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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

A series of 26 drugs was tested for in vitro binding to opiate receptors in the presence and absence of 0.1 M NaCl. The results were correlated with assays for in vivo pharmacological potency. Highly significant correlation was found between binding in the presence and absence of sodium ions and analgesic potency. For 10 drugs tested for anti-diarrheal potency significant correlation was observed with binding to brain opiate receptors when binding was carried out in sodium-containing medium. These data add support to the hypothesis that stereospecific opiate binding sites are pharmacological receptors which mediate analgesia and anti-diarrheal action. We found that neuroleptics can bind to opiate receptors with affinities in the micromolar range, in agreement with reports by others. The anti-diarrheal compound loperamide exhibits no significant central opiate effects but binds to opiate receptors from brain in vitro with high affinity. Evidency is presented suggesting that the lack of specific analgesic effect is the result of poor penetration through the blood--brain barrier. Our results lend further support to the similarity of opiate receptors in the brain and in the intestinal tract.
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PMID:Receptor affinity and pharmacological potency of a series of narcotic analgesic, anti-diarrheal and neuroleptic drugs. 2 40

In man and other animals, urinary excretion of the histidine and histamine metabolite, imidazoleacetate, is increased and that of its conjugated metabolite, ribosylimidazoleacetate, decreased by salicylates. Imidazoleacetate has been reported to produce analgesia and narcosis. Its accumulation as a result of transferase inhibition could play a part in the therapeutic effects of salicylates. To determine the locus of salicylate action, we have investigated the effect of anti-inflammatory drugs on imidazoleacetate phosphoribosyl transferase, the enzyme that catalyzes the ATP-dependent conjugation of imidazoleacetate with phosphoribosylpyrophosphate. As little as 0.2 mM aspirin produced 50% inhibition of the rat liver transferase. In vivo, a 30% decrease in the urinary excretion of ribosylimidazoleacetate has been observed with plasma salicylate concentrations of 0.4 mM. The enzyme was also inhibited by sodium salicylate but not by salicylamide, sodium gentisate, aminopyrine, phenacetin, phenylbutazone, or indomethacin. The last four drugs have been shown previously not to alter the excretion of ribosylimidazoleacetate when administered in vivo. Since both the drug specificity and inhibitory concentrations are similar in vivo and in vitro, it seems probable that the effect of salicylates on imidazoleacetate conjugation results from inhibition of imidazoleacetate phosphoribosyl transferase.
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PMID:Effect of salicylates on histamine and L-histidine metabolism. Inhibition of imidazoleacetate phosphoribosyl transferase. 18 57

SKF 525A, a classical inhibitor of microsomal drug-metabolizing enzymes, is structurally similar to the diphenylpropylamine analgesics, and certain reported effects in animals resemble those produced by opiate drugs. In an opiate radioreceptor assay, SKF 525A was 50 times less potent than methadone in the absence of sodium and 10 times less potent in the prescence of sodium. The nature of the sodium effect indicates SKF 525A to have less opiate agonist character than does methadone. In mice, 2 mg of SKF 525A given intraperitoneally induced less profound analgesia on a hot plate (44 degrees C) than did 0.1 mg of methadone. Analgesia by SKF 525A was prevented by pretreatment of the mice with naloxone. In rats, 50 microgram of SKF 525A given intracerebroventricularly was analgesic.
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PMID:Opiate properties of SKF 525A. 21 Sep 15

The analgesic efficacy of oral naproxen and its sodium salt was compared with that of aspirin and codeine in two separate trials involving 140 and 90 patients, respectively, with postpartum uterine pain in a single-dose, parallel, stratified, randomized, placebo-controlled, double-blind design. With 300 or 600 mg naproxen and with 275 mg naproxen sodium, significant analgesia, measured subjectively by pain intensity differences (PID), was prolonged at least 7 or 8 hr; onset tended to be delayed 2 hr or more. With 650 mg aspirin analgesia began within 1 hr and continued until the fifth hour, while with 60 mg codeine responses were indistinguishable from placebo responses throughout the 8-hr time course. Although time-effect patterns with naproxen sodium and aspirin were different, summed analgesic effects (SPID) showed equal efficacy and superiority over placebo (p less than 0.005). With each of the 2 doses of naproxen, SPID separation from placebo was comparable to that above (p less than 0.02 and 0.005, respectively), but analgesic dose response, though measurable, was not significant. Side effects were not significant with any of the treatments. It appears that naproxen and naproxen sodium are analgesics with efficacy equal to aspirin and may prove to be rational substitutes for currently available analgesics in some painful states in which longer pain relief would be desireable.
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PMID:Naproxen, aspirin, and codeine in postpartum uterine pain. 32 Nov 77

In a double-blind between-patient study of 69 patients with sports injuries of the knee, diclophenac sodium (Voltaren) was significantly superior to oxyphenbutazone (Tanderil) and placebo in improving the degree of swelling and the condition of the injured knee. Both drugs were superior to placebo with regard to analgesia by the second day of treatment. In addition, diclophenac sodium significantly improved the condition of the injured knee by the end of the trial. Three patients dropped out of the trial for reasons not related to the drug. Two patients in the diclophenac sodium group failed to complete the trial due to rapid recovery and 1 each in the diclophenac sodium and oxyphenbutazone groups because of poor tolerability. Nine patients who completed the trial reported mild to moderate side-effects, consisting mainly of drowsiness and nausea.
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PMID:Diclophenac sodium, oxyphenbutazone and placebo in sports injuries of the knee. 33 3

Clinical examination of patients with diseases of the lungs and locomotor system during the surgical treatment and experiments in animals has shown that sodium hydroxybutyrate used as an anesthetizing drug under conditions of the neuroleptic analgesia fails to provide an effective defense against the surgical trauma. This is shown by the instability in the hemodynamic indices, metabolic shifts and the presence of nociceptive viscero-somatic reflexes.
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PMID:[Effect of sodium oxybutyrate on reflex hemodynamic reactions]. 38 15

The guinea pig is notoriously difficult to anesthetize with conventional agents. Cardiorespiratory depression by general depressant anesthetic agents can render the cochlea abnormal. I report a technique that uses the specific neuroleptic and analgesia properties of the agents droperidol and phenoperidine, respectively, in combination with small doses of pentobarbital sodium, which is required only to produce unconsciousness. These agents can be given intraperitoneally, intramuscularly, or intravenously. The regimen allows performance of substantial surgery (including intracranial) and long-term (minimum, six to ten hours) physiological studies, such as those on the cochlea, with excellent cardiorespiratory stability. The method has been in continuous use in this laboratory since 1974 for single-fiber recordings from the cochlear nerve of normal and kanamycin-treated guinea pigs. This method has proved to be substantially more effective than use of pentobarbital, thiopental sodium, urethan, chloralose, or ketamine alone.
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PMID:Neuroleptanesthesia for the guinea pig. An ideal anesthetic procedure for long-term physiological studies of the cochlea. 42 4

Renin activity and aldosterone concentration in plasma and excretion of sodium and potassium in urine were measured during a period of 24 hours in 12 patients undergoing hysterectomy under general anaesthesia or epidural analgesia. Analgesia extended from T4 to S5 and was effective throughout the study. The normal stress-induced increase in plasma renin activity and aldosterone was inhibited by epidural analgesia. Urinary excretion of potassium was significantly lower in the epidural group, but sodium and water retention showed no difference between groups. It is concluded that neurogenic stimuli from the surgical area are important release mechanisms of the renin-aldosterone response to surgery. The results suggest that post-operative sodium retention is caused by factors other than the mineralocorticoid system.
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PMID:Epidural analgesia inhibits the renin and aldosterone response to surgery. 48 83

The effect of a high epidural blockade on postoperative sodium (Na) retention has been studied in 8 patients undergoing cholecystectomy, with a further 8 patients, who received conventional anaesthesia and analgesia, acting as a control group. Preoperatively, all the patients received 90 mmol of Na per day and were in Na balance at the start of operation; this intake was continued for 48 h after the operation by intravenous infusion, and the epidural blockade was maintained with regular supplements of bupivacaine throughout. In addition to urine Na excretion and blood pressure changes, plasma levels of aldosterone, cortisol, renin activity and glucose were measured at appropriate intervals. The Na retention in both the epidural and control groups was the same (139 mmol and 135 mmol respectively at 48 h), but there were significant differences in the measurements of all the other factors. It is concluded that the epidural was providing effective blockade, but that the factors which cause Na retention were not affected by the epidural blockade. These results are at variance with another study of the effect of epidural blockade on postoperative Na retention (Bevan, 1971), and the possible reasons for this are discussed.
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PMID:The effect of epidural analgesia on postoperative sodium balance. 50 60


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