Karasawa A, Nomura H, Nito M, Sonoda R, Tanaka H, Kosaka N, Yamaguchi K, Kobayashi S
Pharmaceutical Research Institute, Kyowa Hakko Kogyo, Co., Ltd., Shizuoka, Japan.
Nihon Yakurigaku Zasshi. 1999 May;113(5):317-26. doi: 10.1254/fpj.113.317.
We investigated the effects of benidipine hydrochloride (benidipine, Coniel) on blood pressure, heart rate and plasma norepinephrine (NE) concentration in spontaneously hypertensive rats and compared them with those of other calcium channel blockers. Benidipine (2 mg/kg, p.o.) was compared with the equihypotensive doses of nifedipine (5 mg/kg), cilnidipine (6 mg/kg) and amlodipine (3 mg/kg). All the 4 calcium channel blockers exhibited significant antihypertensive effects. Nifedipine and cilinidipine significantly increased heart rate, as compared with that in the control group, whereas benidipine or amlodipine did not significantly affect it. The area under the curves for hypotensive effect and tachycardic effect for 10 hr after the drug administration were compared among the 4 compounds. As a result, the tachycardic effect of benidipine was significantly lower than those of nifedipine, cilnidipine and amlodipine, while the hypotensive effects were similar among the 4 compounds. Nifedipine and amlodipine, significantly increased plasma NE concentration, cilnidipine tended to increase it. In contrast, benidipine did not significantly affect plasma NE concentration. These results suggest that the effects of benidipine on plasma NE concentration and heart rate are less prominent than those of the other calcium channel blockers.
我们研究了盐酸贝尼地平（贝尼地平，可力洛）对自发性高血压大鼠血压、心率及血浆去甲肾上腺素（NE）浓度的影响，并将其与其他钙通道阻滞剂进行比较。将贝尼地平（2毫克/千克，口服）与硝苯地平（5毫克/千克）、西尼地平（6毫克/千克）和氨氯地平（3毫克/千克）的等效降压剂量进行比较。所有4种钙通道阻滞剂均表现出显著的降压作用。与对照组相比，硝苯地平和西尼地平显著增加心率，而贝尼地平或氨氯地平对心率无显著影响。比较了4种化合物给药后10小时降压作用和心动过速作用的曲线下面积。结果，贝尼地平的心动过速作用显著低于硝苯地平、西尼地平和氨氯地平，而4种化合物的降压作用相似。硝苯地平和氨氯地平显著增加血浆NE浓度，西尼地平有增加趋势。相比之下，贝尼地平对血浆NE浓度无显著影响。这些结果表明，贝尼地平对血浆NE浓度和心率的影响不如其他钙通道阻滞剂显著。
