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
-
Endogenous Cardioprotective Agents: Role in Pre and Postconditioning
Current Drug Targets A Novel Homologous Model for Gene Therapy of Dwarfism by Non-Viral Transfer of the Mouse Growth Hormone Gene into Immunocompetent Dwarf Mice
Current Gene Therapy The Metformin Paradox
Current Diabetes Reviews Reverse Ayurvedic Pharmacology of Ashwagandha as an Adaptogenic Anti-Diabetic Plant: A Pilot Study
Current Traditional Medicine Repositioning of DHFR Inhibitors
Current Topics in Medicinal Chemistry The Medical and Medico-legal Complications of Bulimia Nervosa : Treatments and Complications
Current Women`s Health Reviews The Importance of Rhodanine Scaffold in Medicinal Chemistry: A Comprehensive Overview
Mini-Reviews in Medicinal Chemistry Inflammation-Induced Thrombosis: Mechanisms, Disease Associations and Management
Current Pharmaceutical Design Role of Insulin in Glucose-Stimulated Insulin Secretion in Beta Cells
Current Diabetes Reviews Novel Approaches to the Pharmacotherapy of Obesity
Current Pharmaceutical Design The Role of Neuronal Insulin/Insulin-Like Growth Factor-1 Signaling for the Pathogenesis of Alzheimer’s Disease: Possible Therapeutic Implications
CNS & Neurological Disorders - Drug Targets Developing Novel Therapeutic Approaches to Frailty
Current Pharmaceutical Design Applications of Natural Polymeric Materials in Solid Oral Modified-Release Dosage Forms
Current Pharmaceutical Design Inhibitors of Apoptosis Proteins (IAPs) as Potential Molecular Targets for Therapy of Hematological Malignancies
Current Molecular Medicine Bleeding Complications in the Course of Treatment with Antidepressants in Elderly Patients
Current Psychiatry Reviews Biologics: An Update and Challenge of Their Pharmacokinetics
Current Drug Metabolism Clopidogrel and Aspirin in Cardiovascular Medicine: Responders or Not -- Current Best Available Evidence
Cardiovascular & Hematological Agents in Medicinal Chemistry Antioxidant Capacity, Phytochemical Analysis and Identification of Active Compounds in Anchomanes difformis
The Natural Products Journal Molecular Docking Studies and Pharmacophore Modeling of Some Insulin Mimetic Agents from Herbal Sources: A Rational Approach towards Designing of Orally Active Insulin Mimetic Agents
Current Traditional Medicine Evolution of Antipsychotic Intervention in the Schizophrenic Psychosis
Current Drug Targets