Articles: opioid-analgesics.
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The haemodynamic and respiratory-depressive effects of 20 micrograms/kg and 40 micrograms/kg of alfentanil in 54 patients with coronary bypass operation were compared with a control group (n = 36). The measurements were carried out at 3 different times, each lasting over a 10 min period: 1. Before induction of anaesthesia but after premedication with flunitrazepam. 2. ⋯ In the intraoperative period this did not occur. The respiratory depression(paO2: -34%, paCO2: +29%) resembles that after fentanyl, except that it starts earlier and lasts for a shorter time. In summary, it can be stated that all effects after alfentanil are similar to those of fentanyl.
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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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Acta Anaesthesiol Belg · Jan 1983
Comparative StudyClinical evaluation of the analgesic potency of lofentanil in postoperative pain.
The efficacy and safety of IM lofentanil, the most potent morphinomimetic drug available, for rapid control of postoperative pain was compared with IM piritramide and placebo in a study of 120 patients. Piritramide 7.5 mg and 15 mg, lofentanil 0.25 micrograms, 0.50 micrograms and 0.75 micrograms had a rapid onset of analgesic effect. ⋯ There were no significant differences in pain relief between the different doses of lofentanil or between the different doses of piritramide. Side effects of very low incidence included nausea, vomiting and sedation in both piritramide and lofentanil groups.
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Clinical neurosurgery · Jan 1983
Treatment of chronic pain of malignant origin with intrathecal opiates.
The acute administration of intrathecal morphine in man results in analgesia mediated by an opiate receptor. Chronically infused intraspinal opiates have an analgetic action mediated by opiate receptors. ⋯ There appear to be at least two classes of opiate receptors in the human and animal spinal cords which mediate analgesia. Our preliminary data suggest that, as in the animal model, DADL, a delta-ligand, shows significant activity in a morphine-tolerant spinal cord.