Thienopirydines in stroke treatment
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Keywords

Cytochrome P-450
ticlopidine
secondary prevention

Abstract

The thienopiryidines are antiplatelet agents with effectiveness similar or superior to ASA (Acetil salicylic acid), metabolized by the cytochrome P-450 system in the liver which can determines the resistance to their effect and questioned interactions with some proton pump inhibitors. Ticlopidine was the first molecule of this family and it was used until the end of nineties. Clopidogrel was the second molecule, 100 times potent. In the coronary disease the use of clopidogrel plus ASA in the acute event and after angioplasty is approved. In the cerebrovascular disease the dual antiplatelet therapy has not shown benefit and an increase in the bleeding complications rate has been reported. Actually there are several trials of dual therapy in the context of acute ischemic stroke and one trial in the secondary stroke prevention. The mechanism of action is over the P2Y(12) receptor which is the main receptor for ADP mediated platelet aggregation, they block it in an indirect way through tiolactones with an irreversible covalently binding. This receptor is actually the investigation core for new platelet aggregation modulating drugs development in indirect (Thienopirydines) and direct blockade as ticagrelor (oral uses) and cangrelor (I.V. use).


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