NAFTIN - naftifine hydrochloride cream 
Merz Pharmaceuticals LLC

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NAFTIN® 
NAFTIFINE HCl 1% CREAM

Rx Only

DESCRIPTION

Naftin® Cream, 1% contains the synthetic, broad-spectrum, antifungal agent naftifine hydrochloride. Naftin® Cream, 1% is for topical use only.

Chemical Name:

(E)-N-Cinnamyl-N-methyl-1- naphthalenemethylamine hydrochloride. Naftifine hydrochloride has an empirical formula of C21H21N•HCl and a molecular weight of 323.86.

Structural Formula

naftifine hydrochloride

Active Ingredient:

Naftifine hydrochloride . . . . . . . . . . . . . 1%

Inactive Ingredients: benzyl alcohol, cetyl alcohol, cetyl esters wax, isopropyl myristate, polysorbate 60, purified water, sodium hydroxide, sorbitan monostearate, and stearyl alcohol. Hydrochloric acid may be added to adjust pH.

CLINICAL PHARMACOLOGY

Naftifine hydrochloride is a synthetic allylamine derivative. The following in vitro data are available, but their clinical significance is unknown. Naftifine hydrochloride has been shown to exhibit fungicidal activity in vitro against a broad spectrum of organisms, including Trichophyton rubrum, Trichophyton mentagrophytes, Trichophyton tonsurans, Epidermophyton floccosum, Microsporum canis, Microsporum audouini, and Microsporum gypseum; and fungistatic activity against Candida species, including Candida albicans. Naftin® Cream, 1% has only been shown to be clinically effective against the disease entities listed in the INDICATIONS AND USAGE section.

Although the exact mechanism of action against fungi is not known, naftifine hydrochloride appears to interfere with sterol biosynthesis by inhibiting the enzyme squalene 2, 3-epoxidase. This inhibition of enzyme activity results in decreased amounts of sterols, especially ergosterol, and a corresponding accumulation of squalene in the cells.

Pharmacokinetics

In vitro and in vivo bioavailability studies have demonstrated that naftifine penetrates the stratum corneum in sufficient concentration to inhibit the growth of dermatophytes.

Following a single topical application of 1% naftifine cream to the skin of healthy subjects, systemic absorption of naftifine was approximately 6% of the applied dose. Naftifine and/or its metabolites are excreted via the urine and feces with a half-life of approximately two to three days.

INDICATIONS AND USAGE

Naftin® Cream, 1% is indicated for the topical treatment of tinea pedis, tinea cruris and tinea corporis caused by the organisms Trichophyton rubrum, Trichophyton mentagrophytes, and Epidermophyton floccosum.

CONTRAINDICATIONS

Naftin® Cream, 1% is contraindicated in individuals who have shown hypersensitivity to any of its components.

WARNINGS

Naftin® Cream, 1% is for topical use only and not for ophthalmic use.

PRECAUTIONS

General

Naftin® Cream, 1% is for external use only. If irritation or sensitivity develops with the use of Naftin® Cream, 1%, treatment should be discontinued and appropriate therapy instituted. Diagnosis of the disease should be confirmed either by direct microscopic examination of a mounting of infected tissue in a solution of potassium hydroxide or by culture on an appropriate medium.

Information for patients

The patient should be told to:

1. Avoid the use of occlusive dressings or wrappings unless otherwise directed by the physician.
2. Keep Naftin® Cream, 1% away from the eyes, nose, mouth and other mucous membranes.

Carcinogenesis, mutagenesis, impairment of fertility

Long-term animal studies to evaluate the carcinogenic potential of Naftin® Cream, 1% have not been performed. In vitro and animal studies have not demonstrated any mutagenic effect or effect on fertility.

Pregnancy

Teratogenic Effects

Pregnancy Category B

Reproduction studies have been performed in rats and rabbits (via oral administration) at doses 150 times or more the topical human dose and have revealed no evidence of impaired fertility or harm to the fetus due to naftifine. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Nursing mothers

It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Naftin® Cream, 1% is administered to a nursing woman.

Pediatric use

Safety and effectiveness in pediatric patients have not been established.

ADVERSE REACTIONS

During clinical trials with Naftin® Cream, 1%, the incidence of adverse reactions was as follows: burning/stinging (6%), dryness (3%), erythema (2%), itching (2%), local irritation (2%).

DOSAGE AND ADMINISTRATION

A sufficient quantity of Naftin® Cream, 1% should be gently massaged into the affected and surrounding skin areas once a day. The hands should be washed after application. If no clinical improvement is seen after four weeks of treatment with Naftin® Cream, 1%, the patient should be reevaluated.

HOW SUPPLIED

Naftin® (naftifine hydrochloride) 1% Cream is supplied in the following sizes:

 

15g – NDC 0259-4126-15 (tube)

 

30g – NDC 0259-4126-30 (tube)

 

60g – NDC 0259-4126-60 (tube)

 

60g – NDC 0259-4126-04 (tubes 4×15g multi-pack)

 

90g – NDC 0259-4126-90 (tube)

 

 

30g – NDC 0259-4126-03 (pump)

 

90g – NDC 0259-4126-09 (pump)

Tubes:	Store below 30°C (86°F).
Pumps:	Store at controlled room temperature: 25°C (77°F);
	excursions permitted between 15°-30°C (59°-86°F).

Manufactured for: Merz Pharmaceuticals, Greensboro, NC 27410

© 2008 Merz Pharmaceuticals
Rev. 5/08 Printed in U.S.A.

5011316

NAFTIN  naftifine hydrochloride   cream

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 0259-4126 Route of Administration TOPICAL DEA Schedule

INGREDIENTS Name (Active Moiety) Type Strength naftifine hydrochloride (naftifine) Active 10 MILLIGRAM  In 1 GRAM benzyl alcohol Inactive   cetyl alcohol Inactive   cetyl esters wax Inactive   isopropyl myristate Inactive   polysorbate 60 Inactive   water Inactive   sodium hydroxide Inactive   sorbitan monostearate Inactive   stearyl alcohol Inactive   hydrochloric acid Inactive

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 0259-4126-15 1 TUBE In 1 CARTON contains a TUBE 1 15 g (GRAM) In 1 TUBE This package is contained within the CARTON (0259-4126-15) 2 0259-4126-30 1 TUBE In 1 CARTON contains a TUBE 2 30 g (GRAM) In 1 TUBE This package is contained within the CARTON (0259-4126-30) 3 0259-4126-04 4 TUBE In 1 CARTON contains a TUBE 3 15 g (GRAM) In 1 TUBE This package is contained within the CARTON (0259-4126-04) 4 0259-4126-60 1 TUBE In 1 CARTON contains a TUBE 4 60 g (GRAM) In 1 TUBE This package is contained within the CARTON (0259-4126-60) 5 0259-4126-90 1 TUBE In 1 CARTON contains a TUBE 5 90 g (GRAM) In 1 TUBE This package is contained within the CARTON (0259-4126-90) 6 0259-4126-03 1 BOTTLE In 1 CARTON contains a BOTTLE, PUMP 6 30 g (GRAM) In 1 BOTTLE, PUMP This package is contained within the CARTON (0259-4126-03) 7 0259-4126-09 1 BOTTLE In 1 CARTON contains a BOTTLE, PUMP 7 90 g (GRAM) In 1 BOTTLE, PUMP This package is contained within the CARTON (0259-4126-09)

Revised: 02/2009Merz Pharmaceuticals LLC