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Clopidogrel, sold under the brand name Plavix among others, is an antiplatelet medication used to reduce the risk of heart disease and stroke in those at high risk. [10] It is also used together with aspirin in heart attacks and following the placement of a coronary artery stent (dual antiplatelet therapy). [10] It is taken by mouth. [10]
Overall mortality rates were similar for each drug. [4] Clopidogrel, unlike prasugrel, was issued a black box warning from the FDA on 12 March 2010, as the estimated 2–14% of the US population who have low levels of the CYP2C19 liver enzyme needed to activate clopidogrel may not get the full effect. Tests are available to predict if a patient ...
Antiplatelet drugs effect may be affected by patient's medications, current medical conditions, food and supplements taken. Antiplatelet drugs effect may be increased or decreased. An increase in antiplatelet effect would increase the risk of bleeding and could cause prolonged or excessive bleeding.
Metabolism of ticlopidine, clopidogrel and prasugrel to an active metabolite. Clopidogrel is a prodrug that is metabolized by two pathways. In one of the pathway most of the dose of clopidogrel (85%) is hydrolyzed by esterases to an inactive carboxylic acid derivate and rapidly cleared via glucoridination followed by renal excretion.
An image of clopidogrel tablet package (Plavix) Caution. Metabolism of P2Y12 inhibitors requires CYP450 enzymes → potential drug interactions; Contraindications. Prasugrel Stroke; Older than 75 years old; Lighter than 60 kg; Statins: Atorvastatin; Simvastatin; Rosuvastatin; Pravastatin; Inhibit HMG-CoA reductase → reduce cholesterol synthesis
A network meta-analysis of 37 studies involving 88,402 STEMI patients and 5,077 major adverse cardiac events (MACE) patients found that use of prasugrel was associated with lower mortality and MACE than other drugs in this class (clopidogrel and ticagrelor).
Glycoprotein IIb/IIIa inhibitors are frequently used during percutaneous coronary intervention (angioplasty with or without intracoronary stent placement).. They work by preventing platelet aggregation and thrombus formation.
Ticagrelor (Brilinta) is often listed with thienopyridine inhibitors and has similar indications for use but is not a thienopyridine. It is a cyclo-pentyltriazolo-pyrimidine that is distinct from the mechanism of the thienopyridines in that it reversibly (rather than irreversibly) inhibits the P2Y 12 receptor.
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