Basic pharmacology of

anaesthesia-related drugs

Premedication Drugs
Premedication is defined as administration of
medication prior to anaesthesia.
Aims:
Anxiolysis
Analgesia
Antisialagogue (drying of airway secretions)
Anti-emetic
Acid aspiration prophylaxis

Midazolam
It is a short acting benzodiazepine.
It is the most common drug used for sedation
and anxiolysis preoperatively
Perioperative indications are
sedative,anxiolysis,amnesic,anticonvulsant
Preoperatively midazolam can be given via
intravenous or orally.

Midazolam

(continued)

Dose : Oral - 0.2mg/kg

IV - 0.1-0.2mg/kg
* should be given 20-40 min preop
Side Effect:
hypotension, respiratory depression,
apnoea
Caution:
reduce dose in elderly ( very sensitive )

Diazepam
It is a long acting benzodiazepine
Perioperative indication are sedation,
termination of status epilepticus
For preoperatively diazepam normally be
given orally
Dose: oral 0.1-0.2mg/kg
Side effect : Sedation, circulatory depression

Morphine
It is an opioid
It be given before op as an analgesia
Can be given via iv or sc
Dose: 0.15-0.2mg/kg. Total dose 10 mg.
Side effect of morphine are histamine
release, hypotension, bronchospasm, nausea,
vomiting, pruritus, dysphoria
Should be used with caution as it can cause
prolonged risk of respiratory depression.

Pethidine
It is an synthetic opioid
Used preoperatively as an analgesia (agent
of choice in asthma)
Can be used postoperatively for
postoperative shivering
Analgesic dose 1-1.5mg/kg IV/IM

Pethidine

(continued)

Side effect :
Respiratory depression, hypotension,
dysphoria
Should be used with caution because it can
cause seizure in high dosage - maximum
daily dose 1 g/day ( 20 mg/kg/day)
Contraindication in pt on MAOI

Atropine sulphate
Anticholinergic
Uses:
Preoperative: Antisialogogue, reduce incidence of
laryngospasm and reflex bradycardia arrythmia
during general anaesthesia
Postoperative: Counteract muscurinic effects of
anticholinergic agents used for reversal of
neuromuscular blocking agents.
Cardiac: Sinus bradycardia or asystole durig
cardiopulmonary resuscitation or drug toxicity.

Dosage:
Administered IV/IM at a dose of
0.015-0.02mg/kg
Antisialogogue:IV (0.3-0.6mg) 30 min before op .
Bradyarrythmias: adult IV/IM 0.5-1 mg max
2mg. Child IV/IM 0.01-0.03 mg/kg max 0.6 mg

Side effects:
Decrease secretions, decreases lower
oesophageal sphincter tone, relaxes bronchial
smooth muscle.
Confusion in elderly.
Obstructive uropathy
Contraindications/Precautions: angle closure
glaucoma, obstructive uropathy, obstructive
disease of GIT.Caution in IHD, MI and fever.

Glycopyrollate
It is an anticholinergic agent
Perioperative indication :
Blockade of muscarinic effects of
anticholinesterases,
Potent antisialogogue
Quaternary ammonium therefore
cannot cross blood brain barrier
Dose iv/im : 0.004-0.008mg/kg 30 min preop

Glycopyrollate (continued)
Side effect : Paradoxical bradycardia in small
doses.
Reduces lower oesophageal
sphincter tone.
Caution in glaucoma and cardiovascular
disease.

Promethazine
It is a phenothiazine group
It has an antihistamine with sedative and
antiemetic propertie
Commonly used as pediatric sedation
Dose 0.25-0.5mg/kg oral
Side effect extrapyramidal reactions

Metoclopromide
A procainamide derivative.
It is a prokinetic drugs .
Act at the dopaminergc receptor.
Increases gastric emptying and lower
oesophageal sphinter tone .
Dopaminergic anti-emetic
Prescribes for premedication drug in patient
at risk of acid aspiration.
e.g: pregnancy, gastric outlet obstruction,
obese,etc

Metoclopromide (continued)
Dose : Oral/IM/IV 5-20mg
Side effect: sedation,extrapyramidal/dystonic
reactions.
Caution with concomitant usage with
neuroleptic and anticholinergic, patient with
abnormal renal or liver function, elderly ..

Ranitidine
Gastric PH increasing drugs
Histamine (H2) receptor antagonist
Reduction in gastric acid secretion.
Use as premedication drug in patient at risk
of acid aspiration

Ranitidine

(continued)

Dose :- Adult : Oral - 150mg ON & morning

IV - 50-100mg 1H preop
Child : Oral - 2 mg/kg/dose 12 hourly
or 4 mg/kg at night
IV - 1mg/kg/dose slowly 6-8
hourly
Side effect : Generally infrequent. Headache,
malaise, dizziness, thrombocytopenia (clinically
insignificant )
No known contraindication . Caution in renal and
hepatic dysfunction

Omeprazole
Proton pump inhibitor.
Gastric PH increasing.
Significantly reduces volume of gastric acid
secretion but no effect on gastric emptying.
Clinical usage: Treatment of peptic ulcer disease,
peptic esophangitis , zollinger Ellison and can also
be use in patient at risk of gastric acid aspiration.

Dosage:
Oral:40mg ON & 2-3h preop
IV :40mg over 30 min
Side effect : In general well tolerated . Headache
and diarrhoea, myalgia, rash and abdominal pain.

Na Citrate 0.3M
Gastric PH increasing drugs.
Uses: Given as premedication drug for patient at
risk of gastric acid aspiration in particular
pregnancy
Dose : Oral 10-30mls <30 min preop

Reversal Drugs
Includes reversal of :
Muscle relaxation
Drug action ( antagonist )

Neostigmine
Anticholinesterase
reversal of non-depolarizing muscle relaxant
treatment of myasthenia gravis
Dose:
Reversal of muscle relaxant IV 0.04-0.05mg/kg in
combination with anticholinergic agent

Adverse/Side effects:
Muscarinic effects: nausea, vomiting, epigastric
discomfort, abdominal cramps, increase salivation
and bronchial secretions, bradycardia, miosis,
hypotension.
Nicotinic effects: Fasciculations, twitching,
generalised weakness, respiratory depression,
paralysis.
Overdosage: CNS stimulation, agitation , fear,
death

Naloxone
Opioid antagonist. Pure mu-receptor antagonist
Uses:
1. Reversal respiratory depression due to opiods.
2.the diagnosis of opioid overdose.
Dosage:
Reversal of opioid: adult IV 1.5mcg/kg IV 0.1 mg
increments at 2-3 minutes intervals to the
desired effect. Child IV 0.005-0.1 mg/kg repeated
every 2-3 min up to 3 doses if necessary

Adverse/ side effects:

Abrupt reversal of analgesia may produce a
catecholamine surge resulting in tachycardia,
hypertension, pulmonary oedema and cardiac
dysrhythmias
Remarks:
Beware of renarcotization if reversing long-acting
opioid.
Caution in opiod addicts-may precipitate acute
withdrawal.

Flumazenil
Benzodiazepine antagonist
Uses: reversal of centrally sedative effects of
benzodiazepines.
Dose: IV 0.2 mg increments up to 1-2 mg
Contraindicated in patient known allergy. Mixed
intoxications with benzodiazepine and cyclic
antidepressants since toxic effect of the latter
may emerge with the reversal of the
benzodiazepine effect.

Caution in severe head injury or epileptic patient.

Side effects:
Arrythmias,seizures
Remarks:
Special precaution in benzodiazepine dependence
because can cause acute withdrawal.
Beware of resedation if long-acting
benzodiazepine

Miscellaneous:
Other drugs that are commonly used in
anaesthesia .

Vasopressor & inotropes

Electrolyte replacement
Antiarrythmias
Antihypertension

Ephedrine
Direct and indirect sympathomimetic ( and
adrenergic action ).
Uses: Treatment of hypotension particularly
following general, spinal or epidural anaesthesia.
As a nasal decongestant.
Dose:3-6 mg repeated ( dilute 30 mg in 10 mls
saline)1 ml increments. IM: 30 mg

Caution in elderly, hypertension and CVS disease.

Can cause tachyphylaxis.
Avoid with MAOI and tricyclic antidepressants
may increase alpha-adrenergic effects of
ephedrine.
Side effect: Increase heart rate and blood
pressure, acute urinary retention, anxiety,
palpitation.

Phenylephrine
Selective direct-acting adrenergic agonist.
Peripheral vasoconstriction
Uses: Treatment of hypotension.
Dose:
IV 0.1-0.5 mg increments.
(10mg in 20 ml saline, 1 ml aliquots.)
IM: 2-5 mg
Infusion: 30-60 /min

Contraindication/precaution:
MAOI.
Caution in elderly or CVS disease
Side- effects:
Reflex Bradycardia, arrhythmias

Adrenaline
Endogenous cathecolamine with alpha and beta
action
Uses:
1. Treatment of anaphylaxis
2. Bronchodilator
3. Positive inotrope
4. Given by nebulizer for croup

Dose:
IV/IM/ETT:
1 ml aliquots of 1:10 000 up to 5-10 ml (0.51mg)
infusion: 2-20 mcg/min(0.04-0.4 mcg/kg/min)
nebulisation:5ml 1:1000
max dose for infiltration: 2 mcg/kg
Dilution: 3mg/50ml=1ml/hr=1g /min
Diluent: Normal saline / D5%
Infusion range: 1.2-12+ ml/h
Initial rate: 5ml/h

Caution in elderly.
Can cause arrhythmias especially with halothane.
Side effects:
Hypertension, tachycardia, anxiety,
hyperglycaemia, arrhythmias.
Reduces uterine blood flow
Remarks: should be administered via central
catheter whenever possible.

Dopamine
Naturally occuring catecholamine with ,1, and
dopaminergic activity.
Uses: Inotropic agent, treatment for hypotension.
Dose: 2-10 mcg/kg/min
Dilution:200mg/50ml (4mg/ml)
alternative regime:
3mg/kg/50ml = 1ml/h = 1g/kg/min
Diluent: 0.9% saline, 5%dextrose
Infusion rate: 2-9 ml/h

Contraindicated in phaeochromocytoma (due to

noradrenaline release),tachyarrythmias and VF.
Caution in patient with peripheral vascular
disease
Remarks:
Should be administered via central catheter.

Dobutamine
1 adrenergic agonist, positive inotrope and
chronotrope. Use in cardiac failure
Dose: 2.5-10 mcg/kg/min
Dilution:250mg/50ml (5mg/ml)

Contraindicated in arrhythmias and hypertension.

Side effects:
Tachycardia, decreased peripheral and pulmonary
vascular resistance.
Remarks:
Can cause phlebitis, but can be
administereed peripherally

Noradrenaline
Potent cathecolamine adrenergic agonist.
Vasoconstriction.
Uses: Treatment of hypotension
Dose:2-20 mcg/min (0.04-0.4 mcg/kg/min)
Dilution: 4 mg/40ml (100 mcg/ml)
Diluent: 5% dextrose

Side effects: Reflex bradycardia, arrhythmia,

hypertension
Remark:
Administered via central catheter only.
Potentiated by MAOI and tricyclic antidepressants

Vasopressin
-ADH.
-vasoconstriction.
Uses:
Treatment of hypotension
Treatment of diabetes insipidus
Dose: 20 unit/ml in 40 ml NS (0.5 unit/ml)
initial rate 2 ml/h ( diluent normal saline )
Extreme caution in coronary vascular disease
Side effects: Pallor, coronary vasoconstriction.

Calcium gluconate
Uses:
1. Electrolyte replacement
2. Positive inotrope.
3. Treatment for hyperkalemia and
hypermagnesaemia.
Description:
Calcium gluconate 10% contains Ca2+ 220
mol/ml.
Calcium chloride contains Ca2+ 680mol/ml

Dose:
2-5 ml 10% solution (10mg/kg, 0.07 mmol/kg)
Side effects:
Arrythmias, hypertension, hypercalcaemia
Remarks:
Less phlebitis than calcium chloride

Potassium chloride
Uses: Electrolyte replacement
Dose:
10-20 mmol/h (max concentration 40 mmol/litre
peripherally).
With ECG monitoring:
Up to 20-40 mmol/h via central line (Max 200
mmol/day)
Dilution: 1 gm in 50mls run over 1 h

Remarks:
Dilute solution before administration with 0.9%
normal saline,Dextrose 5%.
Rapid administration can cause cardiac arrest.
High concentration can cause phlebitis.

Magnesium sulphate
Essential mineral used to treat:
1.Hypomagnesaemia
2.Eclamptic seizures.
3. Arrhythmias
Magnesium sulphate
50%=500mg/ml=2mmol Mg2+/ml.
Normal plasma level Mg2+ 1.5-2.2mEq/litre.

Uses:
1. Hypomagnesaemia: 10-15 mg/kg over 20 min,
then 1 g/h.
2. Arrythmias: 2g over 10 min.
3. Eclampsia: 4g over 10 min then 1 g/h for 24h.
Caution:
Potentiate muscle relaxants.
Monitoring of serum level essential during
treatment. Can cause heart block
Side effects: CNS depression, hypotension

Sodium bicarbonate
Treatment for acidosis
Dose:
Wt(kg)x base deficit x 0.3) mmol
Normally administered undiluted (8.4%
solution)
Remarks:
8.4%=1000mmol/litre. Given via central line if
possible

Amiodarone
Mixed class IC and III antiarrhythmic
useful in treatment of supraventicular and
ventricular arrhythmias.
Dose:
Should be diluted with 5% dextrose only
Loading infusion : 5 mg/kg over 1-2 H then
15mg/kg over 24h
Maximum 1.2 g in 24H

Contraindication:
CI in Sinoatrial heart block, thyroid dysfunction
and pregnancy
Side effects:
Commonly causes thyroid dysfunction, reversible
corneal deposits, prolongation of QT interval.
Lung Fibrosis (rare)
Remarks: administered via central catheter.

Esmolol
Short acting cardioselective beta-blocker.
Metabolized by red cell esterases.
Treatment of supraventricular tachycardia or
intra-operative hypertension
Dose:
SVT: 0.5 mg/kg over 1 min, then 50200g/kg/min.
Hypertension: 25-100 mg then 50-300
g/kg/min
Dilution: 2.5g/50ml (50 mg/ml)

Contraindication:
Asthma, heart failure, AV block
Side effects:
Hypotension, bradycardia

Labetolol
Combined (mild) and adrenergic receptor
antagonist.
Blood pressure control without reflex tachycardia.
Duration 2-4 h
Dose:
5 mg increments up to 100 mg.
Infusion: 20-160mg/h
Contraindicated in asthma,heart failure, AV block.
Side effects: Hypotension, bradycardia,
bronchospasm

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