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Pathway Description
Ticagrelor Action Pathway
Homo sapiens
Drug Action Pathway
Created: 2023-07-12
Last Updated: 2023-11-27
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
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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
Hollopeter G, Jantzen HM, Vincent D, Li G, England L, Ramakrishnan V, Yang RB, Nurden P, Nurden A, Julius D, Conley PB: Identification of the platelet ADP receptor targeted by antithrombotic drugs. Nature. 2001 Jan 11;409(6817):202-7. doi: 10.1038/35051599.
Pubmed: 11196645
Zhang FL, Luo L, Gustafson E, Lachowicz J, Smith M, Qiao X, Liu YH, Chen G, Pramanik B, Laz TM, Palmer K, Bayne M, Monsma FJ Jr: ADP is the cognate ligand for the orphan G protein-coupled receptor SP1999. J Biol Chem. 2001 Mar 16;276(11):8608-15. doi: 10.1074/jbc.M009718200. Epub 2000 Dec 4.
Pubmed: 11104774
Takasaki J, Kamohara M, Saito T, Matsumoto M, Matsumoto S, Ohishi T, Soga T, Matsushime H, Furuichi K: Molecular cloning of the platelet P2T(AC) ADP receptor: pharmacological comparison with another ADP receptor, the P2Y(1) receptor. Mol Pharmacol. 2001 Sep;60(3):432-9.
Pubmed: 11502873
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Pubmed: 11230166
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Pubmed: 14702039
Hillier LW, Fulton RS, Fulton LA, Graves TA, Pepin KH, Wagner-McPherson C, Layman D, Maas J, Jaeger S, Walker R, Wylie K, Sekhon M, Becker MC, O'Laughlin MD, Schaller ME, Fewell GA, Delehaunty KD, Miner TL, Nash WE, Cordes M, Du H, Sun H, Edwards J, Bradshaw-Cordum H, Ali J, Andrews S, Isak A, Vanbrunt A, Nguyen C, Du F, Lamar B, Courtney L, Kalicki J, Ozersky P, Bielicki L, Scott K, Holmes A, Harkins R, Harris A, Strong CM, Hou S, Tomlinson C, Dauphin-Kohlberg S, Kozlowicz-Reilly A, Leonard S, Rohlfing T, Rock SM, Tin-Wollam AM, Abbott A, Minx P, Maupin R, Strowmatt C, Latreille P, Miller N, Johnson D, Murray J, Woessner JP, Wendl MC, Yang SP, Schultz BR, Wallis JW, Spieth J, Bieri TA, Nelson JO, Berkowicz N, Wohldmann PE, Cook LL, Hickenbotham MT, Eldred J, Williams D, Bedell JA, Mardis ER, Clifton SW, Chissoe SL, Marra MA, Raymond C, Haugen E, Gillett W, Zhou Y, James R, Phelps K, Iadanoto S, Bubb K, Simms E, Levy R, Clendenning J, Kaul R, Kent WJ, Furey TS, Baertsch RA, Brent MR, Keibler E, Flicek P, Bork P, Suyama M, Bailey JA, Portnoy ME, Torrents D, Chinwalla AT, Gish WR, Eddy SR, McPherson JD, Olson MV, Eichler EE, Green ED, Waterston RH, Wilson RK: The DNA sequence of human chromosome 7. Nature. 2003 Jul 10;424(6945):157-64. doi: 10.1038/nature01782.
Pubmed: 12853948
Jaiswal BS, Conti M: Identification and functional analysis of splice variants of the germ cell soluble adenylyl cyclase. J Biol Chem. 2001 Aug 24;276(34):31698-708. doi: 10.1074/jbc.M011698200. Epub 2001 Jun 21.
Pubmed: 11423534
Reed BY, Gitomer WL, Heller HJ, Hsu MC, Lemke M, Padalino P, Pak CY: Identification and characterization of a gene with base substitutions associated with the absorptive hypercalciuria phenotype and low spinal bone density. J Clin Endocrinol Metab. 2002 Apr;87(4):1476-85. doi: 10.1210/jcem.87.4.8300.
Pubmed: 11932268
Litvin TN, Kamenetsky M, Zarifyan A, Buck J, Levin LR: Kinetic properties of "soluble" adenylyl cyclase. Synergism between calcium and bicarbonate. J Biol Chem. 2003 May 2;278(18):15922-6. doi: 10.1074/jbc.M212475200. Epub 2003 Feb 27.
Pubmed: 12609998
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