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Carboxymefloquine, the major metabolite of antimalarial drug mefloquine, induces drug metabolizing enzyme and transporter expression by activation of pregnane X receptor.
Abstract Malaria patients are frequently co-infected with HIV and mycobacteria causing tuberculosis, which increases the co-administration of drugs and thereby enhances the risk of pharmacokinetic drug-drug interactions. Activation of pregnane X receptor (PXR) by xenobiotics, including many drugs, induces drug metabolism and transport, thereby possibly resulting in attenuation or loss of the therapeutic response of drugs being co-administered. While several artemisinin-type antimalarial drugs have been shown to activate PXR, data on non-artemisinin-type antimalarials are still missing. Therefore this study aims to...
Source: Antimicrobial Agents and Chemotherapy - October 13, 2014 Category: Microbiology Authors: Piedade R, Traub S, Bitter A, Nüssler AK, Gil JP, Schwab M, Burk O Tags: Antimicrob Agents Chemother Source Type: research