A review. The research of Husted et al. (2006) entitled "Pharmacodynamics, pharmacokinetics, and safety of the oral reversible P2Y12 antagonist AZD6140 with aspirin in patients with atherosclerosis: a double-blind comparison to clopidogrel with aspirin" is reviewed with commentary and refs. The G-coupled P2Y12 receptor plays an important role in ADP-induced platelet aggregation and mediates the potentiation of platelet secretion induced by strong agonists and the stabilization of thrombin-induced platelet aggregates. In their study, Husted et al. investigated the effects of the oral administration of AZD6140, the first oral reversible P2Y12 antagonist, to patients with atherosclerosis. The results showed that AZD6140 at doses above 50 mg BID more effectively inhibited platelet aggregation and with less variability than clopidogrel. The inhibition of platelet aggregation was very rapid compared with that of clopidogrel. The prolongation of the bleeding times was greater in AZD6140-treated patients compared with clopidogrel-treated patients, although no obvious dose-response relationship was obsd. The incidence of bleeding events tended to be higher in patients treated with the three higher doses of AZD6140, compared with that obsd. in patients treated with 50 mg BID or clopidogrel. An unexpected, relatively high frequency of dyspnea was also obsd., and this side effect appeared to increase with increasing doses of AZD6140
P2Y12 receptor antagonists : a rapidly expanding group of antiplatelet agents / M. Cattaneo. - In: EUROPEAN HEART JOURNAL. - ISSN 0195-668X. - 27:9(2006), pp. 1010-1012. [10.1093/eurheartj/ehi851]
P2Y12 receptor antagonists : a rapidly expanding group of antiplatelet agents
M. CattaneoPrimo
2006
Abstract
A review. The research of Husted et al. (2006) entitled "Pharmacodynamics, pharmacokinetics, and safety of the oral reversible P2Y12 antagonist AZD6140 with aspirin in patients with atherosclerosis: a double-blind comparison to clopidogrel with aspirin" is reviewed with commentary and refs. The G-coupled P2Y12 receptor plays an important role in ADP-induced platelet aggregation and mediates the potentiation of platelet secretion induced by strong agonists and the stabilization of thrombin-induced platelet aggregates. In their study, Husted et al. investigated the effects of the oral administration of AZD6140, the first oral reversible P2Y12 antagonist, to patients with atherosclerosis. The results showed that AZD6140 at doses above 50 mg BID more effectively inhibited platelet aggregation and with less variability than clopidogrel. The inhibition of platelet aggregation was very rapid compared with that of clopidogrel. The prolongation of the bleeding times was greater in AZD6140-treated patients compared with clopidogrel-treated patients, although no obvious dose-response relationship was obsd. The incidence of bleeding events tended to be higher in patients treated with the three higher doses of AZD6140, compared with that obsd. in patients treated with 50 mg BID or clopidogrel. An unexpected, relatively high frequency of dyspnea was also obsd., and this side effect appeared to increase with increasing doses of AZD6140Pubblicazioni consigliate
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