title: Vorapaxar for reduction of thrombotic cardiovascular events in myocardial infarction and peripheral artery disease.
abstract: OBJECTIVE
  The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, dosage and administration, cost, and place in therapy of vorapaxar in the secondary prevention of atherosclerotic events are reviewed.
  
  
  CONCLUSIONS
  Vorapaxar is a highly selective, reversible antagonist of protease-activated receptor-1 expressed on platelets. Vorapaxar competitively inhibits thrombin from activating the receptor, thereby decreasing platelet aggregation. Vorapaxar is rapidly absorbed and distributed, with peak plasma levels being reached within 60-90 minutes. Vorapaxar's effective half-life is three to four days and its terminal elimination half-life is eight days. Vorapaxar sulfate 2.5 mg (equivalent to 2.08 mg of vorapaxar) orally daily without a loading dose was clinically effective for the secondary prevention of ischemic events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD) without a history of stroke. Phase II and III trials of vorapaxar given with aspirin or a thienopyridine or both demonstrated a reduction in the primary endpoint of cardiovascular death, MI, and stroke in patients with a history of MI or coronary artery disease and PAD. Patients with a history of stroke were found to have an increased rate of intracranial hemorrhage (ICH), which led to a boxed warning placed on vorapaxar's labeling to warn of the increased risk for bleeding in patients with a history of stroke.
  
  
  CONCLUSIONS
  Vorapaxar is a novel antiplatelet agent that has demonstrated efficacy in reducing atherosclerotic events in patients with a history of MI or PAD without a history of stroke, transient ischemic attack, or ICH when taken in combination with aspirin and clopidogrel.
authors.affiliation: Sally A. Arif, Pharm.D., BCPS (AQ-Cardiology), is Associate Professor of Pharmacy Practice, Chicago College of Pharmacy, Midwestern University, Downers Grove, IL, and Clinical Pharmacist, Department of Pharmacy, Rush University Medical Center, Chicago, IL. Jennifer D'Souza, Pharm.D., CDE, BC-ADM, is Associate Professor of Pharmacy Practice, Chicago College of Pharmacy, Midwestern University. Monika Gil, Pharm.D., BCPS, is Clinical Pharmacist, Department of Pharmacy, Rush University Medical Center. Suzanna Gim, B.A., Pharm.D., M.P.H., is Associate Professor of Pharmacy Practice, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, and Drug Information Specialist, Brookdale University Hospital and Medical Center, Brooklyn. sarif@midwestern.edu.
authors.forename: Sally A
authors.initials: SA
authors.lastname: Arif
authors.affiliation: Sally A. Arif, Pharm.D., BCPS (AQ-Cardiology), is Associate Professor of Pharmacy Practice, Chicago College of Pharmacy, Midwestern University, Downers Grove, IL, and Clinical Pharmacist, Department of Pharmacy, Rush University Medical Center, Chicago, IL. Jennifer D'Souza, Pharm.D., CDE, BC-ADM, is Associate Professor of Pharmacy Practice, Chicago College of Pharmacy, Midwestern University. Monika Gil, Pharm.D., BCPS, is Clinical Pharmacist, Department of Pharmacy, Rush University Medical Center. Suzanna Gim, B.A., Pharm.D., M.P.H., is Associate Professor of Pharmacy Practice, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, and Drug Information Specialist, Brookdale University Hospital and Medical Center, Brooklyn.
authors.forename: Jennifer
authors.initials: J
authors.lastname: D'Souza
authors.affiliation: Sally A. Arif, Pharm.D., BCPS (AQ-Cardiology), is Associate Professor of Pharmacy Practice, Chicago College of Pharmacy, Midwestern University, Downers Grove, IL, and Clinical Pharmacist, Department of Pharmacy, Rush University Medical Center, Chicago, IL. Jennifer D'Souza, Pharm.D., CDE, BC-ADM, is Associate Professor of Pharmacy Practice, Chicago College of Pharmacy, Midwestern University. Monika Gil, Pharm.D., BCPS, is Clinical Pharmacist, Department of Pharmacy, Rush University Medical Center. Suzanna Gim, B.A., Pharm.D., M.P.H., is Associate Professor of Pharmacy Practice, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, and Drug Information Specialist, Brookdale University Hospital and Medical Center, Brooklyn.
authors.forename: Monika
authors.initials: M
authors.lastname: Gil
authors.affiliation: Sally A. Arif, Pharm.D., BCPS (AQ-Cardiology), is Associate Professor of Pharmacy Practice, Chicago College of Pharmacy, Midwestern University, Downers Grove, IL, and Clinical Pharmacist, Department of Pharmacy, Rush University Medical Center, Chicago, IL. Jennifer D'Souza, Pharm.D., CDE, BC-ADM, is Associate Professor of Pharmacy Practice, Chicago College of Pharmacy, Midwestern University. Monika Gil, Pharm.D., BCPS, is Clinical Pharmacist, Department of Pharmacy, Rush University Medical Center. Suzanna Gim, B.A., Pharm.D., M.P.H., is Associate Professor of Pharmacy Practice, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY, and Drug Information Specialist, Brookdale University Hospital and Medical Center, Brooklyn.
authors.forename: Suzanna
authors.initials: S
authors.lastname: Gim
mesh_terms: D001241:Aspirin / Q000008:administration & dosage; D000077144:Clopidogrel; D004347:Drug Interactions; D004359:Drug Therapy, Combination; D006207:Half-Life; D006470:Hemorrhage / Q000139:chemically induced; D006801:Humans; D007783:Lactones / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D009203:Myocardial Infarction / Q000453:epidemiology; D017202:Myocardial Ischemia / Q000517:prevention & control; D058729:Peripheral Arterial Disease / Q000453:epidemiology; D010975:Platelet Aggregation Inhibitors / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D011725:Pyridines / Q000009:adverse effects / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use*; D016032:Randomized Controlled Trials as Topic; D055502:Secondary Prevention; D020521:Stroke / Q000517:prevention & control; D013927:Thrombosis / Q000517:prevention & control*; D013988:Ticlopidine / Q000008:administration & dosage / Q000031:analogs & derivatives
chemical_list: D007783:Lactones; D010975:Platelet Aggregation Inhibitors; D011725:Pyridines; D000077144:Clopidogrel; D013988:Ticlopidine; D001241:Aspirin; C530299:vorapaxar