Clotrimazole (Bay b 5097): In Vitro and Clinical Pharmacological Studies

Author:

Burgess M. A.1,Bodey Gerald P.1

Affiliation:

1. Department of Developmental Therapeutics, The University of Texas M. D. Anderson Hospital and Tumor Institute, Houston, Texas 77025

Abstract

Clotrimazole (Bay b 5097) is a new synthetic antifungal drug with in vitro activity against Candida spp., Torulopsis glabrata , and Saccharomyces spp. Pharmacological studies in man after the oral administration of 1.5 and 3 g of clotrimazole produced mean peak concentrations in the serum of 1.16 and 1.29 μg/ml, respectively, 2 hr after administration. In six patients taking 1.5 g of clotrimazole every 6 hr, there was a progressive decline in the serum concentrations after administration of a dose on days 1, 4, and 8. Nine other patients begun on a similar schedule manifested gastrointestinal symptoms attributed to the clotrimazole and were unable to complete the study. Concentrations of active drug in the urine were less than 1% of the administered dose.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

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