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Pathway Description
Ticagrelor Action Pathway
Homo sapiens
Drug Action Pathway
Ticagrelor also known via brand names Brilinta or Brilique, is a platelet inhibitor used to prevent infarction, stroke or cardiovascular death. Once administered orally it travels to the bloodstream and acts on platelets' P2Y receptors which inhibits the formation of thromboses. An activated P2Y receptor couples with guanine nucleotide-binding protein subunit i2 that inhibits adenylyl cyclase. By inhibiting adenylyl cyclase, it stops the formation of cAMP, leading to a stop of calcium efflux causing platelet aggregation and activation. Grapefruit products should be avoided as it inhibits the CYP3A4 metabolism of ticagrelor and cause an increase in the drug which may lead to an overdose. Herbs and supplements with anticoagulant and antiplatelet activity should be avoided such as garlic, ginger, bilberry, danshen, piracetam and ginkgo biloba. St. John's Wort induces the CYP3A4 metabolism of the drug and will reduce its efficacy and concentration.
References
Ticagrelor Pathway References
Husted S, Emanuelsson H, Heptinstall S, Sandset PM, Wickens M, Peters G: Pharmacodynamics, pharmacokinetics, and safety of the oral reversible P2Y12 antagonist AZD6140 with aspirin in patients with atherosclerosis: a double-blind comparison to clopidogrel with aspirin. Eur Heart J. 2006 May;27(9):1038-47. doi: 10.1093/eurheartj/ehi754. Epub 2006 Feb 13.
Pubmed: 16476694
Storey RF, Husted S, Harrington RA, Heptinstall S, Wilcox RG, Peters G, Wickens M, Emanuelsson H, Gurbel P, Grande P, Cannon CP: Inhibition of platelet aggregation by AZD6140, a reversible oral P2Y12 receptor antagonist, compared with clopidogrel in patients with acute coronary syndromes. J Am Coll Cardiol. 2007 Nov 6;50(19):1852-6. doi: 10.1016/j.jacc.2007.07.058. Epub 2007 Oct 23.
Pubmed: 17980251
Tantry US, Bliden KP, Gurbel PA: AZD6140. Expert Opin Investig Drugs. 2007 Feb;16(2):225-9. doi: 10.1517/13543784.16.2.225.
Pubmed: 17243942
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