Clopidogrel Teva coated pills 75mg N28
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Active ingredients
Clopidogrel
Release form
Pills
Composition
Active ingredient: Clopidogrel Concentration of active ingredient (mg): 75 mg
Pharmacological effect
Platelet aggregation inhibitor. Selectively inhibits the binding of adenosine diphosphate (ADP) to platelet receptors and the activation of GPIIb / IIIa complex, thus inhibiting platelet aggregation. Also inhibits platelet aggregation caused by other agonists, by blocking the increase in platelet activity by released ADP. Does not affect the activity of PDE. Clopidogrel irreversibly alters the receptors for ADP on platelets, so platelets remain non-functional throughout life, and the restoration of normal function occurs as they renew (approximately 7 days).
Pharmacokinetics
After oral administration in a dose of 75 mg, clopidogrel is rapidly absorbed from the gastrointestinal tract. However, plasma concentration increases slightly and after 2 hours after administration does not reach a level that can be determined (0.025 mcg / l). It is intensively metabolized in the liver. The main metabolite is an inactive carboxylic acid derivative and constitutes about 85% of the original substance circulating in the plasma. Cmax of this metabolite in plasma after repeated administration of clopidogrel is about 3 mg / l and is observed approximately 1 hour after administration. The pharmacokinetics of the main metabolite is characterized by a linear dependence in the range of clopidogrel 50-150 mg. Clopidogrel and the main metabolite bind irreversibly to plasma proteins in vitro (98% and 94%, respectively). This relationship remains unsaturated in vitro over a wide range of concentrations. After ingestion of 14C-labeled clopidogrel, about 50% of the dose taken is excreted in the urine and approximately 46% in feces within 120 hours. The T1 / 2 of the main metabolite is 8 hours. Compared to healthy volunteers At a young age, the concentration in the blood plasma of the main metabolite is significantly higher in elderly patients (75 years of age and older), and there are no changes in platelet aggregation and bleeding time. In severe kidney disease (CK 5–15 ml / min), The main metabolite in the blood plasma is lower than in patients with moderately severe kidney diseases (CC 30-60 ml / min) and in healthy volunteers.Although the inhibitory effect on ADP-induced platelet aggregation was reduced compared with that in healthy volunteers, the bleeding time increased to the same extent as in healthy volunteers.
Indications
Prevention of thrombotic complications: after a myocardial infarction (from several days to 35 days), ischemic stroke (from 6 days to 6 months) or in diagnosed peripheral artery disease; 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 arda) in combination with acetylsalicylic acid, in patients receiving drug therapy 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 have not been established); hypersensitivity to the components of the drug. liver and kidneys (including with moderate liver and / or renal failure), injuries, preoperative conditions.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
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 clopidogrel in doses of 300-500 mg / kg / day, no teratogenic effects and negative effects on fertility and fetal development were identified. It is established that clopidogrel and its metabolites are excreted in breast milk.
Dosage and administration
Inside, regardless of the meal.For the prevention of ischemic disorders in patients after myocardial infarction, ischemic stroke and the diagnosed disease of peripheral arteries - 75 mg 1 time / day. Treatment should begin in terms from several days to 35 days after a myocardial infarction and from 7 days to 6 months after an ischemic stroke. In acute coronary syndrome without ST-segment elevation (unstable angina or myocardial infarction without a Q wave), treatment should begin with a single loading dose of 300 mg, and then continue to use the drug at a dose of 75 mg 1 time / day (with simultaneous administration of acetylsalicylic acid in a dose 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 in a dose of 75 mg 1 time / day using the initial loading dose in combination with acetylsalicylic acid with or without thrombolytic therapy. 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.
Side effects
The frequency of side effects is determined according to the following criteria: very often - more than 1/10, often - more than 1/100 and less than 1/10, infrequently - more than 1/1000 and less than 1/100, rarely - more than 1/10000 and less than 1 / 1000, very rarely - less than 1/10000, including isolated cases, On the part of the blood coagulation system: often - bleeding (in most cases - during the first month of treatment), purpura, hematoma; infrequently - conjunctive bleeding; rarely, intracranial bleeding; lengthening of bleeding time, leukopenia, decrease in the number of neutrophils and eosinophilia, decrease in the number of platelets. From the hemopoietic system: very rarely - thrombocytopenic thrombohemolytic purpura, severe thrombocytopenia (platelet count <30,000 / μl), granulocytopenia, agranulocytosis, anemia incl. aplastic anemia, pancytopenia. On the part of the nervous system: infrequently - headache, dizziness, paresthesias; rarely - vertigo; very rarely - confusion, hallucinations.Since the cardiovascular system: often - hematoma; very rarely - severe bleeding, bleeding from the surgical wound, vasculitis, lowering 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, flatulence, constipation; rarely retroperitoneal bleeding; very rarely - colitis (including ulcerative or lymphocytic), pancreatitis, change in taste, stomatitis, hepatitis, acute liver failure, increased activity of liver enzymes, From the musculoskeletal system: very rarely - arthralgia, arthritis, myalgia. From the urinary system: infrequently - hematuria; very rarely - glomerulonephritis, hypercreatininemia. Dermatological reactions: very rarely - bullous rash (erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis), erythematous rash, eczema, lichen planus. Allergic reactions: very rarely - angioedema, urticaria, anaphylactoid reactions, serum sickness. Other: very rarely - fever.
Overdose
Overdose of the drug is not described.
Interaction with other drugs
With simultaneous use with NSAIDs (including naproxen) increases the risk of gastrointestinal bleeding. With simultaneous use with acetylsalicylic acid may increase antiplatelet effects. Because clopidogrel may inhibit the activity of the CYP2C9 isoenzyme, while used with drugs metabolized with this isoenzyme (including with phenytoin, tolbutamine) it is impossible to exclude an increase in their concentrations in the blood plasma.
special instructions
With caution, clopidogrel is used with an increased risk of bleeding due to trauma, surgical interventions, and impaired hemostasis. For planned surgical interventions (if the antiplatelet effect is undesirable), clopidogrel should be canceled 7 days before the operation. Clopidogrel is used with caution in patients with severely impaired liver function,in which the occurrence of hemorrhagic diathesis is possible. If symptoms of excessive bleeding occur (bleeding of the gums, menorrhagia, hematuria), hemostasis (bleeding time, platelet count, platelet functional activity tests) is shown. Regular monitoring of laboratory parameters of the functional activity of the liver is recommended. It is used with caution simultaneously with warfarin, heparin, NSAIDs, and for a long time with acetylsalicylic acid, since At present, the safety of such an application has not been definitively established. In experimental studies, no carcinogenic and genotoxic effects have been identified. Effect on the ability to drive vehicles and control mechanisms It has not been established that clopidogrel has an effect on the ability to drive vehicles and control mechanisms.