英文药名：Arixtra Injection（Fondaparinux Sodium） 中文药名：磺达肝素钠预充式注射器 生产厂家：葛兰素史克 アリクストラ皮下注1.5mg／アリクストラ皮下注2.5mg アリクストラ皮下注5mg／アリクストラ皮下注7.5mg 治疗类别名称 合成Xa的抑制剂 商標名 Arixtra Injection 一般名 フォンダパリヌクスナトリウム（Fondaparinux Sodium） 化学名 Decasodium methyl O-(2-deoxy-6-O-sulfo-2-sulfoamino-α-D-glucopyranosyl)-(1→4)-O-(β-D-glucopyranosyluronic acid)- (1→4)-O-(2-deoxy-3,6-di-O-sulfo-2-sulfoamino-α-D-glucopyranosyl)-(1→4)-O-(2-O-sulfo-α-L-idopyranosyluronic acid)-(1→4)-2-deoxy-6-O-sulfo-2-sulfoamino-α-D-glucopyranoside 分子式 C31H43N3Na10O49S8 分子量 1728.08 構造式 性状 白色粉末。 操作注意事项 确认该异常如着色或悬浮物中的含量的液体，没有观察到。 药效药理 1.对静脉血栓模型效果 在大鼠的凝血活酶诱导的静脉血栓形成模型中，磺达肝素钠抑制由皮下给药腔静脉血栓形成，ED50为0.20mg的/公斤。在大静脉狭窄血栓模型大鼠的腔静脉非狭窄血栓模型，通过静脉给药抑制血栓形成，其ED50为0.028mg/ kg和0.074mg/公斤。在兔子的韦斯勒充血血栓形成模型中，由高于0.17mg/ kg时，在颈静脉抑制血栓形成更皮下使用。 2. 作用机理 磺达肝素结合以高亲和力与ATIII，通过显着增强的ATIII的抗Xa活性，抑制凝血酶产生。磺达肝素的作用是选择性的因子Xa，不同于肝素，几乎不提高ATIII的抗凝血酶活性。 3.对止血作用 在大鼠皮下出血模型，磺达肝素钠比肝素温和的，但表现出剂量依赖性的，没有出血率的增加，治疗指数（是剂量/血栓形成在大鼠皮下出血率增加三倍剂量用于抑制50％）低于肝素和低分子量肝素更高。的磺达肝癸钠增加小鼠和大鼠的出血尾截断，效果硫酸鱼精蛋白的施用被抑制在不影响血栓形成抑制效果。 4.交叉反应性抗体HIT 磺达几乎不结合血小板因子4，它没有显示出交叉反应性与肝素诱导的血小板减少症患者的血清。 5.对人体血液凝血时间的影响 磺达肝癸钠2.5mg的给药，活化部分凝血酶时间（APTT），活化凝血时间（ACT），凝血酶原时间（PT-INR），出血时间，在正常凝血试验如纤溶活性临床显著做的效果没有观察到。 适应病症 静脉血栓栓塞，抑制静脉血栓栓塞的发病中的下一个患者的高风险 ·下肢矫形手术的患者 ·腹部手术的病人 用法与用量 成人，每天一次，每次为2.5mg。此外，对于肾功能衰竭患者，以在一个时间1.5Mg1_nichi使用取决于对肾功能的程度。 包装规格 注射器 1.5毫克（0.3毫升）*10注射器 2.5毫克（0.5毫升）*10注射器 5毫克（0.4毫升）*10注射器 7.5毫克（0.6毫升）*10注射器 制造厂商 葛兰素史克公司 完整资料附件： 1）：http://www.info.pmda.go.jp/go/pack/3339400G1029_1_06/ 2）：http://www.info.pmda.go.jp/go/pack/3339400G3021_1_05/3339400G3021_1_05?view=body Arixtra（fondaparinux sodium） Generic Name: fondaparinux sodium Dosage Form: injection, solution FULL PRESCRIBING INFORMATION ARIXTRA is approved for the treatment and prophylaxis of venous thromboembolism (VTE). Learn more about ARIXTRA’s approved indications below. Treatment of deep vein thrombosis (DVT), including outpatient Treatment of pulmonary embolism (PE), including outpatient VTE prophylaxis after major orthopedic surgery Extended VTE prophylaxis after hip fracture surgery VTE prophylaxis after abdominal surgery  INDICATIONS AND USAGE ARIXTRA Injection is indicated for the prophylaxis of deep vein thrombosis, which may lead to pulmonary embolism: • in patients undergoing hip fracture surgery, including extended prophylaxis; • in patients undergoing hip replacement surgery; • in patients undergoing knee replacement surgery; • in patients undergoing abdominal surgery who are at risk for thromboembolic complications. ARIXTRA Injection is indicated for: • the treatment of acute deep vein thrombosis when administered in conjunction with warfarin sodium, and • the treatment of acute pulmonary embolism when administered in conjunction with warfarin sodium when initial therapy is administered in the hospital. CONTRAINDICATIONS ARIXTRA Injection is contraindicated in patients with severe renal impairment (creatinine clearance <30mL/min). ARIXTRA is eliminated primarily by the kidneys, and such patients are at increased risk for major bleeding episodes (see WARNINGS: Renal Impairment). ARIXTRA prophylactic therapy is contraindicated in patients with body weight <50 kg undergoing hip fracture, hip replacement or knee replacement surgery, and abdominal surgery. During the randomized clinical trials of prophylaxis in the peri-operative period following hip fracture, hip replacement, or knee replacement surgery, occurrence of major bleeding was doubled in patients with a body weight <50 kg compared with those with a body weight ≥50 kg (5.4% versus 2.1%). In the clinical trial in patients undergoing abdominal surgery, the major bleeding rate was also higher in patients with a body weight <50 kg as compared to those with a body weight ≥50 kg (5.3% versus 3.3%), respectively. The use of ARIXTRA is contraindicated in patients withactivemajorbleeding,bacterial endocarditis, in patients with thrombocytopenia associated with a positive in vitro test for anti- platelet antibody in the presence of fondaparinux sodium, or in patients with known hypersensitivity to fondaparinux sodium. WARNINGS ARIXTRA Injection is not intended for intramuscular administration.  ARIXTRA cannot be used interchangeably (unit for unit) with heparin, low molecular weight heparins or heparinoids, as they differ in manufacturing process, anti-Xa and anti-IIa activity, units, and dosage. Each of these medicines has its own instructions for use. Renal Impairment (See also CONTRAINDICATIONS): Hip Fracture, Hip Replacement and Knee Replacement Surgeries: Major bleeding in patients receiving prophylactic therapy in hip fracture, hip replacement, or knee replacement surgery occurred in 1.6% (25/1,565) of patients with normal renal function, in 2.4% (31/1,288) with mild renal 16impairment, in 3.8% (19/504) with moderate renal impairment, and in 4.8% (4/83) with severe renal impairment. When ARIXTRA was used according to the recommended timing of the first injection (6 to 8 hours after surgery), major bleeding occurred in 1.8% (16/905) of patients with normal renal function, in 2.2% (15/675) with mild renal impairment, in 2.3% (6/265) with moderate renal impairment, and in 0% (0/40) with severe renal impairment.  Abdominal Surgery: Major bleeding in patients receiving prophylactic therapy in abdominal surgery occurred in 2.1% (13/606) of patients with normalrenalfunction, in 3.6% (22/613) with mild renal impairment, in 6.7% (12/179) with moderate renal impairment, and in 7.1% (1/14) with severe renal impairment. When ARIXTRA was used according to the recommended timing of the first injection (6 to 8 hours after surgery), major bleeding occurred in 2.1% (10/467) of patients with normal renal function, in 3.3% (16/481) with mild renal impairment, in 5.8%(8/137withmoderate renal impairment, and in 7.7% (1/13) with severe renal impairment. Treatment of Deep Vein Thrombosis and Pulmonary Embolism: Major bleeding in patients receiving treatment for DVT and PE occurred in 0.4% (4/1,132) of patients with normal renal function, in 1.6% (12/733) with mild renal impairment, in 2.2% (7/318) with moderate renal impairment, and in 7.3% (4/55) with severe renal impairment.   ARIXTRA should be used with caution in patients with moderate renal impairment (creatinine clearance 30-50mL/min).  Renal function should be assessed periodically in patients receiving ARIXTRA. The drug should be discontinued immediately in patients who develop severe renalimpairment while on therapy. After discontinuation