Articles: analgesics.
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J. Pharmacol. Exp. Ther. · Mar 1983
Relative involvement of mu, kappa and delta receptor mechanisms in opiate-mediated antinociception in mice.
The antinociceptive properties of morphine (mu), ethylketazocine (kappa), nalorphine (kappa), [D-Ala2, D-Leu5]enkephalin (delta) and [D-Ala2, Met5]enkephalinamide (mu, delta) were assessed using the radiant heat tail-flick and acetic acid-induced writhing assays in mice. The apparent pA2 values for the interaction of naloxone with morphine were the same regardless of the nociceptive stimulus employed or the route of administration of morphine. The apparent pA2 values for the interactions of naloxone with ethylketazocine and nalorphine in the writhing test differed significantly from that for the interaction of morphine and naloxone. ⋯ The apparent pA2 values for the interactions of naloxone with [D-Ala2, D-Leu5] enkephalin differed from those for morphine-naloxone interactions on the writhing test. The highly selective mu antagonist beta-funaltrexamine antagonized the agonist actions of morphine and [D-Ala2, D-Leu5]enkephalin, and, in a previous study, beta-funaltrexamine antagonized the antinociceptive actions of [D-Ala2, Met5]enkephalinamide, but not those of nalorphine. It was concluded that agonist interaction with mu or kappa receptors can result in antinociceptive effects in the acetic acid-induced writhing test, and that an agonist interaction with mu, but not kappa, receptors results in antinociceptive action on the radiant heat tail-flick test, and furthermore, that a possible combination of mu and delta receptor interaction can result in antinociceptive activity in both tests.
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Randomized Controlled Trial Comparative Study Clinical Trial
A 12-hour evaluation of the analgesic efficacy of diflunisal, zomepirac sodium, aspirin, and placebo in postoperative oral surgery pain.
One hundred ninety-nine outpatients with pain following oral surgery were randomly assigned, on a double-blind basis, a single oral dose of diflunisal (500 or 1,000 mg), zomepirac sodium 100 mg, aspirin 650 mg, or placebo. Using a self-rating record, subjects rated their pain and its relief hourly for 12 hours after medication. Measures of total and peak analgesia were derived from these patients' subjective reports. ⋯ Diflunisal 500 and 1,000 mg were comparable to zomepirac in peak analgesia and significantly superior to zomepirac for all measures of total analgesia. The onset of analgesia was comparable for 1,000 mg diflunisal, zomepirac, and aspirin, but more rapid for these treatments than for 500 mg diflunisal. The duration of analgesia was 12 hours for diflunisal, 9 hours for zomepirac, and 3 hours for aspirin.
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The incidence of pain in 170 children recovering from surgery was surveyed in two major teaching hospitals along with an analysis of analgesic medication prescribed and administered. Analgesic medication was not ordered for 16% of the patients and narcotic analgesic medication ordered was not given for 39% of the patients. In 29% of the patients, where an order for "narcotic or non-narcotic analgesic medication' was written, the non-narcotic drug was given exclusively. ⋯ Others expressed a dread of "the needle' as a way of administering analgesics and preferred to suffer pain to an injection. We have concluded that there is considerable scope to improve pain management in children after surgery. This improvement must be based on improved education of medical and nursing staff in contemporary clinical pharmacology and on improved communication between staff, parents and patients.