安帕金疗法对抗芬太尼引起的呼吸抑制。
Ampakine therapy to counter fentanyl-induced respiratory depression.
作者信息
Greer John J, Ren Jun
机构信息
Department of Physiology, Division of Neuroscience, University of Alberta, Edmonton, Alberta, Canada T6G 2S2.
出版信息
Respir Physiol Neurobiol. 2009 Aug 31;168(1-2):153-7. doi: 10.1016/j.resp.2009.02.011. Epub 2009 Mar 4.
Opioid analgesics are the most widely used and effective pharmacological agents for the treatment of acute, postoperative and chronic pain. However, activation of opiate receptors leads to significant depression of respiratory frequency in a subpopulation of patients. Here we test the hypothesis that the AMPAKINE CX717 is effective for alleviating fentanyl-induced respiratory depression without interfering with analgesia. Ampakines are a relatively new class of compounds that are in Phase II clinical trials as potential treatments for cognitive disorders and the enhancement of memory and attentiveness. They function by allosterically binding to amino-3-hydroxy-5-methyl-4-isoxazolepropionate receptors (AMPA)-type glutamate receptors and modulating the kinetics of channel closing, transmitter dissociation and desensitization. AMPA receptor mediated conductances play a central role in controlling respiratory rhythmogenesis and drive to motoneurons. Here, we demonstrate that CX717 counters fentanyl-induced respiratory depression without significantly altering analgesia and sedation, or noticeably affecting the animals' behavior. Collectively, the preclinical data demonstrate the significant potential for the use of ampakines in respiratory medicine.
阿片类镇痛药是治疗急性、术后和慢性疼痛最广泛使用且有效的药物。然而,在部分患者中,阿片受体的激活会导致呼吸频率显著降低。在此,我们检验了如下假设:AMPA 激动剂 CX717 可有效缓解芬太尼引起的呼吸抑制,且不干扰镇痛效果。AMPA 激动剂是一类相对较新的化合物,正处于 II 期临床试验阶段,有望用于治疗认知障碍以及增强记忆力和注意力。它们通过变构结合于 2-氨基-3-羟基-5-甲基-4-异恶唑丙酸受体(AMPA)型谷氨酸受体,调节通道关闭、递质解离和脱敏的动力学过程。AMPA 受体介导的电导在控制呼吸节律生成以及驱动运动神经元方面发挥着核心作用。在此,我们证明 CX717 可对抗芬太尼引起的呼吸抑制,而不会显著改变镇痛和镇静效果,也不会明显影响动物行为。总体而言,临床前数据表明 AMPA 激动剂在呼吸医学领域具有巨大的应用潜力。