Pharmacology: Pharmacodynamics: Mechanism of Action: Clotrimazole, an imidazole derivative, exerts antifungal effects by inhibition of fungal sterol synthesis. Clotrimazole appears to inhibit the enzymatic conversion of 2, 4-methylenedihydrolanosterol to demethylsterol, the precursor to ergosterol, which is an essential building block of the cytoplasmic membrane of the fungi.
Antimicrobial Spectrum: Fungi: Clotrimazole is a broad-spectrum antifungal agent that inhibits the growth of most fungi pathogenic to man, including the following: Candida spp; Dermatophytes (Trichophyton, Microsporum, Epidermophyton), Malassezia furfur.
Gram positive bacteria: Clotrimazole is known to possess in vitro activity against certain Gram positive bacteria.
Pharmacokinetics: Quantified pharmacokinetic studies for Clotrimazole (Candiva Ear Drops) have not been extensively conducted. Following are the relevant pharmacokinetic details of other topical Clotrimazole formulations: Systemic absorption following use of topical Clotrimazole preparations is very low. Estimated bioavailability is less than 0.5%. No Clotrimazole could be detected in the serum and the biochemical monitoring remained unchanged in animal studies with cutaneous Clotrimazole application. Clotrimazole concentrations achieved in the epidermal layers exceed the minimal inhibitory concentrations (MICs) for almost all pathogenic fungi. The highest levels are achieved in the stratum corneum (50 to 100 mcg/mL) and the lowest in the stratum basale papillare (1.53 to 3 mcg/mL). Absorbed Clotrimazole appears to be largely excreted in the feces, primarily via biliary excretion.
Other Services
Country
Account