Antifungal drugs


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Mycoses are infectious diseases caused by fungi. Mycoses are divided into superficial (affect the skin, hair, nails and visible mucous membranes) and deep (affect the subcutaneous tissue and internal organs). Immunocompromised patients often develop fungal infections, which require treatment with local and systemic antifungals.

Antifungals affect the structural elements of the fungus – cell membrane, cell wall and the synthesis of nucleic acids of the fungus.

Topical antifungals are applied in the form of creams, lotions, varnishes. Deep mycoses require treatment with systemic antifungals.

Antifungal azoles. Azoles (imidazoles and triazoles) are synthetic preparations. They disrupt the integrity of the cell wall and suppress the development of fungal infection. Imidazoles for topical application bifonazole, clotrimazole, fenticonazole, flutrimazole, econazole, ketoconazole are most often prescribed in the form of creams for local fungal diseases of smooth skin, candidiasis of the skin and mucous membranes and lichen planus.

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Miconazole is used to prevent and treat candidiasis that develops in the mouth and throat and the gastrointestinal tract. Ketoconazole is used for systemic treatment of superficial mycoses and deep mycoses . The lack of selectivity in the action of imidazoles is the reason for the manifestation of serious side effects.

Ketoconazole . It is available in the form of cream, shampoo and tablets. Gastrointestinal absorption of ketoconazole is higher at low pH values ​​of gastric juice. Antacids, proton pump inhibitors and H2 blockers impair its resorption. Its half-life is 8 hours. It is metabolized by the liver and excreted mainly in the bile. During treatment with ketoconazole, the most common side effects are from the gastrointestinal tract – nausea, vomiting. Asymptomatic elevations in serum transaminases (liver enzymes)are observed in approximately 5 to 10% of patients.

The most serious side effect after the administration of ketoconazole is impaired liver function. The frequency of this side effect is 1:15 000. In men, it is possible to observe gynecomastia (enlargement of the mammary glands), decreased libido, and in women, menstrual disorders are observed. Ketoconazole inhibits the activity of one of the major enzymes involved in the metabolism of many drugs. Therefore, co-administration with ketoconazole should be carefully considered.

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