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

Parturients in whom meperidine HCl, propiomazine HCl, and scopolamine were used for analgesia and amnesia in labor and delivery were studied to determine the efficacy and safety of physostigmine reversal after delivery. Of a total of 120 patients, 108 received physostigmine salicylate at the completion of episiotomy closure, awakening in an average of 7.5 minutes compared with 137.8 in 12 controls. Physostigmine appears to be a safe, rapidly effective agent for reversing the prolonged somnolence of this sedation regimen.
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PMID:Physostigmine reversal of sedation in parturients. 0 75

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

SKF 525-A, given i.p. to mice at doses from 50 to 100 mg/kg, had analgesic activity approximately 40% the analgesic potency of d-propoxyphene HCl, a chemically similar narcotic. While the analgesia produced by propoxyphene was totally antagonized by naloxone, however, that produced by SKF 525-A was only partly reversed. We suspect that SKF 525-A may exert its antinociceptive actions partly by an interaction with CNS narcotic receptors and partly by a nonspecific sedating action.
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PMID:Naloxone-reversible analgesic action of SKF 525-A in mice. 10 35

Four local anaesthetic solutions (2% carbonated lignocaine with or without adrenaline and 0.5% bupivacaine HCl with or without adrenaline) were used randomly for 335 continuous lumbar extradural blocks in labour. Carbonated lignocaine caused a more rapid onset of analgesia than bupivacaine HCl. The addition of adrenaline made little difference to the onset times, prolonged markedly the duration of analgesia with carbonated lignocaine and had little effect on the duration of analgesia with bupivacaine HCl. Tachyphylaxis was a feature with carbonated lignocaine and adrenaline, but not with the other solutions. The incidence of unblocked segments was 7-9% in the four groups. The incidence of unilateral analgesia was 6% with plain lignocaine and 13% in the other groups. Complete pain relief occurred more frequently with bupivacaine HCl than with carbonated lignocaine and the use of adrenaline had little effect on the degree of analgesia.
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PMID:Extradural analgesia in obstetrics: a controlled trial of carbonated lignocaine and bupivacaine hydrochloride with or without adrenaline. 13 Jan 53

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

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

Mice were given single s.c. injections of morphine sulphate (M.S.), heroin hydrochloride (H.HCl) and the sparingly-soluble diheroin pamoate (H.Pam) and 3,5-di-tert-butyl-2,6-dihydroxybenzoate (H.Bnz) in three vehicles, saline, peanut oil, or a slow-release vehicle (SRV) and tested for analgesia by both the tail-clip and hotplate techniques. Duration of analgesia as assessed by the tail-clip method was always longer than that by the hotplate when equivalent doses were used in any vehicle. The H.Pam and H.Bnz salts significantly prolonged the analgesia: the mean duration in mice injected with equivalent amounts of heroin base was 3.0 hr for the group receiving heroin HCl in saline and 7.8 hr after H.Bnz in slow-release vehicle. An inverse relationship was evident between the degree of dissociation of H from the three salts, at pH 7.3 and their durations of analgesia in vivo. This was statistically significant (p less than 0.01) at the higher dose level. All mice were challenged with naloxone hydrochloride (1 mg/kg) 24 hr after the injection of each narcotic agonist preparation. The jumping behaviour elicited by naloxone was not consistently related to dose, salt form, or vehicle employed for the injection of agonists, but from 12.5 too 54.2% of all the mice did jump at that time. The durations of analgesia observed and the intensity of the jumping response correlated significantly with the mean number of jumps per mouse after the naloxone challenge.
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PMID:Analgesia duration and physical dependence in mice after a single injection of three heroin salts and morphine sulphate in various vehicles. 56 22

The clinical effects of equal hyperbaric doses of bupivacaine HCl and tetracaine HCl were studied and compared in 99 adult men undergoing spinal anesthesia for similar surgical procedures. The spinal anesthetic agents were used in random order in various dosages. Comparisons were made of (1) amount of anesthetic agent used, (2) elapsed time for onset of analgesia, (3) elapsed time for obtaining maximum anesthesia, (4) cephalad dermatome level of anesthesia, (5) incidence of motor blockade, and (6) duration of anesthesia. Results with the 2 drugs in equal dose, volume, and specific gravity were almost identical. However, tetracaine provided a motor block in a significantly greater number of patients than did pubivacaine (100 versus 42%, rho less than 0.001) when both drugs were used at the 9.75-mg dose level.
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PMID:Spinal anesthesia: bupivacaine versus tetracaine. 94 52

Five healthy, unmedicated male volunteers, aged 19-25 yr, participated in a double-blind, crossover study. Each subject received, on separate occasions and via a catheter placed at L2, 1.5% etiodocaine HCl20 ml with adrenaline 5 mug/ml, or 0.75% bupivacaine HCl 20 ml with adrenaline 5 mug/ml for extradural analgesia. In addition, in order to calculate the absorption rate of the local anaesthetic agent, each subject received on two further occasions etidocaine HCl 75 mg and bupivacaine HCl 75 mg respectively by i.v. infusion, over a period of 10 min. Spread of sensory analgesia to four segments above and below the site of injection was faster with etidocaine (13 +/- 3 min) (mean +/- SD) than with bupivacaine (22 +/- 8 min). Two-segment regression occurred later for bupivacaine (260 +/- 57 min) than for etidocaine (180 +/- 96 min). Caudal spread of analgesia was more extensive with etidocaine than with bupivacaine. The onset of motor blockade tended to be faster with etidocaine (5.8 +/- 3.0 min), than with bupivacaine (10.0 +/- 3.5 min); regression of motor blockade by one unit was longer with etidocaine (306 +/- 103 min) than bupivacaine (238 +/- 75 min). Sudomotor block occurred earlier with etidocaine (4.0 +/- 2.1 min) than bupivacaine (13.7 +/- 4.8 min). Significant changes in cardiac stroke work and stroke volume occurred. For etidocaine these measurements remained below control values for 120-210 min after injection. The mean maximum arterial plasma concentration of etidocaine was 1.52 +/- 0.64 mug/ml, at 14 +/- 2 min and of bupivacaine was 1.35 +/- 0.63 mug/ml, achieved at 20 +/- 4 min. The systemic absorption of both drugs occurred in a biphasic pattern with a fast and slow half-life of 0.3 and approximately 8 h respectively.
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PMID:Effects of extradural block: comparison of the properties, circulatory effects and pharmacokinetics of etidocaine and bupivacaine. 95 93

ED50 values for analgesia (tail-clip method) at 30 min after heroin HCl administered i.v. or s.c. in groups of Swiss-Webster mice were not significantly different. Nor was the duration of the analgesia following various doses of heroin significantly different after i.v. or s.c. injections, although there was a tendency for the latter route to have a longer effect. Hyperactivity (mean levels in groups of 5 mice, measured by an Activity Meter), though variable, was increased after s.c. injections of heroin in a dose-related manner up to doses of 10 mg/kg. Larger doses progesssively prolonged the peak levels of hyperactivity. Because the degree and duration of both analgesia and hyperactivity were parallel over a wide range of doses of heroin HCl in these mice, a close relationship between the two underlying mechanisms seems very likely.
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PMID:Duration of analgesia and hyperactivity in mice after single injections (S.C. and I.V.) of heroin. 96 37


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