Dermatopharmacology Prof Werner Sinclair Department of Dermatology University of the Free State

Pages 328 – 354 in Textbook (Hunter, Savin and Dahl)

Drugs To Be Discussed 1 Antifungals: Griseofulvin Terbinafin Terbinafin Fluconazole Fluconazole Itraconazole Itraconazole Ketoconazole Ketoconazole Corticosteroids: Topical Systemic SystemicChloroquine

Drugs To Be Discussed 2 Retinoids: Topical Systemic Systemic Benzoyl peroxide ShampoosBarriers Antibiotics: Topical Systemic Systemic Antivirals: Acyclovir Podophyllin Podophyllin Antiscabies: Benzoyl benzoate

Drugs To Be Discussed 3 AntihistaminesAnti-androgensImiquimod

Antifungals GriseofulvinTerbinafinFluconazoleItraconazoleKetoconazole

Griseofulvin Only active against dermatophytes (keratolytic fungi) Fungistatic Absorbed with fatty food (milk) Very safe in children 10 – 20 mg per kg per day

Terbinafin Only active against dermatophytes Fungicidal Tablets and cream Some severe immunological side-effects

Fluconazole Broad spectrum Fungistatic Convenient once per week dosage Can be used in neonates Used for: Candida Cryptococcus Cryptococcus

Itraconazole Very broad spectrum Fungistatic To be taken with meals Capsules and suspension available Used for: Any fungal infection Not better than terbinafin for Not better than terbinafin for dermatophytes dermatophytes

Ketoconazole Broad spectrum Fungistatic To be taken with meals Tablets, cream and shampoo available Used for: Seborrheic dermatitis Pityriasis versicolor Pityriasis versicolor Candidiasis Candidiasis Side-effects: Liver toxicity P450 inducer P450 inducer

Imidazole Creams Variety available Similar spectra Little to choose Price deciding factor E.g.. Ketoconazole, econazole, clotrimazole

Corticosteroids TopicalSystemic

Topical Corticosteroids 3 Strengths Fluorinated vs Non-fluorinated Ointments, Creams, Lotions:

Topical Corticosteroids Ointments: More potent Penetrates deeper Penetrates deeper More atrophy More atrophy Used for: Dry lesions Thick lesions Thick lesions Thick skin Thick skin

Topical Corticosteroids Creams: Less potent Penetrates less Penetrates less Less atrophy Less atrophy Used for: Acute, thin lesions Moist lesions Moist lesions Thin skin (Face, skin folds) Thin skin (Face, skin folds)

Topical Corticosteroids Lotions: Least potent, least atrophy Used for: Hairy areas (scalp) Wet lesions (Watery solutions) Wet lesions (Watery solutions)

Systemic Corticosteroids Prednisone / Prednisolone Potent, fast acting anti-inflammatory Cheap Side-effects: Short term: Almost none Long term: Severe Long term: Severe Used once daily, in the morning

Chloroquine Indications: Cutaneous lupus erythematosus Porphyria cutanea tarda Porphyria cutanea tarda Side-effects: Corneal deposits (Temporary) Maculopathy (Permanent) Maculopathy (Permanent) Other Other

Retinoids Topical: Tretinoin Adapalene Adapalene Tazarotene Tazarotene Comedolytic, anti-inflammatory Indications: Acne (All forms) Anti-aging Anti-aging Other Other

Retinoids Systemic: Isotretinoin Acitretin Acitretin Indications: Acne Psoriasis Psoriasis Lymphomas Lymphomas Many others Many others Side-effects, etc: See acne lecture

Benzoyl peroxide Comedolytic, antiseptic Gel / Cream Superficial, inflammatory acne vulgaris

Shampoos Ketoconazole: Seborrheic dermatitis Pityriasis versicolor Pityriasis versicolor (Not for tinea capitis) (Not for tinea capitis) Coal tar (LPC): Psoriasis Povidone iodine (Betadine) Selenium sulfide (Selsun) Zinc pyrithione

Barriers Zinc/Castor oil BP: Nappy rash

Antibiotics Topical: Mupirocin Fucidic acid Fucidic acid Gentamycin Gentamycin Erythromycin Erythromycin Clindamycin Clindamycin Systemic: Tetracyclines (oxytetracycline, doxycycline, minocycline, lymecycline) Penicillins (amoxycillin, cloxacillin, amoxycillin-clavulanic acid Penicillins (amoxycillin, cloxacillin, amoxycillin-clavulanic acid Erythromycin Erythromycin

Mupirocin Manufactured by Pseudomonas bacteria Broad spectrum Esp effective against Staphylococci Ointment and cream No systemic use Reserved for short term use

Tetracyclines Bacteriostatic antibiotics, potent anti- inflammatory effects inflammatory effects Used widely in acne, rosacea, bullous diseases Oxytetracycline: Rosacea Lymecycline: Drug of choice for acne Minocycline: Acne in white patients (pigmentation) Doxycycline: Acne in black patients (phototoxicity)

Penicillins Cloxacillin, Flucloxacillin, Amoxycillin- Clavulanic acid: Staph infections Amoxycillin, erythromycin: Strep infections

Antivirals Acyclovir: Cream, tablets and IV Used for: Herpes simplex 1 and 2 Herpes zoster Herpes zoster (Cream useless) (Cream useless) Side-effects: Practically none Podophyllin: 25% in TBCo: Used for condylomata acuminata and verrucae

Antiscabies Benzoyl benzoate Only effective treatment for scabies Method of use: See Academic Afternoon on skin infections

Antihistamines Sedating: Promethazine Chlorpheniramine Chlorpheniramine Hydroxyzine (Aterax®) Hydroxyzine (Aterax®)

Antihistamines Sedating: Promethasine Chlorpheniramine Chlorpheniramine Hydroxyzine (Aterax®) Hydroxyzine (Aterax®) Used for: Atopic dermatitis Acute urticaria Acute urticaria Other forms of night-time pruritus Other forms of night-time pruritus

Antihistamines Sedating: Promethasine Chlorpheniramine Chlorpheniramine Hydroxyzine (Aterax®) Hydroxyzine (Aterax®) Used for: Atopic dermatitis Acute urticaria Acute urticaria Other forms of night-time pruritus Other forms of night-time pruritus Side-effects: Sedation (NB: Driving) Photo-allergy (not hydroxyzine) Photo-allergy (not hydroxyzine) Dry mouth Dry mouth

Antihistamines Non-sedating: Loratidine Cetirizine Cetirizine Desloratidine Desloratidine Levocetirizine Levocetirizine Used for: Acute and chronic urticaria Allergic rhinitis Allergic rhinitis Side-effects: Almost none

Anti-androgens Cyproterone acetate Progestogen, blocks 5α-reductase Progestogen, blocks 5α-reductase 2mg in Diane-35® 2mg in Diane-35® 10mg in Androcur 10mg in Androcur Used mostly for acne Used mostly for acne Side-effects: Depression, weight gain Side-effects: Depression, weight gainDrosperinone Ingredient of Yasmin® Ingredient of Yasmin®

Imiquimod (Aldara®) Topical immunostimulant Used for condylomata acuminata Superficial spreading basal cell CA Superficial spreading basal cell CA Side-effects: Severe local inflammation