Product Information
Registration Status: ActiveBRILINTA TABLET 90mg is approved to be sold in Singapore with effective from 2012-03-13. It is marketed by ASTRAZENECA SINGAPORE PTE LTD, with the registration number of SIN14120P.
This product contains Ticagrelor 90mg in the form of TABLET, FILM-COATED. It is approved for ORAL use.
This product is manufactured by AstraZeneca AB in SWEDEN, andAstraZeneca Pharmaceutical Co. in CHINA.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
Ticagrelor (trade name Brilinta in the US, Brilique and Possia in the EU) is a platelet aggregation inhibitor produced by AstraZeneca. Unlike clopidogrel, ticagrelor is not a prodrug and does not require metabolic activation. The drug was approved for use in the European Union by the European Commission on December 3, 2010. The drug was approved by the US Food and Drug Administration on July 20, 2011.
Indication
For the prevention of thrombotic events (for example stroke or heart attack) in patients with acute coronary syndrome or myocardial infarction with ST elevation.
Mechanism of Action
Like the thienopyridines prasugrel, clopidogrel and ticlopidine, ticagrelor blocks adenosine diphosphate (ADP) receptors of subtype P2Y12. In contrast to the other antiplatelet drugs, ticagrelor has a binding site different from ADP, making it an allosteric antagonist, and the blockage is reversible. Moreover, the drug does not need hepatic activation, which might work better for patients with genetic variants regarding the enzyme CYP2C19 (although it is not certain whether clopidogrel is significantly influenced by such variants).
Pharmacokinetics
- Absorption
- Absorbed quickly from the gut, the bioavailability being 36%.
- Distribution
- The steady state volume of distribution of ticagrelor is 88 L.
- Metabolism
- The main metabolite, AR-C124910XX, is formed quickly via CYP3A4 by de-hydroxyethylation at position 5 of the cyclopentane ring. The metabolite reaches 30–40% of ticagrelor's plasma concentrations.
- Elimination
Toxicity
Bleeding is the expected pharmacologic effect of overdosing. If bleeding occurs, appropriate supportive measures should be taken. Other effects of overdose may include gastrointestinal effects (nausea, vomiting, diarrhea) or ventricular pauses.
Active Ingredient/Synonyms
(1S,2S,3R,5S)-3-(7-((1R,2S)-2-(3,4-Difluorophenyl)cyclopropylamino)-5-(propylthio)-3H-(1,2,3)triazolo(4,5-D)pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol | Ticagrelor |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.