Lechi A, Picotti G B, Covi G, Pomari S, Pedrolli E, Cesura A M, Danti G, Mattioli M
Arzneimittelforschung. 1981;31(3):524-6.
2-Hydroxy-(1-hydroxy-[(1-methyl-3-phenylpropyl)amino]-2-ethyl)-5-benzamide (labetalol), a new alpha- and beta-adrenergic blocking agent, was employed in 21 patients with severe hypertension by slow (6 patients) and rapid (15 patients) i.v. infusion. A marked and significant fall of blood pressure was observed in both groups, though more gradual in patients treated by slow infusion. A rapid blood pressure fall with cardiac output decrease was observed by passing from supine to standing position in the first hours after infusion. Therefore, it is advisable to keep a supine position for a few hours. Plasma renin activity decreased after labetalol infusion, but basal plasma renin levels were not related to hypotensive effect of labetalol. In slow infusion patients, plasma noradrenaline levels increased and no changes of plasma adrenaline levels were observed during infusion. The most likely explanation of these variations is an increase of sympathetic activity secondary to hypotension, caused by labetalol, whereas a technical interference seems to be excluded. The simultaneous blockade of alpha- and beta-receptors can inhibit, in this case, the pressor effects of the sympathetic reflex.
2-羟基-(1-羟基-[(1-甲基-3-苯基丙基)氨基]-2-乙基)-5-苯甲酰胺(拉贝洛尔),一种新型的α和β肾上腺素能阻滞剂,通过缓慢静脉输注(6例患者)和快速静脉输注(15例患者)用于21例重度高血压患者。两组患者均观察到血压显著下降,尽管缓慢输注治疗的患者下降更为渐进。输注后的最初几个小时内,从仰卧位变为站立位时,观察到血压快速下降且心输出量减少。因此,建议保持仰卧位几个小时。拉贝洛尔输注后血浆肾素活性降低,但基础血浆肾素水平与拉贝洛尔的降压效果无关。在缓慢输注的患者中,血浆去甲肾上腺素水平升高,输注期间未观察到血浆肾上腺素水平变化。对这些变化最可能的解释是拉贝洛尔引起的低血压继发交感神经活动增加,而技术干扰似乎可以排除。在这种情况下,α和β受体的同时阻断可以抑制交感反射的升压作用。