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Potency Penetration Penetration : depend on thickness and integrity of the Stratum Corneum, concentration, Vehicles, Occlusiveness, frequency of application Formulation enhance the efficacy Be carefull of local and Systemic Toxicity by active ingredients as well as vehicle ingredients
Stratum Corneum
Thickness, temperature and water concentration Integrity of the startum corneum in diseased skin ( abraded ) Vehicles that contain Solvents, Surfactants and Alkohol denature the cornified layer and increase penetration
Frequency of application
Frequency of application have little effect of increasing drug efficacy, but because of wash off/wipe off after the application, we may need to apply more than once
Quantity of application
It need minimal quantity to be spread to cover the diseased, but apply more than needed will not increase the efficacy
4/18/2011
Powder
Absorb moisture and prevent friction, mainly contain Talc, Zinc oxide For intertriginous area Drug formulated as powders : Antipruritus, topical anti mycotic.
Cream
Cream is an emulsion of oil and water O/W : oil in water, oil to be dispersed in the water ( dispersion medium) W/O : Water in Oil, water to be dispersed in oil ( dispersion medium), have cool feeling due to slow evaporation of water phase.
Ointment
White/ yellow Petrolatum Can not absorb water, not suitable for water soluble drug. Greasy but moisturize as it keep water from evaporation No preservative
Pastes
Powder + Ointment ( > 50% non soluble powder, such as talc, Zinc Oxyde )
Solution
Clear and transparant
Lotion/Suspension
Mixture of two-phase system that are insoluble. Insoluble Drug dispersed into a liquid in a concentration up to 20% Non-uniform dosing Milky lotion is not a lotion but an emulsion
4/18/2011
Shake lotion
Powder + lotion Increase the evaporation surface----cool feeling Non-uniform dosing
Gel
Water soluble, clear, not greasy Suitable for hairy area May cause dryness, but gel that contain humectant are not drying the skin May contain alcohol
Corticosteroid topical
The most frequently prescribed New molecule : higher potency while minimizing side effects Anti inflammatory, Immunosuppresive, antiproliferative and vasoconstrictive
Vasoconstriction assay
The ability to cause vasoconstriction usually correlates with its anti inflammatory potency. These assays used to separate the costicosteroid into 7 classes Notice: The same drug can be found in different potency classifications depending on the delivery vehicle used
4/18/2011
Tachyphylaxis
The vasoconstriction effect decrease after a period of time using topical steroid, mean the potency also decrease. Stop the application for a few day, then resume. Prevention of tachyphylaxis : intermittent usage.
Topical Retinoid
All trans Retinoic Acid / Tretinoin Good for Acne Vulgaris Skin irritation Photosensitation (not phototoxic) No teratogenic in topical use for face ( Fitspatricks Dermatology in General Medicine, 7 ed 2008 )
4/18/2011
Topical Antibiotic
Treatment of Acne : Clindamycin, Azelaic Acid, Erythrocin, Sulphacetamide, Metronidazole Treatmant of superficial bacterial infections /burns : Mupirocin, Fusidic acid, Silver Sulphadiazine, Neomycin, Gentamycin, Chloramphenicol, Gramicidin.
Topical Bleaching
Hidroquinone Kojic Acid Tretinoin
Imidazole
Cytochrome p450 system dependent Fungistatic Anti inflammation Limited anti bacterial properties Clotrimazole, Econazole, Ketoconazole, Miconazole, Oxiconazole, Sertaconazole, Sulconazole
Allylamines/Benzylamines
Allylamines: Naftifin Terbinafine Benzylamines: Butenafine
4/18/2011
Polyenes
Nystatin : anti Candida Imidazole is more effective in Vulvovaginal candidiasis. ( its use has diminished) Low concentration: Fungistatic High concentration: Fungicidal Not absorbed by intact skin, mucocal membrane of the GI tract and Vagina