Ticagrelor

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Jesus Rosario Hernandez, M.D. [2]

For patient information about Ticagrelor, click here.

Synonyms / Brand Names: BRILINTA^®

Overview

Ticagrelor (previously known as AZD6140) is a member of a new generation of P2Y₁₂ inhibitors. Chemically, this is a first-in-class member of the cyclo-pentyl-triazolo-pyrimidine (CPTP) family with a mean terminal half-life of approximately 7 h and a median Tmax of 2.6 h. Ticagrelor’s steady-state volume of distribution (87.5 L) indicates it does not extensively distribute into or bind to tissues.

Category

Antiplatelet Agents; ADP receptor inhibitors

FDA Package Insert

BRILINTA (ticagrelor) tablet

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

WARNING: (A) BLEEDING RISK, and (B) ASPIRIN DOSE AND BRILINTA EFFECTIVENESS See full prescribing information for complete boxed warning. (A) BLEEDING RISK BRILINTA, like other antiplatelet agents, can cause significant, sometimes fatal bleeding. Do not use BRILINTA in patients with active pathological bleeding or a history of intracranial hemorrhage. Do not start BRILINTA in patients planned to undergo urgent coronary artery bypass graft surgery (CABG). When possible, discontinue BRILINTA at least 5 days prior to any surgery. Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, percutaneous coronary intervention (PCI), CABG, or other surgery. If possible, manage bleeding without discontinuing BRILINTA. Stopping BRILINTA increases the risk of subsequent cardiovascular events. (B) ASPIRIN DOSE AND BRILINTA EFFECTIVENESS Maintenance doses of aspirin above 100 mg reduce the effectiveness of BRILINTA and should be avoided.

Taking Alcohol with Ticagrelor

Alcohol-Ticagrelor interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Mechanism of Action

Like thienopyridines, ticagrelor is only orally available, but in contrast with these pro-drugs, ticagrelor is direct acting, i.e. does not require metabolic activation. In addition, ticagrelor is a reversible P2Y₁₂ inhibitor with more rapid onset and off set of action compared with clopidogrel. Ticagrelor has 2 metabolites. The major ticagrelor metabolite (AR-C124910XX) has a P2Y₁₂ inhibiting activity comparable to the parent compound while a second metabolite (AR-C133913XX) is inactive. Ticagrelor is rapidly and extensively metabolized in the liver by CYP3A4. The P2Y₁₂ receptor is targeted by ticagrelor via a mechanism that is non-competitive with ADP, suggesting the existence of an independent receptor-binding site. Compared with clopidogrel, ticagrelor provides greater and more consistent platelet inhibition.