Wenzel R R, Spieker L, Qui S, Shaw S, Lüscher T F, Noll G
Departments of Cardiology, Cardiovascular Research, and Clinical Research, University Hospital, Inselspital, Bern; (Switzerland).
Hypertension. 1998 Dec;32(6):1022-7. doi: 10.1161/01.hyp.32.6.1022.
Moxonidine is an I1-imidazoline receptor agonist that reduces blood pressure in hypertensives. Experimental data suggest that moxonidine inhibits central sympathetic activity. However, whether such a mechanism is involved in vivo in humans is still unclear. We investigated the effects of 0.4 mg moxonidine orally on muscle sympathetic nerve activity and heart rate in an open study in 8 healthy volunteers. Furthermore, we studied the effects of 0.4 mg moxonidine on muscle sympathetic nerve activity, heart rate, blood pressure, 24-hour blood pressure profile, and hormone plasma levels in 25 untreated hypertensives in a double-blind, placebo-controlled study. Moxonidine decreased muscle sympathetic nerve activity in both healthy volunteers (P<0.05 versus baseline) and hypertensives (P<0.02 versus placebo). Plasma norepinephrine also decreased (P<0. 01), whereas plasma epinephrine and renin levels did not change (P=NS). Furthermore, moxonidine decreased systolic (P<0.0001) and diastolic (P<0.001) blood pressure. Heart rate decreased after moxonidine in healthy subjects (P<0.05); in hypertensives, heart rate decreased during the night hours (P<0.05) but not during daytime (P=NS). Plasma levels of LDL, HDL, and total cholesterol were not influenced by the drug (P=NS). Moxonidine decreases systolic and diastolic blood pressure by inhibiting central nervous sympathetic activity. This makes this new drug suitable for the treatment of human hypertension and possibly for other cardiovascular diseases with increased sympathetic nerve activity, ie, ischemic heart disease and heart failure.
莫索尼定是一种I1-咪唑啉受体激动剂，可降低高血压患者的血压。实验数据表明，莫索尼定可抑制中枢交感神经活动。然而，这种机制在人体体内是否起作用仍不清楚。在一项针对8名健康志愿者的开放性研究中，我们研究了口服0.4毫克莫索尼定对肌肉交感神经活动和心率的影响。此外，在一项双盲、安慰剂对照研究中，我们研究了0.4毫克莫索尼定对25名未经治疗的高血压患者的肌肉交感神经活动、心率、血压、24小时血压曲线以及激素血浆水平的影响。莫索尼定可降低健康志愿者（与基线相比，P<0.05）和高血压患者（与安慰剂相比，P<0.02）的肌肉交感神经活动。血浆去甲肾上腺素也降低了（P<0.01），而血浆肾上腺素和肾素水平没有变化（P=无显著性差异）。此外，莫索尼定可降低收缩压（P<0.0001）和舒张压（P<0.001）。在健康受试者中，服用莫索尼定后心率降低（P<0.05）；在高血压患者中，夜间心率降低（P<0.05），但白天没有降低（P=无显著性差异）。药物对血浆低密度脂蛋白、高密度脂蛋白和总胆固醇水平没有影响（P=无显著性差异）。莫索尼定通过抑制中枢神经交感神经活动来降低收缩压和舒张压。这使得这种新药适用于治疗人类高血压，也可能适用于治疗交感神经活动增强的其他心血管疾病，即缺血性心脏病和心力衰竭。
