Xarelto pills 2.5 mg 56 pcs
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Active ingredients
Rivaroxaban
Release form
Pills
Composition
Rivaroxaban micronized 2.5 mg. Excipients: microcrystalline cellulose - 40 mg, croscarmellose sodium - 3 mg, hypromellose 5cP - 3 mg, lactose monohydrate - 27.9 mg, magnesium stearate - 600 μg, sodium lauryl sulfate - 500 μg. The composition of the shell: iron dye red oxide - 15 mcg, hypromellose 15cP - 1.5 mg, macrogol 3350 - 500 mcg, titanium dioxide - 485 mcg.
Pharmacological effect
Mechanism of action: Rivaroxaban is a highly selective direct inhibitor of factor Xa, which has high bioavailability when administered. Activation of factor X to form factor Xa through the internal and external coagulation paths plays a central role in the coagulation cascade. Pharmacodynamic effects: In humans, a dose-dependent inhibition of factor Xa was observed. Rivaroxaban has a dose-dependent effect on prothrombin time and closely correlates with plasma concentrations (r = 0.98) if the Neoplastin kit is used for the analysis. When using other reagents, the results will differ. The prothrombin time should be measured in seconds, since the MHO is calibrated and certified only for coumarin derivatives and cannot be used for other anticoagulants. In patients undergoing large orthopedic surgeries, the 5/95 percentile for the prothrombin time (Neoplastin.) 2-4 hours after taking the tablet (ie, at the maximum effect) varies from 13 to 25 seconds. Also, rivaroxaban dose-dependently increases the APTT and the result of HepTest. However, these parameters are not recommended for evaluating the pharmacodynamic effects of rivaroxaban. During treatment with rivaroxaban, monitoring of blood clotting parameters is not required. However, if there is a clinical rationale for this (for example, in case of overdose of the drug or, if necessary, emergency surgical intervention), rivaroxaban concentration can be measured using a calibrated quantitative anti-factor Xa test (for example, STA-Liquid Anti-Xa, manufacturer Diagnostics Stago CAC France or similar). In healthy men and women older than 50 years, a prolongation of the QT interval under the influence of rivaroxaban was not observed.
Indications
- prevention of venous thromboembolism (VTE) in patients undergoing large orthopedic operations on the lower limbs.
Contraindications
- hypersensitivity to rivaroxaban or any excipients contained in a tablet - clinically significant active bleeding (for example, intracranial bleeding, gastrointestinal bleeding) - damage or pathological condition associated with an increased risk of major bleeding, including existing or recent gastrointestinal ulcers, the presence of malignant neoplasms with a high risk of bleeding, recent injuries to the brain or spinal cord, recent surgical interventions on the brain, spinal cord or eyes, recent intracranial hemorrhage, diagnosed or suspected esophageal varices, arteriovenous venous malformations, vascular aneurysm or large anomalies of the structure of the vessels of the brain or spinal cord - concomitant therapy with any other anticoagulum ntami, for example, unfractionated heparin (UFH), low molecular weight heparins (including enoxaparin, dalteparin), heparin derivatives (including fondaparinux), oral anticoagulants (including warfarin, apixaban, dabigatran), except when the patient is transferred from therapy or to therapy with Xarelto, or when UFH is prescribed in low doses to maintain the patency of the central venous or arterial catheter - liver disease occurring with coagulopathy, which causes clinical and significant risk of bleeding, including patients with cirrhosis of classes B and C according to the Child-Pugh classification - pregnancy - lactation period (breastfeeding period) - children and adolescents under 18 years of age (efficacy and safety for patients of this age group have not been established) - severe renal failure with CC less than 15 ml / min (there are no clinical data on the use of rivaroxaban in patients of this category) - hereditary intolerance to lactose or galactose (for example, congenital deficiency lactase or glucose-galactose malabsorption), because the drug contains lactose. The drug should be used with caution: - in the treatment of patients with an increased risk of bleeding (includingwith congenital or acquired tendency to bleeding, uncontrolled severe arterial hypertension, gastric ulcer and duodenal ulcer in the acute stage, recently transferred gastric ulcer and duodenal ulcer, vascular retinopathy, recently transferred intracranial gastric and duodenal ulcer, vascular retinopathy, new intracranial gastric and duodenal ulcers, vascular retinopathy, new intracerebral ulcer of stomach and duodenal ulcer, vascular retinopathy, new intracerebral ulcer of stomach and duodenal ulcer, vascular retinopathy, newly transferred intracranial gastric and duodenal ulcer, vascular retinopathy; after a recent surgery on the brain, spinal cord and eyes, bronchiectasis, or a history of pulmonary hemorrhage) and treatment of patients with moderate renal insufficiency (CC 50–30 ml / min) receiving concomitant drugs that increase the concentration of rivaroxaban in the blood plasma — when treating patients with severe renal insufficiency (CC 30–15 ml / min), caution should be exercised because, due to the underlying disease, such patients are at increased risk of both bleeding and thrombus formation - rivaroxaban is not recommended for use in patients receiving systemic treatment with an antifungal drug groups of azoles (for example, ketoconazole) or HIV protease inhibitors (for example, ritonavir). These drugs are strong inhibitors of the CYP3A4 isoenzyme and P-glycoprotein. As a result, these drugs can increase the concentration of rivaroxaban in plasma to a clinically significant level (an average of 2.6 times), which increases the risk of bleeding. Fluconazole (an antifungal drug of the azoles group), a moderate CYP3A4 inhibitor, has a less pronounced effect on the removal of rivaroxaban and can be used with it simultaneously - patients with severe renal failure (CK 30–15 ml / min) or increased risk of bleeding and patients receiving concomitant systemic treatment with antifungal drugs of the azoles group or HIV protease inhibitors, after the start of treatment should be closely monitored for the timely detection of complications in the form of blood currents. Such monitoring may include regular physical examination of patients, careful observation of the surgical wound drainage and periodic changes in hemoglobin levels.Any decrease in hemoglobin or blood pressure, for which there is no explanation, is a reason to look for a bleeding site - in patients receiving drugs that affect hemostasis (eg, NSAIDs, antiplatelet agents or other antithrombotic agents) - in patients at risk of acute gastric ulcer and duodenal ulcer intestine may be justified by the appointment of prophylactic anti-ulcer treatment.
Use during pregnancy and lactation
Efficacy and safety of Xarelto. in pregnant women have not been established. The data obtained in experimental animal studies showed a pronounced toxicity of rivaroxaban for the mother's body, associated with the pharmacological action of the drug (for example, complications in the form of hemorrhages) and leading to reproductive toxicity. Due to the possible risk of bleeding and the ability to penetrate the Xarelto placental barrier. contraindicated in pregnancy. In women of childbearing age Xarelto. should be used only if effective contraceptive methods are used. Data on the use of Xarelto. for the treatment of women during lactation are absent. The data obtained in experimental animal studies show that rivaroxaban is excreted in breast milk. Xarelto. can be used only after stopping breastfeeding.
Dosage and administration
The drug is taken orally, regardless of the meal. If the patient is unable to swallow the pill whole, Xarelto pill. can be crushed and mixed with water or liquid food, such as applesauce, just before ingestion. The crushed pill Xarelto. You can enter through the gastric tube. The position of the probe in the gastrointestinal tract must be further coordinated with the doctor before taking Xarelto .. The crushed tablet should be administered through a stomach tube in a small amount of water, after which a small amount of water must be injected in order to wash off the remnants of the drug from the probe walls. Prevention of VTE with large orthopedic operations It is recommended to prescribe 10 mg (1 tab.) 1 time / day. The initial dose should be taken 6-10 hours after surgery, provided hemostasis is achieved. Duration of treatment: 5 weeks - after major surgery on the hip joint, 2 weeks - after major surgery on the knee joint.Actions in case of skipping a dose. In case of skipping a dose, the patient should immediately take the drug and the next day continue with the regular dose of 10 mg (1 tab.) / Day, as before. Separate groups of patients Dose adjustment depending on the patient's age (over 65 years), gender, body weight or ethnicity is not required. Rivaroxaban is contraindicated in patients with liver disease, accompanied by coagulopathy, which causes a clinically significant risk of bleeding. Patients with other liver diseases are not required to change the dose. The limited clinical data available in patients with moderate-degree liver failure (class B according to the Child-Pugh classification) indicate a significant increase in the pharmacological activity of the drug. For patients with severe hepatic impairment (Child-Pugh class C), there are no clinical data. When prescribing rivaroxaban in patients with mild renal insufficiency (CK 80-50 ml / min) or moderate severity (CK 50-30 ml / min), no dose reduction is required. The limited clinical data available in patients with renal insufficiency (CK 30–15 ml / min) show a significant increase in rivaroxaban concentrations in these patients. For the treatment of this category of patients rivaroxaban should be used with caution. The use of rivaroxaban is not recommended in patients with CK less than 15 ml / min. Transfer of patients from vitamin K (AVK) antagonists to Xarelto. When transferring patients from AVK to Xarelto., After taking Xarelto. MHO values will be falsely elevated. Therefore, the indicator MHO should not be used to control the anticoagulant effect of Xarelto. Transfer of patients with Xarelto. on AVK There is a possibility of insufficient anticoagulant effect when switching from Xarelto. on avk. In this regard, it is necessary to provide a continuous sufficient anticoagulant effect during a similar transition. It should be noted that Xarelto. may contribute to improving MHO. When transferring a patient from Xarelto. on AVK, both drugs should be given at the same time, until the MHO reaches & # 8805 .2. During the first two days of the transitional period, a standard dose of AVK should be used, and subsequently, be guided by the value of INR.During simultaneous use of Xarelto. and AVK MHO should be determined not earlier than 24 hours after the previous dose, but before taking the next dose of Xarelto .. After discontinuing Xarelto. the value of MHO can be reliably determined 24 hours after the last dose. Transfer of patients from parenteral anticoagulants to Xarelto. For patients receiving parenteral anticoagulants, use Xarelto. It should be started 0-2 hours before the next scheduled parenteral administration of the drug (for example, low molecular weight heparin) or at the time of termination of the continuous parenteral administration of the drug (for example, intravenous administration of unfractionated heparin). Transfer of patients with Xarelto. for parenteral anticoagulants Xarelto should be discontinued. and inject the first dose of the parenteral anticoagulant during the prescription of the next dose of Xarelto.
Side effects
Security Xarelto. evaluated in four phase III studies involving 6097 patients undergoing major orthopedic surgery on the lower extremities (total hip joint prosthetics or total knee joint prosthetics) and 3997 patients hospitalized for somatic pathology treated for a maximum of 39 days, as well as three Phase III studies of venous thromboembolism (VTE) treatment, which included 4556 patients who received Xarelto. either 15 mg 2 times / day for 3 weeks, followed by a dose of 20 mg 1 time / day, or 20 mg 1 time / day with a duration of treatment up to 21 months. In addition, the security of Xarelto. It was also evaluated in 7,750 patients with atrial fibrillation of non-valvular origin in two phase III studies receiving at least one dose of Xarelto, as well as 10,225 patients with ACS who received at least one dose of Xarelto. 2.5 mg (2 times / day) or 5 mg (2 times / day) Xarelto. in combination with either acetylsalicylic acid or acetylsalicylic acid with clopidogrel or ticlopidine. In connection with the pharmacological mechanism of action, the use of the drug Xarelto. may be accompanied by an increased risk of latent or overt bleeding from any organs and tissues, which can lead to post-hemorrhagic anemia.The risk of bleeding can be increased in such groups of patients as, for example, patients with severe uncontrolled arterial hypertension and / or taking concomitant medications that affect hemostasis. Signs, symptoms, and severity (including deaths) will vary depending on the source and the degree or severity of the bleeding and / or anemia. Hemorrhagic complications can manifest as weakness, pallor, dizziness, headache or unexplained edema, shortness of breath or shock, the development of which cannot be explained by other causes. In some cases, as a result of anemia, symptoms of myocardial ischemia, such as chest pain or angina, are observed. When using the drug Xarelto. such well-known complications secondary to severe bleeding, such as interfascial space syndrome and renal failure due to hypoperfusion, were also recorded. Thus, when assessing the condition of any patient receiving anticoagulants, the possibility of bleeding should be considered. The frequency of occurrence of NLR (undesirable drug reactions) with the use of the drug Xarelto. below. Within each group identified in frequency, adverse events are presented in order of decreasing severity. The frequency of occurrence is determined as follows: very often (& # 8805 .1 / 10), often (& # 8805 .1 / 100– <1/10), infrequently (& # 8805 .1 / 1000– <1/100), rarely (& # 8805 .1 / 10 000– <1/1000). All of the undesirable drug reactions that occurred during treatment in patients with phase III studies (cumulative data RECORD1-4, EINSTEIN-DVT (deep vein thrombosis), ROCKET AF, J-ROCKET AF, MAGELLAN, ATLAS and EINSTEIN (DVT / PE / Extension) From the side of the hemopoietic system: often - anemia (including appropriate laboratory parameters), rarely - thrombocythemia (including increased platelet count). * From the side of the cardiovascular system: often - marked reduction in blood pressure, hematoma. Infrequently - tachycardia. From the organ of view: often - hemorrhage in the head (Including bleeding in the conjunctiva) From the digestive system:. Often - bleeding gums, gastrointestinal haemorrhage (including rectal bleeding) in the digestive tract pain, dyspepsia, nausea, constipation *, diarrhea, vomiting * Infrequent - dry mouth..From the side of the liver: infrequently - abnormal liver function. rarely jaundice. From the laboratory indicators: often - increased activity of liver transaminases. infrequently - increasing the concentration of bilirubin, increasing the activity of alkaline phosphatase *, increasing the activity of LDH *, increasing the activity of lipase *, increasing the activity of amylase *, increasing the activity of GGT *. rarely, an increase in the concentration of conjugated bilirubin (with a concomitant increase in ALT activity or without it). The nervous system: often - dizziness, headache. infrequently - intracerebral and intracranial hemorrhage, short-term syncope. On the part of the urogenital system: often - bleeding from the urogenital tract (including hematuria and menorrhagia **), renal failure (including increased creatinine concentration, increased urea concentration) *. On the part of the respiratory system: often - nosebleeds, hemoptysis. On the part of the skin and subcutaneous tissue: often - itching (including infrequent cases of generalized itching), rash, ecchymosis, skin and subcutaneous hemorrhages. infrequently - urticaria. On the part of the immune system: rarely - allergic reactions, allergic dermatitis. On the part of the musculoskeletal system: often - pain in the limbs *. infrequently - hemarthrosis. rarely - hemorrhage in the muscles. On the part of the organism as a whole: often - fever *, peripheral edema, deterioration of general muscle strength and tone (including weakness, asthenia). infrequently - worsening of general well-being (including indisposition). rarely local swelling *. Other: often - bleeding after the procedure (including postoperative anemia and bleeding from a wound), excessive hematoma with bruising. infrequently - discharge from a wound *. rarely - vascular pseudoaneurysm ***. * - were registered after large orthopedic operations. ** - were recorded in the treatment of VTE as very frequent in women <55 years. *** - were recorded as infrequent in the prevention of complications of ACS (after conducting percutaneous interventions). The most frequent NLR in patients who used the drug were bleeding. The most frequent bleeding (& # 8805 .4%) was nasal bleeding (5.9%) and gastrointestinal bleeding (4.2%). Overall, 67% of patients who received at least one dose of rivaroxaban developed adverse reactions that required therapy.In approximately 22% of patients, according to the researchers, adverse reactions were associated with the use of the drug. When using the drug Xarelto. at a dose of 10 mg in patients undergoing knee or hip joint arthroplasty, as well as in patients with prolonged immobilization during hospitalization, bleeding cases were observed in approximately 6.8% and 12.6% of patients, respectively, and anemia in approximately 5.9% and 2.1% of patients, respectively . In patients taking the drug Xarelto. at a dose of 15 mg 2 times / day and a further transition to 20 mg 1 time / day for the treatment of DVT or PE, or 20 mg for the prevention of recurrence of DVT or PE, bleeding was observed in approximately 22.7% of patients, anemia occurred in approximately 2.2% of patients . In patients taking the drug for the prevention of stroke and systemic thromboembolism, the frequency of bleeding of varying severity was 28 per 100 person-years, anemia - 2.5 per 100 person-years. In patients taking the drug to prevent death due to cardiovascular causes and myocardial infarction after ACS, the frequency of bleeding of varying severity was 22 per 100 person-years, anemia was found in 1.4 per 100 person-years. During the post-registration monitoring, cases of the following adverse reactions were reported, the development of which had a temporary connection with the administration of the drug Xarelto. It is not possible to estimate the frequency of occurrence of such adverse reactions in the framework of post-registration monitoring. On the part of the immune system: angioedema, allergic edema. In phase III clinical registration studies (RCTs), such adverse reactions were regarded as infrequent (from> 1/1000 to <1/100). On the part of the liver: cholestasis, hepatitis (including hepatocellular damage). Within the framework of phase 3 RCTs, such undesirable reactions were regarded as rare (from> 1/10 000 to <1/1000). From the hemopoietic system: thrombocytopenia. Within the framework of phase 3 RCTs, such undesirable reactions were regarded as infrequent (from> 1/1000 to <1/100). On the part of the musculoskeletal system: the frequency is unknown - the syndrome of increased subfascial pressure (compartment syndrome) due to bleeding. Urinary system: the frequency is unknown - renal failure / acute renal failure due to bleeding, leading to renal hypoperfusion.
special instructions
Security Xarelto. evaluated in four phase III studies involving 6097 patients undergoing major orthopedic surgery on the lower extremities (total hip joint prosthetics or total knee joint prosthetics) and 3997 patients hospitalized for somatic pathology treated for a maximum of 39 days, as well as three Phase III studies of venous thromboembolism (VTE) treatment, which included 4556 patients who received Xarelto. either 15 mg 2 times / day for 3 weeks, followed by a dose of 20 mg 1 time / day, or 20 mg 1 time / day with a duration of treatment up to 21 months. In addition, the security of Xarelto. It was also evaluated in 7,750 patients with atrial fibrillation of non-valvular origin in two phase III studies receiving at least one dose of Xarelto, as well as 10,225 patients with ACS who received at least one dose of Xarelto. 2.5 mg (2 times / day) or 5 mg (2 times / day) Xarelto. in combination with either acetylsalicylic acid or acetylsalicylic acid with clopidogrel or ticlopidine. In connection with the pharmacological mechanism of action, the use of the drug Xarelto. may be accompanied by an increased risk of latent or overt bleeding from any organs and tissues, which can lead to post-hemorrhagic anemia. The risk of bleeding can be increased in such groups of patients as, for example, patients with severe uncontrolled arterial hypertension and / or taking concomitant medications that affect hemostasis. Signs, symptoms, and severity (including deaths) will vary depending on the source and the degree or severity of the bleeding and / or anemia. Hemorrhagic complications can manifest as weakness, pallor, dizziness, headache or unexplained edema, shortness of breath or shock, the development of which cannot be explained by other causes. In some cases, as a result of anemia, symptoms of myocardial ischemia, such as chest pain or angina, are observed. When using the drug Xarelto. such well-known complications secondary to severe bleeding, such as interfascial space syndrome and renal failure due to hypoperfusion, were also recorded.Thus, when assessing the condition of any patient receiving anticoagulants, the possibility of bleeding should be considered. The frequency of occurrence of NLR (undesirable drug reactions) with the use of the drug Xarelto. below. Within each group identified in frequency, adverse events are presented in order of decreasing severity. The frequency of occurrence is determined as follows: very often (& # 8805 .1 / 10), often (& # 8805 .1 / 100– <1/10), infrequently (& # 8805 .1 / 1000– <1/100), rarely (& # 8805 .1 / 10 000– <1/1000). All of the undesirable drug reactions that occurred during treatment in patients with phase III studies (cumulative data RECORD1-4, EINSTEIN-DVT (deep vein thrombosis), ROCKET AF, J-ROCKET AF, MAGELLAN, ATLAS and EINSTEIN (DVT / PE / Extension) From the side of the hemopoietic system: often - anemia (including appropriate laboratory parameters), rarely - thrombocythemia (including increased platelet count). * From the side of the cardiovascular system: often - marked reduction in blood pressure, hematoma. Infrequently - tachycardia. From the organ of view: often - hemorrhage in the head (including conjunctival bleeding). From the digestive system: often - bleeding gums, gastrointestinal bleeding (including rectal bleeding), pain in the gastrointestinal tract, dyspepsia, nausea, constipation *, diarrhea, vomiting *. Infrequently - dry mouth. On the part of the liver: infrequently - impaired liver function, rarely - jaundice On the part of laboratory parameters: often - an increase in the activity of hepatic transaminases. infrequently - increasing the concentration of bilirubin, increasing the activity of alkaline phosphatase *, increasing the activity of LDH *, increasing the activity of lipase *, increasing the activity of amylase *, increasing the activity of GGT *. rarely, an increase in the concentration of conjugated bilirubin (with a concomitant increase in ALT activity or without it). The nervous system: often - dizziness, headache. infrequently - intracerebral and intracranial hemorrhage, short-term syncope. On the part of the urogenital system: often - bleeding from the urogenital tract (including hematuria and menorrhagia **), renal failure (including increased creatinine concentration, increased urea concentration) *. On the part of the respiratory system: often - nosebleeds, hemoptysis. On the part of the skin and subcutaneous tissue: often - itching (including infrequent cases of generalized itching), rash, ecchymosis, skin and subcutaneous hemorrhages. infrequently - urticaria. On the part of the immune system: rarely - allergic reactions, allergic dermatitis.On the part of the musculoskeletal system: often - pain in the limbs *. infrequently - hemarthrosis. rarely - hemorrhage in the muscles. On the part of the organism as a whole: often - fever *, peripheral edema, deterioration of general muscle strength and tone (including weakness, asthenia). infrequently - worsening of general well-being (including indisposition). rarely local swelling *. Other: often - bleeding after the procedure (including postoperative anemia and bleeding from a wound), excessive hematoma with bruising. infrequently - discharge from a wound *. rarely - vascular pseudoaneurysm ***. * - were registered after large orthopedic operations. ** - were recorded in the treatment of VTE as very frequent in women <55 years. *** - were recorded as infrequent in the prevention of complications of ACS (after conducting percutaneous interventions). The most frequent NLR in patients who used the drug were bleeding. The most frequent bleeding (& # 8805 .4%) was nasal bleeding (5.9%) and gastrointestinal bleeding (4.2%). Overall, 67% of patients who received at least one dose of rivaroxaban developed adverse reactions that required therapy. In approximately 22% of patients, according to the researchers, adverse reactions were associated with the use of the drug. When using the drug Xarelto. at a dose of 10 mg in patients undergoing knee or hip joint arthroplasty, as well as in patients with prolonged immobilization during hospitalization, bleeding cases were observed in approximately 6.8% and 12.6% of patients, respectively, and anemia in approximately 5.9% and 2.1% of patients, respectively . In patients taking the drug Xarelto. at a dose of 15 mg 2 times / day and a further transition to 20 mg 1 time / day for the treatment of DVT or PE, or 20 mg for the prevention of recurrence of DVT or PE, bleeding was observed in approximately 22.7% of patients, anemia occurred in approximately 2.2% of patients . In patients taking the drug for the prevention of stroke and systemic thromboembolism, the frequency of bleeding of varying severity was 28 per 100 person-years, anemia - 2.5 per 100 person-years. In patients taking the drug to prevent death due to cardiovascular causes and myocardial infarction after ACS, the frequency of bleeding of varying severity was 22 per 100 person-years, anemia was found in 1.4 per 100 person-years.During the post-registration monitoring, cases of the following adverse reactions were reported, the development of which had a temporary connection with the administration of the drug Xarelto. It is not possible to estimate the frequency of occurrence of such adverse reactions in the framework of post-registration monitoring. On the part of the immune system: angioedema, allergic edema. In phase III clinical registration studies (RCTs), such adverse reactions were regarded as infrequent (from> 1/1000 to <1/100). On the part of the liver: cholestasis, hepatitis (including hepatocellular damage). Within the framework of phase 3 RCTs, such undesirable reactions were regarded as rare (from> 1/10 000 to <1/1000). From the hemopoietic system: thrombocytopenia. Within the framework of phase 3 RCTs, such undesirable reactions were regarded as infrequent (from> 1/1000 to <1/100). On the part of the musculoskeletal system: the frequency is unknown - the syndrome of increased subfascial pressure (compartment syndrome) due to bleeding. Urinary system: the frequency is unknown - renal failure / acute renal failure due to bleeding, leading to renal hypoperfusion.