Document Detail

Metabolic differences of current thienopyridine antiplatelet agents.
MedLine Citation:
PMID:  23289968     Owner:  NLM     Status:  MEDLINE    
INTRODUCTION: Antithrombotics are one of the most commonly prescribed classes of medication around the world. The thienopyridines are an integral part of antithrombotic therapy and are prescribed for various indications including acute coronary syndrome, peripheral vascular disease and cerebrovascular disease. These drugs have distinct metabolic pathways, which lead to the formation of active metabolites that produce both observed clinical differences as well as pharmacokinetic and pharmacodynamic differences in response.
AREAS COVERED: The authors describe the pharmacokinetic and pharmacodynamic behavior of three of the currently available thienopyridines, namely ticlopidine, clopidogrel and prasugrel. The authors also describe and discuss the drug interaction and pharmacogenomic factors which may impact safety and drug efficacy.
EXPERT OPINION: P2Y(12)-ADP receptor antagonism has proven to be effective at preventing thrombosis. Differences in the activation of these drugs, cytochrome metabolism, concomitant drug use and pharmacogenomics have an impact on thienopyridine use. Clopidogrel remains the thienopyridine drug with the most approved indications for use. Prasugrel has proven to be efficacious but is associated with a higher bleeding risk in comparison to clopidogrel and therefore has to be used in appropriate clinical indications.
Jawed Fareed; Walter Jeske; Indermohan Thethi
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Publication Detail:
Type:  Journal Article; Review     Date:  2013-01-06
Journal Detail:
Title:  Expert opinion on drug metabolism & toxicology     Volume:  9     ISSN:  1744-7607     ISO Abbreviation:  Expert Opin Drug Metab Toxicol     Publication Date:  2013 Mar 
Date Detail:
Created Date:  2013-02-19     Completed Date:  2013-08-15     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  101228422     Medline TA:  Expert Opin Drug Metab Toxicol     Country:  England    
Other Details:
Languages:  eng     Pagination:  307-17     Citation Subset:  IM    
Loyola University Chicago, Department of Pathology and Pharmacology, 2160 S. First Avenue, Maywood, Illinois 60153, USA.
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MeSH Terms
Acute Coronary Syndrome / drug therapy
Aryl Hydrocarbon Hydroxylases / genetics,  metabolism
Drug Interactions
Fibrinolytic Agents / pharmacokinetics*
Hemorrhage / drug therapy
Metabolic Detoxication, Drug
Piperazines / pharmacokinetics*
Platelet Aggregation Inhibitors / pharmacokinetics
Purinergic P2Y Receptor Antagonists / pharmacokinetics
Pyridines / pharmacokinetics*
Thiophenes / pharmacokinetics*
Ticlopidine / analogs & derivatives*,  pharmacokinetics
Reg. No./Substance:
0/Fibrinolytic Agents; 0/Piperazines; 0/Platelet Aggregation Inhibitors; 0/Purinergic P2Y Receptor Antagonists; 0/Pyridines; 0/Thiophenes; 0/thienopyridine; 34K66TBT99/prasugrel; 55142-85-3/Ticlopidine; A74586SNO7/clopidogrel; EC Hydrocarbon Hydroxylases; EC protein, human

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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