Bifonazole and clotrimazole. Their mode of action and the possible reason for the fungicidal behaviour of bifonazole.

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Berg D, Regel E, Harenberg HE, Plempel M

Bifonazole and clotrimazole. Their mode of action and the possible reason for the fungicidal behaviour of bifonazole.

Arzneimittelforschung. 1984;34(2):139-46.

PubMed ID

6372801 [ View in PubMed

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Abstract

Bifonazole (Bay h 4502, Mycospor) and clotrimazole (Bay b 5097, Canesten) are potent inhibitors of ergosterol synthesis in yeasts and dermatophytes. Inhibition of demethylation of 4,4',14-trimethylsterols is accepted as primary mode of action responsible for their fungistatic efficacy. In Candida albicans, Microsporum canis, Trichophyton mentagrophytes as well as in Epidermophyton floccosum the ergosterol precursor 24-methylendihydrolanosterol accumulates, whereas in Torulopsis glabrata lanosterol accumulation occurs, due to the fact that in this organism side chain alkylation proceeds after demethylation reactions. Bifonazole additionally leads to a generally decreased rate of sterol biosynthesis as compared to clotrimazole, due to a direct inhibition of microsomal HMG-CoA-reductase. The additional fungicidal effects of bifonazole are considered to originate from a sequential action by inhibition of HMG-CoA-reductase and of cytochrome P450.

DrugBank Data that Cites this Article

Drugs

Bifonazole

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Bifonazole	Cytochrome P450 51	Protein	Yeast	Yes	Inhibitor	Details