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克罗卡林(BRL 34915)对健康志愿者的心血管影响。

Cardiovascular effects of cromakalim (BRL 34915) in healthy volunteers.

作者信息

Fox J S, Whitehead E M, Shanks R G

机构信息

Department of Therapeutics and Pharmacology, Queen's University of Belfast, Northern Ireland.

出版信息

Br J Clin Pharmacol. 1991 Jul;32(1):45-9. doi: 10.1111/j.1365-2125.1991.tb05611.x.

Abstract
  1. The effect of oral doses of cromakalim 0.5, 1.0, 1.5 and 2.0 mg on several cardiovascular parameters was studied in healthy male volunteers. 2. In the first study, no dose of cromakalim reduced systolic or diastolic blood pressure in the supine or standing position. Reductions of diastolic blood pressure after exercise (P less than 0.01) were observed 4 h after administration of 2.0 mg. 3. There was a trend towards increased heart rate after 2.0 mg at all time intervals, and significant changes were observed in supine and standing heart rate at 2 and 4 h (P less than 0.01). No significant change was observed in exercise heart rate. 4. In the second study small increases in forearm blood flow were observed from 3 h to 5 h after oral administration of 1.0 and 2.0 mg of cromakalim. Forearm vascular resistance was significantly reduced after 2.0 mg (P less than 0.025) when compared with placebo. No change was observed in forearm venous capacitance after either dose of cromakalim, or placebo. Supine heart rate was significantly increased 4 h after 2.0 mg of cromakalim (P less than 0.025). 5. These results show that oral administration of cromakalim decreases diastolic blood pressure and forearm vascular resistance. A hypotensive effect is probably attenuated by reflex tachycardia.
摘要
  1. 在健康男性志愿者中研究了口服剂量为0.5、1.0、1.5和2.0毫克的克罗卡林对多个心血管参数的影响。2. 在第一项研究中,无论仰卧位还是站立位,克罗卡林的任何剂量均未降低收缩压或舒张压。服用2.0毫克后4小时观察到运动后舒张压降低(P<0.01)。3. 在所有时间间隔内,服用2.0毫克后心率有升高趋势,在仰卧位和站立位时,2小时和4小时的心率有显著变化(P<0.01)。运动心率无显著变化。4. 在第二项研究中,口服1.0和2.0毫克克罗卡林后3小时至5小时观察到前臂血流量略有增加。与安慰剂相比,服用2.0毫克后前臂血管阻力显著降低(P<0.025)。服用克罗卡林或安慰剂后,前臂静脉容量均无变化。服用2.0毫克克罗卡林后4小时仰卧位心率显著升高(P<0.025)。5. 这些结果表明,口服克罗卡林可降低舒张压和前臂血管阻力。降压作用可能因反射性心动过速而减弱。

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