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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The analgesic activity of delta9THC, morphine and sodium salicylate was studied concomitantly with changes in brain stem levels of 5HT, 5HIAA, DA and NA. The results show that a correlation exists between analgesia and changes in the serotonergic system of the brain stem. Furthermore morphine sulfate was found to increase the DA concentration of the brain stem while delta9THC increased NA levels. We conclude that serotonergic system may be of major importance in analgesia while simultaneous changes in this system and/or the DA and NA systems may lead to a more pronounced analgesic activity.
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PMID:An attempt to correlated analgesia to changes in brain neuromediators in rats. 0 Jul 46

An increase in the disposition of naloxone to the mouse brain was observed for animals previously exposed to morphine. Compared to controls, mice receiving morphine sulfate (10 mg/kg, sc) 3 hr prior to naloxone had a 28% increase in naloxone concentration in brain (200 to 260 pmol of naloxone per g of brain) 10 min after 3H-naloxone-HCl (0.4 mg/kg, 11.0 micronCi/kg, sc) administration. Also, if similar morphine-pretreated mice received a second dose of morphine sulfate (1.0 mg/kg, sc) concurrent with 3H-naloxone-HCl, the morphine-induced enhancement of 3H-naloxone concentration in brain was unaltered. This drug-treatment protocol paralleled that used by others in pA2-analgesia assays to demonstrate sensitization to naloxone for morphine-pretreated animals. In prior (3 hr) morphine-treated animals, administration of 3H-naloxone-HCl (0.1 mg/kg, 33.3 micronCi/kg) iv resulted in an 11.0% increase in 3H-naloxone brain concentration after 1 min. Thus, the enhancement of naloxone brain concentration was independent of the route of naloxone administration. No enhancement of 3H-naloxone brain concentration could be seen 24 hr after morphine sulfate pretreatment (10 mg/kg, sc), a decline in the effect similar to that seen for morphine-induced sensitization to naloxone. Finally, when morphine pellet-implanted mice (75 mg of morphine base, 72 hr) were administered 3H-naloxone-HCl (0.4 mg/kg, 10.0 micronCi/kg, sc), only a 22.5% enhancement of 3H-naloxone concentration in brain was obtained, as opposed to a reported 8-fold increase in the potency of naloxone. Thus, although a number of similarities exist between the enhancement by morphine of naloxone concentration in brain and its sensitization to the antagonistic activity of naloxone, a quantitative correlation appears to be lacking between the two phenomena.
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PMID:Enhanced naloxone distribution to the brain by morphine pretreatment in mice. 1 9

The enterohepatic circulation of 1-alpha-acetylmethadol (LAAM) was investigated in the rat. Bile containing 3H-LAAM metabolites was collected from a biliary cannulated donor rat after administration of 3H-LAAM (5 mg/kg, 15 muCi/kg, sc) and infused into the intestine of a double biliary-cannulated recipient rat for 1 hr, and tritium excreted into the bile of the recipient rat was monitored. Within 1 hr after the end of infusion significant radioactivity was found in the bile of the recipient rat and by 10 hr 50% of the infused dose of 3H had been re-excreted into bile. The contribution of enterohepatic circulation of LAAM metabolites to the analgesic action of LAAM was also assessed. Pretreatment of rats with neomycin sulfate was used as a method of decreasing enterohepatic circulation of biliary glucuronide conjugates of LAAM metabolites, and such pretreatment had no effect on LAAM analgesia (6 mg/kg) measured by the hot-plate method. In rats with a biliary fistula, a situation in which enterohepatic circulation was completely eliminated, the analgesic response to a dose of LAAM (6 mg/kg, sc) was not different from sham-operated control group. The above findings indicate that enterohepatic circulation of LAAM metabolites does not contribute to the intensity or duration of LAAM analgesia.
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PMID:Role of enterohepatic circulation in the analgesic action of 1-alpha-acetylmethadol in the rat. 4 Jul 71

The addition of d-amphetamine to morphine has been reported to result in an increase of analgesic potency in experimental animals and man, but no data on the toxicity of such combinations are available. This study is intended to provide systematic information on the toxicity, analgesic potency and degree of physical impairment (swimming endurance) of a combination of 12 mg morphine sulfate with 10 mg d-amphetamine HCl per ml which is now under clinical investigation. Mice were used as experimental subjects. Meperidine, methadone and pentazocine were substituted for morphine using clinically equally analgesic doses and keeping the d-amphetamine amount constant. The toxicity of all analgesics especially that of morphine was enhanced in the combination, least so in the case of meperidine. The degree of increase of analgesic power by the addition of d-amphetamine was greatest with morphine and quantitatively in satisfactory agreement with present clinical experiences. However, the relationship between the increases of toxicity and of analgesia is not necessarily most favorable for this drug. For the other three analgesics increases in toxicity and analgesia were more in line, meperidine showing the best ratio. Swimming endurance was decreased with full analgesic doses of all four compounds. The presence of d-amphetamine tended to reverse this depression. The data were analyzed in relation to their possible predictive value for the use of such combinations in man for the therapeutic dose range and in the event of overdosage.
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PMID:A study of the effect of d-amphetamine on the toxicity, analgesic potency and swimming impairment caused by potent analgesics in mice. 24 3

In a double-blind, single-dose study, dextroamphetamine combined with morphine was compared with morphine alone to determine the relative efficacy of the combination given intramuscularly for postoperative pain. Each of 450 patients received one treatment of morphine sulfate (3, 6 or 12 mg) with dextroamphetamine (0, 5 or 10 mg). Analgesia, as measured by the patients' subjective responses to questions about relief of pain, was augmented when dextroamphetamine was given with morphine; the combination of dextroamphetamine, 10 mg, with morphine was twice as potent as morphine alone, and the combination with 5 mg was 1 1/2 times as potent as morphine. In simple performance tests, and in measures of side effects, dextroamphetamine generally offset undesirable effects of morphine (sedation and loss of alertness) while increasing analgesia. Effects on blood pressure, pulse and respiratory rate were minimal.
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PMID:Dextroamphetamine with morphine for the treatment of postoperative pain. 32 Apr 78

In a double-blind control study, oral doses of placebo, propoxyphene napsylate (50 or 100 mg), or codeine sulfate (30 or 60 mg) were administered to 46 postepisiotomy patients, grouped by severity of pain reported at first-dose drug administration. Eight hourly observations by a trained observer provided estimates of analgesia. The analgesia scores for placebo treatments were significantly lower than for the lesser doses of either drug (P less than .05) as well as for the greater doses (P less than .01). At both dose levels, the analgesia scores for both drugs were almost identical. Analgesia with the higher doses was greater than with the lower, but not to a statistically significant extent. The difference in patient responses increased following the second dose. No serious adverse reactions occurred; the elicited and volunteered reports of minor side effects were similar for all five treatments.
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PMID:Codeine and propoxyphene in postepisiotomy pain. A two-dose evaluation. 32 38

Sensory evoked responses were recorded simultaneously from five structures (caudate nucleus, septum, periaqueductal gray, parafascicular nucleus and reticular formation) reported to play roles in morphine's acute actions (analgesia, dyskinesia) and in the development of tolerance. Daily recordings were made from unanesthetized male Holtzman rats before and after a challenge dose of 10 mg/kg of morphine sulfate over a four day period while tolerance was induced by multiple daily injections of morphine. Three patterns of changes were observed in the individual components of the evoked responses. 1) The challenge dose caused an initial increase in the amplitudes of the P2 and N2 components of the response in the naive rats. This effect was attenuated with each day of drug administration until day four, when the challenge dose was observed to exert no effect. This pattern occurred in the parafascicular nucleus and the septum. 2) Initial increase in P2 and N2 components by morphine was augmented for 2-3 days, after which there was a sharp drop to control values by day four. This pattern was observed in the caudate nucleus and the periaqueductal gray region. 3) Morphine caused a mixture of increases and null effects in the components over the four days. This effect was observed in the reticular formation.
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PMID:Neurophysiological assessment of site specific effects of chronic morphine administration in freely behaving rats. 33 15

SC-27166 is the result of continuing efforts to discover selective and orally active antidiarrheal agents. SC-27166, which is chemically unrelated to opiates or neuroleptics, possesses potent constipating and antidiarrheal activity in several animal models. Tolerance to the constipating actions of SC-27166 did not develop in mice. On the other hand, gut tolerance rapidly developed to morphine sulfate and loperamide. The basic mechanism of the antidiarrheal action of SC-27166 is a consequence of increased intestinal circular muscle contractile activity. Supportive pharmacological studies indicated that SC-27166 has equivocal analgesia in mice which is manifested at near toxic dose levels. SC-27166 was also evaluated for potential dependence liability in morphine abstinence-induced jumping in mice. The abstinence-induced jumping was suppressed to a far lesser extent by SC-27166 than by either loperamide or diphenoxylate at equal doses. SC-27166 was also devoid of anticbholinergic activity. When compared with the reference standards morphine and diphenoxylate, these pharmacological studies indicated that SC-27166 has a high degree of separation of undesirable central nervous system actions from its antidiarrheal properties and may have important therapeutic potential.
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PMID:The pharmacology of SC-27166: a novel antidiarrheal agent. 41 12

Previous studies have suggested that in rats probing against the vaginal cervix with a glass of is analgesic, for this stimulus elevates the threshold for eliciting vocalization in response to tail shock. In the present studies pretreatment with naloxone HCl (1 or 10 mg/kg), a potent narcotic antagonist did not antagonize this vaginal stimulation-induced analgesia. Furthermore, vaginal stimulation was found to exert its analgesic effect even in rats made tolerant to, and dependent upon, morphine sulfate. These results suggest that the analgesic effect of vaginal stimulation is not necessarily mediated by an opiate-sensitive neural system. However, we hypothesize that even though vaginal stimulation and other analgesic manipulations may act via different neural substrates, they may nevertheless converge onto a final common mechanism for pain suppression.
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PMID:Analgesia induced by vaginal stimulation in rats is apparently independent of a morphine-sensitive process. 41 36

Intracerebral administration of copper sulfate potentiated morphine analgesia in morphine-tolerant and -dependent mice, but copper failed to affect other abstinence signs. When abstinence was precipitated with a partial antagonist, nalorphine, stereotyped jumping was not inhibited by either calcium or copper. These modifications of narcotic effects by copper were produced without alterations in the brain disposition of morphine. Total radioactivity in the brain following radioactive naloxone administration was also not altered.
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PMID:The effects of divalent ions on morphine analgesia and abstinence syndrome in morphine-tolerant and -dependent mice. 41 58


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