Literature DB >> 8554936

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

J Lötsch1, G Geisslinger, P Mohammadian, K Brune, G Kobal.   

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.

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Year:  1995        PMID: 8554936      PMCID: PMC1365153          DOI: 10.1111/j.1365-2125.1995.tb04556.x

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  38 in total

1.  Cortical responses to painful CO2 stimulation of nasal mucosa; a magnetoencephalographic study in man.

Authors:  J Huttunen; G Kobal; E Kaukoranta; R Hari
Journal:  Electroencephalogr Clin Neurophysiol       Date:  1986-10

2.  Effects of flupirtine on the pain-related evoked potential and the spontaneous EEG.

Authors:  G Kobal; T Hummel
Journal:  Agents Actions       Date:  1988-02

3.  The recording of brain evoked potentials resulting from intra-articular focused ultrasonic stimulation: a new experimental model for investigating joint pain in humans.

Authors:  A Wright; I I Davies
Journal:  Neurosci Lett       Date:  1989-02-13       Impact factor: 3.046

4.  Pain-related somatosensory evoked potentials following CO2 laser stimulation in man.

Authors:  R Kakigi; H Shibasaki; A Ikeda
Journal:  Electroencephalogr Clin Neurophysiol       Date:  1989 Mar-Apr

5.  Analgesic efficacy of i.m. alfentanil.

Authors:  L Arendt-Nielsen; B Oberg; P Bjerring
Journal:  Br J Anaesth       Date:  1990-08       Impact factor: 9.166

6.  Aspirin-like drugs may block pain independently of prostaglandin synthesis inhibition.

Authors:  K Brune; W S Beck; G Geisslinger; S Menzel-Soglowek; B M Peskar; B A Peskar
Journal:  Experientia       Date:  1991-03-15

Review 7.  Evoked potentials as correlates of pain and pain relief in man.

Authors:  C R Chapman
Journal:  Agents Actions Suppl       Date:  1986

8.  Effects of pentazocine and acetylsalicylic acid on pain-rating, pain-related evoked potentials and vigilance in relationship to pharmacokinetic parameters.

Authors:  G Kobal; C Hummel; B Nuernberg; K Brune
Journal:  Agents Actions       Date:  1990-03

9.  Pentazocine and flupirtine effects on spontaneous and evoked EEG activity.

Authors:  B Bromm; R Ganzel; W M Herrmann; W Meier; E Scharein
Journal:  Neuropsychobiology       Date:  1986       Impact factor: 2.328

10.  Cerebral chemosensory evoked potentials elicited by chemical stimulation of the human olfactory and respiratory nasal mucosa.

Authors:  G Kobal; C Hummel
Journal:  Electroencephalogr Clin Neurophysiol       Date:  1988 Jul-Aug
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  11 in total

Review 1.  Preclinical and clinical development of dexketoprofen.

Authors:  D Mauleón; R Artigas; M L García; G Carganico
Journal:  Drugs       Date:  1996       Impact factor: 9.546

2.  (R)-Profens are substrate-selective inhibitors of endocannabinoid oxygenation by COX-2.

Authors:  Kelsey C Duggan; Daniel J Hermanson; Joel Musee; Jeffery J Prusakiewicz; Jami L Scheib; Bruce D Carter; Surajit Banerjee; J A Oates; Lawrence J Marnett
Journal:  Nat Chem Biol       Date:  2011-11       Impact factor: 15.040

Review 3.  Clinical pharmacokinetics of dexketoprofen.

Authors:  M J Barbanoj; R M Antonijoan; I Gich
Journal:  Clin Pharmacokinet       Date:  2001       Impact factor: 6.447

4.  Analgesic effects of propyphenazone in comparison to its combination with caffeine.

Authors:  H G Kraetsch; T Hummel; J Lötsch; R Kussat; G Kobal
Journal:  Eur J Clin Pharmacol       Date:  1996       Impact factor: 2.953

5.  Effects of azapropazone on pain-related brain activity in human subjects.

Authors:  J Lötsch; P Mohammadian; T Hummel; S Florin; K Brune; G Geisslinger; G Kobal
Journal:  Br J Clin Pharmacol       Date:  1995-12       Impact factor: 4.335

Review 6.  Pharmacological importance of stereochemical resolution of enantiomeric drugs.

Authors:  M R Islam; J G Mahdi; I D Bowen
Journal:  Drug Saf       Date:  1997-09       Impact factor: 5.228

7.  R-flurbiprofen reduces neuropathic pain in rodents by restoring endogenous cannabinoids.

Authors:  Philipp Bishay; Helmut Schmidt; Claudiu Marian; Annett Häussler; Nina Wijnvoord; Simone Ziebell; Julia Metzner; Marco Koch; Thekla Myrczek; Ingo Bechmann; Rohini Kuner; Michael Costigan; Faramarz Dehghani; Gerd Geisslinger; Irmgard Tegeder
Journal:  PLoS One       Date:  2010-05-13       Impact factor: 3.240

Review 8.  Pain treatment in multimorbid patients, the older population and other high-risk groups. The clinical challenge of reducing toxicity.

Authors:  C H Wilder-Smith
Journal:  Drug Saf       Date:  1998-06       Impact factor: 5.606

Review 9.  Druggable Targets in Endocannabinoid Signaling.

Authors:  Ann M Gregus; Matthew W Buczynski
Journal:  Adv Exp Med Biol       Date:  2020       Impact factor: 2.622

10.  R-flurbiprofen attenuates experimental autoimmune encephalomyelitis in mice.

Authors:  Katja Schmitz; Natasja de Bruin; Philipp Bishay; Julia Männich; Annett Häussler; Christine Altmann; Nerea Ferreirós; Jörn Lötsch; Alfred Ultsch; Michael J Parnham; Gerd Geisslinger; Irmgard Tegeder
Journal:  EMBO Mol Med       Date:  2014-11       Impact factor: 12.137

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