Description
Clotrimazole Pharmacodynamics
Clotrimazole – imidazole derivative, broad-spectrum antifungal agent for external use. Antifungal effect is associated with disruption of ergosterol synthesis, which is part of the cell membrane of fungi, which changes the permeability of the cytoplasmic membrane and causes subsequent cell lysis. In low concentrations, it is fungistatic and fungicidal in high concentrations, and not only on proliferating cells. In fungicidal concentrations, it interacts with mitochondrial and peroxidase enzymes, resulting in an increase in hydrogen peroxide concentration to toxic levels, which also contributes to the destruction of fungal cells.
Clotrimazole has a broad antifungal spectrum of action in vitro and in vivo, including dermatophytes, yeast-like and mold fungi. Under certain analytical conditions, the values of the minimum suppressive concentration for these types of fungi range from less than 0.062 to 8.0 µg/ml substrate. It is effective against Pityriasis versicolor (Malassezia furfur). In addition to antifungal action, clotrimazole has antimicrobial action against Gram-positive (staphylococci, streptococci) and Gram-negative bacteria (Bacteroides, Gardnerella vaginalis). In vitro clotrimazole suppresses the reproduction of Corinebacteria and Gram-positive cocci – except enterococci – at concentrations of 0.5-10 mcg/ml substrate. Clotrimazole has no effect on lactobacilli. Primary resistant variants of sensitive fungi are very rare; development of secondary resistance in sensitive fungi is also noted in exceptional cases under therapeutic conditions.
Indications
Fungal skin diseases caused by dermatophytes, yeasts (including genus Candida), molds and other fungi and pathogens susceptible clotrimazole.
Contraindications
Hypersensitivity to clotrimazole or excipient (propylene glycol).
Application during pregnancy and lactation
Pregnancy
Data on the use of the drug in pregnant women are limited. Experimental animal studies have shown reproductive toxicity of clotrimazole when administered orally in high doses. When clotrimazole is used externally, negative effects on the reproductive system are not expected. It is possible to use clotrimazole during pregnancy under medical supervision.
Breast-feeding period
Clinical data on the use of the drug in breastfeeding women are limited. Experimental studies on animals suggest that clotrimazole is excreted into breast milk. The risk to the child is not completely excluded. The appropriateness of using the drug during breast-feeding should be decided individually after consultation with the doctor, if the potential benefit to the mother outweighs the possible risk to the baby. If necessary, the question of stopping breast-feeding should be decided.
Dosage and administration
- Outwardly. Solution is applied in a thin layer 2-3 times a day to previously clean (using soap with a neutral pH) and dry skin lesions and gently rub it in. A few drops are enough to treat an area the size of the palm of your hand. The duration of treatment depends on the severity of the disease, localization of pathological changes and the effectiveness of therapy.
- To prevent relapses, therapy is recommended to continue for another 2 weeks after the elimination of symptoms of the disease. There is no need for dose adjustment in patients of young and elderly age.
- If after treatment no improvement occurs or new symptoms appear, it is necessary to consult a physician. Use the drug only according to the route of administration and in the doses stated in the instructions. If necessary, please consult a physician.
