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Drugs Acting on the Skin: An Overview of Topical Medications
- 1. DRUGS ACTING ON SKIN DR. SAROJ K. SUWAL
- 2. FACTS ABOUT SKIN • largest organ of the body, 15% of body weight. • many vital functions, • including protection against external physical, chemical, and biologic assailants,(attack or defense mechanism) • prevention of excess water loss from the body • a role in thermoregulation. three layers: • the epidermis, • the dermis, and • subcutaneous tissue
- 3. DRUGS IN SKIN • Mostly used for relieving dryness and itching • Main uses are To reduce • inflammation , • Skin infections • Topical medicine • administration of drugs via the epidermis (outer layer of the skin) and external mucous membranes • Eg. Ointments ,Creams, gels, sprays, emulsion
- 4. ROUTES • Eye • Ear • Nose • Transdermal • Rectal Vaginal
- 5. OINTMENTS • Semisolid greasy preparation • Medicated type and non medicated type • Single phase preparation • Solid or liquid material is dispersed • Hydrophilic or hydrophobic an oily or greasy consistency and can appear “stiff” as they are applied to the skin Example : Antibiotics ointment Tetracycline, neomycin, mupirocin Antifungal ointment→cotrimazole
- 6. CREAMS • medicines dissolved or suspended in water removable or emollient(moisturiser bases • Multi-phase preparations • Lipophilic phase • Aqueous phase • Are of two types • Emulsions→ make skin soft and cooling agent • Water dispersed in oil(olily cream) • Oil dispersed in water(aquesous cream) OIL- IN-WATER ( O/W) - As- Fluocinolone acetonide cream - • WATER-IN-OIL (W/O)- As- - cold cream
- 7. TYPES OF CREAM • Cleansing and cold cream. • Foundation and vanishing cream. • Night and massage cream. • Head and body cream. • All purpose and general cream
- 8. LOTION • Are liquid or semi liquid preparations • Are to be applied to the unbroken skin without frictions • low-viscosity (By contrast, creams and gels have higher viscosity, typically due to lower water content.) • Eg • Benzyl benzoate lotion • Calamine lotion
- 9. PASTE • Alter the preparations in which powder is suspended in an ointment • Less penetrating, less macerating and less heating than ointment • Eg. Zinc paste • Types • A) Fatty pastes. • b) Non greasy pastes • Are use to protect sub acutely inflamed , lichenified or excoriated skin • Also used to prevent the spreading of active ingredients
- 10. POWDER • Drugs or chemicals in powder form • Used to lessen the friction between skin surface and drying agents • Use especially if soreness and moistness exist • Should be avoid in dry skin • Eg. vancomycin powder Not for use on open wounds unless the powders are sterilized.
- 11. SUNSCREEN •Protect skin from ultraviolet radiation •Eg tiatinus dioxide, zinc oxide and calamine
- 12. ANTI BACTERIAL PREPARATIONS • Antibacterial topical preparations • Common antibacterial topical preparations • Neomycin sulphate • Polymyxin • Sliver sulphazidine • Fusidic acid • Clindamycin
- 13. NEOMYCIN SULPHATE • Used for bacterial skin infection • not effective against fungal or viral infections. • Preparations: • Ointment, cream, dusting powder with other combinations • Contraindications: • Neonates • Dose • Three times daily or according to need
- 14. SIDE EFFECTS • Sensitization if large areas of skin treated • irritation • burning • redness • rash • itching • hearing difficulty→Ototoxicity may be hazard( paticulary in children) • decreased urination
- 15. POLYMYXIN • Similar to neomycin • Dose • BD or more as per requirements • Preparation • Ointment polymyxin B sulphate 10000 units , bacitracin zinc 500units /gm
- 16. SILVER SULPHADIAZINE • Silver sulfadiazine acts only on the cell membrane and cell wall to produce its bactericidal effect • Mostly used for • gram negative infections( eg. Pseudomonas) • many gram- negative and gram-positive bacteria as well as being effective against yeast • In second and third degree burn • Used in chronic infected leg ulcer and pressure sore, • Prophylaxis in infection of skin graft donor site • Extensive abrasions
- 17. PREPRATIONS • preprations • Cream(1%) • Usual dose • Topically daily or as per needed • Thrice a week for ulcer • Contraindications • Pregnancy, neonate, • Hypersensitivity to sulfonamides
- 18. ANTI FUNGAL PREPARATIONS • Mostly topical preparations • Mostly cream based preparations, gels, shampoo, spray • Should be continued after 1 week after disappearance of all sing of infection • Systemic therapy also needed in some cases
- 19. ANTI FUNGAL DRUGS • Clotrimazole(1%) • Econazole nitrate( 1%) • Ketoconazole • Miconazole • Salicylic acid + benzoic acid
- 22. OTHERS Antiviral preprations • Aciclovir Anti parasitic Prepration • Benzyl benzoate Anti pruritic drugs • Calamine lotion • Topical corticosteroids • Betamethasone • Beclomatasone dipropionate • Clobetasol propiconate • Clobetasone butyrate • Fludroxycortisone • Triaminlone acetonide
- 23. ANTIVIRAL -ACYCLOVIR • Uses for • Herpese simplex • Herpes zoster • Varicella zoster • Eye infect by herpes simples
- 24. PREPRATIONS • Cream→ acyclovir 5% • Ointment → for eye ,3% • Tablet • 200mg, 400mg, 800mg • Powder for injections→
- 25. ANTI PARASITIC • Used for scabicide and pediculicides • Benzyl benzoate • Emulsion( 25%) • Treatment of choice for scabies, pediculus captis
- 26. PEDICULICIDES • To kill the lice • permethrin, • Phenothrin • Benzyl benzoate
- 27. ANTI PRURITIC DRUG→ CALAMINE LOTION • Has antipruritic, mild antiseptic and astringent action • skin itches form from sunburn, insect bites, poison, or other mild skin conditions • Lotion containing 15% calamine +5% zinc oxide+5% glycerol, and others • Used for • Pruritis • Skin irritation • Sunburn • Insect bites
- 28. TOPICAL STEROIDS • the treatment of inflammatory and immune-mediated skin conditions. • Oral or injectables can be used for the chronic or autoimmune cases • If corticosteroids are indicated,→ alternate day therapy should be used to minimize the risk of adrenal suppression
- 29. USES • Common indications for topical steroids: • Eczema • Pityriasis rosea • Lichen planus • Alopecia areata • Psoriasis (some forms) • vitiligo
- 30. SPECIAL CONSIDERATIONS • Face • Intertriginous areas • Children • Effect of occlusion • infections and combination formulas (with antibiotics and antifungals)
- 31. TOPICAL STERIODS • Betamethasone • Beclomatasone dipropionate • Clobetasol propiconate • Clobetasone butyrate • Fludroxycortisone • Triaminlone acetonide
- 32. 2 FTU = nearly 1 gram
- 33. • Weak • Hydrocrtisone 0.5-2.5% (with miconazole, Fucidin H with fucidic acid) • Moderate • Clobetasone butyrate 0.05% • Hydrocrtisone with urea • Potent • Mometasone dipropionate 0.025% or furoate 0.1% (with miconazole, Momenta with miconazol & gentamycin) • Betamethasone esters as valerate 0.1% or diproprionate 0.05% (Betnovate, Betaderm, Fucibact B with Fucidic acid, Betazol with miconazole, Diprosalic with salicylic acid) • Very potent • Clobetasol propionate 0.05% (Dermovate, Gamavate) • Diflucortolone valerate (Nerisone)
- 34. SIDE EFFECTS • Perioral dermatitis and rosacea • Tachyphylaxis & steroid addiction • Infections (tinea incognito, herpes simplex, pityriasis versicolor, scabies……) • Adrenal suppression • Glucoma and cataract
- 35. SIDE EFFECTS • Local side effects • Telangiectasia, purpura, epidermal, dermal and subcutaneous atrophy, striae, psuedoscars…… • Folliculitis • Allergic reactions • Hypopigmentation • Hypertrichosis • Delayed wound healing • Alteration in skin elasticity & mechanical properties
- 36. SIDE EFFECTS
- 37. CONTROL OF MICROBIAL GROWTH • Sterilizing Agents– • kill everything (e.g. heat, radiation) • Disinfectants— • kill most things.Too strong for living tissues (e.g. lysol, NH3) • Antiseptics– • milder in action. Can be used topically, but not ingested. (e.g. alcohol, iodine) • Chemotherapeutics— • can be ingested (e.g. penicillin, sulfa drugs)
- 38. ANTISEPTICSVS DISINFICATNS Disinfectants • Destruction or inhibition of growth of all pathogenic organisms (bacteria, viruses, fungii) on non living surfaces • Not used on skin or mucus membrane • High level and low level disinfectants • Toxic and stronger Antiseptics • chemical substances which inhibit the growth or kill microorganisms on living surfaces • Use for skin or mucus membrane • Less toxic than disinfectants If spores are also killed process is Sterlization
- 40. CLASSIFICATION
- 41. PHENOL • Earliest used , • Especially for gram positive and enveloped virus • Not effective against not enveloped virus and spored • • Protoplasmic poison • • Injures tissues & cells at high conc. • • Denaturation of bacterial proteins • •To disinfect urine , faces , pus.
- 42. CHLOROXYLENOL (DETTOL) • Phenol derivative • Does not coagulate proteins, • Covers gram positive mostly • Non corrosive, • Non irritating to skin • Side effects are generally few but can include skin irritation to some • Non toxic to human skin but toxic to cat and fish Uses • Commercial 4.8 % solution used for surgical antisepsis • Skin cream and soap: 0.8% • Mouth wash 1%
- 43. CHLORINE • potent germicide. • Kills pathogens in 30 sec. used to disinfect urban water supplies. Chlorination is the process of adding chlorine to drinking water to disinfect it and kill germs.
- 44. USES OF CHOLOROPHORES • Chlorinated lime (bleaching powder • – obtained by action of chlorine on lime. • – used to disinfect drinking water • (2) Sodium hypochlorite • – Powerful disinfectant used in dairies for milk cans. • – Too Irritant to be used as antiseptic. • – Root canal therapy in dentisry
- 45. CETRIMIDE • ammonium antiseptics• • Detergents: • Cidal to bacteria, fungi & viruses. • • Act by altering permeability of cell membrane • • Efficiently remove dirt and grease • • Widely used as antiseptics & disinfectants for surgical instruments, gloves etc • • Combined with chlorhexidine (savlon)
- 46. ALCOHOL • Ethanol and Isopropyl alcohol • Evaporates quickly • Kill vegetative bacteria and Fungi and some virus • Not effective against spores and enveloped virus • Act by precipitating bacterial proteins ( denaturation and membrane damage
- 47. • Not effective if taken internally • Uses as • Antiseptic, • cleansing agent at 40-90% conc.
- 48. • Irritant • So , should not be applied on mucous membrane, ulcers, open wounds • Uses • Use for skin preparation before injection, surgery • Can damage rubber, plastics • Preparation • Spirit: methyl salicylate 0.5ml • Diethyl phthalate 2% • Castor oil 2.5 %
- 49. ALDEHYDES (FORMALDEHYDE) • Glutaraldehyde, formaldehyde orthopthaldehyde(OPA) • Used for fumigation. • •37 % aqueous solution called as formalin. • MOA • Protoplasmic poison • , denaturates protiens and inactivate nuclelic acid
- 50. • Fumigation is a process of gaseous sterilization which is used for killing of micro-organisms and prevention of microbial growth in air, surface of wall or floor
- 52. Uses • for preserving dead tissues. • Use as antiseptic restricted due to bad odor & irritation • Immersion for 10-12 hours kills all microbial life • • Formaldehyde • Glutaraldehyde is a better sterilizing agent
- 53. CHLORHEXIDINE • effective against a range of microorganisms but not spores • more effective than povidone-iodine • Used as • disinfectant , antiseptic and sterilization • used for skin disinfection before surgery • sterilize surgical instruments • Used for bladder irrigation and catheter patency for blockade Nepal was the first country in the world to use chlorhexidine to treat the umbilical cord of newborn babies, and received a USAID Pioneers Prize for reducing the neonatal death rate
- 54. • MOA • Bactericidal in high concentration and bacteriostatic effect in low concentration • by highly positive charged on membrane of microorganism • Preparation • Solution, pink • Chlorhexidine acetate 0.05% • Lotion blue chlorhexidine gluconate 0.1% • Dusting powder • Chlorohexidine acetate 1% ( gargle)
- 55. • Side effects may include • skin irritation, • teeth discoloration, and • allergic reactions • Teeth stains • eye problems if direct contact • Ototoxic if put to ear → can damage ear drum→ lead to deafness
- 56. POVIDINE IODINE(BETADINE) • iodophors • broad spectrum antiseptic • Rapidly acting broad spectrum (bacteria, fungi,virus) • Used for skin disinfection, vaginal infection , • active bactericidal element • Oral hygiene, boils, furunculosis, burns, ulcers, tinea, surgical srub, disinfecting surgical instruments, non specific vaginitis.
- 57. • Preparations • Povidine iodine 10% in alcoholic solution • Solution Povidine iodine 10% • Dry powder spray • Ointment →Povidine iodine 1% in water miscible basis • Surgical scrub: Povidine iodine 7.5% • Alcoholic tincture : povidone iodine 10%
- 58. USES • All infections • used for the prevention and treatment of infections in the mouth. • Minor wounds • used for the prevention and treatment of skin infection on the skin. • used as an antiseptic and first aid for minor cuts, grazes, abrasions, and blisters. • Vaginal Candidiasis • used to prevent and treat the fungal infection of the vagina • may be used in combination with other medicines for better results. • Skin disinfectant • Povidone Iodine is also used to clean a patient's skin before a surgical procedure is performed.
- 59. Dose • Apply undiluted betadine to minor wound and skin for disinfection • Side effects • Skin irritation • Allergic Skin Reaction • Redness of skin • Acneiform eruptions • Thyroid imbalances • Contraindications • Preterm neonate • Avoid regular used for thyroid distorders • allergy
- 60. HYDROGEN PEROXIDE • Used for skin disinfection (antiseptics) • Antibacterial, anti fungal, antiviral →wide range • Especially for the treatment of wounds that are infected with anaerobic microflora. • – Helps in loosening & removing slough, ear wax etc. • Preparation • Hydrogen peroxide solution ,3%, 6% • Hydrogen peroxide cream 1%
- 61. USES IN MEDICAL • Particularly cleansing and deodorizing wounds and ulcer • Helps in loosening & removing slough, ear wax etc. • rinsing the mouth and throat, • Concentrated solutions (20-30%) is indicated for the treatment of warts, lichen planus. • not be used to treat deep wounds, animal bites, or serious burns. • Can damage normal skin tissue
- 62. HOW ITWORKS • works by releasing oxygen when it is applied to the affected area. • The release of oxygen causes foaming, • which helps to remove dead skin and clean the area. liberates nascent oxygen which oxidizes necrotic matter & bacteria.
- 63. GENTIANVIOLET(GV) • has antibacterial, antifungal, and anthelmintic properties • Inhibit the growth of many fungi (yeasts and dermatophytes, candida) • also has weak antibacterial effects and
- 64. USE • antiseptic dye used to treat fungal infections of the skin (e.g., ringworm, athlete's foot) • may be used on minor cuts and scrapes to prevent infection. • Inhibit some garam positive bacteria especially staphylococcus species • Used on chronic ulcers, furunculosis, bed sores, ring worms
- 65. PREPARATION • 0.5-1% concentration as aqueous solutions • Also available in granules form • Dose • Apply topically 2-3 times daily • Contraindications • Mucus membrane of eye and open wounds
- 66. ADVERSE EFFECTS • Irritations • Mucosal ulceration • Esophagitis • Laryngitis • Tracheitis if swallowed
- 67. POTASSIUM PERMANGANATE • used for cleaning wounds and dermatitis • liberates oxygen in atomic form. • Higher concentrations cause burns and blistering • Preparation • Solution 0.1% in water • Dose • Dilute in 1 in 10 to provide 0.01% solution • Tablet : 400mg , dissolved 1 tablet in 4 liters of water →0.01% solution
- 68. CLINICAL USES: • For different skin disease (fungal infections of the foot, impetigo, pemphigus, superficial wounds, dermatitis, and tropical ulcers.) • Gargling, • irrigating cavities, urethra and wounds. • cleansing and deodorizing suppurating eczematous reactions and wound • Stomach wash in alkaloid poisoning. • In a 2-5% solution is used for burns, bites of mosquitoes and snakes, for quick healing of wounds.
- 69. BORIC ACID • • weak antiseptic , • bacteriostatic. • • used for mouth wash, • irrigation eyes, glossitis. • • Adverse effect: vomiting , • abdominal pain on systemic absorption
- 70. SOAPS • • Anionic detergents • contains common antibacterial ingredients like triclosan and tea tree oil • inhibit the growth of various bacteria, as well as some viruses and fungi • •Weak antiseptics with cleansing action • •Washing with soap and warm water one of the most effective methods of preventing disease transmission • • Affect only Gm+ bacteria
- 71. THANKS