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 (Zn2SiO4H2O)
Willemite (Zn2SiO4)
Smithsonite (ZnCO3)
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

Pharmaceutical Chemistry Chapters 6, 7, 8 & 9 | Suzette Pamela G. Santos | 1FPharmacy

CALAMINE ZnOxFe2O3
- 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 TiO2

-

amorphous, infusible powder

identified by adding H2SO4 producing a orange-red colored Titanium peroxide (TiO3)

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

Pharmaceutical Chemistry Chapters 6, 7, 8 & 9 | Suzette Pamela G. Santos | 1FPharmacy

ANTIMICROBIALS AND ASTRINGENTS

- 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

HYDROGEN PEROXIDE SOLUTION H2O2

USES
-

Aqua oxigenada
3% antiseptic
has an odor resembling that of ozone
acidic to litmus and taste
produces a froth in the mouth
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)

Pharmaceutical Chemistry Chapters 6, 7, 8 & 9 | Suzette Pamela G. Santos | 1FPharmacy

POTASSIUM PERMANGANATE KMnO4

-

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)
KMnO4(+7)- MnO2(+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
I2 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)

Pharmaceutical Chemistry Chapters 6, 7, 8 & 9 | Suzette Pamela G. Santos | 1FPharmacy

SILVER NITRATE AgNO3

-

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 AgNO3
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(NH2)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

Pharmaceutical Chemistry Chapters 6, 7, 8 & 9 | Suzette Pamela G. Santos | 1FPharmacy

ANTIMONY POTASSIUM TARTRATE (SbO)KC4H4O612H2O

-

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)

ASTRINGENT
S - 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 AlNH4(SO4)212H2O / AlK(SO4)212H2O

-

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 AlCl26H2O

-

local external astringent and mild antiseptic

irritating as antiperspirant, replaced by aluminum hydroxychloride

OTHER ALUMINUM-CONTAINING ASTRINGENTS:

ALUMINUM SULFATE Al2(SO4)3214H2O

-

Cake Alum, Pickle Alum, Pearl Alum, Papermakers Alum

ALUMINUM ACETATE
-

Burrows Solution
aluminum oxide and aluminum acetate
stabilized by adding boric acid

ZINC CHLORIDE ZnCl2

-

Butter of Zinc
astringent and dentin desensitizer
escharotics (caustic)

ZINC SULFATE ZnSO47H2O

-

White Vitriol
transparent small needles/prisms, effloresces in dry air
ophthalmic astringent

Pharmaceutical Chemistry Chapters 6, 7, 8 & 9 | Suzette Pamela G. Santos | 1FPharmacy

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 SnF2

-

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 O2
-

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

Pharmaceutical Chemistry Chapters 6, 7, 8 & 9 | Suzette Pamela G. Santos | 1FPharmacy

USES
-

tasteless gas which supports combustion

responsible for oxidative changes in paints, fats, oil
commercial oxygen is stored in green-colored cylinder
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 N2O

-

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 N2
-

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 (NH2CO2NH4)
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

Pharmaceutical Chemistry Chapters 6, 7, 8 & 9 | Suzette Pamela G. Santos | 1FPharmacy

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 NH4Cl

-

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 NaNO2

-

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

SODIUM THIOSULFATE Na2S2O35H2O

-

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 CuSO45H2O

Pharmaceutical Chemistry Chapters 6, 7, 8 & 9 | Suzette Pamela G. Santos | 1FPharmacy

CUPRIC SULFATE CuSO45H2O

-

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 CaSO4

-

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 SiO2

-

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 Al2O34SiO2H2O
-

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.

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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 (, 4He+2)
- heaviest and slowest of all radioactive emissions
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*K shell (1st orbital)
rays
2.
-

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

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11

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 BaSO4

-

Barium Meal, Sulfato de Bario, Esophotrast

most insoluble sulfate
Ba2+ is toxic
used as an opaque contrast medium in the roentgenographic examination of the intestinal tract
and stomach so that they may be photographed

Pharmaceutical Chemistry Chapters 6, 7, 8 & 9 | Suzette Pamela G. Santos | 1FPharmacy

12