Rivaroxaban (BAY 59-7939) is an oral anticoagulant under development by Bayer; it will be marketed as Xarelto. It acts by inhibiting the active form of coagulation factor X (factor Xa).
Use
Expected
Due to the decreased need for monitoring, rivaroxaban is likely to be used to replace warfarin for a number of indications, such as atrial fibrillation.
Trial results
In phase IIb trials it was effective in reducing thromboembolic complications (deep vein thrombosis and pulmonary embolism) after orthopedic surgery[8] and it is under investigation for the prevention of DVT and PE and for anticoagulation in atrial fibrillation.[7] Advantages are the oral administration (a benefit over low molecular weight heparins, which require subcutaneous injections) and no need for monitoring (an advantage over warfarin). In studies, dosages of 2.5-10 mg once or twice daily were used.
Bayer-sponsored phase 3 clinical trials showed that once-daily rivaroxaban achieved superior efficacy and similar safety in the prevention of venous thromboembolism (VTE) in patients undergoing knee replacement or hip arthroplasty surgery in comparison with enoxaparin, a LMWH.
原廠仿單介紹：
Xarelto® 10 mg film-coated tablets.
(Refer to full Summary of Product Characteristics before prescribing.)
Composition:
Active ingredient: 10 mg rivaroxaban.
Excipients1: Microcrystalline cellulose, croscarmellose sodium, lactose monohydrate, hypromellose, sodium laurilsulfate, magnesium stearate, macrogol 3350, titanium dioxide (E171), iron oxide red (E172).
Indication:
Prevention of venous thromboembolism (VTE) in adult patients undergoing elective hip or knee replacement surgery.
For patients undergoing major hip surgery, a treatment duration of 5 weeks is recommended.
For patients undergoing major knee surgery, a treatment duration of 2 weeks is recommended.
Contraindications:
Hypersensitivity to the active substance or to any of the excipients; clinically significant active bleeding; hepatic disease associated with coagulopathy and clinically relevant bleeding risk, pregnancy and lactation.
Warnings and Precautions:
Treatment with rivaroxaban is not recommended in patients: - concomitantly treated systemically with strong concurrent CYP3A4- and P-gp-inhibitors, i.e. azole-antimycotics (such as ketoconazole, itraconazole, voriconazole and posaconazole) or HIV protease inhibitors (e.g. ritonavir), - with severe renal impairment (creatinine clearance <15 ml/min), and due to lack of data: - below 18 years of age, - undergoing hip fracture surgery. The following sub-groups of patients are at increased risk of bleeding and are to be carefully monitored for signs of bleeding complications after initiation of treatment: patients with severe renal impairment (creatinine clearance 15 - 29 ml/min), patients with moderate renal impairment (creatinine clearance 30 - 49 ml/min) concomitantly receiving other medicinal products which increase rivaroxaban plasma concentrations, cirrhotic patients with moderate hepatic impairment (Child Pugh B) if it is not associated with coagulopathy; patients treated concomitantly with medicinal products affecting haemostasis (such as NSAIDs, acetylsalicylic acid, platelet aggregation inhibitors, other antithrombotic agents) or with the moderate concurrent CYP3A4- and P-gp-inhibitor fluconazole; patients with congenital or acquired bleeding disorders, uncontrolled severe arterial hypertension, active ulcerative gastrointestinal disease, recent gastrointestinal ulcerations, vascular retinopathy, recent intracranial or intracerebral haemorrhage, intraspinal or intracerebral vascular abnormalities, recent brain, spinal or ophthalmological surgery. Strong CYP3A4 inducers (e.g. rifampicin, phenytoin, carbamazepine, phenobarbital or St. John’s Wort) should be used with caution since they may lead to reduced rivaroxaban plasma concentrations and thus may reduce efficacy. Special care is to be taken when neuraxial anaesthesia or spinal/epidural puncture is employed. Xarelto contains lactose.
Undesirable effects:
Common: increased GGT, increase in transaminases (incl. increased ALT, AST), anaemia (incl. respective laboratory parameter), nausea, post-procedural haemorrhage (incl. post-operative anaemia, and wound haemorrhage). Uncommon: increase in: lipase, amylase, blood bilirubin, LDH, alkaline phosphatase, tachycardia, thrombocythaemia (incl. platelet count increased), syncope (incl. loss of consciousness), dizziness, headache, constipation, diarrhoea, abdominal and gastrointestinal pain (incl. upper abdominal pain, stomach discomfort), dyspepsia (incl. epigastric discomfort), dry mouth, vomiting, renal impairment (incl. blood creatinine increased, blood urea increased), pruritus (incl. rare cases of generalised pruritus), rash, urticaria (incl. rare cases of generalised urticaria), contusion, pain in extremity, wound secretion, haemorrhage (incl. haematoma and rare cases of muscle haemorrhage), gastrointestinal tract haemorrhage (incl. gingival bleeding, rectal haemorrhage, haememesis), haematuria (incl. blood urine present), genital tract haemorrhage (incl. menorrhagia), hypotension (incl. blood pressure decreased, procedural hypotension), nose bleed, localised oedema, peripheral oedema, feeling unwell (incl. fatigue, asthenia), fever. Rare: bilirubin conjugated increased (with or without concomitant increased ALT), dermatitis allergic, hepatic function abnormal. Frequency not known: bleeding into a critical organ (e.g. brain), adrenal haemorrhage, conjunctival haemorrhage, haemoptysis, hypersensitivity, jaundice.
Classification for supply:
Medicinal product subject to medical prescription.
相關資訊可以參閱：
http://www.xarelto.com/scripts/pages/en/index.php
n engl j med 358;26 www.nejm.org june 26, 2008
原廠描述：
Rivaroxaban是新型口服抗凝血劑，每日服用一次，可預防或治療血塊。Rivaroxaban可針對凝血系統中的Xa因子加以抑制，從而控制凝血酶形成（使血液凝結的酵素）。
Rivaroxaban已進入臨床開發的最後階段，可長期、短期用於有效預防及治療動、靜脈血栓症。這是一項非常完整的開發計畫，預計有近4萬名患者在13項第二、三期試驗中，針對數種適應症接受評估，包括預防大型整形手術患者發生靜脈血栓性栓塞症（venous thromboembolism，簡稱VTE）、治療VTE、預防心房纖維震顫患者發生中風，以及預防急性冠狀症候群患者發生重大心血管事件。
接受整形手術的患者，在術後發生血栓性栓塞症的風險較高。目前醫界使用低分子量肝素（LMWH）或維生素K拮抗劑（vitamin K antagonists，簡稱VKA）預防整形手術患者發生VTE。LMWH並非口服藥，因此非住院患者不易遵守醫囑，持續接受治療達數週。目前只有維生素K拮抗劑可口服施用，但藥效發揮的速度很慢，對不同患者的療效差異也很大。此外，這些藥物會和其他藥物及某些食物產生許多交互作用，這表示，患者必須定期驗血以嚴密監控藥效，並且須隨時調整劑量。拜耳計畫於2007年底在歐洲及2008年在美國首次提出上市許可證申請，用於預防大型整形手術後的VTE。
Rivaroxaban是安全、有效、每日一劑的口服藥物，可在院內及居家環境使用，不需定期監控，因此可成為新型抗凝血藥物。Rivaroxaban也可望成為醫院及居家，用於長期或短期預防及治療的藥物。
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