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

Stress and pain induced by surgical trauma seem to be attenuated when calcium antagonists have been applied. In order to ascertain the effect of nimodipine, a new strong acting calcium channel blocker on plasma levels of various stress hormones twenty patients undergoing cardiovascular surgery where investigated in two groups. Ten patients received high-dose fentanyl anaesthesia (mean: 2,45 mg fentanyl/patient), whereas another ten patients were treated with 0,1 mg fentanyl/patient in addition to nimodipine 1,0 micrograms/kgbw X min (from onset of anaesthesia until start of extracorporeal circulation). Between the two groups were no significant differences with respect to perioperative course and postoperative demand for analgetics. Plasma levels of ACTH, somatotropin, glucose and free glycerol were markedly elevated in all patients (n = 20) intra- and postoperatively, whereas cortisol and prolactin remained unchanged. The present data suggest an additive analgesic effect of nimodipine during surgery. This phenomenon is possibly due to a blocking effect of calcium channel blockers on nociceptive nerves. The present model assumes that calcium is essential in pain perception and that decreased calcium would result in analgesia.
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PMID:[Calcium antagonists in anesthesia. Additive analgesia using nimodipine in heart surgery]. 408 64

During ophthalmic operations the effects of electrostimulation anaesthesia on metabolites, as glucose, glycerol, ketone bodies, and on blood gas and acid base parameters, were investigated in 10 patients with normal circulation and metabolism. They were compared with those of a group operated under neuroleptanesthesia. Both groups of patients were treated with muscle relaxation and controlled normoventilation by a N2O/O2 (1:1) mixture. As the determined parameters gave no evidence of significant differences between the two groups, it is concluded that electrostimulation anaesthesia and neuroleptanaesthesia produce comparable analgesia.
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PMID:[Metabolic investigations under electro-stimulation and neurolept anaesthesia (author's transl)]. 678 95

Ane-Pad (A 2358, Astra Lakemedel AB), a new local anesthetic formulation for application to the skin has been tested in the removal of split skin grafts. Ane-Pad is a thin cotton pad, containing a solution of 10% ketocaine base in a solvent mixture of isopropanol, glycerol and water. The pad has been used on the donor sites of 173 patients with a minimum application time of 1 h before surgery. Eighteen patients complained of slight, transient irritation immediately after application. After removal of the pad erythema was present in 39 patients and oedema in eight. In 157 patients (90.8%) analgesia was adequate. Two patients (1.1%) needed additional anaesthesia. The concentration of ketocaine in the blood was measured in 101 patients and did not exceed 850 ng ml--1. Therewere no systemic side-effects.
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PMID:New anaesthetic formulation for epicutaneous application tested for cutting split skin grafts. 699 Sep 49

Needling of acupuncture points combined with mechanical or electrical stimulation is insufficient for analgesia for surgical interventions. Therefore a new concept of anesthesia was developed: Electrostimulation has been combined with induction of anesthesia, relaxation and controlled ventilation with a mixture of N2O/O2. We have used this method of anesthesia in patients undergoing retinal and vitreous surgery. Our stimulation has been done by self-adhesive electrodes placed bilaterally in the area of trigeminal nerve and cervical plexus. The aim of this study was to investigate the stress response under electrostimulation anesthesia compared with neurolept anesthesia. Therefore the plasma concentrations of adrenaline, noradrenaline, cortisol and some metabolic parameters (glucose, glycerol, NEFA, ketone bodies) as well as heart rate and arterial blood pressure were measured before, during and after surgery. The changes in the parameters under surgery showed that ESA induces a higher stress reaction than NLA. The differences between the two groups are not significant.
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PMID:[Electrostimulation anesthesia in surgery of the retina and vitreous body]. 712 93

Effects of obstetric regional analgesia and of asphyxia on the arterial blood concentrations of the lipid metabolites: glycerol, free fatty acids and beta-hydroxybutyrate were investigated in 85 newborn infants divided into a control group, an asphyxia group, a continuous epidural, an intermittent epidural and a paracervical + pudendal block group: lidocaine was the drug used in the analgesia groups. The postnatal changes in lipid metabolites followed three different patterns. After marked increases in glycerol and free fatty acids a steady level was reached after one hour in the control group and not before two hours in the regional analgesia groups. In the asphyxia group, however, a steady level was found already 10 min after birth. Between 30 and 120 min after birth the beta-hydroxybutyrate concentration increased in the control group, decreased in the asphyxia group and did not change in the three regional analgesia groups. The different patterns of lipid metabolites may indicate differences in sympathetic tone and/or in hormonal influences after birth.
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PMID:Metabolic effects of obstetric regional analgesia and of asphyxia in the newborn infant during the first two hours after birth. II. Arterial plasma concentrations of glycerol, free fatty acids and beta-hydroxybutyrate. 732 34

Glycerin has been used as a drug carrier/depot, but never with local anaesthetics. This study was an attempt to use the slow drug release mechanism to prolong the anaesthetic effects of bupivacaine in epidural block. Twenty-seven adults with cancer pain were prospectively selected according to their primary lesions and problems, but their allocation to study groups was randomized. Group I (n = 13), received 5 ml bupivacaine, 0.125% in normal saline via a previous implanted epidural catheter. When the pain returned to its original intensity, the same amount of the same strength anaesthetic dissolved in 50% glycerin was given via the same catheter. Group II (n = 14) received the same solutions, but in the reverse order. Also five patients in each group received plain 50% glycerin prior to administration of the anaesthetic solutions to serve as controls. The pharmacological effects were assessed by the blinded observers. Analgesia produced with glycerin solution was prolonged compared with the saline solution (12.2 vs 7.2 and 11.6 vs 7.4 hr, P < 0.01). The order of giving the solution did not produce any differences. Plan 50% glycerin did not produce analgesic effects. Neither motor blockade nor other adverse effects or complications were observed in either group. It was concluded that 0.125% bupivacaine in 50% glycerin administered epidurally is not neurotoxic. The prolongation of analgesia observed is attributed to the slow release of bupivacaine from the glycerin base which functions as drug depot. In addition to relief of chronic pain, this novel approach may have other clinical applications such as the relief of labour or postoperative pain.
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PMID:Prolongation of epidural bupivacaine analgesia with glycerin. 851 22

2-Arachidonoyl-glycerol (2-Ara-GI) has been isolated from various tissues and identified as an endogenous ligand for both cannabinoid receptors, CB1 and CB2. Here we report that in spleen, as in brain and gut, 2-Ara-GI is accompanied by several 2-acyl-glycerol esters, two major ones being 2-linoleoyl-glycerol (2-Lino-Gl) and 2-palmitoyl-glycerol (2-Palm-Gl). These two esters do not bind to the cannabinoid receptors, nor do they inhibit adenylyl cyclase via either CB1 or CB2; however, they significantly potentiate the apparent binding of 2-Ara-Gl and its apparent capacity to inhibit adenylyl cyclase. Together these esters also significantly potentiate 2-Ara-Gl inhibition of motor behavior, immobility on a ring, analgesia on a hot plate and hypothermia caused by 2-Ara-Gl in mice. 2-Lino-Gl, but not 2-Palm-GI, significantly inhibits the inactivation of 2-Ara-Gl by neuronal and basophilic cells. These data indicate that the biological activity of 2-Ara-Gl can be increased by related, endogenous 2-acyl-glycerols, which alone show no significant activity in any of the tests employed. This effect ('entourage effect') may represent a novel route for molecular regulation of endogenous cannabinoid activity.
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PMID:An entourage effect: inactive endogenous fatty acid glycerol esters enhance 2-arachidonoyl-glycerol cannabinoid activity. 972 Oct 36

Anandamide [arachidonylethanolamide (AEA)] appears to be an endogenous agonist of brain cannabinoid receptors (CB(1)), yet some of the neurobehavioral effects of this compound in mice are unaffected by a selective CB(1) antagonist. We studied the levels, pharmacological actions, and degradation of AEA in transgenic mice lacking the CB(1) gene. We quantified AEA and the other endocannabinoid, 2-arachidonoyl glycerol, in six brain regions and the spinal cord by isotope-dilution liquid chromatography-mass spectrometry. The distribution of endocannabinoids and their inactivating enzyme, fatty acid amide hydrolase, were found to overlap with CB(1) distribution only in part. In CB(1) knockout homozygotes (CB(1)-/-), the hippocampus and, to a lesser extent, the striatum exhibited lower AEA levels as compared with wild-type (CB(1)+/+) controls. These data suggest a ligand/receptor relationship between AEA and CB(1) in these two brain regions, where tonic activation of the receptor may tightly regulate the biosynthesis of its endogenous ligand. 2-Arachidonoyl glycerol levels and fatty acid amide hydrolase activity were unchanged in CB(1)-/- with respect to CB(1)+/+ mice in all regions. AEA and Delta(9)-tetrahydrocannabinol (THC) were tested in CB(1)-/- mice for their capability of inducing analgesia and catalepsy and decreasing spontaneous activity. The effects of AEA, unlike THC, were not decreased in CB(1)-/- mice. AEA, but not THC, stimulated GTPgammaS binding in brain membranes from CB(1)-/- mice, and this stimulation was insensitive to CB(1) and CB(2) antagonists. We suggest that non-CB(1), non-CB(2) G protein-coupled receptors might mediate in mice some of the neuro-behavioral actions of AEA.
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PMID:Levels, metabolism, and pharmacological activity of anandamide in CB(1) cannabinoid receptor knockout mice: evidence for non-CB(1), non-CB(2) receptor-mediated actions of anandamide in mouse brain. 1108 Jan 95

Since the discovery of an endogenous cannabinoid system, research into the pharmacology and therapeutic potential of cannabinoids has steadily increased. Two subtypes of G-protein coupled cannabinoid receptors, CB(1) and CB(1), have been cloned and several putative endogenous ligands (endocannabinoids) have been detected during the past 15 years. The main endocannabinoids are arachidonoyl ethanolamide (anandamide) and 2-arachidonoyl glycerol (2-AG), derivatives of arachidonic acid, that are produced "on demand" by cleavage of membrane lipid precursors. Besides phytocannabinoids of the cannabis plant, modulators of the cannabinoid system comprise synthetic agonists and antagonists at the CB receptors and inhibitors of endocannabinoid degradation. Cannabinoid receptors are distributed in the central nervous system and many peripheral tissues, including immune system, reproductive and gastrointestinal tracts, sympathetic ganglia, endocrine glands, arteries, lung and heart. There is evidence for some non-receptor dependent mechanisms of cannabinoids and for endocannabinoid effects mediated by vanilloid receptors. Properties of CB receptor agonists that are of therapeutic interest include analgesia, muscle relaxation, immunosuppression, anti-inflammation, antiallergic effects, improvement of mood, stimulation of appetite, antiemesis, lowering of intraocular pressure, bronchodilation, neuroprotection and antineoplastic effects. The current main focus of clinical research is their efficacy in chronic pain and neurological disorders. CB receptor antagonists are under investigation for medical use in obesity and nicotine addiction. Additional potential was proposed for the treatment of alcohol and heroine dependency, schizophrenia, conditions with lowered blood pressure, Parkinson's disease and memory impairment in Alzheimer's disease.
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PMID:Cannabinoids. 1626 85

Both cyclooxygenase-1 and -2 are expressed in the spinal cord, and the spinal COX product prostaglandin E(2) (PGE(2)) contributes to the generation of central sensitization upon peripheral inflammation. Vice versa spinal COX inhibition is considered an important mechanism of antihyperalgesic pain treatment. Recently, however, COX-2 was shown to be also involved in the metabolism of endocannabinoids. Because endocannabinoids can have analgesic actions it is conceivable that inhibition of spinal COX produces analgesia not only by inhibition of PG synthesis but also by inhibition of endocannabinoid breakdown. In the present study, we recorded from spinal cord neurons with input from the inflamed knee joint and we measured the spinal release of PGE(2) and the endocannabinoid 2-arachidonoyl glycerol (2-AG) in vivo, using the same stimulation procedures. COX inhibitors were applied spinally. Selective COX-1, selective COX-2 and non-selective COX inhibitors attenuated the generation of spinal hyperexcitability when applied before and during development of inflammation but, when inflammation and spinal hyperexcitability were established, only selective COX-2 inhibitors reversed spinal hyperexcitability. During established inflammation all COX inhibitors reduced release of spinal PGE(2) almost equally but only the COX-2 inhibitor prevented breakdown of 2-AG. The reversal of spinal hyperexcitability by COX-2 inhibitors was prevented or partially reversed by AM-251, an antagonist at the cannabinoid-1 receptor. We conclude that inhibition of spinal COX-2 not only reduces PG production but also endocannabinoid breakdown and provide evidence that reversal of inflammation-evoked spinal hyperexcitability by COX-2 inhibitors is more related to endocannabinoidergic mechanisms than to inhibition of spinal PG synthesis.
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PMID:Spinal antinociceptive effects of cyclooxygenase inhibition during inflammation: Involvement of prostaglandins and endocannabinoids. 1991 99


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