GYNO-PEVARYL 150MG OVULES

Indications

• Tinea pedis (athlete's foot)
• Tinea cruris (jock itch)
• Tinea corporis (ringworm)
• Candidiasis (yeast infections)
• Dermatophyte infections

Dosage

Children: For children, refer to the BNF for Children for appropriate dosing information.

Adults: Apply to the affected area once daily for 2 to 4 weeks, depending on the specific infection being treated.

Mechanism of action

Econazole interacts with 14-alpha demethylase, a cytochrome P-450 enzyme necessary for converting lanosterol to ergosterol. Inhibition of ergosterol synthesis results in increased cellular permeability and leakage of cellular contents. Additionally, econazole may inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

Pharmacodynamics

Econazole is an antifungal agent related to other azoles such as fluconazole, ketoconazole, itraconazole, and clotrimazole. It prevents fungal organisms from producing vital substances required for their growth and function, making it effective only against fungal infections.

Pregnancy

Econazole should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Econazole may be excreted in human breast milk, use caution when administering to nursing mothers.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Topical cream
• Topical solution
• Vaginal cream

Indications

• Vaginal candidiasis
• Vulval candidiasis
• Superficial fungal infections

Dosage

Children: Refer to BNF for Children for appropriate dosing information.

Adults: For vaginal candidiasis, 1 pessary or 5 g of cream should be applied intravaginally at night for at least 14 days, with the course possibly repeated if necessary. For vulval candidiasis, apply cream 2-3 times a day to the affected area for the same duration.

Mechanism of action

Econazole nitrate exerts its antifungal effects by inhibiting the enzyme lanosterol 14-alpha-demethylase, which is crucial for the conversion of lanosterol to ergosterol in the fungal cell membrane. This disruption in ergosterol synthesis compromises the structural integrity of the fungal cell membrane, leading to increased permeability, cell lysis, and ultimately, cell death.

Pharmacodynamics

Econazole exhibits broad-spectrum antifungal activity against various fungi, including Candida species and dermatophytes. It is effective in treating superficial fungal infections due to its ability to penetrate the skin and mucosal tissues. The drug's effectiveness is enhanced when used consistently over the recommended treatment duration, which is typically at least 14 days for most infections.

Pharmacokinetics

Econazole is primarily administered topically, leading to minimal systemic absorption. When applied to the skin or vaginal mucosa, it achieves localized concentrations sufficient for antifungal activity. The pharmacokinetics of econazole indicate a high degree of binding to skin and mucosal tissues, allowing for sustained release and prolonged antifungal action. The elimination half-life is not well defined due to its local application and limited systemic exposure.

Contra-indications

• Hypersensitivity to econazole nitrate or any of the excipients
• Pregnancy, particularly during the first trimester

Adverse effects

• Skin reactions
• Vaginal burning
• Angioedema

Interactions

• May damage latex condoms and diaphragms

Precautions

• Use with caution in patients with a history of hypersensitivity reactions
• Monitor for skin reactions
• Avoid use during the first trimester of pregnancy

Pregnancy

Oral antifungal treatments should be avoided during pregnancy. Pregnant women may need a longer duration of treatment, usually about 7 days, to clear the infection.

Breast-feeding

Limited data available, but caution is advised as econazole may be excreted in breast milk.

Storage

Store below 25 degrees Celsius. Keep the container tightly closed and protect from light.

Formulations

• Econazole nitrate 10 mg per 1 gram cream
• Econazole nitrate vaginal pessaries

Mechanism of action

Econazole interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary to convert lanosterol to ergosterol. As ergosterol is an essential component of the fungal cell membrane, inhibition of its synthesis results in increased cellular permeability causing leakage of cellular contents. Econazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms, inhibit purine uptake, and impair triglyceride and/or phospholipid biosynthesis.

Pharmacodynamics

Econazole is an antifungal medication related to fluconazole (Diflucan), ketoconazole (Nizoral), itraconazole (Sporanox), and clotrimazole (Lotrimin, Mycelex). Econazole prevents fungal organisms from producing vital substances required for growth and function. This medication is effective only for infections caused by fungal organisms. It will not work for bacterial or viral infections.