FONDAPARINUX SODIUM（FONDAPARINUX）注射剂，用于皮下使用
美国初步批准：2001年
警告：
脊柱/膈肌HEMATOMAS请参阅完整的处方信息以获得完整的盒装警告。
硬膜外或脊髓血肿可能发生在用低分子量肝素（LMWH），类肝素或磺达肝素钠抗凝，并接受神经轴麻醉或经历脊柱穿刺的患者。
这些血肿可能导致长期或永久性麻痹。在安排患者进行脊柱手术时考虑这些风险。可能增加这些患者硬膜外或脊髓血肿发生风险的因素包括：
使用留置硬膜外导管
伴随使用影响止血的其他药物，如非甾体抗炎药（NSAIDs），血小板抑制剂或其他抗凝剂
外伤或重复硬膜外或脊柱穿刺的病史
脊柱畸形或脊柱外科史
经常监测患者神经功能障碍的体征和症状。如果注意到神经系统妥协，则需要进行紧急治疗。
考虑在抗凝或抗凝治疗血栓预防的患者进行神经轴干预前的益处和风险。 [见警告和注意事项和药物相互作用]
最近的主要变化
盒装警告：07/2014
禁忌症：09/2013
警告和注意事项：07/2014
作用机制
磺达肝素钠的抗血栓活性是抗凝血酶III（ATIII）介导的因子Xa选择性抑制的结果。 通过选择性地结合ATIII，磺达肝素钠增强（约300倍）ATIII对因子Xa的固有中和。 因子Xa的中和中断凝血级联，从而抑制凝血酶的形成和血栓形成。
磺达肝素钠不会使凝血酶（活化因子II）失活，并且对血小板功能没有已知的影响。 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。
适用范围及用途
磺达肝素注射钠是一种因子Xa抑制剂（抗凝血剂），适用于：
进行髋部骨折手术（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深静脉血栓形成（DVT）预防。
与华法林联合治疗DVT或急性肺栓塞（PE）。
剂量和管理
预防深静脉血栓形成：止血后每天皮下注射磺达肝素钠2.5mg。初始剂量不得早于手术后6〜8小时，持续5〜9天。对于接受髋骨骨折手术的患者，建议延长预防时间，最多延长24天。
深静脉血栓形成和肺栓塞的治疗：每天一次皮下注射5mg（体重<50kg），7.5mg（50〜100kg）或10mg（> 100kg）的磺达肝素钠。治疗应持续至少5天，直到使用华法林钠达2至3。
不要用作肌内注射。对于皮下使用，不要与其他注射液或输液混合。
剂量形式和强度
含有2.5mg，5mg，7.5mg或10mg的fondaparinux的单剂量预充式注射器。
禁忌症
磺达肝素钠注射剂在以下条件下禁忌：
在预防或治疗静脉血栓栓塞中严重肾损害（肌酐清除率<30mL/min）。
活跃大出血。细菌性心内膜炎。
血小板减少症与磺达肝素钠存在下抗血小板抗体阳性体外试验相关。
包装规格/存储和处理
磺达肝素钠注射剂有以下优点和包装尺寸：
2.5毫克磺达肝素钠0.5毫升单剂量预充式注射器，用一个带有蓝色柱塞杆的27号x 1/2英寸针头。
2单位注射器NDC 55111-678-02
单组份注射器NDC 55111-678-10
5毫克磺达肝素钠在0.4毫升单剂量预充式注射器中，贴上一个带有橙色柱塞杆的27号x 1/2英寸针头。
2单位注射器NDC 55111-679-02
单组份注射器NDC 55111-679-10
在0.6mL单剂量预充式注射器中加入7.5mg磺达肝素钠，并用洋葱柱塞杆固定27号x 1/2英寸针头。
2单机注射器NDC 55111-680-02
单组份注射器NDC 55111-680-10
10毫克磺达肝素钠在0.8毫升单剂量预充式注射器中，用一根带有紫色柱塞杆的27号x 1/2英寸针头。
2单位注射器NDC 55111-681-02
单组份注射器NDC 55111-681-10
储存于20°-25°C（68°-77°F）; [见USP受控室温]。
完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=49e0d7bc-3f49-849b-c77c-98682d1c0d19&audience=consumer
fondaparinux(磺达肝癸钠)用于行大型矫形手术病人预防术后深静脉血栓获得欧美上市许可新药
磺达肝癸钠是由赛诺菲圣德拉堡集团和欧加农公司联合原研，后授权给GSK的、以Xa因子为主要靶点的新一代抗凝药物，于2001年12月获得美国FDA正式批准，2002年在美国、英国、加拿大等多个国家上市
特点
磺达肝癸钠主要是通过和抗凝血酶(ATⅢ)结合，从而加速凝血酶(AT)灭活因子Xa，属一种间接Xa因子抑制剂，具有较强的Xa因子抑制作用。 　　
本品皮下注射给药生物利用度为100%，半衰期约17小时，可一天注射给药一次，和普通肝素相比在用药顺应性上具有明显优势。其排泄主要通过肾脏，肾病患者需要调节剂量。临床试验结果表明在预防血栓栓塞方面磺达肝葵钠较依诺肝素优越，相对危险降低50%。目前应用于术后抗血栓治疗、预防深静脉血栓、以及与华法林联合治疗急性深度静脉血栓(DVT)、急性肺栓塞(PE)的初始治疗等。
此外，磺达肝癸钠还具有以下优点：作用靶点明确，具有显著的剂量-效应关系，临床疗效可预测；药代动力学特性优越，给药方法简便；与血小板或PF4无相互作用，无需监测血小板计数；对一般凝血参数如出血时间(bleeding time)、活化部分凝血激酶时间(aPTT)、凝血酶原时间(PT)、国际标准化比率(INR)无显著影响；完全化学合成，消除了病原微生物污染的风险。
Fondaparinux Injection
pronounced as (fon'' da par' in ux )
IMPORTANT WARNING:
If you have an epidural or spinal anesthesia or a spinal puncture while using a 'blood thinner' such as fondaparinux injection, you are at risk for having a blood clot form in or around your spine that could cause you to become paralyzed. Tell your doctor if you have or have ever had spinal surgery, problems with pain medication given through the spine, a spinal deformity, or if you have bleeding problems. Tell your doctor and pharmacist if you are taking other anticoagulants ('blood thinners') such as warfarin (Coumadin), anagrelide (Agrylin), aspirin or nonsteroidal anti-inflammatory drugs (ibuprofen, naproxen), cilostazol (Pletal), clopidogrel (Plavix), dipyridamole (Persantine), eptifibatide (Integrilin), prasugrel (Effient), ticlopidine, and tirofiban (Aggrastat). If you experience any of the following symptoms, call your doctor immediately: muscle weakness, numbness or tingling (especially in your legs), or inability to move your legs.
Keep all appointments with your doctor and the laboratory. Your doctor may order certain tests to check your body's response to fondaparinux injection.
Talk to your doctor about the risk of using fondaparinux injection.
Why is this medication prescribed?
Fondaparinux injection is used to prevent deep vein thrombosis (DVT; a blood clot, usually in the leg), which can lead to pulmonary embolism (PE; a blood clot in the lung), in people who are having hip surgery, hip or knee replacement, or abdominal surgery. It is also used in along with warfarin (Coumadin, Jantoven) to treat DVT or PE. Fondaparinux injection is in a class of medications called factor Xa inhibitors. It works by decreasing the clotting ability of the blood.
How should this medicine be used?
Fondaparinux injection comes as a solution (liquid) to be injected subcutaneously (just under the skin) in the lower stomach area. It is usually given one time a day for 5 to 9 days or sometimes for up to about 1 month. You will probably begin using fondaparinux injection while you are in the hospital at least 6 to 8 hours after your surgery. Use fondaparinux injection at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Use fondaparinux injection exactly as directed. Do not inject more or less of it or inject it more often than prescribed by your doctor.
If you will continue to use fondaparinux after your hospital stay, you can inject fondaparinux yourself or have a friend or relative perform the injections. Ask your doctor or pharmacist to show you or the person who will be injecting the medication how to inject it. Before you use fondaparinux injection yourself the first time, read the Patient Information that comes with it. This information includes directions for how to use and inject fondaparinux prefilled safety syringes. Be sure to ask your pharmacist or doctor if you have any questions about how to inject this medication.
Each syringe has enough medication in it for one shot. Do not use the syringe and needle more than one time. Your doctor, pharmacist, or healthcare provider will tell you how to throw away used needles and syringes safely.
Do not mix fondaparinux injection with other medications or solutions.
Other uses for this medicine
Fondaparinux injection is also sometimes used to help prevent blood clots in people who have had a heart attack. Talk to your doctor about the risks of using this medication for your condition.
What special precautions should I follow?
Before using fondaparinux injection,
•tell your doctor and pharmacist if you have had a serious allergic reaction (difficulty breathing or swallowing or swelling of the face, throat, tongue, lips, or eyes) to fondaparinux. Your doctor will probably tell you not to use fondaparinux. Also tell your doctor if you are allergic to any other medications, or any of the ingredients in fondaparinux injection. Ask your pharmacist for a list of the ingredients. Also tell your doctor and pharmacist if you are allergic to latex.
•tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention the medications listed in the IMPORTANT WARNING section. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
•tell your doctor if you weigh 110 pounds (50 kg) or less, are bleeding anywhere on your body or have a low number of platelets (blood clotting cells) in your blood, endocarditis (an infection in the heart), or kidney disease. Your doctor will probably tell you not to use fondaparinux injection.
•tell your doctor if you have or have ever had ulcers in your stomach or intestines, high blood pressure, a stroke or ministroke (TIA), eye disease due to diabetes, or liver disease. Also tell your doctor if you have recently had brain, eye, or spinal surgery.
•tell your doctor if you are pregnant, plan to become pregnant, or are breastfeeding. If you become pregnant while taking fondaparinux injection, call your doctor.
•if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking fondaparinux injection.
What special dietary instructions should I follow?
Unless your doctor tells you otherwise, continue your normal diet.
What should I do if I forget a dose?
Give the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not use more than one dose of fondaparinux injection at the same time.
What side effects can this medication cause?
Fondaparinux injection may cause side effects. Tell your doctor if any of these symptoms are severe or do not go away:
•rash, itching, bruising, or bleeding at the injection site
•dizziness
•confusion
•pale skin
•blisters on skin
•difficulty falling asleep or staying asleep
Some side effects can be serious. If you experience any of these symptoms, or those listed in the IMPORTANT WARNING section, call your doctor immediately or get emergency medical treatment:
•unusual bleeding or bruising
•dark red spots under the skin or in the mouth
•hives
•swelling of the face, throat, tongue, lips, or eyes
•difficulty swallowing or breathing
Fondaparinux injection may cause other side effects. Call your doctor if you have any unusual problems while using this medication.
If you experience a serious side effect, you or your doctor may send a report to the Food and Drug Administration's (FDA) MedWatch Adverse Event Reporting program online (http://www.fda.gov/Safety/MedWatch) or by phone (1-800-332-1088).