Conant J, Engler R, Janowsky D, Maisel A, Gilpin E, LeWinter M
Department of Medicine, VA Medical Center, San Diego, CA 92161.
J Cardiovasc Pharmacol. 1989 Apr;13(4):656-61.
beta-adrenergic blocking agents have undesirable effects believed to be mediated through the central nervous system (CNS). If these effects are due to direct CNS action, less lipid soluble agents ought to have fewer effects. Accordingly, several formal psychological tests of items such as mood, motivation, and anxiety were used in a double-blinded crossover study in 17 hypertensive subjects taking equipotent beta blocking agents with high (propranolol) and low (atenolol) lipid solubility. Patients had less negative effects (p less than 0.05) on 12 of 21 items evaluated with atenolol compared to propranolol while peripheral beta blockade [beta 1, exercise heart rate (HR), and blood pressure (BP)] was equivalent. These results suggest that the mental changes which accompany beta blockade therapy are mediated directly in the CNS and that less soluble drugs can be expected to have fewer CNS effects.
β-肾上腺素能阻滞剂具有一些不良作用,据信这些作用是通过中枢神经系统(CNS)介导的。如果这些作用是由于直接的中枢神经系统作用,那么脂溶性较低的药物应该具有较少的作用。因此,在一项双盲交叉研究中,对17名服用具有高(普萘洛尔)和低(阿替洛尔)脂溶性的等效β受体阻滞剂的高血压患者,使用了几种关于情绪、动机和焦虑等项目的正式心理测试。与普萘洛尔相比,使用阿替洛尔评估的21个项目中的12个项目,患者的负面影响较小(p小于0.05),而外周β受体阻滞[β1、运动心率(HR)和血压(BP)]相当。这些结果表明,β受体阻滞剂治疗伴随的精神变化是由中枢神经系统直接介导的,并且可以预期脂溶性较低的药物具有较少的中枢神经系统作用。