近日，美国FDA批准Arixtra(fondaparinux sodium 戊聚糖钠/磺达肝素钠)用于行髋骨骨折手术的患者，作为预防深度静脉血栓的药物，以防止肺栓塞的发生。也扩展到行髋关节置换手术的患者和膝关节置换手术的患者。 ARIXTRA（磺达肝素钠 fondaparinux sodium）注射液 用于皮下注射 美国初步批准：2001年 警告： SPINAL/EPIDURAL HEMATOMASSee完整的处方信息完整的盒装警告。 硬膜外或脊髓血肿可发生在用低分子量肝素（LMWH），类肝素或磺达肝素钠抗凝并正在接受神经轴麻醉或经历脊髓穿刺的患者中。这些血肿可导致长期或永久性麻痹。在安排脊柱手术患者时考虑这些风险。可能增加这些患者发展硬膜外或脊髓血肿的风险的因素包括： •使用留置的硬膜外导管 •伴随使用影响止血的其他药物，例如非甾体抗炎药（NSAID），血小板抑制剂或其他抗凝剂 •创伤性或反复性硬膜外或脊柱穿刺的病史 •脊柱畸形或脊柱手术的病史 经常监测患者的神经损伤的体征和症状。如果注意到神经系统损害，紧急治疗是必要的。 考虑抗凝治疗或抗凝治疗的患者的神经轴干预之前的益处和风险，以预防血栓栓塞。[见警告和注意事项和药物相互作用] 作用机制 磺达肝素钠的抗血栓形成活性是抗凝血酶III（ATIII）介导的因子Xa的选择性抑制的结果。 通过选择性结合ATIII，磺达肝素钠增效剂（约300倍）由ATIII先天中和因子Xa。 因子Xa的中和中断了血液凝固级联，因此抑制了凝血酶形成和血栓形成。 磺达肝素钠不会使凝血酶（活化的因子II）失活，并且对血小板功能没有已知的作用。 在推荐剂量下，磺达肝素钠不影响纤维蛋白溶解活性或出血时间。 适应症和用法 ARIXTRA是因子Xa抑制剂（抗凝剂），适用于： •预防接受髋骨骨折手术（包括延长预防），髋关节置换手术，膝关节置换手术或腹部手术的患者的深静脉血栓形成（DVT）。 •当与华法林联合给药时，治疗DVT或急性肺栓塞（PE）。 剂量和给药 •深静脉血栓形成的预防：建立止血后，每日一次皮下投予ARIXTRA 2.5mg。初始剂量应在手术后不早于6至8小时给予，并持续5至9天。对于接受髋骨骨折手术的患者，建议延长预防至多24天。 •深静脉血栓形成和肺栓塞的治疗：ARIXTRA每日一次皮下注射5mg（体重<50 kg），7.5mg（50至100 kg）或10mg（>100 kg）。治疗应持续至少5天，直至使用华法林钠达到INR 2至3。 不要作为肌内注射使用。对于皮下使用，不要与其他注射或输注混合。 剂量形式和强度 含有2.5mg，5mg，7.5mg或10mg磺达肝素的单剂量，预填充的注射器。 禁忌症 ARIXTRA在以下条件禁忌： •预防或治疗静脉血栓栓塞的严重肾功能损害（肌酐清除率<30mL/min）。 •活动性大出血。 •细菌性心内膜炎。 ·在磺达肝素钠存在下与抗血小板抗体的阳性体外试验相关的血小板减少症。 •体重<50 kg（仅静脉血栓栓塞预防）。 •ARIXTRA的严重超敏反应（例如血管性水肿，过敏性反应/过敏反应）的历史。 警告和注意事项 •在有条件或正在服用伴随药物的患者中谨慎使用，以增加出血的风险。 •肾损害和体重低于50 kg的患者的出血风险增加。 •给予ARIXTRA可能发生血小板减少症。 •建议定期常规全血细胞计数（包括血小板计数），血清肌酐水平和大便潜血检查 •包装（针头护套）含有干燥天然橡胶，可能在乳胶敏感个体中引起过敏反应 不良反应 与ARIXTRA的使用相关的最常见的不良反应是出血并发症。皮下注射后可能发生轻度局部刺激（注射部位出血，皮疹和瘙痒）。 贫血，失眠，伤口引流，低钾血症，头晕，低血压，混乱，大疱性爆发，血肿，术后出血和紫癜可能发生。 要报告可疑的不良反应，请联系Mylan 药物相互作用 终止剂，可能会增加出血的风险，在ARIXTRA开始治疗之前，除非必要。如果需要联合给药，应密切监测患者的出血情况。 在特定人群中使用 •ARIXTRA在儿科患者中的安全性和有效性尚未确定。因为在ARIXTRA治疗期间的出血风险在体重<50kg的成人中增加，所以出血可能是儿科人群中使用ARIXTRA的特别安全问题。 •因为老年患者更有可能减少肾功能，所以在这些患者中应谨慎使用ARIXTRA。 完整资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d3b30c68-cf45-4b46-8ba6-72090f7ba01a ----------------------------------------------------- 注：以下产品美国上市包装，采购以咨询为准！ ----------------------------------------------------- ARIXTRA 10MG/0.8ML PFS 10/PAC  FONDAPARINUX SODIUM     00007-3236-11 ARIXTRA 2.5MG/0.5ML PFS 10/PAC  FONDAPARINUX SODIUM     00007-3230-11 ARIXTRA 5MG/0.4ML PFS SD 10/PAC  FONDAPARINUX SODIUM     00007-3232-11 ARIXTRA 7.5MG/0.6ML SYR PF 10/PAC  FONDAPARINUX SODIUM     00007-3234-11 ARIXTRA PFS 10MG/0.8ML 10  FONDAPARINUX SODIUM     00007-3236-11  ARIXTRA PFS 2.5MG/0.5ML 10  FONDAPARINUX SODIUM     00007-3230-11 ARIXTRA PFS 7.5MG/0.6ML 10  FONDAPARINUX SODIUM     00007-3234-11 ARIXTRA PFS 2.5MG/0.5ML 10  FONDAPARINUX SODIUM     67457-0592-10 ARIXTRA PFS 5MG/0.4ML 10  FONDAPARINUX SODIUM     67457-0593-04  ARIXTRA PFS 10MG/0.8ML 10  FONDAPARINUX SODIUM     67457-0595-08  ARIXTRA PFS 5MG/0.4ML 10  FONDAPARINUX SODIUM     00007-3232-11  ARIXTRA PFS 7.5MG/0.6ML 10  FONDAPARINUX SODIUM     67457-0594-06 -------------------------------------------------- ARIXTRA(fondaparinux sodium)Injection FONDAPARINUX SODIUM (fon-da-par'i-nux) Arixtra Classifications: blood formers, coagulators & anticoagulants; anticoagulant; low-molecular weight heparin Prototype: Enoxaparin Pregnancy Category: B Availability 2.5 mg/0.5 mL, 5 mg/0.4 mL, 7.5 mg/0.6 mL, 10 mg/0.8 mL syringe Actions Fondaparinux sodium causes antithrombin III (ATIII)-mediated selective inhibition of Factor Xa. Fondaparinux selectively binds to ATIII, potentiating the innate neutralization of Factor Xa by ATIII. Neutralization of Factor Xa by fondaparinux interrupts the blood coagulation cascade, inhibiting thrombin formation and, thus, thrombus development. Fondaparinux sodium does not inactivate thrombin (activated Factor II) and has no known effect on platelet function, therefore, it rarely causes thrombocytopenia. Therapeutic Effects Fondaparinux is effective in the prevention and treatment of deep-vein thrombosis. The laboratory value utilized to determine the effectiveness of the drug is the amount of anti-Xa assay expressed in mg. Uses Prophylaxis for DVT or pulmonary embolism (PE) in patients undergoing hip or knee replacement surgery or abdominal surgery; treatment of acute DVT without PE with warfarin, treatment of PE with warfarin. Contraindications Hypersensitivity to fondaparinux; active bleeding; GI bleeding; severe renal impairment with a creatinine clearance of <30 mL/min; weight <50 kg; active major bleeding; bacterial endocarditis; intramuscular administration; thrombocytopenia associated with fondaparinux. Safety and effectiveness in children have not been established. Cautious Use Renal impairment or disease; older adult; indwelling epidural catheter; dental disease, dental work; diabetic retinopathy; diverticulitis; endocarditis, epidural anesthesia; hemophilia, heparin-induced thrombocytopenia (HIT), hepatic disease, hypertension, idiopathic thrombocytopenia purpura (ITP); inflammatory bowel disease, lumbar puncture, spinal anesthesia; stroke, surgery; thrombocytopenia, thrombolytic therapy; vaginal bleeding, menstruation; peptic ulcer disease; pregnancy (category B); bleeding disorders including a history of GI ulceration, etc., history of heparininduced thrombocytopenia; lactation. Route & Dosage DVT, Pulmonary Embolism Prophylaxis Adult: SC >50 kg 2.5 mg q.d. starting at least 6 h postsurgery times 5–9 days; for hip fracture patients, up to 24 d additional use Treatment of DVT, Pulmonary Embolism Adult: SC <50 kg, 5 mg; 50–100 kg, 7.5 mg; >100 kg, 10 mg once daily x 5–9 d Renal Impairment Clcr 30–50 mL/min, use with caution; <30 mL/min, use is contraindicated Administration Subcutaneous Consult physician about discontinuing other agents that may enhance the risk of hemorrhage prior to initiation of fondaparinux. Give no sooner than 6 h after surgery. Adjust doses in older adults based on renal function. Inspect visually for particulate matter and discoloration prior to administration. Do not expel the air bubble from the syringe before the injection. Use prefilled syringe to inject into fatty tissue, alternating injection sites (e.g., between L and R abdominal wall). Store at 25° C (77° F); excursions permitted to 15°–30° C (59°–86° F). Adverse Effects (1%) Body as a Whole: Fever, edema. CNS: Insomnia, dizziness, confusion, headache. CV: Hypotension. GI: Nausea, constipation, vomiting, diarrhea, dyspepsia, elevated LFTs. Endocrine: Hypokalemia. Hematologic: Hemorrhage, anemia, hematoma. Skin: Irritation at injection site, rash, purpura, bullous eruption. Urogenital: UTI, urinary retention. Interactions Drug: anticoagulants, antiplatelets, nsaids, aspirin may increase risk of bleeding. Herbal: Feverfew, ginkgo, ginger may potentiate bleeding. Pharmacokinetics Absorption: Rapidly and completely absorbed from SC injection site. Peak: 2–3 h. Distribution: Primarily in blood. Metabolism: Negligible metabolism. Elimination: Excreted in urine. Half-Life: 18 h. Nursing Implications Assessment & Drug Effects Monitor for S&S of bleeding or hemorrhage. If noted, withhold fondaparinux and notify physician immediately. Monitor closely patients with epidural catheters for signs of paralysis below catheter level. Withhold fondaparinux and notify physician if platelet count falls below 100,000/mm3. Lab tests: Monitor baseline and periodic renal function rests; periodic CBC including platelet count, serum creatinine level, and stool occult blood tests. (Note: PT and aPTT are relatively insensitive measures of fondaparinux activity and unsuitable for monitoring.) Patient & Family Education Report any of the following to a health care provider: signs of unexplained bleeding such as: pink, red, or dark brown urine; red or dark brown vomitus; bleeding gums or bloody sputum; dark, tarry stools. Learn proper injection technique if you are to self-administer this drug. Do not take any OTC drugs without first consulting physician. Do not breast feed while taking this drug without consulting physician.