Plagril, 75 mg 30 pcs.

Pharmacodynamics

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 receptor of platelets and the 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 remainder of their lives (approximately 7-10 days), and recovery of normal platelet function occurs at a rate consistent with the rate of platelet renewal.

Platelet aggregation caused by agonists other than ADP is also inhibited by blocking enhanced platelet activation by the released ADP.

Since the formation of the active metabolite occurs via isoenzymes of the P450 system, some of which may be polymorphic or may be inhibited by other drugs, adequate inhibition of platelet aggregation is not possible in all patients.

When clopidogrel is taken daily at a dose of 75 mg, significant suppression of ADP-induced platelet aggregation is noted from the first day of administration, which gradually increases over 3-7 days and then reaches a constant level (when the equilibrium state is reached). In the equilibrium state, platelet aggregation is suppressed by an average of 40-60 %. After stopping clopidogrel administration platelet aggregation and bleeding time gradually return to the initial level, on average within 5 days

Clopidogrel is able to prevent atherothrombosis in any localization of atherosclerotic vascular lesions, in particular in lesions of the cerebral, coronary or peripheral arteries.

The ACTIVE-A clinical trial showed that patients with atrial fibrillation who had at least one risk factor for vascular complications but were unable to take indirect anticoagulants, clopidogrel combined with acetylsalicylic acid (compared with taking acetylsalicylic acid alone) reduced the incidence of stroke, myocardial infarction, systemic thromboembolism outside the central nervous system (CNS), or vascular death combined, more by reducing the risk of stroke.

The efficacy of clopidogrel in combination with acetylsalicylic acid was detected early and persisted for up to 5 years. The reduction in the risk of major vascular complications, in the group of patients who took clopidogrel in combination with acetylsalicylic acid, was mainly due to a greater reduction in the incidence of strokes.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

The concomitant use of drugs with clopidogrel that are associated with a risk of bleeding should be used with caution (with warfarin, with IIb/IIIa-receptor blockers, with acetylsalicylic acid, with heparin, with thrombolytics, in NSAIDs, with SSRIs).

Special Instructions

Contraindications

Side effects

Overdose

Clopidogrel overdose may lead to increased bleeding time with subsequent complications in the form of bleeding development. If bleeding occurs, appropriate treatment measures are required.

The antidote for clopidogrel has not been established. If rapid correction of prolonged bleeding time is necessary, platelet transfusion is recommended.

Pregnancy use

Pregnancy

Animal studies have shown no direct or indirect adverse effects on pregnancy, fetal development, labor and postnatal development. Because it is not always possible to predict response in humans based on animal studies, and because there are no controlled clinical trial data on clopidogrel administration in pregnant women, clopidogrel administration during pregnancy is not recommended as a precautionary measure unless the physician determines its use is imperative.

Breastfeeding

In studies in rats, clopidogrel and/or its metabolites have been shown to be excreted into breast milk. Whether clopidogrel passes into human breast milk is unknown. Since many drugs may be excreted into the breast milk and have adverse effects on the infant, the attending physician, based on the importance of taking Plagril® for the mother, should recommend her either to stop taking the drug, or to take the drug, but to stop breastfeeding.

Similarities