Which of the following is a thrombin Receptor Antagonist:
Correct Answer: Vorapaxar
Description: Vorapaxar is an orally active thrombin receptor (Protease Activated Receptor-1) Antagonists. Protease Activated Receptor-1 (PAR-1) is the major thrombin receptor on platelets. Vorapaxar is a potent and reversible thrombin receptor antagonist, which selectively antagonizes the PAR-1 to prevent thrombin-mediated platelet activation. Selective PAR-1 blockade by Vorapaxar results in inhibition of thrombin-induced platelet aggregation. Vorapaxar has been found to be effective for secondary prevention in patients with prior MI or peripheral aerial disease. Vorapaxar is only approved for the reduction of thrombotic events in patients with a history of prior MI or with PAD. Use of Vorapaxar is associated with a relatively higher risk of intracranial haemorrhage. Because of an increased risk of intracranial haemorrhage, it is a contraindicated in patients with a history of stroke or TIA> Terutroban is a selective antagonist of the thromboxane receptor. It blocks thromboxane induced platelet aggregation and vasoconstriction. Terutroban testing was stopped in Phase III of the double-blind PERFORM trial where Terutroban failed to meet the primary efficacy endpoint of non-inferiority in comparision with Aspirin. Terutroban is an orally active, selective, and reversible TP antagonist with sho half-life (6-10 h),which has shown to produce dose dependent inhibition of platelet aggregation in patients with peripheral aerial disease (PAD) Ref: Current diagnosis and treatment in cardiology; essential cardiology
Category:
Pharmacology
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