Comparative Pharmacology
Head-to-head clinical analysis: GRISEOFULVIN ULTRAMICROSIZE versus LAMISIL AT.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GRISEOFULVIN ULTRAMICROSIZE versus LAMISIL AT.
GRISEOFULVIN, ULTRAMICROSIZE vs LAMISIL AT
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.
Terbinafine inhibits squalene epoxidase, an enzyme in the fungal ergosterol biosynthesis pathway. This leads to accumulation of squalene and depletion of ergosterol, disrupting fungal cell membrane integrity and causing cell death.
250-375 mg orally once daily or 500-750 mg orally once daily for severe infections.
Terbinafine 250 mg orally once daily for 6 weeks for fingernail onychomycosis or 12 weeks for toenail onychomycosis. Topical: 1% cream applied once daily for 1 week for tinea pedis; 1% solution applied once daily for 1 week for tinea corporis/cruris.
None Documented
None Documented
9-24 hours (mean 15 hours); prolonged in liver disease.
The terminal elimination half-life is approximately 11-17 hours in healthy adults; however, it increases to about 200-400 hours in the distribution phase from tissues (e.g., skin, adipose). Steady-state is reached after 10-14 days of oral dosing.
Renal (<1% unchanged); fecal (36% as metabolites); tissue deposition may persist for weeks.
Terbinafine is extensively metabolized in the liver; approximately 80% of a dose is excreted in urine as metabolites, and 20% in feces. Less than 1% is excreted unchanged in urine.
Category D/X
Category C
Antifungal
Antifungal