Effects of grapefruit juice ingestion--pharmacokinetics and haemodynamics of intravenously and orally administered felodipine in healthy men

European Journal of Clinical Pharmacology
J LundahlG Johnsson

Abstract

To examine the effect of grapefruit juice on the metabolism of felodipine following intravenous and oral administration. The study had a randomised, four-way, crossover design in 12 healthy males. Single doses of felodipine were given as an intravenous infusion for 1 h (1.5 mg) or as an oral extended release (ER) tablet (10 mg). Grapefruit juice (150 ml) or water was ingested 15 min prior to drug intake. Intake of grapefruit juice did not significantly alter the intravenous pharmacokinetics of felodipine compared to control treatment, whereas after oral drug administration it did lead to an increase in the mean AUC and Cmax by 72% and 173%, respectively, and the mean absolute bioavailability was increased by 112%. The fraction of the oral felodipine dose reaching the portal system was increased from 45% to 80% when intake of drug was preceded by grapefruit juice ingestion. The pharmacokinetics of the primary metabolite, dehydrofelodipine, was affected by the intake of juice, resulting in a 46% increase in Cmax. Juice intake immediately before oral felodipine resulted in more pronounced haemodynamic effects of the drug as measured by diastolic blood pressure and heart rate. However, the haemodynamic effects of the intravenous ad...Continue Reading

Citations

Sep 27, 2005·Chinese Journal of Integrative Medicine·Fang Xia, Xiao-yin Chen
Dec 21, 2000·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·H Suzuki, Y Sugiyama
Jan 16, 2003·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·M GiorgiG Soldani
Oct 31, 2002·CMAJ : Canadian Medical Association Journal = Journal De L'Association Medicale Canadienne·J David Spence
Jul 19, 2013·Nutrition and Cancer·Kristine R MonroeMalcolm C Pike
Apr 18, 2001·Journal of Clinical Pharmacology·M J SheltonR DiFrancesco
Nov 1, 2007·Nutrition Journal·Jawad Kiani, Sardar Z Imam
Oct 6, 2005·Biological & Pharmaceutical Bulletin·Yasuharu MizuharaKoichi Yokogawa
Nov 28, 2012·CMAJ : Canadian Medical Association Journal = Journal De L'Association Medicale Canadienne·David G BaileyJ Malcolm O Arnold
Nov 30, 2011·Drug Metabolism and Pharmacokinetics·Kanoko EgashiraIchiro Ieiri
Sep 29, 2004·American Journal of Cardiovascular Drugs : Drugs, Devices, and Other Interventions·David G Bailey, George K Dresser
Dec 15, 2010·Drugs·Kay SedenDavid Back
May 11, 2011·Medicinski pregled·Zoran Z BojanićVladmila V Bojanić
Jan 25, 2011·Expert Opinion on Drug Metabolism & Toxicology·Michael J HanleyDavid J Greenblatt
Jul 16, 2008·Expert Opinion on Drug Metabolism & Toxicology·Aleksandra GaletinJ Brian Houston
Jun 23, 2015·Journal of Clinical Pharmacology·Guohua AnReginald F Frye
Aug 13, 1999·Experimental and Toxicologic Pathology : Official Journal of the Gesellschaft Für Toxikologische Pathologie·I SamojlikV Jakovljević
Aug 13, 1999·Experimental and Toxicologic Pathology : Official Journal of the Gesellschaft Für Toxikologische Pathologie·K Daković-SvajcerV Jakovljević
May 18, 2004·Journal of Clinical Pharmacology·Shiew-Mei Huang, Lawrence J Lesko
Dec 4, 2003·European Journal of Clinical Investigation·G K Dresser, D G Bailey
Nov 15, 2006·Journal of Clinical Pharmacology·S U Mertens-TalcottV Butterweck
Apr 22, 2010·Basic & Clinical Pharmacology & Toxicology·Tuija H NieminenKlaus T Olkkola
Mar 8, 2016·Expert Opinion on Drug Metabolism & Toxicology·Nicolas HohmannGerd Mikus
May 1, 2008·Drug Metabolism and Pharmacokinetics·Motohiro Kato
Mar 9, 2010·Drug Metabolism and Pharmacokinetics·Aleksandra GaletinJ Brian Houston
Sep 30, 2014·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Ya-Jie XiaoBrian Tomlinson
Oct 3, 1998·Clinical Pharmacology and Therapeutics·D G BaileyJ R Bend
Dec 18, 2003·European Journal of Clinical Nutrition·A Dahan, H Altman
Apr 30, 2002·Clinical Pharmacokinetics·Margaret M Doherty, William N Charman
Mar 21, 2001·Pediatric Hematology and Oncology·L M McGregor, P M Rosoff
Nov 13, 2008·Journal of Veterinary Pharmacology and Therapeutics·A J van DijkJ Fink-Gremmels

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