366789-02-8

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• Description

  Rivaroxaban(366789-02-8) is a pure (S)-enantiomer. It is an odorless, non-hygroscopic, white to yellowish powder. Rivaroxaban is only slightly soluble in organic solvents (e.g., acetone, polyethylene glycol 400) and is practically insoluble in water and aqueous media.
  Rivaroxaban, a FXa inhibitor, is the active ingredient in XARELTO Tablets. XARELTO  a kind of orally anticoagulant drug which is used for the prevention of blood clots. Rivaroxaban takes effect through competitively inhibiting free and clot bound factor Xa, which is needed to activate prothrombin (factor II) to thrombin (factor IIa). The later is a serine protease that is required to activate fibrinogen to fibrin, which is the loose meshwork that completes the clotting process.
  
  Each XARELTO tablet contains 10 mg, 15 mg, or 20 mg of rivaroxaban. The inactive ingredients of XARELTO are: croscarmellose sodium, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and sodium lauryl sulfate. Additionally, the proprietary film coating mixture used for XARELTO 10 mg tablets is Opadry(R) Pink and for XARELTO 15 mg tablets is Opadry(R) Red, both containing ferric oxide red, hypromellose, polyethylene glycol 3350, and titanium dioxide, and for XARELTO 20 mg tablets is Opadry(R) II Dark Red, containing ferric oxide red, polyethylene glycol 3350, polyvinyl alcohol (partially hydrolyzed), talc, and titanium dioxide. ;

• Indications and Usage

  Rivaroxaban(366789-02-8) is an antithrombotic drug and was developed in a collaboration between the German Bayer Pharmaceuticals and American Johnson company. It is different from the traditional antithrombotic drug heparin in that Rivaroxaban does not need the participation of antithrombin III and can directly antagonize free and bound Xa factors. Heparin requires the effects of antithrombin III, and has no effect on Xa factors in the prothrombin complex. Rivaroxaban is the first oral direct Xa factor inhibitor in the whole world, and it can selectively and competitively inhibit free and bound Da factors as well as prothrombin activity. It uses a dose-dependent method to extend the partial thromboplastin time (PTT) and activated partial thromboplastin time (aPTT) to extend clotting time and lower thrombin genesis. Rivaroxaban has the characteristics of high bioavailability, wide range of target diseases, stable dose-effect relationship, easy oral intake, and low bleeding risk.
  Rivaroxaban can also prevent and treat venous thrombosis. It is mainly used clinically to prevent deep venous thrombosis (DVT) and pulmonary embolism (PE) in adult patients following hip and knee replacement surgery. It is also used to prevent patients with nonvalvular atrial fibrillation from cerebral apoplexy and noncentral nervous system embolism, and it can lower the recurrence risk of coronary syndromes. ;

• Mechanism of Action

  Rivaroxaban(366789-02-8) is a selective inhibitor of FXa. It does not require a cofactor (such as Anti-thrombin III) for activity. Rivaroxaban inhibits free FXa and prothrombinase activity. Rivaroxaban has no direct effect on platelet aggregation, but indirectly inhibits platelet aggregation induced by thrombin. By inhibiting FXa, rivaroxaban decreases thrombin generation. ;

• What is XARELTO？

  XARELTO (Rivaroxaban,366789-02-8) is a prescription medicine used to:
  1. reduce the risk of stroke and blood clots in people who have a medical condition called atrial fibrillation. With atrial fibrillation, part of the heart does not beat the way it should. This can lead to the formation of blood clots, which can travel to the brain, causing a stroke, or to other parts of the body.
  2. treat blood clots in the veins of your legs (deep vein thrombosis) or lungs (pulmonary embolism) and reduce the risk of them occurring again
  3. reduce the risk of forming a blood clot in the legs and lungs of people who have just had hip or knee replacement surgery It is not known if XARELTO is safe and effective in children.
  4. It is not known if XARELTO is safe and effective in children.
  ;

• Uses

  Rivaroxaban(366789-02-8) is recommended as an option for treating pulmonary embolism and preventing recurrent deep vein thrombosis and pulmonary embolism in adults.
  1. Rivaroxaban (Xarelto, Bayer) is indicated for the 'treatment of deep vein thrombosis and pulmonary embolism, and prevention of recurrent deep vein thrombosis and pulmonary embolism in adults'. For the initial treatment of acute pulmonary embolism, the recommended dosage of rivaroxaban is 15 mg twice daily for the first 21 days followed by 20 mg once daily for continued treatment and prevention of recurrent venous thromboembolism.
  2. Non-Valvular Atrial Fibrillation (NVAF)* to prevent stroke & systemic embolism.
  3. Acute VTE treatment & prevention of recurrent VTE [for deep vein thrombosis (DVT) and pulmonary embolism (PE)].
  4. Prevention of venous thromboembolic events (VTE) in elective total hip or knee replacement surgery (THR, TKR).
  ;

• important information about XARELTO

  For people taking XARELTO for atrial fibrillation:
  People with atrial fibrillation (an irregular heart beat) are at an increased risk of forming a blood clot in the heart, which can travel to the brain, causing a stroke, or to other parts of the body. XARELTO lowers your chance of having a stroke by helping to prevent clots from forming. If you stop taking XARELTO, you may have increased risk of forming a clot in your blood.
  XARELTO can cause bleeding which can be serious, and rarely may lead to death. This is because XARELTO is a blood thinner medicine that reduces blood clotting. While you take XARELTO you are likely to bruise more easily and it may take longer for bleeding to stop.
  You may have a higher risk of bleeding if you take XARELTO and take other medicines that increase your risk of bleeding, including:
  1. aspirin or aspirin containing products
  2. non-steroidal anti-inflammatory drugs (NSAIDs)
  3. warfarin sodium (Coumadin®, Jantoven®)
  4. any medicine that contains heparin
  5. clopidogrel (Plavix®)
  6. selective serotonin reuptake inhibitors (SSRIs) or serotonin norepinephrine reuptake inhibitors (SNRIs)
  7. other medicines to prevent or treat blood clots
  Tell your doctor if you take any of these medicines. Ask your doctor or pharmacist if you are not sure if your medicine is one listed above. ;

• Carcinogenesis, Mutagenesis, Impairment of Fertility

  Rivaroxaban(366789-02-8) was not carcinogenic when administered by oral gavage to mice or rats for up to 2 years. The systemic exposures (AUCs) of unbound rivaroxaban in male and female mice at the highest dose tested (60 mg/kg/day) were 1- and 2-times, respectively, the human exposure of unbound drug at the human dose of 20 mg/day. Systemic exposures of unbound drug in male and female rats at the highest dose tested (60 mg/kg/day) were 2- and 4-times, respectively, the human exposure.
  Rivaroxaban was not mutagenic in bacteria (Ames-Test) or clastogenic in V79 Chinese hamster lung cells in vitro or in the mouse micronucleus test in vivo.
  No impairment of fertility was observed in male or female rats when given up to 200 mg/kg/day of rivaroxaban orally. This dose resulted in exposure levels, based on the unbound AUC, at least 13 times the exposure in humans given 20 mg rivaroxaban daily. ;

• Adverse Reactions

  Bleeding events (may be serious or fatal), back pain, wound secretion, pruritus, pain in extremity, abdominal pain, blister. ;

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