安立生坦
生产厂家：印度西普拉(Cipla)制药公司
功能主治：治疗肺动脉高压的ETAR拮抗剂，一年生存率高
用法用量：用法用量 必须由在肺动脉高压治疗方面有经验的医生决定是否开始本药治疗，并对治疗过程进行监测。 成人剂量 起始剂量为空腹或进餐后口服 5 mg 每日一次;如果耐受则可考虑调整为 10 mg 每日一次。 药片可在空腹或进餐后服用。 不能对药片进行掰半、压碎、或咀嚼。 没有在肺动脉高压患者中进行过高于 10 mg 每日一次剂量的研究。 在开始使用凡瑞克治疗前和治疗的过程中要进行肝功能的监测(见【注意事项】部分)。 育龄期女性 女性只有在妊娠测试阴性、以及使用两种合适的避孕方法进行避孕的情况下才能接受治疗，但如果患者已行输卵管结扎术或选择使用 T 型铜 380A IUD 或 LNg 20 IUS 进行避孕，则不需要采取另外的避孕措施。 接受凡瑞克治疗的育龄期女性应该每月进行妊娠测试(见【禁忌】和【注意事项】部分)。 已存在的肝损害 目前尚无关于已存在的肝损害对安立生坦药代动力学影响的研究。 因为体内和体外证据都表明，安立生坦的清除很大程度上依赖肝脏代谢和胆汁排泄，因此肝脏损害预计会对安立生坦的药代动力学产生明显的影响。 不建议中度或重度肝功能损害患者使用凡瑞克。 目前没有关于凡瑞克在已有轻度肝功能损害的患者中应用的资料;然而，在此类患者中安立生坦的暴露量可能会升高。 肝转氨酶升高 其它内皮素受体拮抗剂(ERAs)与转氨酶(AST，ALT)升高、肝毒性和肝衰竭病例相关。 对于开始服用凡瑞克后发生肝损伤的患者，应全面调查其肝损伤的诱因。 如转氨酶升高 > 5x ULN 或转氨酶升高还伴随胆红素 > 2x ULN，或伴有肝功能不全的症状或体征，并且可排除其他原因，则停用凡瑞克。 与环孢素 A 合用 与环孢素 A 合用时，凡瑞克的剂量应控制在 5 mg 每日一次以内(见【药物相互作用】、【药代动力学】部分)。
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Ambrisentan, also known as Letairis, is a medication used in the treatment of pulmonary arterial hypertension (PAH). PAH is a rare disease that develops when the blood pressure in the pulmonary arteries becomes too high, leading to shortness of breath, chest pain, and eventually heart failure. Ambrisentan has been shown to improve symptoms and reduce hospitalizations in patients with PAH.
Ambrisentan is a selective endothelin receptor antagonist, meaning it blocks the action of endothelin, a naturally occurring hormone that constricts blood vessels. By blocking this action, ambrisentan reduces the resistance in the pulmonary arteries, allowing blood to flow more easily and reducing the workload on the heart.Clinical trials have demonstrated the efficacy of ambrisentan in improving exercise capacity and reducing symptoms such as shortness of breath and fatigue in patients with PAH. In a study of 147 PAH patients, those treated with ambrisentan had a significantly greater improvement in exercise capacity compared to those given a placebo. Ambrisentan was also found to reduce the risk of hospitalization, one of the primary indicators of disease severity in PAH patients.
While ambrisentan has demonstrated efficacy in improving symptoms and outcomes in patients with PAH, it is important to note that the medication does come with some risks and side effects. The most common side effects include headache, nasal congestion, and flushing. Less common but more serious side effects include liver toxicity, fluid retention, and anemia. Patients taking ambrisentan should therefore be closely monitored for signs of liver damage and red blood cell counts.
Overall, ambrisentan is considered to be a highly effective treatment for pulmonary arterial hypertension. It has been approved by the US Food and Drug Administration since 2007 and has helped many patients to manage the symptoms of this challenging disease. Like all medications, however, it should be used with caution and only under the guidance of a qualified healthcare professional.
