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Macitentan | 玛舒腾坦


Opsumit/Macitentan   has Labeled Indication for Pulmonary arterial hypertension: Treatment of pulmonary arterial hypertension (PAH) (WHO Group I) to reduce risks of disease progression and hospitalization.   Oral: 10 mg once daily; maximum 10 mg/day.

Its mechanism of action is to block endothelin (ET)-1 from binding to endothelin receptor subtypes ETA and ETB on vascular endothelium and smooth muscle.  Stimulation of these receptors is associated with vasoconstriction, fibrosis, proliferation, hypertrophy, and inflammation.

[US Boxed Warnings]: For all female patients, macitentan is available only through REMS.  REMS is required because Macitentan was proved to have reproductive risks.  Prescribers must order pregnancy testing for patients of reproductive potential prior to initiation of treatment, monthly during treatment, and for 1 month after stopping treatment.

Macitentan | 玛舒腾坦的适应症为肺动脉高压。治疗肺动脉高压(PAH)以减少疾病进展和住院的风险。  口服:10毫克,每天一次;最多10毫克/天。

Macitentan作用机制是阻断内皮素-1(endothelin1/ ET1)与血管内皮细胞和平滑肌上的内皮素受体亚型ETA和ETB结合。 这些受体的刺激与血管收缩、纤维化、增殖、肥大和炎症有关。

[US Boxed Warnings]:对于所有女性患者,马西天坦只能通过REMS获得。 因为马西天坦被证明有生殖风险,所以需要REMS。 处方医生必须在开始治疗前对有生育能力的患者进行怀孕测试,在治疗期间每月进行一次,并在停止治疗后一个月进行一次。

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