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.
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)
t1/2 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
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