Pharmaceutical Chemistry 1 (Lecture)

TOPICAL AGENTS – ANSWERS AND RATIONALE

1. C. Protectives
 In its broadest pharmacological sense a PROTECTIVE is any agent that isolates the exposed
surface (skin or other membranes from harmful or annoying stimuli. Substances that protect by
mechanical or other physical means are considered to be protectives. While the surface action of
adsorbents and emollients may impart some protection, demulcents and emollients are placed
in separate categories that reflect their primarily dermatological function. The abridge category
of protectives mainly comprises the - dusting powders, adsorbents, mechanical protective agents,
and plasters. (ref. Remington)
 Protectant – a topical drug that provides a physical barrier to the environment. (ref. Ansel’s
Pharmaceutical Drug Dosage Forms and Drug Delivery system – DDS)
2. A. Adsorbent
 It is a drug that binds other chemicals onto its surface; it is used to reduce the free availability of
toxic chemicals. (ex. Kaolin – GIT adsorbent (ref. Ansel’s Pharmaceutical dosage form and drug
delivery system)
 Absorbents – a drug that takes up other chemicals into its substance and is used to reduce the
free availability of toxic chemicals. (ex. Polycarbophil – GIT absorbent)
3. D. Emollient (ref. Ansel’s DDS)
 Demulcent – a bland viscous liquid, usually water based, used to coat and soothe damaged or
inflamed skin or mucous membranes.
 Caustic – a topical that destroys tissue on contact and is useful in removing skin lesions.
 Astringent – a drug used topically to toughen and shrink tissues. (Ex. Aluminum acetate solution);
acts through a local and limited protein coagulant effect. (ref. Shargel)
 Rubefacient – a topical drug that induces a mild skin irritation with erythema; it is used as a
toughening agent (ex. Rubbing alcohol)
 Vesicant – a blistering agent or blister-producing agent; Drugs associated with necrosis of tissue
(re. Shargel)
 Sclerosing agent – an irritant drug suitable for injection into varicose veins to induce their fibrosis
and obliteration.
 Keratolytic – a topical drug that toughens and protects skin; work by dissolving or breaking down
the outermost layer of skin, causing peeling of the stratum corneum.
4. C. Both are true.
 Dusting powders are relatively inert and insoluble substances that are used to cover and protect
epithelial surfaces, ulcers, and wounds. Usually these substances are very finely subdivided
powders. They generally absorb moisture and, therefore, also act as cutaneous desiccants
(HYGROSCOPIC AGENTS). The absorption of skin moisture decrease friction and also discourages
certain bacterial growth. (ref. Remington)
 Several of the dusting powders are incorporated into ointments, creams, and lotions. They also
serve other functions in tablet and other pharmaceutical dosage forms.
5. E. I, II and III
 See rationale of #1
6. B. First statement is false. Second statement is true.
 The water-absorbent powders should NOT be administered to wet, raw surfaces because of the
formation of cakes and adherent crusts. Starch and other carbohydrate powders may become
doughy with absorption of aqueous-based fluids but also may ferment. Consequently, such
powders often contain an antiseptic. Most impalpable powders are absorptive, to some extent.
Absorption of fatty acids and perspiration contributes to deodorant action of such powders.
 Dusting powders, when carried into pores or wounds or left upon skin or epithelial surfaces, eg,
talc, may cause irritation, granulomas, fibrosis, or adhesions.
7. C. I and III
 The beads are composed of a three-dimensional network of cross-linked dextran (Polysaccharide -
> Carbohydrate -> GLUCOSE -> POLYGLUCAN). This network selectively imbides molecule son the
basis of molecular mass (Molecules < 1000 daltons are imbided; molecules 1000 – 5000 daltons
have decreased absorption with increasing molecular weight, and molecules with >5000 daltons
Pharmaceutical Chemistry 1 (Lecture)

are NOT IMBIDED. Four mL of water are absorbed for each gram of dextranomer, and absorption
is continuous so long as unsaturated beads are in proximity to the wound. This therapy is
associated with the rapid and continuous exudate removal form wound surfaces, resulting in a
marked reduction in inflammation, edema, and pain, as well as granuloma tissue formation and
reduction in time for wound healing. (ref. Remington)
8. E. I, II and III
 Dusting powders include:
o Bentonite – a native, colloidal, hydrated aluminum silicate; Chemically (Al2O3.4SiO2.H2O); It
has the property of adsorbing large quantities of water, swelling to approximately 12 times
its original. It gel-forming property is augmented by small amounts of alkaline substances,
such as magnesium oxide. it does not swell in organic solvents. USES: a protective colloid for
stabilization of suspensions. It also has been used as a emulsifier for oil and as base for
plasters, ointments, and similar preparations. PREPARATION: BENTONITE MAGMA (ref.
Remington)
o Bismuth Subsalicylate – aka. Basic Bismuth Subsalicylate; present in Pepto-Bismol; USES: As
an anti-diarrheal agent it shows good activity versus Salmonella but less activity versus
Escherichia coli. As an anti-ulcer, it seems to increase the rate of healing of peptic ulcers. It
also reduces active intestinal secretion induced by E. coli and Vibrio cholerae. This is thought
to be due to the anti-prostaglandin activity by subsalicylate components. It is used also as an
antibiotic for the prophylaxis of traveller’s diarrhea and amoebiasis. It is also used to treat
the common form of gastritis and duodenal ulcer caused by H. pylori. In this circumstance, it
is used in combination with an antibiotic (usually amoxicillin and/or metronidazole) and an
H2-blocker or Proton pump inhibitor, but it is effective when given alone.
 MOA: It forms a glycoprotein-bismuth complex with the mucus that may create a
protective barrier against acid peptic digestion. It may also stimulate PGE2 (Prostacyclin),
which in turn stimulates mucus and bicarbonate secretion. It may stimulate epidermal
growth factor, which may enhance healing of ulcers.
 ADE: Not recommended in patients with renal failure; Ringing of the ears due to the
salicylate component; darkening of the stool due to bismuth sulfide formation -> may
mistakenly suggest GI bleeding. (ref. Remington)
o Boric Acid – aka Boracic acid; Orthoboric acid; USES: Officially recognized as a BUFFER. It is a
very weak germicide (local anti-infective). Aqueous solutions are employed as an eyewash,
mouth wash, and for irrigation of the bladder. A 2.2% solution is isotonic with the lacrimal
fluid. It is also employed as a dusting powder, when diluted with some inert materials. It can
be absorbed through irritated skin, eg. infants with diaper rash. (ref. Remington)
o Calcium carbonate – See previous lectures (Antacids)
o Cellulose – Organic molecule -> POLYSACCHARIDE -> Polymers of glucose -> Beta 1, 4
Glycosidic Linkage
o Magnesium Stearate – Octadecanoic acid, magnesium salt; USES: lubricant in the
manufacture of compressed tablets
o Talc – See previous lectures (Aluminum compounds)
o Titanium Dioxide – aka Titanic Anhydride, Titanium oxide (TiO2); USES: Due to its very high
reflectance at visible and UV wavelengths, it serves as an excellent white pigment. In
ointments and lotions it reflects a very high proportion of incident sunlight, hence, protecting
the skin from sunburn and serving as a sunblock. It is also used in cosmetics and as a dusting
powder. Topically, it is devoid of toxicity. (ref. Remington)
o Zinc Oxide – See previous lectures (Zinc Compounds)
o Zinc Stearate – Octadecanoic acid, zinc salts; USES: In water-repellent ointments and as a
dusting powder in dermatological practice for its desiccating, astringent, and protective
effects. It has been removed form baby dusting powders, owing to accidental, fetal
inhalations (pulmonary inflammation). (ref. Remington)
9. B. I and II
 The TWO principal classes of mechanical protectives are the collodions and plasters. Mechanical
protectives may be somewhat irritating because of the interference with normal percutaneous
Pharmaceutical Chemistry 1 (Lecture)

water transport caused by certain oligomers, resins, and other components, especially in
plasters.
10. E. I, II and III
 Mechanical and Chemical protectives include:
o Aluminum Hydroxide gel – See previous lectures
o Colloidion – Organic compound; contains not less than 5.0%, by weight, Pyroxylin (Gun
cotton)
o Petrolatum gauze – Organic compound
o Gelatin sponge
o Kaolin
o Lanolin – fatty substance obtained from the wool of the sheep
o Mineral oil, olive oil, peanut oil
o Silicones – aka. Polyorganosiloxanes, Silastic; Organosilicon polymers containing chains of
altering oxygen and silicon atoms with substituent organic compounds.
11. C. Zinc Oxide
 ZnO is a mild astringent and a weak antimicrobial compound. It is classified as an astringent and
topical protective. The antimicrobial-astringent action is due to the release of a small amount of
zinc ion from the hydrolysis in the acidic moisture on the skin.
12. E. I, II and III (ref. Block)
13. E. I, II and III
 Zinc carbonate – used for its lubricity and as a drying agent. (ref. Remington)
14. A. Ferric Oxide
 Calamine USP is obtained by calcination (powdered by heating) of the natural ore. The calcined
product is then passed through a 100-mesh sieve to obtain the finely powdered material
necessary for good cohesive and adhesive properties.
 Calamine is classified by the USP as a topical protective. It is used as dusting powders, ointments,
and lotions where it is applied to the skin for its absorbent, soothing, protective properties. (ref.
Block)
15. B. I and II
 Calamine lotion USP is one of the most widely used preparation containing calamine. It contains
equal portions or quantities of Calamine and Zinc Oxide suspended with the aid of Bentonite
Magma in a solution of Calcium hydroxide. The lotion is a protective with a good drying effect
and as a mild astringent action.
 Phenolated Calamine Lotion USP contains 1% liquid phenol which provides a local anesthetic and
anti-pruritic action. (ref. Block)
16. A. I only – see #15
17. E. All of the above
 Zinc Stearate USP consists chiefly of variable proportions of zinc stearate and zinc palmitate, and
zinc oxide. USES: It has mild astringent and antimicrobial properties. It is employed as dusting
powders and ointments as a protective. It has a particular advantage over many products (talc)
in that it is not wetted by moisture making it more desirable in dermatological problems where
large amounts of fluid are exuded.
18. B. is not true – see #17
19. C. Imparts an orange-red color to the solution
 Reaction of Titanium dioxide with Hydrogen peroxide in dilute H2SO4 (Ref. Block)
20. D. Titanium Dioxide
 As a solar protective, it is used in concentration of 5 to 25% in ointments or lotions. Its action is
due primarily to opacity. Organic sun screen agents, eg., p-aminobenzoic acid, act by chemically
absorbing UV radiation.
 It is also used as a white pigment in cosmetics and paints. the very white character of the
pigment may be toned down for cosmetics purpose to a cream color through the addition of
small or trace amounts of iron (III) compounds (eg., Phoshate) during manufacturing process.
21. C. Both are true
 Aluminum is present in 10% in Aluminum Paste; used as a protective to prevent irritation around
intestinal fistulae (an abnormal opening of the intestinal tract through the skin).
Pharmaceutical Chemistry 1 (Lecture)

22. D. Simethicone is an anti-flatulent

 Silicones – aka. Polyorganosiloxanes, Silastic; Organosilicon polymers containing chains of altering
oxygen and silicon atoms with substituent organic compounds, frequently methyl or phenyl,
attached to each silicon atom.
 Silicone polymers are INERT protective substances occurring in liquid form and known generally
as SILICONE OILS. They are primarily DIMETHYLSILICONE ETHERS represented by the general
structure:

 Polymers such as Dimethicone and Simethicone are used in ointments and creams for
application to the skin as water repellent and protective against contact irritants. Simethicone is
also used as a gastric protective and anti-flatulent or gastric defoaming agent. Primarily used as a
prophylactic against chemical irritants. In the form of inhalation sprays, silicone preparation has
been employed in the treatment of pulmonary edema involving frothing fluid in the upper
respiratory tract.
 Silicone oils adhere very well to the skin and exclude contact with the air; they should NOT be
applied over broken or abraded skin or wounds requiring drainage. Contact with the eyes should
also be avoided. (ref. Block)
23. E. I, II and III
 Silicone fluids are also employed to prevent adhesion between components or materials. (ref.
Remington)
24. B. Antiseptic
 Anti-infective agents that are used locally are called GERMICIDES. It describes agents which KILL
microorganism.
 Antiseptic are compounds that KILL (-cidal) or prevent the growth of (-static) microorganisms
when applied to living tissue. The ideal antiseptic should have low-enough toxicity that can be
used directly on skin or wounds; it will exert a rapid and sustained lethal action against
microorganism (the spectrum may be narrow or broad depending on the use).The agent should
have a low surface tension so that it will spread into the wound; it should retain activity in the
presence of body fluids (including pus), be nonirritating to tissues, be nonallergenic; lack
systemic toxicity when applied to skin or mucous membranes, and not interfere with healing. No
antiseptic available today meets all these criteria.
 Disinfectant – is an agent that prevents transmission of infection by the destruction of
pathogenic microorganism when applied to inanimate objects. The ideal disinfectant exerts as
rapidly lethal action against all potentially pathogenic microorganisms and spores, has good
penetrating properties into organic matter, shares compatibility with organic compounds
(particularly soaps), is not inactivated by living tissue, is noncorrosive, and is aesthetically
pleasing (nonstaining and odourless).
 Sanitization – Reduction of microbial load on inanimate surface to a level considered acceptable
for public health purposes.
 Decontamination – destruction or marked reduction in number or activity of microorganisms
 Sterilization – a process intended to kill or remove all types of microorganisms, including spores,
and usually, including viruses with an acceptably low probability of survival; this refers to the use
of disinfectant or other procedure to render an object completely free of microorganisms.
 Disinfection – chemical or physical treatment that destroys most vegetative microbes or viruses,
but not spores, in or on inanimate surfaces.
 Pasteurization – a process that kills nonsporulating microorganisms by hot water or steam at 65
– 100 deg. Celsius. (ref. Wilson and Gisvold’s)
25. D. Both are false
26. D. Disinfection – see #24
27. E. I, II and III – (ref. Remington pp 1649)
28. B. 65 - 100°C – see #24
Pharmaceutical Chemistry 1 (Lecture)

29. D. II and III – see #24

30. C. I and III – see #24
31. E. I, II and III
 The mechanisms of action of inorganic anti-microbial agents can be divided into three general
categories: oxidation, halogenation, and protein precipitation. it is important to note that in
contrast to certain organic compounds known as antibiotics, the site of the action of inorganic
antimicrobial compounds are, for most part, nonspecific. These agents will interact in a similar
fashion with all protein, and in high enough concentrations will affect host proteins as well as
microbial protein. (ref. Block)
 OXIDATION
o Oxidizing agents that are of any value as germicidal agents depend on their ability to liberate
oxygen in the tissues. Many of these agents include hydrogen peroxide, several metal oxides,
sodium perborate, permanganates, halogens (Cl and I), and certain oxalo-halogens. Oxidizing
agents such as hydrogen peroxides, metal peroxides, and sodium perborate act by
generating oxygen and oxygen radicals. Other oxidizing agents, such as KMnO4, denature
proteins in microorganisms through a direct oxidation reaction. Oxidizing reagents are
especially effective against anaerobic bacteria and can be used in cleansing contaminated
wounds. The bubbles that form during the liberation of oxygen help to dislodge debris. The
effectiveness of the oxidizing agents is somewhat limited by their generally poor penetrability
into infected tissues and organic matter. Additionally, the action of the oxidizers is typically
transient. (ref. Gisvold’s)
o The effective oxidative action involves the reducing groups present in most proteins, e.g., the
sulfhydryl group in cysteine. The overall change or destruction of function in specific proteins
is responsible for the ultimate destruction of the microorganisms. Oxidizing the protein will
cause reduction of the antimicrobial agents. (ref. Block)
 HALOGENATION
o This is the reaction occurring with antiseptics of the hypohalite type and, in particular,
hyochlorite, OCl. Since these types of compounds can serve as reagents in the chlorination of
primary and secondary amides, it is expected that a similar reaction can take place under
appropriate conditions with the peptide linkages between the amino acid groups comprising
the amino acid molecule.
o The reaction is ultimately destructive due to the substitution of chlorine atom for the
hydrogen causing changes in the forces (hydrogen bonding) responsible for the proper
conformation of the protein molecule. As in the oxidative case, the changes in conformation
result in changes and destruction of functions.

 PROTEIN PRECIPITATION
o This type of mechanism involves the interaction of proteins with metallic ions having large
charges/radius ratios or strong electrostatic fields. This property is available in transition
metals cations, including metals of Group IB and IIB. Aluminum in Group IIIA, due to its
charge and small ionic radius, is also an effective protein precipitant. Most metals, with the
exception of the alkali and alkaline earth metals, will demonstrate protein precipitant activity.
o The nature of interaction is one of complexation in which the various polar groups on the
protein act as ligands. The complexation of the metal results in a radical change in the
properties of the protein or protein precipitant. Certain metals (mercury, arsenic, and
antimony) show some enzyme specificity, form strong covalent bonds with particular enzyme
systems. The presence of the metal “ties up” important functional groups at the active sites
on the enzyme. The precipitant properties of metal cations can be altered according to the
concentration at the site of action. Increasing concentrations - increasing antimicrobial,
astringent, irritant, and corrosive properties. (ref. Block)
32. C. I and III – see #31
33. A. First is true. Second is false. (ref. Gisvold’s)
 Also known as UREA PEROXIDE. Carbamide peroxide is used as both an antiseptic and
disinfectant. The preparation is especially effective in the treatment of oral ulcerations or in
dental care. The bubbles that are liberated remove debris.
Pharmaceutical Chemistry 1 (Lecture)

34. C. Both are true.

 The compound in formulated with 30% water to make it safer to handle. Benzoyl peroxide
induces proliferation of epithelial cells, leading to sloughing and repair.
35. D. II and III
 Calcium is an alkaline earth metal. see #31
36. D. Both are false. – see #31
37. C. Both are true – (ref. Block)
 Astringents provide a local or surface protein precipitant action. Being a surface phenomenon, it
does not usually result in the destruction of host tissue. The effect can be generally described as
a “SHRINKAGE” or “FIRMING” of the tissue. Astringents can cause constriction of capillaries and
small blood vessels; hence, they are used as STYPTICS to stop bleeding small cuts. Astringents are
also used to reduce the volume of exudate form wounds and skin eruptions. They are also found
as antiperspirants in deodorants because of their ability to constrict pores and destroy
microorganisms that may produce body odors. The concentration of protein precipitants
required for antiperspirant activity is higher than that is required for antimicrobial activity.
Astringents may also stimulate the growth of new tissue.
38. E. I, II and III – (ref. Block pp 310)
 See #37
39. A. First is true. Second is false – (ref. Block pp311)
 Hydrogen peroxide solution usually deteriorates upon standing or upon protracted agitation, and
rapidly decomposes when in contact with many oxidizing or reducing substances. Pure hydrogen
peroxide liquid has astringent properties; however, this form of hydrogen peroxide is not
intended to be applied onto the skin.
40. D. A and B – (ref. Block pp 311)
 When heated to 100°C, pure hydrogen peroxide decomposes explosively to form water and
oxygen. The decomposition is exothermic but the rate of decomposition is very slow in the
absence of catalysts (impurities). Small amount of contaminants or impurities, e.g., divalent and
polyvalent ions of chromium, iron, copper, mercury, etc., will catalyze the decomposition of
unstabilized solutions.
41. B. – (ref. Block pp 312) – discuss properties of H2O2
 Hydrogen peroxide is acid to litmus paper. The compound is a weak acid in aqueous solution,
ionizing primarily to form the peroxide ion. It is a weaker acid than boric acid or carbonic acid.
 Aluminum does NOT act as a catalyst, hence, does not catalyze decomposition of the solution.
Tanks of this metal are good storage containers.
 The solution can be stabilized using different stabilizer. These include 1) acids or acidic salts, 2)
complex-forming, and 3) adsorptive.
o ACIDIC – All acids, inorganic, increase the stability of hydrogen peroxide. Alkaline solutions of
hydrogen peroxide, even if pure, are much more unstable; the instability is due more to the
impurities present in the standard grades of alkalies than to any direct alkaline catalysis. The
presence in trace amounts of acidic substances such as sulfuric acid, phosphoric acid, benzoic
acid, citric acid, or acid salts will greatly increase the stability if hydrogen peroxides solutions.
Based on the chemical equation given below, any additional hydrogen ion will cause the
equilibrium to shift toward hydrogen peroxide.
H2O2  2H + O2
o COMPLEX-FORMING or CHELATING AGENTS – Some common agents used for this purpose
include acetanilid, phenacetin, quinine-sulfate, and 8-hydroxyquinoline. They supposedly
remove heavy metal ions form solution by forming a coordination complex, thereby making
these metals unavailable to catalyze decomposition. These compounds may also act as
“SCREENING AGENTS”. In this way they protect the peroxide from the effects of sunlight.
o ADSORBENTS – Adsorbents (silica, alumina, hydrous antimony oxide, or hydrous stannic oxide)
remove impurities from the solutions. Their function is then somewhat comparable to the
complexing agents. However, it should be noted that the therapeutic uses of hydrogen
peroxide are dependent upon its decomposition by the enzyme catalase, and some of these
stabilizers will also inactivate the enzyme at the site of action.
42. A. Catalase – (ref. Block and Rogers pp. 312-313 and pp. 50 – 51)
Pharmaceutical Chemistry 1 (Lecture)

 2 H2O2  2 H2O + O2
43. D. Both are false. – (ref. Block and Roger’s pp 312 and 52)
 Depending on the chemical environment, hydrogen peroxide will react as either an oxidizing or
reducing agent. The oxidation number of oxygen in the peroxide ion in -1. When hydrogen
peroxide functions as an oxidizing agent each oxygen atom changes from a -1 to -2 forming two
oxide ions. This shows that each molecule of H2O2 has an oxidation number of 2 and requires the
reducing agent to supply 2 electrons. The oxidation reaction is most efficient in an acidic media
and produces water. The reducing action of hydrogen peroxide results in the evolution of
molecular oxygen. This involves the release of two electrons and a change from peroxide ion to
an oxidation state of zero.
o As oxidizing agent: H2O2 + 2H + 2e-  2 H2O
o As reducing agent: H2(O2) -2  O2 (removal of electrons)
44. A. (ref. Block pp 314 and Roger’s pp 57)
 The strength of hydrogen peroxide solutions are expressed in terms of “Volume”. The volume
specification is based on the number of mL of oxygen, measured at standard temperature and
pressure, liberated by 1 mL of the peroxide solution when decomposes. The official solution
containing 3% hydrogen peroxide is often referred to as a 10 volume solution, indicating that
1mL of the solution will liberate a total of 10 mL oxygen. Extending this further, a 6% solution is a
20 Volume solution. Hydrogen peroxide in 6% (20 Vol) solution is used as a hair and fabric bleach.
 USES:
HYDROGEN PEROXIDE
o The primary use is as a mild OXIDIZING ASTRINGENT. This action occurs when the solution
comes in contact with open or abraded tissue, exposing the chemical to the enzyme
CATALASE. Oxygen acts as an OXIDIZING agent on bacteria providing antiseptic action on
those organisms obliged to survive through anaerobic metabolism. This property is referred
to as “AUTO-OXIDATION”. Hydrogen peroxide is effective against E. coli, S. aureus, and
typhoid bacilli. The anti-septic action does not penetrate below the surface to which it is
applied. The foaming caused by the liberation of O2 mechanically cleanses wounds by
dislodging fixed bacteria, particles of dirt, etc., from the surface if the wounds or difficult-to-
reach areas, e.g., ear canal. The mechanical action is an important function which is useful in
removing surgical dressings and in loosening ear wax. Because of the release of oxygen gas,
hydrogen peroxide should never be injected into closed cavities. In addition to the problem
created by having no free exit of gas, the irritating effects of the compound can cause
bleeding and rapid, complete destruction of the H2O2 with the accumulation of much gas.
o The official solution is also used in treating VINCENT’s STOMATITIS, the undiluted being used
as a moth wash. Continued used may cause a condition known as a “HAIRY TONGUE”
(Hypertrophied filiform papillae), which disappears on discontinuation of the medication.
Because of its lack of toxicity, it is a favourite disinfectant for use in the nose and throat. It is
also a chemical ANTIDOTE for cyanide and phosphorus poisoning through oxidation of the
poisonous materials to more or less harmless oxidation products.
o Buddizing process – 0.1% of Hydrogen Peroxide is used to retard the action of the normal
bacterial flora present in milk, and thus the period for souring is extended. Solutions may be
rendered non-pyrogenic by heating with hydrogen peroxide.
45. C. Both are true. (ref. Block pp 314)
 See #44
46. B. I and II – (ref. Block pp 315)
 It is a mixture of zinc peroxide, zinc carbonate, and zinc hydroxide. It contains about 55% of
ZnO2, and will yield about 9% by weight of oxygen.
47. D. II and III – (ref. Block pp 315)
 Zinc peroxide USP slowly hydrolyses in water producing ZINC OXIDE and HYDROGEN PEROXIDE.
This reaction is responsible for its antibacterial action, in that the hydrogen peroxide under the
influence of catalase will release oxygen at the site of infection, and the remaining zinc oxide will
exert an astringent action.
 USES: used as antibacterial and mild astringent in the treatment of infections in various types of
wounds. Its effectiveness is greatest on anaerobic organisms, and those having a strict restriction
Pharmaceutical Chemistry 1 (Lecture)

in their metabolic oxygen requirements. Certain aerobic (haemolytic streptococci) are also
susceptible to the action of this compound. It has also been found used in oral infections
(Vincent’s stomatitis)
48. C. It is effective against Vincent’s stomatitis – (ref. Block pp 315)
 See #47
49. E. I, II and III – (ref. Block pp 315 and Rogers pp 58)
 Other peroxides in current use include: Sodium peroxide, Sodium carbonate peroxide, Sodium
pyrophosphate peroxide, Magnesium peroxide, Calcium peroxide, Barium peroxide, and Zinc
peroxide.
50. A. I only – (Ref. Block pp 316 and Remington pp 1651)
 Monohydrate exhibits greater heat and moisture stability and greater solubility in water.
 Hydrogen peroxide is a germicide active. It is the substance released by the activated neutrophils,
and it is an effective microbicide when applied in close contact with most microorganisms.
However, the enzyme catalase often destroys it before it reaches organisms in wounds.
Effervescence helps cleanse wounds mechanically.
 Iodine is active against bacteria, fungi, spores, yeasts, protozoa and viruses. The advantage of
iodophores or concentrates is that they provide a reservoir (called available iodine) from which to
replenish iodine that is depleted in combining with microbial components and organic materials
resulting in a sustained action. Iodine can complex loosely and heterocyclic groups in tissues
constituents that serve as repository iodine. Most bacteria are killed within 10 seconds by 1%
solution. A 0.15% solution may kill wet bacterial spores, amebic cyst, and enteric viruses in about
15 minutes, but dry spores may require hours. On the skin, a 1% tincture will kill 90% of the
bacteria in 90 seconds.
51. D. II and III – (ref. Block pp 316)
 Sodium perborate undergoes slow hydrolysis in aqueous solution to provide SODIUM
METABORATE and HYDROGEN PEROXIDE. The basic nature of the solution is due to the formation
of SODIUM HYDROXIDE from the hydrolysis of the sodium metaborate. The hydrogen peroxide
formed would be unstable at high pH produced by the hydroxide ions. Therefore, solutions
should be freshly prepared at the time of use.
52. E. I, II and III – (ref, Block 316)
 It is used as an antiseptic. It is present in preparation used in the treatment of oral infections. It is
also used in powdered or “dry” dentrifice preparations. The disadvantage of this type of use is
that the hydrolysis products of the dentrifice lodged between the teeth will produce sodium
hydroxide and local corrosion of enamel or gum tissue. Sodium perborate is also used as a
bleaching agent in nonchlorine laundry bleaches.
53. B. It is oxidized in the presence of HCl and H2S. – (ref. Roger’s pp 286 - 287 and Block pp 317)
 Potassium permanganate is a very strong oxidizing agent. The USP makes the following
statement: “CAUTION: Observe great care should be exercised in handling it, as dangerous
explosions are liable to occur if it comes in contact with organic or other readily oxidizable
material (Cork, charcoal) either in solution or dry state” but especially in a dry state. When mixed
with glycerine, a fire is produced.
 The chemical properties are due to the presence of the PERMANGANATE IONS which react as a
strong oxidizing agent toward many easily oxidizable compounds. Acid solutions (with HCl and
H2S – Reducing agents) of potassium permanganate react to reduce the PERMANGANATE ION,
MnO4 – (Mn+7) to the MANGANOUS ION (Mn+2) with the evolution of oxygen (eq-1). Neutral or
alkaline solutions produce similar reaction with the characteristic brown precipitate of
MANGANESE DIOXIDE (MnO2) (eq-2). The latter reaction is of therapeutic importance since
potassium permanganate is usually applied to the skin as a neutral aqueous solution.
eq-1: 2 KMnO4 + 3 H2SO4  K2SO4 + 2 MnSO4 + 3H2O + 5[O]
eq-2: 2 KMnO4 + H2O  2 MnO2 (brown ppt.) + 2 KOH + 3[O]
 On heating potassium permanganate at 240 °C, it decomposes into very pure oxygen, potassium
manganite (black powdery residue), and manganese dioxide.
2 KMnO4  K2MnO4 + MnO2 + O2 (evolution)
Pharmaceutical Chemistry 1 (Lecture)

 Reducing agents that are oxidized by permanganate ions include hypophosphites, iodides,
bromide, chlorides, ferrous salts, nitrites, sulphites, thiosulfates, peroxides, oxalates, sulfides, and
arsenites. Organic materials such as ethyl alchohol and charcoal generally are readily oxidized.
 pH affects the oxidation reaction of potassium permanganate. In acid solution IODIDES are
oxidized to molecular IODINE. In neutral or alkaline solution, IODIDES are oxidized to IODATES.
 Potassium permanganate oxidizes FERROUS salts to FERRIC salts in acid solution, NITRRITES to
NITRATES (in acid solution), and SULFIDES to FREE SULFUR (in acid solution, sulfuric acid is
formed from sulfur dioxide).
 The antibacterial action of potassium permanganate is dependent upon its oxidation of protein
or other bioorganic substances. The oxygen released is the effective agent. The MANGANESE
DIOXIDE formed leaves a BROWN COLOR on the skin and tissues.
54. D. A and B – (ref. Block pp 317 and Roger’s pp 286)
 See #53
55. D. Both are false – (ref. Block pp 317 and Roger’s pp 287)
 See #53
56. A. I only – (ref. Roger’s pp 287)
 See #53
57. A. Manganese Dioxide – (ref. Block pp 318)
 See #53
58. E. I, II and III (ref. Block 318 and Roger’s 289)
 LIMITATIONS AND DISADVANTAGES:
o Short duration of action
o Low penetrating power
o Skin staining
o Limited to the skin and surface of mucous membrane
59. E. All of the above
 PHARMACOLOGICAL ACTION AND USES: Permanganate ions function most exclusively as
OXIDIZING AGENT and are perhaps the best ones used in therapy. Internally in mild
concentrations there is no noticeable effect except that of oxidation which has been utilized as
for intestinal antisepsis (worthless) and in certain types of poisoning due to phosphorus,
oxalates, and alkaloids, etc.
o Solutions are used externally in concentration ranging from 1:5000 to 1:15,000 (0.2% to
about 0.006%); however, solution up to 1% may be employed in certain types. 1:5000
solutions are considered being the strongest non-irritating strength. The susceptibility of
bacteria is variable.
o Potassium permanganate solutions are primarily used today for skin infections (dermatitis)
caused by bacteria and fungi, and for poisoning produced by plants (poison ivy) and animal
toxins (snake bites). Wet dressings prepared from 1:10,000 solution have been used in the
treatment of vesicular (the presence of small blisters or raised areas containing fluid) stage of
eczema. Similar dressings have been used in severe poison ivy. Solutions of similar strength
have been used in the treatment of the vesicular stage of athlete’s foot (Tinea pedis) and
fungal infections on other portions of the body, e.g., groin (Tinea cruris). It also finds some
use in Vincent’s infection.
60. B. Sodium Hypochlorite Solution – (ref. Block 318)
 DAKIN’S SOLUTION – Sodium hypochlorote solution NF
 MODIFIED DAKIN’S SOLUTION – Diluted Sodium Hypochlorite Solution
61. B. Sodium Hypochlorite Solution – (ref. Remington 1653)
 NaClO – component of Antiformin, Dakin’s Solution, and Hyclorite.
62. A. Modified Dakin’s Solution – (ref. Block 319)
 The solution is prepared by diluting Sodium Hypochlorite Solution with FIVE TIMES the quantity
of purified water, and adjusting the pH with 5% solution of Sodium Bicarbonate until no color is
produced with phenolphthalein. This gives a pH of 8.3 or less. Due to the reduced concentration
and pH, it is the only hypochlorite preparation officially recognized for local application to tissues
as antibacterial.
63. B. First is false. Second is true. – (ref. Block pp 319)
Pharmaceutical Chemistry 1 (Lecture)

 Sodium hypochlorite solution is classified as a DISINFECTANT and NOT SUITABLE for application
to wounds. The alkalinity and oxidizing power of this solution is too strong for use on tissues.
 A diluted form of this solution is known as LABARAQUE’S SOLUTION and consists of sodium
hypochlorite solution which has been diluted in equal volume of water. This solution is also used
primarily as a DISINFECTANT.
64. B. I and II – (ref. Block 320)
 Solutions of Sodium Hypochlorite are STRONG OXIDIZING AGENTS and can cause liberation of
free iodine from solutions of potassium iodide.
 The antibacterial properties are due partly to the liberation of CHLORINE, and to the OXIDIZING
action produced by the liberation of oxygen. Sodium hypochlorite solutions are rapidly
inactivated in the presence of tissue and bacterial protein due to the chlorination reaction. The
facility of this action is improved at a pH near 7, which provides higher concentrations of
HYPOCHLOROUS ACID (HOCl). The Hypochlorite salt is more stable under alkaline conditions.
65. B. Sodium Bicarbonate (ref. Block 320)
 In Diluted Sodium Hypochlorite Solution, the pH is reduced by the addition of Sodium
bicarbonate solution. This has the effect of reducing the caustic effect of the highly alkaline
solution on tissues and of increasing the effective concentration of Hypochlorous acid. The
bicarbonate acts to reduce the hydroxide ion concentration forming carbonate ions. The removal
of the hydroxide ions also increases the concentration of Hypochlorous acid relative to
hypochlorite, thereby improving the antibacterial properties of the solution.
eq-1: OCl- + H2O HClO + OH
HCO3 + OH CO3-2 + H2O
66. C. I and III (ref. Roger’s pp 243)
 Warming the hypochlorite solution will result in the formation of SODIUM CHLORATE and
SODIUM CHLORIDE. This property is a characteristic of all hypochlorites.
3 NaClO  2 NaCl + NaClO3
67. C. It is suitable for wound application (ref. Roger’s 243 – 244)
 A solution of Sodium Hypochlorite will form a precipitate if SILVER CHLORIDE with solutions of
silver nitrate.
 Hypochlorites are active germicides and because of its alkalinity, they are able dissolve necrotic
tissues and many bacteria. Hypochlorites can also dissolve blood clots and prolong clotting time.
Furthermore, because their antiseptic action seems to be due to chlorination of bacterial protein
they are somewhat readily INACTIVATED by combination with tissue proteins as well as with
bacterial protein. This solution is not suitable for application to wounds.
68. C. I and III – (ref. Block 321)
 Chlorinated Lime (Bleaching powder, Chloride of Lime) is the product obtained by passing
chlorine gas over slaked lime. Among other materials, it contains calcium hypochlorites, calcium
hydroxide, and chloride ions. It has a distinct odor of chlorine and decomposes to release
Hypochlorous acid. It is used as a DISINFECTANT in swimming pools and ‘STERILE’ rooms, and as
bleaching agent.
69. C. Both and true (ref. Roger’s 244 – 245)
 Sodium hypochlorite is an oxidizing and bleaching agent. It is a useful as a disinfectant.
 Diluted Sodium Hypochlorite has been used as an antiseptic on pus-forming wounds, and as an
irrigation solution for infections inside certain body openings. The solution may also be used as a
foot bath in the prevention of various fungal infections (athlete’s foot).
 The antibacterial effectiveness may be increased by acidifying the solution at the time of use,
thereby further increasing the concentration of HClO.
70. C. I and III (ref. Block 321)
 Chloramines are organic amines with one or two chlorine atoms bonded to the nitrogen. When
these compounds are dissolved in water, they slowly hydrolyze to release HYPOCHLOROUS ACID.
Chloramine products are used as DISINFECTANTS and in the purification of drinking water
supplies. Two products available include: Chloramine-T and Halazone.
71. B. Hypochlorous acid (ref. Block 321)
 When chlorine gas is dissolved in neutral or acidic water, HYPOCHLOROUS ACID is formed.
72. B. I and II (ref. Gisvold’s 185)
Pharmaceutical Chemistry 1 (Lecture)

 Iodine is the most effective and useful of the germicides. Iodine inactivates protein by
IODINATION of AROMATIC residues (phenylalanyl and tyrosyl) and OXIDATION (sulfhydryl
groups).
73. B. First is false. Second is true. (ref. Gisvold’s 185)
 Mixing with several non-ionic and cationic surfactants can solubilize iodine. Complexes formed
that retain the germicidal properties of iodine while reducing volatility and removing its irritant
properties. These active complexes are called IODOPHORES. IODOPHORES are both
BACTERICIDAL and FUNGICIDAL. (example: Povidone- Iodine)
74. B. Lugol’s solution (ref. Gisvold’s 185)
 Lugol’s solution is also known as STRONG IODINE SOLUTION. It is 5% IODINE in water with
POTASSIUM IODIDE.
75. C. Strong Iodine Solution (ref. Gis pp 185)
 See #75
76. D. Both are false. (ref. Gis. pp 185)
 IODINE TINCTURE – 2% Iodine in 50% Alcohol with Sodium Iodide.
 IODINE SOLUTION – 2% Iodine in Water with Sodium Iodide.
77. D. A and C (ref. Block pp 321 – 323)
 Iodide and Triiodide ions are devoid of antibacterial activity, although the latter spontaneously
reverts to I2 and I-, thus retaining the antibacterial activity.
 The oxidizing activity of iodine is due to the formation of HYPOIODOUS ACID, HIO. Preparations
providing iodine are bactericidal, fungicidal, amebicidal, and virucidal.
 The most notable chemical property of iodine in aqueous solution is that of a mild oxidizing
agent. Although less reactive than chlorine in this respect, it is believed that the oxidizing action
is mediated through the formation of hypoiodous acid.
78. A. (ref. Block 322 – 323)
 Strong oxidizing agents such as potassium chlorate (KClO3) / perchlorate (KClO4) will oxidize
IODINE to IODATE. This demonstrates a possible caution against mixing iodine with other
oxidizing antibacterial.
 Iodine oxidizes IRON to form FERROUS IODIDE. For this reason METAL SPATULAS SHOULD NOT be
used to handle iodine and balance pans should be protected against pitting by using weighing
papers.
79. C. I and III (ref. Block 323)
 See #71
80. B. I and III (ref. Block 323)
 Iodine is a very active element and is, therefore, easily inactivated by organic materials in the
gastrointestinal tract. Very little free iodine is absorbed. Most of the toxicity due to the ingestion
of large quantities is the result of the corrosive action of the element on the gastrointestinal
tract, producing abdominal pain, gastroenteritis, and possible bloody diarrhea. The treatment
usually involves gastric lavage with soluble starch solution, or administration of a 5% sodium
thiosulfate solution. The starch solution forms a complex with iodine (purple color), thus aiding in
the removal from the GIT.
81. B. (ref. Block pp 324)
82. B. (ref. Block 324)
 USES: Iodine Tincture and Iodine Solution have been used as antiseptics on the skin prior to
surgery. There is some indication that Iodine Tincture is more suitable for this purpose, since the
alcohol seems to improve the penetration of the iodine due to a “WETTING” or spreading effect, as
well as providing some additional antibacterial effect.
 Iodine Solution is preferred for application to wounds and abrasions because the alcohol in the
Tincture is very irritating to open tissue and is the entire reason for the stinging effect when this
solution is applied to wounds. The official solution and tincture are effective against bacterial and
fungal infection of the skin.
 Iodine Tincture may be used to disinfect drinking water. Treatment of suspected water supplies
with three drops per quart will kill amebae and bacteria in 15 minutes.
 Iodine preparations of any type are CONTRAINDICATED in patients with prior allergy or
hypersensitivity to iodine.
Pharmaceutical Chemistry 1 (Lecture)

83. E. (ref. Gis. pp 185)

 Povidone –Iodine (Betadine, Polyvinylpyrrolidone-Iodine) is a charge-transfer complex of iodine
with non-ionic surfactant PVP. The complex is extremely water-soluble and releases iodine VERY
SLOWLY. Hence, the preparation provides NON-TOXIC, NON-VOLATILE, and NON-STAINING form
of Iodine that is NOT IRRITATING to the skin or to the wounds.
84. A. (ref. Remington 1652)
 PVP serves as a solubilizing agent aiding in the SLOW release of Iodine. The affinity of Povidone
for Iodine is greater than that of Iodide, so that the concentration of free iodine is less than 1
ppm.
 It KILLS both GRAM-POSITIVE and GRAM-NEGATIVE bacteria, fungi, viruses, protozoa, and yeasts.
However, the preparation is not as effective as the aqueous or alcoholic solution of the
elemental iodine. Although it takes 6 to 8 hours for the skin bacterial population to return to
normal, the effective duration of action for surgical purposes is only about 1 hour.
 USES: Its antiseptic preparations are indicated clinically for the prevention and treatment of
surface infections as well as to degerm the skin prior to injection and hyperalimentation
procedures; for seborrhea; for disinfection of wounds, burns, lacerations, and abrasions; for
preoperative and postoperative scrubbing and washing of hospital operating room personnel ad
for preoperative skin preparation of patients.
 Other Iodophors: Undecoylium chloride (a quaternary ammonium compound) – topical skin
antiseptic.
85. C. (ref. Remington pp 1310 and Block pp 327)
 Silver nitrate is easily reduced to metallic silver to form a silver mirror on available surfaces.
Reducing agents include ferrous salts, Arsenites, Hypophosphites, Tartrates, Sugars, Tannins,
Volatile oils, Formaldehyde, Eugenol, and other organic substances.
 Silver salts are unstable to exposure to light either in the solid of in solution. LIGHT will catalyze
the REDCUTION of silver ions to FREE SILVER. This photoreduction is responsible for the
production of stains when solutions of silver compounds are spilled on the skin or clothing.
 Silver ions form complex with protein molecules and cause DENATURATION and PRECIPITATION.
As a result, Silver ions have ASTRINGENT, CAUSTIC, BACTERICIDAL, and ANTIVIRAL properties.
Silver ions precipitation of proteins involves interactions between the cations and various polar
groups in the protein molecule, e.g., -SH, -NH2, -COOH, and heterocyclic residues (Histidine).
 When applied to tissue in concentration of 0.1% Ag+, the activity is rapidly bactericidal. In low
concentrations, silver-denatured protein is confined to the interstitial spaces and the surface of
denuded, weeping areas, so that only astringent and antimicrobial effects occur; with higher
concentrations, cell membranes are disrupted and caustic effects result. The corroded sites will
become covered with a scab of silver-protein precipitate. The bactericidal effect continues after
the initial application due to slow production of silver ions form silver proteinate and silver chloride.
This sustained action at the tissue level has given rise to colloidal products of silver proteinate
and halides as antibacterials.
86. E. (ref. Remington pp 1310)
 In neutral or alkaline and in acidic condition, Silver Nitrate precipitates Chlorides (AgCl – White),
Bromides (AgBr – Cream), and Iodides (AgI – Yellow) which are insoluble in HNO3. Ammonia
Water dissolves many insoluble silver salts through the formation of SILVER DIAMINE COMPLEX,
Ag(NH3)2+, or SOLUBLE DIAMINO SILVER(I) HYDROXIDE.
87. E. (ref. Remington pp 1310)
 See #85
88. A. (ref. Block 327)
 Olygodynamic action means, that it is active in small quantities.
 Silver preparations are bacteriostatic at concentrations below that required for protein
precipitation. This concentration effect is found in many heavy metals and indicates some
interactions of metals with bacterial enzymes. Solution of silver nitrate is bacteriostatic at
concentration of 1:30,000 and bactericidal at 1:4,000 in the presence of organic matter. Irritation
of the skin becomes a factor at concentration above 1:1000. Colloidal silver preparations remain
bacteriostatic at concentrations of 1:20,000 but require concentrations of about 10% to be
bactericidal.
Pharmaceutical Chemistry 1 (Lecture)

89. D. (ref Remington pp 1310)

 USES: Silver Nitrate is the most widely use soluble silver salt. it is employed as an antibacterial is
solutions ranging in concentrations from 0.1 to 10% recognizing that higher concentrations
present astringent and irritant properties to the tissues. Concentrations of 1:10,000 has been
used on sensitive membranes, e.g., irrigation of urethra and bladder, but has been largely
replaced by the use of colloidal forms of silver. 10% concentration of AgNO3 has been used in
the treatment of infected ulcers in the mouth. In podiatry (branch of medicine that deals with the
diagnosis and treatment of conditions affecting the foot, ankle and related structures of the leg), it
is used as a caustic to destroy excessive granulation tissue, such as corns (aka HELOMA –
thickened skin that is inflamed and painful), calluses, granuloma pyogenicum (aka. Eruprtive
granuloma/ pregnancy tumor – a benign vascular lesion of mucosa and skin), and plantar warts;
reduce neurovascular helomas; remove papillomas; and cauterize small nerve endings and blood
vessels. As an astringent, it is used to treat impetigo vulgaris (a contagious superficial pyoderma
(pu-forming), caused by Staphylococcus aureus and/or group A streptococci (S. pyogenes), which
begins with a superficial flaccid vesicle that ruptures and forms a yellowish crust) and pruritus as
well as indolent ulcers, wounds, and fissures. It is also used as a STYPTIC, especially in dentistry.
 SILVER NITRATE OPHTHALMIC SOLUTION USP
o 1% solution for installation into eyes of newborn babies. Silver nitrates are quite effective
against GONOCOCCAL organisms, and two drops of this solution are placed in each eye as
PROPHYLACTIC measure against OPHTHALMIA NEONATORIUM (aka. Neonatal conjunctivitis;
Causative agents: Staphylococcus aureus, E.coli, P. aeruginosa, Chlamydia trachomatis, and
Neisseria gonorrhoeae).
o The solution is buffered using Sodium acetate to maintain the pH at 4.5 to 6.0.
 The most important us of silver nitrate is the application of 0.5% aqueous solutions in the form
of wet dressing on burned areas of patient suffering from 3Rd degree burns. This involves the
mechanism of sustained action due to the precipitation with protein tissues and chloride ions.
Silver ions have high efficacy against Staphylococcus aureus, various species of Proteus, and
Pseudomonas aeruginosa. 0.5% Silver Nitrate may be recommended as a good INITITAL
treatment; however, it should be alternated with other agents.
 ADE:
o Precipitation of AgCl at the site of application and in dressing depletes plasma chloride and
can cause serious electrolyte disturbances. Electrolyte imbalances may causes low sodium,
metabolic acidosis, and diarrhea.
o Excessive corrosion at the target site and corrosion form inadvertent application or leakage
away from the intended site can also occur.
o Dental cones and pieces of toughened silver nitrate that are accidentally ingested can cause
death.
o Elemental silver form the bioreduction of silver ion may reside permanently at the site of
application and cause a bluish-to-black discoloration called ARGYRIA. Locally injected Sodium
Thiosulfate sometimes can remove the silver.
o Nitrate ion absorbed from large, denuded surfaces can cause METHEMOGLOBINEMIA. Only
concentrations 0.5% or below should be applied to raw wounds, fresh cuts, or broken skin.
 OTHER SOLUBLE SILVER SALTS:
o Silver Lactate: Silver Lactic acid-Allantoin complex (0.9% Silver) has been recommended as an
alternative to silver nitrate in the treatment of third-degree burns.
o Silver Picrate: (Silver Trinitrophenolate) combined antibacterial effect of silver and picrate ion.
It has been used in the form of vaginal suppositories for the treatment of Trichomonas
vaginalis and Monilia albicans. It also causes argyria, and the picric acid causes NEPHRITIS.
90. B. I and II (ref. Remington pp 1310)
 See #89
91. E. (ref. Block 328)
 See #89
92. B. (ref. Block pp 328)
 See #89
93. D. (ref. Block pp 329)
Pharmaceutical Chemistry 1 (Lecture)

 Mild Silver Protein NF is silver rendered colloidal by the presence of, or combination with protein.
It contains a very little free silver ion reducing the tissue effects seen in silver nitrate
preparations. Colloidal solutions of this product have NO ASTRINGENT or IRRITANT effects,
allowing them to be applied to sensitive areas and mucous membranes. This low level of tissue
activity implies that the silver is not readily precipitated by chloride or tissue proteins, indicating
GREATER ability to penetrate tissues than solutions containing silver ions.
94. E. (ref. Block 329)
 The release of ionized silver tend to INCREASE with dilution – the more dilute the solutions can
be more irritating, and irritation can be decreased with increasing concentration of silver protein.
 Silver protein solutions are subject to the same slow ionization of silver. For this reason the NF
makes the following statement: “Caution: Solutions of Mild Silver Protein should be freshly
prepared or contain a suitable stabilizer.”
 As solutions age, they tend to increase in irritating properties, and a precipitate forms. Calcium
Disodium EDTA may be used to stabilize the solutions. It acts by chelating the silver ions released,
thereby preventing the physical breakdown of the colloidal solution, and maintaining the low
irritant effect or action of the product.
95. B. (ref. Block 330)
 The concentrations of Mild Silver Protein usually employed provide BACTERIOSTATIC action. Due
to their low irritability, these are used as local antibacterials on mucous membranes in the nose,
throat, and conjunctive of the eye.
 Strong Silver Protein (Protargin) contains LESS silver than Mild Silver Protein but the protein is
partially hydrolyzed, providing a higher concentration of silver ion. The product is MORE irritating
than Mild Silver Protein. Its action is MORE BACTERICIDAL and it was used for irrigation of urethra
and bladder in the treatment of gonorrhoea just prior to the introduction of sulphonamides and
antibiotics.
 OTHER COLLOIDAL SILVER PREPARATIONS
o Colloidal Silver Iodide – AgI with gelatin; should be freshly prepared and protected from light;
same uses as Mild Silver Nitrate
o Silver Chloride – rendered colloidal with sucrose as stabilizing agent; non-irritating
96. E. (ref. Block 330)
 See the USES on page 330
97. E. (ref. Block 330 -331)
 The stain is due to the deposition of free silver.
98. A. (ref. Block 333)
 When metallic Mercury is heated in air to temperature near its boiling point, it combines with
oxygen to form RED MERCURIC OXIDE. (see Post Lab Discussion – Difference between Yellow and
Red Mercuric Oxide)The difference in COLOR is attributed to the DIFFERENCE in PARTICLES
o RED HgO  COARSE PARTICLES
o YELLOW HgO  FINER PARTICLES
 Mercury compounds exhibit destructive effect on metal, hence, the NF makes the following
statement, “Caution: During its manufacture and storage, Yellow Mercuric Oxide Ophthalmic
Ointment must NOT come in contact with metallic utensils or containers except those made of
stainless steel, tin, or tin-coated materials.” This is to avoid the development of FREE MERCURY
and small metallic particles that may be damaging to the eyes. The OINTMENT is used in the
treatment of mild infections and inflammations of the eye, fungal infections on the skin, and
infestations of body lice.
99. C. (ref. Block 331 – 322) – See Post Lab Discussion for the chemical and Physical properties of
Mercury compounds
100. E. (ref. Block 333)
 Mercuric ions are PROTEIN PRECIPITANTS. They act by binding with polar groups, particularly –SH
groups, present in protein molecules. This is the basis for treating mercury poisoning with
DIMERCAPROL or PENICILLAMINE. This reaction with sulfhydryl groups leads to the formation of
mercaptides.
 The antimicrobial activity of mercurials is best described as BACTERIOSTATIC.
101. E. (ref. Block 333 – 334)
Pharmaceutical Chemistry 1 (Lecture)

102. A. (ref. Block 335)

 Ammoniated Mercury is known as WHITE PRECIPITATE
 Mercuric Chloride is irritating when applied to the skin and should never be used as an antiseptic
for wounds and abraded skin. Its primary use is in DISINFECTANT SOLUTIONS for utensils and
surgical instruments. However, rubber will deteriorate with constant exposure to the solution.
Addition of NaCl to the solution suppresses the ionization, and therefore seems to diminish the
corrosive effect on metals.
103. E. (ref. Block 337)
 Table 9-1 Allotropic forms of sulfur
o Rhombic
o Monoclinic
o Liquid
o Plastic Sulfur (70% Rhombic; 30% Amorphous)
o Amorphous
104. A. (ref. Block 338)
 In the presence of oxidizing agent and water, SULFURIC ACID is formed. When burned in an
oxygen atmosphere, evolves the suffocating fumes of SULFUR DIOXIDE.
105. A. (ref. Block 338)
 Elemental Sulfur is a weak or a poor antiseptic agent.
 The primary topical uses of Sulfur are as FUNGICIDE, PARASITICIDE, and KERATOLYTIC AGENT
(destruction of the keratin in the skin)
106. A. (ref. Block 335 and 339)
 Sublimed Sulfur – Flowers of Sulfur
o It is obtained by condensing the sulfur vapors produced by heating any form of sulfur.
 Precipitated Sulfur – Milk of Sulfur
 USES:
o Both (Sublimed and Precipitated Sulfur) are used as SCABICIDES (Effective in killing Sarcoptes
scabiei- mites). Sulfur is effective against the live parasites, but it has no effect on eggs.
o Sulfur is used primarily as a dermatological agent in the treatment of seborrhea (abnormal
secretion of sebum from the sebaceous glands giving an oily and scaly appearance to the
skin), acne, psoriasis, etc. In these cases, sulfur is used as a keratolytic agent.
107. C. (ref. Block 340)
 Sulfurated Potash is also known as Liver of Sulfur. It is used in the preparation of WHITE LOTION
NF. It has been used as PARASITICIDE (SCABICIDE), and in the treatment of acne and psoriasis.
108. B. (ref. Block 340 – 341)
 Selenium is toxic in large doses, but it also appears to be an important nutrient in trace
quantities. Selenium may cause:
o Irritation of Gastric mucosa
o the appearance of fat deposits in the liver
o damage in the renal tubules
o damage blood-forming organs (spleen and bone-marrow)
 It has been used as a 2.5% suspension (Selsun) in the treatment of Seborrheic dermatitis
(Dandruff). It can cause contact dermatitis on prolonged contact. Selenium has a CYTOSTATIC
ACTION (reduces cell turnover of epidermal cells around the base of the hair shaft and around
the follicle) in patients with or without dandruff.
 Cadmium Sulfide (Capsebon)
o Cadmium has properties closely related to those of Zinc. The metal is a PROTEIN PRECIPITANT
with toxicity similar to mercury and greater than zinc. It is used in the treatment of dandruff.
It is LESS IRRITATING than Selenium Sulfide.
109. C. (ref. Block 335 and 341)
 Boric Acid
o It has a weak BACTERIOSTATIC AGENT. It is non-irritating when applied to intact skin and
mucous membranes.
o it is used in OPHTHALMIC preparations as a BUFFER and in saturated solution (4.5%) as a
BACTERIOSTATIC EYE WASH.
Pharmaceutical Chemistry 1 (Lecture)

110. B.
111. E. (ref. Block 345 - 346)
 Arsenicals are protoplasmic poisons by virtue of their reaction with sulfhydryl-containing enzymes
to block or destroy important metabolic pathways. In general, there no useful therapeutic action
of topical arsenical. However, continued exposure of the skin to these compounds can produce
necrosis of the tissue and contact dermatitis.
 Inorganic arsenic has been used in the treatment of LEUKEMIA because of its repressive action
on the bone marrow (NO LONGER USED in present-day therapy)
o INORGANIC ARSENIC (Arsenic Trioxide NF – As2O3, Arsenous acid, White Arsenic)
 Organic Arsenicals are virtually the only derivatives presently used for the therapeutic effects of
arsenic. These are employed in the treatment of certain parasitic diseases produced by protozoa
and helminths (worms and worm-like parasites).
o Organic Arsenicals are more selective between hosts and parasitic cells.
o Trivalent arsenicals penetrate the host cells (mammalian cells) to a greater` extent than the
pentavalent arsenicals, therefore, the latter derivatives are less toxic to the patient under
arsenical therapy.
o Parasite selectivity depends on the organisms involved.
 TRIVALENT – are more selective and effective against the Treponema organism that
produces syphilis (Treponema pallidum).
 PENTAVALENT – are more useful as veterinary anthelminthics and in the treatment of
amoebiasis and trypanosomiasis (protozoal infections)
o Carbasone – used in the treatment of amoebiasis; for vaginal use in the treatment of
Trychomonas vaginalis
o Glycobiarsol – Bismuth containing organic arsenical; treatment of intestinal amoebiasis
o Tryparsamide – For the treatment of Trypanosomiasis; has been largely replaced by
TRIVALENT arsenical (MELARSOPROL) which has greater efficacy and lower toxicity.
112. C. (ref. Block 345 – 346)
 Sodium cacodylate – is an INORGANIC ARSENICAL that has been used in the treatment of
psoriasis.
 Stibophen – Antimony containing compound
113. B. (ref. Block 346 – 347)
 Antimony forms TRIVALENT and PENTAVALENT compounds. Compounds containing Antimony are
less readily absorbed and produce more local irritation upon topical application to the skin.
TRIVALENT compounds have specific interactions with –SH-containing enzymes.
 Due to the irritant properties, antimony-containing compounds have been used as emetics.
However, this use, as well as uses as expectorants and nauseants, has been abandoned in
modern therapeutics. The primary use of organoantimony derivatives is in the treatment of
certain helminthic infections (Schistosomiasis and Filariasis) and protozoal infections
(Leishmaniasis).
o PENTAVALENT compounds are more active against PROTOZOAL PATHOGENS.
o TRIVALENT COMPOUNDS are more active against HELMINTHS.
114. C. (Ref. Block 347)
 ANTIMONY POTASSIUM TARTRATE – aka TARTAR EMETIC; DRUG OF CHOICE in infections caused
by Schistosoma japonicum.
 STIBOPHEN – This compound in used in the treatment of SCHISTOSOMIASIS. It is more effective
than Antimony Potassium Tartrate against Schistosomal species haematobium and mansoni, but
LESS effective against S. japonicum.
115. E. (ref. Block 348)
 Astringents are used:
o as STYPTICS – stop bleeding from small cuts by promoting coagulation of blood and
constricting small capillaries
o as ANTIPERSPIRANT – to decrease secretion of perspiration by constricting pores at the
surface of the skin
o Restriction of blood supply to the surface of the mucous membranes as a means of
REDUCING INFLAMMATION
Pharmaceutical Chemistry 1 (Lecture)

o direct actions on the skin to remove unwanted tissues (require higher concentrations)
 ALUMINUM COMPOUNDS (See Post Lab Discussion – Aluminum (Properties, Reactions, and
Compounds)
o Aluminum Chloride – external astringent and antiseptic; was found to be TOO IRRITATING
o Aluminum Hydroxychloride – as an antiperspirant; has replaced the more acidic and irritating
Aluminum chloride
o Aluminum Sulfate – astringent, antiseptic, antiperspirant
o Aluminum Subacetate Solution – astringent; applied as soak or wash or in the form of wet
dressings
o Aluminum Acetate Solution – aka BURROW’S SOLUTION; topical antiseptic and astringent
o Alum (Aluminum Ammonium Sulfate) – Topical astringent; it can be used as footbaths as a
means of toughening the skin. The protein precipitant actions of Alums are also utilized in
the preparation of precipitated diphtheria and tetanus toxoids,
116. B. – See #115)
117. E. (ref. 351 – 352)
 ZINC CHLORIDE – is a very strong protein precipitant, a powerful astringent, and a mild antiseptic
USES:
 Escharotic (agent that causes the sloughing of the tissue, aiding in the formation of scar
tissue to improve healing)
 Densensitizer of dentin
118. E. (Ref. Block 352 – 353)
 ZINC SULFATE – externally used as an ophthalmic astringent (Zinc Sulfate Ophthalmic Solution); it
has also been used internally as an EMETIC (irritation of the gastric mucosa).
 OTHER ZINC COMPOUNDS
o WHITE LOTION – prepared by the addition of Sulfurated Potash solution slowly to a solution
of Zinc Sulfate; It is used topically for the effects of SULFIDE IONS and the astringent action of
ZINC ions. It has been used in the treatment of acne vulgaris, seborrhea dermatitis, and other
dermatological problems.
 TOUGHENED SILVER NITRATE – See BLOCK pp 353 for discussion