莫索尼定——第二代中枢抗高血压药

A new type antihypertensive agent

莫索尼定是第二代中枢抗高血压药，它主要作用于延髓腹外侧头端的Ｉ１咪唑啉受体，通过抑制外周交感神经活性而产生降压作用；并能有效地减轻心肌肥厚，防止心律失常发作；改善肾功能；扩瞳、降低眼内压；对唾液、胃酸的分泌及血糖、血脂代谢无不良影响。它作用于中枢α２肾上腺素受体，是产生口干、疲劳等副作用的原因，但发生率较第一代中枢降压药可乐定小得多。莫索尼定确切的降压机制仍有待于深入研究。

Moxonidine is a secondgeneration, centrally acting antihypertensive drug with a distinctive mode of action. Moxonidine activates I1imidazoline receptors (I1receptors) in the rostroventrolateral medulla (RVLM), thereby reducing the activity of the sympathetic nervous system, leading to a pronounced and longlasting blood pressure reduction. Chronic administration of moxonidine in hypertension effectively reduces the left ventricular hypertrophy and renal glomerulosclerosis. It is active against ventricular arrhythmia in a variety of experimental settings. It exerts beneficial effects on glucose metabolism and blood lipids in genetically hypertensive obese rats, and lowers intraocular pressure, suggesting a possible benefit in glaucoma. Side effects such as sedation or reduction in salive flow have been attributed only to actions at 2 adrenergic receptors of moxonidinc. Further studies are needed to verify the mechanism of this agent.