马昔腾坦
生产厂家：印度纳科Natco制药有限公司
功能主治：肺动脉高压的内皮素受体拮抗剂，降低发病率和死亡率
用法用量：用法用量 应该由在肺动脉高压治疗方面具有经验的医生启动治疗，并对治疗进行监测。 剂量本品的推荐剂量是10mg，每日一次口服。 可随餐或空腹服用。 不建议患者将药片掰半、压碎或咀嚼服用。 尚未在PAH患者中进行过高于10mg，每日一次剂量的研究，故不建议使用。 漏服应每天在固定时间服用本品。 如果漏服应尽快补服，并在固定时间服用下一剂药物，同时需告知患者不得服用双倍剂量来弥补漏服的那次剂量。 育龄期女性的妊娠试验育龄期女性只有妊娠试验结果为阴性时才可开始使用本品治疗。 治疗期间应每月进行一次妊娠试验(见[孕妇及晡乳期妇女用药]部分)。 肝功能不全患者根据药代动力学数据，在轻度、中度或重度肝功能损伤患者中，无需进行剂量调整(见[药代动力学]部分)。 然而，在中度或重度肝功能损伤的PAH患者中，尚没有应用本品的临床经验。 不推荐在中度肝损伤患者中使用本品。 不得在重度肝损伤患者中或肝脏转氨酶出现有临床意义增高(高于正常上限3倍(>3xULN))的患者中启动本品治疗。 在开始使用本品前应进行肝酶检查，并在治疗期间依据临床情况复查。 (见[注意事项]部分)。 肾功能不全患者根据药代动力学数据，在肾功能损伤患者中不需调整剂量。 尚无本品在重度肾功能损伤PHA患者中使用的临床经验，建议在此人群使用要谨慎。 肾功能不全的患者使用本品治疗过样中出现低血压和贫血的风险可能更高，因此，应考虑监测血压和血红蛋白。 不推荐在接受透析的患者中使用本品(见[药代动力学]部分)。
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Pulmonary hypertension (PH) is a life-threatening condition that affects the blood vessels in the lungs. It causes high blood pressure in the pulmonary arteries, leading to shortness of breath, fatigue, and chest pain. Currently, there is no cure for PH, and available treatments only help alleviate its symptoms.
However, a new medication called macitentan is offering hope to PH patients. Macitentan is an endothelin receptor antagonist, which means it blocks the action of a protein called endothelin that constricts blood vessels in the lungs. By inhibiting endothelin, macitentan improves blood flow to the lungs and reduces PH symptoms.Macitentan was approved by the U.S. Food and Drug Administration (FDA) in 2013 for the treatment of pulmonary arterial hypertension (PAH), a subset of PH characterized by elevated pressure in the arteries that supply blood to the lungs. In clinical trials, macitentan was shown to improve exercise capacity and reduce hospitalization rates among PAH patients.
Moreover, macitentan has demonstrated its effectiveness in treating chronic thromboembolic pulmonary hypertension (CTEPH), another form of PH caused by the presence of blood clots in the lungs. In a phase III clinical trial, macitentan significantly improved pulmonary vascular resistance and exercise capacity in CTEPH patients.
One of the advantages of macitentan over other PAH therapies is its long-lasting effect. Macitentan has a half-life of about 16 hours, which means it remains active in the body for a prolonged period compared to other drugs, allowing for once-daily dosing.
Macitentan is not without its side effects, however. Common adverse reactions include headache, edema, and nausea. Additionally, macitentan can cause liver damage, so patients need to have regular liver function tests while on treatment.
Despite these limitations, macitentan represents a significant step forward in the management of PH. Its approval has expanded the treatment options available to PAH and CTEPH patients, who previously had limited choices for their condition. Moreover, ongoing studies are exploring macitentan's potential in other PH subtypes, such as pulmonary venous hypertension.
In conclusion, macitentan is a promising new drug for pulmonary hypertension that offers hope to patients suffering from this debilitating condition. Its effectiveness in improving pulmonary vascular resistance and exercise capacity, combined with once-daily dosing, makes it a valuable addition to the PH treatment armamentarium. As research continues, we may see further advances in macitentan's use, potentially leading to better outcomes for PH patients.
