英文药名：TREPROST for injection（Treprostinil） 中文药名：曲前列环素注射剂 生产厂家：持田药业 治疗类别名称 前列腺素I2衍生物制剂 欧文商標名 TREPROST 20mg for injection TREPROST 50mg for injection TREPROST 100mg for injection TREPROST 200mg for injection 一般名 トレプロスチニル 一般名（欧名） Treprostinil 化学名 {[(1R,2R,3aS,9aS)-2-Hydroxy-1-[(3S)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-cyclopenta[b]naphthalen-5-yl]oxy}acetic acid 分子式 C23H34O5  分子量 390.51 構造式 性状 曲前列环素是白色的粉末为淡黄色。产物，N和非常易溶于N-二甲基甲酰胺和易溶于甲醇，乙醇（99.5），并且几乎不溶于水。 审批条件 由于临床试验的情况下在日本是非常有限的，上市后，直到一定数量案件的数据被集成，通过实施的所有情况下，使用效果的调查，该药物以及了解病人使用的背景资料，搜集有关这种药物的安全性和有效性的数据在年初，采取必要措施，正确使用此药 药效药理 与前列环素，曲前列素，血管扩张作用，血小板凝集抑制活性，抑制收缩和血栓形成肺动脉，也能够降低肺动脉压力和肺血管阻力，疗效对肺动脉高压它被认为是表示。 1.实效性肺动脉高压模型 抑制肺动脉高压和肺血管阻力的上升，由于麻醉猫的低氧负荷。 抑制肺动脉高压和肺血管阻力的上升，由于麻醉猪新生儿低氧负荷。 2.血管扩张作用 由U-46619收缩兔肠系膜动脉血管平滑肌是血栓烷A2衍生物被放宽（体外）。 通过连续静脉给药于狗和猫，肺动脉压，肺血管阻力，血压和总外周血管阻力降低。 3.抑制血小板聚集作用 由人血小板凝集和ADP胶原抑制大鼠血小板凝集（体外）。 通过连续静脉给药抑制兔血小板聚集与ADP。此外，皮下给药和口服给药时，由ADP抑制大鼠血小板凝集。 通过连续静脉给药，抑制血小板凝集的狗[19]的冠状动脉狭窄相关的冠血流量减少。 适应症 肺动脉高压（WHO功能分级II级，III和IV） 用法用量 通常情况下，1.25ng/公斤/在剂量率的曲前列素的成年人开始连续静脉给药或连续皮下注射分钟。如果初始剂量率不能用这种药物的全身性副作用是不能容忍的，减量的管理率0.625ng/kg/分钟。 同时充分观察患者的状况，在原则上，前四个星期，然后增加至1.25ng每周/kg/min，最多2.5ng每周/公斤/分钟，这取决于临床症状的增加是确定最佳剂量率。如果你想超过1.25或2.5ng/公斤/每周分增加，将精心管理，同时充分证实了患者的耐受性。在确定给药的最佳速率，和的副作用和这种药物作为指标的肺动脉高血压症状的改善。 包装规格 注射：20毫克*1瓶 注射：50毫克*1瓶 注射：100毫克*1瓶 注射：200毫克*1瓶 生产厂商 持田药业有限公司 完整处方资料附件； 1：http://www.kegg.jp/medicus-bin/japic_med?japic_code=00063157 2：http://www.mochida.co.jp/dis/medicaldomain/circulatory/treprost/home/index.html Remodulin® (treprostinil) Injection for the treatment of pulmonary arterial hypertension (PAH) by subcutaneous and intravenous administration.  Remodulin will be sold in Japan under the brand name Treprost™ by Mochida Pharmaceutical Co., Ltd., under an exclusive distribution agreement with United Therapeutics. About United Therapeutics United Therapeutics Corporation is a biotechnology company focused on the development and commercialization of unique products to address the unmet medical needs of patients with chronic and life-threatening conditions. About Remodulin (treprostinil) Injection Remodulin is a prostacyclin vasodilator indicated in the United States for the treatment of pulmonary arterial hypertension (PAH) (WHO Group 1) to diminish symptoms associated with exercise.  Studies establishing effectiveness included patients with NYHA Functional Class II-IV symptoms and etiologies of idiopathic or heritable PAH (58%), PAH associated with congenital systemic-to-pulmonary shunts (23%), or PAH associated with connective tissue diseases (19%).  Remodulin may be administered as a continuous subcutaneous infusion or continuous intravenous infusion; however, because of the risks associated with chronic indwelling central venous catheters, including serious blood stream infections, continuous intravenous infusion should be reserved for patients who are intolerant of the subcutaneous route, or in whom these risks are considered warranted.  In patients with PAH requiring transition from Flolan® (epoprostenol sodium), Remodulin is indicated to diminish the rate of clinical deterioration.  The risks and benefits of each drug should be carefully considered prior to transition. Important Safety Information Chronic intravenous infusions of Remodulin are delivered using an indwelling central venous catheter. This route is associated with the risk of blood stream infections, or BSI, and sepsis, which may be fatal. Therefore, continuous subcutaneous infusion is the preferred mode of administration. Remodulin should be used only by clinicians experienced in the diagnosis and treatment of PAH. Remodulin is a potent pulmonary and systemic vasodilator.  It lowers blood pressure, which may be further lowered by other drugs that also reduce blood pressure.  Remodulin inhibits platelet aggregation and therefore, may increase the risk of bleeding, particularly in patients on anticoagulants. Remodulin dosage adjustment may be necessary if inhibitors or inducers of CYP2C8 are added or withdrawn.  Initiation of Remodulin must be performed in a setting with adequate personnel and equipment for physiological monitoring and emergency care.  Therapy with Remodulin may be used for prolonged periods, and the patient's ability to administer Remodulin and care for an infusion system should be carefully considered. Remodulin dosage should be increased for lack of improvement in, or worsening of, symptoms and it should be decreased for excessive pharmacologic effects or for unacceptable infusion site symptoms. Abrupt withdrawal or sudden large reductions in dosage of Remodulin may result in worsening of PAH symptoms and should be avoided. Caution should be used in patients with hepatic or renal insufficiency. The most common side effects of Remodulin included those related to the method of infusion.  For subcutaneous infusion, infusion site pain and infusion site reaction (redness and swelling) occurred in the majority of patients.  These symptoms were often severe and could lead to treatment with narcotics or discontinuation of Remodulin.  For intravenous infusion, line infections, sepsis, arm swelling, tingling sensations, bruising, and pain were most common. General side effects (> 5% more than placebo) were diarrhea, jaw pain, vasodilatation and edema.