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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]
Often a combination of aspirin plus an ADP/P2Y inhibitor [7] (such as clopidogrel, prasugrel, ticagrelor, or another) is used to obtain greater effectiveness than with either agent alone. This is known as "dual antiplatelet therapy" (or DAPT ).
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.
The drugs clopidogrel (Plavix), prasugrel (Efient, Effient), ticagrelor (Brilinta), and cangrelor (Kengreal) bind to this receptor and are marketed as antiplatelet agents. [ 5 ] For acute coronary syndrome
Aside from aspirin, three antiplatelet agents taken by mouth have been approved for use in acute coronary syndromes, clopidogrel, ticagrelor and prasugrel; all reduce platelet aggregation by inhibiting the P2Y 12 receptor, a type of adenosine phosphate receptor, on the surface of platelets. Not all three of them are equally indicated in all ...
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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Unlike clopidogrel (Plavix), which is a prodrug, cangrelor is an active drug not requiring metabolic conversion. Poor interim results led to the abandonment of the two CHAMPION clinical trials in mid-2009. [6] The BRIDGE study, for short term use prior to surgery, continues. [7]
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