRUGS FOR HYPOGLYCEMIA


Glucagon Injection 1mg/vial

Glucagon is a hyperglycaemic agent that mobilises hepatic glycogen which is released into the
blood as glucose. Glucagon will not be effective in patients whose liver glycogen is depleted. For
that reason, glucagon has little or no effect when the patient is fasting, or is suffering from adrenal
insufficiency, chronic hypoglycaemia or alcohol-induced hypoglycaemia.

61
Indications

Treatment of severe hypoglycaemic reactions, which may occur in the management of insulin
treated persons with diabetes.

Contraindications

Hypersensitivity to glucagon or any of the excipients. GlucaGen is contraindicated in


phaeocromocytoma.

Interactions

Insulin reacts antagonistically towards glucagon.


Indomethacin: Glucagon may lose its ability to raise blood glucose or paradioxically may even
produce hypoglycaemia
Warfarin: Glucagon may increase the anticoagulant effect of warfarin.
Interactions between

 06.02 – THYROID & ANTITHYROID DRUGS

THYROID HORMONES
Thyroxine Sodium Tablet 50microgram/tab
Thyroxine Sodium Tablet 100microgram/tab
Thyroxine Sodium* Tablet* 25microgram/tab*

Levothyroxine (T4) is a naturally occurring hormone produced by the thyroid gland and converted
to the more active hormone triiodothyronine (T3) in peripheral tissues. The precise signals
controlling the conversion of T4 to T3 within the cell are not known. The thyroid hormones are
required for normal growth and development, particularly of the nervous system. They increase
the resting or basal metabolic rate of the whole organism and have stimulatory effects on the
heart, skeletal muscle, liver and kidney. Thyroid hormones enhance lipolysis and the utilization of
carbohydrate.

100 microgram levothyroxine is equivalent in activity to 20 to 30 microgram liothyronine/


triiodothyronine or 60 mg Thyroid BP and/or local pharmacopoeia specification.

Pharmacokinetic Properties

Absorption and Distribution

Following oral administration the absorption of levothyroxine is incomplete and variable especially
when taken with food. The amount absorbed increases during fasting conditions.

Levothyroxine is nearly totally bound to serum protein.

62
Metabolism and Elimination

The main pathway for the metabolism of levothyroxine (T4) is its conversion, by deiodination, to
the active metabolite triiodothyronine (T3). Further deiodination of T4 and T3 leads to production
of inactive products.

Levothyroxine is eliminated slowly from the body with a half-life of approximately 7 days in a
normal person. This may be reduced in hyperthyroid states or increased in hypothyroid patients.

Renal or hepatic diseases do not appear to have any significant effect on the disposition of
levothyroxine.

In man approximately 20-40% of levothyroxine is eliminated in the faeces and approximately 30-
55% of a dose of levothyroxine is excreted in the urine.

Indications

Levothyroxine is indicated for the treatment of hypothyroidism.

This product should only be prescribed for use in new patients, or those who cannot tolerate other
thyroxine products.

ANTITHYROID DRUGS
Carbimazole Tablet 5mg/tab
Propylthiouracil Tablet 50mg/tab

Therapeutic Indications

Primary thyrotoxicosis, even in pregnancy.

Secondary thyrotoxicosis - toxic nodular goitre.

However, carbimazole really has three principal applications in the therapy of hyperthyroidism:

i. Definitive therapy - induction of a permanent remission.

ii. Preparation for thyroidectomy.


iii. Before and after radio-active iodine treatment.

 06.03 – CORTICOSTEROIDS

Fludrocortisone Acetate Tablet 100microgram/tab


Prednisolone Tablet 5mg/tab
Prednisolone Tablet 25mg/tab
Dexamethasone Tablet 500microgram/tab
Dexamethasone Injection 5mg/amp
Hydrocortisone Tablet 10mg/tab
63
Hydrocortisone Injection 100mg/vial
Methylpredinsolone Injection 40mg/amp or vial
Methylpredinsolone Injection 500mg/amp or vial

fludrocortisone acetate The physiological action is similar to that of hydrocortisone. However,


the effects of fludrocortisone acetate, particularly on electrolyte balance, but also on
carbohydrate metabolism, are considerably heightened and prolonged. In small oral doses, it
produces marked sodium retention and increased urinary potassium excretion. It also causes a
rise in blood pressure, apparently because of these effects on electrolyte levels.

In larger doses, fludrocortisone acetate inhibits endogenous adrenal cortical secretion, thymic
activity, and pituitary corticotropin excretion; promotes the deposition of liver glycogen; and,
unless protein intake is adequate, induced negative nitrogen balance. The approximate half-life of
fludrocortisone is 18-36 hours. It is highly protein bound and is eliminated by the kidneys, mostly
as inactive metabolites. Duration of action is 1 to 2 days.

Indications

Partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's
disease and for the treatment of salt losing adrenogenital syndrome.

Dosage and Administration

Addison's Disease

The combination of Florinef with a glucocorticoid such as hydrocortisone or cortisone provides


substitution therapy approximating normal adrenal activity with minimal risks of unwanted effects.
The usual dose is 0.1mg or Florinef daily, although dosage ranging from 0.1mg three times a
week to 0.2mg daily has been employed. In the event transient hypertension develops as a
consequence of therapy, the dose should be reduced to 0.05mg daily. Florinef is preferably
administered in conjunction with cortisone (10 to 37.5mg daily in divided doses) or hydrocortisone
(10 to 30mg daily in divided doses).

Methylprednisolone action is a potent anti-inflammatory steroid. It has greater anti-inflammatory


potency than prednisolone even less tendency than prednisolone to induce sodium and water
retention. The relative potency of methylprednisolone to hydrocortisone is at least four to one.

Pharmacokinetics

The mean elimination half-life ranges from 2.4 to 3.5 hours in normal, healthy adults and appears
to be independent of the route of administration.

The mean oral time of peak concentration was 1.1 - 2.2 hours.

Methylprednisolone is widely distributed throughout the body and is described by a two-


compartment model. The mean volume of distribution reported in 34 adult volunteers ranged from
41 to 61.5 L.

MEDROL readily crosses the blood-brain barrier into the central nervous system with peak CSF
levels being 5 - 6% of the corresponding plasma levels. Methylprednisolone peak CSF levels

64
occurred within five minutes to one hour after IV administration of a 500mg dose to patients with
lupus cerebritis.

Methylprednisolone crosses the placental barrier. Although there is no data regarding


methylprednisolone passage into breast milk of humans, it is present in breast milk of animals.

Methylprednisolone is metabolized in the liver to inactive metabolites, the major ones being 20B-
hydroxymethyl-prednisolone and 20B-hydroxy-6a-methylprednisone.

Methylprednisolone clearance is altered by concurrent administration of troleandomycin,


erythromycin, rifampin, anticonvulsants, and theophylline. No dosing adjustments are necessary in
renal failure. Methylprednisolone is hemodializable.

Following IV administration of radiolabelled 6-methylprednisolone to six cancer patients, 75% of


total reactivity was recovered in the urine after 96 hours and 9% in the faeces after five days.
Twenty percent of the total dose was excreted in the bile, but the time course was not cited.

Indications

MEDROL (methylprednisolone) is indicated in the following conditions:

Endocrine Disorders:

Primary or secondary adrenocortical insufficiency (hydrocortisone or cortisone is the first choice;


synthetic analogs may be used in conjunction with mineralocorticoids where applicable; in infancy
mineralocorticoid supplementation is of particular importance).

 Congenital adrenal hyperplasia


 Nonsuppurative thyroiditis
 Hypercalcemia associated with cancer

Non-Endocrine Disorders:

a. Rheumatic Disorders: As adjunctive therapy for short-term administration (to tide the
patient over an acute episode or exacerbation) in:

 psoriatic arthritis
 rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may
require low-dose maintenance therapy)
 ankylosing spondylitis
 acute and subacute bursitis
 acute nonspecific tenosynovitis
 acute gouty arthritis
 post-traumatic osteoarthritis
 synovitis of osteoarthritis
 epicondylitis
b. Collagen Diseases: During an exacerbation or as maintenance therapy in selected cases
of:
 systemic lupus erythematosus

65
Actions

Dexamethasone is a synthetic corticosteroid exhibiting both anti-inflammatory and immuno-


suppressant properties. The anti-inflammatory potency of dexamethasone has been estimated as
25x that of hydrocortisone. It has little mineralocorticoid activity.

Pharmacokinetics

Dexamethasone is readily absorbed after oral administration achieving peak plasma


concentrations after one hour. Binding to plasma proteins is less than for most other
corticosteroids.

The biological half-life is approximately 190 minutes. Dexamethasone penetrates tissue and
cerebrospinal fluid.

Elimination occurs via metabolism and renal excretion.

Indications

Dexamethasone is indicated for replacement therapy in secondary adrenal insufficiency arising


from insufficient corticotrophin secretion. It is not indicated for primary adrenal insufficiency states,
such as Addisons disease or after adrenalectomy. In such cases hydrocortisone and
fludrocortisone in combination is more appropriate.

Dexamethasone is also indicated for allergic disorders such as bronchial asthma and allergic skin
reactions, blood disorders such as leukaemia, thrombocytopoenia and haemolytic anaemias

 06.04 – SEX HORMONES

 06.05 – HYPOTHALAMIC,PITUIT. HORM.&ANTIESTEROGENS

POSTERIOR PITUITARY HORMONES


Injection 20U/amp
Vasopressin
Spray* 10microgm/metered*
Desmopressin Acetate* Nasal spray
spray 5-6ml Unit

(desmopressin acetate) is a synthetic analogue of the natural pituitary hormone 8-


arginine vasopressin (ADH), an antidiuretic hormone affecting renal water conservation.
Indication :
is indicated as antidiuretic replacement therapy in the management of central cranial
diabetes insipidus and for management of the temporary polyuria and polydipsia following
head trauma or surgery in the pituitary region. It is ineffective for the treatment of
nephrogenic diabetes insipidus.

HORMONE ANTAGONISTS

Octreotide Injection 100microgm/amp

66
Octreotide is a synthetic octapeptide analogue of naturally occurring somatostatin with similar
pharmacological effects, but with a considerably prolonged duration of action. It inhibits the
secretion of serotonin and the gastro-entero-pancreatic peptides: gastrin, vasoactive intestinal
peptide, insulin, glucagon, secretin, motilin, and pancreatic polypeptide, and of growth hormone
(GH). Octreotide, like somatostatin, decreases splanchnic blood flow.

In animals, octreotide is a more potent inhibitor of growth hormone, glucagon and insulin release
than somatostatin with greater selectivity for GH- and glucagon-suppression.

In healthy subjects octreotide, like somatostatin, has been shown to inhibit:

 Release of growth hormone (GH) stimulated by arginine, exercise and insulin-induced


hypoglycaemia
 Postprandial release of insulin, glucagon, gastrin, other peptides of the GEP system, and
arginine-stimulated release of insulin and glucagon
 Thyrotropin releasing hormone (TRH) stimulated release of thyroid stimulating hormone
(TSH).

Unlike somatostatin, octreotide inhibits GH secretion preferentially over insulin and its
administration is not followed by rebound hypersecretion of hormones .

Indications

 For symptomatic control and reduction of growth hormone and IGF-1 plasma levels in
patients with acromegaly, including those who are inadequately controlled by surgery,
radiotherapy or dopamine agonist treatment. Octreotide treatment is also indicated in
acromegalic patients unfit or unwilling to undergo surgery, or in the interim period until
radiotherapy becomes fully effective.
 For the relief of symptoms associated with the following functional tumours of the gastro-
entero-pancreatic endocrine system:
 Carcinoid tumours with features of the carcinoid syndrome
 Vasoactive intestinal peptide secreting tumours (VIPomas).
 Octreotide is not an antitumour therapy and is not curative in these patients.
 For reduction of the incidence of complications following pancreatic surgery

09. DRUGS AFFECTING NUTRITION AND BLOOD

 09.01 – ANEMIAS & SOME OTHER BLOOD DISORDERS

IRON
Ferrous Sulphate Capsule or
Tablet 35-65 mg/tab /cap
Ferrous Sulphate 50ml/bottle
Solution 25-30 mg/1ml

Iron Dextran or Iron Succharate Injection 100mg/amp

67
Ferrous sulfate is a type of iron. You normally get iron from the foods you eat. In your body, iron
becomes a part of your hemoglobin and myoglobin. Hemoglobin carries oxygen through your
blood to tissues and organs. Myoglobin helps your muscle cells store oxygen.

Ferrous Sulfate is an essential body mineral. Ferrous sulfate is used to treat iron deficiency
anemia (a lack of red blood cells caused by having too little iron in the body). Overdose symptoms
may include nausea, severe stomach pain, bloody diarrhea, coughing up blood or vomit that looks
like coffee grounds, shallow breathing, weak and rapid pulse, pale skin, blue lips, and seizure
(convulsions).

Take ferrous sulfate on an empty stomach, at least 1 hour before or 2 hours after a meal. Avoid
taking antacids or antibiotics within 2 hours before or after taking ferrous sulfate.

DRUGS USED IN MEGALOBLASTIC ANEMIA


Cyanocoblamine( vitamin Injection
B12) 1mg/amp
Folic Acid Tablet
1mg/tab
Folic Acid Tablet
1mg/tab

Actions of vit B12

Several chemically related forms of vitamin B12, differing in slight modification of a side chain
attached to the cobalamin nucleus have been isolated. Two such variants of vitamin B 12 are
cyanocobalamin and hydroxocobalamin.

Vitamin B12 is essential for normal growth, haematopoiesis, and production of all epithelial cells
and maintenance of myelin throughout the nervous system. Whenever nucleic acid synthesis
occurs and therefore whenever cell reproduction occurs, vitamin B 12 is required.

The amounts of vitamin B12 needed to maintain normal blood forming functions are small and low
doses are sufficient to correct the usual symptoms of vitamin B 12 deficiency. Pharmacokinetics

Hydroxocobalamin produces higher and more prolonged serum levels of vitamin B 12 than
cyanocobalamin when given by intramuscular injection in the same dosage. Hydroxocobalamin
disperses more slowly from the site of injection than cyanocobalamin, is more strongly bound to
plasma proteins and accumulated in the liver to a greater extent.

Hydroxocobalamin is excreted in the bile and urine, but more slowly than cyanocobalamin.

Hydroxocobalamin combines with cyanide and thus acts as a cyanide antagonist in vivo resulting
in the formation of cyanocobalamin.

68
Actions Folic acid

is a member of the vitamin B group and is the substrate for the production of tetrahydrofolate by
enzymatic reduction in vivo. Tetrahydrofolate is a coenzyme for various metabolic pathways
including purine and pyrimidine nucleotide synthesis, and ultimately DNA synthesis.
Pharmacokinetics

Orally administered folic acid is rapidly absorbed mainly from the wall of the proximal small
intestine as the 5-methyltetrahydrofolate metabolite. This metabolite is extensively bound to
plasma proteins in the portal circulation. Folic acid is rapidly absorbed from normal diets and is
widely distributed in body tissues with the liver as the principal storage site. Folate is also
distributed in breast milk.

DRUGS USED IN RENAL ANEMIA


Erythropoietin (Epoetin) Injection
1000 U
Erythropoietin (Epoetin)* Injection*
2000 U
Erythropoietin (Epoetin) Injection
4000 U

Erythropoietin

MOA : is a glycoprotein hormone that controls erythropoiesis, or red blood cell


production.
it is produced by the peritubular capillary endothelial cells in the kidney, and is the
hormone that regulates red blood cell production.
EPO is also involved in the wound healing process.

USES: This medication is used to treat anemia (low red blood cell
count) in people with long-term serious kidney disease (chronic renal
failure), people receiving zidovudine to treat HIV, and people
receiving chemotherapy for certain types of cancer (non-myeloid
cancers). It may also be used in anemic patients to reduce the need
for blood transfusions before certain planned surgeries that have a
high risk of blood loss (usually combined with the "blood thinner"
warfarin). Epoetin alfa helps to reverse anemia and improves your
energy and activity level. It works by signaling the bone marrow to
make more red blood cells. This medication is very similar to the
natural substance in your body (erythropoietin) that prevents anemia.

HOW TO USE: Read the Medication Guide and Patient Information


Leaflet provided by your pharmacist before you start using this
medication and each time you get a refill. Learn all preparation and
usage instructions in the product package. If you have any questions,
ask your doctor or pharmacist.This medication is given as an
injection under the skin or into a vein, usually 1 to 3 times a week or
as directed by your doctor. Hemodialysis patients should receive this
medication by injection into a vein.Do not shake this medication.
Before using, check this product visually for particles or discoloration.
If either is present, do not use the liquid. If you are injecting this
medication under the skin, change the location of the injection site

69
every time to avoid problem areas under the skin.Learn how to store
and discard needles and medical supplies safely

SIDE EFFECTS: Headache, body aches, diarrhea, and irritation at


the injection site may occur. If any of these effects persist or worsen,
tell your doctor or pharmacist promptly.Remember that your doctor
has prescribed this medication because he or she has judged that
the benefit to you is greater than the risk of side effects. Many people
using this medication do not have serious side effects.Epoetin alfa
may sometimes cause or worsen high blood pressure, especially in
patients with long-term kidney failure. This effect may be caused by
the number of red blood cells increasing too quickly, usually within
the first 3 months of starting treatment. If you have high blood
pressure, it should be adequately controlled before beginning
treatment with this medication.

STORAGE: Store the medication in the refrigerator between 36-46


degrees F (2-8 degrees C). Do not freeze. Let the medication come
to room temperature before using. For

 09.02 – FLUIDS & ELECTROLYTES

ORAL ELECTROLYTES & POTASSIUM REMOVAL


Potassium Chloride Efferves. Tablet
600mg/tab
Sachet
Oral Rehydration Salt(ORS) Nacl 3.5+Kcl 1.5+NaCitrate
2.9g+Anhydrous Glucose
20g/sachet
Sodium Bicarbonate Tablet
300-650 mg/tab

Potassium Chloride

Potassium is a mineral that is found in many foods and is needed for several functions of your
body, especially the beating of your heart.

Potassium chloride is used to prevent or to treat low blood levels of potassium (hypokalemia).
Potassium levels can be low as a result of a disease or from taking certain medicines, or after a
prolonged illness with diarrhea or vomiting. You should not use potassium chloride if you have
kidney failure, Addison's disease, Do not crush, chew, break, or suck on an extended-release
tablet or capsule. Swallow the pill whole. Breaking or crushing the pill may cause too much of the
drug to be released at one time. Sucking on a potassium tablet can irritate your mouth or throat.
Take potassium chloride with food or just after a meal. severe burns or other tissue injury, if you
are dehydrated, if you take certain diuretics.
these serious side effects:
 confusion, anxiety, feeling like you might pass out;
 uneven heartbeat;
 extreme thirst, increased urination;
70
 leg discomfort;
 muscle weakness or limp feeling;
 numbness or tingly feeling in your hands or feet, or around your mouth;
 severe stomach pain, ongoing diarrhea or vomiting;
 black, bloody, or tarry stools; or
 coughing up blood or vomit that looks like coffee grounds.

Less serious side effects may include:

 mild nausea or upset stomach;


 mild or occasional diarrhea;
 slight tingling in your hands or feet

ORS Oral Rehydration Salts (ORS) available in a sachet to make a liter of solution. a very
suitable and effective simple solution for rehydrating a child can be made by using salt, sugar and
water.

1. Put the contents of the ORS packet in a clean container. Check the packet for
directions and add the correct amount of clean water. Too little water could make the
diarrhoea worse.
2. Add water only. Do not add ORS to milk, soup, fruit juice or soft drinks. Do not add
sugar.
3. Stir well, and feed it to the child from a clean cup. Do not use a bottle.

INTRAVENOUS SOLUTIONS & ELECTROLYTES


Sodium Chloride 3 % Solution Injection
10 ml/ amp
Dextrose 50% Solution Injection
50ml/bottle
Potassium Chloride Injection
20mmol/20ml vial
Sodium Bicarbonate 5% Injection
250ml/glass bottle
Sodium Bicarbonate 8.4% Injection
50ml/vial
Sterile Water Injection
5ml/amp

PLASMA & PLASMA SUBSTITUTES


Human Albumen Solution Injection
(Hepatitis,HIV&Other infectious 20-25%

71
disease agent ) 50ml/glass bottle
Plasma Protein Solution Injection
(Hepatitis,HIV&Other infectious 4-5%Protien
disease agent ) 250ml/glass bottle 85%Albumin

Albumen

refers generally to any protein that is water soluble, which is moderately soluble in concentrated
salt solutions, and experiences heat denaturation. They are commonly found in blood plasma, and
are unique to other plasma proteins in that they are not glycosylated. Substances containing
albumin, such as egg white, are called albuminoids.A number of serum transport proteins are
known to be evolutionarily related, including serum albumin, alpha-fetoprotein, vitamin D-binding
protein and afamin . Albumin is the main protein of plasma; it binds water, cations (such as Ca 2+,
Na+ and K+), fatty acids, hormones, bilirubin and drugs - its main function is to regulate the
colloidal osmotic pressure of blood. Alpha-fetoprotein (alpha-fetoglobulin) is a fetal plasma protein
that binds various cations, fatty acids and bilirubin. Vitamin D-binding protein binds to vitamin D
and its metabolites, as well as to fatty acids.

It is considered appropriate to use Albumin in the following conditions:

1. Volume expansion for:


a. Shock (other than blood loss) when systolic blood pressure is less than 90
mm Hg; central venous pressure or pulmonary capillary wedge pressure are
low or when excessive volumes of crystalloids are required to maintain blood
pressure. Should be used in conjunction with crystalloids.
b. Shock due to blood loss after a crystalloid solution when estimated blood
loss is less than 10 - 15% of total volume.
c. Acute edematous states when the serum albumin is less than 3 g/dL.
d. After the removal or loss of 1.5 L or more of ascitic fluid. Second line
agent after crystalloids after removal of 4 liters or more of ascitic fluid
e. After hepatic resection (>40%) depending on function of residual liver -
after crystalloid use.
f. Thermal Injury in conjunction with crystalloids if all of the following are
true:
 Burns cover greater than 50% of BSA
 Treatment is 24 hours after occurrence of burn
 Crystalloid therapy has failed to correct hypovolumenia
g. Nutritional Intervention in patients with diarrhea associated with enteral
feeding if ALL of the following conditions are met:
 Diarrhea greater than 2 liters a day
 Serum albumin is less than 2.0 g/dL.
 Failure of short-chain peptide and elemental formulas
 Other causes of diarrhea have been considered and ruled out
(documented)
2. In Surgery:

 As a priming fluid in pump oxygenators during cardiopulmonary bypass


surgery to maintain the patient’s hematocrit at 20% and the serum albumin
concentration at 2.5 g/dL. In cases in which it is extremely important to avoid

72
pulmonary interstitial fluid accumulation, nonprotein colloids in addition to
crystalloids may be used. For post op volume expansion, albumin is third
choice after crystalloids and nonprotein colloids.
2. Should not be used as a source of protein.
3. Hyperbilirubinemia of the Newborn - may be used as an adjuvant to exchange
transfusions and only with concurrent transfusion of blood ( Albumin only)
4. Nephrotic Syndrome - short term albumin use, in conjunction with diuretic
therapy, for acute, severe peripheral or pulmonary edema.
5. Organ transplantation - In postoperative liver transplant patients in the control
of ascites and peripheral edema if ALL of the following conditions are met: 
 Serum albumin is less than 2.5 g/dl
 Pulmonary capillary wedge pressure is less than 12 mm Hg.
 Hematocrit is greater than 30%
6. Plasmapheresis - In large-volume plasma exchange of greater than 20 ml/kg in
one session or greater than 20 ml/kg/week in repeated sessions.

Blood plasma is the yellow liquid component of blood in which the blood cells in whole blood are normally
suspended. It makes up about 55% of the total blood volume. It is the intravascular fluid part of
extracellular fluid (all body fluid outside of cells). It is mostly water (93% by volume) and contains
dissolved proteins, glucose, clotting factors, mineral ions, hormones and carbon dioxide

 09.04 – MINERALS

Calcium Gluconate 10% Injection


10ml/amp
Magnesium Sulphate 50% Injection
2ml/amp

Calcium Gluconate is the calcium salt of gluconic acid, an oxidation product of glucose,
and contains 9.3% calcium, which is about one-third of the calcium in strength of calcium
chloride USP.
Indication
Calcium gluconate is used to treat conditions arising from calcium deficiencies such as hypocalcemic
tetany, hypocalcemia related to hypoparathyrodism and hypocalcemia due to rapid growth or pregnancy. It
is also used in the treatment of black widow spider bites to relieve muscle cramping and as an adjunct in
the treatment of rickets, osteomalacia, lead colic and magnesium sulfate overdosage. Calcium gluconate
has also been employed to decrease capillary permeability in allergic conditions
Dosege
Calcium Gluconate should be administered intravenously either directly or by infusion. The dose is
dependent upon the individual requirements of the patient. Calcium Gluconate may also be administered by
intermittent infusion at a rate not exceeding 200 mg/min, or by continuous infusion.
Usual Dosage Adults: 500 mg - 2 grams (5-20 mL)

Children: 200-500 mg (2-5 mL) Infants: not more than 200 mg (not more than 2 mL)

Side effect : Patients may complain of tingling sensations, a sense of oppression or heat waves
and a calcium or chalky taste following the intravenous administration of calcium gluconate.

Rapid intravenous injection of calcium salts may cause vasodilation, decreased blood pressure, bradycardia, cardiac
arrhythmias, syncope and cardiac arrest. Use in digitalized patients may precipitate arrhythmias. Local necrosis and
abscess formation may occur with intramuscular injection. Calcium salts are contraindicated in patients with

73
ventricular fibrillation or hypercalcemia. Intravenous administration of calcium is contraindicated when serum calcium
levels are above normal.

Magnesium sulfate is indicated in the following conditions:

Convulsions (treatment) - Intravenous magnesium sulfate is indicated for immediate control of life-threatening
convulsions in the treatment of severe toxemias (pre-eclampsia and eclampsia) of pregnancy and in the treatment of
acute nephritis in children.

Hypomagnesemia (prophylaxis and treatment) - Magnesium sulfate is indicated for replacement therapy in
magnesium deficiency, especially in acute hypomagnesemia accompanied by signs of tetany similar to those of
hypocalcemia.

Magnesium sulfate is also used to prevent or treat magnesium deficiency in patients receiving total parenteral
nutrition.

Tetany, uterine (treatment) - Magnesium sulfate is indicated in uterine tetany as a myometrial relaxant.

DOSAGE AND ADMINISTRATION Intramuscular: Adults and older children: For severe hypomagnesemia, 1 to 5 g
(2 to 10 mLof 50% solution) daily in divided doses; administration is repeated daily until serum levels have returned to
normal. If deficiency is not severe, 1 g (2 mL of 50% solution) can be given once or twice daily. Serum magnesium
levels should serve as a guide to continued dosage.

Intravenous: 1 to 4 g magnesium sulfate may be given intravenously in 10% to 20% solution, but only with great
caution; the rate should not exceed 1.5 mL of 10% solution or equivalent per minute until relaxation is obtained.

Intravenous Infusion: 4 g in 250 mL of 5% Dextrose Injection at a rate not exceeding 3 mL per minute.

Usual Dose Range: 1 to 40 g daily.

Electrolyte Replenisher: Intramuscular 1 to 2 g in 50% solution four times a day until serum magnesium is within
normal limits.

Usual Pediatric Dose: Intramuscular 20 to 40 mg per kg of body weight in a 20% solution repeated as necessary.

For Eclampsia: Initially 1 to 2 g in 25% or 50% solution is given intramuscularly. Subsequently, 1 g is given every 30
minutes until relief is obtained. The blood pressure should be monitored after each injection.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration,
whenever solution and container permit.

SIDE EFFECTS

Flushing, sweating, sharply lowered blood pressure, hypothermia, stupor and ultimately, respiratory depression.

74
09.05 – VITAMINS

Retinol Injection
(VitaminA) 100,000 U/amp
Pyridoxine Hcl Tablet
(Vitamin B6) 40-50mg/tab
Cholecalciferol (Vitamin Solution
D3)or Ergocalciferol 2,000-5,000 U/ml
(Vitamin D2) 10-30ml
bottle
Alfacalcidol (1-alfa- Solution
Hydroxyvitamin D3) 20ml 2microgm/ml
bottle
Calcitriol Capsule
1,25-Dihydroxyvitamin D3 0.25microgm/cap
or Alfacalcidol
(1-alfa- Hydroxyvitamin D3)

Calcitriol Capsule
1,25Dihydroxyvitamin D3 or 0.5microgm or
Alfacalcidol
(1-alfa- Hydroxyvitamin D3) 1microgm/cap
Phytomenadione Tablet
(Vitamin K1) 10mg/tab
Phytomenadione Injection
(Vitamin K1) 1mg/0.5mlamp
Phytomenadione Injection
(Vitamin K1) 10mg/amp
Multivitamins Tablet or Capsule
or Syrup

Retin-A Micro (tretinoin gel) microsphere, 0.1% and 0.04%, is indicated for topical application in the treatment of acne
vulgaris. The safety and efficacy of the use of this product in the treatment of other disorders have not been
established. Retin-A Micro (tretinoin gel) microsphere, 0.1% and 0.04%, should be applied once a day, in the evening,
to the skin where acne lesions appear, using enough to cover the entire affected area lightly. Application of excessive
amounts of gel may result in “caking” of the gel, and will not provide incremental efficacy.

A transitory feeling of warmth or slight stinging may be noted on application. In cases where it has been necessary to
temporarily discontinue therapy or to reduce the frequency of application, therapy may be resumed or the frequency
of application increased as the patient becomes able to tolerate the treatment. Frequency of application should be
closely monitored by careful observation of the clinical therapeutic response and skin tolerance. Efficacy has not been
established for less than once daily dosing frequencies.

During the early weeks of therapy, an apparent exacerbation of inflammatory lesions may occur. If tolerated, this
should not be considered a reason to discontinue therapy.

Therapeutic results may be noticed after two weeks, but more than seven weeks of therapy are required before
consistent beneficial effects are observed.
75
Patients treated with Retin-A Micro (tretinoin gel) microsphere, 0.1% and 0.04%, may use cosmetics, but the areas to
be treated should be cleansed thoroughly before the medication is applied.

Side effect : Irritation Potential over the twelve week period showed that cutaneous irritation scores for erythema,
peeling, dryness, burning/stinging, or itching peaked during the initial two weeks of therapy, decreasing thereafter.

Precaution

General

 The skin of certain individuals may become excessively dry, red, swollen, or blistered. If the degree of
irritation warrants, patients should be directed to temporarily reduce the amount or frequency of application of
the medication, discontinue use temporarily, or discontinue use all together. Efficacy at reduced frequencies
of application had not been established. If a reaction suggesting sensitivity occurs, use of the medication
should be discontinued. Excessive skin dryness may also be experienced; if so, use of an appropriate
emollient during the day may be helpful.
 Unprotected exposure to sunlight, including sunlamps, should be minimized during the use of Retin-A Micro
(tretinoin gel) microsphere, 0.1% and 0.04%, and patients with sunburn should be advised not to use the
product until fully recovered because of heightened susceptibility to sunlight as a result of the use of tretinoin.
Patients who may be required to have considerable sun exposure due to occupation and those with inherent
sensitivity to the sun should exercise particular caution. Use of sunscreen products (SPF 15) and protective
clothing over treated areas are recommended when exposure cannot be avoided.

Phytonadione is a vitamin, which is a clear, yellow to amber, viscous, odorless or nearly odorless liquid. It is
insoluble in water Vitamin K1 Injection (Phytonadione Injectable Emulsion, USP) is a yellow, sterile, nonpyrogenic
aqueous dispersion available for injection by the intravenous, intramuscular and subcutaneous routes. Each milliliter
contains phytonadione 2 or 10 mg, polyoxyethylated fatty acid derivative 70 mg, dextrose, hydrous 37.5 mg in water
for injection; benzyl alcohol 9 mg added as preservative

Vitamin K1 Injection is indicated in:

 anticoagulant-induced prothrombin deficiency caused by coumarin or indanedione derivatives;


 prophylaxis and therapy of hemorrhagic disease of the newborn;
 hypoprothrombinemia due to antibacterial therapy;
 hypoprothrombinemia secondary to factors limiting absorption or synthesis of vitamin K, e.g., obstructive
jaundice, biliary fistula, sprue, ulcerative colitis, celiac disease, intestinal resection, cystic fibrosis of the
pancreas, and regional enteritis;
 other drug-induced hypoprothrombinemia where it is definitely shown that the result is due to interference with
vitamin K metabolism, e.g., salicylates.

Directions for Dilution

 Vitamin K1 Injection may be diluted with 0.9% Sodium Chloride Injection, 5% Dextrose Injection, or 5%
Dextrose and Sodium Chloride Injection. Benzyl alcohol as a preservative has been associated with toxicity in
newborns. Therefore, all of the above diluents should be preservative-free

76
 Prophylaxis of Hemorrhagic Disease of the Newborn
 Treatment of Hemorrhagic Disease of the Newborn
 Anticoagulant-Induced Prothrombin Deficiency in Adults

 To correct excessively prolonged prothrombin time caused by oral anticoagulant therapy—2.5 to 10 mg or up


to 25 mg initially is recommended. In rare instances 50 mg may be required. Frequency and amount of
subsequent doses should be determined by prothrombin time response or clinical condition

SIDE EFFECTS

 Transient "flushing sensations" and "peculiar" sensations of taste have been observed, as well as rare
instances of dizziness, rapid and weak pulse, profuse sweating, brief hypotension, dyspnea, and cyanosis.

 Pain, swelling, and tenderness at the injection site may occur.

 The possibility of allergic sensitivity including an anaphylactoid reaction, should be kept in mind.

 Infrequently, usually after repeated injection, erythematous, indurated, pruritic plaques have occurred; rarely,
these have progressed to scleroderma-like lesions that have persisted for long periods. In other cases, these
lesions have resembled erythema perstans.

 Hyperbilirubinemia has been observed in the newborn following administration of phytonadione. This has
occurred rarely and primarily with doses above those recommended

10. MUSCULOSKELETAL&JOINT DISEASES

 10.01 – DRUGS USED IN RHEUMATIC DISEASES & GOUT

NONSTERODIAL ANTIINFLAMMATORY DRUGS


Ibuprofen Tablet
400mg/tab
Diclofenac Sodium Tablet
50mg/tab
Diclofenac Sodium Injection
75mg/amp
Indomethacin Capsule
25mg/cap
Indomethacin Suppository
100mg/supp

77
tablets contain the active ingredient ibuprofen, which is (±) - 2 - (p - isobutylphenyl) propionic acid.
Ibuprofen is a white powder

a nonsteroidal anti-inflammatory drug (NSAID), is available in 400 mg tablets for oral administration. Use the lowest
effective dose for the shortest duration consistent with individual patient treatment goals are indicated for relief of the
signs and symptoms of rheumatoid arthritis and osteoarthritis. tablets are indicated for relief of mild to moderate pain.
tablets are also indicated for the treatment of primary dysmenorrhea . Do not exceed 3200 mg total daily dose. If
gastrointestinal complaints occur, administer the tablets with meals or milk. Suggested Dosage: 1200 mg-3200 mg
daily (300 mg qid; 400 mg, 600 mg or 800 mg tid or qid). Individual patients may show a better response to 3200 mg
daily, as compared with 2400 mg The most frequent type of

adverse reaction occurring with MOTRIN tablets is gastrointestinal. (Nausea†, epigastric pain†, heartburn†, diarrhea,
abdominal distress, nausea and vomiting, indigestion, constipation, abdominal cramps or Pain, fullness of GI tract (bloating and flatulence)

(Diclofenac sodium) Enteric-Coated Tablets of 75 mg


is indicated:

 For relief of the signs and symptoms of osteoarthritis


 For relief of the signs and symptoms of rheumatoid arthritis
 For acute or long-term use in the relief of signs and symptoms of ankylosing spondylitis
 For the relief of osteoarthritis, the recommended dosage is 100-150 mg/day in divided doses (50 mg b.i.d. or
t.i.d., or 75 mg b.i.d.).

 For the relief of rheumatoid arthritis, the recommended dosage is 150-200 mg/day in divided doses (50 mg
t.i.d. or q.i.d., or 75 mg b.i.d.).

 For the relief of ankylosing spondylitis, the recommended dosage is 100-125 mg/day, administered as 25 mg
q.i.d., with an extra 25-mg dose at bedtime if necessary.

Side effects are:

 Gastrointestinal experiences including: abdominal pain, constipation, diarrhea, dyspepsia, flatulence, gross
bleeding/perforation, heartburn, nausea, GI ulcers (gastric/duodenal) and vomiting.

 Abnormal renal function, anemia, dizziness, edema, elevated liver enzymes, headaches, increased bleeding
time, pruritus, rashes and tinnitus.

 Additional adverse experiences reported occasionally include:

 Body as a Whole: fever, infection, sepsis

 Cardiovascular System: congestive heart failure, hypertension, tachycardia, syncope

 Digestive System: dry mouth, esophagitis, gastric/peptic ulcers, gastritis, gastrointestinal bleeding, glossitis,
hematemesis, hepatitis, jaundice

78
 Hemic and Lymphatic System: ecchymosis, eosinophilia, leukopenia, melena, purpura, rectal bleeding,
stomatitis, thrombocytopenia

 Metabolic and Nutritional: weight changes

 Nervous System: anxiety, asthenia, confusion, depression, dream abnormalities, drowsiness, insomnia,
malaise, nervousness, paresthesia, somnolence, tremors, vertigo

 Respiratory System: asthma, dyspnea

 Skin and Appendages: alopecia, photosensitivity, sweating increased

 Special Senses: blurred vision

 Urogenital System: cystitis, dysuria, hematuria, interstitial nephritis, oliguria/polyuria, proteinuria, renal
failure

(Indomethacin) Capsules, Suppositories, is supplied in three dosage forms. Capsules INDOCIN for oral
administration contain either 25 mg or 50 mg of indomethacin ,Indomethacin has been found effective in active stages
of the following:

SIDE FFECTS nausea** with or without vomiting dyspepsia** (including indigestion, heartburn and
epigastric pain) diarrhea abdominal distress or pain constipation, headache vertigo somnolence
depression and fatigue

DRUGS FOR GOUT


Colchicine Tablet
500microgram /tab

Allopurinol Tablet
100mg/tab
Allopurinol Tablet
300mg/tab
Hydroxychloroquine Tablet
Sulphate 200mg/tab
Colchicine

Gout Flares

COLCRYS™ (colchicine, USP) tablets are indicated for treatment of acute gout flares when taken at the first sign of a
flare.

Familial Mediterranean fever (FMF)

79
COLCRYS™(colchicine, USP) tablets are indicated in adults and children 4 years or older for treatment of familial
Mediterranean fever (FMF).

ALLOPURINOL:

Each scored white tablet contains 100 mg allopurinol and the inactive ingredients lactose, magnesium stearate, potato
starch, and povidone. Each scored peach tablet contains 300 mg allopurinol and the inactive ingredients corn starch,

is indicated in:

1. the management of patients with signs and symptoms of primary or secondary gout (acute attacks, tophi, joint
destruction, uric acid lithiasis, and/or nephropathy).
2. the management of patients with leukemia, lymphoma and malignancies who are receiving cancer therapy
which causes elevations of serum and urinary uric acid levels. Treatment with ZYLOPRIM should be discontinued
when the potential for overproduction of uric acid is no longer present.
3. the management of patients with recurrent calcium oxalate calculi whose daily uric acid excretion exceeds
800 mg/day in male patients and 750 mg/day in female patients. Therapy in such patients should be carefully
assessed initially and reassessed periodically to determine in each case that treatment is beneficial and that the
benefits outweigh the risks.

The average is 200 to 300 mg/day for patients with mild gout and 400 to 600 mg/day for those with moderately severe
tophaceous gout. The appropriate dosage may be administered in divided doses or as a single equivalent dose with
the 300 mg-tablet. Dosage requirements in excess of 300 mg should be administered in divided doses. The minimal
effective dosage is 100 to 200 mg daily and the maximal recommended dosage is 800 mg daily.

SIDE EFFECT : Ecchymosis, fever, headache.Cardiovascular: Necrotizing angiitis, vasculitis. Gastrointestinal:


Hepatic necrosis, granulomatous hepatitis, hepatomegaly, hyperbilirubinemia, cholestatic jaundice, vomiting,
intermittent abdominal pain, gastritis, dyspepsia. Hemic and Lymphatic: Thrombocytopenia, eosinophilia,
leukocytosis, leukopenia. Musculoskeletal: Myopathy, arthralgias. Nervous: Peripheral neuropathy, neuritis,
paresthesia, somnolence.

80
10.02 DRUGS USED IN NEUROMUSCULAR DISORDERS

ANTICHOLINESTERASE
Neostigmine Methysulphate Injection
500microgram/amp
Pyridostigmine Bromide Injection

Neostigmine Methylsulfate, an anticholinesterase agent

Neostigmine Methylsulfate Injection, USP is indicated for:

- the symptomatic control of myasthenia gravis when oral therapy is impractical.


- the prevention and treatment of postoperative distention and urinary retention after mechanical obstruction has been excluded.
- reversal of effects of non-depolarizing neuromuscular blocking agents (e.g., tubocurarine, metocurine, gallamine or
pancuronium) after surgery. Symptomatic control of myasthenia gravis: One mL of the 1:2000 solution (0.5 mg)
subcutaneously or intramuscularly. Subsequent doses should be based on the individual patient's response.In most
patients, however, oral treatment with Neostigmine Bromide tablets, 15 mg each, is adequate for control of symptoms.

Prevention of postoperative distention and urinary retention: 0.25 mg subcutaneously or intramuscularly as soon
as possible after operation;repeat every 4 to 6 hours for two or three days.

Treatment of postoperative distention: One mL of the 1:2000 solution (0.5 mg) subcutaneously or intramuscularly,
as required.

Treatment of urinary retention: One mL of the 1:2000 solution (0.5 mg) subcutaneously or intramuscularly. If
urination does not occur within an hour, the patient should be catheterized.After the patient has voided, or the bladder
has been emptied, continue the 0.5 mg injections every three hours for at least 5 injections.

Reversal of Effects of Non-depolarizing Blocking Agents: When Neostigmine Methylsulfate Injection, USP is
administered intravenously, it is recommended that Atropine Sulfate (0.6 to 1.2 mg) also be given intravenously using
separate syringes.Some authorities have recommended that the Atropine be injected several minutes before the
Neostigmine rather than concomitantly. The usual dose is 0.5 to 2 mg Neostigmine Methylsulfate Injection, USP given
by slow intravenous injection, repeated as required.Only in exceptional cases should the total dose of Neostigmine
Methylsulfate exceed 5 mg.It is recommended that the patient be well ventilated and a patent airway maintained until
complete recovery of normal respiration is assured.The optimum time for administration of the drug is during
hyperventilation when the carbon dioxide level of the blood is low. It should never be administered in the presence of
high concentrations of halothane or cyclopropane.In cardiac cases and severely ill patients, it is advisable to titrate the
exact dose of Neostigmine Methylsulfate required, using a peripheral nerve stimulator device.In the presence of
bradycardia, the pulse rate should be increased to about 80/minute with Atropine before administering Neostigmine.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration,
whenever solution and container permit. Side effects are generally due to an exaggeration of pharmacological effects
of which salivation and fasciculation are the most common.Bowel cramps and diarrhea may also occur.

81
The following additional adverse reactions have been reported following the use of either Neostigmine Bromide or
Neostigmine Methylsulfate.

Allergic: Allergic reactions and anaphylaxis.

Neurologic: Dizziness, convulsions, loss of consciousness, drowsiness, headache, dysarthria, miosis and visual
changes.

Cardiovascular: Cardiac arrhythmias (including bradycardia, tachycardia, A-V block and nodal rhythm) and
nonspecific EKG changes have been reported, as well as cardiac arrest, syncope and hypotension.These have been
predominantly noted following the use of the injectable form of Neostigmine Methylsulfate. Respiratory: Increased
oral, pharyngeal and bronchial secretions, dyspnea, respiratory depression, respiratory arrest and bronchospasm.
Dermatologic: Rash and urticaria. Gastrointestinal: Nausea, emesis, flatulence and increased peristalsis.
Genitourinary: Urinary frequency. Musculoskeletal: Muscle cramps and spasms, arthralgia. Miscellaneous:
Diaphoresis, flushing and weakness.

SKELETAL MUSCLE RELAXANT


Baclofen Tablet
10mg/tab

Baclofen is a muscle relaxant and antispastic, available as 10 mg and 20 mg tablets for oral administration.
Baclofen is useful for the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly
for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity.

Patients should have reversible spasticity so that baclofen treatment will aid in restoring residual function.

Baclofen may also be of some value in patients with spinal cord injuries and other spinal cord diseases.

Baclofen is not indicated in the treatment of skeletal muscle spasm resulting from rheumatic disorders.

The efficacy of baclofen in stroke, cerebral palsy, and Parkinson’s disease has not been established and, therefore, it
is not recommended for these conditions

Neuropsychiatric: Confusion (1-11%), headache (4-8%), insomnia (2-7%); and, rarely, euphoria, excitement,
depression, hallucinations, paresthesia, muscle pain, tinnitus, slurred speech, coordination disorder, tremor, rigidity,
dystonia, ataxia, blurred vision, nystagmus, strabismus, miosis, mydriasis, diplopia, dysarthria, epileptic seizure.

Cardiovascular: Hypotension (0-9%). Rare instances of dyspnea, palpitation, chest pain, syncope.

Gastrointestinal: Nausea (4-12%), constipation (2-6%); and, rarely, dry mouth, anorexia, taste disorder, abdominal
pain, vomiting, diarrhea, and positive test for occult blood in stool.

Genitourinary: Urinary frequency (2-6%); and, rarely, enuresis, urinary retention, dysuria, impotence, inability to
ejaculate, nocturia, hematuria.
82
Other: Instances of rash, pruritus, ankle edema, excessive perspiration, weight gain, nasal congestion.

Some of the CNS and genitourinary symptoms may be related to the underlying disease rather than to drug therapy.
The following laboratory tests have been found to be abnormal in a few patients receiving baclofen: increased SGOT,
elevated alkaline phosphatase, and elevation of blood sugar.

 10.03 – DRUGS FOR THE RELIEF OF SOFT TISSUE INFLAMM.

Hyaluronidase Injection
1500U/amp

INDECATION

Subcutaneous Fluid Administration

HYLENEX recombinant is indicated as an adjuvant in subcutaneous fluid administration for


achieving hydration.

Dispersion and Absorption of Injected Drugs

HYLENEX recombinant is indicated as an adjuvant to increase the dispersion and absorption of


other injected drugs.

Subcutaneous Urography

HYLENEX recombinant is indicated as an adjunct in subcutaneous urography for improving


resorption of radiopaque agents.

HYLENEX recombinant may be added to small volumes of solution, such as fluid replacement
solutions or solutions of drugs for subcutaneous injection. Subcutaneous fluids should be
administered as directed by a physician. The dosage of subcutaneous fluids administered is
dependent upon the age, weight, and clinical condition of the patient as well as laboratory
determinations. The rate and volume of subcutaneous fluid administration should not exceed
those employed for intravenous infusion. For premature infants or during the neonatal period, the
daily dosage should not exceed 25 mL/kg of body weight, and the rate of administration should
not be greater than 2 mL per minute.
11. DRUGS ACTING ON THE EYE

 11.01 – ANTIINFECTIVE EYE PREPARATIONS

ANTIBACTERIALS
Bacitracin eye ointment Tube
500U/g 3-5g/tube

83
Chloramphenicol eye drops Bottle
0.5 % 5-15ml/bottle
Chloramphenicol eye ointment Tube
0.1 % 3-5g/tube
Chloramphenicol eye drops Bottle
0.5 % single use
Erythromycin eye ointment Tube
0.5 % 3-
5g/tube
Gentamicin eye or ear drops Bottle
0.3 % 5-
10ml/bottle
Gentamicin eye ointment Tube
0.3 % 3-
5g/tube
Gentamicin eye drops Bottle
0.3 % single
use
Polmyxin B Sulphate Bottle
+ Neomycin Sulphate 10,000U +
3.5mg/ml
5ml/bottle
Tetracycline Hcl eye Tube
ointment 1 % 3-5g/tube
Ofloxacin* Bottle*
0.3 %
5ml/bottle*
Fusidic acid 1%eye Bottle*
drops 1%
5g/bottle*
Natamycin 5 % eye Bottle
drops 15ml/bottle
Acyclovir eye Tube
ointment 3 % 4.5g/tube
‫أ‬

 11.02 – ANTIINFLAMMATORY PREPARATIONS

CORTICOSTEROIDS
Dexamethasone Bottle
0.1 % 5-
10ml/bottle
Betamethasone Sodium Tube
Phosphate 0.1% or 0.1 % OR
Dexamethasone 0.05 % 0.05 %

3-5g/tube

84
Fluorometholone eye Bottle
drops 0.1 %
5ml/bottle

OTHER ANTIINFLAMMATORY PREPARATIONS


SodiumCromoglycate Bottle
eye drops 2%
10ml/bottle
SodiumCromoglycate Tube
eye drops 4 % 5g/tube
Diclofenac Sodium Bottle*
eye drops* 0.1 %
5ml/bottle*

 11.03 – MYDRIATICS & CYCLOPLEGICS

ANTIMUSCARINICS
Atropine Sulphate eye Bottle
drops 0.5 %
5ml/bottle
Atropine Sulphate eye Tube
ointment 1 % 3-5g/tube
Tropicamide eye Bottle
drops 1%5
-15ml/bottle
Naphazoline Hcl or Bottle
Oxymetazoline Hcl 1 % or
eye drops
0.025%
15ml/bottle
Phenylephrine Hcl eye Bottle
drops 2.5 %
15ml/bottle
Phenylephrine Hcl eye Bottle
drops 10 % 5-
10ml/bottle

 11.04 – TREATMENT OF GLAUCOMA

Bottle
Pilocarpine eye drops 2% 10ml/bottle
Betaxolol Hcl or Bottle
Carteolol Hcl eye 0.5% or
drops
1%5ml/bottle
Timolol Maleate Bottle
eye drops 0.5%
5ml/bottle

85
Bottle**
Latanoprost eye 50microgm
drops** 2.5ml/bottle**
Acetazolamide Tablet /
Capsule 250mg/cap or
tab
Acetazolamide Injection
500mg/vial

 11.05 – LOCAL ANESTHETICS

Lidocaine Hcl &


Fluorescein Sodium eye Bottle 4% &
drops 0.25%

single use

 11.06 – MISCELLANEOUS OPTHALMIC PREPARATIONS

PREPARATION FOR TEAR DEFICIENCY


Artificial eye – tear Bottle
drops 10-
15ml/bottle

12. EAR , NOSE &OROPHARYNEX DRUGS

 12.01 – DRUGS ACTING ON THE EAR

ANTIINFECTIVE PREPARATION

Chloramphenicol Bottle
ear drops 0.5 % 10-15ml/bottle
Clotrimazole OR
Econazole drops Bottle 1 %10-20ml/bottle
Gentamycin Bottle
Sulfate 0.3 % &
Betamethasone
86
0.1% OR
Gentamycin 5-10ml/bottle
Sulfate 0.3%
&Hydrocortisone
1% ear drops
Polymyxin B Bottle
Sulfate, Neomycin 10,000U/ml,3,400U/ml&1%
Sulphate OR 10,000U/l&0.5
&Hydrocortisone 10ml/bottle
OR Polymyxin B
Sulfate,
Hydrocortisone
ear drops

 12.02 – DREUGS ACTING ON THE NOSE

DRUGS USED IN NASAL ALLERGY


Beclomethasone Metered
Dipropionate OR Spray 50microgram/
Budesonide 200 metered spray
spray unit OR
Fluticasone
Propionate Nasal
Spray,120spray
unit
Sodium
Cromoglycate Bottle 2 % 20-
N.spray 30ml/bottle

TOPICAL NASAL DECONGESTANT


Naphazoline Hcl Bottle
&Chlorpheneramine
Maleate N. drops
500microgram/ml
Bottle
Xylometazoline Hcl 0.05%
N.drops 10ml/bottle

 12.03 – DRUGS ACTING ON THE OROPHARYNEX

MOUTHWASHES
Chlorhexidine Bottle
Gluconate M.W. 0.2% 150-
300l/bottle

 13.02 – TOPICAL CORTICOSTEROIDS

Hydrocortisone 1% Tube
skin cream 1 % 10-

87
15g/tube
Hydrocortisone 1% Tube
+Clioquinol 3% skin 15-30g/tube
cream
Betamethasone Tube
Valerate 0.1%OR 10-30g/tube
Betamethasone
Dipropionate 0.05%
skin oint.
Betamethasone Bottle
Valerate 0.1%OR 20-
Betamethasone 60ml/bottle
Dipropionate 0.05%
sclap lotion

 13.04 – PREPARATIONS FOR ACNE & HIRSUTISM

TOPICAL ANTIBIOTICS
Clindanycin1% OR Solution
Erthromycin 2% 30-
topical solution 50ml/bottle

TOPICAL RETINOIDS
Tretinoin 0.05% skin Tube
cream 20-50g/tube

ORAL RETINOIDS
Isotretinoin Capsule
5mg/cap

 13.06 – ANTIINFECTIVE SKIN PREPARATIONS

Silver Sulfadiazine Tube


1% skin cream 50g/tube
Silver Sulfadiazine Tube
1% skin cream 500g/jar
Fusidic Acid 2% skin Tube
oint 15g/tube

TOPICAL ANTIFUNGALS
Ketoconazole 2% OR Tube
Econazole 1% OR 15-30g/tube
Clotrimazole 1% skin
cream

88
Nystatin Tube
100,000U/gskin oint. 15-30g/tube

14. IMMUNOLOGIC PRODUCTS

 14.02 – IMMUNOGLOBULINS

Human normal immunoglobulin for intravenous


injection, containing primarily immunoglobulin
fraction (more than 90 % IgG and trace amounts of
IgA and IgM) which is sterile and free of hepatitis,
HIV and any other infectious disease agent , 2-5
g/vial

 14.03 – ANTIVENOMS

Scorbion antivenin (polyvalent antiscorbion


serum) for injection, containing a sterile purified
equine immunoglobulin capable of neutralizing the
venoms of all or most local scorbion species
( Androctonus crassicauda , Buthus rptochelys ,
Buthus yotuatensis nigroaca leatus , Composubuthus
arabicus , Leiurus quinquestiatus and Scorpio
maurus ) , 1ml/amp or vial
Snake antivenin (polyvalent antissnake serum) for
injection, containing a sterile purified equine
immunoglobulin capable of neutralizing the venoms
of all or most local snakes(Atractaspis microlepidota,
Bitis arietans,Cerasates cerasates , Echis
carinatus ,Echis coloratus,Naja haje Arabicus and
Walterinnesia aegyptia) , 10-20ml/amp or vial

89
15. DRUGS USED IN ANESTHESIA
 15.01 – GENERAL ANESTHESIA

INTRAVENOUS ANESTHETICS
Thiopental Sodium
Injection 500mg/vial

Ketamine Hcl
Injection 200mg/vial
Propofol
Injection 200mg/vial

INHALATIONAL ANESTHETICS
Isoflurane
Inhalation 100ml/bottle
Sevoflurane*
Inhalation 250ml/bottle*
*

ANTIMUSCARINIC PREMEDICATION DRUGS


Atropine
Sulphate Injection 600micrograms/amp

MUSCLE RELAXANTS
Atracurium
Besylate Injection 10mg/amp
Pancuronium
Bromide Injection 4mg/amp
Succinylcholine
Chloride Injection 100mg/amp or vial
Vecuronium
Bromide Injection 10mg/amp or vial

Thiopental Sodium

is a rapid-onset short-acting barbiturate general anaesthetic. Thiopental is a core medicine in the


World Health Organization's "Essential Drugs List", which is a list of minimum medical needs for a
basic healthcare system Thiopental is an ultra-short-acting barbiturate and has been used
commonly in the induction phase of general anesthesia. Its use in the United States and
elsewhere has been largely replaced with that of propofol. Following intravenous injection the drug
rapidly reaches the brain and causes unconsciousness within 30–45 seconds. At one minute, the
drug attains a peak concentration of about 60% of the total dose in the brain. Thereafter, the drug
distributes to the rest of the body and in about 5–10 minutes the concentration is low enough in
the brain such that consciousness returns.[citation needed]

90
A normal dose of thiopental (usually 4–6 mg/kg) given to a pregnant woman for operative delivery
(caesarian section) rapidly makes her unconscious, but the baby in her uterus remains conscious.
However, larger or repeated doses can depress the baby. [citation needed]

Thiopental is not used to maintain anesthesia in surgical procedures because, in infusion, it


displays zero-order elimination kinetics, leading to a long period before consciousness is
regained. Instead, anesthesia is usually maintained with an inhaled anesthetic (gas) agent.
Inhaled anesthetics are eliminated relatively quickly, so that stopping the inhaled anesthetic will
allow rapid return of consciousness. Thiopental would have to be given in large amounts to
maintain an anesthetic plane, and because of its 11.5–26 hour half-life, consciousness would take
a long time to return.[7]

In veterinary medicine, thiopental is used to induce anesthesia in animals. Since thiopental is


redistributed to fat, certain breeds of dogs – primarily the sight hounds – can have prolonged
recoveries from thiopental due to their lack of body fat and their lean body mass. Thiopental is
always administered intravenously, as it can be fairly irritating; severe tissue necrosis and
sloughing can occur if it is injected incorrectly into the tissue around a vein.

Ketamine

is a drug used in human and veterinary medicine. Its hydrochloride salt is sold as Ketanest,
Ketaset, and Ketalar. Pharmacologically, ketamine is classified as an NMDA receptor antagonist.
[2]
At high, fully anesthetic level doses, ketamine has also been found to bind to opioid μ receptors
and sigma receptors.[3][4] Like other drugs of this class such as tiletamine and phencyclidine (PCP),
it induces a state referred to as "dissociative anesthesia"[5] and is used as a recreational drug.
Indications for use as an anaesthetic:

 Pediatric anesthesia (as the sole anesthetic for minor procedures or as an induction agent followed by
muscle relaxant and endotracheal intubation)
 Asthmatics or patients with chronic obstructive airway disease
 As part of a cream, gel, or liquid for topical application for nerve pain—the most common mixture is
10% ketoprofen, 5% Lidocaine, and 10% ketamine. Other ingredients found useful by pain
specialists and their patients as well as the compounding pharmacists who make the topical mixtures
include amitriptyline, cyclobenzaprine, clonidine, tramadol, and mepivicaine and other longer-acting
local anaesthetics.
 In emergency medicine in entrapped patients suffering severe trauma[21]
 Emergency surgery in field conditions in war zones
 To supplement spinal / epidural anesthesia / analgesia utilizing low doses

In medical settings, ketamine is usually injected intravenously or intramuscularly. [22] Since it


suppresses breathing much less than most other available anaesthetics, [23] ketamine is still used in
human medicine as an anesthetic, however, due to the hallucinations which may be caused by
ketamine, it is not typically used as a primary anesthetic, although it is the anaesthetic of choice
when reliable ventilation equipment is not available. Ketamine tends to increase heart rate and
blood pressure. Because ketamine tends to increase or maintain cardiac output, it is sometimes
used in anesthesia for emergency surgery when the patient's fluid volume status is unknown (e.g.,
from traffic accidents). Ketamine can be used in podiatry and other minor surgery, and
occasionally for the treatment of migraine. There is ongoing research in France, the Netherlands,
Russia, Australia and the US into the drug's usefulness in pain therapy, depression suppression,
and for the treatment of alcoholism[24] and heroin addiction.[25]

Propofol

is used for induction of anesthesia, having largely replaced sodium thiopental for this indication.[1]
Propofol is also used to sedate individuals who are receiving mechanical ventilation. In critically ill
patients it has been found to be superior to lorazepam both in effectiveness as well as overall
91
cost; as result, the use of propofol for this indication is now encouraged whereas the use of
lorazepam for this indication is discouraged.

Propofol is also used for sedation, for example, prior to endoscopic procedures, and has been
found to have less prolonged sedation and a faster recovery time compared to midazolam.
Propofol is used for induction of anesthesia, having largely replaced sodium thiopental for this
indication.[1] Propofol is also used to sedate individuals who are receiving mechanical ventilation.
In critically ill patients it has been found to be superior to lorazepam both in effectiveness as well
as overall cost; as result, the use of propofol for this indication is now encouraged whereas the
use of lorazepam for this indication is discouraged. [3] Propofol is also used for sedation, for
example, prior to endoscopic procedures, and has been found to have less prolonged sedation
and a faster recovery time compared to midazolam.

Isoflurane

(2-chloro-2-(difluoromethoxy)-1,1,1-trifluoro-ethane) is a halogenated ether used for inhalational


anesthesia. Together with enflurane and halothane, it replaced the flammable ethers used in the
pioneer days of surgery. Its name comes from being a structural isomer of enflurane, hence they
have the same empirical formula. It is a racemic mixture of (R) and (S) optical isomers. Its use in
human medicine is now starting to decline, being replaced with sevoflurane, desflurane and the
intravenous anaesthetic propofol. Isoflurane is still frequently used for veterinary anaesthesia.

Isoflurane is always administered in conjunction with air and/or pure oxygen. Often nitrous oxide is
also used. Although its physical properties imply that anaesthesia can be induced more rapidly
than with halothane, its pungency can irritate the respiratory system, negating this theoretical
advantage conferred by its physical properties. It is usually used to maintain a state of general
anesthesia that has been induced with another drug, such as thiopentone or propofol. It vaporizes
readily, but is a liquid at room temperature. It is completely nonflammable.

Isoflurane reduces pain sensitivity (analgesia) and relaxes muscles. The mechanism by which
general anesthetics produce the anesthetic state is not clearly understood, but likely involves
interactions with multiple receptor sites to interfere with synaptic transmission. Isoflurane binds to
GABA receptors, glutamate receptors and glycine receptors, and also inhibits conduction in
activated potassium channels. Glycine inhibition helps to inhibit motor function, while bonding to
glutamate receptors mimics the effects of NMDA. It activates calcium ATPase through an increase
in membrane fluidity, and binds to the D subunit of ATP synthase and NADH dehydrogenase. In
addition, a number of general anesthetics attenuate gap junction communication, which could
contribute to anesthetic action.

ANTAGONISTS FOR CENTRAL & RESPIRATORY DEPRESSION

Flumazenil Injection
500microgram/amp
Naloxone Hcl Injection 40microgram/amp
Naloxone Hcl Injection 400microgram/amp

ANTAGONISTS FOR MALIGNANT HYPERTHERMIA

Dantrolene Injection 20mg/vial


Sodium
92
*

 15.02 – LOCAL ANETHESIA

Lidocaine Hcl 2 % Injection


20ml/vial
Lidocaine Hcl 5 Injection
%preservative free 2ml/amp
for Spinal
Anesthesia
Lidocaine Hcl 1 % Injection
with adrenaline 20ml/vial
1:200,000
Lidocaine Hcl 2 % Injection
with adrenaline 1.8ml/cartridge
1:80,000 for Dental
Anesthesia
Lidocaine Hcl 5 % Ointment 15g/tube
Lidocaine Hcl 2 % Sterile Gel 15g/tube
Lidocaine Hcl 10 Aerosol 50ml/container
% Spray
Bupivacaine Hcl Injection 20ml /vial or
0.25 % Injection* amp
Bupivacaine Hcl 10ml /vial or
0.25 % OR amp*
Ropivacaine Hcl
0.2% *

Bupivacaine Hcl Injection 20ml /vial or


0.5 % amp
Prilocaine Hcl 3% Injection
with Felypressin 1.8ml/cartridge
1:1850,000/ml for
Dental Anesthesia

93
17. ANTIDOTES

17.01 REMOVAL&ELIMINATION

PREVENTION OF ABSORPTION
Activated Charcoal 100g
powder/cont.

17.02 SPECIFIC DRUGS

Acetylcysteine 10 % 1g/vial or amp


Deferoxamine injection 500mg/vial
Digoxin immune Fab(Antidigoxin Fab 40mg/vial
Fragments)injection
Methylene blue injection 100microgram/amp
Physostigmine Salicylate injection 2mg/amp
Dimercaprol injection 100mg/amp
Pralidoxime Chloride OR Mesylate 1g/amp
injection

94
18. CHEMICALS
18.01 SEMISOLIDS

Paraffain. White soft 25kg/container

18.02 LIQUIDS

Castor Oil 1liter/bottle


Glycerol ( Glycerin) 5liters
/container
Hydrogen Peroxide 6% Solution (20vols) 500ml/bottle
Povidone-Iodine 7.5 % Surgical scub solution 240ml/container
Povidone-Iodine 10 % solution 240ml/container

ALBUMIN

Guidelines for Use

Amikacin

95
Guidelines for Use

 Indication for Use:

1. Culture and sensitivity proves isolated organism responsible for a clinical


infection which is resistant or only moderately sensitive to gentamicin or
tobramycin.

2. Empirical in presumed infections in patient either currently on or recently


on another aminoglycoside or with nosocomial infection in a hospital area with
high frequency of gentamicin resistance. If culture proves sensitive to
gentamicin or tobramycin, switching is recommended.

3. Combination therapy with ticarcillin in renally impaired patients.

 Dose:
          15 mg/kg/day in 2 or 3 doses. Not to exceed 1.5 grams/day for any
adult.
                    Modify in renal failure. Conform to MIC of organism.
 Monitor:
Serum creatnine obtained before therapy or within 24 hours of initiation of
therapy.
Serum creatnine obtained twice weekly during therapy. If 2mg/dl, then every
other day.
Blood levels — peak and trough — if patient treated for longer than 72 hours.
If dose adjusted — draw levels again in 48 hr. — repeat every 4-7.
 Adverse Reactions:

                    — decreased renal function, ototoxicity, hypersensitivity.

Alteplase, recombinant

Guidelines for Use

Use of Tissue Plasminogen Activator is considered appropriate under the


following conditions.

1. Patient diagnosis of acute myocardial infarction with prolonged (greater


than 30 minutes) chest pain and associated ST-segment elevations on their
ECG.

2. The chest pain and ECG changes are not relieved by three sublingual
nitroglycerin/nifedipine or a nitroglycerin drip.

3. Therapy must occur within 12 hours, preferably 6 hours, from clinical onset
or myocardial infarction.

4. Medical history reveals none of the following

a. Active, internal bleeding

96
b. History of any cerebrovascular event

c. Recent (two months) intracranial/intraspinal surgery or trauma.

d. Intracranial neoplasm, aneurysm or AV malformation

e. Known bleeding diathesis

f. Severe, uncontrolled arterial hypertension

g. Recent (within 10 days) severe trauma, traumatic CPR > 5 minutes or


traumatic intubation.

Extreme caution should be used in using Alteplase in the following situations:

a. Advanced age (over 75)

b. Pregnancy

c. Hypertension - 180/110 or either separately

d. Acute pericarditis or subacute bacterial endocarditis

e. Recent major surgery or trauma at a non-compressible site

f. Any conditions producing a prolonged prothrombin time

g. Any other conditions in which bleeding would constitute a significant risk or


management problem.

Dose:

Administered by intravenous infusion therapy for one dose only.

67 Kg or > - 100 mg over 90 minutes - administered as 15 mg IV bolus


followed by 50 mg over 30 minutes and 35 mg over the next 60 minutes.

< 67 Kg - 15 mg IV bolus followed by 0.75 mg/kg (not to exceed 50 mg) over


30 minutes and then 0.5 mg/kg (not to exceed 35 mg) over the next 60
minutes.

Anticoagulants (heparin, aspirin, dipyridamole) will be administered


concurrently or following therapy (within 24 hours) with Alteplase;

Monitor:

1. Excessive bleeding from any puncture sites

2. ECG - reperfusion arrhythmias

Outcome:

1. Patient responds favorably to therapy (relief of symptoms of MI)

97
2. Patient is monitored appropriately during therapy

3. Patient does not experience any major bleeding events.

98

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