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右美托咪定对健康受试者心血管及副交感神经的影响。

Cardiovascular and parasympathetic effects of dexmedetomidine in healthy subjects.

作者信息

Penttilä Jani, Helminen Antti, Anttila Markku, Hinkka Susanna, Scheinin Harry

机构信息

Department of Pharmacology and Clinical Pharmacology, University of Turku, Finland.

出版信息

Can J Physiol Pharmacol. 2004 May;82(5):359-62. doi: 10.1139/y04-028.

Abstract

We evaluated the cardiovascular effects of intravenously (i.v.) and buccally administered dexmedetomidine, a selective alpha2-adrenoceptor agonist. Six healthy male subjects were studied unmedicated and after 2 micro g/kg i.v. or buccal doses of dexmedetomidine, using repeated recordings of ECG and blood pressure. Cardiac parasympathetic activity was estimated by measurements of high-frequency (HF) heart rate variability. Intravenous, but not buccal, dexmedetomidine raised systolic blood pressure by 11 +/- 5 mmHg (mean +/- SEM) and diastolic by 16 +/- 3 mmHg (maxima at 10 min). Later on, both i.v., and buccal dexmedetomidine produced a very similar hypotensive effect: on average, >or=10 mmHg reductions in systolic and diastolic pressure at 3 h. Intravenous dosing was followed by a decline in heart rate (-11 +/- 2 beats/min) accompanied by a trend toward enhanced HF variability (maximal effect at 10 min), which probably reflected baroreflex-mediated parasympathetic efferent neuronal activation. Buccal dexmedetomidine increased significantly the HF variability (maximum at 45 min) without influencing heart rate. We conclude that dexmedetomidine, when administered by a method that avoids concentration peaks, e.g., buccal dosing, can be used to produce a prolonged augmentation of cardiac parasympathetic efferent neuronal activity.

摘要

我们评估了静脉注射(i.v.)和经颊给药的右美托咪定(一种选择性α2肾上腺素能受体激动剂)对心血管系统的影响。对6名健康男性受试者在未用药时以及静脉注射2μg/kg或经颊给予右美托咪定后进行了研究,采用重复记录心电图和血压的方法。通过测量高频(HF)心率变异性来评估心脏副交感神经活动。静脉注射而非经颊给药的右美托咪定使收缩压升高11±5 mmHg(平均值±标准误),舒张压升高16±3 mmHg(10分钟时达到最大值)。随后,静脉注射和经颊给药的右美托咪定均产生了非常相似的降压效果:平均而言,3小时时收缩压和舒张压降低≥10 mmHg。静脉给药后心率下降(-11±2次/分钟),同时高频变异性有增强趋势(10分钟时达到最大效应),这可能反映了压力反射介导的副交感传出神经元激活。经颊给予右美托咪定显著增加了高频变异性(45分钟时达到最大值),但不影响心率。我们得出结论,当通过避免浓度峰值的方法给药时,例如经颊给药,右美托咪定可用于延长心脏副交感传出神经元活动的增强。

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