EFFECTS OF FLURBIPROFEN ENANTIOMERS ON PAIN-RELATED CHEMO-SOMATOSENSORY EVOKED-POTENTIALS IN HUMAN-SUBJECTS

被引:51
作者
LOTSCH, J
GEISSLINGER, G
MOHAMMADIAN, P
BRUNE, K
KOBAL, G
机构
[1] Department of Experimental and Clinical Pharmacology and Toxicology, University of Erlangen-Nurnberg, Erlangen
关键词
CHEMO-SOMATOSENSORY; EVENT-RELATED POTENTIALS; ANALGESICS; FLURBIPROFEN; ENANTIOMERS;
D O I
10.1111/j.1365-2125.1995.tb04556.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 CO, 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.
引用
收藏
页码:339 / 346
页数:8
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