Endothelinrezeptorantagonisten

Endothelinrezeptorantagonisten is a class of drugs that block the action of endothelin, a potent vasoconstrictor. Endothelin is a peptide that binds to endothelin receptors (ETA and ETB) on the surface of cells, leading to various physiological effects, including smooth muscle contraction and cell proliferation. In conditions like pulmonary arterial hypertension (PAH), endothelin signaling is dysregulated, contributing to disease progression.

These antagonists work by preventing endothelin from binding to its receptors, thereby reducing its harmful effects. They are primarily used in the treatment of PAH, where they help to lower blood pressure in the pulmonary arteries, improve exercise capacity, and slow the progression of the disease. Different endothelin receptor antagonists have varying affinities for the ETA and ETB receptors. Some are selective for ETA receptors, while others block both ETA and ETB receptors.

Commonly prescribed endothelin receptor antagonists include bosentan, ambrisentan, and macitentan. These medications are typically taken orally. Treatment with endothelin receptor antagonists requires careful monitoring due to potential side effects, which can include liver abnormalities, fluid retention, and anemia. They are an important therapeutic option for patients with PAH, significantly improving outcomes and quality of life.