Pradaxa capsules 150 mg 180 pcs
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Active ingredients
Dabigatran etexilate
Composition
Dabigatran etexilate mesilate 172.95 mg, which corresponds to the content of dabigatran etexilate 150 mg Auxiliary substances: acacia gum - 8.86 mg, tartaric acid, coarse-grained - 44.28 mg, tartaric acid, powder - 59.05 mg, tartaric acid, crystalline - 73.81 mg, hypromellose - 4.46 mg , Dimethicone - 0.08 mg, talc - 34.31 mg, hyprolose (hydroxypropylcellulose) - 34.59 mg. The composition of the capsular shell: a capsule of hypromellose (HPMC) with overprinted in black ink - 90 * mg. Composition of HPMC capsules: carrageenan (E407) - 0.285 mg, potassium chloride - 0.4 mg, titanium dioxide (E171) - 5.4 mg, indigo carmine (E132) - 0.054 mg, dye sunsets yellow (E110) - 0.004 mg, hypromellose (hydroxypropylmethylcellulose) - 79.35 mg, purified water - 4.5 mg. The composition of black ink (%, mass.): Shellac - 24-27%, butanol - 1-3%, isopropanol - 1-3%, iron dye black oxide (E172) - 24-28%, purified water - 15-18 %, propylene glycol - 3-7%, ethanol - 23-26%, ammonia water - 1-2%, potassium hydroxide - 0.05-0.1%.
Pharmacological effect
Direct inhibitor of thrombin. Dabigatran etexilate is a low molecular weight, non-pharmacologically active precursor of the active form of dabigatran. After ingestion of dabigatran, etexilate is rapidly absorbed from the gastrointestinal tract and, by hydrolysis catalyzed by esterases, in the liver and blood plasma is converted into dabigatran. Dabigatran is a potent competitive reversible direct inhibitor of thrombin and the main active substance in blood plasma. Since thrombin (serine protease) converts fibrinogen to fibrin in the process of coagulation, the suppression of its activity prevents the formation of a blood clot. Dabigatran inhibits free thrombin, fibrin-binding thrombin and thrombin-induced platelet aggregation. In experimental studies on various models of thrombosis in vivo and ex vivo, the antithrombotic effect and the anticoagulant activity of dabigatran after iv administration and dabigatran etexilate were confirmed after oral administration. A direct correlation between the concentration of dabigatran in the blood plasma and the severity of the anticoagulant effect was established. Dabigatran lengthens APTT, ekarinovo clotting time (EVS) and thrombin time (TV). Prevention of venous thromboembolism (VTE) after endoprosthetics of large joints. Results of clinical studies in patientsthose who underwent orthopedic operations - endoprosthetics of the knee and hip joints - confirmed the retention of hemostasis parameters and the equivalence of the use of dabigatran etexilate in doses of 75 mg or 110 mg 1-4 hours after surgery and the subsequent maintenance dose of 150 mg or 220 mg 1 time / day for 6- 10 days (with surgery on the knee joint) and 28-35 days (on the hip joint) compared with enoxaparin at a dose of 40 mg 1 time / day, which was used the day before and after surgery. The equivalence of the antithrombotic effect of dabigatran etexilate was shown when used in doses of 150 mg or 220 mg compared to enoxaparin at a dose of 40 mg / day when assessing the main endpoint, which includes all cases of venous thromboembolism and mortality from any causes. Prevention of stroke and systemic thromboembolism in patients with atrial fibrillation With prolonged, on average about 20 months, use in patients with atrial fibrillation and with moderate or high risk of stroke or systemic thromboembolism, it was shown that dabigatran etexilate at a dose of 110 mg, used 2 times / day, was not inferior to warfarin in terms of the effectiveness of stroke prevention and systemic thromboembolism in patients with atrial fibrillation, and in the dabigatran group, a decrease in the risk of intracranial bleeding was noted and boiling in bleeding. The use of the drug in a higher dose (150 mg 2 times / day) significantly reduced the risk of ischemic and hemorrhagic stroke, cardiovascular death, intracranial bleeding, and general bleeding rate, compared with warfarin. A lower dose of dabigatran was characterized by a significantly lower risk of major bleeding compared with warfarin. The net clinical effect was assessed by determining a combined endpoint, including the incidence of stroke, systemic thromboembolism, pulmonary embolism, acute myocardial infarction, cardiovascular mortality, and major bleeding. The annual incidence of these events in patients who received dabigatran etexilate was lower than in patients who received warfarin. Changes in laboratory parameters of liver function in patients who received dabigatran etexilate were observed with comparable or lower frequency compared with patients receiving warfarin.Thromboembolic prophylaxis in patients with prosthetic heart valves During clinical studies of phase II use of dabigatran and warfarin in patients who underwent surgery to replace a heart valve with a mechanical prosthesis (recently performed operations and surgeries more than 3 months ago), an increase in the incidence of thromboembolism and general the number of bleeding (mainly due to small bleeding) in patients who received dabigatran etexilate. In the early postoperative period, major bleeding was mainly characterized by a hemorrhagic effusion in the pericardium, especially in patients to whom dabigatran etexilate was prescribed in the early period (on day 3) after surgical replacement of the heart valves. Treatment of acute deep vein thrombosis (THV) and / or pulmonary thromboembolism (PE) and prevention of deaths caused by these diseases The results of clinical studies in patients with acute THV and / or PEH who initially received parenteral therapy for at least 5 days, it was confirmed that dabigatran etexilate in a dose of 150 mg, used 2 times / day, was not inferior to warfarin in terms of effectiveness in reducing the frequency of recurrent symptomatic DVT and / or pulmonary embolism and deaths due to these diseases during the 6-month treatment period. In patients who received dabigatran etexilate, bleeding was observed much less frequently than in patients who received warfarin. The incidence of myocardial infarction in all ongoing studies with VTE in all treatment groups was low. Prevention of recurrent DVT and / or pulmonary embolism and deaths caused by these diseases The results of a clinical study in patients with recurrent DVT and pulmonary embolism who had received anticoagulant therapy for 3 to 12 months and needed to continue it, confirmed that treatment with dabigatran etexilate 150 mg 2 times / day was not inferior to the therapeutic effect of warfarin (p = 0.0135). In patients who received dabigatran etexilate, bleeding was observed much less frequently than in patients who received warfarin. In a study comparing dabigatran etexilate with placebo in patients already receiving vitamin K antagonists for 6 to 18 months, it was found that dabigatran was superior to placebo in preventing recurrent symptomatic DVT / TELA, including deaths from an unknown cause, reducing the risk over the period treatment was 92% (less than 0.0001).The incidence of myocardial infarction in all ongoing studies with VTE in all treatment groups was low. Indicators of liver function In studies using active comparison drugs, possible changes in liver function indicators occurred in patients who received dabigatran etexilate, with comparable or lower frequency than in patients who received warfarin. In the study with placebo, there was no significant difference in changes in liver function indicators, which may have clinical significance, between the groups using dabigatran etexilate and placebo.
Indications
- prevention of venous thromboembolism in patients after orthopedic surgeries; prevention of stroke, systemic thromboembolism and reduction of cardiovascular mortality in patients with atrial fibrillation; treatment of acute deep vein thrombosis and / or thromboembolism of the pulmonary artery and prevention of deaths caused by these diseases — prevention. deep veins and / or thromboembolism of the pulmonary artery and deaths caused by these diseases.
Contraindications
- severe renal failure (CC less than 30 ml / min) - active clinically significant bleeding, hemorrhagic diathesis, spontaneous or pharmacologically induced hemostasis - organ damage as a result of clinically significant bleeding, including hemorrhagic stroke during the previous 6 months before the start of therapy - significant risk the development of large bleeding from existing or recent ulceration of the gastrointestinal tract, the presence of malignant tumors with a high risk of bleeding, recent damage to the heads The leg or spinal cord, recent surgery on the brain or spine, or ophthalmic surgery, recent intracranial hemorrhage, the presence or suspicion of varicose veins of the esophagus, congenital arteriovenous defects, vascular aneurysms or large intravertebral or intracerebral vascular disorders - co-administration of any other anticoagulants, including unfractionated heparin, low molecular weight heparins (including enoxaparin, dalteparin), derivatives of heparin (including fondaparinux), oral anticoagulants (including warfarin, rivaroxaban, apixaban),except when switching to or from treatment with Pradaxa. or in the case of using unfractionated heparin in doses necessary to maintain a central venous or arterial catheter - simultaneous administration of ketoconazole for systemic use, cyclosporine, itraconazole, tacrolimus and dronedarone — abnormal liver function and liver disease that may affect survival — the presence of a prosthetic heart valve - children's and teenage age up to 18 years (clinical data are absent) - hypersensitivity to dabigatran or dabigatran etexil atu or to one of the excipients. The drug should be used with caution in conditions that increase the risk of bleeding: - 75 years of age and older - moderate decrease in kidney function (CC 30-50 ml / min) - simultaneous use of P-glycoprotein inhibitors (except for those indicated in the section "Contraindications") body weight less than 50 kg - simultaneous use of NSAIDs (including acetylsalicylic acid), clopidogrel, selective serotonin reuptake inhibitors and selective noradrenaline reuptake inhibitors, as well as other drugs that can disrupt hemostasis — congenital or acquired diseases of the blood coagulation system — thrombocytopenia or functional defects of platelets — a recent biopsy or extensive trauma — bacterial endocarditis — esophagitis, gastritis, or gastroesophageal reflux disease.
Use during pregnancy and lactation
Data on the use of dabigatran etexilate during pregnancy are not available. The potential risk in a person is unknown. In experimental studies have not established adverse effects on fertility or postnatal development of newborns. Women of reproductive age should avoid becoming pregnant during treatment with Pradaxa. When pregnancy occurs, the use of the drug is not recommended, except in cases where the expected benefit outweighs the possible risk. If you need to use the drug during breastfeeding, due to the lack of clinical data, breastfeeding is recommended to stop (as a precautionary measure).
Dosage and administration
Capsules should be taken orally, 1 or 2 times / day, regardless of the time of meals, with a glass of water to facilitate the passage of the drug in the stomach. Do not open the capsule. To remove the capsules from the blister: - tear up one individual blister from the blister packaging along the perforation line, - remove the capsule from the blister by peeling off the foil, - do not squeeze the capsules through the foil. The drug is prescribed for adults. Prevention of venous thromboembolism (VTE) in patients after orthopedic operations: the recommended dose is 220 mg 1 time / day (2 capsules, 110 mg each). In patients with moderate renal impairment due to the risk of bleeding, the recommended dose is 150 mg 1 time / day (2 capsules, 75 mg each). Prevention of VTE after knee arthroplasty: the use of the drug Pradaxa. should begin after 1-4 hours after completion of the operation with receiving 110 mg (1 caps.), followed by increasing the dose to 220 mg (2 caps.) / day 1 time / day for the next 10 days. If hemostasis is not achieved, treatment should be postponed. If treatment has not begun on the day of surgery, therapy should begin with taking 220 mg (2 capsules) / day 1 time / day. Prevention of VTE after hip arthroplasty: the use of the drug Pradaxa. should begin after 1-4 hours after completion of the operation with a dose of 110 mg (1 capsule), followed by increasing the dose to 220 mg (2 capsules) / day 1 time / day for the next 28-35 days. If hemostasis is not achieved, treatment should be postponed. If treatment has not begun on the day of surgery, therapy should begin with taking 220 mg (2 capsules) / day 1 time / day. Prevention of stroke, systemic thromboembolism and reduction of cardiovascular mortality in patients with atrial fibrillation: the use of Pradaxa is recommended. in a daily dose of 300 mg (1 capsule. 150 mg 2 times / day). Therapy must be continued for life. Treatment of acute DVT and / or pulmonary embolism and prevention of deaths caused by these diseases: the use of the drug Pradaxa is recommended. in a daily dose of 300 mg (1 caps. 150 mg 2 times / day) after parenteral treatment with an anticoagulant for at least 5 days. Therapy should be continued until 6 months. Prevention of recurrent THV and / or pulmonary embolism and death caused by these diseases: the use of the drug Pradaxa is recommended. in a daily dose of 300 mg (1 capsule. 150 mg 2 times / day). Therapy can continue for life, depending on the individual risk factors.Use in patients with impaired renal function: Before therapy, in order to avoid administering the drug to patients with severe impaired renal function (CC less than 30 ml / min), it is necessary to preliminarily evaluate CC. In connection with the lack of data on the use of the drug in patients with severely impaired renal function (CC less than 30 ml / min), the use of the drug Pradaxa. contraindicated. Renal function should be assessed in the course of treatment when there is a suspicion of a possible decrease or deterioration of renal function (for example, in case of hypovolemia, dehydration, simultaneous use of certain drugs). During clinical studies of the drug Pradaxa. As a method for assessing kidney function, the calculation of QC using the Cockroft-Gault formula was used. Dabigatran is derived from hemodialysis, but clinical experience with patients undergoing hemodialysis is limited. When using the drug Pradaxa. in order to prevent venous thromboembolism in patients after orthopedic operations with moderate renal impairment (CC 30-50 ml / min), the daily dose should be reduced to 150 mg (2 capsules 75 mg 1 time / day). When using the drug Pradaxa. In order to prevent stroke, systemic thromboembolism and reduce cardiovascular mortality in patients with atrial fibrillation with moderate renal impairment (CC 30-50 ml / min), dose adjustment is not required. The use of the drug is recommended in a daily dose of 300 mg (1 capsule. 150 mg 2 times / day). Renal function should be assessed at least once a year. When using the drug Pradaxa. for the purpose of treating acute DVT and / or PE, and preventing deaths caused by these diseases, dose adjustment is not required in patients with CC greater than 30 ml / min. The use of the drug is recommended in a daily dose of 300 mg (1 capsule. 150 mg 2 times / day). When using the drug Pradaxa. In order to prevent recurrent THV and / or pulmonary embolism and deaths caused by these diseases in patients with moderate renal impairment (CC 30-50 ml / min), dose adjustment is not required. The use of the drug is recommended in a daily dose of 300 mg (1 capsule. 150 mg 2 times / day). Renal function should be assessed at least once a year. Use in elderly patients: Due to the fact that the increase in drug exposure in elderly patients (over 75 years old) is often due to a decrease in kidney function, it is necessary to evaluate kidney function before prescribing the drug. Renal function should be assessed at least once a year or more often, depending on the clinical situation.Dose adjustment of the drug should be carried out depending on the severity of renal dysfunction. Prevention of venous thromboembolism after orthopedic surgeries in patients over 75 years of age: experience with use is limited. The recommended dose is 150 mg (2 caps. 75 mg in a single dose). When using the drug Pradaxa. in patients older than 80 years for the prevention of stroke, systemic thromboembolism and reduction of cardiovascular mortality in patients with atrial fibrillation Pradaxa. should be taken in a daily dose of 220 mg (1 capsule. 110 mg 2 times / day). Treatment of acute DVT and / or pulmonary embolism and prevention of deaths caused by these diseases in patients over 75 years of age: dose adjustment is not required. The use of the drug is recommended in a daily dose of 300 mg (1 capsule. 150 mg 2 times / day). Prevention of recurrent THV and / or pulmonary embolism and death caused by these diseases in patients over 75 years of age: dose adjustment is not required. The use of the drug is recommended in a daily dose of 300 mg (1 capsule. 150 mg 2 times / day). Use in children: In patients under the age of 18, the efficacy and safety of the use of the drug Pradaxa. not studied, so the use of the drug in children is not recommended. Patients with different body weight: Prevention of venous thromboembolism after orthopedic operations in patients with a body weight of less than 50 kg and more than 110 kg of experience use is limited. In accordance with the pharmacokinetic and clinical data dose adjustment is not required. However, observation of such patients is recommended. Prevention of stroke, systemic thromboembolism and reduction of cardiovascular mortality in patients with atrial fibrillation: dose adjustment is not required according to pharmacokinetic and clinical data. However, patients weighing less than 50 kg should be monitored. Treatment of acute DVT and / or pulmonary embolism and prevention of deaths caused by these diseases: do not require dose adjustment depending on body weight. Prevention of recurrent THV and / or pulmonary embolism and deaths caused by these diseases: dose adjustment is not required depending on body weight. The simultaneous use of the drug Pradaxa. with active inhibitors of P-glycoprotein (amiodarone, quinidine, verapamil) Prevention of venous thromboembolism after orthopedic operations: while using amiodarone, quinidine or verapamil, the dose of Pradaxa. should be reduced to 150 mg 1 time / day (2 capsules. 75 mg).Patients taking the drug Pradaxa. after orthopedic operations, it is not recommended to simultaneously begin the use of verapamil and connect it to therapy in the future. Prevention of stroke, systemic thromboembolism and reduction of cardiovascular mortality in patients with atrial fibrillation: dose adjustment is not required, the use of the drug is recommended in a daily dose of 300 mg (1 caps. 150 mg 2 times / day). Treatment of acute DVT and / or pulmonary embolism and prevention of deaths caused by these diseases: dose adjustment is not required. The use of the drug is recommended in a daily dose of 300 mg (1 capsule. 150 mg 2 times / day). Prevention of recurrent THV and / or pulmonary embolism and death caused by these diseases: dose adjustment is not required. The use of the drug is recommended in a daily dose of 300 mg (1 capsule. 150 mg 2 times / day). Use in patients with an increased risk of bleeding: Prevention of stroke, systemic thromboembolism and reduction of cardiovascular mortality in patients with atrial fibrillation: the presence of factors such as age 75 years or older, moderate reduction in renal function (CC 30-50 ml / min), simultaneous use of P-glycoprotein inhibitors, or a history of gastrointestinal bleeding may increase the risk of bleeding. In patients with one or more of these risk factors, at the discretion of the physician, a decrease in the daily dose of Pradaxa may be possible. up to 220 mg (1 capsule. 110 mg 2 times / day). Treatment of acute DVT and / or pulmonary embolism and prevention of deaths caused by these diseases: the presence of such factors as age 75 years or older, a moderate decrease in kidney function (CC 30-50 ml / min) or an indication of a history of gastrointestinal bleeding risk of bleeding. In patients with a single risk factor, dose adjustment is not required. For patients with multiple risk factors, clinical data are limited. In these patients, the drug should be used only in cases where the expected benefit exceeds the risk of bleeding. Prevention of recurrent THV and / or pulmonary embolism and deaths caused by these diseases: the presence of factors such as 75 years or older, a moderate decrease in kidney function (CC 30-50 ml / min) or an indication of a history of gastrointestinal bleeding bleeding.In patients with one risk factor: dose adjustment is not required. For patients with multiple risk factors, clinical data are limited. In these patients, the drug should be used only in cases where the expected benefit exceeds the risk of bleeding. The transition from the use of the drug Pradaxa. parenteral anticoagulants: Prevention of venous thromboembolism in patients after orthopedic surgeries: parenteral administration of anticoagulants should be started 24 hours after taking the last dose of Pradaxa. should begin 12 hours after taking the last dose of Pradaxa. Treatment of acute DVT and / or pulmonary embolism and prophylaxis with deaths caused by these diseases: parenteral administration of anticoagulants should be started 12 hours after taking the last dose of Pradaxa .. Prevention of recurrent DVT and / or PEAL and deaths caused by these diseases: parenteral use of anticoagulants should be started 12 hours after the last dose Pradaxa .. The transition from parenteral use of anticoagulants to the use of the drug Pradaxa.: The first dose of the drug Pradaxa. appointed instead of the canceled anticoagulant in the range of 0-2 hours before the next injection of alternative therapy, or simultaneously with the cessation of continuous infusion (for example, in / in the use of unfractionated heparin). The transition from the use of vitamin K antagonists to the use of the drug Pradaxa .: Prevention of stroke, systemic thromboembolism and reduction of cardiovascular mortality in patients with atrial fibrillation: the use of vitamin K antagonists is stopped, the use of the drug Pradaxa. possible with an MHO less than 2.0. Treatment of acute DVT and / or pulmonary embolism and prevention of deaths caused by these diseases: stop the use of vitamin K antagonists, the use of the drug Pradaxa. possible with an MHO less than 2.0. Prevention of recurrent THV and / or pulmonary embolism and deaths caused by these diseases: the use of vitamin K antagonists is stopped, the use of the drug Pradaxa. possible with an MHO less than 2.0.The transition from the use of the drug Pradaxa. for use of vitamin K antagonists: Prevention of stroke, systemic thromboembolism and reduction of cardiovascular mortality in patients with atrial fibrillation: with QA & # 8805 .50 ml / min, vitamin K antagonists may be used in 3 days, and with QA 30-50 ml / min - 2 days before discontinuation of the drug Pradaxa .. Treatment of acute DVT and / or PATE and prevention of deaths caused by these diseases: with KK & # 8805 .50 ml / min the use of vitamin K antagonists is possible for 3 days, and with KK 30 -50 ml / min - 2 days before discontinuation of the drug Pradaxa .. Prevention of re tsdiviruyuschego DVT and / or pulmonary embolism and deaths caused by these diseases: with KK & # 8805 .50 ml / min, vitamin K antagonists can be used in 3 days, and in KK 30-50 ml / min - 2 days before discontinuation of Pradaxa .. Cardioversion: Prophylaxis of stroke, systemic thromboembolism and reduction of cardiovascular mortality in patients with atrial fibrillation. Conducting planned or emergency cardioversion does not require discontinuation of Pradaxa therapy. Missed dose: Prevention of venous thromboembolism in orthopedic patients operations: it is recommended to take the usual daily dose of the drug Pradaxa. at the usual time the next day. In case of missing individual doses, you should not take a double dose of the drug. Prevention of stroke, systemic thromboembolism and reduction of cardiovascular mortality in patients with atrial fibrillation: a missed dose of Pradaxa. can be taken if 6 hours or more remains before taking the next dose, if the period is less than 6 hours, the missed dose should not be taken. In case of missing individual doses, you should not take a double dose of the drug. Treatment of acute DVT and / or pulmonary embolism and prevention of deaths caused by these diseases: missed dose of Pradaxa. can be taken if 6 hours or more remains before taking the next dose, if the period is less than 6 hours, the missed dose should not be taken. In case of missing individual doses, you should not take a double dose of the drug. Prevention of recurrent THV and / or pulmonary embolism and deaths caused by these diseases: missed dose of Pradaxa. can be taken if 6 hours or more remains before taking the next dose, if the period is less than 6 hours, the missed dose should not be taken. In case of missing individual doses, you should not take a double dose of the drug.