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外周阿片受体的激活对心率变异性没有影响。

Activation of peripheral opioid receptors has no effect on heart rate variability.

作者信息

Ellidokuz Ender, Kaya Dayimi, Uslan Ihsan, Celik Ataç, Esen Ali Metin, Barutça Irfan

机构信息

Department of Internal Medicine and Gastroenterology, School of Medicine, Celal Bayar University, Manisa, Turkey.

出版信息

Clin Auton Res. 2008 Jun;18(3):145-9. doi: 10.1007/s10286-008-0469-9. Epub 2008 Apr 30.

DOI:10.1007/s10286-008-0469-9
PMID:18449593
Abstract

Opioid receptors involved in regulating the motility of the gastrointestinal tract have been localized in both contractile and neuronal tissues. Trimebutine, a peripheral opioid receptor agonist, modulates gastrointestinal motor activity in both directions and also may act on cardiac tissue. This study investigated the effects of trimebutine in clinical doses on cardiac autonomic functions with heart rate variability. The effect of trimebutine on cardiac autonomic outflows was evaluated in 11 healthy subjects. Trimebutine (200 mg) or placebo was administered orally at random in a double-blind, cross-over manner. Continuous electrocardiography recordings were obtained before and after drug administration during three states: rest, controlled breathing, and a hand grip exercise. Heart rate variability analysis showed that there was no significant difference between subjects administered with placebo or trimebutine throughout rest, controlled breathing, or the hand grip exercise. We concluded that trimebutine, in clinical doses, has no significant effect on cardiac autonomic functions.

摘要

参与调节胃肠道蠕动的阿片受体已定位在收缩组织和神经组织中。曲美布汀是一种外周阿片受体激动剂,可双向调节胃肠运动活动,也可能作用于心脏组织。本研究通过心率变异性研究了临床剂量曲美布汀对心脏自主神经功能的影响。在11名健康受试者中评估了曲美布汀对心脏自主神经输出的影响。曲美布汀(200mg)或安慰剂以双盲、交叉方式随机口服给药。在休息、控制呼吸和握力运动三种状态下,给药前后均进行连续心电图记录。心率变异性分析表明,在整个休息、控制呼吸或握力运动过程中,服用安慰剂或曲美布汀的受试者之间没有显著差异。我们得出结论,临床剂量的曲美布汀对心脏自主神经功能没有显著影响。

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Activation of peripheral opioid receptors has no effect on heart rate variability.外周阿片受体的激活对心率变异性没有影响。
Clin Auton Res. 2008 Jun;18(3):145-9. doi: 10.1007/s10286-008-0469-9. Epub 2008 Apr 30.
2
The action of trimebutine maleate on gastrointestinal motility is mediated by opiate receptors in human subjects.马来酸曲美布汀对人体胃肠道动力的作用是由阿片受体介导的。
Gastroenterol Clin Biol. 1987;11(3 Pt 2):102B-104B.
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J Gastroenterol. 2002;37(11):888-95. doi: 10.1007/s005350200150.
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[Effects of trimebutine on motility of the small intestine in humans].曲美布汀对人体小肠运动的影响
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The involvement of opiate receptors in the effects of trimebutine on intestinal motility in the conscious dog.阿片受体在曲美布汀对清醒犬肠道运动影响中的作用
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Peripheral antagonistic action of trimebutine and kappa opioid substances on acoustic stress-induced gastric motor inhibition in dogs.曲美布汀和κ阿片类物质对犬声应激诱导的胃运动抑制的外周拮抗作用。
Eur J Pharmacol. 1988 Jan 27;146(1):57-63. doi: 10.1016/0014-2999(88)90486-4.

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本文引用的文献

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Pharmacokinetic and bioequivalence evaluation of two formulations of 100 mg trimebutine maleate (Recutin and Polybutin) in healthy male volunteers using the LC-MS/MS method.采用液相色谱-串联质谱法(LC-MS/MS)对100毫克马来酸曲美布汀两种制剂(Recutin和Polybutin)在健康男性志愿者中的药代动力学和生物等效性进行评估。
Clin Chim Acta. 2007 Jan;375(1-2):69-75. doi: 10.1016/j.cca.2006.06.006. Epub 2006 Jun 14.
2
The effect of dopamine type-2 receptor blockade on autonomic modulation.多巴胺2型受体阻断对自主神经调节的影响。
Clin Auton Res. 2003 Aug;13(4):275-80. doi: 10.1007/s10286-003-0097-3.
3
The effect of metoclopramide on QT dynamicity: double-blind, placebo-controlled, cross-over study in healthy male volunteers.
甲氧氯普胺对QT间期动态变化的影响:在健康男性志愿者中进行的双盲、安慰剂对照、交叉研究。
Aliment Pharmacol Ther. 2003 Jul 1;18(1):151-5. doi: 10.1046/j.1365-2036.2003.01641.x.
4
Fine tuning of sympathetic transmitter release via ionotropic and metabotropic presynaptic receptors.通过离子型和代谢型突触前受体对交感神经递质释放进行精细调节。
Pharmacol Rev. 2002 Mar;54(1):43-99. doi: 10.1124/pr.54.1.43.
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QT interval effects of cisapride in the clinical setting.西沙必利在临床环境中的QT间期效应。
Int J Cardiol. 2001 Sep-Oct;80(2-3):179-83. doi: 10.1016/s0167-5273(01)00485-5.
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Modulation of sympathetic actions on the heart by opioid receptor stimulation.阿片受体刺激对心脏交感神经活动的调节作用。
J Biomed Sci. 2001 Jul-Aug;8(4):299-306. doi: 10.1007/BF02258370.
7
Opioids and cardioprotection.阿片类药物与心脏保护作用
Pharmacol Ther. 2001 Feb;89(2):123-37. doi: 10.1016/s0163-7258(00)00106-6.
8
Domperidone should not be considered a no-risk alternative to cisapride in the treatment of gastrointestinal motility disorders.在治疗胃肠动力障碍方面,不应将多潘立酮视为西沙必利的无风险替代药物。
Circulation. 2000 Oct 17;102(16):1883-5. doi: 10.1161/01.cir.102.16.1883.
9
Identification of opioid receptors in the sympathetic and parasympathetic nerves of guinea-pig atria.豚鼠心房交感神经和副交感神经中阿片受体的鉴定。
Fundam Clin Pharmacol. 2000 Jul-Aug;14(4):387-94. doi: 10.1111/j.1472-8206.2000.tb00420.x.
10
Effects of trimebutine maleate on delayed rectifier K+ currents in guinea-pig ventricular myocytes.马来酸曲美布汀对豚鼠心室肌细胞延迟整流钾电流的影响。
J Pharm Pharmacol. 2000 Apr;52(4):403-8. doi: 10.1211/0022357001774156.