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Information about Vorapaxar

Vorapaxar is an inhibitor of platelet aggregation that is used to decrease the risk of further cardiovascular thrombotic events in patients with a history of myocardial infarction or peripheral vascular disease. 

Liver safety of Vorapaxar

Vorapaxar therapy is associated with a low rate of serum aminotransferase elevations, but has not been linked to instances of clinically apparent acute liver injury.

Mechanism of action of Vorapaxar

Vorapaxar (vor" a pax' ar) is an inhibitor of the protease-activated receptor 1 (PAR-1) that is found on platelets and is activated by thrombin resulting in platelet aggregation and formation of a vascular clot.  The aggregation of platelets also plays an important role in the growth of atheromatous plaques, which can lead to coronary, cerebral and peripheral arterial occlusions.  In large clinical trials, vorapaxar therapy has been shown to decrease the frequency of recurrence of myocardial infarction and cardiovascular events in patients at high risk of complications of atherosclerosis. 

FDA approval information for Vorapaxar

Vorapaxar was approved for use in the United States in 2014 and current indications are for reduction of atherosclerotic events (myocardial infarction, vascular death) in patients with a history of myocardial infarction or peripheral vascular disease.  Vorapaxar is contraindicated in patients with a history of stroke or transient ischemic attacks because of an increased risk of intracerebral bleeding. 

FDA approval information for Vorapaxar

Vorapaxar is available in 2.08 mg tablets under the brand name Zontivity.  The usual dose is one tablet (2.08) mg daily. 

Side effects of Vorapaxar

Side effects are not common, but can include headache, dizziness, fatigue, gastrointestinal upset, nausea, arthralgia and rash.  Uncommon, but potentially severe adverse reactions including bleeding and particularly intracerebral bleeding in patients with a history of stroke.

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