Naftin

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Naftin

Classes

Topical Dermatological Antifungals

Administration
Topical Administration

For topical dermatologic use only; not for ophthalmic, oral, or intravaginal use.
Wash hands before and after application. When treating hand infections, do not wash patient's hands after application. Use gloves for topical application if required by universal precautions.
Rub topical cream or gel gently into the affected area(s). Apply an amount sufficient to cover the affected area and the immediate (approximately a 0.5 inch margin) surrounding skin. Avoid getting in the eyes, nose, mouth, or other mucous membranes.
Avoid occlusive dressing of the affected areas unless otherwise directed by the prescriber.
Improvement of dermal tinea infection is gradual, and improvements in the treated condition may continue for weeks after naftifine therapy is discontinued. The manufacturer recommends that patients not be considered therapeutic failures until 2 to 4 weeks of therapy have passed.

Adverse Reactions
Severe

agranulocytosis / Delayed / Incidence not known

Moderate

erythema / Early / 0.5-0.5
contact dermatitis / Delayed / Incidence not known
leukopenia / Delayed / Incidence not known

Mild

skin irritation / Early / 2.0-5.0
rash / Early / 0.5-0.5
pruritus / Rapid / 1.0
dizziness / Early / Incidence not known
headache / Early / Incidence not known

Common Brand Names

Naftin, Naftin-MP

Dea Class

Rx

Description

Topical allylamine antifungal
Indicated for the interdigital tinea pedis, tinea cruris, and tinea corporis
Similar efficacy and adverse events profiles to topical azole antifungals

Dosage And Indications
For the treatment of tinea cruris. Topical dosage (1% gel)

NOTE: Indicated for infections caused by Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, and Epidermophyton floccosum.

Adults

Gently massage into the affected area and surrounding skin twice daily (morning and evening). Therapeutic response may be delayed; reevaluate if no clinical improvement is observed after 4 weeks of treatment. Instruct patients to discontinue treatment if irritation or sensitivity develops.

Topical dosage (1% cream)

NOTE: Indicated for infections caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.

Adults

Gently massage into the affected area and surrounding skin once daily. Therapeutic response may be delayed; reevaluate if no clinical improvement is observed after 4 weeks of treatment. Instruct patients to discontinue treatment if irritation or sensitivity develops.

Topical dosage (2% cream)

NOTE: Indicated for infections caused by Trichophyton rubrum.

Adults, Adolescents, and Children 12 years and older

Gently massage into the affected area and approximately 0.5 inches of surrounding skin once daily for 2 weeks. Instruct patients to discontinue treatment if irritation or sensitivity develops. During clinical trials, 25% of patients with tinea cruris were completely cured following 2 weeks of treatment with the 2% cream; mycological cure rate was 72%.

For the treatment of interdigital tinea pedis. Topical dosage (1% gel)

NOTE: Indicated for infections caused by Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, and Epidermophyton floccosum.

Adults

Gently massage into the affected area and surrounding skin twice daily (morning and evening). Therapeutic response may be delayed; reevaluate if no clinical improvement is observed after 4 weeks of treatment. Instruct patients to discontinue treatment if irritation or sensitivity develops.

Topical dosage (2% gel)

NOTE: Indicated for infections caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.

Adults, Adolescents, and Children 12 years and older

Gently massage into the affected area and surrounding skin once daily for 2 weeks. Instruct patients to discontinue treatment if irritation or sensitivity develops.

Topical dosage (1% cream)

NOTE: Indicated for infections caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.

Adults

Gently massage into the affected area and surrounding skin once daily. Therapeutic response may be delayed; reevaluate if no clinical improvement is observed after 4 weeks of treatment. Instruct patients to discontinue treatment if irritation or sensitivity develops.

Topical dosage (2% cream)

NOTE: Indicated for infections caused by Trichophyton rubrum.

Adults, Adolescents, and Children 12 years and older

Gently massage into the affected area and approximately 0.5 inches of the surrounding skin once daily for 2 weeks. Instruct patients to discontinue treatment if irritation or sensitivity develops. During clinical trials, 18% of patients with interdigital tinea pedis were completely cured following 2 weeks of treatment with the 2% cream; mycological cure rate was 67%.

For the treatment of tinea corporis. Topical dosage (1% gel)

NOTE: Indicated for infections caused by Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, and Epidermophyton floccosum.

Adults

Gently massage into the affected area and surrounding skin twice daily (morning and evening). Therapeutic response may be delayed; reevaluate if no clinical improvement is observed after 4 weeks of treatment. Instruct patients to discontinue treatment if irritation or sensitivity develops.

Topical dosage (1% cream)

NOTE: Indicated for infections caused by Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.

Adults

Gently massage into the affected area and surrounding skin once daily. Therapeutic response may be delayed; reevaluate if no clinical improvement is observed after 4 weeks of treatment. Instruct patients to discontinue treatment if irritation or sensitivity develops.

Topical dosage (2% cream)

NOTE: Indicated for infections caused by Trichophyton rubrum.

Adults, Adolescents, and Children 2 years and older

Gently massage into the affected area and approximately 0.5 inches of surrounding skin once daily for 2 weeks. Instruct patients to discontinue treatment if irritation or sensitivity develops. During clinical trials, 46% of patients with tinea cruris were completely cured following 2 weeks of treatment with the 2% cream; mycological cure rate was 63%.

For the treatment of distal subungual onychomycosis† or white superficial onychomycosis† (tinea unguium) due to susceptible dermatophytes (i.e., Trichophyton rubrum) or Candida species in patients unable to tolerate oral antifungal therapy. Topical dosage (1% gel)

NOTE: Naftifine gel has not been shown to be effective for onychomyosis of the toenail.

Adults

Gently massage the 1% topical gel into the affected fingernail area twice a day for at least 6 months. Monthly nail trimming and debridement should accompany topical antifungal nail treatment. Clinical cure has been observed in 40 to 80% of patients.

†Indicates off-label use

Dosing Considerations
Hepatic Impairment

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Renal Impairment

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

Drug Interactions

There are no drug interactions associated with Naftifine products.

How Supplied

Naftifine Hydrochloride/Naftin Topical Gel: 1%, 2%
Naftifine Hydrochloride/Naftin/Naftin-MP Topical Cream: 1%, 2%

Maximum Dosage
Adults

No maximum dosage information is available.

Geriatric

No maximum dosage information is available.

Adolescents

No maximum dosage information is available for the 2% gel or 2% cream; safety and efficacy have not been established for all other formulations.

Children

12 years: No maximum dosage information is available for the 2% gel or 2% cream; safety and efficacy have not been established for all other formulations.
2 to 11 years: No maximum dosage information is available for the 2% cream; safety and efficacy have not been established for all other formulations
< 2 years: Safety and efficacy have not been established.

Infants

Safety and efficacy have not been established.

Neonates

Safety and efficacy have not been established.

Mechanism Of Action

Naftifine exerts its antifungal effect by selective inhibition of the enzyme squalene 2,3-epoxidase, a key enzyme in ergosterol biosynthesis in fungi. Typically, squalene is transformed into ergosterol in the fungus. Ergosterol is a component of fungal membranes necessary for normal cell growth and function. The inhibition of the enzyme creates a deficiency in ergosterol and an accumulation of squalene. An abundance of squalene leads to cell death due to a decrease in phospholipid and glycoprotein synthesis and membrane destruction. Naftifine has fungicidal activity against dermatophytes, and exhibits fungistatic activity against Candida sp. At higher concentrations, naftifine can be fungicidal against Candida sp. Naftifine does not inhibit human sterol production. Naftifine has also been shown to possess local bactericidal properties against both gram-positive and gram-negative bacteria. The excellent anti-inflammatory properties of naftifine appear to be due to vasoconstriction via inhibition of inflammatory mediators, such as prostaglandins, leukotrienes, and histamine. Research also suggests that the allylamine antifungals, like naftifine, may enhance selected functions of polymorphonuclear leukocytes.

Pharmacokinetics

Naftifine is administered topically. Following topical application, measurable concentrations of naftifine are absorbed into the plasma and the drug penetrates the stratum corneum in sufficient quantities to inhibit growth of dermatophytes; however, it is not known if naftifine distributes into human milk or crosses the placenta. Roughly 14 to 29% of the absorbed dose is metabolized in the liver. Up to 64% of an absorbed dose and its metabolites is excreted in the urine and 36% in the bile. The metabolites have no pharmacologic activity. Unlike the imidazoles, the allylamine group of antifungals has limited effect on the cytochrome P450 enzyme system. Naftifine has a half-life of approximately 2 to 3 days.
 
Affected cytochrome P450 enzymes and drug transporters: None

Topical Route

Up to 4.2% and 6% of naftifine gel and cream, respectively, are absorbed after single applications to the skin.

Pregnancy And Lactation
Pregnancy

There are no available data on naftifine use during human pregnancy to evaluate a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal studies, no adverse effects on embryofetal development were observed with oral doses up to 37-times the maximum recommended human dose (MRHD) administered during organogenesis to pregnant rats or subcutaneous doses up to 4- and 7-times MRHD administered during organogenesis to pregnant rats and rabbits, respectively.[55334]

There is no information available on the presence of naftifine in human milk, the effects of the drug on the breast-fed infant, or the effects of the drug on milk production after topical application to women who are breast-feeding. The lack of clinical data precludes a clear determination regarding the risk of naftifine to a nursing infant. Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for naftifine and any potential adverse effects on the breast-fed infant from naftifine or the underlying maternal condition. Based on data that roughly 3% of the drug is absorbed systemically, it was predicted that a breast-feeding infant may ingest 0.3 mcg/kg from human milk. To minimize infant exposure, advise lactating mothers to avoid topical naftifine application to the breast area. Clotrimazole and miconazole may be potential alternatives to consider during breast-feeding. However, assess the site of infection, local susceptibility patterns, and specific microbial susceptibility before choosing an alternative agent.[26994] [48145] [48147] [40267] [40140] [55334]