CLOPIDOGREL PILLS 75MG

Packaging

28 pcs.

28 pieces

Mechanism of action

Clopidogrel is a specific and active inhibitor of platelet aggregation; has a coronarodilating effect. Selectively reduces the binding of ADP to platelet receptors and the activation of GPI Ib / IIIa receptors under the action of ADP. easing platelet aggregation. Reduces platelet aggregation caused by other agonists, preventing their activation by released ADP, does not affect the activity of phosphodiesterase (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. The 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 thrombotic complications:

• after myocardial infarction (from several days to 35 days), ischemic stroke (from 6 days to 6 months) or for diagnosed peripheral arterial disease;
• in acute coronary syndrome without ST segment elevation (unstable angina or myocardial infarction without abnormal Q wave), including patients undergoing percutaneous coronary artery bypass surgery, in combination with Acetylsalicylic acid;
• in acute coronary syndrome with ST-segment elevation (acute myocardial infarction) in combination with acetylsalicylic acid, in patients receiving medication with the possible use of thrombolytic therapy.

Contraindications

• severe liver failure;
• acute bleeding (for example, with peptic ulcer or intracranial hemorrhage);
• pregnancy;
• breastfeeding period;
• age up to 18 years (safety and efficacy not established);
• Hypersensitivity to the components of the drug. With caution, the drug should be prescribed for diseases of the liver and kidneys (including those with moderate hepatic and / or renal failure), injuries, and preoperative conditions.

Pregnancy and Breastfeeding

Adequate and strictly controlled clinical studies of the safety of Clopidogrel during pregnancy have not been conducted. Application is possible only in cases of extreme necessity.

It is not known whether clopidogrel is excreted in human breast milk. If necessary, use during lactation should decide on the termination of breastfeeding.

In experimental animal studies with the use of clopidogrel in doses of 300-500 mg / kg / day, no teratogenic effect and a negative effect on fertility and fetal development were detected. It is established that clopidogrel and its metabolites are excreted in breast milk.

Cautions

During the period of treatment, it is necessary to monitor the indicators of the hemostatic system (activated partial thromboplastin time (APTT), platelet count, tests of the functional activity of platelets); regularly examine the functional activity of the liver.
Clopidogrel should be used with caution in patients at risk of severe bleeding from trauma, surgery; patients receiving acetylsalicylic acid, non-steroidal anti-inflammatory drugs (including COX-2 inhibitors), Heparin or glycoprotein IIb / IIIa inhibitors. Careful monitoring of patients is necessary to identify any signs of bleeding, including hidden, especially during the first weeks of use of the drug and / or after invasive procedures on the heart or surgical operations. For planned surgical interventions, treatment with clopidogrel should be stopped 7 days before the operation.
Patients should be warned that stopping the bleeding will take longer than usual, so they should inform the doctor about each case of bleeding.
Rare cases of thrombotic thrombocytopenic purpura (TTP) have been observed after taking clopidogrel. This condition was characterized by thrombocytopenia and microangiopathic hemolytic anemia in combination with neurological symptoms, impaired renal function or fever. The development of TTP is a threat to life and requires the adoption of urgent measures, including plasmapheresis. Due to insufficient data, clopidogrel should not be administered in the acute period of ischemic stroke (in the first 7 days). The drug should be prescribed with caution in patients with impaired renal function.
Clopidogrel should be prescribed with caution in patients with moderate hepatic impairment, who may develop hemorrhagic diathesis.
Patients with congenital intolerance to galactose, glucose-galactase malabsorption syndrome and lactase deficiency should not take clopidogrel.

Composition

1 pill contains clopidogrel hydrosulfate 97.875 mg, down to clopidogrel - 75 mg;
Excipients:pregelatinized starch. anhydrous lactose (anhydrous milk sugar), macrogol (polyethylene glycol 6000). Magnesium stearate. microcrystalline cellulose (PH 112), hydrogenated castor oil;film coating composition:Selecoot AQ – 01673 (hypromellose (hydroxypropylmethylcellulose), macrogol (polyethylene glycol 400), macrogol (polyethylene glycol 6000), titanium dioxide, aluminum varnish based on the dye Ponso 4 R).

Dosage and administration

Clopidogrel is taken orally, regardless of the meal.
For the prevention of ischemic disorders in patients after myocardial infarction, ischemic stroke and diagnosed peripheral arterial disease - 75 mg 1 time / day. Treatment should begin in the period from several days to 35 days after myocardial infarction and from 7 days to 6 months after ischemic stroke.
In acute coronary syndrome without ST segment elevation (unstable stenocardia or myocardial infarction without Q wave) treatment should begin with the appointment of a single loading dose of 300 mg, and then continue to use the drug at a dose of 75 mg 1 time / day (with the simultaneous appointment of acetylsalicylic acid at a dose of 75-325 mg / day). Since the use of acetylsalicylic acid in high doses is associated with a high risk of bleeding, the recommended dose should not exceed 100 mg. The course of treatment is up to 1 year.
In acute myocardial infarction with ST segment elevation the drug is prescribed at a dose of 75 mg 1 time / day using the initial loading dose in combination with acetylsalicylic acid with or without thrombolytics. For patients over the age of 75, treatment with clopidogrel should be carried out without the use of a loading dose.Combination therapy starts as soon as possible after the onset of symptoms and continues for at least 4 weeks.

Adverse reactions

Frequency: very often - more than 1/10, often - more than 1/100 and less than 1/10, rarely - more than 1/1000 and less than 1/100, rarely - more than 1/10000 and less than 1/1000, very rarely - less 1/10000, including isolated cases.
On the part of the blood-forming organs: infrequently - thrombocytopenia, leukopenia, eosinophilia; seldom - neutropenia, incl. pronounced; very rarely - thrombotic thrombocytopenic purpura, anemia incl. aplastic, pancytopenia, agranulocytosis, severe thrombocytopenia, granulocytopenia.
Allergic reactions: very rarely - Anaphylactic reactions, serum sickness.
From the nervous system: infrequently - headache, dizziness, paresthesias, intracranial bleeding, incl. fatal; very rarely - confusion, hallucinations, taste disturbance.
From the senses: infrequently - bleeding in the conjunctiva, eyes, retina; rarely - vertigo.
From the side of the cardiovascular system: often - hematoma; very rarely - severe bleeding, bleeding from the surgical wound, vasculitis, decrease in blood pressure.
On the part of the respiratory system: very often - nosebleeds; very rarely - bronchospasm, interstitial pneumonitis, pulmonary hemorrhage, hemoptysis.
On the part of the digestive system: often - diarrhea, abdominal pain, dyspepsia, bleeding from the gastrointestinal tract; infrequently - gastric and duodenal ulcers, gastritis, vomiting, nausea, constipation, flatulence; rarely retroperitoneal bleeding; very rarely - pancreatitis, colitis, incl.ulcerative or lymphocytic, stomatitis, acute liver failure, hepatitis, impaired liver function tests, bleeding from the gastrointestinal tract with a fatal outcome.
On the part of the skin: often - subcutaneous hemorrhage; infrequently - skin rash, itching, purpura; very rarely - angioedema, urticaria, erythematous rash, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, eczema, lichen planus.
On the part of the musculoskeletal system: very rarely - hemarthrosis, arthritis, arthralgia, myalgia.
From the genitourinary system: infrequently - hematuria; very rarely - glomerulonephritis, hypercreatininemia.
Local reactions: often - bleeding at the injection site.
Laboratory indicators: infrequently - lengthening of bleeding time.
Other: very rarely - fever.

The combined use of clopidogrel with Warfarin is not recommended, since such a combination can increase the intensity of bleeding.
The administration of glycoprotein IIb / IIIa inhibitors together with clopidogrel increases the risk of bleeding.
The use of nonsteroidal anti-inflammatory drugs with clopidogrel increases the risk of bleeding.
The concomitant use of clopidogrel with CYP2C19 inhibitors (for example, omeprazole) is not recommended.
No clinically significant pharmacodynamic interactions were observed with the use of clopidogrel together with Atenolol, Nifedipine, phenobarbital, cimetidine, estrogen, Digoxin, theophylline, tolbutamide, antacid agents.

Symptoms: prolongation of bleeding time and subsequent complications.
Treatment: if bleeding occurs, appropriate therapy should be performed. If rapid correction of prolonged bleeding time is necessary, platelet transfusion is recommended. There is no specific antidote.

Store at a temperature not higher than 25 ° С. Keep out of reach of children.