纳洛酮，哌替啶，还有发抖。

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Kurz M, Belani KG, Sessler DI, Kurz A, Larson MD, Schroeder M, Blanchard D

纳洛酮，哌替啶，还有发抖。

麻醉学。1993 12月;79(6):1193-201。doi: 10.1097 / 00000542-199312000-00009。

PubMed ID

8267194 (PubMed视图

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摘要

背景:据报道，与等镇痛剂量的吗啡(一种几乎纯的阿片受体激动剂)相比，能结合mu和kappa阿片受体的哌嗪在治疗寒颤方面更有效。此外，布托啡诺，一种kappa受体激动剂/拮抗剂，比芬太尼更好地治疗颤抖，芬太尼主要结合mu受体。这些数据表明，哌替啶的许多特殊抗冻活性可能是由其kappa活性介导的。因此，作者验证了以下假设:低剂量纳洛酮(阻断大多数mu-受体)将最低限度地损害哌嗪的抗寒颤活性，但高剂量纳洛酮(阻断所有mu和大多数kappa受体)将在很大程度上阻止哌嗪的抗寒颤活性。方法:12名志愿者每人参加2天。两日均以中心静脉输注冷液诱发寒战。20分钟后，6名志愿者在一天内接受了安慰剂输注生理盐水，或输注0.5微克。kg-1。另一种是Min-1盐酸纳洛酮(“低剂量”，旨在阻断mu受体)。第二组6名志愿者在一天内注射生理盐水，或者注射11.5微克/公斤的盐酸纳洛酮，然后注射5微克.公斤-1的纳洛酮。Min-1(“高剂量”，旨在阻断mu和kappa受体)。在整个研究过程中，持续输液。治疗天数的顺序(生理盐水和纳洛酮)是随机分配的，研究是双盲的。 Fifteen minutes after the test infusion was started, all 12 volunteers were given an intravenous bolus of 1 mg/kg meperidine hydrochloride. Pupillary diameter and light reflex amplitude were used to quantify opioid-receptor agonist activity; shivering intensity was evaluated using oxygen consumption. RESULTS: Administration of naloxone alone did not alter oxygen consumption, pupil size, or the pupillary light reflex. No pupillary constriction was detected in either group when naloxone and meperidine were combined; in contrast, meperidine alone decreased pupil size and amplitude of the light reflex 30%. The meperidine bolus decreased oxygen consumption nearly to control values when the volunteers were given saline placebo. Combined administration of meperidine and low-dose naloxone also significantly reduced oxygen consumption, but the reduction and the duration of the reduction was less than during saline. When the volunteers were given high-dose naloxone, meperidine only slightly reduced oxygen consumption, and the values rapidly returned to premeperidine levels. CONCLUSIONS: These data indicate that the antishivering property of meperidine is not fully mediated by mu-receptors. Although meperidine has well-known nonopioid actions, stimulation of kappa receptors seems a likely alternative explanation for much of the drug's antishivering action.

引用本文的药物库数据

药物靶点

药物	目标	种类	生物	药理作用	行动
哌替啶	kappa型阿片受体	蛋白质	人类	是的	不可用	细节