Absolute bioavailability and pharmacokinetics of valsartan, an angiotensin II receptor antagonist, in man

European Journal of Clinical Pharmacology
G FleschP Lloyd

Abstract

The pharmacokinetics of orally and intravenously administered valsartan were determined in two studies. In a first pilot study, three i.v. doses of valsartan were given in an ascending manner (5, 10 and 20 mg) to evaluate tolerability and basic pharmacokinetics of the i.v. formulation. In a second study, the absolute bioavailability of 80 mg valsartan from a capsule and a buffered solution was compared with a 20 mg i.v. dose. The concentrations of valsartan in plasma and urine were measured using HPLC. The disposition of valsartan after an i.v. dose was characterized by biphasic decay kinetics, with a distribution phase (half-life 1.0 h), followed by a longer elimination phase (half-life 9.5 h). The volume of distribution at steady state was 16.9 l, and the total body clearance 2.2 l.h-1. 29% of the i.v. dose was recovered unchanged in the urine. Plasma levels peaked 2 h after oral administration of the 80 mg capsule. Thereafter, plasma levels declined biexponentially with a terminal t1/2 of 7.0 h. Cmax was reached 1 h after administration of the solution, and t1/2 was 7.5 h. On average 7.3% (capsule) and 12.6% (solution) of the dose was excreted in the urine as the unchanged drug. The fraction of dose absorbed and systemically...Continue Reading

Citations

Nov 26, 2009·Journal of Pharmacokinetics and Pharmacodynamics·Agnès PoirierThierry Lavé
Sep 13, 2008·Archives of Pharmacal Research·Zong-Zhu PiaoBeom-Jin Lee
Aug 31, 2010·Archives of Pharmacal Research·Young Joon ParkHyo-Kyung Han
Jun 21, 2001·The Journal of Clinical Hypertension·D A Sica
Dec 17, 2008·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Koji AbeKim L R Brouwer
May 22, 2001·Journal of Clinical Pharmacology·L R Schwocho, H N Masonson
Jan 30, 2010·AAPS PharmSciTech·Howida Kamal Ibrahim, Doaa A El-Setouhy
Jul 1, 2004·Nihon yakurigaku zasshi. Folia pharmacologica Japonica·Motohiko ChachinHisashi Satoh
May 17, 2011·Patient Preference and Adherence·Rossana Baracco, Gaurav Kapur
Jul 21, 2005·Clinical Pharmacokinetics·Domenic A SicaSiddhartha Ghosh
Nov 17, 2009·Drugs·Henry R BlackRita Samuel
May 2, 2013·Journal of Microencapsulation·Durga Maheswari ParvataneniLakshmi Narasu Mangamoori
Sep 25, 2012·Expert Opinion on Drug Metabolism & Toxicology·Cassandra D Benge, James A S Muldowney
Aug 21, 2015·Drug Development and Industrial Pharmacy·Vijaykumar NekkantiGuru V Betageri
Jun 8, 2012·Drug Development and Industrial Pharmacy·Venkatesh R ChallaC Maheswari
Aug 20, 2009·Expert Opinion on Drug Metabolism & Toxicology·Robyn Kondrack, Syed Mohiuddin
Jul 5, 2005·Expert Opinion on Investigational Drugs·A Chioléro, M Burnier
Mar 1, 2014·Clinical Pharmacology in Drug Development·Gangadhar SunkaraVenkateswar Jarugula
Nov 22, 2008·European Journal of Clinical Investigation·A StorkaM Wolzt
Jan 31, 2009·Journal of Clinical Pharmacology·Jeffrey BlumerGangadhar Sunkara
May 11, 2012·Acta Anaesthesiologica Scandinavica·R NabbiH J Woehlck
Apr 7, 2016·Pharmaceutical Development and Technology·Ying HuangXuefeng Mei
Aug 1, 2015·CPT: Pharmacometrics & Systems Pharmacology·R LiT S Maurer
Mar 16, 2001·Expert Opinion on Pharmacotherapy·P A Thürmann
May 12, 2009·Drug Metabolism and Pharmacokinetics·Bahru HabtemariamGoonaseelan Pillai
Jun 9, 2016·Drugs·Hae-Young Lee, Byung-Hee Oh
Dec 15, 2015·Biopharmaceutics & Drug Disposition·Seung Jun YangHyo-Kyung Han
Jul 24, 2014·Archives of Pharmacal Research·Kyung Ran LeeKyeong Ho Kim
Mar 12, 2003·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Harumi KitagawaAngela L Burnett
Aug 18, 2004·Blood Pressure Monitoring·Yves LacourcièreHelmut Schumacher
Nov 20, 2018·The Annals of Pharmacotherapy·Dawn BattiseDonald S Nuzum

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antihypertensive Agents: Mechanisms of Action

Antihypertensive drugs are used to treat hypertension (high blood pressure) which aims to prevent the complications of high blood pressure, such as stroke and myocardial infarction. Discover the latest research on antihypertensive drugs and their mechanism of action here.