For platelet inhibition it has to undergo oxidative ring-opening by cytochrome P450 enzymes
Ticlopidine and clopidogrel belong to the same chemical family of thienopyridine adenosine diphosphate (ADP)-receptor antagonists
The use of ticlopidine is currently discouraged because of
It is a prodrug that is metabolised to an active form, which blocks the ADP receptor that is involved in GPIIb/IIIa receptor
Their mode of action has not been defined, but it
Ticlopidine, the first FDA-approved thienopyridine, was shown to be effective in reducing coronary events in high r
Ticlopidine, 231,232 a potent thienopyridine antiplatelet agent, is a P2Y 12 ADP receptor antagonist that is discussed in detail in Chapter 54
Purinergic P2Y Receptor Antagonists
Platelet P2Y12 receptor inhibition plays a pivotal role in preventing thrombotic vascular events in patients with ACS and in patients undergoing percutaneous coronary intervention (PCI)
Thienopyridines are a class of selective, irreversible [1] ADP receptor / P2Y12 inhibitors used for their anti- platelet activity
Ticlopidine was the first thienopyridine introduced into clinical practice, but its potentially serious haematological
6
Mechanism of Action: Irreversible antagonism of the P2Y12 ADP receptor
Receptors, Purinergic P2Y12
The results of large clinical trials have demonstrated an overall benefit of clopidogrel over aspirin in the prevention of vascular ischemic events Platelet adenosine diphosphate (ADP) receptor antagonists (ticlopidine, clopidogrel, prasugrel, and ticagrelor) are a major advance in the treatment of atherothrombotic diseases, especially acute coronary syndromes (ACS)
This group of drugs includes: clopidogrel, ticlopidine, ticagrelor, prasugrel, and cangrelor
Thienopyridines, namely ticlopidine and clopidogrel, inhibit platelet function by working as noncompetitive antagonists to the P2Y 12 G-protein-coupled receptor found on the surface of platelets; this receptor typically binds ADP and activates platelet aggregation
However, ticlopidine is accompanied by occasional life-threatening adverse hematological events
The use of ticlopidine is currently discouraged because of the long delay of inhibitory action and most importantly, its risk of life-threatening side effects, including neutropenia, aplastic anemia, thrombotic thrombocytopenic purpura Antiplatelet agents can be divided into three major types: glycoprotein platelet inhibitors (eg, abciximab, eptifibatide, tirofiban) platelet aggregation inhibitors (eg, aspirin, cangrelor, cilostazol, clopidogrel, dipyridamole, prasugrel, ticlopidine, ticagrelor) protease-activated receptor-1 antagonists (eg, vorapaxar)
9 Despite a generally strong interest in the P2Y12 receptor, relatively little is known regarding the P2Y4 subtype which demonstrates to mediate chloride secretion, regulate amyloid precursor protein (APP) production Ticlopidine