Tioconazole
Indications
Tioconazole is indicated for the local treatment of vulvovaginal candidiasis (moniliasis). As Tioconazole 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 Tioconazole.
Pharmacology
Tioconazole interacts with 14-α demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol, an essential component of the yeast membrane. In this way, tioconazole inhibits ergosterol synthesis, resulting in increased cellular permeability. Tioconazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms and the uptake of purine, impair triglyceride and/or phospholipid biosynthesis, and inhibit the movement of calcium and potassium ions across the cell membrane by blocking the ion transport pathway known as the Gardos channel.
Dosage And Administration
Topical: Apply & massage gently into the affected & surrounding skin area once or twice a day. In intertriginous areas, apply sparingly & smoothed in well to avoid macerating effects. Duration: 1-6 weeks.
Vaginal candidiasis:
- Adult: As 6.5% ointment: Admin intravaginally at bedtime as a single dose.
- Child: ≥12 yr Admin at bedtime as a single dose.
Contraindications
Tioconazole is contraindicated in individuals who have been shown to be sensitive to imidazole antifungal agents or to other components of the ointment.
Side Effects
Occasional local transient & mild irritation; if hypersensitivity reaction develop, treatment should be discontinued & appropriate therapy should be instituted.
Pregnancy And Lactation
Pregnancy Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Precautions And Warnings
Not for ophthalmic use.
Therapeutic Class
Drugs used in Vaginal and Vulval condition, Topical Antifungal preparations.
Use in special populations
Safety and effectiveness in pregnant and diabetic patients have not been established.