Vorapaxar, Zontivity, Protease-Activated Receptor-1 Antagonist, PAR-1 Antagonist

  • Mechanism
  1. Protease-Activated Receptor-1 Antagonist (PAR-1 Antagonist)
  2. Inhibits Platelet aggregation for 4 weeks after dose
  • Indications
  1. Thrombotic event prevention in patients with significant cardiovascular history
  2. Not intended to be used alone
  3. Limited to patients with very high Cardiovascular Risk
  4. Adjunctive therapy to low dose Aspirin or Clopidogrel (Plavix)
    1. Myocardial Infarction
    2. Peripheral Arterial Disease
  • Contraindications
  1. Prior Cerebrovascular Accident (CVA) or Transient Ischemic Attack (TIA)
    1. Vorapaxar is associated with an increase risk of Hemorrhagic CVA in patients with prior cerebrovascular events
  2. Combination with other antiplatelet agents (other than Aspirin or Clopidogrel)
    1. Has not been studied with Prasugrel (Effient) or Ticagrelor (Brilinta)
  3. Avoid with strong CYP3A4 inhibitors or strong CYP3A4 inducers
  • Dosing
  1. Take 2.08 mg orally daily
  • Drug Interactions
  1. Strong CYP3A4 inhibitors (e.g. Clarithromycin, Ritonavir, Ketoconazole)
  2. Strong CYP3A4 inducers (e.g. Carbamazepine, Phenytoin, Rifampin)
  • Precautions
  1. Long Half-Life
  2. No antidote in the case of severe bleeding
  • Safety
  1. Pregnancy Category B
  2. Contraindicated in Lactation