黴菌感染 Treatment of onychomycosis and moccasin-type tinea pedis, cutaneous candidiasis

Antifungal Agent
Synthetic allylamine derivative that inhibits squalene epoxidase, a key enzyme in sterol biosynthesis in fungi. This results in a deficiency in ergosterol within the fungal cell membrane and results in fungal cell death.

Absorption:
1. Absorption: >70%
2. Bioavailability: 40% (as a result of first-pass metabolism)
3. Time to peak, plasma: Within 2 hours
Distribution:
1. Distributed to sebum and skin predominantly
2. Protein binding: (Plasma) >99%
Metabolism:
Hepatic predominantly via CYP1A2, 3A4, 2C8, 2C9, and 2C19 to inactive metabolites
Excretion:
1. Urine (80%, primarily as inactive metabolites); feces (20%)
2. Half-life elimination: (Terminal half-life) 200 to 400 hours; very slow release of drug from skin and adipose tissues occurs

1. Previous hypersensitivity to terbinafine or naftifine.
2. For patients with pre-existing liver disease or renal impairment, it is not recommended.

Not recommended

Avoid

Fatigue, headache, dizziness, gastrointestinal disturbances, skin rash, pruritus, alopecia, elevation of hepatic function tests

Superficial mycosis: 125 mg PO BID or 250 mg PO QD
Systemic mycosis: 250–500 mg PO QD

There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); however, clearance is decreased 50% in patients with CrCl ≤50 mL/minute.

Contraindicated in chronic or active hepatic disease