Remifentanil offers a wide range of clinical uses and has been successfully
combined with general anesthetics. However, there are few human experiment
al studies demonstrating the analgesic property of remifentanil. It was our
aim to determine the analgesic effect of remifentanil with regard to dose-
dependent increments in a human model of heat pain threshold assessment. Tw
enty healthy volunteers were randomized in a double-blinded cross-over desi
gn to receive an infusion of remifentanil or saline. The stepped infusion w
as increased every 5 min by 0.01 mug(.)kg(-1.)min(-1) up to 0.17 mug(.)kg(-
1)min(-1) and terminated in case of defined safety limits. Thermal sensory
testing of the heat pain threshold was performed every 5 min at the left fo
rearm. The dose-response relationship and the effective dose for at least 5
0% of the subjects (ED50) were determined. Remifentanil led to a clear dose
-dependent increase of the heat pain threshold differing significantly from
placebo (P < 0.0007). The ED50 of remifentanil equals 0.05 <mu>g(.)kg(-1.)
min(-1) (first quartile 0.025 mug(.)kg(-1.)min(-1) and third quartile 0.06
mug(.)kg(-1).min(-1)) in this experimental setting. In conclusion, an opioi
d-mediated analgesic effect of remifentanil was determined in a human heat
pain threshold model. The dose of 0.05 mug(.)kg(-1.)min(-1) is an effective
and safe increment in healthy volunteers.