Abstract
Clopidogrel, an antiplatelet agent, prevents platelet aggregation by inhibiting the adenosine disphosphate (ADP) P2Y12 receptor, which is located on the platelet surface. Although dual antiplatelet therapy appears to be efficient, a considerable number of patients continue to experience adverse cardiovascular events, such as stent thrombosis. The percentage of low response to antiplatelet therapy varies from 4% to 30% of patients depending on the cut-off values. In addition, several factors such as poor absorption, drug-to-drug interactions, inadequate dosing, elevated body mass index, insulin resistance and the nature of acute coronary syndromes have been implicated in low clopidogrel response. Recently, studies have focused on the role of genetic polymorphisms encoding enzymes that participate in clopidogrel hepatic metabolism or receptors involved in intestinal absorption and ADP induced platelet aggregation, which may affect the percentage of platelet inhibition after clopidogrel administration. The management of clopidogrel resistance remains a controversial issue and additional studies are required to evaluate the safety and efficacy of increased loading of clopidogrel or replacement with other new antiplatelet agents such as prasugrel.
Keywords: Clopidogrel resistance, cytochrome P450, gene polymorphisms, platelets, thrombus, Clopidogrel, atherosclerosis, adenosine disphosphate, atherosclerotic disease, multifactorial pattern, cytochrome, carbon monoxide, enzymes, phospholipids, detoxification, coagulation, body mass index, polymorphisms, platelet, healthy Caucasians, coronary artery disease, erythromycin, antiplatelet therapy, percentile distribution, platelet function analyzer (PFA), vasodilator, phosphoprotein
Current Medicinal Chemistry
Title: The Role of the Cytochrome P450 Polymorphisms in Clopidogrel Efficacy and Clinical Utility
Volume: 18 Issue: 3
Author(s): D. Tousoulis, G. Siasos, M. Zaromytidou, N. Papageorgiou, E. Stefanadi, E. Oikonomou and C. Stefanadis
Affiliation:
Keywords: Clopidogrel resistance, cytochrome P450, gene polymorphisms, platelets, thrombus, Clopidogrel, atherosclerosis, adenosine disphosphate, atherosclerotic disease, multifactorial pattern, cytochrome, carbon monoxide, enzymes, phospholipids, detoxification, coagulation, body mass index, polymorphisms, platelet, healthy Caucasians, coronary artery disease, erythromycin, antiplatelet therapy, percentile distribution, platelet function analyzer (PFA), vasodilator, phosphoprotein
Abstract: Clopidogrel, an antiplatelet agent, prevents platelet aggregation by inhibiting the adenosine disphosphate (ADP) P2Y12 receptor, which is located on the platelet surface. Although dual antiplatelet therapy appears to be efficient, a considerable number of patients continue to experience adverse cardiovascular events, such as stent thrombosis. The percentage of low response to antiplatelet therapy varies from 4% to 30% of patients depending on the cut-off values. In addition, several factors such as poor absorption, drug-to-drug interactions, inadequate dosing, elevated body mass index, insulin resistance and the nature of acute coronary syndromes have been implicated in low clopidogrel response. Recently, studies have focused on the role of genetic polymorphisms encoding enzymes that participate in clopidogrel hepatic metabolism or receptors involved in intestinal absorption and ADP induced platelet aggregation, which may affect the percentage of platelet inhibition after clopidogrel administration. The management of clopidogrel resistance remains a controversial issue and additional studies are required to evaluate the safety and efficacy of increased loading of clopidogrel or replacement with other new antiplatelet agents such as prasugrel.
Export Options
About this article
Cite this article as:
Tousoulis D., Siasos G., Zaromytidou M., Papageorgiou N., Stefanadi E., Oikonomou E. and Stefanadis C., The Role of the Cytochrome P450 Polymorphisms in Clopidogrel Efficacy and Clinical Utility, Current Medicinal Chemistry 2011; 18 (3) . https://dx.doi.org/10.2174/092986711794839151
DOI https://dx.doi.org/10.2174/092986711794839151 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Calcium Related Genes in Dogs as Potential Cardiac Biomarkers for the Detection of Chronic Mitral Valve Disease
Recent Patents on Biomarkers Focus on the Multimodal Role of Biomarkers in Breast Cancer
Current Pharmaceutical Design Reduction in Estimated Glomerular Filtration Rate (eGFR) Results in an Increased Risk of Spontaneous Hemorrhagic Transformation in Patients with Large-artery Atherosclerosis Stroke
Current Neurovascular Research Polymorphism of Secretary PLA2G2A Gene Associated with Its Serum Level in Type2 Diabetes Mellitus Patients in Northern Iran
Endocrine, Metabolic & Immune Disorders - Drug Targets In Silico Computations of Selective Phytochemicals as Potential Inhibitors Against Major Biological Targets of Diabetes Mellitus
Current Computer-Aided Drug Design Prevention of Gestational Diabetes Mellitus (GDM) and Probiotics: Mechanism of Action: A Review
Current Diabetes Reviews Assessment of Endothelial Function by Positron Emission Tomography
Current Cardiology Reviews Myocardial Infarction with and without ST-segment Elevation: a Contemporary Reappraisal of Similarities and Differences
Current Cardiology Reviews A Systematic Review on Pharmaceutical Diabetic Care Services in the United Arab Emirates (UAE)
Current Diabetes Reviews Protein Degradation by the Ubiquitin-Proteasome Pathway and Organ Fibrosis
Current Medicinal Chemistry Dyslipidemia, Vascular Atheroma and Statins
Current Vascular Pharmacology Apoptosis Induction by Thalidomide: Critical for Limb Teratogenicity but Therapeutic Potential in Idiopathic Pulmonary Fibrosis?
Current Molecular Pharmacology Screening of Enzyme Inhibitors from Traditional Chinese Medicine
Combinatorial Chemistry & High Throughput Screening DNA Damage and Epigenetic Changes in Kidney Diseases - Focused on Transcription Factors in Podocytes
Current Hypertension Reviews Hypothyroidism and Endothelial Function: A Marker of Early Atherosclerosis?
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery New Cell Therapy Using Bone Marrow-Derived Stem Cells/Endothelial Progenitor Cells to Accelerate Neovascularization in Healing of Experimental Ulcerative Colitis
Current Pharmaceutical Design Recent Developments on Endothelin Antagonists as Immunomodulatory Drugs - from Infection to Transplantation Medicine
Recent Patents on Cardiovascular Drug Discovery Water Soluble Vitamins and their Role in Diabetes and its Complications
Current Diabetes Reviews Etiopathogenesis, Classical Immunotherapy and Innovative Nanotherapeutics for Inflammatory Neurological Disorders
Current Nanoscience LncRNA as a Therapeutic Target for Angiogenesis
Current Topics in Medicinal Chemistry