Articles: narcotic-antagonists.
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Clin. Pharmacol. Ther. · Jan 2001
Randomized Controlled Trial Clinical TrialADL 8-2698, a trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine, prevents gastrointestinal effects of intravenous morphine without affecting analgesia.
ADL-8-2698 is a novel peripherally restricted opioid antagonist that may selectively prevent opioid-induced gastrointestinal effects without reversing analgesia. Gastrointestinal transit time (lactulose hydrogen breath test) was measured in 14 volunteers with oral and intravenous placebo, oral placebo and intravenous morphine (0.05 mg x kg(-1)), and oral ADL 8-2698 (4 mg) and intravenous morphine (0.05 mg x kg(-1)) in a double blind, cross-over study. Morphine prolonged gastrointestinal transit time from 69 to 103 minutes (P = .005); this was prevented by ADL 8-2698 (P = .004). ⋯ Analgesia and pupil constriction were measured. Morphine analgesia and pupil constriction were unaffected by ADL 8-2698 and differed from placebo (P < .002). We conclude that ADL 8-2698 prevents morphine-induced increases in gastrointestinal transit time by means of selective peripheral opioid anitagonism without affecting central opioid analgesia.
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It is now well established that the analgesic actions of opioids can be modified by "anti-analgesic" or "antiopioid" peptides, among them cholecystokinin (CCK). Although the focus of much recent work concerned with CCK-opioid interactions has been at the level of the spinal cord, CCK also acts within the brain to modify opioid analgesia. The aim of the present study was to characterize the actions of CCK in a brain region in which the circuitry mediating the analgesic actions of opioids is relatively well understood, the rostral ventromedial medulla (RVM). ⋯ Opioid suppression of ON-cell firing was not significantly altered by CCK. Thus CCK acting within the RVM attenuates the analgesic effect of systemically administered morphine by preventing activation of the putative pain inhibiting output neurons of the RVM, the OFF cells. CCK thus differs from another antiopioid peptide, orphanin FQ/nociceptin, which interferes with opioid analgesia by potently suppressing all OFF-cell firing.
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Drug Alcohol Depend · Dec 2000
Clinical Trial Controlled Clinical TrialBuprenorphine and naloxone co-administration in opiate-dependent patients stabilized on sublingual buprenorphine.
Buprenorphine and naloxone sublingual (s.l.) dose formulations may decrease parenteral buprenorphine abuse. We evaluated pharmacologic interactions between 8 mg s.l. buprenorphine combined with 0, 4, or 8 mg of naloxone in nine opiate-dependent volunteers stabilized on 8 mg s.l. buprenorphine for 7 days. ⋯ Buprenorphine and naloxone bioavailability was approximately 40 and 10%, respectively. Intravenous buprenorphine and naloxone produced subjective effects similar to those of s.l. buprenorphine and did not precipitate opiate withdrawal.
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Anaesth Intensive Care · Dec 2000
Case ReportsIntraoperative high-dose remifentanil in a patient on naltrexone therapy.
Naltrexone hydrochloride is a synthetic opioid receptor antagonist recently used in efforts to provide rapid opioid detoxification. Other clinical uses include alleviating itch due to cholestasis or uraemia. We report a case where unrecognised naltrexone therapy for itch affected anaesthesia, resulting in high opioid requirements. We also discuss other analgesic options utilized.
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Because of questions about the basis for the use of naloxone in resuscitation of the newborn, we wished to evaluate the use of naloxone at our institution and an affiliated hospital. ⋯ The use of naloxone in practice may not conform to the American Academy of Pediatrics' guidelines for use in resuscitation of the newborn. The use of naloxone in resuscitation of the newborn should be reevaluated.