Description
Release form
Film-coated tablets.
Packing
28 pcs.
Pharmacological action
Egithromb is an antiplatelet drug, a specific and active inhibitor of platelet aggregation. It has a coronary dilating effect, selectively reduces the binding of adenosine diphosphate (ADP) to platelet receptors and the activation of glycoprotein IIb / IIIa receptors under the influence of ADP, thereby reducing platelet aggregation.
Reduces platelet aggregation caused by other agonists of these receptors, preventing their activation by free ADP, does not affect the activity of PDE. 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 ingestion (40% inhibition) of an initial dose of 400 mg. The maximum effect (60% inhibition of aggregation) develops after 4-7 days of constant intake at a dose of 50-100 mg / day. The antiplatelet effect lasts the entire period of platelet life (7-10 days).
In the presence of 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).
Indications
Prevention of ischemic disorders (myocardial infarction, stroke, peripheral arterial thrombosis, sudden vascular death) in patients with atherosclerosis, including:
– After myocardial infarction.
– After an ischemic stroke.
– Against the background of diagnosed diseases of the peripheral arteries.
– In acute coronary syndrome without ST segment elevation (unstable angina or myocardial infarction without Q wave formation) in combination with acetylsalicylic acid.
– In acute myocardial infarction with ST segment elevation in combination with acetylsalicylic acid in patients receiving conservative treatment who are indicated for thrombolytic therapy.
Contraindications
– Severe liver failure.
– Active pathological bleeding (peptic ulcer or intracranial hemorrhage).
– Pregnancy.
– Lactation (breastfeeding).
– Age under 18 years (effectiveness and safety have not been proven).
– Hypersensitivity to the drug.
With caution, the drug should be used with moderate liver failure, chronic renal failure, with pathological conditions that increase the risk of bleeding (including trauma, surgery), while taking acetylsalicylic acid, NSAIDs (including COX-2 inhibitors), heparin and glycoprotein IIb / IIIa inhibitors.
Use during pregnancy and lactation
There are no clinical data on the use of the drug Egithromb during pregnancy, therefore, clopidogrel should not be prescribed during pregnancy. There is no information on the excretion of clopidogrel with breast milk in humans, so the use of the drug during lactation is contraindicated.
Special instructions
Caution is advised to use the drug in patients with an increased risk of bleeding due to trauma, surgical intervention, in patients with injuries prone to bleeding (especially gastrointestinal and intraocular), as well as in patients receiving acetylsalicylic acid, NSAIDs (including COX-2 inhibitors), heparin or glycoprotein IIb / IIIa inhibitors. Patients should be carefully monitored to identify any signs of bleeding, including latent, especially during the first weeks of using the drug and / or after invasive procedures on the heart or surgical operations. The simultaneous use of clopidogrel and warfarin is not recommended, t. to. it can increase bleeding.
During the treatment period, it is necessary to monitor the parameters of the hemostatic system (APTT, platelet count, platelet functional activity tests) to regularly examine the functional activity of the liver.
In the case of surgical interventions, if an antiplatelet effect is undesirable, the treatment should be discontinued 7 days before surgery.
Patients should be warned that since stopping bleeding due to the use of clopidogrel (in combination with acetylsalicylic acid or without it) requires more time, they should inform the doctor about each case of unusual bleeding. Patients should also inform the doctor about taking the drug if they have surgery and before taking any new drug.
After taking clopidogrel, thrombotic thrombocytopenic purpura was very rare, 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 – a potentially fatal condition that requires immediate treatment, including using plasmapheresis.
Due to a lack of data, clopidogrel cannot be recommended for acute (less than 7 days) ischemic strokes. Experience with clopidogrel in patients with impaired renal function is limited, therefore, Egithromb should be prescribed with caution in this category of patients. In severe violations of liver function, the risk of hemorrhagic diathesis should be considered. The experience of using the drug in patients with moderate impaired liver function is limited, therefore, Egithromb should be prescribed with caution in this category of patients.
The drug does not affect or slightly affects the ability to drive vehicles and work with mechanisms.
Composition
1 tablet contains: clopidogrel hydrosulfate 97.86 mg, which corresponds to the content of clopidogrel 75 mg.
Excipients: microcrystalline cellulose and silicon dioxide colloidal anhydrous (microcrystalline silicon cellulose), hyprolose (with a low degree of substitution (L-HPC B1)), hydrogenated castor oil, Opadry white YI-7000 (hypromellose, titanium dioxide, macrogol 400).
Dosage and administration of
The drug is taken orally. Adults and elderly patients Egithromb is prescribed 75 mg 1 time / day. regardless of the meal. Treatment should be started from a few 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 angina or myocardial infarction without Q wave), clopidogrel should be started with a single shock dose of 300 mg, and then continue to take 75 mg 1 time / day. in combination with acetylsalicylic acid (at a dose of 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 of not more than 100 mg. Clinical trial data indicate the possibility of using the drug for up to 12 months, and the maximum clinical advantage is noted after 3 months.
Acute myocardial infarction with ST segment elevation: Egithromb should be taken at a dose of 75 mg 1 time / day. Treatment should be started with a loading dose and combined with acetylsalicylic acid and thrombolytics or without thrombolytics. For patients older than 75 years of age, the course of the drug Egithromb should be prescribed without an initial loading dose. Combination therapy should be read as soon as possible after the development of symptoms and continue for at least 4 weeks.
Side effects of
From the blood coagulation system: most often bleeding (especially often in patients receiving clopidogrel with acetylsalicylic acid, or clopidogrel with acetylsalicylic acid and heparin) sometimes – an increase in bleeding time and a decrease in the number of platelets (thrombocytopenia (thrombocytopenia) – thrombotic thrombocytopenic purpura (1/200 000 patients taking the drug).
From the side of the central nervous system and peripheral nervous system: sometimes – headache, dizziness, rare paresthesia – systemic dizziness is very rare – confusion, hallucinations, disorders of taste sensations.
From the digestive system: often- gastrointestinal bleeding, diarrhea, abdominal pain, dyspepsia sometimes – hemorrhagic stroke, stomach ulcer, duodenal ulcer, gastritis, nausea, vomiting, constipation, bloating very rarely – pancreatitis, colitis (in including ulcerative or lymphocytic colitis), stomatitis, acute liver failure, hepatitis, impaired liver function tests.
From the cardiovascular system: sometimes – arterial hypotension, very rarely – vasculitis.
From the hemopoietic system: sometimes – leukopenia, neutropenia and eosinophilia very rarely – severe thrombocytopenia (platelet count Dermatological reactions: sometimes – itching very rarely – bullous dermatitis (erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), erythematous rash, eczema, lichen planus.
Allergic reactions: skin rash is very rare – urticaria, angioedema, serum sickness, anaphylactoid reactions.
On the part of the respiratory system: very rarely – bronchospasm, interstitial pneumonitis.
From the musculoskeletal system: very rarely – arthralgia, arthritis, myalgia.
From the urinary system: very rarely – increased serum creatinine, glomerulonephritis.
Other: very rare – fever.
Drug interaction
Enhances the antiplatelet effect of acetylsalicylic acid, heparin, thrombolytics, indirect anticoagulants, NSAIDs), increases the risk of gastrointestinal bleeding, therefore, the simultaneous use of these funds requires caution.
Clopidogrel should be used with caution in patients who may be at risk of increased bleeding due to trauma or surgery if they take IIb / IIIa glycoprotein inhibitors at the same time. The simultaneous use of clopidogrel and warfarin is not recommended, because at the same time, bleeding may increase.
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 significantly change with the simultaneous use of phenobarbital, cimetidine or estrogens. The pharmacokinetics of digoxin or theophylline did not change with the simultaneous administration of clopidogrel. Antacids do not affect the absorption of clopidogrel.
A study of human hepatic microsomes showed that the clopidogrel metabolite related to carboxylic acids can inhibit the activity of the CYP2C9 isoenzyme. This can increase plasma levels of drugs such as phenytoin, tolbutamide, and NSAIDs, which are metabolized with CYP2C9. The use of phenytoin and tolbutamide together with clopidogrel is safe.
Overdose
Symptoms: Prolonged bleeding time may occur, which can lead to bleeding complications.
Treatment: Platelet transfusion may eliminate the effects of clopidogrel if rapid reduction of prolonged bleeding is necessary. No antidotes of the pharmacological activity of clopidogrel were detected.
Storage conditions
The product should be stored out of reach of children at a temperature not exceeding 25 ° C.
Shelf life
3 years.
Deystvuyushtee substance
Clopidogrel
dosage form
tablets
Appointment
Appointment
Adults prescribed by a doctor
