Description
Clotrimazole Pharmacodynamics
Clotrimazole – imidazole derivative, broad-spectrum antifungal agent. 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
Genital infections caused by (Candida vulvovaginitis.)
Candida yeast-like fungi
Contraindications
– Hypersensitivity to clotrimazole or other ingredients of the drug
– Under 12 years of age
– I trimester of pregnancy
Use during pregnancy and lactation Fertility
No studies on the effect of clotrimazole on fertility have been conducted in humans, in animal studies the drug has not affected fertility.
Pregnancy
Data on the use of the drug in pregnant women are limited. Experimental animal studies have shown no direct or indirect adverse effects of the drug on fertility. Clotrimazole in the dosage form of vaginal tablets is contraindicated for use in the first trimester of pregnancy. The appropriateness of use in the second and third trimesters of pregnancy should be decided individually after consultation with your doctor.
Breast-feeding period
Available data from pharmacodynamic/toxicological studies in animals have demonstrated excretion of clotrimazole with milk. Breast-feeding should be discontinued during treatment with clotrimazole.
Dosage and administration
- Adults and children over 12 years For intravaginal use.
- Vaginal pills are introduced into the vagina, as deeply as possible, in a supine position, with the legs slightly bent, 1 tablet 2 times a day for 3 days or 1 tablet 1 time a day for 6-7 days (evening before going to bed).
- If symptoms persist for more than 7 days, it is recommended to consult a doctor.
Repeated course of treatment is possible after consultation with a physician. - If symptoms recur within 2 months, the patient should consult a physician.
Use the drug only according to the method of use and in the doses specified in the instructions for use. - If necessary, please consult a physician before using the drug.
- Special patient groups
Children
For children over 12 years of age the dosage regimen is the same as for adults. - Clotrimazole vaginal tablets should not be used in children under 12 years of age.