caa a22 4500 477056385 CHVBK 20180405111347.0 cr unu---uuuuu 170330e19960901xx s 000 0 eng 10.1007/s002280050165 doi (NATIONALLICENCE)springer-10.1007/s002280050165 Effect of the lipase inhibitor orlistat on the pharmacokinetics of four different antihypertensive drugs in healthy volunteers [Elektronische Daten] [C. Weber, Y. K. Tam, G. Schmidtke-Schrezenmeier, J. H. G. Jonkmann, P. van Brummelen] Objective: To study the influence of the lipase inhibitor orlistat on the pharmacokinetics of the antihypertensive drugs atenolol, furosemide, captopril and nifedipine. Methods: Four open-label, crossover studies were performed on six to eight healthy male volunteers. Orlistat was given in doses of 50 mg 3 times daily mid-meal for 7 (nifedipine and captopril) or 8 days (atenolol and furosemide). The four antihypertensive drugs (atenolol 100-mg tablet, furosemide 40-mg tablet, captopril 50-mg tablet and nifedipine 20-mg slow-release tablet) were administered in single doses twice, once before and once together, with orlistat at the end of the orlistat treatment period. Results: The plasma concentration time profiles and the pharmacokinetic parameters estimated for these drugs were in the expected range, except for furosemide, whose bioavailability was lower than reported in the literature. This was probably due to the fact that furosemide was given during a meal. There were minor, but statistically significant, differences in one of the pharmacokinetic parameters of furosemide and nifedipine (no difference for captopril and atenolol) when these drugs were given alone and in combination with orlistat: the half-life of furosemide was slightly longer, the time to peak plasma concentrations of nifedipine was slightly longer. None of these are considered to be clinically significant changes. Conclusions: The lipase inhibitor orlistat given 50 mg 3 times daily does not alter the pharmacokinetics of atenolol, furosemide, nifedipine and captopril to a clinically significant extent. Springer-Verlag Berlin Heidelberg, 1996 Key words Orlistat nationallicence Furosemide nationallicence Atenolol nationallicence Captopril nationallicence Nifedipine nationallicence pharmacokinetics nationallicence healthy volunteers nationallicence Weber C. F. Hoffmann-La Roche Ltd., Department of Clinical Pharmacology, Clinical Research and Development, CH-4070, Basel, Switzerland, CH aut Tam Y. K. University of Alberta, Edmonton, Canada, CA aut Schmidtke-Schrezenmeier G. LAB, Gesellschaft für Pharmakologische Untersuchungen, Neu-Ulm, Germany, DE aut Jonkmann J. H. G. Pharma Bio-Research International BV, Zuidlaren, The Netherlands, NL aut van Brummelen P. F. Hoffmann-La Roche Ltd., Department of Clinical Pharmacology, Clinical Research and Development, CH-4070, Basel, Switzerland, CH aut https://doi.org/10.1007/s002280050165 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s002280050165 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Weber C. F. Hoffmann-La Roche Ltd., Department of Clinical Pharmacology, Clinical Research and Development, CH-4070, Basel, Switzerland, CH aut NATIONALLICENCE 700 1- Tam Y. K. University of Alberta, Edmonton, Canada, CA aut NATIONALLICENCE 700 1- Schmidtke-Schrezenmeier G. LAB, Gesellschaft für Pharmakologische Untersuchungen, Neu-Ulm, Germany, DE aut NATIONALLICENCE 700 1- Jonkmann J. H. G. Pharma Bio-Research International BV, Zuidlaren, The Netherlands, NL aut NATIONALLICENCE 700 1- van Brummelen P. F. Hoffmann-La Roche Ltd., Department of Clinical Pharmacology, Clinical Research and Development, CH-4070, Basel, Switzerland, CH aut Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer