Central Acting Antihypertensive Drugs: Past, Present, and Future

The central antihypertensive drugs such as methyldopa or clonidine have been agents of importance in the therapy of hypertension. Due to the side effects and the rebound hypertensive phenomenon in the case of clonidine, the use of these agents have been clearly diminished. There are several evidences that a new type of receptor, imidazoline receptor, is present in the central nervous system and in the periphery. A specific agonist for these receptors, rilmenidine, has been studied in experimental animals and in hypertensive patients. Clinical studies have shown that rilmenidine exhibits similar efficacy but a better tolerability compared to clonidine. Rilmenidine may represent a good alternative in the therapy of hypertension.