Naftifine (Monograph)

Brand name: Naftin
Drug class: Allylamines
ATC class: D01AE22
VA class: DE102
Chemical name: (E)-N-Methyl-N-(3-phenyl-2-propenyl)-1-naphthalenemethanamine hydrochloride
Molecular formula: C₂₁H₂₁N•HCl
CAS number: 65473-14-5

Introduction

Antifungal; synthetic allylamine structurally and pharmacologically related to terbinafine.

Uses for Naftifine

Dermatophytoses

Treatment of tinea corporis (body ringworm) and tinea cruris (jock itch) caused by Epidermophyton floccosum, Microsporum canis^{† [off-label]}, Trichophyton mentagrophytes, T. rubrum, T. tonsurans, T. verrucosum^{† [off-label]}, or T. violaceum^{† [off-label]}.

Treatment of tinea pedis (athlete's foot) or tinea manuum^{† [off-label]} caused by Epidermophyton floccosum, Microsporum canis^{† [off-label]}, Trichophyton mentagrophytes, T. rubrum, T. tonsurans, T. verrucosum^†, or T. violaceum^†.

Topical antifungals usually effective for treatment of uncomplicated tinea corporis and tinea cruris. An oral antifungal may be necessary when tinea corporis or tinea cruris is extensive, dermatophyte folliculitis is present, the infection is chronic or does not respond to topical therapy, or the patient is immunocompromised because of coexisting disease or concomitant therapy.

Topical antifungals usually effective for treatment of uncomplicated tinea pedis. An oral antifungal may be necessary for the treatment of hyperkeratotic areas on the palms and soles, for chronic moccasin-type (dry-type) tinea pedis, and for tinea unguium (fingernail or toenail dermatophyte infections, onychomycosis).

Gel has been used in the treatment of tinea unguium (onychomycosis)^†.

Cutaneous Candidiasis†

Treatment of cutaneous candidiasis^† caused by Candida albicans. Less active than imidazole derivatives.

Naftifine Dosage and Administration

Administration

Topical Administration

Apply topically to the skin as a cream or gel.

Do not apply to the eye, nose, mouth, or other mucous membranes.

Do not use with occlusive dressings or wrappings, unless otherwise directed by clinician.

Apply a sufficient amount of topical cream or gel; rub gently into the affected area and surrounding skin.

Wash hands after applying.

Dosage

Available as naftifine hydrochloride; dosage expressed in terms of naftifine.

Adults

Dermatophytoses

Tinea Corporis or Tinea Cruris

Topical

Cream: Apply once daily for 2–4 weeks.

Gel: Apply twice daily (morning and evening) for 2–4 weeks.

Clinical improvement usually occurs within the first week of treatment. If clinical improvement does not occur after 4 weeks of treatment, reevaluate diagnosis. Severe infections may require prolonged treatment.

Tinea Pedis

Topical

Cream: Apply once daily for 4–6 weeks.

Gel: Apply twice daily (morning and evening) for 4–6 weeks.

Clinical improvement usually occurs within the first week of treatment. If clinical improvement does not occur after 4 weeks of treatment, reevaluate diagnosis. Severe infections may require prolonged treatment.

Special Populations

No special population dosage recommendations at this time.

Cautions for Naftifine

Contraindications

• Known hypersensitivity to naftifine or any ingredient in the formulation.

Warnings/Precautions

Warnings

Administration Precautions

For external use only. Use only for topical application to the skin; not for ophthalmic use.

Avoid contact with eyes, nose, mouth, and other mucous membranes.

Sensitivity Reactions

Contact dermatitis has been reported occasionally.

If irritation or sensitivity occurs, discontinue drug and initiate appropriate therapy.

General Precautions

Selection and Use of Antifungals

Prior to use, confirm diagnosis by direct microscopic examination of scrapings from infected tissue mounted in potassium hydroxide (KOH) or by culture.

Specific Populations

Pregnancy

Category B.

Lactation

Not known whether distributed into milk following topical application. Use with caution.

Pediatric Use

Safety and efficacy not established.

Common Adverse Effects

Burning, stinging.

Drug Interactions

No formal drug interaction studies to date.

Naftifine Pharmacokinetics

Absorption

Bioavailability

Following topical application, approximately 3–6% absorbed.

Distribution

Extent

Not known whether naftifine crosses the placenta.

Distributed into milk in rats; not known whether distributed into human milk.

Elimination

Metabolism

Metabolized by oxidation and by N-dealkylation.

Elimination Route

Systemically absorbed drug excreted in urine (40–60%) as unchanged drug and metabolites and in feces.

Half-life

2–3 days.

Stability

Storage

Topical

Cream

<30°C; cream is stable for 24 months after the date of manufacture.

Gel

Room temperature.

Actions and Spectrum

• Allylamine antifungal.

• Usually fungicidal against susceptible dermatocytes. Usually fungistatic against Candida; may be fungicidal at high concentrations.

• Exact mechanism unknown; appears to interfere with sterol biosynthesis by inhibiting the enzyme squalene monooxygenase (squalene 2,3-epoxidase). The resulting accumulation of squalene (the usual substrate of the enzyme) in the cells and decreased amounts of sterols, especially ergosterol, may contribute to the antifungal effects.

• Spectrum of antifungal activity includes many fungi, including dermatophytes and yeasts. Also may have in vitro activity against some gram-positive and -negative bacteria, and Leishmania.

• Candida: Active in vitro against Candida albicans, C. krusei, C. parapsilosis, and C. tropicalis; however, less active than imidazole derivatives against Candida.

• Dermatophytes and other fungi: Active in vitro against Aspergillus flavus, A. fumigatus, Blastomyces dermatitidis, Cryptococcus neoformans, Epidermophyton floccosum, Histoplasma capsulatum, Microsporum audouinii, M. canis, M. gypseum, Petriellidium boydii, Sporothrix schenckii, Trichophyton mentagrophytes, T. rubrum, T. tonsurans, T. verrucosum, and T. violaceum.

• Also has anti-inflammatory activity when applied topically.

• No reports to date of resistance in organisms originally susceptible to naftifine.

Advice to Patients

• Importance of completing full course of treatment, even if symptoms improve.

• Importance of contacting clinician if improvement does not occur within 4 weeks.

• Importance of notifying clinician if condition worsens or treated area shows signs of increased irritation.

• Importance of applying to affected areas as directed and avoiding contact with eyes, nose, mouth, or other mucous membranes.

• Advise patients to wash their hands after touching the affected areas.

• Importance of not using occlusive dressings, unless otherwise directed by clinician.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.

• Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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