Overview
active substance - clotrimazole 1 g,
Excipients: cetostearyl alcohol, octyldodecanol, polysorbate 60, sorbitan stearate, synthetic spermaceti, benzyl alcohol, purified water.
Description
Homogeneous mass of white color
Pharmacotherapeutic group
Antifungal drugs for external use. Derivatives of imidazole and triazole. Clotrimazole.
ATX Code D01AC01
Pharmacological properties
Pharmacokinetics
After applying Clotrimazole cream to the skin, clotrimazole is absorbed by the epidermis. Higher concentrations of clotrimazole are found in the horny and prickly layers of the epidermis, as well as in the papillae and the reticular layer of the dermis. Clotrimazole is poorly absorbed through the skin and mucous membranes and has virtually no systemic effect.
Clotrimazole is metabolized in the liver to inactive substances excreted in urine and feces.
Pharmacodynamics
Clotrimazole inhibits cell growth and division. In additionally concentrations it acts fungistatically, in large - fungicidal. The antimycotic effect of clotrimazole is associated with a violation of the synthesis of ergosterol, which is part of the cell membrane of fungi, and binding to phospholipids of the fungal cell wall.
Clinical studies have shown that the effect of clotrimazole is similar to the effect of imidazole derivatives - econazole and ketoconazole.
In a Beclotrim cell, clotrimazole also inhibits the biosynthesis of protein, fats, DNA and polysaccharides, destroys cellular nucleic acids and increases potassium loss. It can inhibit the activity of enzymes and the biosynthesis of triglycerides and phospholipids in the cell wall. In high concentrations, clotrimazole causes damage to the cell membrane through mechanisms independent of sterol synthesis.
Clotrimazole used to treat infections caused by C.albicans, inhibits the transformation of the blastophore into its invasive form. Changes in the structure of the cell membrane lead to cell death. The degree of influence of the drug depends on the degree of susceptibility of the microorganism to clotrimazole.
Clotrimazole is characterized by a wide range of antifungal and antimicrobial effects, inhibits growth and leads to the death of dermatophytes (Epidermophyton floccosum, Microsporum canis, Trichophyton mentagrophytes, Trichophyton rubrum),yeast-like mushrooms (Candida sp., Cryptococcus neoformans), dimorphic mushrooms (Coccidioides immitis, Histoplasma capsulatum, Paracoccidicides brasiliensis) and protozoa (Trichomonas vaginalis).
Clotrimazole has an antimicrobial effect against gram-positive microorganisms: Streptococcus, Staphylococcus, Gardnerella vagiinalis and gram-negative microorganisms (Bacteroides) No effect on Beclotrim acid bacteria (Lactobacilli).
In vitro clotrimazole inhibits reproduction Corynebacteria and gram-positive cocci - with the exception of enterococci - in a concentration of 0.5-10 μg / ml of substrate.
In vitro Clotrimazole has a wide fungistatic and fungicidal effect. Its effect on dermatophytes is similar to the effect exerted by griseofulvin, and on organisms of the genus Candida - polyenes (amphotecin B and nystatin).
At concentrations below 1 µg / ml, clotrimazole inhibits most strains. Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum and Microsporum canis.
At a concentration of 3 μg / ml, clotrimazole inhibits the growth of most bacteria: Pitorosporum orbiculare, Beclotrim fumigatus, Candida species, including Candida albicans, some strains Staphylococcus aureus, Streptococcus pyogenis, and also some strains Proteus vulgaris and Salmonella. Clotrimazole is active against Sporotrix, Cryptococcus, Cefalosporium and Fusarium. Concentrations above 100 mcg / ml are effective against Trichomonas vaginalis.
Clotrimazole-resistant strains are extremely rare, the only described strain with characteristic resistance - Candida guilliermondi.
There are no reports of resistance among clotrimazole-sensitive strains after plating Candida albicans and Trichophyton mentagrophytes. No clotrimazole resistance was observed in the strains C. albicans with resistance to polyene antibiotics.
Indications for use
- local prescribe of skin infections of the surfaces of the hands, feet, body, legs and legs caused by dermatophytes (Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum and Microsporum canis)
