

Clopidogrel is a prodrug, one of the active metabolites of which is an inhibitor of platelet aggregation. The active metabolite of clopidogrel selectively inhibits the binding of adenosine diphosphate (ADP) to the P2Y12 platelet receptor and subsequent ADP-mediated activation of the GPIIb / IIIa complex, leading to suppression of platelet aggregation. Due to irreversible binding, platelets remain immune to ADP stimulation for the rest of their life (approximately 7-10 days), and the restoration of normal platelet function occurs at a rate corresponding to the rate of platelet renewal. Platelet aggregation induced by agonists other than ADP is also inhibited by blocking the increased platelet activation by released ADP. Since the formation of an active metabolite occurs with the help of isoenzymes of the P450 system, some of which may differ in polymorphism or may be inhibited by other drugs, not all patients may have adequate inhibition of platelet aggregation. With a daily intake of clopidogrel at a dose of 75 mg, from the very first day of administration, there is a significant suppression of ADP-induced platelet aggregation, which gradually increases over 3-7 days and then reaches a constant level (upon reaching an equilibrium state). In an equilibrium state, platelet aggregation is suppressed by an average of 40-60%. After discontinuing clopidogrel, platelet aggregation and bleeding time gradually return to baseline, on average, within 5 days ... Clopidogrel is able to prevent the development of atherothrombosis in any localization of atherosclerotic vascular lesions, in particular, with lesions of the cerebral, coronary or peripheral arteries. The ACTIVE-A clinical trial showed that in patients with atrial fibrillation who had at least one risk factor for vascular complications, but were unable to take indirect anticoagulants, clopidogrel in combination with acetylsalicylic acid (compared with taking only acetylsalicylic acid) reduced the incidence of combined stroke, myocardial infarction, systemic thromboembolism outside the central nervous system (CNS), or vascular death, largely by reducing the risk of stroke. The effectiveness of taking clopidogrel in combination with acetylsalicylic acid was detected early and lasted up to 5 years. The decrease in the risk of major vascular complications in the group of patients taking clopidogrel in combination with acetylsalicylic acid was mainly due to a greater decrease in the incidence of strokes. The risk of developing a stroke of any severity when taking clopidogrel in combination with acetylsalicylic acid decreased, and there was also a tendency to a decrease in the incidence of myocardial infarction in the group treated with clopidogrel in combination with acetylsalicylic acid, but there were no differences in the incidence of non-CNS thromboembolism or vascular death. In addition, taking clopidogrel in combination with acetylsalicylic acid reduced the total number of days of hospitalization for cardiovascular reasons.
No customer reviews for the moment.
Studies and clinical trials of Acetylsalicylic acid, Clopidogrel (Click to expand)