Comparative Pharmacology
Head-to-head clinical analysis: DIFLUCAN IN DEXTROSE 5 IN PLASTIC CONTAINER versus LAMISIL AT.
Head-to-head clinical analysis: DIFLUCAN IN DEXTROSE 5 IN PLASTIC CONTAINER versus LAMISIL AT.
DIFLUCAN IN DEXTROSE 5% IN PLASTIC CONTAINER vs LAMISIL AT
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Diflucan (fluconazole) inhibits fungal cytochrome P450 14α-demethylase (CYP51), blocking the conversion of lanosterol to ergosterol, a key component of the fungal cell membrane. This disrupts membrane integrity and function, leading to fungal cell death. At high concentrations, it may also directly damage fungal membranes.
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 IV loading dose, then 100-200 mg IV once daily; for invasive candidiasis, 800 mg IV loading dose then 400 mg IV once daily.
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 30 hours (range 20-50 hours) in adults with normal renal function; prolonged to 98 hours in end-stage renal disease, requiring dose adjustment.
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.
Approximately 80% of the dose is excreted unchanged in urine via glomerular filtration and tubular secretion; about 11% is excreted as metabolites in urine; fecal excretion accounts for less than 5%.
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