Gynazole-1

Uses

Gynazole-1 vaginal cream is used for the local treatment of vulvovaginal candidiasis (infections caused by Candida). The diagnosis should be confirmed by KOH smears and/or cultures. Gynazole-1 vaginal cream is safe and effective in non-pregnant women; however, the safety and effectiveness of this product in pregnant women has not been established.

Gynazole-1 is also used to associated treatment for these conditions: Vulvovaginal Candidiasis

How Gynazole-1 works

The exact mechanism of the antifungal action of butoconazole is unknown, however, it is presumed to function as other imidazole derivatives via inhibition of steroid synthesis. Imidazoles generally inhibit the conversion of lanosterol to ergosterol via the inhibition of the enzyme cytochrome P450 14α-demethylase, resulting in a change in fungal cell membrane lipid composition. This structural change alters cell permeability and, ultimately, results in the osmotic disruption or growth inhibition of the fungal cell.

Dosage

Gynazole-1 dosage

The recommended dose of Gynazole-1 is one applicatorful of cream (approximately 5 grams of the cream) intravaginally. This amount of cream contains approximately 100 mg of butoconazole nitrate.

Side Effects

Of the 314 patients treated with Gynazole-1 for 1 day in controlled clinical trials, 18 patients (5.7%) reported complaints such as vulvar/vaginal burning, itching, soreness and swelling, pelvic or abdominal pain or cramping, or a combination of two or more of these symptoms. In 3 patients (1%) these complaints were considered treatment-related. Five of the 18 patients reporting adverse events discontinued the study because of them.

Toxicity

Oral, rat: LD₅₀ = >1720 mg/kg.

Precaution

If clinical symptoms persist, tests should be repeated to rule out pathogens, to confirm the original diagnosis, and to rule out other conditions that may predispose a patient to recurrent vaginal fungal infections.

Food Interaction

Elimination Route

Following vaginal administration of butoconazole nitrate vaginal cream, 2% to 3 women, 1.7% (range 1.3-2.2%) of the dose was absorbed on average.

Pregnancy & Breastfeeding use

Pregnancy Category C. In pregnant rats administered 6 mg/kg/day of butoconazole nitrate intravaginally during the period of organogenesis, there was an increase in resorption rate and decrease in litter size; however, no teratogenicity was noted. This dose represents a 130- to 353-fold margin of safety based on serum levels achieved in rats following intravaginal administration compared to the serum levels achieved in humans following intravaginal administration of the recommended therapeutic dose of butoconazole nitrate.

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 butoconazole nitrate is administered to a nursing woman

Contraindication

Gynazole-1 is contraindicated in patients with a history of hypersensitivity to any of the components of the product.

Special Warning

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

Storage Condition

Store at 25°C

Innovators Monograph

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