The NSAID dexketoprofen trometamol is as potent as mu-opioids in the depression of wind-up and spinal cord nociceptive reflexes in normal rats.
The aim of this study was to examine the potency of the antinociceptive effects of the non-steroidal antiinflammatory drug (NSAID), Dexketoprofen Trometamol (the active enantiomer of ketoprofen) on spinal cord nociceptive reflexes. These effects were compared with those of the mu-opioid receptor agonist fentanyl in normal animals. The experiments were performed in male Wistar rats anaesthetised with alpha-chloralose. The nociceptive reflexes were recorded as single motor units in peripheral muscles, activated by mechanical and electrical stimulation. Both dexketoprofen and fentanyl inhibited responses evoked by mechanical and electrical stimulation with doses in the same nanomolar range (dexketoprofen ID50s: 100 and 762 nmol kg-1 and fentanyl: 40 and 51 nmol kg-1, respectively). Dexketoprofen and fentanyl also significantly inhibited wind-up. Since fentanyl has been shown to be some 1000 times more potent than morphine in this type of experiments, we conclude that dexketoprofen has central analgesic actions in normal animals and depresses nociceptive responses with a potency similar to that of mu-opioid agonists.
Mazario
J
J
Departamento de Fisiología, Facultad de Medicina, Campus Universitario, Universidad de Alcalá, Alcalá de Henares, 28871, Madrid, Spain.
Roza
C
C
Herrero
J F
JF
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D001812:Blood-Brain Barrier; D003864:Depression, Chemical; D004558:Electric Stimulation; D005283:Fentanyl / Q000494:pharmacology*; D007660:Ketoprofen / Q000494:pharmacology*; D008297:Male; D010146:Pain / Q000503:physiopathology*; D051381:Rats; D017208:Rats, Wistar; D017450:Receptors, Opioid, mu / Q000819:agonists*; D012016:Reference Values; D012018:Reflex / Q000187:drug effects*; D013237:Stereoisomerism; D013314:Stress, Mechanical
D000894:Anti-Inflammatory Agents, Non-Steroidal; D017450:Receptors, Opioid, mu; D007660:Ketoprofen; D005283:Fentanyl