Lopirel pills 75mg №14

Dosage form

Pills

Composition

Clopidogrel hydrosulfate

Excipients: lactose, microcrystalline cellulose, crospovidone (type A), glyceryl dibehenate, talc, Opadry II 85 G34669 pink (polyvinyl alcohol, talc, titanium dioxide (E171), macrogol 3350, lecithin (E322), iron dye red oxide (E172).

Packing

14 pieces

Mechanism of action

LOPIREL - antiplatelet drug, a specific and active inhibitor of platelet aggregation. It has a coronarodilating effect. Selectively reduces the binding of ADP to platelet receptors and the activation of GPI Ib / IIIa receptors by the action of ADP, thereby reducing platelet aggregation. Reduces platelet aggregation caused by other agonists, preventing their activation by released ADP, does not affect the activity of PDE. Irreversibly binds to ADP receptors of platelets, which remain immune to stimulation of ADP throughout the life cycle (about 7 days).

Inhibition of platelet aggregation is observed 2 hours after administration (40% inhibition) of the initial dose of 400 mg. The maximum effect (60% suppression of aggregation) develops after 4-7 days of continuous administration at a dose of 50-100 mg / day.Antiplatelet effect persists throughout the life of platelets (7-10 days).

In the presence of atherosclerotic lesion of the vessel prevents the development of atherothrombosis, regardless of the localization of the vascular process (cerebrovascular, cardiovascular or peripheral lesions).

Indications and usage

Prevention of atherothrombosis:

- in patients undergoing myocardial infarction, ischemic stroke, or diagnosed with peripheral artery disease;

- in patients with acute coronary syndrome without ST segment elevation (unstable angina or myocardial infarction without Q wave on an ECG), in combination with Acetylsalicylic acid, including patients who underwent stenting for percutaneous coronary intervention;

- in patients with acute coronary syndrome with ST-segment elevation (acute myocardial infarction) in combination with acetylsalicylic acid, receiving drug treatment with possible use of thrombolytic therapy.

Contraindications

- severe liver failure;

- hemorrhagic syndrome;

- acute bleeding (including intracranial hemorrhage) and diseases predisposing to its development (gastric ulcer and duodenal ulcer in the acute phase, ulcerative colitis, tuberculosis, lung tumors, hyperfibrinolysis);

- pregnancy;

- lactation period (breastfeeding);

- neonatal period;

- age up to 18 years (efficiency and safety have not been established);

- intolerance to galactose, lactase deficiency or malabsorption of glucose-galactose (because the preparation contains lactose);

- hypersensitivity to the drug.

Dosage and administration

The drug is taken orally, regardless of the meal.

Patients after myocardial infarction, ischemic stroke, or with peripheral artery disease, the drug is prescribed 75 mg 1 time per day. Treatment should begin from the first days to 35 days in patients after myocardial infarction and from 7 days to 6 months in patients after ischemic stroke.

In acute coronary syndrome without ST-segment elevation (unstable stenocardia, myocardial infarction without Q wave on the ECG), including patients who underwent stenting for percutaneous coronary intervention, treatment with Lopirel should be started with a single dose of 300 mg and then continued a dose of 75 mg 1 time / day (in combination with acetylsalicylic acid). Since the use of acetylsalicylic acid in high doses is associated with an increased risk of bleeding, the dose of acetylsalicylic acid recommended for this indication does not exceed 100 mg. The maximum beneficial effect is observed at 3 months of treatment. The course of treatment is up to 1 year.

Patients with acute coronary syndrome with ST segment elevation (acute myocardial infarction) in combination with acetylsalicylic acid,receiving medication with the possible use of thrombolytic therapy, Lopirel is prescribed once in a dose of 75 mg 1 time / day with an initial single dose of a loading dose in combination with acetylsalicylic acid and thrombolytics (or without thrombolytics). Combination therapy is started as soon as possible after the onset of symptoms and continues for at least 4 weeks. In patients older than 75 years, treatment with Lopirel should begin without taking a loading dose.

With the simultaneous use of Clopidogrel with Warfarin may increase the intensity of bleeding (this combination is not recommended).

Acetylsalicylic acid does not alter the inhibitory effect of clopidogrel on ADP-induced platelet aggregation, but clopidogrel potentiates the effect of acetylsalicylic acid on platelet aggregation induced by collagen. However, the simultaneous use of acetylsalicylic acid in a dose of 500 mg 2 times / day did not cause any significant increase in bleeding time, prolonged due to the use of clopidogrel. The safety of long-term simultaneous use of acetylsalicylic acid and clopidogrel has not been established, however, clopidogrel and acetylsalicylic acid can be used simultaneously for up to one year.

According to a clinical study conducted on healthy volunteers, the simultaneous use of clopidogrel and Heparin does not require dose adjustment of the latter and does not affect the antiplatelet effect of clopidogrel,however, the safety of such a combination has not yet been established (caution is required with this combination).

The safety of simultaneous use of clopidogrel with thrombolytics is not currently established (with this combination, caution is required).

In a clinical study conducted with the participation of healthy volunteers, with the combined use of clopidogrel and Naproxen, an increase in the number of hidden Gastrointestinal bleeding was observed. However, due to the lack of clinical studies of the interaction of the drug with other NSAIDs, it is currently not established whether there is an increased risk of developing gastrointestinal bleeding when using other drugs of this group (caution is required for a combination of clopidogrel and NSAIDs).

Clinically significant pharmacodynamic interaction with the use of clopidogrel together with Atenolol and / or Nifedipine was not detected.

The pharmacodynamic activity of Lopirela remains almost unchanged when used simultaneously with phenobarbital, cimetidine, or estrogen.

The pharmacokinetic properties of Digoxin or theophylline do not change when combined with clopidogrel.

Antacid agents do not alter the absorption of clopidogrel.

The data obtained during studies with microsomes of human liver, suggests that clopidogrel can inhibit the activity of the CYP2C9 isoenzyme.As a result, it is possible to increase plasma concentrations of certain drugs, such as phenytoin and tolbutamide, because they are metabolized by CYP2C9. The results of the study CAPRIE indicate the safety of phenytoin and tolbutamide together with clopidogrel.

Storage conditions

At a temperature not higher than 30 ° C.

3 years