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CHAPTER VI: TOPICAL AGENTS

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

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

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

Soapstone steatite (lump form) Foliated Talc has a plate-like structure - desirable for cosmetic and pharmaceutical purpose very low adsorptive properties; used as filtering aid (allowing filtration without danger or removing important constituents Lubricating-protective dusting powder protects areas from further irritation when used on broken skin, it produces sterile abscesses or granulomas (nodule of inflamed tissue where granulation is occurring)

ZINC OXIDE
- Zinc White, Lana o Algodon Filosoficos, Flores de Zinc Preparation: - heating strongly in a furnace a mixture of coke and zinc mineral Calamine (Zn2SiO4H2O) Willemite (Zn2SiO4) Smithsonite (ZnCO3) Franklinite (ZnO + Manganese and iron oxide) Zincite (ZnO, red variety) - medicinal grade by calcinations of zinc carbonate gradually absorbs carbon dioxide from air, forming basic zinc carbonate forms Lewis acid (Zinc chloride) when treated with dilute HCl Zn+2 antibacterial, ANTIMICROBIAL AND ASTRINGENT

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

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

CALAMINE ZnOxFe2O3
- Zinc oxide + Ferric Oxide Official forms: 1. Ointment 2. Paste 3. Zinc oxide with salicylic acid paste USES topical protective o dusting powders, ointments, lotions soothing, adsorbent, protective better cosmetic acceptability than Zinc oxide for dermatological problems Calamine Lotion contains Calamine and Zinc oxide suspended with the aid of Bentonite Magma in a calcium hydroxide solution - protective with a good drying effect and mild astringent action Phenolated Calamine Lotion (1% liquefied phenol) local anesthetic and antipruritic

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

TITANIUM DIOXIDE TiO2


amorphous, infusible powder identified by adding H2SO4 producing a orange-red colored Titanium peroxide (TiO3)

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

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

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

ANTIMICROBIALS AND ASTRINGENTS


- non selective (kills bacteria, kills skin) Mechanism of Actions 1. Oxidation - generally non-metals and certain types of anions hydrogen peroxide metal peroxide permanganates halogens oxohalogens anions - effective action involves the reducing group present in most proteins (e.g. sulfhydryl) 2. Halogenation - destructive to the functions of specific proteins destroy the function, destroy the microorganism 3. Protein Precipitant - involves interaction of proteins with metallic ions with large radius ratio or strong electrostatic fields Group 1-B Group 2-B Aluminum most metal cations except of alkali and alkaline earth ASTRINGENT - burning/constriction action on the surface - application of very dilute solution of metal cation to tissue provides a local/surface protein precipitant action shrinkage / firming of tissues Control of Antimicrobial/Astringent Action 1. Adjust the concentration 2. Place in a vehicle that will slowly releasing to the site of action a solution containing glycerin and polyethylene glycol 3. Complexation with a ligand - provides a controlled release, minimizing toxicity and activity on host cells 4. Synthesize into Insoluble Form Suspension ointment cream - slow release of active agent

HYDROGEN PEROXIDE SOLUTION H2O2


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

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

POTASSIUM PERMANGANATE KMnO4


Mineral Chamaleon dark purple crystalline compound, opaque in transmitted light and of blue metallic luster in reflected light sweetish astringent taste oxidation (mechanism of action) KMnO4(+7)- MnO2(+4) Mn+2 brown ppt poured directly on the skin (effective but produces brown spots) Low penetrating power, short duration of action

USES treatment for dermatitis (skin infections) caused by bacteria and fungi poisoning produced by plant and animal toxins wet dressing treatment of vesicular (small blisters or raised areas with fluid) stage of eczema, athletes foot(Tinea pedis) and fungal infections on other portions of the body

SODIUM HYPOCHLORTE SOLUTION NaOCl


- Dakins Solution Chlorinated Soda Solution - disinfectant - clear pale greenish yellow liquid - dissolves blood clots and delay healing Labarraques Solution diluted solution containing 2.5%, disinfectant - disinfectant and laundry bleach germicidal agent Modified Dakins Solution - can be used wounds with pus, without sutures (can be dissolved) - removing necrotic tissues and antiseptic (diluted) - can be used as foot bath OTHER CHLORINE-CONTAINING COMPOUNDS: 1. Chlorinated Lime Bleaching Powder - Calcium chloride hypochlorite - disinfectant in swimming pools, and sterile rooms, bleaching agent 2. Chloramines organic amines - releases hypochlorous acid (water purifier) - antimicrobial action is due to the presence of HOCl

IODINE I
Iodinum, Jodum grayish granules with a metallic luster I2 solution (germicidal) toxic but inactivated in the GI tract produces gastroenteritis, and bloody diarrhea gastric lavage causes the person to vomit the iodostarch complex (blue) Iodine Solution and Iodine Tincture antimicrobial purposes most effective topical agents available antiseptic on skin prior to surgery tincture may be used to disinfect drinking water

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

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

SILVER NITRATE AgNO3


Azotas Argentious , Cristales Lunares protein precipitant (mechanism of action) astringent, antibacterial 0.01% irritant(corrosive) 10% has an oligo-dynamic action antibacterial even in a low concentration (1%) extended use can cause a darkening of the skin due to deposition of free silver below the epidermis (argyria) - OPHTHALMIC SOLUTION 1% effective against ophthalmia neonatorum (gonorrhea) microorganism causing blindness in babies more effective than penicillin - 0.5% in the form of wet dressing on third degree burns SIDE EFFECT electrolyte imbalance should be used alternately with other organic medication Toughened AgNO3 lunar caustic, molded into pencil form by adding HCl AgCl lessens the friability of the pencil (for hard to reach areas) USES caustic, escharotics and germicide for small sepsic wounds (ulcerations) in condenser (purification of water) as linings mas matagal sterile yung water

AMMONIATED MERCURY Hg(NH2)Cl


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

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

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

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

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

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ANTIMONY POTASSIUM TARTRATE (SbO)KC4H4O6 H2O


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

ASTRINGENT S - local protein precipitant


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

ALUM AlNH4(SO4)212H2O / AlK(SO4)212H2O


Tawas, Ammonium Alum, Potassium Alum sweetish strongly astringent taste source of Aluminum ion useful as topical astringent irritants/caustics footbaths toughening the skink and avoid formation of blisters used in the preparation of several biological products Precipitated diphtheria and tetanus toxoids vaccines, injected to produce antibodies

ALUMINUM CHLORIDE AlCl26H2O


local external astringent and mild antiseptic irritating as antiperspirant, replaced by aluminum hydroxychloride

OTHER ALUMINUM-CONTAINING ASTRINGENTS:

ALUMINUM SULFATE Al2(SO4)3214H2O


Cake Alum, Pickle Alum, Pearl Alum, Papermakers Alum

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

ZINC CHLORIDE ZnCl2


Butter of Zinc astringent and dentin desensitizer escharotics (caustic)

ZINC SULFATE ZnSO47H2O


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

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

CHAPTER VII: DENTAL PRODUCTS


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

SODIUM FLUORIDE NaF


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

STANNOUS FLUORIDE SnF2


Tin Difluoride topical fluoride application 8%

DENTRIFICES

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

CHAPTER VIII: MISCELLANEOUS INORGANIC PHARMACEUTICAL AGENTS


INHALANTS
gases

OXYGEN O2
Dephlogisticated Air, Aire Vital, Fire Air, Aire Puro Commercial Production: 1. Fractional Distillation of Liquid Aire (Linde Process) - air is liquefied by low temperature and high pressure 2. Electrolysis of Water - electricity passed through water containing 15% sodium/potassium hydroxide, breaking down water into its components, hydrogen and oxygen - oxygen is liberated at the anode

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

USES -

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

CARBON DIOXIDE
- Carbonic Acid Gas/ Carbonic Anhydride - stored in gray metallic cylinders Dry Ice solid carbon dioxide, used as refrigerant USES 1. Respiratory stimulant for persons suffering from impairment of the respiratory organs 2. dry ice destroys tissue by freezing it, treatment of acne, angiomas (tumor made up of blood), calluses, eczema, moles, psoriasis and warts 3. used to make carbonated drinks

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

NITROUS OXIDE N2O


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

NITROGEN N2
Azote stored in black cylinder pharmaceutical air to displace air in parenteral and topical preparations

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

AMMONIUM CARBONATE
Preston Salt, Sal Volatile, Bakers Ammonia, Ammonium Sesquicarbonate ammonium bicarbonate + ammonium carbamate (NH2CO2NH4) basis of smelling salts, valuable in hysterical syncope leavening agent Bakers ammonia Officially categorized as Source of Ammonia

AROMATIC AMMONIA SPIRIT


composed of two active ingredients Ammonium carbonate Strong Ammonia Solution respiratory stimulant by inhalation of vapors

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

EXPECTORANT AND EMETICS


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

AMMONIUM CHLORIDE NH4Cl


Sal Ammoniac, Salmiac, Ammonium Muriate increases secretions especially the saliva, mucous and sweat SYSTEMIC ACIDIFIER Chloride replenisher

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

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

SODIUM NITRITE NaNO2


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

SODIUM THIOSULFATE Na2S2O35H2O


Antichlor Hypo antidote for cyanide and iodine poisoning fixer in photographic films in bleaching paper pulps CHEMICAL ANTIDOTE CN -----> SCN toxic non-toxic

ACTIVATED CHARCOAL
Carbon Ligni residue from destructive distillation of organic materials, treated to increase adsorptive power obtained by incomplete combustion of wood activation removing previously adsorbed substances, reduces its particle size GENERAL PURPOSE ANTIDOTE Mechanical antidote 1. adsorb Activated charcoal, Kaolin 2. ppt CuSO45H2O

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

CUPRIC SULFATE CuSO45H2O


Blue Vitriol, Blue Stone, Caparrosa Azul, Piedra Lipis antidote for phosphorous poisoning 300 mg emetic 10-30 mg astringent and tonic

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

CALCIUM SULFATE CaSO4


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

COLLOIDAL SILICON DIOXIDE SiO2


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

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

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

BENTONITE Al2O34SiO2H2O
Soap Clay, Mineral Soap, Wilkinite native, colloidal, hydrated aluminium silicate has an earthly taste also used as stabilizer in industrial emulsions exerts detergent effect (used in soaps and cleansers) clarifying agent with adsorptive powers for dyes and other coloring matters.

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CHAPTER IX: RADIOPHARMACEUTICALS AND CONTRAST MEDIA


isotopes different form of an element, which vary in the number of neutrons contained in the nuclei When radioactive isotopes decay, they emit certain particles or quantities of energy that are characteristic of the particular isotope involved. Major Particles of Decay 1. Alpha Particles ( , 4He+2) - heaviest and slowest of all radioactive emissions Beta Particles ( -) negatively charged species having a mass of an electron moves at a faster velocity more penetrating power negatrons - emitted by unstable nuclei having neutrons in excess of protons - if neutron/proton ratio exceeds stable limits, transformation of neutron to proton occurs, with the expulsion of beta radiation element undergoing this type of transformation will decay to the element having the next highest atomic number positron ( +) - a proton is transformed into a neutron, accompanied by the emission of positron elements emitting positron radiation will decay to the element having the next lowest atomic number 3. Gamma Radiation ( ) - a photon of electromagnetic radiation - demonstrates both wave and particle properties - rays are of short wavelength, similar to x-ray - travels at a speed of light - emission of gamma ray is almost always accompanied by the emission of other forms of radiation K-Process process wherein a type of radiation similar to gamma rays is seen in the emission of x*K shell (1st orbital) rays 2. Biological Effects of Radiation - can lead to necrosis and complete destruction of the tissue or organ Radiopharmaceuticals are preparation containing isotopes which are used internally for therapeutic and diagnostic purposes Isotopes important as radiopharmaceuticals are: 1. Those emitting beta and gamma radiation since they can penetrate body tissues 2. Isotopes which can be concentrated in specific manner in certain organ or cells 3. Isotopes which should be eliminated from the body easily and aside from the associated radioactivity, they and the decay products should be of low toxicity

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Radiopharmaceutical Preparations 1. Sodium Chromate Cr 51 Injection - Chromitope Sodium Rachromate -51 diagnostic determination of red blood cell mass, volume and survival time, and scanning of spleen 2. Gold Au 198 Injection - Aurcoloid -198, Aureotope, Auroscan diagnostic preparations for scintillation scanning of the liver 3. Sodium Iodide I 123 Solution (Iodotope I 125) diagnostic aid in the study of the function of the thyroid gland scanning thyroid gland Sodium Iodide I 131 Capsules & Solution (Iodotope I-131) determine the blood and plasma volumes determination of cardiac output 4. Sodium Rose Bengal I -131 Injection - Robengatope I-131 radioactive tracer in the determination of the liver function 5. Sodium Iodohippurate I-131 Injection - Hippuran -131 diagnostic agent to determine kidney function 6. Chlormerodin Hg 197 Injection and Hg 203 Injection Scintillation scanning of the kidneys and brain 7. Sodium Phosphate P 32 Solution - Phosphotope Treatment of polycythemia vera (increase in RBC) localization of intraocular tumors 8. Technetium T 99 Injection - Sodium Pertechnetate Brain scanning to determine the presence and location of neoplastic lesions 9. Cyanacobalamin Co-57 and Co-60 Capsules and Solutions diagnostic agent for pernicious anemia

Radiopaque Contrast Media


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

BARIUM SULFATE BaSO4


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

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