Description
Latin name
Lopirel
Release form
Tablets.
packaging 14 pcs
Pharmacological action
LOPIREL is an antiplatelet drug, a specific and active inhibitor of platelet aggregation. It has a coronary dilating effect. Selectively reduces the binding of ADP to platelet receptors and the activation of GPI Ib / IIIa receptors by ADP, thereby reducing platelet aggregation. Reduces platelet aggregation caused by other agonists, preventing their activation by released 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 atherothrombosis:
– in patients who have had myocardial infarction, ischemic stroke, or with a diagnosed peripheral artery disease
– in patients with acute coronary syndrome without ST segment elevation (unstable cardiac angina pectoris or infarction) in combination with acetylsalicylic acid, including patients who have had stenting with percutaneous coronary intervention
– in patients with acute coronary syndrome with ST segment elevation (acute myocardial infarction) in combination with acetylsalicylic acid receiving medical treatment with the possible use of thrombolyte.
Contraindications
– severe hepatic failure
– hemorrhagic syndrome
– acute bleeding (including intracranial hemorrhage) and diseases predisposing to its development (peptic ulcer, duodenal ulcer, non-tuberculous ulcer, tuberculosis, pulmonary hyperfibrinolysis)
– pregnancy
– lactation (breastfeeding)
– neonatal period
– age under 18 years (efficacy and safety not established)
– not tolerated galactose bridge, lactase deficiency or malabsorption of glucose-galactose (since lactose is part of the drug)
– hypersensitivity to the drug components.
Use during pregnancy and lactation
The drug Lopirel is contraindicated in pregnancy and lactation (breastfeeding).
Composition
1 tablet contains clopidogrel hydrosulfate 97.87 mg, corresponding to 75 mg of clopidogrel base.
Excipients: lactose, microcrystalline cellulose, crospovidone (type A), glyceryl dibehenate, talc, Opadry II 85 G34669 pink (polyvinyl alcohol, talc, titanium dioxide (E171), macrogol 3350, lecithin (E322), iron oxide red (E172).
Dosage and administration of
The drug is taken orally, regardless of food intake.
For patients who have had a myocardial infarction, ischemic stroke, or with peripheral artery disease, the drug is prescribed 75 mg 1 time / day. Treatment should be started from the first 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 pectoris, myocardial infarction without Q wave on ECG), including patients in which stenting was performed with percutaneous coronary intervention, treatment with Lopirel should be started with a single dose of a loading dose of 300 mg, and then continued at a dose of 75 mg 1 time / day (in combination with acetylsalicylic acid). Since the use of acetylsalicylic acid in high doses is associated with an increased risk of bleeding, the recommended dose of acetylsalicylic acid for this indication does not exceed 100 mg. The maximum beneficial effect is observed by 3 months of treatment. The course of treatment is up to 1 year.
Patients with acute coronary syndrome with ST segment elevation (acute myocardial infarction) in combination with acetylsalicylic acid receiving medical treatment with the possible use of thrombolytic therapy, Lopirel is prescribed once at a dose of 75 mg 1 time / day with the initial single dose of the loading dose in combination with acetylsalicylic acid and thrombolytics (or without thrombolytics). Combination therapy is started as soon as possible after the onset of symptoms and continues for at least 4 weeks. In patients older than 75 years of age, treatment with Lopirel should be started without taking a loading dose.
Side effects
Determination of the frequency of adverse reactions: often (> 1/100, <1/10), sometimes (> 1/1000, <1/100), rarely (> 1/10 000, <1/1000), very rarely (<1/10 000). From the side of the central nervous system: sometimes – headache, dizziness, paresthesia very rarely – confusion, hallucinations, violation of taste sensations. From the digestive system: often – dyspepsia, abdominal pain, diarrhea sometimes – nausea, gastritis, flatulence, constipation, vomiting, stomach and duodenal ulcer very rarely – colitis (including ulcerative or lymphocytic), pancreatitis. From the hepatobiliary system: very rarely – hepatitis, increased activity of hepatic transaminases. From the hemopoietic system: sometimes – leukopenia, a decrease in the number of neutrophilic and eosinophilic granulocytes, platelet count reduction is very rare – severe thrombocytopenia (platelet count 30 109 / l), granulocytopenia, agranulocytosis, anemia and aplastic anemia / pancytopenia. From the blood coagulation system: sometimes – an increase in bleeding time is very rare – thrombotic thrombocytopenic purpura (1 case per 200,000 patients) often – bleeding of various localization and intensity. Most cases of bleeding were noted during the 1st month of treatment (especially intracranial, gastrointestinal and retroperitoneal bleeding), severe cases of skin bleeding (purpura), hemorrhages in the joints and soft tissues (hemarthrosis, hematoma), eye bleeding (conjunctival, ocular, retinal ), nosebleeds, from the respiratory tract (hemoptysis, pulmonary hemorrhage), hematuria and bleeding from an operating wound. Dermatological reactions: sometimes – rash and itching very rarely – bullous rash (erythema multiforme), erythematous rash, lichen planus. Allergic reactions: very rarely – urticaria, anaphylactoid reactions. From the cardiovascular system: very rarely – vasculitis, arterial hypotension. From the respiratory system: very rarely – bronchospasm. From the musculoskeletal system: very rarely – arthralgia, arthritis. From the urinary system: very rarely – glomerulonephritis, an increase in serum creatinine. Other: very rare – fever. Drug Interaction Increased bleeding rate may be exacerbated with the use of clopidogrel with warfarin (this combination is not recommended). Acetylsalicylic acid does not alter the inhibitory effect of clopidogrel on ADP-induced platelet aggregation, however clopidogrel potentiates the effect of acetylsalicylic acid on platelet aggregation induced by collagen. However, the concurrent administration of acetylsalicylic acid at a dose of 500 mg 2 times / day did not cause any significant increase in bleeding time, prolonged due to clopidogrel. The safety of long-term simultaneous use of acetylsalicylic acid and clopidogrel has not been established, however, clopidogrel and acetylsalicylic acid can be used simultaneously for up to one year. According to a clinical study conducted on healthy volunteers, the simultaneous use of clopidogrel and heparin does not require dose adjustment of the latter and does not affect the antiaggregant action of clopidogrel, however, the safety of such combination has not yet been established (caution is required with this combination). The safety of concurrent use of clopidogrel with thrombolytics has not been established at this time (caution is required with this combination). In a clinical study conducted with the participation of healthy volunteers, with the combined use of clopidogrel and naproxen, an increase in the number of hidden gastrointestinal bleeding was observed. However, due to the lack of clinical studies of the interaction of the drug with others The safety of concurrent use of clopidogrel with thrombolytics has not been established at this time (caution is required with this combination). In a clinical study conducted with the participation of healthy volunteers, with the combined use of clopidogrel and naproxen, an increase in the number of hidden gastrointestinal bleeding was observed. However, due to the lack of clinical studies of the interaction of the drug with others The safety of concurrent use of clopidogrel with thrombolytics has not been established at this time (caution is required with this combination). In a clinical study conducted with the participation of healthy volunteers, with the combined use of clopidogrel and naproxen, an increase in the number of hidden gastrointestinal bleeding was observed. However, due to the lack of clinical studies of the interaction of the drug with othersThere is currently no evidence of an ugly NSAID if there is an increased risk of gastrointestinal bleeding when using other drugs in this group (caution is required with the combination of clopidogrel and NSAIDs). No clinically relevant pharmacodynamic interaction was observed with clopidogrel in combination with atenolol and / or nifedipine. The pharmacodynamic activity of Lopirel is virtually unchanged when co-administered with phenobarbital, cimetidine or estrogens. The pharmacokinetic properties of digoxin or theophylline do not change when used together with clopidogrel. Antacids do not alter the absorption of clopidogrel. Data from studies with human liver microsomes indicate that that clopidogrel may inhibit CYP2C9 isoenzyme activity. As a result, some drugs, such as phenytoin and tolbutamide, may be increased in blood plasma because they are metabolized by CYP2C9. The results of the CAPRIE study indicate the safety of phenytoin and tolbutamide in combination with clopidogrel. Overdose Symptoms: Increased bleeding time. Treatment: Clopidogrel effect may be eliminated by platelet transfusion if rapid correction of increased bleeding time is required. There is no specific antidote. Storage conditions At a temperature not exceeding 30 ° C. Expiration 3 years. Deystvuyuschee substances clopidogrel Dispensing conditions from pharmacies Prescription dosage form dosage form tablets Actavis Ltd, Iceland
