Amin H M, Sopchak A M, Esposito B F, Henson L G, Batenhorst R L, Fox A W, Camporesi E M
Department of Anesthesiology, State University of New York, Syracuse, USA.
J Pharmacol Exp Ther. 1995 Jul;274(1):34-9.
Remifentanil is a new mu opioid analgesic of the synthetic phenylpiperidine class. It has an extremely short half-life (10-20 min) due to its breakdown by nonspecific estrases. We studied the effects of continuous infusion of remifentanil, compared with alfentanil, on the respiratory response to hypoxia. In addition, we examined the efficacy of naloxone to reverse remifentanil-mediated depression of respiration. Spontaneous recovery after the end of the infusion was also assessed. Twelve adult males participated in the study. On three sessions, separated by 7 to 14 days, the participants received continuous infusion over 240 min of alfentanil (0.5 microgram/kg/min), remifentanil (0.025 microgram/kg/min) or remifentanil (0.1 microgram/kg/min). Naloxone (6 micrograms/kg) was given at 95 min. On a fourth session, remifentanil (0.1 microgram/kg/min) was infused and placebo was given instead of naloxone. Base-line hypoxic challenge was induced at 30 min before starting the infusion. Eight hypoxic challenges were conducted at 10 min after starting the infusion and half-hourly thereafter. Two postinfusion challenges were performed at 250 and 280 min. The slope (liter/min/SPO2) of the ventilatory response and the predicted ventilation at SPO2 of 80% (VE80) (liter/min) significantly decreased during the infusion with remifentanil and alfentanil. A significant difference was noted between the two doses of remifentanil. Naloxone administration was associated with reversal of the depressed hypoxic responses during the infusion of alfentanil and the low dose of remifentanil. Termination of remifentanil infusion was associated with a prompt spontaneous recovery of the blunted hypoxic responses that was not detected with alfentanil.(ABSTRACT TRUNCATED AT 250 WORDS)
瑞芬太尼是一种新型的合成苯基哌啶类μ阿片类镇痛药。由于其被非特异性酯酶分解,它具有极短的半衰期(10 - 20分钟)。我们研究了与阿芬太尼相比,持续输注瑞芬太尼对低氧呼吸反应的影响。此外,我们还检测了纳洛酮逆转瑞芬太尼介导的呼吸抑制的效果。同时也评估了输注结束后的自发恢复情况。12名成年男性参与了该研究。在间隔7至14天的三个时间段中,参与者接受了240分钟的阿芬太尼(0.5微克/千克/分钟)、瑞芬太尼(0.025微克/千克/分钟)或瑞芬太尼(0.1微克/千克/分钟)的持续输注。在95分钟时给予纳洛酮(6微克/千克)。在第四个时间段,输注瑞芬太尼(0.1微克/千克/分钟)并给予安慰剂而非纳洛酮。在开始输注前30分钟进行基线低氧刺激。在开始输注后10分钟及之后每半小时进行8次低氧刺激。在250和280分钟进行两次输注后刺激。在输注瑞芬太尼和阿芬太尼期间,通气反应的斜率(升/分钟/血氧饱和度)以及血氧饱和度为80%时的预测通气量(VE80)(升/分钟)显著降低。两种剂量的瑞芬太尼之间存在显著差异。在输注阿芬太尼和低剂量瑞芬太尼期间,给予纳洛酮可使低氧反应的抑制得到逆转。停止输注瑞芬太尼后,低氧反应迅速自发恢复,而阿芬太尼未观察到这种情况。(摘要截选至250字)