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在兔子身上,新型超短效β受体阻滞剂兰地洛尔比艾司洛尔具有更强的负性变时作用,而对血压的影响较小。

In rabbits, landiolol, a new ultra-short-acting beta-blocker, exerts a more potent negative chronotropic effect and less effect on blood pressure than esmolol.

作者信息

Sasao J, Tarver S D, Kindscher J D, Taneyama C, Benson K T, Goto H

机构信息

Department of Anesthesiology, University of Kansas Medical Center, Kansas City, Kansas 66160-7415, USA.

出版信息

Can J Anaesth. 2001 Nov;48(10):985-9. doi: 10.1007/BF03016588.

Abstract

PURPOSE

To compare the cardiovascular and sympathetic effects of a new ultra-short-acting, highly cardioselective beta- blocker, landiolol, with esmolol, using an in vivo rabbit model.

METHODS

Different bolus doses of landiolol (0.3, 1.0, 3.0 and 10.0 mgkg(-1)) or esmolol (0.5, 1.5 and 5.0 mgkg(-1)) were given intravenously, and the effects on heart rate (HR) mean arterial pressure (MAP) and renal sympathetic nerve activity (RSNA) were compared.

RESULTS

Both landiolol and esmolol produced a dose-dependent decrease in HR. The maximum percent reductions of HR were similar with landiolol 3 mgkg(-1) and esmolol 5 mgkg(-1) (-14.0 +/- 0.9% and -13.9 +/- 1.4%, mean +/- SE, respectively). HR decreased more rapidly with landiolol than with esmolol. Esmolol produced a dose-dependent decrease in MAP that was not observed with landiolol. The percent maximum reduction of MAP was -38.2 +/- 3.2% with esmolol 5 mg*kg(-1). RSNA increased in a dose-dependent fashion with esmolol, but no changes were noted with landiolol.

CONCLUSION

These results suggest that, in rabbits, landiolol has slightly more potent negative chronotropic action than esmolol with significantly less effects on blood pressure.

摘要

目的

使用体内兔模型,比较新型超短效、高心脏选择性β受体阻滞剂兰地洛尔与艾司洛尔对心血管和交感神经的作用。

方法

静脉注射不同推注剂量的兰地洛尔(0.3、1.0、3.0和10.0mg·kg⁻¹)或艾司洛尔(0.5、1.5和5.0mg·kg⁻¹),并比较其对心率(HR)、平均动脉压(MAP)和肾交感神经活动(RSNA)的影响。

结果

兰地洛尔和艾司洛尔均使HR呈剂量依赖性降低。兰地洛尔3mg·kg⁻¹和艾司洛尔5mg·kg⁻¹时HR的最大降低百分比相似(分别为-14.0±0.9%和-13.9±1.4%,均值±标准误)。兰地洛尔使HR降低的速度比艾司洛尔更快。艾司洛尔使MAP呈剂量依赖性降低,而兰地洛尔未观察到这种情况。艾司洛尔5mg·kg⁻¹时MAP的最大降低百分比为-38.2±3.2%。艾司洛尔使RSNA呈剂量依赖性增加,而兰地洛尔未观察到变化。

结论

这些结果表明,在兔中,兰地洛尔的负性变时作用比艾司洛尔略强,对血压的影响明显较小。

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