Drug information of Tioconazole

Tioconazole


Tioconazole is an imidazole antifungal used to treat fungal and yeast infections.

Mechanism of effect

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.

Pharmacodynamic

Tioconazole is a broad-spectrum imidazole 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

Peak Plasma: 18 ng/mL in 2-24 hr

Onset of action: 24 hr (symptom improvement); 7 days (complete relief)

Metabolism: Glucuronidation of the imidazole ring

Distribution: Vaginal fluid (24-72 hr)

Excretion: Urine and feces

Drug indications

Vaginal Candidiasis

Dosage

Adult

Vaginal Candidiasis

Insert 1 applicatorful (5 g of 6.5% ointment) intravaginally qHS once

Pediatric

Safety & efficacy not established

Drug contraindications

diabetes , pregnancy , Hypersensitivity

Side effects

Headache , vaginitis

Alerts

None

Points of recommendation

  • If vaginal yeast infections happen often, talk with the doctor.
  • If you have HIV infection, talk with your doctor.
  • Do not use tioconazole if you have belly pain, fever, or bad-smelling vaginal discharge. Talk with your doctor.
  • Protect clothing and fabrics from staining.
  • Do not have vaginal sex while using tioconazole.
  • Do not use tioconazole for itching caused by a health problem other than a vaginal yeast infection. Talk with the doctor.
  • Condoms or diaphragms may not work to prevent pregnancy or stop the spread of diseases passed through sex while using tioconazole and for a period of time after you stop tioconazole. You will need to use some other kind of birth control for some time after the last dose. Be sure you know how long to do this.
  • Do not douche or use other vaginal products like tampons while you are using tioconazole. You may need to avoid these things for some time after the last dose.
  • This medicine may cause harm if swallowed. If tioconazole is swallowed, call a doctor or poison control center right away.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using tioconazole while you are pregnant.
  • Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.
  • Keep out of your mouth, nose, and eyes (may burn).
  • Use at bedtime.
  • Wash your hands before and after use.
  • Do not open until you are ready to use.
  • Do not use the applicators more than 1 time.

Pregnancy level

Group c - Not adequate studies in pregnant women


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