Moxonidine: pharmacology, clinical pharmacology and clinical profile

Management strategies in hypertension evolve in response to an increased understanding of underlying pathophysiological processes and developments and refinements in drug treatments. Recent research has identified the regulatory role of the imidazoline (I1) receptor in sympathetic outflow and blood pressure regulation and this has led to the development of moxonidine, a highly selective centrally acting antihypertensive agent. At a practical level, moxonidine is suitable for single daily dosing in hypertension. Furthermore, in comparative studies moxonidine has a low incidence of symptomatic adverse effects comparable, for example, to that of the ACE inhibitor drugs, captopril and enalapril. The antihypertensive efficacy of moxonidine has now been established in a series of comparative clinical trials against all other first-line antihypertensive drug classes but, in line with current concepts, it may be necessary to look beyond blood pressure reduction. For example, centrally acting agents are known to be effective for promoting the regression of LV hypertrophy and studies in hypertensive patients have shown that antihypertensive treatment with moxonidine successfully leads to significant reductions in LV mass indices. Furthermore, there is now evidence that moxonidine has a beneficial effect on insulin sensitivity such that there are likely to be improvements in the overall metabolic profile. Thus, the clinical characteristics of moxonidine indicate that it is well suited for consideration among the first-line antihypertensive treatment choices.