Griseofulvin

Dr.Anup Goswami
Dept. of Dermatology
RIMS, Imphal

1. GRISEOFULVIN IN DERMATOLOGY Moderator: Prof. Th. Nandakishore Presenter: Dr. Anup Goswami

2. Griseofulvin Griseofulvin - antifungal antibiotic (isolated from Penicillium sp) It is a secondary metabolite produced by the fungus Penicillum griseofulvum . insoluble in water

3. Mode of action Fungistatic Inh fungal cell mitosis and nucleic acid syn Binds to fungal microtubes  altering fungal mitosis (metaphase) Active against most dermatophytes But not against Candida and other fungi causing deep mycosis.

4. Biosynthetic Pathway of Fungal Cell Membrane & Site of Action of other Antifungal Drugs

5. Pharmacokinetics Absorption : incompletely absorbed from the GI tract, increased by decreasing particle size and admin with fatty meals; -peak plasma conc > 4 hours (t-max) Distribution Keratin precursor cells, stratum corneum Protein-binding: 84%. Metabolism : Hepatic Excretion Renal (50 %), via faeces ( 36%), via sweat; 9-24 hours (elimination half-life) t 1/2 h : 9 – 24

6. Indications Treatment of following dermatophyte infections Tinea cruris : commonly referred to as jock itch, is a fungal infection in the groin area Tinea corporis : also known as ringworm Tinea pedis : known as Athlete's foot

7. Indications Tinea barbae : Superficial dermatophyte infection that is limited to the bearded areas of the face and neck and occurs almost exclusively in older adolescent and adult males Tinea capitis :  Fungal infection of the scalp. It is also called ringworm of the scalp

8. Indications Tinea unguium when caused by one or more of the following species of fungi: Epidermophyton floccosum Microsporum audouinii Microsporum gypseum Trichophyton crateriform Trichophyton gallinae Trichophyton interdigitalis schoenleini Trichophytum sulphureum Trichophytum tonsurans Trichophytum verrucosum Trichophyton megnini Trichophyton mentagrophytes Trichophyton rubrum Trichophyton

9. Dosage Oral: Dermatophytosis Adult: 0.5-1 g daily in single or divided doses for Child: 10-15 mg/kg daily. Food (before/after) Should be taken with food. (Take immediately after meals.) Infection Dose Tinea capitis 4 – 6 weeks Tinea corporis 2 – 4 weeks Tinea pedis 4 – 8 weeks Tinea unguium ( onychomycosis ) Finger- atleast 4 mnths Toe- atleast 6 mnths

10. Griseofulvin is not effective in the following: 1. Superficial mycosis: candidiasis tinea versicolor 2. Deep mycosis: - sporotrichosis histoplasmosis Chromoblastomycosis blastomycosis actinomycosis coccidioidomycosis nocardiosis

11. Contraindications Griseofulvin is contraindicated in severe hepatic disease Pregnancy (category C) porphyria monilial infection systemic lupus  erythematosus

12. Adverse Effects Allergic reactions Nausea & diarrhea Headache Sleep disturbances Lathergy Photosensitivity Disulfirum like reaction

13. Clinical Trial Fungal infection: Tinea capitis (TC) Fungus: Trichophyton violaceum n = 75 International Journal of Dermatology 2012, 51, 455–458 Drug Griseofulvin Terbinafine Fluconazole Number of patients 25 25 25 Cure rate (%) 96 88 84 Griseofulvin remains the drug of choice in the treatment of TC

14. Clinical Trial Treatment of " tinea pedis " with  griseofulvin  and topical antifungal cream Condition Treatment Outcome Plantar scaling type of tinea pedis Combination was not better than  griseofulvin  alone Intertriginous tinea pedis Combination was definitely better than  griseofulvin  alone Topical 1 percent clotrimazole was much less effective than  griseofulvin . Ref. Cutis. 1978 Aug;22(2):197-9 Combination: oral griseofulvin , topical clotrimazole

15. THANK YOU