Comparative abuse liability of intravenously
administered remifentanil and fentanyl
by
Baylon GJ, Kaplan HL, Somer G, Busto UE, Sellers EM
Department of Pharmacology,
and Centre for Research in Women's Health,
University of Toronto,
Ontario, Canada.
J Clin Psychopharmacol 2000 Dec; 20(6): 597-606

ABSTRACT

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 microg/kg), fentanyl (0.4, 0.8, 1.3, 2.0, 3.0, and 4.5 microg/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, O2 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 > or = 5 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.

Morphine
Fentanyl
Tramadol
Naloxone
Sufentanil
Oxycodone
Carfentanil
Endomorphins
Fentanyl : structure
Fentanyl and ketamine
Remifentanil: structure
Opioids and anaesthesia
Remifentanil/ muscular pain
Super-additive reward of remifentanil plus cocaine

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