Contents

Search

ticagrelor (Brilinta)

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: - 180 mg loading dose, then 60-90 mg PO BID - use with aspirin 81 mg PO QD Monitor: - digoxin levels when starting or stopping ticagrelor [3] Pharmacokinetics: - more rapid onset of action than clopidogrel - does not require 1st pass metabolism - no known genetic polymorphisms affecting metabolism [9] Adverse effects: - increased risk of bleeding, fatal hemorrhage - dyspnea Drug interactions: - aspirin doses > 100 mg QD decrease effectiveness of ticagrelor [2] - avoid using strong CYP3A3 inhibitors or inducers [3] 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 Notes: - stop 5 days prior to surgery Comparative biology: - antibacterial activity against drug-resistant gram-positive bacteria in vitro & in a mouse study [13] - superior to vancomycin against MRSA & S epidermidis.

Interactions

drug adverse effects of antiplatelet agents

Related

PLATO study

General

P2Y12-receptor inhibitor

Database Correlations

PUBCHEM correlations

References

  1. Wallentin L Ticagrelor versus Clopidogrel in Patients with Acute Coronary Syndromes www.nejm.org August 30, 2009 PMID: 19717846 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 PMID: 19717845 http://content.nejm.org/cgi/content/full/NEJMe0906549
  2. 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. Prescriber's Letter 18(8): 2011 (subscription needed) http://www.prescribersletter.com
  4. Prescriber's Letter 19(5): 2012 COMMENTARY: Antiplatelets After Acute Coronary Syndrome or Coronary Stent CHART: Comparison of Oral Antithrombotics Detail-Document#: 280526 (subscription needed) http://www.prescribersletter.com
  5. 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. Deprecated Reference
  7. AstraZeneca Global. Jan 14, 2015 PEGASUS-TIMI 54 study of BRILINTA 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. 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. Medical Knowledge Self Assessment Program (MKSAP) 17, 18. American College of Physicians, Philadelphia 2015, 2018.
  10. 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. Johnston SC et al Ticagrelor versus Aspirin in Acute Stroke or Transient Ischemic Attack. N Engl J Med. May 10, 2016 PMID: 27160892 http://www.nejm.org/doi/full/10.1056/NEJMoa1603060
  12. Bonaca MP et al Long-Term Use of Ticagrelor in Patients with Prior Myocardial Infarction. N Engl J Med. March 14, 2015 PMID: 25773268 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 PMID: 25773507 http://www.nejm.org/doi/full/10.1056/NEJMe1502137
  13. 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: 31066863 https://jamanetwork.com/journals/jamacardiology/fullarticle/2732487