tioconazole

Action and Spectrum

Actions and Spectrum:

• tioconazole is an antifungal medication that is used to treat vaginal yeast infections. Its mechanism of action involves inhibiting the synthesis of ergosterol, an essential component of fungal cell membranes. Without ergosterol, fungal cell membranes become weakened and more permeable, which ultimately leads to fungal cell death.
• The spectrum of activity of tioconazole is primarily limited to fungi of the genus Candida, which is the most common cause of vaginal yeast infections. It is also effective against some strains of dermatophytes, which are fungi that can cause skin and nail infections.

tioconazole is a broad-spectrum antifungal medication that is effective against a wide range of fungal species within its spectrum of activity. However, it is ineffective against all types of fungi, and it should not be used to treat infections caused by other types of pathogens, such as bacteria or viruses.

Drug Interaction

Adverse Reaction

Frequency not defined

Headache

Vulvovaginal burning, vaginitis, pruritus

Abdominal cramping

Black Box Warning

None

Contraindication / Caution

Contraindications/caution:

Contraindications:

• Hypersensitivity: tioconazole is contraindicated in patients with known hypersensitivity to the medication or its components. Patients who experience an allergic reaction or hypersensitivity to tioconazole should discontinue the medication and seek medical attention immediately.
• Pregnancy: tioconazole is classified as a pregnancy category C medication, meaning it may not be safe to use during pregnancy. Pregnant women should only use tioconazole if the benefits of treatment outweigh the potential risks to the fetus. Healthcare providers should carefully consider the risks and benefits of treatment before prescribing tioconazole to pregnant women.
• Breastfeeding: tioconazole can be excreted in breast milk and may pose a risk to nursing infants. Breastfeeding women should consult with their healthcare provider before using tioconazole to discuss the risks and benefits of treatment.
• Children: tioconazole has not been studied in pediatric populations, and its safety and efficacy in children are not well established. As such, tioconazole is generally not recommended for children under 12.

Cautions:

None

Pregnancy / Lactation

Pregnancy consideration: It may not be safe to use during pregnancy. Pregnant women should only use tioconazole if the benefits of treatment outweigh the potential risks to the fetus.

Lactation:

• Excretion of the drug in human breast milk is known
• tioconazole may pose a risk to nursing infants.

Pregnancy category:

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology:

tioconazole is an antifungal medication that treats various fungal infections, including vaginal yeast infections. It belongs to the class of drugs known as imidazoles and works by inhibiting the growth and reproduction of fungi.

When applied topically, tioconazole is rapidly absorbed through the skin and has a long half-life, meaning it stays active in the body for a long time. The drug is metabolized in the liver and eliminated from the body through urine and feces.

tioconazole is effective against various fungi, including Candida albicans, the most common cause of vaginal yeast infections. It is also effective against other Candida species, dermatophytes, and some types of bacteria.

Pharmacodynamics:

tioconazole exerts its pharmacodynamic effects by inhibiting the synthesis of ergosterol, a key component of fungal cell membranes. Ergosterol is essential for maintaining the structural integrity and fluidity of the fungal cell membrane. tioconazole binds to the fungal cytochrome P450 enzyme, disrupting the biosynthesis of ergosterol and thereby impairing the growth and survival of fungi

Pharmacokinetics:

Absorption

tioconazole is available in various topical formulations, including creams, ointments, and suppositories. tioconazole is absorbed through the skin or mucous membranes and reaches the systemic circulation when applied topically. The rate and extent of absorption depend on the formulation, the application site, and other factors that affect skin permeability.

Distribution

tioconazole is distributed primarily to vaginal fluid and other tissues with fungal infections. It has a long half-life, meaning it stays in the body long after administration.

Metabolism

tioconazole is metabolized primarily by glucuronidation of the imidazole ring in the liver, which makes it more water-soluble and easier to eliminate from the body. The metabolites of tioconazole are inactive and are eliminated in the urine and feces.

Elimination and Excretion

tioconazole and its metabolites are eliminated mainly in the urine and feces. The elimination half-life of tioconazole is approximately 2-3 days.

Adminstartion

Administration:

tioconazole is a topical antifungal medication available in various formulations, including creams, ointments, and suppositories. The exact administration instructions may vary depending on the specific formulation and the treated condition. However, here are some general guidelines:

Cream or ointment: tioconazole cream or ointment is usually applied to the affected skin area, such as the vagina or the skin folds, once daily for 1 to 7 days, depending on the severity of the infection. The cream or ointment should be applied using the applicator or your fingers, as directed by your healthcare provider.

Suppository: tioconazole suppository is inserted into the vagina once daily for 1 to 3 days, depending on the severity of the infection. The suppository should be inserted as far as possible into the vagina while lying on your back, as directed by your healthcare provider.

Patient Information Leaflet

Patient information leaflet

Generic Name: tioconazole

Why do we use tioconazole?

tioconazole is an antifungal medication used for the treatment of various fungal infections, including:

• Vulvovaginal candidiasis: tioconazole is commonly used to treat vaginal yeast infections caused by an overgrowth of the fungus Candida. Symptoms of vaginal yeast infections include itching, burning, and discharge.
• Tinea corporis: tioconazole can be used to treat ringworm, a fungal infection that affects the skin on the body, including the arms, legs, and trunk. Symptoms of ringworm include red, scaly patches on the skin that may be itchy or painful.

Tinea cruris: tioconazole is also used to treat jock itch, a fungal infection that affects the skin around the groin and inner thighs. Symptoms of jock itch include red, itchy, and flaky patches on the skin.