GYNAZOLE 1- butoconazole nitrate cream
Lumara Health, Inc.
GYNAZOLE 1�
Butoconazole Nitrate Vaginal Cream USP, 2%
IN ONE PREFILLED DISPOSABLE APPLICATOR
For Vaginal Use Only.
Rx Only
DESCRIPTION
GYNAZOLE � 1� Butoconazole Nitrate Vaginal Cream USP, 2% contains butoconazole nitrate 2%, an imidazole derivative with antifungal activity. Its chemical name is (�)-1-[4- (p-chlorophenyl)-2- [(2,6-dichlorophenyl) thio]butyl] imidazole mononitrate, and it has the following chemical structure:
8F200ZLJ1 Image 2.JPG
Butoconazole nitrate is a white to off-white crystalline powder with a molecular weight of 474.79. It is sparingly soluble in methanol; slightly soluble in chloroform, methylene chloride, acetone, and ethanol; very slightly soluble in ethyl acetate; and practically insoluble in water. It melts at about 159�C with decomposition.
GYNAZOLE � 1� Butoconazole Nitrate Vaginal Cream USP, 2% contains 2% butoconazole nitrate in a cream of edentate disodium, glyceryl monoisostearate, methylparaben, mineral oil, polyglyceryl-3 oleate, propylene glycol, propylparaben, colloidal silicon dioxide, sorbitol solution, purified water, and microcrystalline wax.
CLINICAL PHARMACOLOGY
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. Peak plasma levels (13.6-18.6 ng radioequivalents/mL of plasma) of the drug and its metabolites are attained between 12 and 24 hours after vaginal administration.
Microbiology -
The exact mechanism of the antifungal action of butoconazole nitrate 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, 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.
Butoconazole nitrate is an imidazole derivative that has fungicidal activity in vitro against Candida spp. and has been demonstrated to be clinically effective against vaginal infections due to Candida albicans. Candida albicans has been identified as the predominant species responsible for vulvovaginal candidiasis.
INDICATIONS AND USAGE
GYNAZOLE � 1� Butoconazole Nitrate Vaginal Cream USP, 2% is indicated for the local treatment of vulvovaginal candidiasis (infections caused by Candida). The diagnosis should be confirmed by KOH smears and/or cultures (see CLINICAL STUDIES).
Note: GYNAZOLE � 1� Butoconazole Nitrate Vaginal Cream USP, 2% is safe and effective in non-pregnant women; however, the safety and effectiveness of this product in pregnant women has not been established (see PRECAUTIONS - Pregnancy).
CONTRAINDICATIONS
