Egitromb pills coated 75mg N28
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Active ingredients
Clopidogrel
Release form
Pills
Composition
Clopidogrel hydrogensulphate 97.86 mg, which corresponds to a content of clopidogrel 75 mg Excipients: cellulose silicic microcrystalline - 198.2 mg (microcrystalline cellulose - 194,236 mg Colloidal anhydrous silica - 3.964 mg) giproloza (low-substituted (L-HPC B1)) - 12 mg, hydrogenated castor oil - 12 mg. The composition of the shell: opadry white Y-I-7000 - 10 mg (hypromellose - 6.25 mg, titanium dioxide - 3.125 mg, macrogol 400 - 0.625 mg).
Pharmacological effect
Antiplatelet drug. Specific and active inhibitor of platelet aggregation. Selectively reduces the binding of adenosine diphosphate (ADP) to platelet receptors and the activation of GPI Ib / IIIa receptors by the action of 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). 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. 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).
Pharmacokinetics
Clopidogrel is rapidly absorbed from the gastrointestinal tract after repeated administration at 75 mg / day. Bioavailability is high. However, the concentration of clopidogrel in plasma is low and after 2 h does not reach the limit of measurement (0.025 μg / l). Distribution Binding to plasma proteins - 98-94%. Metabolism Metabolized in the liver. The main metabolite is an inactive carboxylic acid derivative, whose Tmax after repeated ingestion in a dose of 75 mg is reached after 1 hour (Cmax - about 3 mg / l). Withdrawal Withdrawn by the kidneys - 50% and through the intestine with feces - 46% (within 120 hours after administration). T1 / 2 of the main metabolite after a single dose and repeated administration - 8 hours. Concentrations of metabolites released by the kidneys - 50%.Pharmacokinetics in special clinical situations The concentration of the main metabolite in plasma after taking the drug at a dose of 75 mg / day is lower in patients with severe renal insufficiency (CC 5–15 ml / min) compared with patients with moderate renal insufficiency (CC from 30 to 60 ml / min) and healthy individuals.
Indications
- Prevention of atherothrombotic complications in adult patients with myocardial infarction (with prescription from several days to 35 days), ischemic stroke (with prescription from 7 days to 6 months) or occlusive peripheral artery disease; - prevention of atherothrombotic complications in adult patients with acute coronary syndrome with ST-segment elevation with the possibility of carrying out thrombolytic therapy (in combination with acetylsalicylic acid); - prevention of atherothrombotic complications in adult patients with acute coronary syndrome without ST-segment elevation (unstable angina, myocardial infarction without Q wave), including in patients undergoing stenting (in combination with acetylsalicylic acid); - prevention of atherothrombotic and thromboembolic complications, including stroke, in atrial fibrillation in adult patients who have at least one risk factor for the development of vascular complications that indirect anticoagulants cannot take and have a low risk of bleeding (in combination with acetylsalicylic acid).
Contraindications
- Hepatic failure severe; - active bleeding (peptic ulcer or intracranial hemorrhage); - pregnancy; - lactation period (breastfeeding); - age up to 18 years (effectiveness and safety are not proven); - hypersensitivity to the active substance or any auxiliary component of the drug. The drug should be used with caution in moderate liver failure, chronic renal failure, in pathological conditions that increase the risk of bleeding (including trauma, surgery), simultaneous administration of acetylsalicylic acid, NSAIDs (including inhibitors of COX-2), warfarin, heparin and inhibitors of glycoprotein IIb / IIIa, low activity of the CYP2C19 isoenzyme (in these patients, when using clopidogrel in recommended doses, less active metabolite of clopidogrel is produced and its antiagr is less pronounced Exact actionIn this connection, when using clopidogrel in recommended doses for acute coronary syndrome or percutaneous coronary intervention, a higher incidence of cardiovascular complications is possible than in patients with normal activity of an isoenzyme CYP2C19).
Use during pregnancy and lactation
Clinical data on the use of the drug Egitromb during pregnancy are not available, so do not prescribe clopidogrel during pregnancy. Information on the allocation of clopidogrel with breast milk is not available, therefore, the use of the drug during lactation is contraindicated.
Dosage and administration
The drug is taken orally, regardless of the meal. For adults and elderly patients, Egitromb is prescribed 75 mg 1 time / day. Treatment should begin in terms from several 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), Egitromb should be started with a single loading dose of 300 mg, and then continue to receive 75 mg once a day in combination with acetylsalicylic acid (75 - 325 mg / day). Since the use of acetylsalicylic acid in higher doses is associated with an increased risk of bleeding, it is recommended to prescribe it in doses not higher than 100 mg. Data from clinical trials indicate the possibility of using Egitromb for up to 12 months, and the maximum effect of therapy is noted by 3 months of use. In acute myocardial infarction with ST segment elevation, Egithrombus should be taken in a dose of 75 mg 1 time / day. Treatment should begin with a loading dose and be combined with the intake of acetylsalicylic acid and thrombolytic agents or without thrombolytic agents. The effectiveness of therapy for more than 4 weeks has not been studied. When atrial fibrillation Egitromb should be taken 1 time / day in a dose of 75 mg. In combination with the drug Egitromb should begin and then continue taking acetylsalicylic acid (75-100 mg / day). Skipping the next dose If less than 12 hours have passed after skipping the next dose, you should immediately take the missed dose of the drug, the next dose should be taken at the usual time.If it has been more than 12 hours after skipping the next dose, you need to take the next dose at the usual time (you should not take a double dose). Special patient groups Patients with genetically determined reduced activity of the isoenzyme CYP2C19 Low activity of the CYP2C19 isoenzyme is associated with a decrease in the antiplatelet effect of clopidogrel. The use of the drug in higher doses (600 mg - loading dose, then 150 mg - 1 time / day) in patients with low activity of the isoenzyme CYP2C19 increases the antiplatelet effect of clopidogrel. However, at present, clinical studies that take into account clinical outcomes have not established the optimal dosage regimen for clopidogrel for such patients. Elderly patients do not require dose adjustment. There is no experience of using the drug in children. Experience with Egitromba in patients with impaired renal function is limited. Experience with the use of the drug in patients with liver diseases of moderate severity (in which manifestations of hemorrhagic diathesis may occur) is limited.
Side effects
Bleeding is the most common reaction, most often it occurs during the first month of taking the drug. Cases of severe bleeding have been reported in patients taking clopidogrel simultaneously with acetylsalicylic acid or clopidogrel with acetylsalicylic acid and heparin. Determination of the frequency of adverse reactions: often (> 1/100, less than 1/10); infrequently (> 1/1000, less than 1/100); rarely (> 1/10 000, less than 1/1000); very rarely (less than 1/10 000). Within each frequency class, unwanted effects are presented in order of decreasing severity. On the part of the blood coagulation system: often - hematoma. On the part of the hemopoietic system: infrequently - an increase in bleeding time and a decrease in the number of platelets, leukopenia, neutropenia, eosinophilia; very rarely - thrombotic thrombocytopenic purpura (TTP) (1/200 000 patients taking the drug), severe thrombocytopenia (platelet count ≤30 × 109 / l), agranulocytosis, granulocytopenia, aplastic anemia / pancytopenia, anemia. From the side of the central nervous system and peripheral nervous system: infrequently - headache, dizziness, paresthesia; rarely, systemic vertigo; very rarely - confusion, hallucinations, disorders of taste.On the part of the digestive system: often - gastrointestinal bleeding, diarrhea, abdominal pain, dyspepsia; infrequently - hemorrhagic stroke, stomach ulcer, duodenal ulcer, gastritis, nausea, vomiting, constipation, intestinal distention; very rarely - pancreatitis, colitis (including ulcerative or lymphocytic colitis), stomatitis, acute liver failure, hepatitis, impaired liver function tests. Since the cardiovascular system: very rarely - vasculitis, arterial hypotension. On the part of the skin: infrequently - itching; very rarely - bullous dermatitis (erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), erythematous rash, eczema, lichen planus. Allergic reactions: rarely - skin rash; very rarely - urticaria, angioedema, serum sickness, anaphylactoid reactions. On the part of the respiratory system: very rarely - bronchospasm, interstitial pneumonitis. On the part of the musculoskeletal system: very rarely - arthralgia, arthritis, myalgia. From the urinary system: very rarely - an increase in the content of serum creatinine, glomerulonephritis. Other: very rarely - fever.
Overdose
Symptoms: prolongation of bleeding time is possible, which can lead to bleeding complications. Treatment: if you need to quickly reduce the lengthened bleeding time, platelet transfusions can eliminate the effects of clopidogrel. No antidotes of the pharmacological activity of clopidogrel were detected.
Interaction with other drugs
Enhances the antiplatelet effect of acetylsalicylic acid, heparin, thrombolithics, indirect anticoagulants, NSAIDs (including COX-2 inhibitors), increases the risk of bleeding from the gastrointestinal tract, therefore the simultaneous use of these drugs requires caution. With simultaneous use of clopidogrel with glycoprotein IIb / IIIa inhibitors, caution should be exercised, since Patients have an increased risk of increased bleeding due to injury or surgery. The simultaneous use of clopidogrel and warfarin is not recommended, because this may increase bleeding. No clinically significant pharmacodynamic interaction was found in cases of simultaneous use of clopidogrel with atenolol, nifedipine, or a combination of atenolol with nifedipine. In addition, the pharmacodynamic activity of clopidogrel did not change significantly with simultaneous use of phenobarbital, cimetidine or estrogen.The pharmacokinetics of digoxin or theophylline did not change with the simultaneous administration of clopidogrel. Antacid drugs do not affect clopidogrel absorption. A study of human liver microsomes has shown that a metabolite of clopidogrel relating to carboxylic acids can inhibit the activity of the CYP2C9 isoenzyme. This may increase plasma concentrations of drugs such as phenytoin, tolbutamide, and NSAIDs that are metabolized with the participation of the CYP2C9 isoenzyme. The use of phenytoin and tolbutamide together with clopidogrel is safe. Since Clopidogrel is metabolized before the formation of its active metabolite using the CYP2C19 system, the use of drugs that inhibit this system may lead to a decrease in the concentration of the active metabolite of clopidogrel. The simultaneous use of strong or moderate inhibitors of the isoenzyme CYP2C19 (for example, omeprazole) with clopidogrel should be avoided. If proton pump inhibitors should be used simultaneously with clopidogrel, a drug should be prescribed with the least inhibition of a CYP2C19 isoenzyme, such as pantoprazole.
special instructions
The drug should be used with caution in patients with an increased risk of bleeding in case of injury, surgical intervention, in patients with lesions prone to bleeding (especially gastrointestinal and intraocular), as well as in patients receiving acetylsalicylic acid, NSAIDs (in t. including inhibitors of COX-2), heparin or glycoprotein IIb / IIIa inhibitors. Patients should be carefully monitored to detect any signs of bleeding, incl. latent, especially during the first weeks of use of the drug and / or after invasive procedures on the heart or surgical operations. The simultaneous use of clopidogrel and warfarin is not recommended, because may increase bleeding. During the period of treatment, it is necessary to monitor indicators of the hemostatic system (APTT, platelet count, tests of functional platelet activity); regularly examine the functional activity of the liver. In the case of surgical interventions, if the antiplatelet effect is undesirable, the treatment should be stopped 7 days before the operation. Patients should be warned that since stopping the clopidogrel resulting from the use of the drug (with or without acetylsalicylic acid) requires more time to bleed, they should inform the doctor about any unusual bleeding.Patients should also inform the doctor about taking the drug if they are to undergo surgery and before taking any new drug. After administration of clopidogrel, thrombotic thrombocytopenic purpura 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. Thrombotic thrombocytopenic purpura is a potentially fatal condition that requires immediate treatment, including using plasmapheresis. Due to the lack of data, clopidogrel cannot be recommended for acute (less than 7 days) ischemic strokes. The experience with clopidogrel in patients with impaired renal function is limited, therefore, this category of patients with clopidogrel should be prescribed with caution. For severe violations of liver function, the risk of hemorrhagic diathesis should be considered. Experience with the use of the drug in patients with moderate liver dysfunction is limited; therefore, this category of patients should be prescribed clopidogrel with caution. Influence on the ability to drive motor vehicles and control mechanisms The drug does not affect or slightly affects the ability to drive vehicles and mechanisms.