Ticagrelor: Difference between revisions
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'''| [[Ticagrelor patient counseling information|Patient Counseling Information]]''' | '''| [[Ticagrelor patient counseling information|Patient Counseling Information]]''' | ||
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==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== | ==Mechanism of Action== | ||
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Revision as of 22:24, 11 March 2014
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.[1]
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
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.[2][3]
References
- ↑ Wallentin, Lars (August 30, 2009). "Ticagrelor versus Clopidogrel in Patients with Acute Coronary Syndromes". NEJM.
- ↑ H. Spreitzer (February 4, 2008). "Neue Wirkstoffe - AZD6140". Österreichische Apothekerzeitung (in German) (3/2008): 135. Check date values in:
|date=(help) - ↑ Owen, RT, Serradell, N, Bolos, J (2007). "AZD6140". Drugs of the Future. 32 (10): 845–853. doi:10.1358/dof.2007.032.10.1133832.