Gynazole-1
Gynazole-1 - General Information
Gynazole-1 is an imidazole antifungal used in gynecology.
Pharmacology of Gynazole-1
Gynazole-1 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 candidasis.
Gynazole-1 for patients
WARNINGS
This cream contains mineral oil. Mineral oil may weaken latex or rubber products such as condoms or vaginal contraceptive diaphragms; therefore, use of such products within 72 hours following treatment with GYNAZOLE·1ô is not recommended.
Recurrent vaginal yeast infections, especially those that are difficult to eradicate, can be an early sign of infection with the human immunodeficiency virus (HIV) in women who are considered at risk for HIV infection.
PRECAUTIONS
General
If clinical symptoms persist, tests should be repeated to rule out other pathogens, to confirm the original diagnosis, and rule out other conditions that may predispose a patient to recurrent vaginal fungal infections.
Carcinogenesis, Mutagenesis, Impairment of Fertility
Carcinogenesis: Long term studies in animals have not been performed to evaluate the carcinogenic potential of this drug.
Mutagenicity: Butoconazole nitrate was not mutagenic when tested in the Ames bacterial test, yeast, chromosomal aberration assay in CHO cells, CHO/HGPRT point mutation assay, mouse micronucleus, and rat dominant lethal assays.
Impairment of Fertility: No impairment of fertility was seen in rabbits or rats administered butoconazole nitrate in oral doses up to 30 mg/kg/day (5 times the human dose based on mg/M 2 ) or 100 mg/kg/day (10 times the human dose based on mg/M 2 ), respectively.
Pregnancy
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.
Butoconazole nitrate has no apparent adverse effect when administered orally to pregnant rats throughout organogenesis at dose levels up to 50 mg/kg/day (5 times the human dose based on mg/M 2 ). Daily oral doses of 100, 300 or 750 mg/kg/day (10, 30 or 75 times the human dose based on mg/M 2 respectively) resulted in fetal malformations (abdominal wall defects, cleft palate), but maternal stress was also evident at these higher dose levels. There were, however, no adverse effects on litters of rabbits who received butoconazole nitrate orally, even at maternally stressful dose levels (e.g., 150 mg/kg, 24 times the human dose based on mg/M 2 ).
Butoconazole nitrate, like other azole anti-fungal agents, causes dystocia in rats when treatment is extended through parturition. However, this effect was not apparent in rabbits treated with as much as 100 mg/kg/day orally (16 times the human dose based on mg/M 2 ).
There are, however, no adequate and well-controlled studies in pregnant women. GYNAZOLE·1ô should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
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.
Gynazole-1 Interactions
Gynazole-1 Contraindications
Butoconazole Nitrate is contraindicated in patients with a history of hypersensitivity to any of the components of the product.
Additional information about Gynazole-1
Gynazole-1 Indication: For the local treatment of vulvovaginal candidiasis (infections caused by Candida)
Mechanism Of Action: 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Butoconazole
Synonyms: Butoconazol [INN-Spanish]; Butoconazole nitrate; Butoconazolum [INN-Latin]
Drug Category: Antifungal Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Butoconazole: Femstat; Femstat 3; Gynazole-1;
Absorption: 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.
Toxicity (Overdose): Oral, rat: LD50 = >1720 mg/kg.
Protein Binding: Not Available
Biotransformation: Not Available
Half Life: Not Available
Dosage Forms of Gynazole-1: Cream Intravaginal
Chemical IUPAC Name: 1-[4-(4-chlorophenyl)-2-(2,6-dichlorophenyl)sulfanylbutyl]imidazole
Chemical Formula: C19H17Cl3N2S
Butoconazole on Wikipedia: https://en.wikipedia.org/wiki/Butoconazole
Organisms Affected: Fungi, yeast and protozoans
