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When ticlopidine and clopidogrel were first brought to the market, ticlodipine in 1978 and clopidogrel in 1998, the mechanism of action of these two major antithrombotic drugs was not fully understood. What had been shown was that they were potent inhibitors of ADP-induced platelet aggregation, but the P2Y 12 receptor
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 ).
P2Y 12 is a chemoreceptor for adenosine diphosphate (ADP) [5] [6] that belongs to the G i class of a group of G protein-coupled (GPCR) purinergic receptors. [7] This P2Y receptor family has several receptor subtypes with different pharmacological selectivity, which overlaps in some cases, for various adenosine and uridine nucleotides.
[34] [35] ADP-induced platelet aggregation and activation are hence hindered. Examples include clopidogrel, prasugrel and ticagrelor. Clopidogrel has a common drug interaction with CYP2C19 inhibitors, particularly omeprazole and esomeprazole which are indicated for treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
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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Prasugrel is a member of the thienopyridine class of ADP receptor inhibitors, like ticlopidine (trade name Ticlid) and clopidogrel (trade name Plavix). These agents reduce the aggregation ("clumping") of platelets by irreversibly binding to P2Y 12 receptors. Prasugrel inhibits platelet aggregation more rapidly, more consistently, and to a ...