NAFTIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for NAFTIN (NAFTIN).
Naftin (naftifine hydrochloride) is an allylamine antifungal agent that inhibits squalene epoxidase, blocking the conversion of squalene to lanosterol, thereby disrupting ergosterol synthesis in fungal cell membranes.
| Metabolism | Following topical application, systemic absorption is minimal (<6%). The absorbed fraction undergoes hepatic metabolism via cytochrome P450 enzymes, primarily oxidation and glucuronidation. |
| Excretion | Primarily hepatic via CYP450 metabolism; renal excretion of metabolites accounts for approximately 70-80% of elimination, with <1% excreted unchanged in urine. Fecal excretion accounts for 10-20%. |
| Half-life | Terminal elimination half-life is approximately 2-4 hours, but clinical effects persist longer due to lipophilic properties and tissue binding. Dosing intervals of 12-24 hours are recommended. |
| Protein binding | Approximately 80-85% bound to serum albumin. |
| Volume of Distribution | Apparent volume of distribution is approximately 1.4 L/kg, indicating extensive distribution into tissues including the stratum corneum, dermis, and sebaceous glands. |
| Bioavailability | Topical: Systemic bioavailability is <3% due to minimal percutaneous absorption; does not require dose adjustment for hepatic or renal impairment. |
| Onset of Action | Topical application: Onset of antifungal action occurs within 24-48 hours, with symptomatic improvement seen by 1 week. |
| Duration of Action | Duration of action after last dose: Clinical mycologic cure continues for up to 1-2 weeks after cessation of therapy. Relapse may occur if treatment is discontinued prematurely. |
| Molecular Weight | 293.4 |
Apply a thin layer to affected area and surrounding skin once daily (naftifine 1% cream) or twice daily (naftifine 1% gel) for 2-4 weeks, depending on infection type.
| Dosage form | CREAM |
| Renal impairment | No dose adjustment required for renal impairment. Naftifine is primarily topical with negligible systemic absorption. |
| Liver impairment | No dose adjustment required for hepatic impairment due to minimal systemic absorption. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established; use only if clearly needed. |
| Geriatric use | No specific dose adjustment; apply same as adult dosing. Elderly may use thinning skin precautions. |
| 1st trimester | There are no adequate and well-controlled studies in pregnant women. NAFTIN (naftifine hydrochloride) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. |
| 2nd trimester | Same as T1: no adequate studies; use only if clearly needed. |
| 3rd trimester | Same as T1: no adequate studies; use only if clearly needed. |
Clinical note
Comprehensive clinical and safety monograph for NAFTIN (NAFTIN).
| Placental transfer | Unknown; no data available on placental transfer in humans. |
| Breastfeeding | It is not known whether naftifine is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when NAFTIN is administered to a nursing woman. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to naftifine hydrochloride or any component of the formulation
| Precautions | For external use only., Avoid contact with eyes, nose, mouth, or mucous membranes., Discontinue if irritation or allergic reaction occurs., Use in pregnancy only if clearly needed (limited data). |
| Food/Dietary | No known food interactions. |
| Clinical Pearls | Apply once or twice daily for 4 weeks. Avoid occlusive dressings unless directed. For tinea pedis, continue treatment for 2 weeks after resolution. Not for ophthalmic or intravaginal use. |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | NAFTIN (naftifine hydrochloride) is not systemically absorbed to significant levels following topical application. Animal studies have not shown teratogenicity, and no adequate human studies exist. Systemic exposure is minimal, but as a precaution, use during pregnancy only if clearly needed. There is no known first, second, or third trimester risk based on limited data. |
| Fetal Monitoring | No specific maternal or fetal monitoring is required due to negligible systemic absorption. However, monitor for local skin reactions or allergic contact dermatitis at application site. |
| Fertility Effects | No known effects on fertility based on animal studies with topical application. No human data available. |
| Patient Advice | Apply a thin layer to affected and surrounding area. · Wash hands before and after application. · Do not use on eyes or inside vagina. · Complete full course even if symptoms improve. · Avoid covering area with bandage or wrap unless told by doctor. · Report any signs of irritation or allergy. |