Egitromb, pills 75mg 28pcs

Composition

1 tablet, film-coated, contains:

Active ingredient:

clopidogrel hydrosulfate 97.86 mg (based on clopidogrel — 75 mg);

excipients:

microcrystalline silicon cellulose (MCC, colloidal anhydrous silicon dioxide);

hyprolose (with a low degree of substitution (L-HPC In 1);

hydrogenated castor oil;

Opadry white Y-I-7000 (hypromellose, titanium dioxide, macrogol 400)

Pharmacological action

Pharmacodynamics

Egitromb is an antiplatelet agent. Specific and active inhibitor of platelet aggregation. Selectively reduces the binding of adenosine diphosphate (ADP) to platelet receptors and the activation of GPI IIb/IIIa receptors by ADP, thus weakening platelet aggregation.

Reduces platelet aggregation caused by other agonists, preventing their activation by released ADP, does not affect the activity of phosphodiesterase (PDE). It irreversibly binds to platelet ADP receptors, which remain immune to ADP stimulation throughout the life cycle (about 7 days). Inhibition of platelet aggregation is observed 2 hours after use (40% inhibition) of the initial dose. The maximum effect (60% suppression of aggregation) develops after 4-7 days of continuous use at a dose of 50-100 mg / day. The antiplatelet effect persists for the entire period of platelet life (7-10 days). If there is an atherosclerotic lesion of the vessel, it prevents the development of atherothrombosis, regardless of the localization of the vascular process (cerebrovascular, cardiovascular or peripheral lesions).

Pharmacokinetics

Clopidogrel is rapidly absorbed after repeated use of 75 mg per day. Bioavailability is high. However, the concentration of the initial substance in plasma is low and after 2 hours does not reach the measurement limit (0.025 mcg/l). Binding to plasma proteins is 98-94%.

It is metabolized in the liver. The main metabolite is an inactive carboxylic acid derivative, whose TCmax after repeated oral doses of 75 mg is reached in 1 hour (Cmax-about 3 mg/l). Excreted by the kidneys-50% and through the intestines with feces – 46% (within 120 hours after use). Half-life of the main metabolite after single and repeated use is 8 hours.

Concentrations of metabolites excreted by the kidneys are 50%. The concentration of the main metabolite in plasma after taking 75 mg / day is lower in patients with severe kidney disease (creatinine clearance 5-15 ml/min) compared with patients with moderate kidney disease (creatinine clearance from 30 to 60 ml/min) and healthy individuals.

Indications

Prevention of thrombotic complications in patients with myocardial infarction, ischemic stroke or peripheral artery occlusion;

For the prevention of thrombotic complications in acute coronary syndrome in combination with acetylsalicylic acid (ASA): with ST segment elevation if thrombolytic therapy is possible; without ST segment elevation (unstable angina, non-Q-wave myocardial infarction), including in patients undergoing stenting.

Use during pregnancy and lactation

Due to the lack of clinical data on the use of the drug in pregnant women, clopidogrel should not be prescribed during pregnancy.

There is no information about the excretion in human breast milk, so the use of the drug during lactation is contraindicated.

Contraindications

• hypersensitivity to the active or any auxiliary component of Egitromb;
• severe liver failure;
• active pathological bleeding (peptic ulcer or intracranial hemorrhage);
• pregnancy and lactation (see the section “Pregnancy and lactation”);
• age up to 18 years (efficacy and safety have not been proven).

With caution: moderate hepatic insufficiency, chronic renal failure( CRF), pathological conditions that increase the risk of bleeding (including trauma, surgery), simultaneous use of ASA, NSAIDs (including COX-2 inhibitors), heparin and glycoprotein IIb/IIIa receptor inhibitors

Side effects

From the central nervous system: infrequent: headache, dizziness and paresthesia; rare: systemic dizziness; very rare: confusion, hallucinations, taste disorders.

From the gastrointestinal tract: frequent: gastrointestinal bleeding, diarrhea, abdominal pain, dyspepsia; infrequent: hemorrhagic stroke, stomach ulcer, duodenal ulcer, gastritis, nausea, vomiting, constipation, bloating; very rare: pancreatitis, colitis (including ulcerative or lymphocytic colitis), stomatitis, acute liver failure, hepatitis.

From the cardiovascular and hematopoietic system: frequent: hematoma; infrequent: increased bleeding time and reduced platelet count (thrombocytopenia), leukopenia, neutropenia and eosinophilia; very rare: vasculitis, hypotension, thrombotic thrombocytopenic purpura (TTP) (1/200 000 patients taking the drug) (see section “Special instructions”), severe thrombocytopenia (platelet count < 30 x 109/L), agranulocytosis, granulocytopenia, aplastic anemia/ pancytopenia, anemia.

Skin disorders: infrequent: allergic reactions (skin rash), pruritus; very rare: angioedema, bullous dermatitis (erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), erythematous rash, urticaria, eczema and lichen planus.

Respiratory system disorders: very rare: bronchospasm, interstitial pneumonitis. Other: very rare: arthralgia, arthritis, myalgia, anaphylactoid reactions, serum sickness, fever, abnormal liver function tests, increased blood creatinine, glomerulonephritis.

Interaction

Increases the antiplatelet effect of acetylsalicylic acid, heparin, thrombolytics, indirect anticoagulants, nonsteroidal anti-inflammatory drugs (NSAIDs), increases the risk of gastrointestinal bleeding, so the simultaneous use of these drugs requires caution.

Clopidogrel should be used with caution in patients who may be at risk of increased bleeding from trauma or surgery if taking glycoprotein IIb/IIIa inhibitors at the same time.

Concomitant use of clopidogrel and warfarin is not recommended, as it may increase bleeding (see also section “Special instructions”). There were no clinically significant pharmacodynamic interactions in cases of concomitant use of clopidogrel with atenolol, nifedipine or a combination of atenolol and nifedipine. In addition, the pharmacodynamic activity of clopidogrel did not significantly change with the simultaneous use of phenobarbital, cimetidine or estrogens. The pharmacokinetics of digoxin or theophylline were not affected by concomitant use of clopidogrel. Antacids do not affect the absorption of clopidogrel. A study of human liver microsomes has shown that a carboxylic acid metabolite of clopidogrel can inhibit the activity of cytochrome P450 2C9. This can increase plasma levels of drugs such as phenytoin, tolbutamide, and NSAIDs that are metabolized by cytochrome P450 2C9. Phenytoin and tolbutamide can be safely co-administered with clopidogrel.

How to take, course of use and dosage

Adults and elderly patients should take clopidogrel orally 75 mg once a day, regardless of food intake.

Treatment should begin within a few days to 35 days in patients after a myocardial infarction and from 7 days to 6 months in patients after an ischemic stroke. In acute non-ST-segment elevation coronary syndrome (unstable angina or non-Q-wave myocardial infarction), clopidogrel should be started with a single shock dose of 300 mg, and then continued with 75 mg once a day in combination with acetylsalicylic acid (ASA 75-325 mg per day).

Overdose

An overdose of clopidogrel can prolong the bleeding time and lead to bleeding-related complications. If bleeding is detected, appropriate treatment should be prescribed.

No antidotes to the pharmacological activity of clopidogrel were found. If it is necessary to quickly reduce the extended bleeding time, platelet transfusion can eliminate the effects of clopidogrel.

Special instructions

During treatment, it is necessary to monitor the parameters of the hemostatic system (APTT, platelet count, tests of platelet functional activity); regularly examine the functional activity of the liver. Clopidogrel should be used with caution in patients at risk of increased bleeding from trauma, surgery, in patients with injuries prone to bleeding (especially gastrointestinal and intraocular), as well as in patients receiving ASA, nonsteroidal anti-inflammatory drugs (including COX-2 inhibitors), heparin or glycoprotein IIb/IIIa inhibitors. Patients should be carefully monitored for any signs of bleeding, including latent bleeding, especially during the first weeks of use of the drug and/or after invasive heart procedures or surgical operations. Concomitant use of clopidogrel and warfarin is not recommended, as it may increase bleeding.

In the case of surgical interventions, if the antiplatelet effect is undesirable, the course of treatment should be stopped 7 days before the operation.

Patients should be warned that, since it takes longer to stop the bleeding that occurs during the use of clopidogrel (with or without ASA), they should inform the doctor about each case of unusual bleeding.Patients should also inform the doctor about taking the drug if they are going to undergo surgery and before taking any new drug.

After taking clopidogrel, thrombotic thrombocytopenic purpura (TTP) was detected very rarely, sometimes after short-term use. This condition is characterized by thrombocytopenia and microangiopathic hemolytic anemia in combination with neurological signs, impaired renal function, or fever. TTP is a potentially fatal condition that requires immediate treatment, including plasmapheresis. Due to the lack of data, clopidogrel should not be recommended for acute (less than 7 days) ischemic strokes. Experience with the use of clopidogrel in patients with impaired renal function is limited, so these patients should be prescribed clopidogrel with caution. Patients with severe hepatic impairment should be aware of the risk of hemorrhagic diathesis, experience with the drug in patients with moderate hepatic impairment is limited, so these patients should be prescribed clopidogrel with caution. Ability to drive vehicles Clopidogrel does not affect or slightly affects the ability to drive vehicles and work with mechanisms.

Form of production

Film-coated tablets

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Clopidogrel

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Prevention of heart attacks and strokes, Prevention of thrombosis