Coplavix, 100 mg+75 mg 100 pcs

Coplavix is a prodrug, one of whose metabolites is active and inhibits 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 glycoprotein IIb/IIIa complex, leading to suppression of platelet aggregation.

The irreversible binding ensures that 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 the enhanced platelet activation by the released ADP.

Because 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 equilibrium is reached).

In the equilibrium state platelet aggregation is suppressed by an average of 40-60%. After discontinuation of clopidogrel, platelet aggregation and bleeding time gradually return to baseline within an average of 5 days. When comparing pharmacodynamic properties of clopidogrel in men and women, less inhibition of ADP-induced platelet aggregation is observed in women, but no sex differences in prolongation of bleeding time are found.

. In patients with recent myocardial infarction, stroke, and diagnosed peripheral arterial occlusive disease, taking Coplavix at a dose of 75 mg/day significantly reduces the risk of ischemic complications (combined rate of myocardial infarction, stroke cardiovascular death and is most effective in patients with peripheral arterial occlusive disease, especially when combined with a history of myocardial infarction, and is also more effective in patients younger than 75 years;

. In patients with acute coronary syndrome without ST-segment elevation (unstable angina, myocardial infarction), the use of Coplavix (loading dose – 300 mg, then 75 mg/day) in combination with acetylsalicylic acid (ASA) (75 – 325 mg once daily) and other standard therapies regardless of concomitant therapies (heparin therapy, glycoprotein IIb/Sha blockers, hypolipidemic drugs, beta-adrenoblockers, angiotensin-converting enzyme (ACE) inhibitors) and ASA doses, significantly reduces the overall risk of ischemic complications: acute myocardial infarction, stroke, and cardiovascular death with a 17% reduction in relative risk with conservative treatment; after percutaneous transluminal coronary angioplasty (PTCA) with or without stenting by 29% and after aortocoronary bypass surgery by 10%.

. In patients with acute myocardial infarction (MI) with ST-segment elevation, administration of Coplavix (during the first 12 hours of MI a loading dose of 300 mg, then 75 mg/day) in combination with ASA (loading dose of 150-325 mg, then 75-162 mg once daily) and a fibrinolytic and when indicated, with heparin reduces the combined rate of coronary artery occlusion related to the area of infarction or fatal outcomes or development of recurrent MI detected by angiography at the time of discharge from the hospital; and for patients who did not undergo angiography at discharge, the incidence of death or recurrent MI until day 8 of the MI or until hospital discharge, mainly by reducing the incidence of coronary artery occlusion related to the infarction zone.

In patients with acute MI with ST-segment elevation, ST-segment reduction or left bundle branch block, administration of Coplavix 75 mg/day in combination with ASA 162 mg once daily leads to a reduction in the rate of death from either cause and the cumulative rate of first repeat MI, stroke and fatal outcomes.

Indications

Prevention of atherothrombotic complications (in combination with acetylsalicylic acid) in patients with acute coronary syndrome:

Active ingredient

Composition

1 tablet contains clopidogrel hydrosulfate in form II – 97.875 mg (in terms of clopidogrel 75 mg), acetylsalicylic acid – 100 mg.

Auxiliary substances:

Mannitol 68.925 mg,

Macrogol-6000 34.000 mg,

microcrystalline cellulose -144.764 mg,

low-substituted hyprolose – 19.567 mg,

hydrogenated castor oil – 3,300 mg,

stearic acid – 1,161 mg,

colloidal silica -0,631 mg,

corn starch -11,111 mg

How to take, the dosage

Adults and the elderly

Coplavix should be taken orally, regardless of meals. This tablet containing 300 mg of clopidogrel is intended for use as a loading dose in patients with acute coronary syndrome.

Acute coronary syndrome without ST-segment elevation (unstable angina pectoris, myocardial infarction without Q-wave)

Treatment with clopidogrel should be started with a single loading dose of 300 mg and then continued with a dose of 75 mg once daily (combined with acetylsalicylic acid in doses of 75-325 mg daily). Since the use of higher doses of acetylsalicylic acid is associated with an increased risk of bleeding, the recommended dose of acetylsalicylic acid for this indication should not exceed 100 mg. The maximum favorable effect is observed by the third month of treatment. The course of treatment is up to 1 year.
Acute coronary syndrome with ST-segment elevation (acute myocardial infarction with ST-segment elevation)

. Clopidogrel is administered as a single dose of 75 mg once daily with an initial single loading dose of 300 mg in combination with acetylsalicylic acid and thrombolytics (or without thrombolytics). Combination therapy is started as soon as possible after the onset of symptoms and continued for at least four weeks. In patients older than 75 years, treatment with clopidogrel should be started without its loading dose.

As for the maintenance dose of clopidogrel, which is 75 mg, Plavicke 75 mg tablets are produced for its administration.

Patients with genetically determined decreased CYP2CJ9 isoenzyme function

The weak CYP2C19-metabolizer status is associated with decreased antiaggregant effect of clopidogrel. A high-dose regimen (600 mg -load dose, then 150 mg once daily) in weak metabolizers increases the antiaggregant effect of clopidogrel. However, the optimal dosing regimen for patients with reduced CYP2C19 isoenzyme metabolism in clinical outcome studies has not yet been established.

Interaction

Warfarin: concomitant administration with clopidogrel may increase the intensity of bleeding, so this combination is not recommended.

Glycoprotein IIb/IIIa blockers: Administration of glycoprotein IIb/IIIa blockers together with clopidogrel requires caution in patients with increased risk of bleeding (in trauma and surgical interventions or other pathological conditions) (see “Special indications”).

Acetylsalicylic acid: Acetylsalicylic acid does not alter the effect of clopidogrel inhibiting ADP-induced platelet aggregation, but clopidogrel potentiates the effect of acetylsalicylic acid on collagen-induced platelet aggregation. However, concomitant administration of acetylsalicylic acid at 500 mg twice daily for 1 day with clopidogrel did not significantly increase bleeding time caused by clopidogrel administration. Pharmacodynamic interaction is possible between clopidogrel and acetylsalicylic acid, which leads to an increased risk of bleeding. Therefore, caution should be exercised when using them concomitantly, although in clinical trials patients received combined therapy with clopidogrel and acetylsalicylic acid for up to one year.

Heparin: according to data from a clinical trial conducted with healthy subjects, no change in heparin dose was required when taking clopidogrel and its anticoagulant effect was not altered. Concomitant use of heparin did not alter the antiaggregant effect of clopidogrel. Pharmacodynamic interaction is possible between clopidogrel and heparin, which may increase the risk of bleeding, so the simultaneous use of these drugs requires caution.

Trombolytics: the safety of concomitant use of clopidogrel, fibrin-specific or fibrin-unspecific thrombolytics and heparin has been studied in patients with acute myocardial infarction. The frequency of clinically significant bleeding was similar to that observed when thrombolytics and heparin were used together with acetylsalicylic acid.

Non-steroidal anti-inflammatory drugs (NSAIDs): In a clinical study involving healthy volunteers, the combined use of clopidogrel and naproxen increased latent blood loss through the gastrointestinal tract. However, due to the lack of studies on the interaction of clopidogrel with other NSAIDs, it is currently not known whether there is an increased risk of gastrointestinal bleeding when clopidogrel is taken together with other NSAIDs. Therefore, the prescription of NSAIDs, including COX-2 inhibitors, in combination with clopidogrel should be used with caution.

Other combination therapy

Since clopidogrel is metabolized to form its active metabolite partially by the CYP2C19 isoenzyme, the use of drugs inhibiting this system may lead to decreased concentration of the active metabolite of clopidogrel. The clinical significance of this interaction has not been established. Strong or moderate CYP2C19 inhibitors (e.g., omeprazole) should be avoided concomitantly with clopidogrel. If proton pump inhibitors are to be taken concomitantly with clopidogrel, the proton pump inhibitor with the lowest CYP2C19 isoenzyme inhibitory activity, such as pantoprazole, should be used.

Special Instructions

Contraindications

Hypersensitivity to clopidogrel or any of the excipients of the drug.

Severe hepatic insufficiency.

Acute bleeding, such as bleeding from a peptic ulcer or intracranial hemorrhage.

Rare hereditary lactose intolerance, lactase deficiency and glucose-galactose malabsorption syndrome.

Pregnancy and lactation.

Children under 18 years of age (safety and effectiveness has not been established).

Side effects

Overdose

Pregnancy use

Similarities