波生坦 (Stayveer, Tracleer)

概览

Bosentan is a dual endothelin receptor antagonist used to treat pulmonary arterial hypertension.

作用机制

Endothelin-1 (ET-1) is a neurohormone, the effects of which are mediated by binding to ET and ET receptors in the endothelium and vascular smooth muscle. It displays a slightly higher affinity towards ET receptors than ET receptors. ET-1 concentrations are elevated in plasma and lung tissue of patients with pulmonary arterial hypertension, suggesting a pathogenic role for ET-1 in this disease. Bosentan is a specific and competitive antagonist at endothelin receptor types ET and ET.

适应症

Used in the treatment of pulmonary arterial hypertension (PAH), to improve exercise ability and to decrease the rate of clinical worsening (in patients with WHO Class III or IV symptoms).

• NYHA Functional Class II-IV Pulmonary arterial hypertension
• Ocular Inflammation
• Ocular bacterial infections