Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0344307 (analgesia)
 28,200 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Acute administration of 2-deoxy-D-glucose (2-DG), an antimetabolic glucose analogue induces a powerful analgesia which adapts following repeated administration. 2-DG analgesia displays significant cross-tolerance with morphine, and like morphine analgesia, is potentiated in hypophysectomized rats. The present study examined further the role of opiates in 2-DG analgesia by examining whether the opiate antagonist, naloxone, would affect 2-DG analgesia, and whether ineffective doses of 2-DG and morphine would interact in a synergistic fashion to induce analgesia. Nociceptive thresholds were measured by the flinch-jump test. Naloxone doses of 1, 5, 10 and 20 mg/kg were all ineffective in reducing significantly 2-DG (600 mg/kg) induced pain threshold elevations. Naloxone failed to attenuate 2-DG (350 mg/kg) analgesia whether administered before or after the 2-DG injection. On the other hand, simultaneous administration of sub-analgesic doses of 2-DG (200 mg/kg) and morphine (2.5 mg/kg) summated to produce significant analgesia. This, 2-DG analgesia is similar to opiates in its tolerant and summative actions, yet dissimilar in that naloxone is ineffective in reversing its effects.
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PMID:2-Deoxy-D-glucose analgesia: influences of opiate and non-opiate factors. 50 9

Pain threshold elevations induced in rats following acute exposure to stressful cold-water swims and to inescapable foot shocks are significantly attenuated by hypophysectomy. The present study investigated the effects of hypophysectomy upon the dose-dependent and time-dependent analgesia induced by morphine and by the glucoprivic agents, 2-deoxy-D-glucose (2-DG) and insulin. Two reflex pain tests, the tail-pinch and the flinch-jump were employed. In normal rats, insulin induced prolonged (180 min) analgesia at doses of 16 U/kg on the tail-pinch test and 256 U/kg on the flinch-jump test. However, the same agents induced small and brief pain threshold elevations in hypophysectomized animals. By contrast, though 2-DG increased both measures in both groups, its effects were more marked in hypophysectomized rats. Hypophysectomized rats also exhibited a potentiated analgesic effect on both tests following high doses of morphine. On the other hand, low doses of morphine transiently increased tail-pinch thresholds in normal, but not hypophysectomized subjects. These data provide further evidence of multiple pain-inhibitory mechanisms in which the pituitary plays a complex, but integral part.
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PMID:Differential effects of hypophysectomy upon analgesia induced by two glucoprivic stressors and morphine. 50 10

Acute exposure to many environmental stressors induces significant analgesia. The present study examined whether 2-deoxy-D-glucose (2-DG), an antimetabolic glucose analogue, which induces glucoprivation and peripheral sympatho-adrenal discharge, would also produce analgesia as measured by either an operant liminal escape or a reflex tail-pinch procedure. In the liminal escape paradigm, 9 rats were tested at weekly intervals in 6 randomly selected testing conditions: 30 min pre-test injections of four 2-DG doses (100, 225, 350 and 700 mg/kg, IP) and 180 min pre-test injections of the 2 higher doses. Moderate analgesia occurred at the lower 2-DG doses 30 min after injection, while profound analgesia occurred at the higher doses. After 180 min, only the 700 mg/kg 2-DG dose produced moderate analgesia, which was further enhanced by food deprivation. Rats tested in the tail-pinch paradigm displayed a similar dose-dependent analgesia course. These results demonstrate that 2-DG decreases nociceptive sensitivity, possibly through stress-induced activation of an intrinsic pain-inhibitory system.
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PMID:2-Deoxy-D-glucose-induced decrements in operant and reflex pain thresholds. 73 41

So as to determine the effects of some factors on the duration of bupivacaine spinal anaesthesia, a prospective controlled study was carried out on 152 ASA I or II patients. They were randomly allocated to six groups. The patients of group I were given 4 ml of 0.5% bupivacaine at 27 degrees C. The patients of group II were given 4 ml of a mixture including 3 ml of 0.5% bupivacaine, 1 ml fentanyl in 1 ml of 10% dextrose solution. The group III was given 4 ml of a mixture including 3 ml of 0.5% bupivacaine, 0.20 mg adrenaline. The group IV was given 4 ml of a mixture including 3 ml of 0.5% bupivacaine, 0.15 mg clonidine. The patients of group V were given 4 ml of 0.5% bupivacaine at 20 degrees C and those of group VI were given 4 ml of 0.5% bupivacaine at 5 degrees C. There is significant difference between regression times of sensory analgesia of group II and group I, group IV and group III, group VI and group V. The choice of product to lengthen analgesia in spinal anaesthesia depends on the use of each anaesthesist, the characteristic of patients and the duration of surgery.
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PMID:[Factors changing the length of analgesia in spinal anesthesia]. 134 Nov 33

A double blind study was conducted on 84 subjects (needing surgery) of both sexes who were randomly divided into two groups. In group I 30 ml of 0.33 per cent bupivacaine (20 ml 0.5% bupivacaine + 10 ml of N saline) was injected epidurally and in group II 20 ml of 0.5 per cent bupivacaine + 10 ml of dextraven - 150 (6% solution in 5% dextrose). The subject were observed for the onset of block, degree of motor blockade, period of analgesia and complications during and after surgery. Dextran - 150 mixture significantly prolonged the duration of action of bupivacaine (13.5 +/- 6.25 h) when given epidurally, without affecting the onset, muscular paralysis, quality of block and the incidence of complications.
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PMID:Prolongation of bupivacaine effect in epidural block by dextraven-150. 169 88

Flavone and 10 hydroxy and glucoside flavone derivatives were synthesised. They were tested for their analgesic effect in mice employing acetic acid-induced writhing and tail immersion methods. Subcutaneously all the tested compounds exhibited significant analgesic activity with varying potencies in both assay models. The activity of flavone and its 5-; 7-; 2'-; 5,7- and 7,8-hydroxy derivatives apparently involves an opiate-like mechanism, since their activity was reversed by naloxone pretreatment. It is suggested that flavonoid substances may utilise more than one mechanism in eliciting analgesia.
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PMID:Analgesic activity of certain flavone derivatives: a structure-activity study. 232 11

A new spinal analgesic formulation, 'heavy bupivacaine', was compared clinically with a commonly used agent. Sixty patients, who required spinal analgesia for transurethral prostatectomy, received either 1.5 ml of hyperbaric 0.5% cinchocaine (Nupercaine, Percaine, Dibucaine) in 6% dextrose or 2.5 ml of hyperbaric 0.5% bupivacaine (Marcain) in 8% dextrose. The onset, rate of rise, plateau height of the sensory block, reduction in blood pressure and peak expiratory flow rate, and the operative and post-operative blood loss did not differ significantly. Motor blockade was significantly less with bupivacaine. It is concluded that hyperbaric bupivacaine is an acceptable alternative to hyperbaric cinchocaine for spinal analgesia for transurethral prostatectomy.
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PMID:Hyperbaric bupivacaine and hyperbaric cinchocaine: a comparison of their use for spinal anaesthesia. 243 Jul 97

Two galactosyl derivatives of [DMet2,Pro5] enkephalin-amide (compound 1), namely [DMet2,Pro5] enkephalin [N1.5-beta-D-galactopyranosyl] amide (compound 2) and O1.5-(beta-D-galactopyranosyl) [DMet2,Hyp5] enkephalin-amide (compound 3) have been synthesized. Such glycosylpeptides have been shown to be extremely potent analgesic agonists. The conformational analysis of these three compounds in DMSO-d6 solution has been carried out using two-dimensional NMR methods. Both the parent compound (1) and the beta N-galactosyl derivative (2) show similar NMR parameters which are consistent with fairly rigid beta-strands at both the N-terminus and C-terminus, connected by a glycine residue that displays a mixture between multiple conformational states. Thus, although the beta N-galactosyl derivative (2) has been shown to be significantly more potent than the parent compound (1) in the tail immersion and paw pressure tests of analgesia, no correlation can be established between the conformation of (1) and (2) in DMSO and the difference in analgesic activity. In contrast, important conformational differences with respect to (1) and (2) have been detected in the beta O-galactosyl derivative (3). In this case, only one of the likely conformations for (1) and (2) are consistent with the experimental data. These data show that the position of the galactose residue in compound (3) causes Gly3 to loose flexibility leading to a more rigid folded conformation. Such a change in conformation could be related to the difference in analgesic activity between (2) and (3).
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PMID:Synthesis and conformational analysis of a series of galactosyl enkephalin analogues showing high analgesic activity. 258 86

Spontaneous or induced diabetes, as well as glucose loading, reduce opiate antinociception, presumably through induction of hyperglycemia. While peripheral administration of alloxan is a potent pancreatic beta-cell toxin, intracerebroventricular (ICV) alloxan reduces glucoprivic feeding in the absence of hyperglycemia, presumably through interactions with specific brain glucoreceptors. Our laboratory demonstrated that opioid-mediated 2-deoxy-D-glucose (2DG) antinociception is significantly reduced by central pretreatment with alloxan, and that this deficit is reversed by coadministration with 3M-D-glucose. The present study compared ICV and intravenous (IV) routes of alloxan (200 micrograms) upon morphine (1-10 mg/kg, SC) analgesia on the tail-flick and jump tests in rats, and evaluated these effects in terms of concomitant changes induced by ICV alloxan upon nonopioid-mediated continuous cold-water swim (CCWS: 2 degrees C for 3.5 min) antinociception. Two weeks following central, but not peripheral pretreatment with alloxan, morphine (2.5 and 5.0 mg/kg, SC) antinociception was markedly (30-56%) reduced on both nociceptive tests. In contrast, central pretreatment with alloxan respectively reduced (30 min) and subsequently potentiated (60 and 90 min) CCWS antinociception on the jump test. Alterations in antinociception by central alloxan occurred in the absence of changes in basal nociceptive thresholds, hypothermia or hyperglycemia. These data suggest that central alloxan may be acting upon either specific, but unidentified brain glucoreceptors and/or a glucoprivic control mechanism.
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PMID:Differential actions of central alloxan upon opioid and nonopioid antinociception in rats. 262 9

Recently several reports have described the usefulness of meperidine as the sole agent for spinal anesthesia. In this study, meperidine 50mg mixed with 10% dextrose 0.5ml was used for the spinal anesthetic agent for Cesarean section in 182 cases. The subarachnoid injection of meperidine resulted in anesthesia similar to that noted with the intrathecal administration of local anesthetics. Sensory and motor blockades in all patients with meperidine spinal anesthesia were obtained. Prolonged analgesic effect (453.7 +/- 158.1 minutes) and rapid motor recovery (75.9 +/- 17.2 minutes) were obtained. Side effects included nausea (49 patients), hypotension (95 patients) and pruritus (30 patients). Hypotension was easily treated with rapid hydration and ephedrine. Eighteen patients complained of mild pain during the last period of operation. At birth, all newborns cried immediately and the mean Apgar scores were 9.8 +/- 0.4 at one minute and 10 at 5 minutes. It is concluded that meperidine, which has advantages such as rapid motor recovery, prolonged postoperative analgesia, and mild complications which may be easily treated, can serve as a good alternative agent for spinal anesthesia for Cesarean section.
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PMID:Intrathecal meperidine as the sole agent for cesarean section. 263 46


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