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盐酸兰地洛尔的剂量探索研究:一种用于控制日本冠状动脉计算机断层扫描血管造影时心率的短效β1-受体阻滞剂。

Dose-finding study of landiolol hydrochloride: a short-acting β1-blocker for controlling heart rate during coronary computed-tomography angiography in Japan.

机构信息

Department of Cardiology, Tokyo Medical University, 6-7-1, Nishi-shinjuku, Shinjuku-ku, Tokyo, 160-0023, Japan,

出版信息

Adv Ther. 2013 Sep;30(9):803-18. doi: 10.1007/s12325-013-0053-0. Epub 2013 Sep 24.

Abstract

INTRODUCTION

Coronary computed-tomography angiography (CCTA) has high diagnostic performance, but it sometimes does not allow evaluation because of artifacts. Currently, the use of a β-blocker is recommended to prevent motion artifacts, but the β-blocker (metoprolol, propranolol, etc.) commonly used has a slow onset and long duration of action. Landiolol hydrochloride is an intravenous β1-blocker with a very short half-life. We investigated the efficacy and optimal dose of this drug for reduction of heart rate in patients undergoing CCTA.

METHODS

Eighty-seven subjects with ischemic heart disease were divided into three groups to receive landiolol hydrochloride at a dose of 0.125 (Group L), 0.25 (Group M), or 0.5 mg/kg (Group H). CCTA was performed at 3-7 min after administration, and heart rate, blood pressure, and image quality were assessed.

RESULTS

Heart rate decreased rapidly after completion of landiolol hydrochloride administration in all groups, with a heart rate reduction of 15.55 ± 6.56% in Group L, 16.48 ± 7.80% in Group M, and 21.49 ± 6.13% in Group H (Group L vs Group H, P = 0.0008; Group M vs Group H, P = 0.0109). Since there was no significant difference in heart rate during imaging among the three groups, although there was a significant difference between groups L and H and groups M and H in terms of percent change in heart rate, coronary stenosis was diagnosable in all groups with no significant difference.

CONCLUSION

Landiolol hydrochloride showed a rapid onset and short β-blocking effect, and was most effective at a dose of 0.5 mg/kg. However, the diagnosable proportion had no significant differences among the three groups in CCTA. Therefore, the clinically recommended dose was 0.125 mg/kg or less, considering the heart rate of patients with suspected coronary stenosis during CCTA.

摘要

简介

冠状动脉计算机断层扫描血管造影(CCTA)具有较高的诊断性能,但有时由于伪影而无法进行评估。目前,建议使用β受体阻滞剂来预防运动伪影,但常用的β受体阻滞剂(美托洛尔、普萘洛尔等)起效慢、作用时间长。盐酸拉贝洛尔是一种具有极短半衰期的静脉用β1受体阻滞剂。我们研究了该药在接受 CCTA 的患者中降低心率的疗效和最佳剂量。

方法

87 例缺血性心脏病患者分为三组,分别接受盐酸拉贝洛尔 0.125mg/kg(L 组)、0.25mg/kg(M 组)或 0.5mg/kg(H 组)。给药后 3-7 分钟行 CCTA,评估心率、血压和图像质量。

结果

三组患者在完成盐酸拉贝洛尔给药后心率均迅速下降,L 组心率下降 15.55±6.56%,M 组下降 16.48±7.80%,H 组下降 21.49±6.13%(L 组与 H 组比较,P=0.0008;M 组与 H 组比较,P=0.0109)。由于三组患者在成像期间心率无显著差异,尽管 L 组和 H 组、M 组和 H 组之间的心率变化百分比有显著差异,但所有组的冠状动脉狭窄均能诊断,且无显著差异。

结论

盐酸拉贝洛尔起效迅速,β阻断作用时间短,0.5mg/kg 剂量最有效。然而,在 CCTA 中,三组之间的可诊断比例没有显著差异。因此,考虑到 CCTA 中疑似冠状动脉狭窄患者的心率,推荐的临床剂量为 0.125mg/kg 或更低。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f62c/3824371/ebf14d8a0bfc/12325_2013_53_Fig1_HTML.jpg

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