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1 Dermatopharmacology Prof Werner Sinclair Department of Dermatology University of the Free State Outcomes for this Lecture After this lecture the student should be able to: Name the most important characteristics and uses of the following antifungals: Griseofulvin Terbinafine Ketoconazole Fluconazole Itraconazole Topical imidazole creams Discuss the characteristics and uses of the different strengths and formulations of topical steroids Name the indications for and most important side-effects effects of chloroquine Discuss the indications and use of topical retinoids Discuss the origin, characteristics of and indications for mupirocin Discuss the use of tetracyclines in dermatology Name the uses of the different types of antihistamines (sedating vs non-sedating) in dermatology Name the indications for and side-effects effects of anti-androgens androgens and imiquimod 1
2 Drugs To Be Discussed1 Antifungals: Griseofulvin Terbinafin Fluconazole Itraconazole Ketoconazole Corticosteroids: Topical Systemic Chloroquine Drugs To Be Discussed2 Retinoids: Topical Systemic Benzoyl peroxide Shampoos Barriers Antibiotics: Topical Systemic Antivirals: Acyclovir Podophyllin Antiscabies: Benzoyl benzoate 2
3 Drugs To Be Discussed3 Antihistamines Anti-androgens Imiquimod Griseofulvin Terbinafin Fluconazole Itraconazole Ketoconazole Antifungals 3
4 Griseofulvin Only active against dermatophytes (keratolytic fungi) Fungistatic Absorbed with fatty food (milk) Very safe in children mg per kg per day Terbinafin Only active against dermatophytes Fungicidal Tablets and cream Some severe immunological side-effects effects 4
5 Broad spectrum Fungistatic Fluconazole Convenient once per week dosage Can be used in neonates Used for: Candida 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 dermatophytes 5
6 Ketoconazole Broad spectrum Fungistatic To be taken with meals Tablets, cream and shampoo available Used for: Seborrheic dermatitis Pityriasis versicolor Candidiasis Side-effects: effects: Liver toxicity P450 inducer Imidazole Creams Variety available Similar spectra Little to choose Price deciding factor E.g.. Ketoconazole, econazole, clotrimazole 6
7 Corticosteroids Topical Systemic Topical Corticosteroids 3 Strengths Fluorinated vs Non-fluorinated Ointments, Creams, Lotions, Shampoos 7
8 Topical Corticosteroids Ointments: More potent Penetrates deeper More atrophy Used for: Dry lesions Thick lesions Thick skin Topical Corticosteroids Creams: Less potent Penetrates less Less atrophy Used for: Acute, thin lesions Moist lesions Thin skin (Face, skin folds) 8
9 Topical Corticosteroids Lotions: Least potent, least atrophy Used for: Hairy areas (scalp) Wet lesions (Watery solutions) Topical Corticosteroids Shampoos Clobetasol: Used for psoriasis of the scalp 9
10 Systemic Corticosteroids Prednisone / Prednisolone Potent, fast acting anti-inflammatoryinflammatory Cheap Side-effects: effects: Short term: Almost none Long term: Severe Used once daily, in the morning Chloroquine Indications: Cutaneous lupus erythematosus Porphyria cutanea tarda Side-effects: effects: Corneal deposits (Temporary) Maculopathy (Permanent) Other 10
11 Topical: Tretinoin Retinoids Adapalene Tazarotene Comedolytic, anti-inflammatoryinflammatory Indications: Acne (All forms) Anti-aging Other Retinoids Systemic: Isotretinoin Acitretin Indications: Acne Psoriasis Lymphomas Many others Side-effects, effects, etc: See acne lecture 11
12 Benzoyl peroxide Comedolytic, antiseptic Gel / Cream Superficial, inflammatory acne vulgaris Shampoos Ketoconazole: Seborrheic dermatitis Pityriasis versicolor Coal tar (LPC): Psoriasis (Not for tinea capitis) Povidone iodine (Betadine) Selenium sulfide (Selsun) Zinc pyrithione 12
13 Barriers Zinc/Castor oil BP: Nappy rash Antibiotics Topical: Mupirocin Fucidic acid Gentamycin Erythromycin Clindamycin Systemic: Tetracyclines (oxytetracycline, doxycycline, minocycline, lymecycline) Penicillins (amoxycillin, cloxacillin, amoxycillin-clavulanic clavulanic acid Erythromycin 13
14 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 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) 14
15 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 (Cream useless on skin) Side-effects: effects: Practically none Podophyllin: 25% in TBCo: Used for condylomata acuminata and verrucae 15
16 Benzoyl benzoate Antiscabies Only effective treatment for scabies Method of use: See lecture on skin infections Antihistamines Sedating: Promethazine Chlorpheniramine Hydroxyzine (Aterax ) 16
17 Antihistamines Sedating: Promethasine Chlorpheniramine Hydroxyzine (Aterax ) Used for: Atopic dermatitis Acute urticaria Other forms of night-time time pruritus Antihistamines Sedating: Promethasine Chlorpheniramine Hydroxyzine (Aterax ) Used for: Atopic dermatitis Acute urticaria Other forms of night-time time pruritus Side-effects: effects: Sedation (NB: Driving) Photo-allergy (not hydroxyzine) Dry mouth 17
18 Antihistamines Non-sedating: Loratidine Cetirizine Desloratidine Levocetirizine Used for: Acute and chronic urticaria Allergic rhinitis Side-effects: effects: Almost none Anti-androgens Cyproterone acetate Progestogen, blocks 5α-reductase 2mg in Diane-35 10mg in Androcur Used mostly for acne Side-effects: effects: Depression, weight gain Drosperinone Ingredient of Yasmin 18
19 Imiquimod (Aldara ) Topical immunostimulant Used for condylomata acuminata Superficial spreading basal cell CA Side-effects: effects: Severe local inflammation 19
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