Tioconazole

BRAND NAMES

It is sold under the brand names Trosyd and Gyno-Trosyd, originally by Pfizer, then Johnson & Johnson, and currently by Kenvue. Tioconazole ointments are used to treat vaginal yeast infections in women.

MECHANISM OF ACTION

Tioconazole works by targeting 14-α demethylase, a cytochrome P450 enzyme responsible for converting lanosterol into ergosterol—an essential component of fungal cell membranes. By inhibiting this enzyme, tioconazole disrupts ergosterol production, leading to increased membrane permeability and cell damage.

PHARMACOKINETICS

Absorption:

Tioconazole has minimal systemic absorption, whether applied topically to the skin or intravaginally. This low absorption profile minimizes the risk of systemic side effects and drug interactions, making it suitable for localized treatment of fungal infections.

Distribution:

Tioconazole is an antifungal medication primarily designed for localized action, leading to high concentrations at the application site and minimal systemic (body-wide) absorption. Its distribution is confined to the specific area of treatment, such as the vaginal fluid or the skin.

Metabolism:

Tioconazole, when taken orally, undergoes extensive metabolism, with the primary metabolites being glucuronide conjugates.

Excretion:

When tioconazole is administered topically, it is excreted through both the urine and feces. Only small amounts of the drug are absorbed systemically, limiting overall exposure to the body.

PHARMACODYNAMICS

Tioconazole is a broad-spectrum antifungal agent from the imidazole class, effective in inhibiting the growth of pathogenic yeasts that affect humans. In laboratory studies, it has shown fungicidal activity against Candida albicans, various other Candida species, and Torulopsis glabrata.

The drug works by disrupting the synthesis of key components required to maintain the integrity and function of the fungal cell membrane. This interference compromises membrane structure, ultimately inhibiting fungal growth and survival.

ADMINISTRATION

Tioconazole for treating vaginal yeast infections is administered as a single, pre-filled applicator dose of 6.5% vaginal ointment. For superficial skin infections, a 1% cream is applied topically. Tioconazole is for topical use only and should not be taken orally.

DOSAGE AND STRENGTH

Before discussing the dosage and strength of Tioconazole, it is important to note that this information is for general knowledge only and should not be taken as medical advice. Always consult with a healthcare provider for diagnosis, treatment, and to determine the appropriate dosage and strength for your specific condition.

DRUG INTERACTIONS 

Does tioconazole interact with other medications? Currently, there are no known drug interactions with tioconazole. However, it is important to always inform your healthcare provider about all prescription and over-the-counter (OTC) medications, vitamins, minerals, herbal products, and any other supplements you are taking.

FOOD INTERACTIONS 

There are no known food interactions with tioconazole because it is a topical antifungal, not an oral medication. It is applied to the skin or used as a vaginal ointment, and systemic absorption into the bloodstream is negligible. While there are no direct food interactions, some lifestyle and diet recommendations may support recovery from a fungal infection.

CONTRAINDICATIONS

Tioconazole should not be used by individuals who are allergic to azole antifungals or any ingredients in the ointment or cream.

SIDE EFFECTS:

Common (Mild) Side Effects:

• Mild vaginal 

• Burning

• Itching Irritation

If you experience burning, itching, or irritation that becomes bothersome, inform your healthcare provider.

Serious Side Effects 

• Difficulty breathing or wheezing
• Rapid or irregular heartbeat
• Fever or feeling generally unwell
• Swollen lymph nodes
• Swelling of the face, lips, mouth, tongue, or throat can occur.
• Difficulty swallowing or a tight sensation in the throat
• Skin rash, itching, or hives (pale red bumps)
• Nausea or vomiting
• Dizziness, lightheadedness, or fainting
• Stomach cramps

OVER DOSE 

Overdose of topical or intravaginal Tioconazole is unlikely because systemic absorption is negligible. Most reported symptoms of overdose are local and related to using excessive amounts topically. In cases of accidental swallowing, systemic effects are possible but uncommon, as the drug is mainly used externally. Animal studies have shown that high oral doses can affect the liver.

TOXICITY

Signs of overdose may include skin redness (erythema), stinging or burning sensations, blistering, peeling, swelling (edema), itching (pruritus), hives (urticaria), general skin irritation, and muscle cramps.