For patient information about Ticagrelor, click here.
Synonyms / Brand Names: BRILINTA®
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.
ADP receptor inhibitors;Triazolopyrimidines;Organofluorides;Alcohols;AstraZeneca
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
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.
- Wallentin, Lars (August 30, 2009). "Ticagrelor versus Clopidogrel in Patients with Acute Coronary Syndromes". NEJM.
- H. Spreitzer (February 4, 2008). "Neue Wirkstoffe - AZD6140" (in German). Österreichische Apothekerzeitung (3/2008): 135.
- Owen, RT, Serradell, N, Bolos, J (2007). "AZD6140". Drugs of the Future 32 (10): 845–853. doi:10.1358/dof.2007.032.10.1133832.
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