[Analgesic activity of a non-steroidal anti-inflammatory agent, tolmetin sodium in experimental animals (author's transl)].

Abstract

Effect of tolmetin sodium on the pain-like responses caused by various nociceptive stimuli was examined in experimental animals. Tolmetin sodium showed a potent inhibitory activity on the acetic acid-induced writhing in mice and rats, and its potency, (ED50 = 23.4 and 3.01 mg/kg, p.o.) was about 2.4--10.3 times that of ibuprofen and aspirin. The hypertension induced by intraarterial injection of bradykinin toward the spleen of dogs was inhibited by tolmetin sodium (ED50 = 80 mg/kg, i.v.), but the hypertension by a simultaneous injection of bradykinin and PGE1 was not inhibited by tolmetin sodium and sulpyrine, though pentazocine inhibited both hypertensions. The pain-like response caused by pressing mechanically the inflamed paws or joints of rats induced by kaolin-carrageenin or adjuvant was inhibited by tolmetin sodium (30--100 or 20--40 mg/kg, p.o., respectively), and the potency was approximately equal that of ibuprofen and phenylbutazone. Tolmetin sodium produced a significant inhibition of the pain-like response induced by electrical stimulation of tooth pulp of dogs, but showed no effect when the methods of Haffner and D'Amour-Smith were applied to mice. Anti-writhing action of tolmetin sodium was not antagonized by naloxone. From these results, it was concluded that tolmetin sodium has a potent inhibitory activity on the pain-like responses induced by the chemical nociceptive stimuli and by the mechanical pressure stimulus of the inflamed tissue, especially on the writhing. The analgesic activity probably involves a peripheral mechanism.

• Authors: H Nakamura, K Ishii, S Motoyoshi, C Imazu, Y Yokoyama, M Shimizu
• Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica (Nihon Yakurigaku Zasshi) Vol. 75 Issue 4 Pg. 405-17 (May 1979) ISSN: 0015-5691 [Print] Japan
• PMID: 535831 (Publication Type: English Abstract, Journal Article)

Chemical References

• Analgesics
• Anti-Inflammatory Agents
• Pyrroles
• Naloxone
• Tolmetin
• Bradykinin

Topics

• Analgesics
• Animals
• Anti-Inflammatory Agents (antagonists & inhibitors, pharmacology)
• Blood Pressure (drug effects)
• Bradykinin (antagonists & inhibitors)
• Dogs
• Female
• Male
• Naloxone (pharmacology)
• Pyrroles (pharmacology)
• Rats
• Tolmetin (antagonists & inhibitors, pharmacology)