Comparative abuse liability of intravenously administered remifentanil and fentanyl
Comparative abuse liability of intravenously administered remifentanil and fentanyl
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DOI：
10.1097/00004714-200012000-00002
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发表时间：
2000-12-01
影响因子：
2.9
通讯作者：
Sellers, EM
中科院分区：
文献类型：
--
作者：
Baylon, GJ;Kaplan, HL;Sellers, EM
瑞芬太尼是一种短效酯酶代谢阿片类镇痛药。本研究通过随机、双盲、交叉研究比较了瑞芬太尼与芬太尼和安慰剂的滥用风险。12名娱乐性阿片类药物使用者通过静脉输液泵接受瑞芬太尼（0.6、1.2、1.8、2.4和3.0马克杯/千克）、芬太尼（0.4、0.8、1.3、2.0、3.0和4.5马克杯/千克）和安慰剂的剂量增加。主观测量（Cole/Addiction Research Center Inventory [ARCI]量表和视觉模拟量表[VAS]项目如“高”和“良好效果”）和生理变量（血压、O-2饱和度、瞳孔直径）被记录。对于每项测量，与基线的差异被缩小到反应曲线下面积（AUC）和峰值，每个受试者对两种活性药物类别的最大耐受剂量的反应和对几次安慰剂输注的平均反应被输入12 × 3方差分析。药物与安慰剂效应的所有差异都是显著的。虽然在药物输注后4分钟内可测量到的大多数峰值效应反映了更大的瑞芬太尼效应，但只有一个高VAS具有统计学意义。相比之下，只能在药物输注后大于或等于5分钟进行的观察主要表明芬太尼峰值效应显著增加，包括高VAS、喜欢VAS、良好效果VAS和Cole/ARCI滥用潜力。芬太尼的auc通常显著大于相应的瑞芬太尼auc。寻求更持久药物效果的吸毒者可能会选择芬太尼而不是瑞芬太尼，但这些数据并不能完全排除一些既能获得药物又能获得输注设备的人滥用瑞芬太尼的可能性，或者那些喜欢短暂、重复效果的人滥用瑞芬太尼的可能性。
Remifentanil is a short-acting, esterase-metabolized opioid analgesic. This study compared the abuse Liability of remifentanil with that of fentanyl and placebo in a randomized, double-blind, crossover study. Twelve recreational users of opioids received increasing doses of remifentanil (0.6, 1.2, 1.8, 2.4, and 3.0 mug/kg), fentanyl (0.4, 0.8, 1.3, 2.0, 3.0, and 4.5 mug/kg) and placebo via an intravenous infusion pump. Subjective measures (Cole/Addiction Research Center Inventory [ARCI] scales and visual analog scale [VAS] items such as "High" and "Good Effects") and physiologic variables (blood pressure, O-2 saturation, pupil diameter) were recorded. For each measure, the differences from baseline were reduced to an area under the response curve (AUC) and a peak, and each subject's response to the maximum tolerable dose for each of the two active drug classes and mean response to several placebo infusions were entered into a 12 x 3 analysis of variance. All differences in drug versus placebo effects were significant. Although a majority of the peak effects that were measurable within 4 minutes after drug infusion reflected greater remifentanil effects, only one, High VAS, was statistically significant. In contrast, observations that could only be made greater than or equal to5 minutes after drug infusion predominantly indicated significantly greater fentanyl peak effects, including High VAS, Liking VAS, Good Effects VAS, and Cole/ARCI Abuse Potential. Fentanyl AUCs were generally significantly larger than the corresponding remifentanil AUCs. A drug abuser seeking longer-lasting drug effects might select fentanyl over remifentanil, but these data do not completely rule out remifentanil abuse by some individuals with access to both the drug and the infusion equipment or by those who prefer briefer, repeated effects.