Department of Anaesthesia and Intensive Care, Royal Adelaide Hospital, University of Adelaide, Adelaide, Australia.
Eur J Anaesthesiol. 2010 Mar;27(3):241-6. doi: 10.1097/EJA.0b013e328331a361.
Pain relief using intermittent subcutaneous injections of an opioid (e.g. morphine) avoids the need for venous access and does not require complex or expensive pumps and devices. Although data on the pharmacokinetics of subcutaneous morphine exist, there are no comparable data for fentanyl in healthy volunteers. Therefore, the aim of this study was to characterize the pharmacokinetics of 200 microg fentanyl administered as a single bolus dose via the subcutaneous route in healthy opioid-naive volunteers.
Nine healthy male volunteers were given 200 microg of subcutaneous fentanyl for more than 30 s. Opioid effects were blocked by administration of naltrexone. Venous blood samples taken at intervals from 5 min to 10 h after the dose were assayed using a liquid chromatography-mass spectrometry method. Pharmacokinetic data were analysed using a noncompartmental analysis approach.
After subcutaneous bolus dose administration, the median maximum concentration of fentanyl was 0.55 ng ml(-1) (range 0.28-0.87 ng ml(-1)), reached at a median time of 15 min (range 10-30 min). The terminal half-life was 10.00 h (range 5.48-16.37 h).
Absorption of subcutaneous fentanyl was relatively rapid and similar to the rate of absorption previously reported for subcutaneous morphine; the terminal half-life for fentanyl was substantially longer (10 h) than that of morphine (2.1 h), and blood concentrations were no more variable than that after administration by other nonintravenous routes.
使用阿片类药物（如吗啡）间歇性皮下注射来缓解疼痛，可避免静脉通路的需要，且不需要复杂或昂贵的泵和设备。虽然有关于皮下注射吗啡药代动力学的数据，但在健康志愿者中，没有类似芬太尼的数据。因此，本研究的目的是描述健康的阿片类药物初治志愿者单次皮下给予 200μg 芬太尼时的药代动力学特征。
9 名健康男性志愿者接受超过 30 秒的 200μg 芬太尼皮下注射。给予纳曲酮阻断阿片类药物的作用。在给药后 5 分钟至 10 小时的间隔时间内采集静脉血样，使用液相色谱-质谱法进行检测。使用非房室分析方法对药代动力学数据进行分析。
皮下推注给药后，芬太尼的中位数最大浓度为 0.55ng/ml（范围 0.28-0.87ng/ml），中位数达峰时间为 15 分钟（范围 10-30 分钟）。终末半衰期为 10.00 小时（范围 5.48-16.37 小时）。
皮下芬太尼的吸收相对较快，与先前报告的皮下吗啡吸收速率相似；芬太尼的终末半衰期明显长（10 小时）于吗啡（2.1 小时），且血药浓度的变异性不比其他非静脉途径给药后更大。
