Comparative pharmacokinetics and pharmacodynamics of platelet adenosine diphosphate receptor antagonists and their clinical implications.

Clinical Pharmacokinetics
Christopher N FloydAlbert Ferro

Abstract

Over the last two decades or more, anti-platelet therapy has become established as a cornerstone in the treatment of patients with ischaemic cardiovascular disease, since such drugs effectively reduce arterial thrombotic events. The original agent used in this context was aspirin (acetylsalicylic acid) but, with the advent of adenosine diphosphate (ADP) receptor antagonists, the use of dual anti-platelet therapy has resulted in further improvement in cardiovascular outcomes when compared with aspirin alone. The first group of platelet ADP receptor antagonists to be developed was the thienopyridine class, which comprise inactive pro-drugs that require in vivo metabolism to their active metabolites before exerting their inhibitory effect on the P2Y(12) receptor. Clopidogrel has been the principal ADP receptor antagonist in use over the past decade, but is limited by variability in its in vivo inhibition of platelet aggregation (IPA). The pharmacokinetics of clopidogrel are unpredictable due to their vulnerability to multiple independent factors including genetic polymorphisms. Expression of the 3435T/T genetic variant encoding the MDR1 gene for the P-glycoprotein efflux transporter results in a significantly reduced maximum drug ...Continue Reading

References

Aug 25, 2001·Lancet·S R MehtaUNKNOWN Clopidogrel in Unstable angina to prevent Recurrent Events trial (CURE) Investigators
Nov 19, 2002·JAMA : the Journal of the American Medical Association·Steven R SteinhublUNKNOWN CREDO Investigators. Clopidogrel for the Reduction of Events During Observation
Dec 18, 2002·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Thomas A Clarke, Lucy A Waskell
Feb 3, 2004·The Journal of Clinical Investigation·Robert T Dorsam, Satya P Kunapuli
Mar 17, 2005·European Heart Journal·Sigmund SilberUNKNOWN Task Force for Percutaneous Coronary Interventions of the European Society of Cardiology
Jun 29, 2005·Circulation·James D BeckSteven Offenbacher
Jan 18, 2006·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Jessica L Fayer RehmelBarbara J Ring
Feb 10, 2006·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Mary F PaineDarryl C Zeldin
Nov 2, 2006·British Journal of Clinical Pharmacology·Joseph A JakubowskiKenneth J Winters
Nov 23, 2006·Clinical Pharmacology and Therapeutics·Dirk TaubertEdgar Schömig
Apr 4, 2007·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Nagy A FaridMark J Goldberg
Sep 11, 2007·Bioorganic & Medicinal Chemistry Letters·Brian SpringthorpePaul A Willis
Nov 6, 2007·The New England Journal of Medicine·Stephen D WiviottUNKNOWN TRITON-TIMI 38 Investigators
Nov 22, 2007·Journal of Cardiovascular Pharmacology·Christopher D PayneKenneth J Winters
Mar 29, 2008·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Eric T WilliamsNagy A Farid
Aug 30, 2008·Journal of Thrombosis and Haemostasis : JTH·I AlgaierI von Kügelgen
Sep 13, 2008·Current Medical Research and Opinion·David S SmallKenneth J Winters
Oct 24, 2008·Arteriosclerosis, Thrombosis, and Vascular Biology·Christian Weber
Dec 25, 2008·The New England Journal of Medicine·Tabassome SimonUNKNOWN French Registry of Acute ST-Elevation and Non-ST-Elevation Myocardial Infarction (FAST-MI) Investigators
Mar 10, 2009·The American Journal of Cardiology·Betti GiustiGian Franco Gensini

❮ Previous
Next ❯

Citations

Apr 17, 2013·Molecular Diagnosis & Therapy·C F SamerJ A Desmeules
Dec 18, 2013·British Journal of Anaesthesia·H T BenzonR O Bonow
Sep 3, 2013·Pharmacology & Therapeutics·Christopher N Floyd, Albert Ferro
Jun 12, 2013·Expert Opinion on Drug Metabolism & Toxicology·Stavros ApostolakisEduard Shantsila
Oct 12, 2013·European Journal of Clinical Investigation·Eva-Luise HoblBernd Jilma
Jan 11, 2014·Journal of Thrombosis and Haemostasis : JTH·J M Siller-MatulaG Delle-Karth
May 7, 2014·International Journal of Cancer. Journal International Du Cancer·Simon GebremeskelMichael Bezuhly
Jun 24, 2015·Drug Metabolism and Pharmacokinetics·Nontaya NakkamWichittra Tassaneeyakul
Apr 22, 2015·Pharmacogenomics·Henrik Berg RasmussenUNKNOWN INDICES Consortium
Apr 15, 2015·Prostaglandins & Other Lipid Mediators·Christopher N Floyd, Albert Ferro
Jun 13, 2018·Journal of Cardiovascular Medicine·Carlo Di MarioFrancesco Rossi
Aug 15, 2015·Arteriosclerosis, Thrombosis, and Vascular Biology·Thomas HoeferTimothy D Warner
Oct 17, 2018·VASA. Zeitschrift für Gefässkrankheiten·Joseph PultarThomas Gremmel
Mar 6, 2019·Biomedical Chromatography : BMC·Hajnal KelemenLajos Attila Papp
May 21, 2013·Pharmacological Reviews·Julie A Johnson, Larisa H Cavallari
May 6, 2019·British Journal of Clinical Pharmacology·Simon B DimmittRobin E Ferner
Jan 22, 2020·Journal of Cardiovascular Pharmacology and Therapeutics·Maximilian TscharreThomas Gremmel
Apr 21, 2017·Journal of Cardiovascular Translational Research·Patricia P WadowskiThomas Gremmel
Jul 27, 2018·Research and Practice in Thrombosis and Haemostasis·Thomas GremmelDeepak L Bhatt
Sep 26, 2013·Journal of Cardiovascular Pharmacology and Therapeutics·Owen MogabgabRobert P Giugliano
Jun 1, 2017·Vox Sanguinis·T Gremmel, S Panzer
Jan 13, 2018·Clinical & Experimental Metastasis·Alison J GareauMichael Bezuhly
Jul 12, 2019·Research and Practice in Thrombosis and Haemostasis·Patricia P WadowskiThomas Gremmel

❮ Previous
Next ❯

Related Concepts

Related Feeds

Cardiovascular Disease Pathophysiology

Cardiovascular disease involves several different processes that contribute to the pathological mechanism, including hyperglycemia, inflammation, atherosclerosis, hypertension and more. Vasculature stability plays a critical role in the development of the disease. Discover the latest research on cardiovascular disease pathophysiology here.