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Interaction of Ibuprofen and Probenecid with Drug Metabolizing Enzyme Phenotyping Procedures Using Caffeine as the Probe Drug by Fatima Vrtic; Walter E. Haefeli; Jürgen Drewe; Stephan Krähenbühl; Markus Wenk is a Medicine article available to read on EtoBox.

What is Interaction of Ibuprofen and Probenecid with Drug Metabolizing Enzyme Phenotyping Procedures Using Caffeine as the Probe Drug about?

**Aims** To examine the suspected inhibitory potential of the over‐the‐counter (OTC) drug ibuprofen on N‐acetyltransferase 2 (NAT2) __in vitro__ and __in vivo__ and the possible implications for phenotyping procedures using caffeine as probe drug. **Methods** We first studied the inhibitory effect of ibuprofen on NAT2 __in vitro__, using human liver cytosol and sulfamethazine as substrate. __In vivo__ 15 fast and 15 slow acetylating healthy volunteers were treated with a single dose of ibuprofen (800 mg) orally and phenotyped for NAT2, CYP1A2, and xanthine oxidase (XO) with caffeine as probe drug before and during drug treatment. Because of unexpected __in vivo__ results with ibuprofen this study was repeated in 20 healthy volunteers with probenecid, a model substrate of renal organic anion transport (OAT). For phenotyping tests a urine sample was collected 6 h after caffeine (200 mg) intake. The caffeine metabolites acetyl‐6‐formylamino‐3‐methyluracil (AFMU), 1‐methylxanthine (1MX), 1‐methyluric acid (1MU), and 1,7‐dimethyluric acid (17MU) were quantified by HPLC, and the corresponding metabolic ratios for CYP1A2, NAT2, and XO were then calculated. Genotyping for NAT2 was performe

Who reads Interaction of Ibuprofen and Probenecid with Drug Metabolizing Enzyme Phenotyping Procedures Using Caffeine as the Probe Drug?

Author

Fatima Vrtic; Walter E. Haefeli; Jürgen Drewe; Stephan Krähenbühl; Markus Wenk

Publisher

John Wiley and Sons; Wiley (Blackwell Publishing); Blackwell Publishing Inc.; Wiley; Research Square (ISSN 0306-5251)

Published

2003

Language

EN

Field

Medicine (Health Sciences)