Xarelto - instructions for use, reviews, analogs and formulations (tablets 2.5 mg, 10 mg, 15 mg and 20 mg) of the drug for the treatment of thrombosis, embolism and prevention of stroke and heart attack in adults, children and pregnancy. Composition
In this article, you can read the instructions for using the drug Xarelto. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Xarelta in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Xarelta in the presence of existing structural analogues. Use for treatment of thrombosis, embolism and prevention of stroke and heart attack in adults, children, as well as during pregnancy and lactation. Composition of the preparation.
Xarelto - selective direct inhibitor of factor 10a for oral administration. Activation of factor 10 with the formation of factor 10a through its own and external pathways plays a central role in the coagulation cascade.
Rivaroxaban (the active substance of the drug Xarelto) has a dose-dependent effect on prothrombin time and is characterized by a high correlation with the concentration in the blood plasma when analyzed with the Neoplastin kit (other results will differ if other reagents are used).
Also, Rivaroxaban dose-dependently increases the APTT and the Heptest result, but these parameters are not recommended for evaluating the pharmacodynamic effects of rivaroxaban.
Composition
Rivaroxaban (micronized) + excipients.
Pharmacokinetics
After oral administration at a dose of 10 mg, Xarelto is rapidly absorbed, the absolute bioavailability is high and is 80-100%. The intake of food does not affect the AUC and Cmax of rivaroxaban. The pharmacokinetics of rivaroxaban are characterized by moderate variability; Individual variability (coefficient of variability) is 30-40%, except for the day and the next day after the operation, when the variability is high (70%).The binding with plasma proteins, mainly with albumin, is 92-95%. Rivaroxaban is excreted mainly in the form of metabolites (approximately 2/3 of the dose), half of them excreted by the kidneys, and the other half with the feces. 1/3 of the applied dose is directly excreted by the kidneys in the form of unchanged substance, it is believed, mainly through active renal secretion. The metabolism of rivaroxaban occurs with the participation of CYP3A4 and CYP2J2 isoenzymes, as well as enzymes independent of the cytochrome P450 system. The main participants in the biotransformation are a morpholino group undergoing oxidative decomposition, and amide groups undergoing hydrolysis.
Indications
- prevention of stroke, heart attack and systemic thromboembolism in patients with non-valvular atrial fibrillation;
- treatment of deep vein thrombosis and thromboembolism of the pulmonary artery and prevention of their recurrence;
- prevention of venous thromboembolism in patients undergoing extensive orthopedic surgery on the lower limbs.
Forms of release
Tablets coated with 2.5 mg, 10 mg, 15 mg and 20 mg.
Instructions for use and reception scheme
Inside, with food.
If the patient is not able to swallow the whole tablet, the Xarelto tablet can be ground and mixed with water or liquid food, such as apple puree, just before taking. After taking a crushed tablet Xarelto 15 or 20 mg, you must immediately take food.
A crushed Xarelto tablet can be injected through a gastric tube. The position of the probe in the digestive tract must be agreed with the doctor in advance before taking Xarelto. The ground tablet should be injected through a gastric tube in a small amount of water, after which a small amount of water must be introduced in order to wash off the drug residues from the probe walls. After taking a crushed Xarelto tablet, 15 or 20 mg, it is necessary to immediately receive enteral feeding.
Prevention of stroke and systemic thromboembolism in patients with non-valvular atrial fibrillation
The recommended dose is 20 mg 1 time per day.
For patients with impaired renal function (Cl creatinine 49-30 ml / min), the recommended dose is 15 mg 1 time per day.
The recommended maximum daily dose is 20 mg.
Duration of treatment
Xarelto therapy should be considered as a long-term treatment, until the benefits of treatment exceed the risk of possible complications.
Actions when skipping the dose
If the next dose is missed, the patient should immediately take Xarelto and on the next day continue to take the medication regularly according to the recommended regimen. Do not double the dose taken to compensate for missed earlier.
Side effect
- anemia;
- thrombocythemia;
- post-procedural hemorrhage (including postoperative anemia and bleeding from the wound);
- tachycardia;
- arterial hypotension (including hypotension during procedures);
- hemorrhage (including hematomas and rare cases of hemorrhage in the muscles);
- gastrointestinal hemorrhages (including hememesis, bleeding gums, bleeding from the rectum, hematuria, spotting from the genital tract, nosebleeds);
- nausea, vomiting;
- constipation, diarrhea;
- pain in the abdominal cavity;
- a feeling of discomfort in the stomach;
- dyspeptic phenomena;
- dry mouth;
- localized or peripheral edema;
- fatigue;
- weakness;
- asthenia;
- fever;
- urticaria (including cases of generalized urticaria);
- allergic dermatitis;
- dizziness;
- headache;
- syncopal states;
- pain in the limbs;
- itching (including cases of generalized itching);
- rashes on the skin;
- kidney failure (increase in blood levels of creatinine, urea);
- increased LDH levels, increased levels of AAT and AAT, increased levels of lipase, amylase, bilirubin, and the level of alkaline phosphatase.
Contraindications
- clinically significant active bleeding (eg, intracranial, gastrointestinal);
- liver diseases accompanied by coagulopathy, which increases the risk of clinically significant bleeding;
- pregnancy;
- hypersensitivity to rivaroxaban.
Application in pregnancy and lactation
Contraindicated in pregnancy.
special instructions
It is not recommended to use rivaroxaban in patients with severe renal insufficiency (CC less than 15 ml / min).
Caution should be applied Xarelto in the treatment of patients with moderate renal insufficiency (KK 30-49 ml / min),receiving concomitant therapy with drugs that can cause an increase in the concentration of rivaroxaban in blood plasma, as well as in patients with QC less than 15-30 ml / min. In patients with severe renal insufficiency, the concentration of rivaroxaban in the blood plasma can be significantly increased, which can lead to an increased risk of bleeding.
Patients with severe renal insufficiency with an increased risk of bleeding and patients receiving concomitant systemic therapy with antifungal azole agents or HIV protease inhibitors should be closely monitored after the initiation of treatment to detect hemorrhagic complications in a timely manner. Such control may include regular physical examination of the patient, careful observation of the surgical wound to be separated from the drainage, and periodic determination of the hemoglobin level.
Caution should be used rivaroxaban in the treatment of patients with an increased risk of bleeding, incl. if there are congenital or acquired diseases that lead to bleeding; uncontrolled AH severedegree; Gavage peptic ulcer in the acute stage; recently suffered peptic ulcer of the gastrointestinal tract; cardiovascular retinopathy; recent intracranial or intracerebral haemorrhage; intraspinal or intracerebral vascular pathology; the recently transferred neurosurgical (operation on the head, spinal cord) or ophthalmologic intervention.
Care should be taken when administering rivaroxaban to patients receiving drugs that affect hemostasis, for example, non-steroidal anti-inflammatory drugs (NSAIDs), platelet aggregation inhibitors or other antithrombotic agents.
Drug Interactions
With simultaneous application of rivaroxaban and strong inhibitors of the isoenzyme CYP3A4 and P-glycoprotein may lead to a decrease in renal and hepatic clearance and thus significantly increase the AUC of rivaroxaban.
The combined use of rivaroxaban and the azole Ketoconazole antifungal agent (400 mg once daily), a potent inhibitor of CYP3A4 and P-glycoprotein, resulted in a 2.6-fold increase in the mean equilibrium AUC of rivaroxaban and a 1.7-fold increase in mean Cmax of rivaroxaban,which is accompanied by a significant increase in the pharmacodynamic effects of the drug.
With the simultaneous use of rivaroxaban and the HIV protease inhibitor ritonavir (600 mg twice daily), which is a potent inhibitor of CYP3A4 and P-glycoprotein, resulted in a 2.5-fold increase in the mean equilibrium AUC of rivaroxaban and a 1.6-fold increase in mean Cmax of rivaroxaban, increased pharmacodynamic effects of the drug. In this regard, it is necessary to use with caution Xarelto in the treatment of patients simultaneously receiving systemic azole antifungal drugs or HIV protease inhibitors.
Clarithromycin (500 mg twice daily), a potent inhibitor of CYP3A4 and medium intensity inhibitor of the P-glycoprotein, caused a 1.5-fold increase in the mean AUC and a 1.4-fold increase in Cmax of rivaroxaban. This increase in AUC and an increase in Cmax varies within the norm and is considered clinically insignificant.
Erythromycin (500 mg 3 times a day), moderately inhibiting the isoenzyme CYP 3A4 and P-glycoprotein, caused a 1.3-fold increase in the mean equilibrium values of AUC and Cmax of rivaroxaban. This increase in AUC and an increase in Cmax varies within the norm and is considered clinically significant.
The simultaneous administration of rivaroxaban and rifampicin, which is a potent inducer of CYP 3A4 and P-glycoprotein, resulted in approximately a 50% decrease in the average AUC of rivaroxaban and a parallel decrease in its pharmacodynamic effects. The combined use of rivaroxaban with other potent inducers of CYP3A4 (eg, phenytoin, carbamazepine, Phenobarbital or St. John's wort) can also lead to a decrease in rivaroxaban concentrations in the blood plasma. Reducing the concentration of rivaroxaban in blood plasma is clinically insignificant.
After the combined use of enoxaparin (in a single dose of 40 mg) and rivaroxaban (in a single dose of 10 mg), an additive effect was observed with respect to the activity of the antifactor 10a, which is not accompanied by additional effects on the coagulation parameters (prothrombin time, APTT).
Enoxaparin did not alter the pharmacokinetics of rivaroxaban.
There was no pharmacokinetic interaction between Xarelto and Clopidogrel (300 mg shock dose with the subsequent administration of a maintenance dose of 75 mg), but in a subgroup of patients, a clinically significant increase in bleeding time,which did not correlate with platelet aggregation and the level of P-selectin or GP2b / 3a receptor.
After the simultaneous administration of rivaroxaban and 500 mg of naproxen, no clinically relevant prolongation of bleeding time was observed. However, in individuals, a more pronounced pharmacodynamic response is possible.
Interaction with food: rivaroxaban in a dose of 10 mg can be taken during meals or separately.
Influence on laboratory tests: the effect on blood coagulation indices (prothrombin time, APTT, Heptest) corresponds to what is expected given the mechanism of action of rivaroxaban.
Analogues of the drug Xarelto
Xarelto does not have a structural analogue for the active ingredient. The drug contains a unique active ingredient in its composition.
Analogues on the pharmacological group (agents for the treatment of thrombosis and embolism):
- Aveliesin Brown;
- Agrenoks;
- Actylase;
- Angiovitis;
- Aspizol;
- Aspirin Cardio;
- Acenocoumarol;
- Acetylsalicylic acid;
- Brilint;
- Bufferin;
- Warfarin Nycomed;
- Vinpocetine;
- Wobenzym;
- Heparin;
- Godasal;
- Dextran;
- Detromb;
- Dipyridamole;
- Zilt;
- Calciparin;
- Cardiomagnet;
- Carinate;
- Karinat Forte;
- Clexan;
- Cleaver;
- Clopidex;
- Collorite;
- Complymine;
- Coplawix;
- Xantinol nicotinate;
- Courantil;
- Lapal;
- Listab;
- Myristin;
- Parsedil;
- Pelentan;
- Pentoxifylline;
- Plavix;
- Plagril;
- Plolid;
- Pradax;
- Ralofect;
- Reogluman;
- Reopoliglyukin;
- Ribasan forte;
- Cincumar;
- Streptase;
- Tagren;
- Tyclid;
- Ticlo;
- Trombo ACC;
- Thrombopol;
- Troparin;
- Ukidan;
- Urokinase medak;
- Phenylin;
- Fibrinolysin;
- Phlogenzyme;
- Cibor;
- Egitromb.
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