纳洛酮、哌替啶和颤抖。

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Kurz M, Belani公斤,Sessler DI, Kurz,拉尔森博士,施罗德M,布兰查德D

纳洛酮、哌替啶和颤抖。

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

PubMed ID

8267194 (在PubMed

]

文摘

背景:哌替啶,结合μ和κ阿片受体,据说更有效治疗颤抖比equianalgesic剂量的吗啡(近纯mu-receptor受体激动剂)。此外,布托啡诺kappa-receptor受体激动剂/拮抗剂,对待颤抖比芬太尼,主要结合μ受体。这些数据表明,哌替啶的特殊antishivering活动可能是由其卡帕活动。因此,作者测试假设哌替啶将最低限度的antishivering活动受低剂量纳洛酮(大多数mu-receptors阻塞),但在很大程度上预防大剂量纳洛酮(阻塞所有μ和大多数κ受体)。方法:12个志愿者每个参加2天。在这两天,颤抖是中央静脉输液引起的冷流体。二十分钟后,6个志愿者服用安慰剂注入生理盐水的一天,或注入0.5 microgram.kg-1。最低为1盐酸纳洛酮(“低剂量”,旨在阻止μ受体)。第二组的6个志愿者被盐水丸和注入一天,或一丸11.5微克/公斤盐酸纳洛酮注入纳洛酮在5 micrograms.kg-1紧随其后。最低为1(“高剂量”,旨在阻止μ和κ受体)在另一天。继续输液的时间学习。治疗的顺序天(生理盐水与纳洛酮)是随机分配,双盲研究。 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.

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药物靶点

药物	目标	类	生物	药理作用	行动
哌替啶	Kappa-type阿片受体	蛋白质	人类	是的	不可用	细节