Vagistat-1

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Vagistat-1

Classes

Gynecological Antifungals

Administration
Intravaginal Administration

Tioconazole is usually administered intravaginally at bedtime as a single-dose treatment.
Wash hands before and after administration.
Read package directions carefully. The applicator should be opened just before use in order to prevent contamination. To use tioconazole vaginal ointment, gently insert the applicator tip high in the vagina and push the plunger to release the ointment into the vagina; gently remove the applicator.

Adverse Reactions
Moderate

contact dermatitis / Delayed / 1.0-10.0
vaginal pain / Early / 0-1.0
dyspareunia / Delayed / 0-1.0
dysuria / Early / 0-1.0

Mild

pruritus / Rapid / 1.9-6.0
vaginal irritation / Early / 1.9-6.0
nocturia / Early / 0-1.0

Common Brand Names

Monistat 1 Simple Therapy, Vagistat-1

Dea Class

OTC

Description

Imidazole antifungal
Fungicidal against Candida sp.
Single intravaginal dose is effective

Dosage And Indications
For the treatment of vulvovaginal candidiasis (VVC). For the treatment of uncomplicated VVC in persons without HIV. Intravaginal dosage Adults

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally before bedtime as a single dose.

Pregnant Adults†

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally before bedtime for 7 days.

Children and Adolescents 12 to 17 years

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally before bedtime as a single dose.

Pregnant Adolescents†

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally before bedtime for 7 days.

For the treatment of severe or recurrent VVC†. Intravaginal dosage Adults

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally before bedtime for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.

Adolescents

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally before bedtime for 7 to 14 days. Subsequent intermittent topical treatment may be considered for maintenance of recurrent VVC as an alternative to fluconazole.

For the treatment of uncomplicated VVC in persons living with HIV†. Intravaginal dosage Adults

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally before bedtime for 3 to 7 days.

Adolescents

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally before bedtime for 3 to 7 days.

Dosing Considerations
Hepatic Impairment

No dosage adjustment needed.

Renal Impairment

No dosage adjustment needed.

Drug Interactions

There are no drug interactions associated with Tioconazole products.

How Supplied

Monistat 1 Simple Therapy/Vagistat-1 Vaginal Ointment: 6.5%

Maximum Dosage
Adults

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally/day.

Geriatric

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally/day.

Adolescents

1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally/day.

Children

12 years: 1 applicatorful (300 mg tioconazole/4.6 g ointment) intravaginally/day.
1 to 11 years: Safety and efficacy have not been established.

Infants

Safety and efficacy have not been established.

Neonates

Safety and efficacy have not been established.

Mechanism Of Action

Tioconazole exerts its effect by disrupting normal fungal cell membrane permeability. Ergosterol is an essential component of the fungal cell membrane. Tioconazole inhibits ergosterol synthesis by interacting with 14-alpha demethylase, a cytochrome P-450 enzyme necessary for converting lanosterol to ergosterol. Inhibition of ergosterol synthesis results in increased cellular permeability, causing leakage of cellular contents such as phosphorous-containing compounds and potassium.

Pharmacokinetics

Tioconazole is administered intravaginally. Systemic absorption after a single intravaginal application in nonpregnant women is negligible.

Other Route(s)

Intravaginal Route
One dose (applicatorful) of tioconazole 6.5% provides 3 days of in vitro antifungal activity, with vaginal concentrations maintained above the MIC. Systemic absorption after a single intravaginal application in nonpregnant women is negligible.

Pregnancy And Lactation
Pregnancy

There are limited data regarding the use of tioconazole in pregnant women. Tioconazole did not adversely affect fetal viability or growth when administered orally to pregnant rats at doses up to 165 mg/kg/day during the period of organogenesis. However, tioconazole can cause dystocia in rats when treatment is extended through parturition; effects include prolongation of pregnancy, in utero deaths, and impaired pup survival. These effects are only observed with oral doses exceeding 20 mg/kg/day and intravaginal doses greater than 9 mg/kg/day. It is not known if tioconazole crosses the human placenta; however, there is negligible systemic absorption following intravaginal administration. Clinically significant exposure to the fetus is unlikely. According to CDC guidelines, many experts recommend 7 days of therapy with a topical azole preparation for the treatment of vulvovaginal candidiasis that occurs during pregnancy. Because tioconazole is administered as a single-dose treatment and the data regarding use in pregnant women is limited, an alternative antifungal (e.g., clotrimazole, miconazole or nystatin) should be considered. Pregnant women are advised to consult a healthcare professional prior to use.

There are no data regarding use of tioconazole during breast-feeding; excretion into breast milk is unknown. Systemic absorption following intravaginal administration is negligible. Although it's unlikely to produce detectable concentrations in breast-milk, nursing mothers are advised to consult a health care professional prior to use. 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 administered drug, health care providers are encouraged to report the adverse effect to the FDA.