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| __NOTOC__
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| {{Ticagrelor}}
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| {{CMG}}; {{AE}} {{JH}}
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| '''''For patient information about Ticagrelor, click [[Ticagrelor (patient information)|here]].'''''
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| {{SB}} BRILINTA<sup>®</sup>
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| ==Overview==
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| '''Ticagrelor''' (previously known as AZD6140) is a member of a new generation of [[P2Y12|P2Y<sub>12</sub>]] 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.<ref>{{cite journal|title=Ticagrelor versus Clopidogrel in Patients with Acute Coronary Syndromes|last=Wallentin|first=Lars|date=August 30, 2009 |journal=NEJM|url=http://content.nejm.org/cgi/content/full/NEJMoa0904327}}</ref>
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| ==Category==
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| Antiplatelet Agents; ADP receptor inhibitors
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| ==FDA Package Insert==
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| ====BRILINTA (ticagrelor) tablet ====
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| ''' [[Ticagrelor indications and usage|Indications and Usage]]'''
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| '''| [[Ticagrelor dosage and administration|Dosage and Administration]]'''
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| '''| [[Ticagrelor dosage forms and strengths|Dosage Forms and Strengths]]'''
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| '''| [[Ticagrelor contraindications|Contraindications]]'''
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| '''| [[Ticagrelor warnings and precautions|Warnings and Precautions]]'''
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| '''| [[Ticagrelor adverse reactions|Adverse Reactions]]'''
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| '''| [[Ticagrelor drug interactions|Drug Interactions]]'''
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| '''| [[Ticagrelor use in specific populations|Use in Specific Populations]]'''
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| '''| [[Ticagrelor overdosage|Overdosage]]'''
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| '''| [[Ticagrelor description|Description]]'''
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| '''| [[Ticagrelor clinical pharmacology|Clinical Pharmacology]]'''
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| '''| [[Ticagrelor nonclinical toxicology|Nonclinical Toxicology]]'''
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| '''| [[Ticagrelor clinical studies|Clinical Studies]]'''
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| '''| [[Ticagrelor how supplied storage and handling|How Supplied/Storage and Handling]]'''
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| '''| [[Ticagrelor patient counseling information|Patient Counseling Information]]'''
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| '''| [[Ticagrelor labels and packages|Labels and Packages]]'''
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| <font color="#F8F8FF">
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| {| style="border: 3px solid #696969;" align="center"
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| | style="background: #000000; border: 0px; padding: 0 5px; width: 800px;" |
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| <center>
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| '''WARNING: (A) BLEEDING RISK, and (B) ASPIRIN DOSE AND BRILINTA EFFECTIVENESS'''
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| </center>
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| <center>
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| ''See full prescribing information for complete boxed warning.''
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| </center>
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| <b>
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| (A) BLEEDING RISK
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| * BRILINTA, like other antiplatelet agents, can cause significant, sometimes fatal bleeding.
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| * Do not use BRILINTA in patients with active pathological bleeding or a history of intracranial hemorrhage.
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| * Do not start BRILINTA in patients planned to undergo urgent coronary artery bypass graft surgery (CABG). When possible, discontinue BRILINTA at least 5 days prior to any surgery.
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| * Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, percutaneous coronary intervention (PCI), CABG, or other surgery.
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| * If possible, manage bleeding without discontinuing BRILINTA. Stopping BRILINTA increases the risk of subsequent cardiovascular events.
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| (B) ASPIRIN DOSE AND BRILINTA EFFECTIVENESS
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| * Maintenance doses of aspirin above 100 mg reduce the effectiveness of BRILINTA and should be avoided.
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| </b>
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| |}
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| </font>
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| ==Taking Alcohol with Ticagrelor==
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| Alcohol-Ticagrelor interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
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| ==Mechanism of Action==
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| 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|P2Y<sub>12</sub>]] 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|P2Y<sub>12</sub>]] 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|P2Y<sub>12</sub>]] 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.<ref>{{cite journal
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| | author = H. Spreitzer
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| | date = [[February 4]], [[2008]]
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| | title = Neue Wirkstoffe - AZD6140
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| | journal = Österreichische Apothekerzeitung
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| | issue = 3/2008
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| | pages = 135
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| | language = German
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| }}</ref><ref>{{cite journal
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| | author = Owen, RT, Serradell, N, Bolos, J
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| | title = AZD6140
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| | journal = Drugs of the Future
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| | year = 2007
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| | volume = 32
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| | issue = 10
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| | pages = 845–853
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| | doi = 10.1358/dof.2007.032.10.1133832
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| }}</ref>
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| ==References==
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| {{Reflist|2}}
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| {{Antithrombotics}}
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| [[Category:ADP receptor inhibitors]]
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| [[Category:Cardiovascular Drugs]]
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| [[Category:Drugs]] | | [[Category:Drugs]] |