Comparative Pharmacology
Head-to-head clinical analysis: GRIS PEG versus LAMISIL AT.
Head-to-head clinical analysis: GRIS PEG versus LAMISIL AT.
GRIS-PEG vs LAMISIL AT
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Griseofulvin binds to and disrupts microtubule function by interfering with the polymerization of tubulin, thereby inhibiting fungal cell mitosis and nucleic acid synthesis.
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.
For tinea capitis and other dermatophyte infections: 500 mg oral daily as a single dose or in divided doses. For more severe infections, up to 1 g daily in divided doses.
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 14-24 hours. With continuous therapy, time to steady-state is ~3-5 days.
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 renal (as glucuronide conjugates): ~80%; fecal/biliary: ~10-15%; unchanged drug <1%.
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