Takakura S, Satoh Y, Satoh H, Mori J, Kohsaka M
Department of Pharmacology, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Arch Int Pharmacodyn Ther. 1992 Sep-Oct;319:38-48.
The effects of an intravenous injection of the novel calcium channel blocker, nilvadipine, on the relative regional cerebral blood flow and relative regional skin blood flow were studied in anesthetized cats using the laser-Doppler method. The effects of nilvadipine were compared with those of nicardipine hydrochloride (nicardipine). Nilvadipine and nicardipine both increased the relative regional cerebral blood flow dose-dependently, in spite of their hypotensive effect. At a dose of 32 micrograms/kg, nilvadipine and nicardipine increased the relative regional cerebral blood flow by 61 +/- 8% and 25 +/- 10% of the predrug value, respectively, 15 min after administration. At this time, both drugs induced a comparable degree of hypotension: -18 +/- 3% of the predrug value for nilvadipine and -25 +/- 2% for nicardipine. After nilvadipine, the relative regional cerebral blood flow enhanced by 45 +/- 10% 180 min after drug administration, whereas after nicardipine, it returned to the predrug value within 60 min. In contrast, the increase in relative regional skin blood flow produced by nilvadipine (32 micrograms/kg) and nicardipine (32 micrograms/kg) was 23 +/- 15% and 32 +/- 8% of the predrug value, respectively, 5 min after drug administration. The effect of nicardipine on the relative regional skin blood flow, compared with that of control, was significantly higher. These results indicate that nilvadipine exhibits a pronounced and longer-lasting effect on the relative regional cerebral blood flow, compared with the relative regional skin blood flow, and that its action on the relative regional cerebral blood flow is more potent than that of nicardipine.
采用激光多普勒法，在麻醉猫身上研究了新型钙通道阻滞剂尼伐地平静脉注射对相对局部脑血流量和相对局部皮肤血流量的影响。将尼伐地平的作用与盐酸尼卡地平（尼卡地平）的作用进行了比较。尽管尼伐地平和尼卡地平都有降压作用，但二者均剂量依赖性地增加相对局部脑血流量。给药后15分钟，在剂量为32微克/千克时，尼伐地平和尼卡地平分别使相对局部脑血流量比给药前的值增加61±8%和25±10%。此时，两种药物引起的低血压程度相当：尼伐地平为给药前值的-18±3%，尼卡地平为-25±2%。给予尼伐地平后，给药180分钟后相对局部脑血流量增加45±10%，而给予尼卡地平后，在60分钟内恢复到给药前值。相比之下，给药5分钟后，尼伐地平（32微克/千克）和尼卡地平（32微克/千克）引起的相对局部皮肤血流量增加分别为给药前值的23±15%和32±8%。与对照组相比，尼卡地平对相对局部皮肤血流量的影响显著更高。这些结果表明，与相对局部皮肤血流量相比，尼伐地平对相对局部脑血流量表现出明显且持久的作用，并且其对相对局部脑血流量的作用比尼卡地平更强。
