Sica Domenic A
Division of Nephrology, Medical College of Virginia, Virginia Commonwealth University, Richmond, VA 23298-0160, USA.
J Clin Hypertens (Greenwich). 2007 May;9(5):399-405. doi: 10.1111/j.1524-6175.2007.07161.x.
Centrally acting agents stimulate alpha(2) receptors and/or imadozoline receptors on adrenergic neurons situated within the rostral ventrolateral medulla and, in so doing, sympathetic outflow is reduced. Centrally acting agents also stimulate peripheral alpha(2) receptors, which, for the most part, is of marginal clinical significance. Central a agonists have had a lengthy history of use, starting with alpha-methyldopa, which has had a dramatic decline in use, in part, because of bothersome side effects. Patients who require multidrug therapy with otherwise resistant hypertension, such as diabetic and/or renal failure patients, are typically responsive to these drugs, as are patients with sympathetically driven forms of hypertension. Perioperative forms of hypertension respond well to clonidine, a circumstance where the additional anesthesia- and analgesia-sparing effects of this drug may offer additional clinical benefits. Clonidine can be used adjunctively with other more traditional therapies in heart failure, particularly when hypertension is present. Sustained-release moxonidine, however, is associated with early mortality and morbidity when used in patients with heart failure. Escalating doses of drugs in this class often give rise to salt and water retention, in which case diuretic therapy becomes a valuable adjunctive therapy.
中枢作用药物刺激位于延髓头端腹外侧的肾上腺素能神经元上的α₂受体和/或咪唑啉受体，从而减少交感神经输出。中枢作用药物还刺激外周α₂受体，在很大程度上，这在临床上意义不大。中枢性α激动剂有很长的使用历史，始于α-甲基多巴，其使用量已大幅下降，部分原因是其令人烦恼的副作用。需要联合多种药物治疗的顽固性高血压患者，如糖尿病和/或肾衰竭患者，通常对这些药物有反应，交感神经驱动型高血压患者也是如此。围手术期高血压对可乐定反应良好，在这种情况下，该药物额外的麻醉和镇痛作用可能会带来更多临床益处。可乐定可与心力衰竭的其他更传统疗法联合使用，尤其是在存在高血压时。然而，缓释莫索尼定用于心力衰竭患者时与早期死亡率和发病率相关。这类药物剂量增加往往会导致盐和水潴留，在这种情况下，利尿剂治疗成为一种有价值的辅助治疗。
