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Topical Agents
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Definition Topical : Place the use of these drugs or compounds on the surface Ex: Antiseptic Systemic: The drugs are absorbed into circulatory system and distributed to various organs or tissues.
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Types of inorganic topical agents
The compounds used topically will be divided into broad categories based on their usual action or uses. There are TWO types: 1- Protective agents. 2- Antimicrobial agents.
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Protective agents Are substances which may be applied to skin to protect certain areas from irritation. Properties of protective agents are insoluble in water ( H2O), and chemically inert ( unreactive), in order to prevent interactions between the protective substance and the tissue. Also, small fine partials(large surface area).
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Classification of protective agents
1- Dusting powders. 2-Suspensions. 3- Ointments
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Talc MgO.4SiO2.H2O Hydrous magnesium silicate, very fine white powder, smoothly, greasy feeling to the touch( soapstone). Talc is characterized as fine powder ( 80/100) mesh particle size, odorless, insoluble in water ,dil HCl, bases.
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Uses of Talc 1- It is useful in lubricating, protective dusting,
Can be prevent any friction. 2-Used for wound & surgical incision because can produce sterile abscesses 3- Used in medical gloves.( plastic disposable) 4- Used in cosmetic may be perfumed Medical Talc by mixing boric acid with talc as antimicrobial agents.
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Zinc Oxide The chemical formula for Zinc oxide is ZnO
Is a very fine, oderless, amorphous , white or fait yellow powdwer, can heated ∙C Zno is insoluble in water, alcohol, but react with dil HCl ZnO + HCl ZnCl2 + H2O
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Uses of Zinc Oxide 1- Is a mild astringent and weak antimicrobial agents. Used as powder, ointments to protect the skin. 2- Dusting powder used in the treatment of skin ulceration & other dermatological problems. Medicated zinc oxide by mixing with boric acid as antimicrobial agents.
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Calamine The formula is ZnO.xFe2O3
Can be synthesized by mixing ZnO with ferric oxide. It is a fine powder, water insoluble, alcohols ,adhering to the skin.
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Uses of Calamine Calamine can be used as topical protective agent.
1- It is USP product used as dust powder, calamine lotion ( applied to skin )pink color. Calamine is applied to the skin for its adsorbent, protective properties, used in dermatological problems.
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The calamine lotion contain ZnO and ferric oxide equally mixed Bentonite magma in the solution of Calcium hydroxide. Phenolated calamine lotion( USP ) contains 1% liquid which provide a local anesthetic and anti- itching action.
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Titanium Dioxide TiO2 as topical protective agent, it is characterized by off white powder color, tasteless, odorless. A 1 to 10 aqueous suspension of the solution is neutral to litmus paper. It is insoluble in water , HCl. HNO3, dil H2SO4. It is soluble in HF, Conc. H2SO4.Also, in H2O2 TiO H2O TiO3 Tritium dioxide Titanium trioxide
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Uses of TiO2 TiO2 is a protective agent, topically, used as Sun screen light ( UV light radiation) due to its highly refractive index. Many pharmaceutical preparation as TiO2 cream, 5, 10, ..25% ointments. Other organic sun screen agent p- amino-benzoic acid ( PABA). TiO2 used in cosmetic and paints.
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Aluminum Aluminum ( Al ) is a silver- white metal as protective agents , highly affinity to O2 forming Al2O3as protective layer. It is insoluble in water, alcohols, and uncreative towards HNO3,H2SO4 It react rapidly with dil HCl HCl + Al AlCl3. 6H2O Aluminum, paste ( ZnO with base ) used for prevent irritation.
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Silicon Polymer There are inert protective substances occurring in liquid form known as Silicon oils; e.g.dimethyl silicon ( Dimethicon,or Simethicone ) CH CH CH3 CH3 Si-O- ( Si - O ) Si - CH3 CH CH CH3 Very well adhere to skin, but not wound, be avoided contact to the eyes.
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Topical Agents 3rd Year Pharmacy
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Outline Classification a- protective b- antimicrobial agents
A- protective products Talc , Zinc oxide ZnO, Calamine, Titinum oxide TiO2, Al products& silicon polymer Antimicrobials Mechanism 1-oxidation H2O2,ZnO,KMnO4, Iodine 2- Halogenations NaOCl 3- protein ppt AgNO3.
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Protective Agents Protective
Any agent that isolates the exposed surface from harmful or annoying stimuli Properties of protective agents: Insoluble in water Chemical Inertness Adsorbent
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Deeper penetration of topical agents are also seen in many cases which are beneficial. (Penetration of antiseptics into the tissue below the skin prevents the possibility of deeper infections)-
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Protective Agents Talc
Talc (Mg3Si4O10(OH)2 protective: native hydrous magnesium silicate, common name and chemical formula. Soapstone can be grinding in 80/100 mesh particle size. As grease touch., insoluble in water, Uses as protective agents , as lubricants and in pharmaceuticals, as cosmetics, ceramics, for plastic cloves,
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Zinc Oxide ( ZnO ) White or fait yellow color powder, insoluble in water. Other formulation as Zinc Oxide ointment for adult, & Zinc Oxide in Glycerin for children. Dusting powder, used astringent and protective topical agent, mild antiseptic, used in the acne preparation, eczema,& psoriasis It is usually used in the manufacture of plasters.
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Calamine ZnO and Fe2O3
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It used as dusting powder, lotions, ointments, as smoothing agents, for sunburn, eczema, urticaria. Calamine lotion is very popular.
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Boric Acid H3BO3 Is a weak acid, used as antiseptic, and as chemical precursor for many reactions. Uses: 1- Antiseptic 2- dilute solution for eye wash 3-Acne 4- Vaginal douche against bacteria. 5-It used as protective against athlete foot.
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Titanium dioxide TiO2 Topical protective agents as cream is used against sunscreen to protect the skin aganist ultra-violet light ( U.V.). The organic topical protective agents is P-aminobenzoic acid ( PABA) .
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Antimicrobial Agents Antiseptic:
Any agent which kills or inhibits the growth of microorganisms found in living tissue. Disinfectant: Any agent which kills or inhibits the growth of microorganisms found in inanimate objects. Germicide: General term for fungicide, bactericide, amoebicide
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Mechanisms of action of antimicrobials
There are THREE proposal mechanisms: 1-Oxidation 2-Halogenation Protein Precipitation3-
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Oxidation cell membrane of bacteria
SH SH S---S
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Halogenation the protein of the cell membrain
H2N CHR CO NH CHR1--- (HOCl) NaOCl H2NCHRCONCl CHR!...
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Protein pption that kill the microbe
H2NCHR1CONHCHR2---- AgNO3 H2NCHR1CONHCHR2--- Ag
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Hydrogen Peroxide H2O2 liquid not store in glass bottles because it decompose ,it store in white plastic container, keep in cold dark place to prevent decomposition. There are many uses : 1- Antiseptic for wash wound , teeth and ear 2-Bleaching color ( hair ). 3- Laundry for cloths.
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Sodium Perborate Antimicrobial: Composite of H2O2, NaBO2 and NaOH Used as bleaching agent in non-chlorine laundry bleaches
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Potassium Permanganate KMnO4
Chemically is a strong oxidizing agent, solid purple crystalline , odorless. Store in well closed container. Uses: 1- Oxidizing agent for skin disease in different concentrations 1: 5000, 1:15000 2- used in swimming pool for athlete foot. 3- Strong oxidizing for many organic reactions.
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Iodine I2 It is dark violet ,insoluble in water , but the
I2 + KI = I3 – Complex soluble in water as iodine solution, soluble in alcohol known as tincture iodine Iodine solution weak solution ( 25g I2 + 25g KI ) in 100ml And strong solution ( 50g I2 + 50g KI ) in 100 ml. Iodine preparations and compounds Antimicrobial property due to oxidation and Iodination disinfectants A chemical reagents in analytical reagent. In drug synthesis. In Povidin iodine as new product.
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Povidone Iodine ( PVP – I)
is a stable chemical complex of poly vinyl pyrrolidine iodide. It is broad spectrum antiseptic for wounds. It is used disinfectant .
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2- Halogenation Dakin's Solution
Sodium hypochlorite solution, (usp) Contains 4-6% of NaOCl, It is made from bleach that has been diluted and treated to decrease irritation. Chlorine, the active ingredient in Dakin's solution, is a strong antiseptic that kills most forms of bacteria and viruses..
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3- Protein ppt (Silver Nitrate AgNO3)
Prepare as 1% AgNO3 , protective from light due to oxidation. Effective against gonococcal organism. Antimicrobial activity of these compounds is due to protein precipitant action. 1% used eye newborn babies.
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