Characteristics of Clotrimazole
Clotrimazole, which has a molecular weight of 344.84, is a white odorless drug that is used in yeast and yeast-like lesions. Clotrimazole is poorly soluble in water and ether, readily soluble in polyethylene glycol 400, chloroform and ethanol. The drug is used both in the treatment of men, and women and children. The most commonly prescribed clotrimazole in gynecology, general therapy, dermatology, venereology and obstetrics. Clotrimazole from thrush is released as solutions, tablets, creams and ointments with special applicators.
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Pharmacological action of clotrimazole against thrush
Antiprotozoal, antifungal, antibacterial. Clotrimazole, a topical preparation with an antifungal effect, is derived from imidazole.
The result of the drug is a disruption in the metabolism of ergosterol, which is the main constituent of the fungal cell structure, the permeability of the fungal cell membrane, provokes the release of potassium from the cell membrane, the phosphorous compounds that make up the cell, and the destruction of intracellular nucleic acids. Retards the connection of phospholipids and triglycerides. It makes the peroxidase and oxidative enzymes less active, so that the amount of hydrogen peroxide inside the cells becomes toxic. This, in turn, leads to the fact that cellular organelles are destroyed and the cell is necrotic. Fungicidal and fungistatic effect depends on concentration. Delays the transformation of Candida Albico's blast spores into a mold penetrating inside.
Clotrimazole is slightly absorbed through the mucous membranes and skin.
Intravaginal injection - absorbed 3-10% of the drug.
In the liver, a number of transformations of clotrimazole occur before metabolites that are not active, after which it is isolated with feces. Absorbed clotrimazole is influenced by subcellular enzymatic reactions in the liver, which is why the oxidation reactions occurring in it are accelerated.
In large quantities in the vaginal secretion and in the small in the blood stream, two to three days are found.
No evidence has been obtained of the carcinogenic effects of clotrimazole on the living organism in studies on rats. Mutagenic effects, judging by studies on hamsters, are also not found.
Clotrimazole is characterized by a wide spectrum of action, especially with external application, which covers almost all fungi of pathogenic origin (which are the cause of human infection). Its activity extends to
- filamentous fungi (dermatophytes);
- mushrooms Candida and other yeast mushrooms;
- dimorphic fungal lesions;
Clotrimazole has a high potential for penetration into tissues. In the epidermis it is much more than in the subcutaneous fat and in the dermis. The drug is not characterized by systemic action. In the human body, clotrimazole from thrush finds Candida mushrooms and affects their membranes, which is why they completely lose their vitality.
Clotrimazole from thrush usually gives good results in the treatment of vaginal candidiasis. In addition, the doctor can prescribe a comprehensive treatment, combined with other drugs (often tableted). The effect of clotrimazole treatment on thrush usually comes from the first days of treatment with the drug. But this does not mean that the treatment should be stopped, it is necessary to go through the entire course of treatment prescribed by a doctor, otherwise the disease can go on into a chronic form.
Interaction with other drugs
Weaken the action of amfittericin B, nitamycin, nystatin.