Abstract

BEVACQUA, Raúl J.; BORTMAN, Guillermo  and  PERRONE, Sergio V.. Endothelin receptor antagonists for pulmonary arterial hypertension. Insuf. card. [online]. 2013, vol.8, n.2, pp.77-94. ISSN 1852-3862.

Pulmonary arterial hypertension (PAH) is a consequence of acute or chronic disorder of the pulmonary vasculature, which is characterized by increased pulmonary artery pressure as a result of increased pulmonary vascular resistance. The pathophysiology of PAH is characterized by pulmonary vascular vasoconstriction, smooth muscle cell proliferation, and thrombosis. These changes are a result of an imbalance between vasodilators (prostacyclin, nitric oxide, vasoactive intestinal peptide) and vasoconstrictors (thromboxane A₂, endothelin, serotonin), growth inhibitors and mitogenic factors, and antithrombotic and prothrombotic factors. Recent advances in treatment are directed at restoring the balance between these systems. Endothelin receptor antagonists (bosentan, ambrisentan), phosphodiesterase type 5 inhibitors (sildenafil, tadalafil), and prostacylin (epoprostenol, iloprost, treprostinil, beraprost) represent the different classes of medications that are currently used in monotherapy and in combination to treat PAH. The purpose of this review is to provide the reader with an update on the treatment of PAH with antagonists of endothelin receptors.

Keywords : Pulmonary arterial hypertension; Pathophysiological pathways; Endothelin receptor antagonist; Bosentan; Ambrisentan; Combination therapy.

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