(为靶标的阿片类药物曲马多了兴奋性性质的角色——一个临床前研究使用alfentanil作为比较)。

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Freye E, Latasch L·冯·Bredow G,聂鲁达B

(为靶标的阿片类药物曲马多了兴奋性性质的角色——一个临床前研究使用alfentanil作为比较)。

Schmerz。1998年2月28日,12(1):19到24。

PubMed ID

12799988 (在PubMed

]

文摘

曲马多、吗啡的镇痛与意味着力量十分之一经常用于治疗慢性和术后疼痛。先前的报道表明,曲马多可能诱发癫痫活动时一起选择性5 -羟色胺再摄取抑制剂(SSRI)。因此,它的主要作用方式可能会质疑,据称是由于与阿片受体结合,部分是由于抑制单胺再摄取。因此我们开始研究其潜在的诱发癫痫活动和量化影响EEG-power光谱和中央调制清醒的感觉传入纤维和受过专门训练的狗(n = 7)。为了演示如果阿片受体介导这些影响,增量剂量曲马多有这是紧随其后的是纳洛酮可能逆转。在冲洗时间相同的动物暴露在分级剂量alfentanil,纯mu-receptor受体激动剂。这是紧随其后的是阿片拮抗物纳洛酮逆转。脑电图(EEG)和与事件相关的诱发电位(9)被用来演示可能兴奋性的影响。为了推导出9月前爪子是电刺激(第吉尔机枪兵II商标)而从躯体感觉诱发电位是捡起侧皮层电极使用粘贴上去的。256扫描平均(Lifescan)和峰振幅测量证明中枢神经系统励磁控制(%)。 Additionally, the raw electroencephalogram was viewed for epileptogenic changes and its power computed into the various power bands alpha, beta, delta und theta using FFT over a time epoch of 60 s. Following control, graded doses of either tramadol (2-5-10 mg/kg i.v.) or alfentanil (10-30-60 microg/kg i.v.) were given every 15 min while the EEG and the SEP were recorded. Thereafter naloxone (20 microg/kg i.v.) was injected for reversal. Tramadol did not suppress the amplitude of the SEP at any dose. High doses (>5 mg/kg i.v.) resulted in an increase (+100%) of the amplitude of the evoked potential. This was accompanied by short-term muscle fibrillations, and a short-term spike-and-wave activity in the EEG followed by a long-lasting theta-dominance. These effects could not be reversed by naloxone. In contrast to tramadol, alfentanil induced a dose-related depression of amplitude in the SEP with a maximum of 82% suggesting a depressive effect of modulation of afferents in the sensory cortex. This effect was fully naloxone reversible and was followed by a rebound in amplitude of the SEP together with an increase in fast beta-waves in the EEG. Tramadol very little mediates its central action via the mu-opioid receptor as the present effects were not naloxone reversible. Consistent with the results is the very low affinity of tramadol to the opioid receptor which is several thousand times less than that of morphine. Most likely, inhibition of central norepinephrine and serotonin reuptake as well as the reduction in 5-HT-turnover may contribute to the effects of tramadol. Due to the monoamine reuptake inhibition an increase in transmission may result, triggering off excitatory phenomena with spike-and-wave activity in the CNS. Such excitatory effects, however, may only be seen when tramadol is used in doses exceeding the therapeutic range.

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药物靶点

药物	目标	类	生物	药理作用	行动
烯丙羟吗啡酮	Mu-type阿片受体	蛋白质	人类	是的	拮抗剂	细节