Comparative Pharmacology
Head-to-head clinical analysis: KETOZOLE versus LAMISIL AT.
Peer-Reviewed Evidence
Head-to-head clinical analysis: KETOZOLE versus LAMISIL AT.
KETOZOLE vs LAMISIL AT
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Ketoconazole is an imidazole antifungal agent that inhibits fungal cytochrome P450 14α-demethylase, thereby blocking the conversion of lanosterol to ergosterol, a key component of the fungal cell membrane. This leads to increased membrane permeability and cell death.
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.
200 mg orally once daily with food.
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
Terminal elimination half-life is approximately 2 hours (range 1.5–3.5 hours). Clinically, duration of antifungal effect extends beyond plasma half-life due to persistent tissue levels.
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.
Primarily hepatic metabolism; renal excretion of unchanged drug <1%. Biliary/fecal excretion accounts for ~20-35% of metabolites.
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 C
Category C
Antifungal
Antifungal