ticagrelor (Brilinta)
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Introduction
Brintellix (vortioxetine) & Brilinta (ticagrelor) name confusion.[8]
Indications
- secondary prevention in patients with cardiovascular disease
- prevention of cardiovascular events in patients admitted to the hospital
- acute coronary syndrome (FDA-approved 2011)
- myocardial infarction[7]
- percutaneous coronary intervention[6]
* ticagrelor 90 mg BID no better than aspirin 100 mg QD for preventing cardiovascular event or cardiovascular death after transient ischemic attack or ischemic stroke[10][11]
Dosage
Pharmacokinetics
- more rapid onset of action than clopidogrel
- does not require 1st pass metabolism
- no known genetic polymorphisms affecting metabolism[9]
Monitor
- digoxin levels when starting or stopping ticagrelor[3]
Adverse effects
- increased risk of bleeding, fatal hemorrhage
- dyspnea
- drug adverse effects of antiplatelet agents
- drug adverse effects of antithrombotic agent(s)
- drug adverse effects of P2Y12 receptor inhibitor(s)
Drug interactions
- aspirin doses > 100 mg QD decrease effectiveness of ticagrelor[2]
- avoid using strong CYP3A3 inhibitors or inducers[3]
- 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
- reversible, direct-acting inhibitor of ADP receptor P2Y12
- more rapid onset and more pronounced platelet inhibition than clopidogrel
Clinical trials
- see PLATO study
Comparative biology
- antibacterial activity against drug-resistant gram-positive bacteria in vitro & in a mouse study[13]
- superior to vancomycin against MRSA & S epidermidis.
Notes
- stop 5 days prior to surgery
More general terms
Additional terms
References
- ↑ Wallentin L Ticagrelor versus Clopidogrel in Patients with Acute Coronary Syndromes www.nejm.org August 30, 2009 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/19717846 <Internet> http://content.nejm.org/cgi/content/full/NEJMoa0904327
Schomig A Ticagrelor - Is There Need for a New Player in the Antiplatelet-Therapy Field? www.nejm.org August 30, 2009 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/19717845 <Internet> http://content.nejm.org/cgi/content/full/NEJMe0906549 - ↑ 2.0 2.1 FDA NEWS RELEASE: July 20, 2011 FDA approves blood-thinning drug Brilinta to treat acute coronary syndromes http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm263964.htm
- ↑ 3.0 3.1 3.2 Prescriber's Letter 18(8): 2011 (subscription needed) http://www.prescribersletter.com
- ↑ Prescriber's Letter 19(5): 2012 COMMENTARY: Antiplatelets After Acute Coronary Syndrome or Coronary Stent CHART: Comparison of Oral Antithrombotics Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=280526&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Jneid H et al 2012 ACCF/AHA Focused Update of the Guideline for the Management of Patients with Unstable Angina/Non-ST-Elevation Myocardial Infarction (Updating the 2007 Guideline and Replacing the 2011 Focused Update). A report of the American College of Cardiology Foundation/American Heart Association Task Force of Practice Guidelines. http://circ.ahajournals.org/content/early/2012/07/16/CIR.0b013e318256f1e0.full.pdf+html
- ↑ 6.0 6.1 Deprecated Reference
- ↑ 7.0 7.1 AstraZeneca Global. Jan 14, 2015 PEGASUS-TIMI 54 study of BRILINTA<TM> meets primary endpoint in both 60mg and 90mg doses. http://www.astrazeneca.com/Media/Press-releases/Article/20150114--PEGASUS-TIMI-54-study--BRILINTA-meets-primary-endpoint-in-60mg-and-90mg-doses
- ↑ 8.0 8.1 FDA MedWatch. July 30, 2015 Brintellix (vortioxetine) and Brilinta (ticagrelor): Drug Safety Communication - Name Confusion. https://mail.google.com/mail/u/0/?tab=wm#inbox/14edfa25fc57b461
- ↑ 9.0 9.1 Medical Knowledge Self Assessment Program (MKSAP) 17, 18. American College of Physicians, Philadelphia 2015, 2018.
- ↑ 10.0 10.1 AstraZeneca News Release. March 23, 2016 AstraZeneca reports top-line results from the Brilinta SOCRATES trial in stroke. https://www.astrazeneca.com/media-centre/press-releases/2016/astrazeneca-reports-top-line-results-from-the-brilinta-socrates-trial-in-stroke-23032016.html
- ↑ 11.0 11.1 Johnston SC et al Ticagrelor versus Aspirin in Acute Stroke or Transient Ischemic Attack. N Engl J Med. May 10, 2016 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/27160892 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1603060
- ↑ Bonaca MP et al Long-Term Use of Ticagrelor in Patients with Prior Myocardial Infarction. N Engl J Med. March 14, 2015 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/25773268 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1500857
Keaney JF Jr Balancing the Risks and Benefits of Dual Platelet Inhibition. N Engl J Med. March 14, 2015 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/25773507 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMe1502137 - ↑ 13.0 13.1 Lancellotti P, Musumeci L, Jacques N et al Antibacterial Activity of Ticagrelor in Conventional Antiplatelet Dosages Against Antibiotic-Resistant Gram-Positive Bacteria. JAMA Cardiol. Published online May 8, 2019. PMID: https://www.ncbi.nlm.nih.gov/pubmed/31066863 https://jamanetwork.com/journals/jamacardiology/fullarticle/2732487