Gyne-Lotrimin (clotrimazole)

Clotrimazole, an imidazole derivative, is a synthetic azole antifungal agent.

Clotrimazole is a broad-spectrum antifungal agent that exerts its antifungal activity by interfering with the biosynthesis of ergosterol, a major component of the fungal cell membrane. As a result, cell membrane permeability is altered, causing loss of potassium and other cellular constituents. Ergosterol also plays a role in directly stimulating the growth of fungal cells.

The combined effects of these actions result in a dose- and time-dependent inhibition of fungal growth.

Clotrimazole is generally considered to be fungistatic, but exhibits fungicidal effects at higher concentrations. In vitro, clotrimazole exhibits fungistatic and fungicidal activity against most strains of Trichophyton rubrum, T. mentagrophytes, Epidermophyton floccosum, and Microsporum canis, and Candida species including Candida albicans. In general, the in vitro activity of clotrimazole corresponds to that of tolnaftate and griseofulvin against the mycelia of dermatophytes (Trichophyton, Microsporum, and Epidermophyton), and to that of the polyenes (amphotericin B and nystatin) against Candida.

Resistance to clotrimazole has been observed in some Candida isolates, particularly in immunocompromised patients, and has been linked to overexpression of efflux pump genes. Cross resistance can occur among the azole antifungals (e.g., clotrimazole, ketoconazole, miconazole).

Following oral administration of a lozenge containing 10 mg of clotrimazole and dissolution of the lozenge in the mouth (which takes approximately 30 minutes), concentrations of clotrimazole sufficient to inhibit most species of Candida are present in saliva for up to 3 hours. Administration of a 10-mg clotrimazole lozenge every 3 hours reportedly maintains salivary concentrations of clotrimazole greater than the MIC of the drug for most species of Candida. The long-term effective concentration of clotrimazole in saliva appears to be related to slow release of the drug from the oral mucosa to which the drug is apparently bound.

The total amount of clotrimazole absorbed following dissolution in the mouth of a lozenge containing the drug has not been determined to date.

Following topical and vaginal administration, clotrimazole appears to be minimally absorbed. Following application to the skin, the highest concentrations of clotrimazole are present in the stratum corneum; lower drug concentrations occur in the stratum spinosum and the papillary and reticular dermis.

USES: This medication is used to treat vaginal yeast infections. Clotrimazole reduces vaginal burning, itching, and discharge that may occur with this condition. This medication is an azole antifungal.

It works by stopping the growth of yeast (fungus) that causes the infection. The vaginal product comes in 2 forms (a vaginal cream or tablet). Some products come with a skin cream to be applied to the area around the outside of the vagina.

Ask your doctor before using this medication for self-treatment if this is your first vaginal infection. This medication only works for vaginal fungal infections. You may have a different type of infection (such as bacterial vaginosis) and may need a different medication.

If you have fever, chills, flu-like symptoms, stomach/abdominal pain, or a bad-smelling vaginal discharge, do not use this medication. Contact your doctor right away because these may be signs of a more serious infection.

Generic name: clotrimazole
Pronunciation: (kloe-TRIM-a-zole)
Drug class: Vaginal Antifungal Agents
Therapeutic class: Vaginal Products

The following indications are listed for Gyne-Lotrimin:

• Vulvovaginal Candidiasis

Also known as: Vaginal Candidiasis, Vulvovaginal Candidosis, Vulvovaginal Moniliasis.