Tioconazole is an imidazole antifungal indicated for the intravaginal treatment of vulvovaginal candidiasis. Tioconazole is a 1-dose treatment; however, complete relief of symptoms in just 1 day is atypical. Some symptom relief may be experienced within 1 day and complete relief of symptoms noted within 7 days. Tioconazole possesses fungicidal activity against Candida albicans and Candida parapsilosis. The petrolatum base of tioconazole ointment may damage the latex from which condoms or vaginal contraceptive diaphragms are made and cause them to fail; therefore, use of these contraceptive devices is not recommended during and for 3 days after tioconazole treatment. A mild increase in vaginal burning, irritation, and itching may occur when using tioconazole.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Intravaginal Administration
-Efficacy is unaffected by menstruation. However, avoid concurrent use with tampons as they may absorb the medication.
-The applicator is prefilled with the vaginal ointment.
-While firmly holding the capped end of the applicator, push the tip of the plunger into the base of the applicator.
-Remove cap from the top of the applicator using a pull-twist action.
-Gently insert the applicator into the vagina as far as it will comfortably go.
-Push the plunger into the applicator until it will go no farther.
-Remove the applicator and plunger from the vagina and dispose of in the trash. Do not flush the applicator or plunger.
A mild increase in vaginal burning, vaginal irritation, and vaginal pruritus may occur when using tioconazole. Tioconazole is a 1-dose treatment; however, complete relief of symptoms in just 1 day is atypical. Some symptom relief may be experienced within 1 day and complete relief of symptoms noted within 7 days. In a comparative trial (n = 80), single-dose tioconazole vaginal ointment was associated with significantly more local irritation or itching (30%) than a 3-day course of clotrimazole 100 mg vaginal tablets (5%). Discontinue tioconazole therapy and promptly evaluate if rash or hives, abdominal pain, fever, chills, nausea, vomiting, or foul-smelling vaginal discharge occurs.
The petrolatum base of tioconazole ointment may damage the latex from which condoms or vaginal contraceptive diaphragms are made and cause them to fail, reducing their effectiveness in preventing sexually transmitted infection or pregnancy; therefore, use of these contraceptive devices is not recommended during and for 3 days after tioconazole treatment. Although tioconazole may be used during menstruation, advise against concurrent tampon use as tampons may absorb the medication; recommend use of external pads or napkins during tioconazole therapy. Concurrent use of douches, spermicides, or other vaginal products is also not recommended. It is generally recommended to avoid vaginal intercourse during and for the first few days after tioconazole therapy.
Guidelines recommend 7 days of therapy with a topical azole preparation for the treatment of vulvovaginal candidiasis during pregnancy. Tioconazole is FDA-approved as a single-dose treatment. Consider an alternative topical azole antifungal or utilize a 7-day course of tioconazole during pregnancy. Tioconazole has been used during pregnancy with no treatment-related complications observed; most pregnancies were in the second or third trimester when tioconazole therapy was initiated.
It is not known if tioconazole is excreted in human milk. Systemic absorption after intravaginal administration is considered negligible and detectable milk concentrations are unlikely during breast-feeding. A tioconazole 1% cream has been used safely in neonates and infants with candidal diaper rash or impetigo.
Per the manufacturer, this drug has been shown to be active against most strains of the following microorganisms either in vitro and/or in clinical infections: Candida albicans, Candida sp.
NOTE: The safety and effectiveness in treating clinical infections due to organisms with in vitro data only have not been established in adequate and well-controlled clinical trials.
For the treatment of vulvovaginal candidiasis (VVC):
-for the treatment of uncomplicated VVC in persons without HIV:
Intravaginal dosage:
Adults: 4.6 g (300 mg tioconazole) intravaginally as a single dose at bedtime.
Pregnant Adults*: 4.6 g (300 mg tioconazole) intravaginally once daily at bedtime for 7 days.
Children and Adolescents 12 to 17 years: 4.6 g (300 mg tioconazole) intravaginally as a single dose at bedtime.
Pregnant Adolescents*: 4.6 g (300 mg tioconazole) intravaginally before bedtime for 7 days.
-for the treatment of uncomplicated VVC in persons living with HIV*:
Intravaginal dosage:
Adults: 4.6 g (300 mg tioconazole) intravaginally before bedtime for 3 to 7 days.
Adolescents: 4.6 g (300 mg tioconazole) intravaginally before bedtime for 3 to 7 days.
-for the treatment of severe or recurrent VVC:
Intravaginal dosage:
Adults: 4.6 g (300 mg tioconazole) 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. The FDA-approved dosage is 4.6 g (300 mg tioconazole) intravaginally as a single dose at bedtime.
Adolescents: 4.6 g (300 mg tioconazole) 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. The FDA-approved dosage is 4.6 g (300 mg tioconazole) intravaginally as a single dose at bedtime.
Maximum Dosage Limits:
-Adults
300 mg/day intravaginally.
-Geriatric
300 mg/day intravaginally.
-Adolescents
300 mg/day intravaginally.
-Children
12 years: 300 mg/day intravaginally.
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.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
There are no drug interactions associated with Tioconazole products.
Tioconazole is an imidazole antifungal that works by inhibiting the biosynthesis of ergosterol, an essential component of the fungal cell membrane. Azole antifungals block ergosterol synthesis by inhibiting lanosterol 14-alpha demethylase, a cytochrome P-450 dependent enzyme, which is needed to convert lanosterol to ergosterol. The depletion of ergosterol within the fungal cell membrane results in increased cellular permeability causing leakage of cellular content.
Tioconazole displays fungicidal activity against Candida albicans and Candida parapsilosis.
Tioconazole is administered intravaginally.
Affected cytochrome P450 isoenzymes and drug transporters: none
-Route-Specific Pharmacokinetics
Other Route(s)
Intravaginal Route
Minimal systemic absorption of tioconazole has been demonstrated after the application of tioconazole 6% vaginal ointment in persons with vaginal candidiasis. Animal studies have confirmed minimal systemic exposure after radiolabeled tioconazole was applied intravaginally.