Tioconazole, 1-[2-{(2-chloro-3-thienyl)methoxy}-2(2,4-dichlorophenyl)ethyl]1,H-imidazole, is a topical antifungal agent. Its chemical formula is C₁₆H₁₃Cl₃N₂OS with a molecular weight of 387.7.

VAGISTAT-1 (tioconazole 6.5%) is formulated in a base of white, soft paraffin and aluminum magnesium silicate with butylated hydroxyanisole (BHA) added as a preservative. Each applicator-full of VAGISTAT-1 provides approximately 4.6 grams of ointment containing 300 mg of tioconazole.

Last updated on RxList: 12/8/2004

VAGISTAT-1 is indicated for the local treatment of vulvovaginal candidiasis (moniliasis). As VAGISTAT-1 has been shown to be effective only for candidal vulvovaginitis, the diagnosis should be confirmed by KOH smears and/or cultures. Other pathogens commonly associated with vulvovaginitis should be ruled out by appropriate methods.

Studies have shown that women taking oral contraceptives have a cure rate similar to those not taking such agents when treated with VAGISTAT-1.

Safety and effectiveness in pregnant and diabetic patients have not been established (see PRECAUTIONS).

VAGISTAT-1 has been found to be effective as a single- dose treatment for vulvovaginal candidiasis. Using the prefilled applicator, insert one applicator- full intravaginally. Administration of VAGISTAT-1 just prior to bedtime may be preferred.

VAGISTAT-1 is supplied in a ready-to-use, prefilled, single-dose vaginal applicator (NDC 0087-0657-40). Each applicator-full will deliver approximately 4.6 grams of VAGISTAT-1 containing 65 mg of tioconazole per gram of ointment.

Storage: Store at controlled room temperature 15°-30° C (59°-86° F).

WARNING: Manufactured with 1,1,1-trichloroethane, a substance which harms public health and environment by destroying ozone in the upper atmosphere.

Last updated on RxList: 12/8/2004

The incidence of adverse reactions to VAGISTAT-1 is based on clinical trials involving 1000 patients. Burning and itching were the most frequent side effects occurring in approximately 6% and 5% of the patients, respectively. In most instances these did not interfere with the course of therapy.

There were occasional reports (less than 1%) of other side effects including irritation, discharge, vulvar edema and swelling, vaginal pain, dysuria, nocturia, dyspareunia, dryness of vaginal secretions, desquamation, and burning sensation.

Last updated on RxList: 12/8/2004

No information provided.

General

VAGISTAT-1 is intended for intravaginal administration only. Applicators should be opened just prior to administration to prevent contamination. Administration of VAGISTAT-1just prior to bedtime may be preferred. The VAGISTAT-1 ointment base may interact with rubber or latex products such as condoms or vaginal contraceptive diaphragms; therefore, use of such products within 72 hours following treatment is not recommended.

If clinical symptoms persist, appropriate microbiological tests should be repeated to rule out other pathogens and to confirm the diagnosis.

Carcinogenesis

No long-term studies in animals have been performed to evaluate the carcinogenic potential of tioconazole.

Mutagenesis

Tioconazole did not demonstrate mutagenic activity at the levels examined in tests at either the chromosomal or subchromosomal level.

Impairment of Fertility

No impairment of fertility was seen in male rats administered tioconazole hydrochloride in oral doses up to 150 mg/kg/day. However, there was evidence of preimplantation loss in female rats at oral dose levels above 35 mg/kg/day.

Pregnancy

Pregnancy Category C: Tioconazole hydrochloride had no adverse effects on fetal viability or growth when administered orally to pregnant rats at doses of 55, 110, and 165 mg/kg/day during the period of organogenesis. A drug- related increase in the incidence of dilated ureters, hydroureters, and hydronephrosis observed in the fetuses of this study was transient and no longer evident in pigs raised to 21 days of age. These effects did not occur following intravaginal administration of approximately 10 mg/kg/day in a 2% cream. There was no evidence of major structural anomalies. No embryotoxic or teratogenic effects were observed in rabbits receiving oral dose levels as high as 165 mg/kg/day or daily intravaginal application of approximately 2-3 mg/kg in a 2% tioconazole cream during organogenesis. Tioconazole hydrochloride, like other azole antimycotic agents, causes dystocia in rats when treatment is extended through parturition. Associated effects in rats include prolongation of pregnancy, in utero deaths, and impaired pup survival. The ''no-effect'' level for this phenomenon is 20 mg/kg/day orally and approximately 9 mg/kg/day intravaginally. No effect on parturition occurred in rabbits at 50 mg/kg/day orally.

There are no adequate and well-controlled studies in pregnant women. VAGISTAT® -1 (tioconazole 6.5%) 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, nursing should be temporarily discontinued while VAGISTAT-1 is administered.

Pediatric Use

Safety and effectiveness in children have not been established.

Last updated on RxList: 12/8/2004

VAGISTAT-1 is contraindicated in individuals who have been shown to be sensitive to imidazole antifungal agents or to other components of the ointment.

Last updated on RxList: 12/8/2004

Tioconazole is a broad-spectrum antifungal agent that inhibits the growth of human pathogenic yeasts. Tioconazole exhibits fungicidal activity in vitro against Candida albicans, other species of the genus Candida, and against Torulopsis glabrata.

Pharmacokinetics

Systemic absorption of tioconazole after a single intravaginal application of VAGISTAT-1 in nonpregnant patients is negligible.

Last updated on RxList: 12/8/2004

The VAGISTAT-1 ointment base may interact with rubber or latex products such as condoms or vaginal contraceptive diaphragms; therefore, use of such products within 72 hours following treatment is not recommended.

Last updated on RxList: 12/8/2004

IMPORTANT NOTE: This is a summary and does not contain all possible information about this product. For complete information about this product or your specific health needs, ask your health care professional. Always seek the advice of your health care professional if you have any questions about this product or your medical condition. This information is not intended as individual medical advice and does not substitute for the knowledge and judgment of your health care professional. This information does not contain any assurances that this product is safe, effective, or appropriate for you.

TIOCONAZOLE - VAGINAL

(tie-oh-CON-uh-zole)

COMMON BRAND NAME(S): Vagistat-1

USES: This medication is used to treat vaginal yeast infections. Tioconazole ointment reduces vaginal burning, itching, and discharge that may occur with this condition. This medication is an azole antifungal. It works by stopping the growth of yeast (fungus) that causes the infection.

If you have fever, chills, flu-like symptoms, stomach/abdominal pain, or a bad-smelling vaginal discharge, do not use this medication. Contact your doctor immediately because these may be signs of a more serious infection.

HOW TO USE: Read the Patient Information Leaflet that comes with this product. Consult your doctor or pharmacist if you have any questions.

Use the medication 1 time only, usually at bedtime or as directed by your doctor. Wash your hands before using the medication. Use the medication applicator supplied. Follow the package instructions on how to fill the applicator with the ointment. Lie on your back with your knees toward your chest. Insert one applicator full of the ointment into the vagina as far as it will comfortably go. Slowly press the plunger of the applicator all the way down to apply the medication. If you have itching/burning around the outside of the vagina (vulva), you should also apply some medication to that area. Discard the applicator. Wash your hands after use.

Dosage is based on your medical condition and response to treatment.

Do not use tampons, douches, spermicides, or other vaginal products while using this medication. Unscented sanitary napkins may be used for your menstrual period or to protect your clothing from leakage of the medication.

Tell your doctor if your condition persists for 3 days after completing the treatment, or returns 1 week after.

SIDE EFFECTS: Headache, body pain, vaginal/urethral burning/itching/pain, or menstrual cramps may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

If your doctor has directed you to use this medication, remember that he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching, swelling, severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

Contact your doctor for medical advice about side effects. The following numbers do not provide medical advice, but in the US you may report side effects to the Food and Drug Administration (FDA) at 1-800-FDA-1088. In Canada, you may call Health Canada at 1-866-234-2345.

PRECAUTIONS: Before using tioconazole, tell your doctor or pharmacist if you are allergic to it; or to other azole antifungal agents (e.g., clotrimazole, fluconazole); or to petrolatum; or if you have any other allergies.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: diabetes, immune system problems, infection with HIV, 4 or more vaginal yeast infections per year.

Ask your doctor whether you can have sexual intercourse while using this product. Avoid using a diaphragm, cervical cap, or latex condoms for birth control while using this product and for 3 days after treatment. Some ingredients may damage these products, causing them to possibly break. Use other forms of birth control such as polyurethane condoms.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: antibiotics taken by mouth, corticosteroids (e.g., prednisone), drugs that weaken the immune system (e.g., cyclosporine, cancer chemotherapy such as methotrexate).

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: This product may be harmful if swallowed. If overdose or swallowing is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Do not share this medication with others.

Dry the genital area thoroughly after showering, bathing, or swimming. Avoid wearing tight jeans, nylon underwear, pantyhose, a wet bathing suit, or damp/sweaty exercise clothes for long periods. Wear cotton underwear, and change your underwear daily. This may help to prevent the growth of yeast.

If your sexual partner experiences symptoms, they should contact their doctor immediately.

MISSED DOSE: Not applicable.

STORAGE: Store at room temperature between 59-86 degrees F (15-30 degrees C) away from light and moisture. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised July 2008 Copyright(c) 2008 First DataBank, Inc.