Ando K, Noda H, Ogata E, Fujita T
Fourth Department of Internal Medicine, University of Tokyo School of Medicine, Japan.
J Cardiovasc Pharmacol. 1992 Jul;20(1):7-10.
To clarify the hemodynamic and endocrine mechanisms of the hypotensive effect of amosulalol, an alpha- and beta-adrenoceptor antagonist, 19 patients with essential hypertension received amosulalol (20-80 mg/day; average 48.4 mg/day) for 16 weeks. Mean blood pressure (MBP) was significantly decreased (105 +/- 1 vs. 120 +/- 1 mm Hg, p less than 0.001), associated with a decrement in heart rate (HR). Although both cardiac index (CI, 3.68 +/- 0.09 vs. 3.91 +/- 0.09 L/min/m2, p less than 0.001) and total peripheral resistance index (TPRI, 2,271 +/- 78 vs. 2,441 +/- 79 dynes.s.cm-5.m2, p less than 0.001) were reduced, changes in TPRI positively correlated with those of MBP (r = 0.9155, p less than 0.001) but the change in CI did not (r = 0.3568, NS). Plasma renin activity (PRA, 0.55 +/- 0.09 vs. 0.95 +/- 0.14 ng/ml/h, p less than 0.05) and aldosterone concentration (4.6 +/- 0.4 vs. 8.6 +/- 0.5 ng/dl, p less than 0.001) were also decreased with amosulalol. Thus, the hypotensive effect of amosulalol may be due mainly to vasodilation by alpha 1-blocking action. In addition, this hypotensive effect may be facilitated by either beta-blocking action such as decreased cardiac output (CO), with suppression of reflex tachycardia or of the renin-angiotensin-aldosterone system.
为阐明α、β肾上腺素能受体拮抗剂阿罗洛尔降压作用的血流动力学和内分泌机制,19例原发性高血压患者接受阿罗洛尔治疗(20 - 80毫克/天;平均48.4毫克/天),疗程16周。平均血压(MBP)显著下降(105±1对120±1毫米汞柱,p<0.001),同时心率(HR)降低。虽然心脏指数(CI,3.68±0.09对3.91±0.09升/分钟/平方米,p<0.001)和总外周阻力指数(TPRI,2271±78对2441±79达因·秒·厘米⁻⁵·平方米,p<0.001)均降低,但TPRI的变化与MBP的变化呈正相关(r = 0.9155,p<0.001),而CI的变化则不然(r = 0.3568,无显著性差异)。阿罗洛尔治疗后血浆肾素活性(PRA,0.55±0.09对0.95±0.14纳克/毫升/小时,p<0.05)和醛固酮浓度(4.6±0.4对8.6±0.5纳克/分升,p<0.001)也降低。因此,阿罗洛尔的降压作用可能主要归因于α₁阻断作用引起的血管舒张。此外,这种降压作用可能通过β阻断作用得以加强,如心输出量(CO)降低、反射性心动过速受抑制或肾素 - 血管紧张素 - 醛固酮系统受抑制。