Comparative Pharmacology
Head-to-head clinical analysis: GRISEOFULVIN ULTRAMICROSIZE versus LAMISIL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GRISEOFULVIN ULTRAMICROSIZE versus LAMISIL.
GRISEOFULVIN, ULTRAMICROSIZE vs LAMISIL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Binds to tubulin, disrupting microtubule function and inhibiting fungal cell mitosis; deposited in keratin precursor cells, making keratin resistant to fungal invasion.
Allylamine antifungal that inhibits squalene epoxidase, an enzyme in the ergosterol biosynthesis pathway, leading to accumulation of squalene and disruption of fungal cell membrane function.
250-375 mg orally once daily or 500-750 mg orally once daily for severe infections.
250 mg orally once daily for 2-6 weeks for dermatophyte infections; 250 mg orally once daily for 12 weeks for onychomycosis.
None Documented
None Documented
9-24 hours (mean 15 hours); prolonged in liver disease.
Terminal elimination half-life is approximately 17-24 hours in healthy adults. However, it can prolong to about 36-40 hours in patients with renal or hepatic impairment. The prolonged half-life allows for once-daily dosing. Due to extensive tissue distribution, the functional half-life (terminal phase from tissues) may be longer.
Renal (<1% unchanged); fecal (36% as metabolites); tissue deposition may persist for weeks.
Approximately 70% of the administered dose is excreted in the urine as metabolites, with less than 5% as unchanged drug. About 20% is eliminated via feces. Terbinafine undergoes extensive hepatic metabolism; renal elimination of metabolites is the primary route.
Category D/X
Category C
Antifungal
Antifungal