Abstract
Alpha2 agonists including rilmenidine, clonidine and α methylnoradrenaline all seem to have a predominantly central action in lowering blood pressure.Studies using the peripheral decarboxylase inhibitor α-methyldopa hydrazine in both experimental animals and humans support the predominant central action of the active metabolite of methyldopa, α methylnoradrenaline.Comparative studies on the antihypertensive potency of selective α2 agonists like rilmenidine, guanfacine, clonidine and lofexidine suggest that the relative ability to bind to α1 andα2 adrenoceptors is not critical but the ability to enter the central nervous system is essential for antihypertensive efficacy.
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