Articles: narcotic-antagonists.
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The present study investigated the possible role of nitric oxide (NO) in the development of the withdrawal contractures of guinea pig isolated ileum after acute activation of mu- and kappa-opioid receptors. After a 4-min in vitro exposure to morphine (mu-opioid receptor preferring, but not selective, agonist), [D-Ala2-N-methyl-Phe4-Gly5-ol-]enkephalin (DAMGO; highly selective mu-opioid receptor agonist), or trans(+/-)-3,4-dichloro-N-methyl-N-2(1-pyrrolidynyl)cyclohexyl-ben zeneacetamide (U50-488H; highly selective kappa-opioid receptor agonist), the guinea-pig isolated ileum exhibited a strong contracture after the addition of naloxone. ⋯ Finally, glyceryl trinitrate on its own (3-300 microM) significantly increased the naloxone-induced contraction after exposure to mu- and kappa-opioid receptor agonist and it was also able to reverse the inhibition of opioid withdrawal caused by L-N(G)-nitro arginine methyl ester. These results provide evidence that NO has a role in the development of opioid withdrawal and that mu- or kappa-opioid receptors are involved.
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Drug Alcohol Depend · Oct 1998
Randomized Controlled Trial Clinical TrialEfficacy of orally administered methylnaltrexone in decreasing subjective effects after intravenous morphine.
Opioid compounds are commonly used analgesics. After opioid administration, troublesome subjective effects, such as dysphoria, dizziness, nausea, and pruritus, have been reported. While some if not all of these are believed to occur due to central nervous system effects of opioids, the anecdotal reports heard from volunteers in our other studies suggest that a peripheral opioid antagonist reduced some of these effects. ⋯ Oral methylnaltrexone 19.2 mg/kg significantly decreased these four ratings. Plasma methylnaltrexone concentrations at two different oral doses were also measured to correlate between pharmacological effects of the compound and its plasma levels. Our results suggested that methylnaltrexone has a potential therapeutic value in decreasing some undesirable subjective effects associated with opioid medications.
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Brain Res. Dev. Brain Res. · Sep 1998
Effects of preweanling chronic naltrindole administration on stress-induced antinociceptive responses in rats.
The effect of a daily injection of the delta-selective opioid antagonist naltrindole (1 mg/kg), from birth to postnatal day 19, on the development of stress-induced-antinociception (SIA) and on the antinociceptive response to the mu-selective agonist alfentanil (65 microg/kg) in female rats was investigated. Functional blockade of the delta-receptor during the preweanling period markedly reduced the antinociceptive response to swim-stress in 25-day-old rats, and SIA was only mediated by delta-receptors at this age. ⋯ The lack of interference with mu-receptor function was confirmed as alfentanil responses were unaffected by preweanling naltrindole treatment. The data show independence of mu- and delta-receptors in the control of SIA during development and an impairment of delta- but not mu-mediated SIA after chronic delta-antagonist treatment.
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Reg Anesth Pain Med · Sep 1998
Randomized Controlled Trial Comparative Study Clinical TrialComparison of intravenous nalbuphine infusion versus naloxone in the prevention of epidural morphine-related side effects.
Epidural morphine is accepted as an efficient means of postoperative pain management. However, development of side effects such as nausea and vomiting and pruritus has been reported. This study compared the efficacy of intravenous infusions of nalbuphine or naloxone in the prevention of epidural morphine-related side effects. ⋯ We found that coadministration of either nalbuphine or naloxone with epidural morphine reduces the incidence of morphine-related side effects. However, unlike naloxone, nalbuphine did not attenuate the analgesic effect of epidural morphine.
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The effect of neuropeptide FF in the periaqueductal gray on pain behaviour was studied in rats with a chronic neuropathy induced by unilateral ligation of two spinal nerves. Neuropeptide FF produced in a non-monotonic fashion a significant attenuation of tactile allodynia. The antiallodynic effect was not significantly modulated by naloxone administered systemically or intracerebrally. ⋯ The results indicate that neuropeptide FF in the periaqueductal gray may produce a selective attenuation of tactile allodynia in neuropathic rats. This antiallodynic effect is at least partly independent of naloxone-sensitive opioid receptors. Furthermore, neuropeptide FF in the periaqueductal gray attenuates antinociception induced by intracerebrally but not systemically administered morphine.