Tioconazole-1 (tioconazole)

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Tioconazole is administered intravaginally as a 6.5% ointment. Although the following dosage forms are not commercially available in the US, tioconazole also has been administered intravaginally as a 100- or 300-mg vaginal suppository+, 100-mg vaginal tablet+, 6% vaginal ointment, or 2% vaginal cream+; applied topically to the skin as a 1 or 2% cream+ or 1% lotion+; applied topically to the nails as a 28% lotion+; and applied topically to the feet as a 1% powder+.

Commercially available prefilled single-dose applicators containing tioconazole 6.5% vaginal ointment are intended for intravaginal administration only. Contact with eyes should be avoided.

Tioconazole 6.5% vaginal ointment should be used for self-medication of recurrent vulvovaginal candidiasis only in otherwise healthy, nonpregnant women previously diagnosed by a clinician.

Patients should be instructed how to use the vaginal applicators and should be given a copy of the instructions provided by the manufacturer. The applicator should be opened just prior to administration to prevent contamination.

Tioconazole 6.5% vaginal ointment contains a petrolatum base that may interact with rubber or latex products, including condoms or vaginal contraceptive diaphragms, and alternative methods of contraception should be used during the first 72 hours after an intravaginal dose of the drug.

Tioconazole vaginal ointment may be administered during menstruation, but sanitary napkins should be used instead of vaginal tampons; some clinicians suggest that use of the vaginal ointment be delayed until after the menstrual flow has ceased.

Since only small amounts of tioconazole are absorbed systemically following intravaginal administration, drug interactions are unlikely in patients receiving the single-dose intravaginal regimen used in the treatment of vulvovaginal candidiasis. While results of animal studies indicate that tioconazole may induce hepatic cytochrome P-450 isoenzymes and the drug therefore theoretically could induce the metabolism of drugs metabolized by these enzymes, it is unlikely that such drug interactions could occur with intravaginal tioconazole.

Results of clinical studies indicate that efficacy of intravaginal tioconazole is not affected by concomitant use of oral contraceptives.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

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There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

• No disease contraindications

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Rare or Very Rare

• Abnormal vaginal bleeding
• Anaphylaxis
• Angioedema
• Bronchospastic pulmonary disease
• Dyspnea
• Toxic epidermal necrolysis
• Urticaria

Less Frequent

• Dysmenorrhea
• Fever
• Genital organ pruritus
• Vaginal discharge

Rare or Very Rare

• Acute abdominal pain
• Chills
• Contact dermatitis
• Cystitis
• Dizziness
• Facial edema
• Flu-like symptoms
• General weakness
• Headache disorder
• Nausea
• Pruritus of skin
• Skin rash
• Vaginal burning
• Vaginal irritation
• Vaginitis
• Vulvovaginal pain

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There are no adequate and controlled studies evaluating use of intravaginal tioconazole in pregnant women, and the drug should be used during pregnancy only when the potential benefits justify the possible risks to the fetus. A single dose of the commercially available tioconazole 6.5% vaginal ointment has been used in a limited number of pregnant women for the treatment of vulvovaginal candidiasis+, and a single-dose of other tioconazole preparations not commercially available in the US (i.e., 2% vaginal cream, 100-mg vaginal tablet, 300-mg vaginal suppository, 6% vaginal ointment) have been used effectively to treat uncomplicated vulvovaginal candidiasis in pregnant women. In most cases, the tioconazole dose was administered during the second or third trimester of pregnancy, but some women received the dose during the first trimester. There generally were no apparent adverse effects on the pregnancy, delivery, or fetus following a single intravaginal dose of tioconazole; however, there have been a few reports of adverse pregnancy outcomes (i.e., spontaneous abortion, breech delivery, premature birth). While these effects do not appear to be drug-related, it is difficult to distinguish drug- from disease-related effects. The optimal regimen for the treatment of vulvovaginal candidiasis in pregnant women has not been identified, and further study is needed to evaluate safety and efficacy of single-dose regimens in these women. If treatment of vulvovaginal candidiasis is considered necessary in pregnant women, the US Centers for Disease Control and Prevention (CDC) and some clinicians recommend use of an intravaginal azole antifungal given for 7 days.

Reproduction studies in rats using oral tioconazole hydrochloride in dosages of 55-165 mg/kg daily during the period of organogenesis did not reveal evidence of adverse effects on fetal viability or growth, and there was no evidence of major structural anomalies in offspring. While there was evidence of a drug-related increase in the incidence of dilated ureters, hydroureters, and hydronephrosis in the fetuses of these rats, these effects were transient and were no longer evident in the pups at 21 days of age; these effects did not occur in rats following intravaginal administration of tioconazole 2% cream in a dosage of 10 mg/kg daily. Similar studies in rabbits using oral tioconazole dosages as high as 165 mg/kg daily or intravaginal 2% cream in a dosage of 2-3 mg/kg daily during organogenesis did not reveal evidence of embryotoxic or teratogenic effects.

In rats, when tioconazole administration was extended through parturition, the drug caused dystocia, prolonged gestation, and in utero deaths and resulted in an increase in the number of stillborn pups and a decrease in pup survival; pups that survived developed normally. These adverse effects on parturition occurred only when the drug was given orally in dosages exceeding 20 mg/kg daily or intravaginally in dosages exceeding 9 mg/kg daily during the last third of pregnancy, and did not occur at lower oral or intravaginal dosages, when tioconazole was terminated before the last third of pregnancy, or when high oral dosage (150 mg) was confined to a few days before delivery. No effect on parturition was noted in pregnant rabbits given oral tioconazole at dosages of 50 mg/kg daily during the last 10 days of pregnancy. Similar effects on parturition (e.g., dystocia, prolonged gestation) also have been reported in animal studies with high doses of other imidazole-derivative azole antifungals (e.g., econazole, ketoconazole, miconazole, sulconazole).

Since it is not known whether tioconazole is distributed into milk, women should temporarily discontinue breast-feeding while they are receiving the drug.

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