Itch Relief (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: Clotrimazole is used to treat skin infections such as athlete's foot, jock itch, ringworm, and other fungal skin infections (candidiasis). This medication is also used to treat a skin condition known as pityriasis (tinea versicolor), a fungal infection that causes a lightening or darkening of the skin of the neck, chest, arms, or legs. Clotrimazole is an azole antifungal that works by preventing the growth of fungus.

Generic name: clotrimazole
Pronunciation: (kloe-TRIM-a-zole)
Drug class: Topical Antihistamines
Therapeutic class: Dermatological

The following indications are listed for Itch Relief:

• Cutaneous Candidiasis
• Diaper Rash
• Tinea Corporis
• Tinea Cruris
• Tinea Pedis
• Tinea Versicolor

Also known as: Corporeal Ringworm, Cutaneous Candidosis, Cutaneous Moniliasis, Dermatomycosis Pedis, Dhobie Itch, Diaper Dermatitis, Eczema Marginatum, Jock Itch, Pityriasis Versicolor, Tinea Circinata, Tinea Furfuracea, Tinea Glabrosa, Tinea Inguinalis, Tinea Of The Foot.