title: Pharmacology of antithrombotic drugs: an assessment of oral antiplatelet and anticoagulant treatments.
abstract: Antithrombotic drugs, which include antiplatelet and anticoagulant therapies, prevent and treat many cardiovascular disorders and, as such, are some of the most commonly prescribed drugs worldwide. The first drugs designed to inhibit platelets or coagulation factors, such as the antiplatelet clopidogrel and the anticoagulant warfarin, significantly reduced the risk of thrombotic events at the cost of increased bleeding in patients. However, both clopidogrel and warfarin have some pharmacological limitations including interpatient variability in antithrombotic effects in part due to the metabolism, interactions (eg, drug, environment, and genetic), or targets of the drugs. Increased knowledge of the pharmacology of antithrombotic drugs and the mechanisms underlying thrombosis has led to the development of newer drugs with faster onset of action, fewer interactions, and less interpatient variability in their antithrombotic effects than previous antithrombotic drugs. Treatment options now include the next-generation antiplatelet drugs prasugrel and ticagrelor, and, in terms of anticoagulants, inhibitors that directly target factor IIa (dabigatran) or Xa (rivaroxaban, apixaban, edoxaban) are available. In this Series paper we review the pharmacological properties of these most commonly used oral antithrombotic drugs, and explore the development of antiplatelet and anticoagulant therapies.
authors.affiliation: TIMI Study Group, Division of Cardiovascular Medicine, Brigham and Women's Hospital, Harvard Medical School, Boston, MA, USA. Electronic address: jmega@partners.org.
authors.forename: Jessica L
authors.initials: JL
authors.lastname: Mega
authors.affiliation: Assistance Publique-Hôpitaux de Paris, Hôpital Saint Antoine, Department of Clinical Pharmacology and Unité de Recherche Clinique (URCEST), Paris, France; Université Pierre et Marie Curie, Paris, France; Institut National de la Santé et de la Recherche Médicale, National Institute of Health and Medical Research, U-698, Paris, France.
authors.forename: Tabassome
authors.initials: T
authors.lastname: Simon
mesh_terms: D000284:Administration, Oral; D000925:Anticoagulants / Q000008:administration & dosage / Q000494:pharmacology*; D001777:Blood Coagulation / Q000187:drug effects; D001792:Blood Platelets / Q000187:drug effects; D003577:Cytochrome P-450 Enzyme System / Q000187:drug effects; D006801:Humans; D010975:Platelet Aggregation Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D058921:Purinergic P2Y Receptor Antagonists / Q000008:administration & dosage
chemical_list: D000925:Anticoagulants; D010975:Platelet Aggregation Inhibitors; D058921:Purinergic P2Y Receptor Antagonists; D003577:Cytochrome P-450 Enzyme System