波生坦
生产厂家：印度西普拉(Cipla)制药公司
功能主治：口服活性内皮素拮抗剂，治疗肺动脉高压
用法用量：用法用量 本品应由有治疗肺动脉高压丰富经验的医生决定是否开始本药治疗，并对治疗过程进行严格监测。 推荐剂量和剂量调整本品的初始剂量为一天2次、每次62.5mg，持续4周，随后增加至推荐的维持剂量125mg，一天2次。 高于一天2次、一次125mg的剂量不会带来足以抵消肝毒性风险增加的额外益处。 本品应在早、晚进食前或后服用。 转氨酶持续升高患者的剂量调整在治疗前必须检测肝脏转氨酶水平，并在治疗期间每月复查一次。 如果发现转氨酶水平升高，就必须改变监测和治疗。 下表为本品治疗过程中，转氨酶持续增高>3倍正常值上限患者剂量调整和推荐监测的总结。 如果肝脏转氨酶升高并伴有肝损害临床症状(如贫血、恶心、呕吐、发热、腹痛、黄疸、嗜睡和乏力、流感样症状(关节痛、肌痛、发热))或胆红素升高≥2倍正常值上限时，必须停药且不得重新应用本品。 ALT/AST水平>3且≤5×ULN应再做一次肝脏功能检查进行确证;如确证，则应减少每日剂量或者停药，并至少每2周监测一次转氨酶水平。 如果转氨酶恢复到用药前水平，可以酌情考虑继续或者重新用药。 ALT/AST水平>5且≤8×ULN应再做一次肝脏功能检查进行确证;如确证，应停药，并至少每2周监测一次转氨酶水平。 一旦转氨酶恢复到治疗前水平可考虑重新用药。 ALT/AST水平>8×ULN必须停药，且不得重新用药。 重新用药：仅当使用本品的潜在益处高于潜在风险，且转氨酶降至治疗前水平时，方可考虑重新用药。 重新用药时应从初始剂量开始，且必须在重新用药后3天内进行转氨酶检测，2周后再进行一次检测，随后根据上述建议进行监测。 治疗前有肝损伤患者的用药中度和重度肝脏损伤患者应禁用本品，轻度肝损伤患者不需调整剂量。 (见[禁忌]、[注意事项]、[药代动力学])。 低体重患者用药体重低于40kg且年龄大于12岁的患者推荐的初始剂量和维持剂量均为62.5mg，每天2次。 本品在12岁到18岁患者中应用的安全性和有效性数据有限。 与利托那韦联合使用服用利托那韦的患者联合使用本品：在接受利托那韦治疗至少10天的患者中，本品的起始剂量为62.5mg，根据个体患者的耐受性每天1次或隔天1次。 服用本品的患者联合使用利托那韦：开始给予利托那韦前至少应停用本品36个小时。 使用利托那韦至少10天后，再恢复给予本品的剂量为62.5mg，根据个体患者的耐受性每天1次或隔天1次。 漏服如果本品预定给药过程中出现了漏服，不得服用双倍剂量来弥补漏服的那次剂量。 患者应在规定的下次给药时间再服用本品。 治疗中止尚无肺动脉高压患者在推荐剂量下突然中止使用本品的经验。 但是为了避免同类疾病的其它治疗药物停药时出现临床情况突然恶化，应对患者进行密切监测，并考虑逐步减量(停药前的3~7天将剂量减至一半)。 在停药期间应加强病情监测。
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Pulmonary Arterial Hypertension (PAH) is a chronic and life-threating condition that leads to high blood pressure in the lungs. PAH is caused by increased resistance in the blood vessels connecting the heart to the lungs, which results in heart failure and death. Over the years, different medications have been developed to manage PAH, but none has been able to provide a cure for this deadly disease.
However, in 2001, the pharmaceutical company Actelion introduced a novel medication for PAH management, called Bosentan. Bosentan is an endothelin receptor antagonist that works by blocking the effects of endothelin. Endothelin is a naturally-occurring chemical in the body that plays a role in blood vessel regulation. In PAH patients, the levels of endothelin are abnormally high, leading to vasoconstriction and increased pulmonary vascular resistance. Bosentan's mechanism of action targets this process, leading to decreased pulmonary vascular resistance, dilation of blood vessels, and overall improved blood flow.Bosentan is the first medication approved by the US FDA for the treatment of PAH. Clinical studies have shown that Bosentan reduces the number of PAH-related hospitalizations and improves exercise tolerance in patients with PAH. Bosentan has also been found to improve a patient's quality of life, an essential aspect of disease management, by reducing the symptoms of PAH, such as shortness of breath, fatigue, and chest pain.
Bosentan is administered orally, twice daily. The recommended starting dose for Bosentan is 62.5 mg twice a day for four weeks, after which the dosage is increased to 125 mg twice a day. However, Bosentan's use is not without side effects. The side effects of Bosentan include headaches, dizziness, flushing, nasal congestion, and liver toxicity. As a result, patients on Bosentan therapy require frequent liver function tests to monitor for evidence of liver disease.
In conclusion, Bosentan is a breakthrough medication for the management of PAH. It is effective in reducing the number of hospitalizations related to PAH and improving a patient's quality of life. Its oral administration and ease of use make it a more convenient option for patients with PAH. While Bosentan's side effects are notable, with proper monitoring and management, Bosentan's benefits outweigh its side effects. Overall, Bosentan has revolutionized the management of PAH and given hope to patients with this deadly disease.
