Subject: Pharm Chem -1 LEC (Chemistry & Pharmacy of Inorganic Medicinals)

Year& Section: Pre-Final Lecture for BS PH- 3A, 3B, 3C, 3D & 3E Revised: 082015
Schedule: 3A = 7-8 am, MWF; 3C = 8-9 Am, TThS ; 3E = 11:00-12:00 Noon MWF
3B = 7-8am, TThS; 3D = 9-10 Am TThS

Unit VII. TOPICAL AGENTS

They are those used on body surfaces. They are Preparations for External Used Only.
These Include: 1. Protective Agents 2. Antimicrobials & 3. Astringents

I. PROTECTIVES
These are substances, which may be applied to the skin to protect certain areas from irritation,
usually by mechanical means.
A desirable protective should have the following characteristics:
a. Insolubility property that limits the absorption of the compounds through the skin, makes it
difficult to wash them off and diminish metallic properties on tissues.
b. Chemically Inert this property is necessary in order to prevent the interactions between the
protective substances and the tissue.
Adsorbent action of PROTECTIVES is a necessary action and important since absorption of
moisture on skin surfaces lessens irritation and mechanical friction.
Protective and adsorbent action is maximized with Decreasing Particle Size.
A fine state of subdivision of the particle size also offers a smooth substance, which is
soothing to apply and aids in preventing irritation due to rubbing or friction.
PROTECTIVES are generally applied as Dusting Powders, Suspensions containing the
insoluble protective substance or ointments.
Protective substances are available for use internally for GI irritations but its preparation is
different from that with topical use.
Topical protectives and Adsorbents are usually applied to areas of the skin which are
subject to constant irritation due to moisture and or friction or areas which have already
become irritated or inflamed due to friction, allergy, and the like.
If the area to which the protective is to be applied is abraded and exuding fluid, adsorbent-type
protectives should not be used since these substances will mix with the exudates and dry to a
crust, which adhere to the open tissues.

1. TALC ( 3MgO.4SiO )
Synonyms: French chalk, Soapstone, Piedra grasca, Creta Gallica
*TALC is the softest mineral known. Hardest ???
*The lump form called Steatite is known as SOAPSTONE.
*The most desirable form for cosmetic and pharmaceutical purposes is known as foliated talc and
has a paste-like structure.
*TALC has a very low adsorptive property, which is an important filtration aid without the danger of
removing important constituents.
USES: a. Lubricating, protective dusting powder
b. To prevent irritation due to friction and to protect areas from further irritation
c. Preparations, which may be perfumed for cosmetic purposes or medicated with
antimicrobial agents such as boric acid
*When talc is used on broken skin wounds and surgical incisions, it can produce
sterile abscesses or granulomas ( a nodule of inflamed tissue in which granulation is
occuring)

2. ZINC OXIDE (ZnO)

Synonyms: Zinc white, Flores de Zinc, Lana or Algodon Filosoficos
*Zinc oxide occurs as calamine, willemite, smithsonite, franklinite, or zincite
USES: a. It is used as an astringent and protective
b. It is used as a protective in ointments, pastes, and dusting powders in the treatment of skin
ulceration and other dermatological problems.
c. It is found in combination with other protectives and antimicrobial agents.
 3. CALAMINE, USP.
Calamine USP is a zinc oxide with a small proportion of ferric oxide.
The presence of ferric oxide gives the substance a pink color, which varies according to the
method of preparation and the amount of ferric oxide present.
USES: a. It is used in dusting powders, ointments and lotions where it is applied to the skin
for its soothing, adsorbent, protective properties.
b. Dermatological problems particularly those involving the exudation of fluids, respond
reasonably well to the application of products containing calamine.
c. Calamine Lotion is a protective with a good drying effect and a mild astringent
action.
d. Phenolated Calamine Lotion contains 1% liquefied phenol, which provides a
local anesthetic and antipruritic action.

4. ZINC STEARATE
USES: a. It is mild astringent and antimicrobial properties,
b. It is employed in dusting powders and ointments as a protective.
c. It is used as a lubricant in manufacture of tablets.
It is not wetted by moisture. This property makes the material more desirable in dermatological
problems where large amounts of fluids are exuded, because it will not form crusty patches over
the areas being treated.
The inhalation of zinc stearate dust can cause pulmonary inflammation. It is for this reason
that its routing use as dusting powder for infants and children should be strongly discouraged.

5. TITANIUM DIOXIDE A Solar Ray Protectant; Opacifying Agent.

USES: a. It is used as a topical protective.
b. It is used as solar ray protective. ( SUN BLOCK ).
c. It is used as a white pigment in cosmetics and paints.
It is primarily used for its opacity due to its high refractive index. The high refractivity makes
the compound useful for screening our ultraviolet radiation, thus the presence of titanium
dioxide in various sun creams and sunscreen products.

SILICON POLYMERS
SIMETHICONE or DIMETHICONE is 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.
Silicon oils adhere very well to the skin and exclude contact with the air. It is for this reason that
they should not be applied over broken or abraded skin or wounds requiring drainage. Contact with
eyes should also be avoided.
Its primary use is as a prophylactic against chemical irritants.

II. ANTIMICROBIALS AND III. ASTRINGENTS

MECHANISMS OF ACTION OF ANTIMICROBIAL AGENTS

A. OXIDATION
These compounds are generally non-metals and certain types of anion. These include
hydrogen peroxide, metal peroxides, the permanganates, halogens, and certain oxohalogen
anions. The effective oxidative action of these compounds involves the reducing groups present in
most proteins (sulfhydryl groups). The overall change or destruction of function in specific proteins
is responsible for the ultimate destruction of the microorganism. The chemical result of oxidizing the
protein is reduction of the antimicrobial agent.

B. HALOGENATION
This is a reaction occurring with antiseptics of the hypohalite type and in particular,
hypochlorite, OCI. The reaction is ultimately destruction to the function of specific proteins because
the substitution of the chlorine atom for the hydrogen produces changes in the bonding responsible
for the proper confirmation of the protein molecule
C.PROTEIN PRECIPITATION
This type of mechanism involves the interaction of proteins with metallic ions having large
charge/radius ratio or strong electrostatic fields. This property is available in transition metal cation.
Most metal cations, with the exception of the alkali and alkaline earth metals, will demonstrate protein
precipitant activity.
The nature of the interaction is one of the complexation in which the various polar groups on
the protein act as ligands. The complexation of the metal results in the radical change in the
properties of the protein or protein precipitant.

ASTRINGENT
The application of very dilute solution of a metal cation to tissue primarily provides a local
surface protein precipitant action.
This activity is usually designated as being astringent.
Its effect can be observed or felt when applied to skin or mucous membrane.
This effect can be generally described as shrinkage or firming of tissues.

Control of Antimicrobial/Astringent Action

In the case of water soluble compounds control of activity is accompanied by making solutions
of the appropriate concentration for the desired use.
Soluble compounds may be controlled by placing them in vehicle, which will slow their release
to the site action.
Complexation with a ligand also provides a controlled release of some of these agents,
minimizing toxicity and activity at host cells.
Other compounds may be synthesized into an insoluble form and used in suspensions,
ointments, or creams for their antimicrobial action because of active agent.

1. HYDROGEN PEROXIDE (HO) Synonyms: Aqua oxigenada; Aqua oxinada

This agent easily undergoes decomposition and therefore ways have been developed to
render it more stable.
It should be kept in a cool place protected from light and dust.
Amber-colored bottles are used as containers
Preservatives such as acetanilide are added.
It may be stabilized with any organic and inorganic acids, complexing agents, or
adsorbents.

USE(s):
a. the agent is used primarily as a mild oxidizing antiseptic. This action is produced
when the solution comes in contact with open or abraded tissue, exposing the chemical
to the enzyme catalase.
b. Hydrogen peroxide in 20 volumes is used as a hair and fabric bleach.
c. It is also used undiluted for its antiseptic and cleansing effects on wounds.
d. When diluted with 1 part of water, it can be used as a mouthwash or gargle in the
treatment of bacterial infections of the throat and mouth.
e. Half-strength may be used as vaginal douche.

2. POTASSIUM PERMANGANATE (KMnO)

Synonym: Mineral Chameleon
This is a strong oxidizing agent both in the dry state and in solution.
The Caution should appear: Observe great care in handling potassium permanganate as
dangerous explosions may occur if brought in contact with organic or other readily oxidizable
substances, either in solution or in dry state.
The compound in the dry state forms explosive mixtures with such materials as charcoal and
will produce fire when mixed with glycerin. It will also oxidize alcohol.
Its antimicrobial action is dependent upon its oxidation of protein or other bioorganic
substances in neutral media. The oxygen released is the effective agent. The manganese
dioxide formed as the permanganate is reduced leaves a brown stain on the skin and tissue.

USE(s): (KMnO)
 a. It is used for both their antibacterial and antifungal actions.
b. Today, it is used for the skin infection (dermatitis) caused by bacteria and fungi.
c. It is used for poisoning produced by plant and animal toxins.
d. Wet dressings prepared from a 1:10,000 solution have been used in the treatment of
vesicular (presence of small blisters or raised areas containing fluid) stage of eczema,
athlete's foot and fungal infections on other portions of the body.

3. SODIUM HYPOCHLORITE SOLUTION (NaOCl)

Synonyms: Dakin's solution; chlorinated soda solution
USE(s):
a. it is used as a disinfectant and laundry bleach.
b. it is an effective germicidal agent that can be used to disinfect areas, instrument, and
utensils, which have been exposed to pathogenic organisms.

4. DILUTED SODIUM HYPOCHLORITE SOLUTION

USE(s):
a. This agent has been used in the past as an antiseptic on Pus-forming Wounds and as
irrigation solution for infections inside certain body openings.
b. Its solution may be used as a footbath in prevention of various Fungal Infections.

Other Chlorine-Containing Compounds

5. CHLORINATED LIME
Synonyms: Bleaching powder; Chloride of Lime
Chemically, it is known as Calcium Chloride Hypochlorite.
It is used as a disinfectant in swimming pools and sterile rooms and as a bleaching agent.

6. CHLORAMINES
These are organic amines used as a disinfectant and in the purification of drinking
water supplies.
The antimicrobial action of chlorinated compounds is that when chlorine gas is
dissolved in neutral or acidic water, Hypochlorous Acid is formed. This is the basis of
using chlorine as disinfectant in swimming pools and water supplies. The antimicrobial
action is due to the presence of HOCl.

7. IODINE Synonyms: Iodinum; Jodum

The most notable chemical property of iodine in aqueous solution is that of a mild
oxidizing agent.
Iodine will oxidize iron to form ferrous iodide.
Iodine is a very active element and is easily activated by organic materials in the GI
tract.
Most of the toxicity due to the ingestion of large quantities of iodine is a result of the
corrosive action of the element in the GI tract, producing abdominal pains,
gastroenteritis, and possibly bloody diarrhea.
The treatment usually involves gastric lavage with a soluble starch solution or
administration of a 5% sodium thiosulfate solution. The starch forms a complex with the
iodine, thus aiding in its removal from the starch.

USE(s):
a. iodine tincture and iodine solution are used as antiseptics on skin prior to surgery. These
are also used as antibacterial and antifungal agents.
b. iodine tincture may be used to disinfect drinking water.
c. when diluted, these solutions may be applied to wounds.

Povidone Iodine is a complex of iodine with Povidone which is a polymer also known as
polyvinylpyrrolidone.
Povidone-iodine is a member of a class of compounds referred to as Iodophors.
Iodophors are complexes of iodine with carrier organic molecules serving as a solubilizing
agent.

USE(s): This has the same uses as Iodine solution and tincture. However, the preparations
 have not been shown to be as effective as aqueous or alcoholic solutions of element iodine.
Povidone iodine has been used in gargles and mouthwashes for the treatment of infections in
the oral cavity (Vincent's Angina).

8. SILNER NITRATE
Synonyms: Azotaz Argenticus; Cristales Lunares
extended use of silver preparations is likely to causes darkening of the skin due to the
deposition of free silver below the epidermis. This condition is known as argyria.
It is employed as an antimicrobial agent in solutions.
Silver nitrate ophthalmic solution is a 1% solution for instillation into the eyes of newborn
babies.
Silver salts are effective against gonococcol organisms and two drops in each eye is a
prophylactic measure against infections produced by gonococcal organisms.
The most recent important use for silver nitrate is the application of 0.5% aqueous solution in
the form of wet dressing on burned areas of patients suffering from third degree burns.
Silver ion is effective in reducing infection due to staphylococcus aureus, various species of
Proteus, and Pseudomonas aeruginosa.
The common side effects associated with this treatment involves electrolyte imbalance due to
precipitation of chloride.

* Toughened silver nitrate (lunar caustic, silver nitrate) is used as escharotic and germicide especially
for small septic wounds and ulcers. ( Ph 3C )

9. AMMONIATED MERCURY Synonym: White Precipitate

The antiseptic action of mercury on microorganisms and body tissues is due primarily to the
mercuric ion, which will react with many polar groups on the amino acids of proteins but has a
particular affinity for sulfhydryl(-SH) groups.
The inhibition of bacterial sulfhydryl containing enzymes by the metal ions leads to an
inhibition in metabolic growth and function
Use(s): a, It is used as a local anti-infective : topically, as a 5% ointment to skin or as a 3%
ophthalmic ointment to conjunctiva.

10.a SUBLIMED SULFUR Synonyms: Flower of sulfur; azufre

10.b.PRECIPATED SULFUR Synonyms: Milk of sulfur

Both forms of sulfur are categorized as scabicides.

Precipated sulfur is used in sulfur ointment
Sulfur is used primarily as a dermatological agent in the treatment of seborrhea (an abnormal
secretion of sebum from the sebaceous glands, giving an oily or scaly apperance to the skin),
acne, psoriasis, etc.
It is used for its keratolytic property.

c. SULFURATED POTASH Synonym: Liver of sulfur

Use(s): This is an official agent as a pharmaceutical aid as a source of sulfide. It is used
in the preparation of white lotion. It is used as a parasiticide and in the treatment of acne
and psoriasis.

11.SELENIUM SULFIDE Synonym: Selenium disulfide

Use: it is used as an anti-seborrheic agent.

12. ANTIMONY POTASSIUM TARTRATE Synonym: Tartar emetic

Use(s): this compound was formerly used as an emetic and expectorant. Its official category
and only rational use is a treatment of schistosomiasis. It is still the drug of choice in infections
produced by Schistosoma japonicum but better agents are available for other species.
ASTRINGENT t are protein precipitants of limited penetrative power. Some of the uses for
astringent compounds:

a. STYPTIC to stop bleeding from small cuts by promoting coagulation of blood and
construction of small capillaries.
b. ANTIPERSPIRANT - to decrease secretion of perspiration by constricting pores at the
surface of the skin.
c. Restriction of the supply of blood to the surface of mucous membrane as a means of
reducing inflammation.
d. Direct actions on skin to remove unwanted tissue. This requires higher concentration or
a stronger protein precipitant, sometimes termed as CORROSIVE.

1. A L U M Synonyms: Tawas, Ammonium Alum, Potassium Alum

USE(s):
a. Alum serves as a source of aluminum ion, making it useful as a topical astringent.
b. it can be used in foot-bath as a means of toughening the skin and avoid formation of
blisters.
c. it is the active ingredient in styptic pencils, where it is used to stop bleeding from small cuts.
d. the protein precipitant properties of alum are used in the preparation of several biological
products.

2. ALUMINUM CHLORIDE
USE(s):
a. it is used as a local external astringent and mild antiseptic.
b. it is used in aqueous solution in concentration ranging from 10-25%.
c. it was initially used as an astringent but was found to be irritating to sensitive tissues and
also damaged to clothing due in part to the formation of HCl by hydrolysis.

Other Aluminum-Containing Astringent

a. ALUMINUM SULFATE Synonyms: Pickle Alum; Pearl Alum; Papermaker's Alum

b. Aluminum Acetate Solution Synonym: Burrow's Solution

3. ZINC CHLORIDE Synonym: Buffer of Zinc

USE(s):
a. Astringent and dentin desensitizer
b. it is used as an ESCHAROTIC due to the properties of zinc chloride.

4. ZINC SULFATE Synonym: White vitriol

Use: it is used externally as an ophthalmic astringent.