ANTIFUNGAL DRUGS FOR CUTAENOUS MYCOTIC INFECTION Flashcards
What are the three different fungi that causes majority if cutaneous infection?
- Trichophyton
- Microsporum
- Epidermorphyton
It is a mold-like fungi that causes cutaneous infection
dermatophytes or tinea
Most common site is tinea pedis
What is the 1st drug of choice for dermatophyte?
Squalene epoxidase inhibitors
what are the 3 squalene epoxidase inhibitor?
- Terbinafine
- Naftifine
- Butenafine
MOA of Squalene epoxidase inhibitors
Inhibition of the enzyme squalene epoxidase that converts squalene to squalene oxide thereby blocking production of ergosterol
What is the drug of choice for treating dermatophyte oncychomycoses (fungal infections of nails)?
Terbinafine
spectrum of terbinafine
- effective against Trichophyton than either itraconazole or griseofulvin
Pharmacokinetics of terbinafine
- prolong therepy (3 months)
- Oral administration may be used for tinea capitis (infection in scalp)
-Topical terbinafine - tinea pedis, tinea corporis (ringworm), tinea cruris (“jock itch) and tinea versicolor dure to malassezia furfur
Adverse effect of terbinafine
- diarrhea
- dyspepsia
- nausesa
- headache
- rash
what drugs is allylamines?
- terbinafine
- NAftifine
Inhibition of the enzyme squalene epoxidase that converts squalene to squalene oxide
They are extensively metabolized by P450s, very greasy so low solubility leading to low bioavailability
Which CYP enzyme does terbinafine inhibit
CYP2D6
Oral use for terbinafine
Nail infections
Which drugs are non-allylamines squalene epoxidase inhibitors
Butenafine and Tolnaftate
naftifine administration
- cream and gel for 2 to 4 weeks
Target:
- tinea corporis, tinea cruris, and tinea pedis
Butenafine spectrum
Broader spectrum than tolnaftate and allylamines.
- Trichophyton rubrum, Epidermophyton and Malassezia
A drug that causes disruption of the mitotic spindle and inhibition of fungal mitosis
Griseofulvin
griseofulvin is replaced by? in treating onychomycosis?
terbinafine
because griseofulvin requires a long duration (6 to 12 weeks)
contraindication of griseofulvin
pregancy and patients with porphyria
what three species cause these mycoses?
epidermophyton spp, trichophyton spp, microsporum spp
it is a polyene antifungal
Nystatin
what antifungal drug resembles amphotericin B
Nystatin
spectrum of nystatin
cutaneous and oral candida infections
Pharmacokinetics of nystatin
administered orally,
Treatment of
oropharyngeal candidiasis, intravaginally for vulvovaginal candidiasis and topically for cutaneous candidaiasis
