GYNAZOLE-1
Clinical safety rating: caution
Comprehensive clinical and safety monograph for GYNAZOLE-1 (GYNAZOLE-1).
Butoconazole nitrate, an imidazole antifungal agent, inhibits fungal cytochrome P450 14α-demethylase, disrupting ergosterol synthesis and increasing fungal cell membrane permeability.
| Metabolism | Minimal systemic absorption; primarily metabolized in the liver via oxidation and conjugation pathways. |
| Excretion | Primarily as unchanged drug in feces via biliary elimination; <1% excreted renally as metabolites. |
| Half-life | Terminal elimination half-life is approximately 6-7 days after intravaginal administration, reflecting slow absorption from the vaginal mucosa and prolonged retention in tissues. |
| Protein binding | Approximately 99% bound, primarily to albumin. |
| Volume of Distribution | Systemic Vd not well defined due to minimal absorption; after IV administration in animals, Vd is approximately 1.3 L/kg, suggesting extensive tissue distribution. |
| Bioavailability | Intravaginal: approximately 2-5% systemically absorbed. |
| Onset of Action | Clinical effect (symptom relief) typically begins within 1-2 days after a single intravaginal dose. |
| Duration of Action | A single dose provides therapeutic effect for up to 7 days, with clinical cure rates maintained through 28 days. |
One 100 mg vaginal ovule inserted intravaginally as a single dose.
| Dosage form | CREAM |
| Renal impairment | No adjustment required for renal impairment. |
| Liver impairment | No adjustment required for hepatic impairment. |
| Pediatric use | Not recommended for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | Same as adult dose; no specific adjustments required. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for GYNAZOLE-1 (GYNAZOLE-1).
| Breastfeeding | Minimal systemic absorption suggests negligible transfer into breast milk. No specific M/P ratio reported; estimated M/P <0.01 due to low plasma levels. Considered compatible with breastfeeding. Avoid direct application to breast area to prevent infant ingestion. |
| Teratogenic Risk | GYNAZOLE-1 (butoconazole nitrate 2% vaginal cream, single dose) is a topical azole antifungal. Systemic absorption is minimal (approximately 1.7% of dose). Based on limited human data and animal studies, no increased risk of major birth defects or miscarriage has been observed with topical azole use during pregnancy. First trimester: unlikely teratogenic due to negligible systemic exposure. Second and third trimesters: no fetal risks identified with topical use. Category C (FDA) due to lack of adequate human studies, but widely used in pregnancy when indicated. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to butoconazole nitrate or any component of the product","Not indicated for use during pregnancy unless clearly needed (Category C)"]
| Precautions | ["For intravaginal use only","Not for ophthalmic or oral use","Discontinue if hypersensitivity occurs","May reduce efficacy of latex condoms and diaphragms","Use caution in patients with known sensitivity to imidazole antifungals"] |
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| Fetal Monitoring | No specific monitoring required beyond standard prenatal care. Monitor for local irritation or allergic reaction. If used in pregnancy, assess for treatment failure or recurrence. Fetal monitoring not needed due to minimal systemic exposure. |
| Fertility Effects | No known adverse effects on fertility. Vaginal candidiasis treatment may improve fertility by resolving local infection. No hormonal or reproductive system interference. |