vorapaxar (Zontivity)
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Introduction
FDA-approval May 2014[3][4][5]
Indications
- prevention of atherothrombotic events (myocardial infarction, stroke, TIA) in high-risk patients[5]
- peripheral artery disease[7]
* FDA-approved for use in combination with low-dose aspirin or clopidogrel[6]
* do not use alone[7]
Contraindications
- history of intracranial hemorrhage, stroke or TIA
- secondary prevention of myocardial infarction in conjunction with dual anti-platelet therapy[1]
Dosage
* each tablet contains 2.5 mg of vorapaxar sulfate, providing 2.08 mg of vorapaxar[7]
Pharmacokinetics
Adverse effects
- hemorrhage
- intracranial hemorrhage
- moderate or severe bleeding 4.2% vs 2.5% for placebo[4]
- risk of hemorrage mitigates its benefit in preventing atheroembolic events[2]
Drug interactions
- interaction with prasugrel (Effient) not studied
- interaction with ticagrelor (Brilinta) not studied[7]
- avoid using with strong CYP3A4 inhibitors
- clarithromycin ...
- avoid using with strong CYP3A4 inducers
- phenytoin ...
- drug interaction(s) of oral anticoagulants with selective serotonin reuptake inhibitor (SSRI)
- drug interaction(s) of anti-platelet agents with SSRIs
- drug interaction(s) of antiplatelet agents with proton pump inhibitors
- drug interaction(s) of warfarin with antiplatelet agents
- drug interaction(s) of aspirin, P2Y12 inhibitors & anticoagulants
Mechanism of action
- protease-activated receptor-1 antagonist[7]
- inhibits thrombin-induced platelet activation
Notes
- cost: $267 for 30 day supply (2014)
More general terms
References
- ↑ 1.0 1.1 Tricoci P et al for the TRACER Investigators. Thrombin-receptor antagonist vorapaxar in acute coronary syndromes. N Engl J Med 2011 Nov 13; <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/22077816 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1109719
- ↑ 2.0 2.1 Morrow DA et al. for the TRA 2P-TIMI 50 Steering Committee and Investigators. Vorapaxar in the secondary prevention of atherothrombotic events. N Engl J Med 2012 Mar 24 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/22443427 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1200933
- ↑ 3.0 3.1 N Engl J Med Journal Watch. Jan 21, 2014 http://www.jwatch.org (subscription required)
Clarke T FDA advisory panel backs Merck's blood clot-preventing drug. Reuters. Jan 15, 2014 http://www.reuters.com/article/2014/01/15/us-merck-vorapaxar-idUSBREA0E1KV20140115 - ↑ 4.0 4.1 4.2 4.3 Wood S Medcape. May 8, 2014 FDA Approves PAR-1 Antagonist Zontivity (Vorapaxar) to Reduce MI, Stroke Risk http://www.medscape.com/viewarticle/824886
- ↑ 5.0 5.1 5.2 FDA News Release: May 8, 2014 FDA approves Zontivity to reduce the risk of heart attacks and stroke in high-risk patients. http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm396585.htm
- ↑ 6.0 6.1 6.2 Prescriber's Letter 21(8): 2014 No Detail Document. (subscription needed) http://www.prescribersletter.com
- ↑ 7.0 7.1 7.2 7.3 7.4 7.5 7.6 7.7 7.8 Prescriber's Letter 21(9): 2014 Comparison of Oral Antiplatelets Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=300909&pb=PRL (subscription needed) http://www.prescribersletter.com