Articles: narcotic-antagonists.
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This study performed in freely moving rats evaluated the ability of specific opioid receptor antagonists to reverse the inhibitory effects of morphine on carrageenin-induced c-Fos expression in the spinal cord. Our study focused on the superficial dorsal horn (laminae I-II), which is the main termination site of nociceptive primary afferent fibers and is rich in opioid receptors. In order to replicate clinical routes of administration, all agents were administered intravenously (i.v.). ⋯ In contrast, nor-binaltorphimine (nor-BNI-1+1 mg/kg), a kappa-opioid receptor antagonist, had no significant effect on the effects of morphine. These results indicate the major contribution of mu-opioid receptors to the antinociceptive effects of systemic morphine at the level of the superficial dorsal horn. The observed effect of NTI is not necessarily related to a direct action of morphine on delta-opioid receptors and some possible actions of this antagonist are discussed.
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Randomized Controlled Trial Clinical Trial
Effects of prophylactic nalmefene on the incidence of morphine-related side effects in patients receiving intravenous patient-controlled analgesia.
Opioid-related side effects associated with intravenous patient-controlled analgesia can be reduced by a low-dose naloxone infusion. The influence of nalmefene, a pure opioid antagonist with a longer duration of action, on opioid-related side effects has not been evaluated. This study was designed to determine the dose-response relation for nalmefene for the prevention of morphine-related side effects in patients receiving intravenous patient-controlled analgesia. ⋯ Compared with placebo, prophylactic administration of nalmefene significantly decreased the need for antiemetics and antipruritic medications in patients receiving intravenous patient-controlled analgesia with morphine.
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Noxious mechanical and chemical stimuli were applied to the toes of the left hind limb of decerebrated, spinalized rabbits and their effects on a hind limb spinal withdrawal reflex and expression of Fos-like immunoreactivity in the spinal cord were measured. The animals were prepared so as to minimize nociceptive inputs arising from surgery. A single crush stimulus applied with a pair of haemostatic forceps caused long-lasting (c. 20 min) inhibition of reflexes evoked in medial gastrocnemius motoneurons by electrical stimulation of the skin at the heel. ⋯ Opioid-mediated inhibition of the heel-gastrocnemius withdrawal reflex of the rabbit was evoked by noxious mechanical but not by chemical stimulation of the toes. Of these stimuli, the former gave rise to greater activation of neurons in central and lateral lamina I of segments L7 and S1, the region of termination of afferent fibres from the heel and the location of some enkephalin-positive neuronal cell bodies. Thus, noxious mechanical stimulation of the toes elicits inhibition of the heel-gastrocnemius withdrawal reflex, probably via activation of enkephalinergic neurons in the lateral half of lamina I in the L7 and S1 segments.
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Anesthesia and analgesia · Mar 1999
Randomized Controlled Trial Comparative Study Clinical TrialA comparison among nalbuphine, meperidine, and placebo for treating postanesthetic shivering.
Postanesthetic shivering (PS) is distressing for patients and may induce a variety of complications. In this prospective, double-blinded, randomized study, we evaluated the value of nalbuphine, compared with meperidine and saline, for treating PS. Ninety adult patients were included in the study. Group 1 (n = 30) received i.v. nalbuphine 0.08 mg/kg, Group 2 (n = 30) received i.v. meperidine 0.4 mg/kg, and Group 3 (n = 30) received i.v. saline. Treatment that stopped shivering was considered to have been successful. The results demonstrated that, 5 min after treatment, both nalbuphine and meperidine provided a rapid and potent anti-shivering effect on PS, with high response rates of 80% and 83%, compared with those of saline (0%) (P < 0.01). Thirty minutes after injection, the response rates of nalbuphine and meperidine were 90% and 93%, respectively, compared with 17% in the saline group (P < 0.01). The differences between nalbuphine and meperidine were not significant. We conclude that nalbuphine may be an alternative to meperidine for treating PS. ⋯ We evaluated nalbuphine versus meperidine and saline for treating postanesthetic shivering. Our results demonstrate that both nalbuphine and meperidine provide a similar rapid and potent anti-shivering effect. Nalbuphine may be an alternative to meperidine for treating postanesthetic shivering.
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In this study, we evaluated the gastric effects of methylnaltrexone, an opioid receptor antagonist that does not cross the blood-brain barrier in vivo, on mu, kappa and delta opioid agonists induced brainstem unitary responses in an in vitro neonatal rat brainstem-gastric preparation. Single units in the medial subnucleus of the nucleus tractus solitarius (NTS), responding to electrical stimulation of subdiaphragmatic vagal fibers, were recorded. Selective opioid receptor agonists and antagonists were applied only to the gastric compartment of the bath chamber and thus, the brainstem functions of the preparation were not affected by the drugs. ⋯ Naloxone, a non-selective opioid receptor antagonist, reversed the inhibitory effects of DAMGO and U-50,488H at much lower concentrations (3.8% and 0.5%, respectively) compared to methylnaltrexone. Only 18% of the NTS neurons evaluated showed inhibitory responses to a delta receptor agonist, DPDPE, (19.7+/-5.0% at 10 microM), and this inhibition could not be reversed by methylnaltrexone in the concentration range we tested. In addition, when methylnaltrexone (1.0 microM) alone was applied to the gastric compartment, there was an activation (8.5+/-2.1%) of the NTS neurons receiving subdiaphragmatic vagal inputs, suggesting an endogenous gastric opioid action in the modulation of brainstem neuronal activities.