Description: Clotrimazole Cream contains clotrimazole, a synthetic antifungal agent having the chemical name {1-(o-Chloro-α, α -diphenylbenzyl)imidazole};Clotrimazole is an odorless, white crystalline substance. It is practically insoluble in water, sparingly soluble in ether and very soluble in polyethylene glycol 400, ethanol and chloroform.
Pharmacological effects: Clotrimazole is a broad-spectrum antifungal agent that is used for the treatment of dermal infections caused by various species of pathogenic dermatophytes, yeasts, and Malassezia furfur. The primary action of clotrimazole is against dividing and growing organisms.
In vitro,clotrimazole exhibits fungistatic and fungicidal activity against isolates of Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum,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 budding fungi (Candida). Using an in vivo (mouse) and an in vitro (mouse kidney homogenate) testing system, clotrimazole and micronazole were equally effective in preventing the growth of the pseudomycelia and mycelia of Candida albicans.Strains of fungi having a natural resistance to clotrimazole are rare. Only a single isolate of Candida guilliermondi has been reported to have primary resistance to clotrimazole.No single-step or multiple-step resistance to clotrimazole has developed during successive passages of Candida albicans and Trichophyton mentagrophytes. No appreciable change in sensitivity was detected after successive passage of isolates of C. albicans, C krusei, or C. pseudotropicalis in liquid or solid media containing clotrimazole. Also, resistance could not be developed in chemically induced mutant strains of polyene-resistant isolates of C. albicans. Slight, reversible resistance was noted in three isolates of C. albicans tested by one investigator. There is a single report that records the clinical emergence of C. albicans strain with considerable resistance to flucytosine and micronazole, and with cross-resistance to clotrimazole, the strain remained sensitive to nystatin and amphotericin B.
Pharmacokinetics: Clotrimazole appears to be well absorbed in humans following oral administration and is eliminated mainly as inactive metabolites. Following topical and vaginal administration, however, clotrimazole appears to be minimally absorbed.Six hours after the application of radioactive clotrimazole 1% cream and 1% solution onto intact and acutely inflamed skin, the concentration of clotrimazole varied from 100 mcg/cm3 in the stratum corneum to 0.5 to 1 mcg/cm3 in the stratum reticulare, and 0.1 mcg/cm3 in the subcutis. No measurable amount of radioactivity (≤0.001 mcg/mL) was found in the serum within 48 hours after application under occlusive dressing of 0.5 mL of the solution or 0.8 g of the cream. Only 0.5% or less of the applied radioactivity was excreted in the urine.Following intravaginal administration of 100 mg 14C-clotrimazole vaginal tablets to nine adult females, an average peak serum level, corresponding to only 0.03 μg equivalent/mL of clotrimazole, was reached one to two days after application. After intravaginal administration of 5 g of 1% 14C-clotrimazole vaginal cream containing 50 mg active drug, to five subjects (one with candidal colpitis), serum levels corresponding to approximately 0.01 μg equivalents/mL were reached between 8 and 24 hours after application.
Indications: Treating vaginal yeast infections and relieving external itching and irritation caused by yeast infections. Clotrimazole cream is an antifungal agent. It works by weakening the cell membrane of the fungus, resulting in the death of the fungus.
Precautions: If irritation or sensitivity develops with the use of Clotrimazole Cream, treatment should be discontinued and appropriate therapy instituted.Use the medication for the full treatment time even though the symptoms may have improved. Notify the physician if there is no improvement after four weeks of treatment.Inform the physician if the area of application shows signs of increased irritation (redness, itching, burning, blistering, swelling, oozing) indicative of possible sensitization.Avoid the use of occlusive wrappings or dressings.
Adverse reaction: The following adverse reactions have been reported in connection with the use of this product: erythema, stinging, blistering, peeling, edema, pruritis, urticaria, burning, and general irritation of the skin.
