Title : Clinical pharmacology of aprocitentan (an endothelin receptor antagonist) – The most recent quality progress in treatment of resistant hypertension
Abstract:
Hypertension is a common condition characterized by persistently high blood pressure (140/90 mmHg or higher). Lowering high blood pressure reduces the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions. Regardless of outstanding results and improvements in the pharmacological management of hypertension, clinical programs in patients remaining hypertensive despite a minimum of three drugs at their optimal dose, and sometimes even up to six antihypertensives, clearly suggested a need for further investigations and transformational progress in this field. It has been determined that endothelin-1 (ET-1), a potent vasoconstrictor, was implicated in the pathogenesis of hypertension. By targeting the ET transduction signaling pathway, to this point several vasoactive substances were identified to inhibit the binding of ET-1 to ET(A) and ET(B) receptors, to reduce the harmful effects of ET-1, including vasoconstriction, fibrosis, cell proliferation, endothelial dysfunction progression, as well as local inflammation. Aprocitentan is a recently registered endothelin receptor antagonist prescribed for the combination treatment of hypertension that is not adequately controlled with other drugs. Given the previous facts, the main objectives of this presentation will be to clarify the pharmacological properties of aprocitentan, including pharmacodynamics, pharmacokinetics, indications, and contraindications for use, adverse drug reactions, as well as the most important drug interactions. This will provide a better understanding of this new-in-pharmacotherapy drug for resistant hypertension, consequently helping clinicians in its suitable prescribing and adequate clinical use.
