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纳布啡和氟哌啶醇单独及联合使用对健康受试者的精神运动、呼吸和神经内分泌的影响。

Psychomotor, respiratory and neuroendocrinological effects of nalbuphine and haloperidol, alone and in combination, in healthy subjects.

作者信息

Saarialho-Kere U

机构信息

Department of Pharmacology and Toxicology, University of Helsinki, Finland.

出版信息

Br J Clin Pharmacol. 1988 Jul;26(1):79-87. doi: 10.1111/j.1365-2125.1988.tb03367.x.

Abstract
  1. Actions and interactions on performance and respiration of single intramuscular doses of 0.15 mg kg-1 nalbuphine and oral haloperidol twice daily for 2 days were studied double-blind and cross-over in 12 healthy volunteers. 2. Objective measurements of performance (choice reaction, tracking, attention, flicker fusion, Maddox wing, digit symbol substitution) and respiratory function (minute volume, end-tidal carbon dioxide), and subjective assessments on visual analogue scales were done at baseline and 1 h, 2.5 h and 4 h after the injection of nalbuphine. Plasma concentrations of nalbuphine were estimated by radioreceptor ([3H]-dihydromorphine) assay, and those of prolactin and growth hormone by radioimmunoassay. 3. Nalbuphine affected digit substitution, reaction time, extraocular muscle balance and flicker recognition, and depressed respiration most clearly 1 and 2.5 h post injection. Motor skills were impaired only briefly. Haloperidol alone proved inert on performance but enhanced the decremental effects of nalbuphine on digit substitution and exophoria at 1 h. It did not interact with nalbuphine on the ventilatory function. 4. Plasma concentrations of nalbuphine expressed as morphine equivalents ranged from 5 to 52 ng ml-1, indicating considerable mu-opiate affinity. Treatment with haloperidol increased plasma prolactin moderately whilst nalbuphine raised it markedly 1 and 2.5 h post injection. Nalbuphine elevated plasma growth hormone at 1 h post injection only.
摘要
  1. 对12名健康志愿者进行了双盲交叉研究,观察单次肌内注射0.15mg/kg纳布啡以及每日口服两次氟哌啶醇,连续2天,对其行为表现和呼吸的作用及相互作用。2. 在注射纳布啡的基线、1小时、2.5小时和4小时,对行为表现(选择反应、跟踪、注意力、闪烁融合、马多克斯杆、数字符号替换)和呼吸功能(分钟通气量、呼气末二氧化碳)进行客观测量,并在视觉模拟量表上进行主观评估。通过放射受体([3H]-二氢吗啡)测定法估算纳布啡的血浆浓度,通过放射免疫测定法估算催乳素和生长激素的血浆浓度。3. 纳布啡影响数字替换、反应时间、眼外肌平衡和闪烁识别,注射后1小时和2.5小时呼吸抑制最为明显。运动技能仅短暂受损。单独使用氟哌啶醇对行为表现无影响,但在1小时时增强了纳布啡对数字替换和外隐斜的递减作用。它在通气功能方面与纳布啡无相互作用。4. 以吗啡当量表示的纳布啡血浆浓度范围为5至52ng/ml,表明其对μ-阿片受体有相当大的亲和力。氟哌啶醇治疗适度增加血浆催乳素,而纳布啡在注射后1小时和2.5小时显著升高血浆催乳素。纳布啡仅在注射后1小时升高血浆生长激素。

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