Xarelto refers to anticoagulants of direct action.
This group of drugs, promotes suppression of blood clotting activity and prevents thrombogenesis, due to the reduced formation of fibrin.
They affect the biosynthesis of certain elements of the body, allowing to change the viscosity of the blood, which leads to the inhibition of coagulation processes. Anticoagulant Xarelto is allowed to be used with both therapeutic and prophylactic purposes.
Clinical and pharmacological group
Anticoagulant direct action.
Conditions of leave from pharmacies
It is released on prescription.
How much does Xarelto cost? The average price in pharmacies is at the level of1 500 rubles.
Form of issue and composition
"Xarelto" comes in the form of tablets, covered with a special soluble film shell with a pink-brown or red-brown shell. They are round and have biconvex faces with engraving. On their fracture, a homogeneous white mass is visible, which is surrounded by a colored dissolvable shell.
- The tablet of the preparation contains: rivaroxaban micronized in an amount of 10, 15 or 20 mg, and auxiliary components: cellulose microcrystalline, croscarmellose sodium, hypromellose 5cP, lactose monohydrate, magnesium stearate and sodium lauryl sulfate.
- The film coating of the tablet coating consists of: iron dye red oxide, hypromellose 15cP, titanium dioxide and macrogol 3350.
On sale are offered packages from 5 to 100 pieces.
For the active substance of this drug - rivaroxaban, characterized by rapid effects, predictable dose-response and high bioavailability. It does not require monitoring of coagulation parameters, there is practically no risk of incompatibility with other food products or drugs.
Xarelto is used as a prophylactic against stroke in patients suffering from atrial fibrillation, while demonstrating good efficacy and tolerability. This anticoagulant can be taken once a day, observing a fixed dose.
Rivaroxaban has a high absolute bioavailability of 80-100%. The main component is rapidly absorbed with the onset of maximum concentration after 2-4 hours. Getting into the body, there is a significant connection of the main part of rivaroxaban with the proteins of the blood plasma, namely plasma albumin. Excretion of the drug is carried out mainly in the form of metabolites.
Indications for use
Prophylactic agent for venous thromboembolism in people who underwent significant surgical interventions on the lower extremities. For orthopedic interventions, 10 mg tablets are recommended.
- Xarelto for 15 and 20 mg is used as a preventive agent for atrial fibrillation of non-valvular origin. In this case, the drug helps to prevent systemic thromboembolism and stroke.
The drug is used to treat deep vein thrombosis and pulmonary embolism and as a preventive measure to prevent recurrence of PE and DVT.
General contraindications for Xarelto tablets:
- Children and adolescence under 18;
- The period of breastfeeding;
- Hypersensitivity to the components of the drug;
- Diseases of the liver that occur with coagulopathy, which causes a clinically significant risk of bleeding;
- Severe renal insufficiency (creatinine clearance less than 15 ml / min);
- Clinically significant active bleeding (eg, intracranial and gastrointestinal);
- Congenital lactase deficiency, glucose-galactose malabsorption, lactose intolerance;
- Concomitant treatment with any other anticoagulants, for example, oral anticoagulants (dabigatran, warfarin, apixaban), low molecular weight heparins (dalteparin, enoxaparin), unfractionated heparin (UFH), heparin derivatives (fondaparinux); Exceptions are cases where the patient is transferred from therapy or on Xarelto therapy, or when UFH is administered at low doses to maintain the permeability of the central venous or arterial catheter.
Contraindications to the use of tablets, depending on the amount of active ingredient contained in them:
- "2.5": treatment of acute coronary syndrome by means of antiaggregants in patients who underwent transient ischemic attack or stroke;
- "10", "15" and "20": damage or condition that increases the risk of developing large bleeding (eg, aneurysm or pathology of the vessels of the spinal cord or brain, surgery on the eyes, brain or spinal cord, arteriovenous malformations, recent traumas of the brain or spinal cord, intracranial hemorrhage, presumed or diagnosed varicose veins of the esophagus, the presence of malignant tumors with a high risk of bleeding, a recent transferred or existing gastrointestinal ulcer);
- "10": cases when surgery for a fracture of the femur is indicated.
The states / diseases in which Xarelto tablets are administered with caution:
- Simultaneous use with drugs that affect hemostasis;
- Renal failure of severe degree (creatinine clearance 15-29 ml / min), in connection with the possibility of increasing the concentration of rivaroxaban in blood plasma;
- Systemic therapy with antifungal azole agents or human immunodeficiency virus protease inhibitors, with the exception of fluconazole;
- Renal failure of moderate severity (creatinine clearance 30-49 ml / min), in which patients receive drugs that increase the concentration of rivaroxaban in blood plasma;
- Increased risk of bleeding: including bronchiectasis or pulmonary hemorrhage in an anamnesis, congenital or acquired tendency to bleeding, peptic ulcer and duodenal ulcer guts in the acute phase, recently transferred acute stomach and duodenum ulcer, vascular retinopathy, uncontrolled severe arterial hypertension, vascular pathology spinal cord or brain, recent intracerebral or intracranial hemorrhage, after a recent surgery on the eyes, brain or spinal cord).
Use in pregnancy and lactation
Studies related to the safety and efficacy of the Xarelto drug during pregnancy have been conducted on animals. As a result, the toxic effect of rivaroxaban on the future mother and child was found. The drug is contraindicated in pregnancy due to a high risk of penetration of the active substance through the placenta and the possibility of bleeding. Women who are in childbearing age are only allowed medication when using contraception.
The results of studies of the possibility of taking Xarelto in breastfeeding, conducted on animals, showed that the active substance is excreted with milk. Experiments have shown that when feeding toxic substances can enter the child's body. Starting Xarelto is only allowed after the end of the lactation period.
Dosage and route of administration
In the instructions for use indicated: Xarelto tablets of 10 milligrams are taken regardless of meals, 15 and 20 milligrams - at meals.
After large operations on the knee joint, the duration of treatment is two weeks, after large operations on the hip joint - five weeks. The initial dose is taken six to ten hours after surgery, if hemostasis is reached. The therapeutic dose is one tablet per day.
If you miss a dose, you should immediately take Xarelto tablet and continue to take the drug on the next day, respectively, with recommendations. To compensate for the missed dose, double the dose taken is prohibited.
During the course of drug therapy in patients with hypersensitivity to Rivaroxaban, the following side effects were observed:
- Hemoptysis, frequent nasal bleeding;
- Peripheral edema;
- General weakness, malaise;
- Possible hemorrhages in the eyeball;
- Violation of the function of the liver, the development of jaundice;
- Increase in the level of hepatic transaminase activity;
- Increased bilirubin concentration;
- Allergic reactions of the skin - itching, hives, rashes, hemorrhages under the skin;
- From the hemopoietic system - the development of iron deficiency anemia, thrombocytopenia;
- Headaches, faintness, dizziness, hemorrhage into the brain substance;
- From the heart and blood vessels - lowering blood pressure, bruising and bruising under the skin, in rare cases, tachycardia;
- On the part of the digestive tract - dyspepsia, flatulence, nausea, dry mouth, bleeding gums, exacerbation of chronic diseases of the digestive canal, the risk of developing gastrointestinal bleeding.
When an overdose of the drug development of bleeding or other adverse reactions has not been reported. With an excessive dose (from 50 mg and above), a limited absorption of the drug is possible, leading to plateau concentrations without further increase in the average concentration of rivaroxaban in plasma.
To eliminate the symptoms of overdose it is recommended to take activated charcoal (hemodalysis is not effective). Then, if necessary, should be symptomatic treatment. There is no specific antidote.
If bleeding occurs, it is necessary to postpone the next dose of the drug or cancel the treatment for 5 to 13 hours. Treatment is selected individually, depending on the severity and localization of bleeding. If bleeding can not be eliminated, specific procoagulant preparations of the reverse action (concentrate prothrombin complex, concentrate of activated prothrombin complex or recombinant factor VIIa).
In the process of using the drug, it is important to regularly monitor the parameters of the blood coagulation system.
In general, Xarelto does not affect the ability to drive. In extremely rare cases, undesirable reactions are noted in the form of impaired attention and general malaise, which requires caution.
In elderly patients, the risk of bleeding increases with the use of Xarelto. Therefore, a careful dose selection is required.
Before performing surgical operations, the use of the drug is important to cancel at least one day before the beginning of the drug.
It is necessary to refrain from the joint use of rivaroxaban and dronedarone, since there is no clinical data on this combination.
It was found that Clarithromycin, Erythromycin and Fluconazole may lead to different changes in the concentration of rivaroxaban, but this is considered the order of normal variability and is clinically insignificant.
Simultaneous use of Xarelto with the strongest inhibitors of the isoenzyme CYP3A4 and P-gp can cause a decrease in renal and hepatic clearance, which leads to a significant increase in the systemic effect and pharmacodynamic effect of the drug.
The use of Xarelto and rifampicin, which refers to the strong inducers of CYP3A4 and P-gp, leads to a decrease in the pharmacodynamic effects of the drug. Therefore, treatment with this drug with other strong inducers should be done with caution.
We picked up some feedback from people who took Xarelto:
- Andrei. I use the drug for just over 2 years, with a dosage of 20 mg per day. Diagnosis of "atrial fibrillation and flutter". I can talk about the effectiveness of the drug, complications did not arise.
- Albina. Xarelto is an effective drug and is definitely safer than, for example, Warfarin. Works well for the prevention of thrombosis, as well as for atrial fibrillation. The medicine is excellent, only one minus is a high price.
- Inna. After surgery on the legs (the suture hurts), the doctor made this appointment: Xarelto, Reopoliglyukin (before lunch and in the evening, after dinner) and other means in different forms of release (droppers, pills). I note that Xarelto helps well to prevent the formation of blood clots in the vessels, especially after surgical interventions. Thanks to taking the drug, the postoperative period passed quickly and without complications.
- Katerina. I was given a serious diagnosis - thrombosis of LEL, iliac and deep veins of lower extremities. As an anticoagulant (a drug that thin the blood) was appointed "Xarelto", took it for 3.5 months. During this time, no side effects were found. However, refusing to take this medication forced his price and my desire to breastfeed. Pros: no side effects, ease of administration, no need to maintain a constant control of blood coagulability. Cons: price, contraindicated in breastfeeding.
Xarelto is an original drug that has no analogues of Russian or foreign in composition. If the doctor has appointed this drug, it is not recommended to replace it, since it is almost impossible to find an equivalent replacement.
Russian or imported analogues of Xarelto are such drugs:
- Aspekard - is much cheaper;
- Acetylsalicylic acid (analogous to cheap);
Before using analogues, consult your doctor.
Storage conditions and shelf life
Tablets should be kept away from children at a temperature of not more than 30 degrees. Shelf life is 3 years from the date of manufacture, indicated on the package. Do not use the drug after the expiration date.
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