Nizoral Description

NIZORALŪ (ketoconazole) 2% Shampoo is a red-orange liquid for topical application, containing the broad spectrum synthetic antifungal agent ketoconazole in a concentration of 2% in an aqueous suspension. It also contains: coconut fatty acid diethanolamide, disodium monolauryl ether sulfosuccinate, F.D.&C. Red No. 40, hydrochloric acid, imidurea, laurdimonium hydrolyzed animal collagen, macrogol 120 methyl glucose dioleate, perfume bouquet, sodium chloride, sodium hydroxide, sodium lauryl ether sulfate, and purified water.

Ketoconazole is cis -1-acetyl-4-[4-[[2-(2,4-dichlorophenyl)-2-(1 H -imidazol-1-ylmethyl)-1,3 - dioxolan-4-yl]methoxy]phenyl]piperazine and has the following structural formula:

Nizoral Indications And Usage

NIZORALŪ (ketoconazole) 2% Shampoo is indicated for the treatment of tinea (pityriasis) versicolor caused by or presumed to be caused by Pityrosporum orbiculare (also known as Malassezia furfur or M. orbiculare ).

Note: Tinea (pityriasis) versicolor may give rise to hyperpigmented or hypopigmented patches on the trunk which may extend to the neck, arms and upper thighs. Treatment of the infection may not immediately result in normalization of pigment to the affected sites. Normalization of pigment following successful therapy is variable and may take months, depending on individual skin type and incidental sun exposure. Although tinea versicolor is not contagious, it may recur because the organism that causes the disease is part of the normal skin flora.

Nizoral Contraindications

NIZORALŪ (ketoconazole) 2% Shampoo is contraindicated in persons who have shown hypersensitivity to the active ingredient or excipients of this formulation.

Nizoral Precautions

General: If a reaction suggesting sensitivity or chemical irritation should occur, use of the medication should be discontinued.

Information for Patients: May be irritating to mucous membranes of the eyes and contact with this area should be avoided.

There have been reports that use of the shampoo resulted in removal of the curl from permanently waved hair.

Carcinogenesis, Mutagenesis, Impairment Of Fertility

The dominant lethal mutation test in male and female mice revealed that single oral doses of ketoconazole as high as 80 mg/kg produced no mutation in any stage of germ cell development. The Ames Salmonella microsomal activator assay was also negative. A long-term feeding study of ketoconazole in Swiss Albino mice and in Wistar rats showed no evidence of oncogenic activity.

Pregnancy: Teratogenic Effects: Pregnancy Category C

Ketoconazole is not detected in plasma after chronic shampooing. Ketoconazole has been shown to be teratogenic (syndactylia and oligodactylia) in the rat when given orally in the diet at 80 mg/kg/day (10 times the maximum recommended human oral dose). However, these effects may be related to maternal toxicity, which was seen at this and higher dose levels.

There are no adequate and well-controlled studies in pregnant women. Ketoconazole should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing mothers: Ketoconazole is not detected in plasma after chronic shampooing. Nevertheless, caution should be exercised when NIZORALŪ (ketoconazole) 2% Shampoo is administered to a nursing woman.

Pediatric Use: Safety and effectiveness in children have not been established.

Nizoral Overdosage

NIZORALŪ (ketoconazole) 2% Shampoo is intended for external use only. In the event of accidental ingestion, supportive measures should be employed. Induced emesis and gastric lavage should usually be avoided.