Gynazole-1

Gynecological Antifungals

For storage information, see specific product information within the How Supplied section.

Butoconazole preparations are for intravaginal use only; do not apply to the eye, mouth, or skin.
Butoconazole is usually administered at bedtime; use special applicator supplied by the manufacturer.
Instruct patient on proper administration and treatment course.
Therapy should be continued during menstruation. However, instruct patient not to use tampons during the treatment course.
Instruct patient not to use douches or spermicides during the treatment course and to abstain from sexual activity during treatment. Vaginal butoconazole products may damage condoms, diaphragms, and cervical caps, and cause them to fail.
If an adequate response is not achieved, the diagnosis should be reconfirmed and other pathogens commonly associated with vulvovaginitis ruled out.

vaginal pain / Early / 1.0-1.0

abdominal pain / Early / 1.0-1.0
vaginal irritation / Early / 1.0-1.0
pelvic pain / Delayed / 1.0-1.0
pruritus / Rapid / 1.0-1.0

Gynazole-1

Rx

Imidazole antifungal agent that is fungicidal in vitro against Candida spp.; available as a vaginal preparation; multiple dose products available OTC; single dose product available by prescription only.

1 applicatorful (100 mg butoconazole/5 g cream) intravaginally as a single dose.[46358]

1 applicatorful (100 mg butoconazole/5 g cream) intravaginally once daily for 7 days.

1 applicatorful (100 mg butoconazole/5 g cream) intravaginally as a single dose.

1 applicatorful (100 mg butoconazole/5 g cream) intravaginally once daily for 7 days.

1 applicatorful (100 mg butoconazole/5 g cream) intravaginally once daily for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.

1 applicatorful (100 mg butoconazole/5 g cream) intravaginally once daily for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.

1 applicatorful (100 mg butoconazole/5 g cream) intravaginally once daily for 3 to 7 days.

1 applicatorful (100 mg butoconazole/5 g cream) intravaginally once daily for 3 to 7 days.

No dosage adjustment needed.

No dosage adjustment needed.

There are no drug interactions associated with Butoconazole products.

Gynazole-1 Vaginal Cream: 2%

1 applicatorful (100 mg butoconazole/5 g cream) intravaginally/day.

1 applicatorful (100 mg butoconazole/5 g cream) intravaginally/day.

Safety and efficacy have not been established; however, 1 applicatorful (100 mg butoconazole/5 g cream) intravaginally/day has been used off-label.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

As other azole antifungals, butoconazole exerts its antifungal activity by altering cellular membranes, resulting in increased membrane permeability, secondary metabolic effects, and growth inhibition. Although not fully determined, butoconazole is thought to interfere with ergosterol synthesis through by interacting with 14-alpha demethylase, a cytochrome P-450 enzyme that is necessary for the conversion of lanosterol to ergosterol, an essential component of the membrane. In contrast, amphotericin B binds to ergosterol after it is synthesized. Like imidazole derivatives, the fungicidal activity of butoconazole at high concentrations may result from a direct physiochemical effect of the drug on the fungal cell.

Butoconazole is administered intravaginally. The distribution of butoconazole after intravaginal administration has not been determined. The plasma half-life of ranges from 21—24 hours. Metabolism of any systemically-absorbed drug occurs in the liver.

Intravaginal Route
When butoconazole is administered intravaginally, small amounts are slowly absorbed systemically. Following intravaginal administration of approximately 5 g of radiolabeled butoconazole nitrate 2% cream (approximately 100 mg of the drug total) to healthy women, peak plasma concentrations 24 hours after administration ranged from 19—44 ng/mL. Following vaginal administration of butoconazole nitrate 2% vaginal cream for one dose to three women, 1.7% (range 1.3—2.2%) of the dose was absorbed on average. Peak plasma levels of the drug and its metabolites are attained between 12 and 24 hours after vaginal administration. Based on limited data, radioactivity was apparent in plasma 2—8 hours after intravaginal administration and persisted for 4—5 days.

No adequate, well-controlled studies have been conducted with butoconazole in human pregnancy. Guidelines recommend the use of butoconazole intravaginally in pregnant persons. Following vaginal application, approximately 1.7% of the dose is absorbed systemically. In animal studies, fertility was not impaired following oral administration at doses of up to 5 to 10 times the recommended human dose. Butoconazole, when given intravaginally in excess doses to pregnant rats, did not cause teratogenicity. While oral doses of 5 to 50 mg/kg did not result in fetal malformations in pregnant rats, oral doses of 100 to 750 mg/kg/day have resulted in adverse effects such as abdominal wall defects, cleft palate to the fetus; maternal stress was also evident at the higher dosing range.

There are no data describing the effects of butoconazole during breast-feeding and its' excretion in human milk is unknown. Following vaginal application, approximately 1.7% of the dose is absorbed systemically. According to the manufacturer, caution is advised when administering to nursing mothers. Fluconazole, clotrimazole, and miconazole may be potential alternatives to consider during breast-feeding. However, site of infection, local susceptibility patterns, and specific microbial susceptibility should be assessed before choosing an alternative agent. Consider the benefits of breast-feeding, the risk of potential infant drug exposure, and the risk of an untreated or inadequately treated condition. If a breast-feeding infant experiences an adverse effect related to a maternally ingested or administered drug, health care providers are encouraged to report the adverse effect to the FDA.