Effects of flurbiprofen enantiomers on pain-related chemo-somatosensory evoked potentials in human subjects

Br J Clin Pharmacol. 1995 Oct;40(4):339-46. doi: 10.1111/j.1365-2125.1995.tb04556.x.

Abstract

1. The aim of the study was to investigate the analgesic effects of flurbiprofen enantiomers using an experimental pain model based on both chemo-somatosensory event-related potentials (CSSERP) and subjective pain ratings. 2. Healthy female volunteers (n = 16, age 23-36 years) participated in a placebo-controlled, randomised, double-blind, four-way crossover study. Single doses of (S)-flurbiprofen (50 mg), (R)-flurbiprofen (50 and 100 mg) and placebo were administered orally. Measurements were taken before and 2 h after administration of the medications. During each measurement, 32 painful stimuli of gaseous carbon dioxide (200 ms duration, interval approximately 30 s) of two concentrations (60 and 65% CO2 v/v) were applied to the right nostril. EEG was recorded from five positions and CSSERP were obtained in response to the painful CO2- stimuli. Additionally, subjects rated the perceived intensity of the painful stimuli by means of a visual analogue scale (VAS). 3. The CSSERP-amplitude P2, a measure of analgesic effect, decreased after administration of both (R)- and (S)-flurbiprofen, while it increased after placebo. This was statistically significant at recording positions C4 (P < 0.01) and Fz (P < 0.05). The analgesia-related decreases in evoked potential produced by (R)-flurbiprofen were dose-dependent. Comparing similar doses of (R)- and (S)-flurbiprofen, the decrease in CSSERP-amplitudes produced by the (S)-enantiomer was somewhat more pronounced, indicating a higher analgesic potency. 4. The present data indicate that both enantiomers of flurbiprofen produce analgesic effects. Since (R)-flurbiprofen caused only little toxicity in rats as compared with the (S)-enantiomer or the racemic compound, a reduction of the quantitatively most important side effects in the gastrointestinal tract might be achieved by employing (R)-flurbiprofen in pain therapy.

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Analgesics / adverse effects
  • Analgesics / blood
  • Analgesics / chemistry
  • Analgesics / pharmacology*
  • Double-Blind Method
  • Electroencephalography
  • Evoked Potentials, Auditory / drug effects
  • Evoked Potentials, Somatosensory / drug effects*
  • Female
  • Flurbiprofen / adverse effects
  • Flurbiprofen / blood
  • Flurbiprofen / chemistry
  • Flurbiprofen / pharmacology*
  • Humans
  • Pain / physiopathology*
  • Placebos
  • Stereoisomerism

Substances

  • Analgesics
  • Placebos
  • Flurbiprofen