CHAPTER VI: TOPICAL AGENTS

- used on body surfaces; body cavities that open to the outside (oral, nasal, otic, vaginal and colon)

PROTECTIVES
- substances applied to the skin to protect certain areas from irritation (from mechanical origin)

Desirable Properties of Protectives
1. Insolubility limits the absorption of the compounds through the skin; difficult to wash them off
2. Chemically inert prevents interaction with tissues; biologically inactive
3. Adsorptive adsorbs moisture form skin, lessening friction and irritation
(smaller particle size, larger surface area)
soothing to apply, less irritation due to rubbing

TALC
- French Chalk, Soapstone, Piedra GRASSA, Creta Gallica
- native hydrous magnesium silicate sometimes containing small portion of Aluminum silicate
- fine white crystalline powder, adheres readily to the skin
- SOFTEST MINERAL KNOWN

Soapstone steatite (lump form)
Foliated Talc has a plate-like structure
- desirable for cosmetic and pharmaceutical purpose

- very low adsorptive properties; used as filtering aid (allowing filtration without danger or removing important
constituents
- Lubricating-protective dusting powder protects areas from further irritation

when used on broken skin, it produces sterile abscesses or granulomas (nodule of inflamed tissue where
granulation is occurring)


ZINC OXIDE
- Zinc White, Lana o Algodon Filosoficos, Flores de Zinc
Preparation:
- heating strongly in a furnace a mixture of coke and zinc mineral
Calamine (Zn
2
SiO
4
H
2
O)
Willemite (Zn
2
SiO
4
)
Smithsonite (ZnCO
3
)
Franklinite (ZnO + Manganese and iron oxide)
Zincite (ZnO, red variety)
- medicinal grade by calcinations of zinc carbonate

- gradually absorbs carbon dioxide from air, forming basic zinc carbonate
- forms Lewis acid (Zinc chloride) when treated with dilute HCl
- Zn
+2
antibacterial, ANTIMICROBIAL AND ASTRINGENT





USES
1. ASTRINGENT and TOPICAL PROTECTIVE
mild astringent and weak antimicrobial
o in the treatment of skin ulceration and other dermatological problems
2. primary ingredient of Calamine


CALAMINE ZnOxFe
2
O
3
- Zinc oxide + Ferric Oxide
Official forms:
1. Ointment
2. Paste
3. Zinc oxide with salicylic acid paste

USES
topical protective
o dusting powders, ointments, lotions
soothing, adsorbent, protective
better cosmetic acceptability than Zinc oxide
for dermatological problems

Calamine Lotion contains Calamine and Zinc oxide suspended with the aid of Bentonite Magma in a
calcium hydroxide solution
- protective with a good drying effect and mild astringent action
Phenolated Calamine Lotion (1% liquefied phenol)
local anesthetic and antipruritic

ZINC STEARATE
- zinc stearate and zinc palmitate
- mild astringent and antimicrobial
- not wetted by moisture
wont form crust patches over the area being treated
- USED AS LUBRICANT in tablets, as well as magnesium stearate
inhalation of zinc stearate dust can cause pulmonary inflammation

TITANIUM DIOXIDE TiO
2

- amorphous, infusible powder
- identified by adding H
2
SO
4
producing a orange-red colored Titanium peroxide (TiO
3
)

USES
- topical protective
used for its opacity due to its high refractive index
screens out UV reactions, sun creams and sun screen
- solar ray protective
most efficient solar ray protective
- white pigment
in cosmetic and paints
white pigment + ferric oxide = skin tone (pinkish)



SILICON POLYMERS
- Silicone Oil
inert protective in liquid form
dimethylsilicone ethers
Dimethicone/Simethicone
o water repellent and protective against contact irritants
prophylactic agent against chemical irritants
cleaning agent





- non selective (kills bacteria, kills skin)
Mechanism of Actions
1. Oxidation
- generally non-metals and certain types of anions
hydrogen peroxide
metal peroxide
permanganates
halogens
oxohalogens anions
- effective action involves the reducing group present in most proteins (e.g. sulfhydryl)
2. Halogenation
- destructive to the functions of specific proteins
destroy the function, destroy the microorganism
3. Protein Precipitant
- involves interaction of proteins with metallic ions with large radius ratio or strong electrostatic fields
Group 1-B
Group 2-B
Aluminum
most metal cations except of alkali and alkaline earth

ASTRINGENT
- burning/constriction action on the surface
- application of very dilute solution of metal cation to tissue provides a local/surface protein precipitant action
shrinkage / firming of tissues

Control of Antimicrobial/Astringent Action
1. Adjust the concentration
2. Place in a vehicle that will slowly releasing to the site of action
a solution containing glycerin and polyethylene glycol
3. Complexation with a ligand
- provides a controlled release, minimizing toxicity and activity on host cells
4. Synthesize into Insoluble Form
Suspension
ointment
cream
- slow release of active agent

ANTIMICROBIALS AND ASTRINGENTS


HYDROGEN PEROXIDE SOLUTION H
2
O
2

- Aqua oxigenada
- 3% antiseptic
- has an odor resembling that of ozone
- acidic to litmus and taste
- produces a froth in the mouth
USES
- mild oxidizing antiseptic
- destroy most pathogenic bacteria
- mechanical cleansing action of dirt, bacteria and debris from the wound or hard-to-reach areas
- 6% solution used as hair and fabric bleach
- antiseptic and cleansing on wounds (undiluted)
- mouthwash, vaginal douche(half-strength)


POTASSIUM PERMANGANATE KMnO
4

- Mineral Chamaleon
- dark purple crystalline compound, opaque in transmitted light
and of blue metallic luster in reflected light
- sweetish astringent taste
- oxidation (mechanism of action)
- KMnO
4
(+7)
- MnO
2
(+4)
Mn
+2

brown ppt
- poured directly on the skin (effective but produces brown spots)
Low penetrating power, short duration of action
USES
treatment for dermatitis (skin infections) caused by bacteria and fungi
poisoning produced by plant and animal toxins
wet dressing treatment of vesicular (small blisters or raised areas with fluid) stage of eczema, athletes
foot(Tinea pedis) and fungal infections on other portions of the body

SODIUM HYPOCHLORTE SOLUTION NaOCl
- Dakins Solution Chlorinated Soda Solution
- disinfectant
- clear pale greenish yellow liquid
- dissolves blood clots and delay healing
Labarraques Solution diluted solution containing 2.5%, disinfectant
- disinfectant and laundry bleach
germicidal agent
Modified Dakins Solution - can be used wounds with pus, without sutures (can be dissolved)
- removing necrotic tissues and antiseptic (diluted)
- can be used as foot bath

OTHER CHLORINE-CONTAINING COMPOUNDS:
1. Chlorinated Lime Bleaching Powder
- Calcium chloride hypochlorite
- disinfectant in swimming pools, and sterile rooms, bleaching agent
2. Chloramines organic amines
- releases hypochlorous acid (water purifier)
- antimicrobial action is due to the presence of HOCl



IODINE I
- Iodinum, Jodum
- grayish granules with a metallic luster
- I
2
solution (germicidal)
- toxic but inactivated in the GI tract
produces gastroenteritis, and bloody diarrhea
gastric lavage causes the person to vomit the iodostarch complex (blue)
- Iodine Solution and Iodine Tincture antimicrobial purposes
most effective topical agents available
antiseptic on skin prior to surgery
tincture may be used to disinfect drinking water

POVIDONE-IODINE
- polyvinylpyrrolidone (PVP)
- member of iodophors (solubilizing agent)
less irritating iodine without losing antimicrobial effectiveness
- useful for application in sensitive areas and mucous membranes
- recommended for surgical scrubs and preoperative antisepsis
- gargles and mouthwashes for the treatment of infections in the oral activity (Vincents angina)



SILVER NITRATE AgNO
3

- Azotas Argentious , Cristales Lunares
- protein precipitant (mechanism of action)
- astringent, antibacterial 0.01%
- irritant(corrosive) 10%
- has an oligo-dynamic action
antibacterial even in a low concentration (1%)
extended use can cause a darkening of the skin due to deposition of free silver below the epidermis
(argyria)
- OPHTHALMIC SOLUTION 1%
effective against ophthalmia neonatorum (gonorrhea)
microorganism causing blindness in babies
more effective than penicillin
- 0.5% in the form of wet dressing on third degree burns
SIDE EFFECT electrolyte imbalance
should be used alternately with other organic medication

Toughened AgNO
3

- lunar caustic, molded into pencil form by adding HCl
AgCl lessens the friability of the pencil (for hard to reach areas)
USES
- caustic, escharotics and germicide for small sepsic wounds (ulcerations)
- in condenser (purification of water) as linings
mas matagal sterile yung water




AMMONIATED MERCURY Hg(NH
2
)Cl
- White Precipitate
- for EXTERNAL preparations only, due to its toxicity (Hg
+2
is toxic)
- antiseptic on microorganisms
- local anti-infective
- ointment
- ophthalmic ointment to conjunctivas

SUBLIMED SULFUR
- Flowers of Sulfur, Azufre
- fine yellow crystalline (rhombic) powder
- obtained by condensing the sulfur vapors produced by heating any form of sulfur

PRECIPITATED SULFUR
- Milk of Sulfur
- scabicide, treatment of seborrhea, keratolytic agent
kills sarcoptes scabiei
- effective against live parasite, but has no effect on eggs

SULFURATED POTASH
- Liver of Sulfur
- potassium polysulfides + potassium thiosulfate
- used in the preparation of white lotion (scabicide)
- parasiticide
- treatment of acne and psoriasis

SELENIUM SULFIDE
- Selenium Disulfide
- bright orange powder with a faint odor
- toxic in large quantities, but important nutrient in trace amounts
- not well absorbed through skin
- used in shampoos 1%-2.5%, anti-seborrheic

ANTIMONY POTASSIUM TARTRATE (SbO)KC
4
H
4
O
6

H
2
O
- Tartar Emetic
- expectorant (brown mixture)
- treatment of schistosonomiasis (Schistosoma japonicum)
parasite, thrives in fresh water
infects the liver, attacks the vascular system, laki tyan
- Stibophen drug of choice for haematobium and mansoni (parenterally)












- local protein precipitant
- able to coagulate protein on the surface of cells
USES
1. Styptic stop bleeding from small cuts
promotes coagulation of blood and constricts the tissues
2. Antiperspirant decrease secretion of perspiration by constricting pores
3. Antiphlogistic restricts the supply of blood to the mucous membranes (reducing inflammation)
4. Corrosive removes unwanted tissues

ALUM AlNH
4
(SO
4
)
2
12H
2
O / AlK(SO
4
)
2
12H
2
O
- Tawas, Ammonium Alum, Potassium Alum
- sweetish strongly astringent taste
- source of Aluminum ion
useful as topical astringent
- irritants/caustics
- footbaths toughening the skink and avoid formation of blisters
- used in the preparation of several biological products
Precipitated diphtheria and tetanus toxoids
vaccines, injected to produce antibodies

ALUMINUM CHLORIDE AlCl
2
6H
2
O
- local external astringent and mild antiseptic
- irritating as antiperspirant, replaced by aluminum hydroxychloride

OTHER ALUMINUM-CONTAINING ASTRINGENTS:
ALUMINUM SULFATE Al
2
(SO
4
)
32
14H
2
O
- Cake Alum, Pickle Alum, Pearl Alum, Papermakers Alum

ALUMINUM ACETATE
- Burrows Solution
- aluminum oxide and aluminum acetate
- stabilized by adding boric acid

ZINC CHLORIDE ZnCl
2
- Butter of Zinc
- astringent and dentin desensitizer
- escharotics (caustic)

ZINC SULFATE ZnSO
4
7H
2
O
- White Vitriol
- transparent small needles/prisms, effloresces in dry air
- ophthalmic astringent



ASTRINGENT
S


CHAPTER VII: DENTAL PRODUCTS

Dental carries tooth decay
- caused by lactic acid (dissolves the enamel)
remedied by brushing and flossing
intake of fluoride
excess results to dental fluorosis (mottled enamel)
o adsorbs the color of the food, chalky and soft enamel
lethal dose is 2-5 grams
2 hypothesis
1. fluoride decreases the solubility of enamel
2. enzyme inhibitory property
- prevents the formation of lactic acid
daily intake = 2.2 mg

SODIUM FLUORIDE NaF
prophylactic agent
- 2% applied topically at age 3, 7, 11, 13

STANNOUS FLUORIDE SnF
2

- Tin Difluoride
- topical fluoride application 8%

DENTRIFICES
PUMICE
- Pumice Stone, Piedra Pomez
- complex silicates of Al, K, Na
- gritty gray powder
- dental abrasive
Grades of Fineness:
1. Pumice Flour/Superfine Pumice
2. Fine Pumice
3. Coarse Pumice














CHAPTER VIII: MISCELLANEOUS INORGANIC PHARMACEUTICAL
AGENTS

INHALANTS
- gases

OXYGEN O
2

- Dephlogisticated Air, Aire Vital, Fire Air, Aire Puro

Commercial Production:
1. Fractional Distillation of Liquid Aire (Linde Process)
- air is liquefied by low temperature and high pressure
2. Electrolysis of Water
- electricity passed through water containing 15% sodium/potassium hydroxide, breaking down water into its
components, hydrogen and oxygen
- oxygen is liberated at the anode


- tasteless gas which supports combustion
- responsible for oxidative changes in paints, fats, oil
- commercial oxygen is stored in green-colored cylinder
USES
- relieves pathological conditions accompanied by difficulty in breathing
- given in cases of carbon monoxide/coal gas/nitrous oxide/chloroform poisoning

CARBON DIOXIDE
- Carbonic Acid Gas/ Carbonic Anhydride
- stored in gray metallic cylinders
Dry Ice solid carbon dioxide, used as refrigerant

USES
1. Respiratory stimulant for persons suffering from impairment of the respiratory organs
2. dry ice destroys tissue by freezing it, treatment of acne, angiomas (tumor made up of blood), calluses, eczema,
moles, psoriasis and warts
3. used to make carbonated drinks

HELIUM He
- inert gas
- does not support combustion
- must be stored in brown green cylinders
- 80%helium+20%oxygen used to overcome difficulty in respiration
- used in high pressure underwater diving, reduces the risk of bends (formation of bubbles in the blood)
- causes the pitch of sounds to be increases, producing a Donald Duck sound





NITROUS OXIDE N
2
O
- Laughing Gas
produces inebriation in small doses (nakakahigh)
- maintains and revives the combustion of substances
- anesthetic in large doses
inhaled (momentary anesthesia)
extraction of teeth/opening of the abscesses

NITROGEN N
2
- Azote
- stored in black cylinder
- pharmaceutical air to displace air in parenteral and topical preparations

RESPIRATORY STIMULANTS
- causes a reflex action taking a sudden deep breath, to revive unconscious person

AMMONIUM CARBONATE
- Preston Salt, Sal Volatile, Bakers Ammonia, Ammonium Sesquicarbonate
- ammonium bicarbonate + ammonium carbamate (NH
2
CO
2
NH
4
)
- basis of smelling salts, valuable in hysterical syncope
- leavening agent Bakers ammonia
- Officially categorized as Source of Ammonia

AROMATIC AMMONIA SPIRIT
- composed of two active ingredients
Ammonium carbonate
Strong Ammonia Solution
- respiratory stimulant by inhalation of vapors

EXPECTORANT AND EMETICS
- stimulates the flow of respiratory tract secretions
- used in the treatment of respiratory disorders
terpinhydrate has direct effect over bronchial secretory cells
- act with a reflex action by irritating the gastric mucosa, thereby stimulating respiratory tract secretions
- emetics in low doses have sometimes been used in cough preparations

AMMONIUM CHLORIDE NH
4
Cl
- Sal Ammoniac, Salmiac, Ammonium Muriate
- increases secretions especially the saliva, mucous and sweat
- SYSTEMIC ACIDIFIER
- Chloride replenisher

POTASSIUM IODIDE KI
- Kalium Jodatum
- expectorant (antitussive)
- antifungal angent
- treatment of goiter



ANTIDOTES
- counteracts a poison
1. Physiological Antidote
- counteracts the effects of a poison by producing other effects
2. Chemical Antidote
- changing the chemical nature of the poison
3. Mechanical Antidote
- prevents the adsorption of the poison into the body

SODIUM NITRITE NaNO
2

- Natrium, Nitrosum
- antidote to cyanide poisoning (2% solution, intravenously)
CN attaches to ----> hemoglobin
|
methemoglobin (di makaattach si CN)

SODIUM THIOSULFATE Na
2
S
2
O
3
5H
2
O
- Antichlor Hypo
- antidote for cyanide and iodine poisoning
- fixer in photographic films
- in bleaching paper pulps
- CHEMICAL ANTIDOTE
CN -----> SCN
toxic non-toxic

ACTIVATED CHARCOAL
- Carbon Ligni
- residue from destructive distillation of organic materials, treated to increase adsorptive power
- obtained by incomplete combustion of wood
activation removing previously adsorbed substances, reduces its particle size

- GENERAL PURPOSE ANTIDOTE

Mechanical antidote
1. adsorb Activated charcoal, Kaolin
2. ppt CuSO
4
5H
2
O

CUPRIC SULFATE CuSO
4
5H
2
O
- Blue Vitriol, Blue Stone, Caparrosa Azul, Piedra Lipis
- antidote for phosphorous poisoning
- 300 mg emetic
- 10-30 mg astringent and tonic






TABLETING AIDS
- diluents are filler materials which bring the tablets up to acceptable size
- physiologically inert
- Lactose is a common diluent

CALCIUM SULFATE CaSO
4

- Gypsum, Alabaster, Satin Spar, Light spar (dihydrated)
- marketed as Drierite, used as rechargeable desiccant
- hemihydrated (Plaster of Paris) is used as supportive casts and dental impressions

COLLOIDAL SILICON DIOXIDE SiO
2

- prepared by vapour-phase hydrolysis
- used as tablet diluents, suspending, and thickening agent

LUBRICANTS
- makes it possible to eject the tablet cleanly without leaving a residue behind in the mold
- most are insoluble soaps (heavy metals of fatty acids)
Calcium Stearate
Magnesium Stearate
source of higher fatty acids

SUSPENDING AGENTS
- act by altering the surface character of the solvent(surfactant) and others are thickening agents

BENTONITE Al
2
O
3
4SiO
2
H
2
O
- Soap Clay, Mineral Soap, Wilkinite
- native, colloidal, hydrated aluminium silicate
- has an earthly taste
- also used as stabilizer in industrial emulsions
- exerts detergent effect (used in soaps and cleansers)
- clarifying agent with adsorptive powers for dyes and other coloring matters.



















CHAPTER IX: RADIOPHARMACEUTICALS AND CONTRAST MEDIA

isotopes different form of an element, which vary in the number of neutrons contained in the nuclei
When radioactive isotopes decay, they emit certain particles or quantities of energy that are characteristic of the
particular isotope involved.

Major Particles of Decay
1. Alpha Particles (,
4
He
+2
)
- heaviest and slowest of all radioactive emissions

2. Beta Particles (
-
)
- negatively charged species having a mass of an electron
- moves at a faster velocity
- more penetrating power
negatrons
- emitted by unstable nuclei having neutrons in excess of protons
- if neutron/proton ratio exceeds stable limits, transformation of neutron to proton occurs, with the expulsion of
beta radiation
element undergoing this type of transformation will decay to the element having the next
highest atomic number
positron (
+
)
- a proton is transformed into a neutron, accompanied by the emission of positron
elements emitting positron radiation will decay to the element having the next lowest atomic
number
3. Gamma Radiation ()
- a photon of electromagnetic radiation
- demonstrates both wave and particle properties
- rays are of short wavelength, similar to x-ray
- travels at a speed of light
- emission of gamma ray is almost always accompanied by the emission of other forms of radiation
K-Process process wherein a type of radiation similar to gamma rays is seen in the emission of x-
rays
*K shell (1st orbital)

Biological Effects of Radiation
- can lead to necrosis and complete destruction of the tissue or organ

Radiopharmaceuticals are preparation containing isotopes which are used internally for therapeutic and diagnostic
purposes

Isotopes important as radiopharmaceuticals are:
1. Those emitting beta and gamma radiation since they can penetrate body tissues
2. Isotopes which can be concentrated in specific manner in certain organ or cells
3. Isotopes which should be eliminated from the body easily and aside from the associated radioactivity, they and
the decay products should be of low toxicity

Radiopharmaceutical Preparations
1. Sodium Chromate Cr 51 Injection
- Chromitope Sodium Rachromate -51
diagnostic determination of red blood cell mass, volume and survival time, and
scanning of spleen



2. Gold Au 198 Injection
- Aurcoloid -198, Aureotope, Auroscan
diagnostic preparations for scintillation scanning of the liver

3. Sodium Iodide I 123 Solution (Iodotope I 125)
diagnostic aid in the study of the function of the thyroid gland
scanning thyroid gland

Sodium Iodide I 131 Capsules & Solution (Iodotope I-131)
determine the blood and plasma volumes
determination of cardiac output

4. Sodium Rose Bengal I -131 Injection
- Robengatope I-131
radioactive tracer in the determination of the liver function

5. Sodium Iodohippurate I-131 Injection
- Hippuran -131
diagnostic agent to determine kidney function

6. Chlormerodin Hg 197 Injection and Hg 203 Injection
Scintillation scanning of the kidneys and brain

7. Sodium Phosphate P 32 Solution
- Phosphotope
Treatment of polycythemia vera (increase in RBC)
localization of intraocular tumors

8. Technetium T 99 Injection
- Sodium Pertechnetate
Brain scanning to determine the presence and location of neoplastic lesions

9. Cyanacobalamin Co-57 and Co-60 Capsules and Solutions
diagnostic agent for pernicious anemia

Radiopaque Contrast Media
- chemical compounds containing elements of high atomic number which will stop the passage of x-ray

BARIUM SULFATE BaSO
4
- Barium Meal, Sulfato de Bario, Esophotrast
- most insoluble sulfate
- Ba
2+
is toxic
- used as an opaque contrast medium in the roentgenographic examination of the intestinal tract and stomach
so that they may be photographed