Clotrimazole: Effects, Uses & Risks

Clotrimazole belongs to the broad-spectrum antifungal agents. The drug is used for the therapy of various fungal infections (mycoses).

What is clotrimazole?

Clotrimazole belongs to the broad-spectrum antifungal agents. It is given to treat fungal infections on the skin. Clotrimazole is an antifungal agent that comes from the imidazole group. It is administered to treat fungal infections on the skin. Because clotrimazole exerts its effect against various fungi, it is used as a broad-spectrum antifungal agent. Clotrimazole was developed between 1967 and 1969 in Germany at the research facilities of Bayer AG. Experimental as well as clinical studies followed between 1970 and 1972 to test the efficacy and tolerability of the antifungal agent. The first patents were issued in the USA in 1972. One year later, clotrimazole was launched on the German market under the brand name Canesten. The drug could be administered as a cream, vaginal tablet and solution. Because clotrimazole proved to be well tolerated, the antifungal agent was exempted from prescription requirements from 1977. Since the early 1980s, the efficacy of clotrimazole has been clarified by studies. Even in the present, the drug is used against numerous fungal skin infections.

Pharmacological effect

Clotrimazole belongs to the group of triazoles and imidazoles. The action of the antifungal agent is based on destroying the cell wall formation of harmful fungi. In this way, the growth of the fungi can be limited. Clotrimazole causes inhibition of the substance ergosterol. Ergosterol production, which takes place in various steps, is carried out by different enzymes. By inhibiting a specific enzyme, clotrimazole ensures that the build-up of ergosterol is interrupted. This results in a disruption of cell wall formation during cell division. This results in an inhibition of fungal growth, so that the fungus cannot spread further. In medicine, the anti-fungal effect is also referred to as fungistatic. With correspondingly high dosages, a fungicidal effect is also possible. Clotrimazole also has the property of being able to act against specific corynebacteria. For this reason, the antifungal agent is also suitable for the treatment of infections with these rod-shaped germs. After oral administration, 90 percent of clotrimazole is absorbed. After about four hours, the antimycotic has reached most tissues of the organism. It reaches its highest concentration after a period of 25 hours in the liver, adipose tissue, skin and adrenal glands. Inactivation of the drug also takes place in the liver. Ninety percent of clotrimazole is excreted in the feces. The remaining ten percent passes out of the body in the urine.

Medical use and application

Clotrimazole can be used to treat most disease-causing fungi. These primarily include fungal infections on the skin and female vagina, as well as nail fungal infections that occur on the hands and feet. The dosage forms of clotrimazole against skin fungi (dermatophytes), molds or yeasts are different. Thus, large-area fungal infections can be effectively treated with sprays. These are also suitable for spraying objects. These include shoes, in the case of athlete’s foot. Creams are mainly used to treat the genital region. However, vaginal suppositories or vaginal tablets can also be administered. Mostly inflammatory yeast infections are treated. Clotrimazole is also suitable for the treatment of superinfections caused by bacteria that can be treated with clotrimazole. Vaginal tablets are also effective in the treatment of trichomoniasis, which is an infection caused by the microorganism Trichomonas vaginalis. As a powder, clotrimazole is used to treat fungal skin infections. It is also possible to use the powder to prevent fungal infections. The dry effect of the powder is particularly beneficial, as fungi prefer to multiply in a moist environment. The dosage of clotrimazole depends on the extent of the fungal disease. The agent is applied or sprayed directly onto the affected area. The usual dose is one to three applications per day. In total, clotrimazole therapy takes two to four weeks.To prevent relapse, it is recommended to continue therapy for one to two weeks after the symptoms have subsided.

Risks and side effects

Side effects rarely occur as a result of treatment with clotrimazole, as the drug is generally well tolerated. However, some people may sometimes experience itching, temporary redness of the skin, stinging, burning, and dry skin. Occasionally, allergic reactions also occur. Clotrimazole should not be used if the patient suffers from hypersensitivity to the antifungal agent. During the first stage of pregnancy, clotrimazole should be administered for the treatment of vaginal fungal infection only under the strict supervision of a physician. There is a suspicion that the antifungal drug could cause a miscarriage. If the absorption of clotrimazole is localized on the skin, on the other hand, no harm to the child is to be feared. During breastfeeding, application of the antifungal agent to the breast should be avoided. The same applies to the administration of the active substance to babies and young children. With the simultaneous treatment of clotrimazole and other antifungal agents such as nystatin, natamycin and amphotericin B, interactions are possible. Thus, this leads to a decrease in the effectiveness of clotrimazole. At the same time, clotrimazole may reduce the positive effects of these drugs. Furthermore, there is a risk that the effect of the agent may be reduced by the use of cosmetics, deodorants, or intimate hygiene products.