Xarelto (Rivaroxaban) tablets

Composition 

In 1 tablet contains: rivaroxaban micronized 2.5 – 20 mg 

Packaging 

14 – 100 PCs

Pharmacological action

Xarelto is the anticoagulant of direct action. Rivaroxaban is a highly selective direct inhibitor of factor XA with a high oral bioavailability. 

The activation of factor X with the formation of factor XA via internal and external paths clotting plays a Central role in the coagulation cascade. 

The man was observed a dose-dependent inhibition of factor XA. Rivaroxaban has a dose-dependent effect on prothrombin time and closely correlated with the concentrations in plasma (r=0/98), if used for the analysis of a set Neoplastin . When using other reagents results will vary. Prothrombin time should be measured in seconds, since MHO is calibrated and certified only for coumarin derivatives and may not apply to other anticoagulants. Patients undergoing large orthopaedic surgery, the 5/95-percentile for prothrombin time (Neoplastin) 2-4 hours after taking the pill (i.e. maximum effect) vary from 13 to 25 seconds. Also rivaroxaban dose-dependent increases APTT and HepTest result, however, these options are not recommended to assess the pharmacodynamic effects of rivaroxaban. Rivaroxaban also affects the activity of anti-XA factor, however, the standards for calibration do not exist. 

During the period of treatment with rivaroxaban to monitor the parameters of blood coagulation is not required. 

In healthy men and women older than 50 years, the prolonged QT interval is influenced by rivaroxaban were observed.

Testimony

Prevention of venous thromboembolism (VTE) in patients undergoing big orthopedic surgical interventions on the lower extremities.

Contraindications

Clinically significant active bleeding, such as: 

Intracranial bleeding. 

Gastrointestinal bleeding. 

Diseases of the liver, flowing with the blood clotting disorder, which causes clinically significant risk of bleeding. 

Pregnancy. 

Lactation (breastfeeding). 

Childhood and adolescence till 18 years (efficiency and safety for patients in this age group have not been established). 

Hypersensitivity to rivaroxaban or any subsidiary, the substances contained in the tablet. 

The use of rivaroxaban has not been studied in clinical trials for surgical interventions in patients for a fracture of the femur. Therefore, the use of rivaroxaban is not recommended for these patients. 

Clinical data on the use of rivaroxaban in patients with renal failure, severe (CC< 15ml/min) are absent. Therefore, the use of rivaroxaban is not recommended for these patients.

Method of application and doses

For the prevention of VTE in large orthopedic surgery

Appoint 1 tablet (10 mg) 1 times/day. 

Duration of treatment: 5 weeks after major surgery on the hip, 2 weeks after major surgery on the knee joint. 

Rivaroxaban can be taken with or without food. 

The initial dose should be taken 6-10 hours after surgery provided that hemostasis achieved. 

In the case of missing dose, the patient should take rivaroxaban immediately and the next day to continue treatment for 1 tablets/day, as previously. 

Correction of the dose depending on the age of the patient (older 65 years), sex, body weight, or ethnic group is not required. 

With liver disease

Rivaroxaban is contraindicated in patients with liver diseases involving coagulopathy, which causes a clinically significant risk of bleeding. Patients with other liver changes dose is not required. The limited available clinical data obtained in patients with moderate hepatic impairment (class b child-Pugh), indicate a significant strengthening of pharmacological activity of the drug. For patients with severe liver failure (class C classification for child-Pugh) clinical data is lacking. 

If you have kidney disease

In the appointment of rivaroxaban in patients with renal failure light (QC 80-50 ml/min) or moderate (ck<,50-30 ml/min) the severity of the dose reduction is not required.

Side effects

On the part of the blood: often – anemia (including respective laboratory parameters), rare – thrombocythemia (including elevated levels of platelets). 

From the side of cardiovascular system: rarely – tachycardia, hypotension (including blood pressure reduction, hypotension during the procedure). 

From the digestive system: often – nausea , increased activity of GGT , transaminases (including ALT , ACT). Rarely, constipation, diarrhea, abdominal pain (including pain in the upper abdomen, discomfort in the stomach), dyspepsia (including epigastric discomfort), dry mouth, vomiting, increased activity of lipase, amylase, LDH, alkaline phosphatase, increased concentrations of bilirubin . Rarely – infringements of function of a liver, an increased concentration of conjugated bilirubin (with concomitant increased ALT or not). 

CNS: rarely – dizziness, headache, brief loss of consciousness (including syncope). 

From the urinary system: rarely – renal failure (including increased creatinine concentration , increasing the concentration of urea ). 

From the blood coagulation system: often – bleeding after the procedure (including the postoperative anemia and bleeding from wounds). Rarely, hemorrhage (including hematoma, and rare cases of hemorrhage into muscles), bleeding from the gastrointestinal tract (including bleeding from the gums, rectum, bloody vomit), hematuria (including microhematuria) hemorrhage from the genital tract (including menorrhagia), epistaxis. 

From the body as a whole: rarely, local swelling, malaise (including fatigue, General weakness), fever, peripheral edema. 

Allergic reactions: infrequently – itching (including rare cases of generalised pruritus), rash, urticaria (including rare cases of generalised urticaria). Rarely – allergic dermatitis. 

Other: infrequently – post-traumatic hematoma, discharge from wounds, pain in the limbs. 

In other clinical studies of rivaroxaban 

Described isolated cases of hemorrhage in the adrenal glands and the conjunctiva, and also bleeding from ulcers of the gastrointestinal tract with a fatal outcome. 

In rare cases, jaundice and hypersensitivity. 

Rarely, hemoptysis. 

Described isolated intracranial bleeding, especially in patients with arterial hypertension and/or host related antihemostatic drugs which in single cases may be potentially life-threatening.

Overdose

Symptoms: overdose of rivaroxaban may lead to haemorrhagic complications due to pharmacodynamic properties of the drug. The specific antidote of rivaroxaban is unknown. 

Leoncie: in case of overdose to decrease absorption of rivaroxaban can be used activated carbon. Administration of activated charcoal within 8 hours after the overdose allows you to reduce the absorption of rivaroxaban.

Storage conditions

Keep at temperature not exceeding 30°C.