4/18/2011

Efficacy Dermatologic Topical Therapy

David Sudarto Oeiria, Dr, Sp.KK Spesialis Ilmu Kesehatan Kulit dan Kelamin (IDN) Konsultan Bedah Kulit Kosmetik ( IDN) Dermatologist(JPN), Dermatologic Surgeon(JPN) Plastic Surgeon (JPN)

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

Regional difference in penetration

1. Mucosal membrane 2. Scrotum 3. Eyelids 4. Face 5. Chest and back 6. Upper arm and thigh 7. Lower arm and Leg 8. Dorsum of hands and feets 9. Palmar and plantar skin 10Nail Most penetration with 1 and less penetration with increasing numbers

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

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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

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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

Potency ranking of topical corticosteroid

Class 1 : super potent Class 2 : potent Class 3 : potent, upper mid-strength Class 4 : Mid-strength Class 5 : Lower mid-strength Class 6 : Mild- Strength Class 7 : Least Strength

KLASIFIKASI KORTIKOSTEROID TOPIKAL BERDASARKAN POTENSINYA

KELAS 1 SUPER POTENT clobetasone propionate salap 0,05% betamethasone dipropionate Cream/Oint 0,05% KELAS 2 POTENT betamethasone dipropionate krim 0,05%( Diprolene AF cream ) fluocinonide salap dan krim 0,05% Desoximetasone salap dan krim 0,25% KELAS 3 POTENT, upper mid strength betamethasone dipropionate krim 0,05%( Diprosone cream) betamethasone valerate salap 0,1% KELAS 4 MID-STRENGTH _ triamsinolone acetonide Oint 0,1% fluocinolone acetonide Oint 0,025% mometasone furoate Cream 0,1%

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KLASIFIKASI KORTIKOSTEROID TOPIKAL BERDASARKAN POTENSINYA

KELAS 5 Lower MID-STRENGTH betamethasone valerate krim 0,1% fluocinolone acetonide krim 0,025% hydrocortisone valerate krim 0,2%( locoid lipocream) triamsinolone acetonide krim 0,1% Fluticazole propionate 0.05% cream ( Cutivate cream ) KELAS 6 MILD Strength desonide krim 0,05% fluocinolone acetonide krim 0,01% betamethasone valerate lotion 0,1% Alclomethasone dipropionate 0.05% KELAS 7 Least potent Hydrocortisone methylprednisolone dexamethasone

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.

Side effect of topical Corticosteroid

Atrophic Changes Acneiform Reactions Hypertrichosis Pigmentary Changes : hypopigmentation Development of Infections: candida, Viral infections Allergic Reaction to vehicle, Parfum, Preservative and to corticosteroid itself

Systemic Side effects

Increase ocular pressure, if apply to periorbial skin Suppression of Hypothalamus-pituitaryadrenal Axis Retarded growth of Children Metabolic Side effect : Hyperglycemia---DM

Other Topical Therapy

Topical Antibiotic Topical Retinoid Topical Bleaching for melasma Topical Antifungal

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 )

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Topical Tretinoin Preparation

Lotion( 0.05%) Gel (0.01%, 0.025%) Cream : Retin A ( 0.025% & 0.05%, 0.1%), Renova ( 0.02%; 0.05% was discontinued )

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

Topical Anti Fungal

Three classes of topical antifungal: 1. Imidazoles 2.Allylamines and Benzylamines 3.Polyenes

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

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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

Antifungal that do not fit well into the major classes

Ciclopirox Olamine; High penetration of the keratin, good for topical treatment of Onychomycosis Tolnaftate : low effectivity Undecylenic Acid: low effectivity