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)

The effects of thoracic epidural analgesia (TEA) on myocardial performance and metabolism and on the severity of an acute myocardial ischaemia, were studied in eight anesthetized open-chest dogs. TEA reduced mean arterial blood pressure (AP) by 26%, heart rate (HR) by 20%, left ventricular dP/dt by 37%, and myocardial oxygen consumption by 27%. Although arterial concentrations of free fatty acids, glucose and lactate were unchanged, their myocardial uptake was reduced in proportion to the reduction in mechanical activity of the heart. Acute ischaemic injury was estimated from epicardial ECG recordings 10 min after occlusion of a branch of the left anterior descending coronary artery. In seven of eight dogs TEA caused a substantial reduction in the severity of the acute myocardial ischaemic injury. In the eight dogs investigated, the sum of ST segment elevations in epicardial ECG recordings was reduced from 34.0 +/- 3.4 to 23.3 +/- 2.8 mV (mean +/- SEM, P less than 0.01). After restoration of AP and HR to control values with phenylephrine and atrial pacing, the favourable effect of TEA on myocardial ischaemic injury was abolished. It is concluded that TEA effected a reduction in the severity of myocardial ischaemia in open-chest dogs, mainly through reduction of myocardial mechanical activity with consequent reduction of myocardial metabolism.
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PMID:Cardiac effects of thoracic epidural analgesia before and during acute coronary artery occlusion in open-chest dogs. 74 Dec 2

A novel analog of dynorphin (1-13), D-Ala2,F5Phe4-dynorphin amide, was prepared and its pharmacological spectrum of activity was investigated. In a hot plate test on Swiss Webster and C57Bl mice, a 20 micrograms intracerebroventricular (icv) dose of the analog produced analgesia, which was greater in potency and duration than the parent dynorphin. This action of D-Ala2,F5Phe4-dynorphin amide was antagonized by the opiate receptor antagonist naloxone (2 mg/kg ip), administered either before or after the peptide. In addition to its analgesic action in mice, D-Ala2,F5Phe4-dynorphin amide produced a Straub tail and a catatonic-like state, both of which were also attenuated by naloxone. On the electrically-stimulated mouse vas deferens preparation, in vitro, D-Ala2,F5Phe4-dynorphin amide inhibited contractile activity and had an IC50 of 108.2 +/- 34.7 nM (SEM), about 4-fold weaker than that of dynorphin. This action was also attenuated by naloxone. An icv dose of 150 micrograms of D-Ala2,F5Phe4-dynorphin amide in mice, and a cumulative series of icv doses up to 2600 micrograms in anesthetized rats, failed to produce a lethal effect. No pathological changes were observed in mouse liver and kidney at 24 h after a 50 mg/kg dose of the peptide analog. In rats anesthetized with diallylbarbital (70 mg/kg ip) and urethane (280 mg/kg ip), D-Ala2,F5Phe4-dynorphin amide did not modify blood pressure, heart rate and respiratory rate. However, when mice were injected peripherally with single doses of D-Ala2,F5Phe4-dynorphin amide, convulsive episodes were produced, and lethal effects were observed with an LD50 of 60.0 mg/kg (95% confidence limits: 49.7-70.2 mg/kg) at 48 h. This action of D-Ala2,F5Phe4-dynorphin amide was not attenuated by naloxone (2.0 mg/kg, ip). Although analgesic and behavioral effects of D-Ala2,F5Phe4-dynorphin amide (e.g. Straub tail and catatonic-like state) are opiate-like, the lethal effect may be the consequence of actions of the peptide on non-opiate systems, Thus, the novel fluorinated dynorphin analog, D-Ala2,F5Phe4-dynorphin amide, may be a useful chemical tool for the study of opiate systems and their occasionally unanticipated biological or toxic actions.
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PMID:D-Ala2,F5Phe4-dynorphin amide, an opiate with analgesic and toxic properties. 135 36

Caudal epidural analgesia was achieved in 6 adult horses on 3 successive occasions at weekly intervals by injection of lidocaine, xylazine, and a combination of lidocaine/xylazine through indwelling epidural catheters. Analgesia was defined as a lack of response to pinprick and hemostat pressure in the skin of the perineal area. A significant (P < 0.05) difference was not found for time of onset of analgesia between lidocaine (4.3 +/- 0.8 minutes, mean +/- SEM) and the lidocaine/xylazine combination (5.3 +/- 1.3 minutes). Time to onset of analgesia after administration of xylazine was significantly (P < 0.05) longer (32.0 +/- 3.4 minutes) than that for either of the other 2 treatments. Duration of analgesia was significantly (P < 0.05) longer for the combination (329.8 +/- 6.2 minutes) than for either drug used alone (lidocaine, 87.2 +/- 7.5 minutes; xylazine, 204.2 +/- 12.9 minutes). Pulse and respiratory rates were not significantly altered by any of the drugs. Neurologic sequelae were not clinically apparent after administration of the drugs or after chronic epidural catheterization.
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PMID:Comparison of lidocaine, xylazine, and xylazine/lidocaine for caudal epidural analgesia in horses. 142 56

The ventilatory response to CO2 was measured to evaluate the degree of respiratory depression after epidural sufentanil. After cesarean section performed with bupivacaine epidural anesthesia, 14 patients received either 30 micrograms (n = 7) or 50 micrograms (n = 7) of epidural sufentanil. Respiratory measurements were made before and 15, 45, and 120 min after sufentanil injection. The presence and severity of sedation and other nonrespiratory side effects were evaluated throughout the study. Plasma sufentanil assays were performed on blood samples obtained at frequent intervals during the first 2 h. Although changes in resting ventilation did not occur, both sufentanil doses depressed the ventilatory response to CO2. After sufentanil 30 micrograms, the slope of the CO2 response curve decreased significantly at 45 and 120 min (control value, 2.33 +/- 0.3 L.min-1.mm Hg-1 [mean +/- SEM] vs 1.61 +/- 0.24 and 1.72 +/- 0.15, respectively, P less than 0.05). After sufentanil 50 micrograms, significant decreases occurred at 15 and 45 min (control value, 2.84 +/- 0.71 vs 1.81 +/- 0.48 and 1.48 +/- 0.31 L.min-1.mm Hg-1, respectively). The mean maximal decrease in the slope occurred at 45 min and was more pronounced after 50 micrograms (-42.3% +/- 7.4%) than after 30 micrograms (-27.4% +/- 9.9%). Analgesia was similar in both groups. Side effects, particularly sedation, were more severe with the 50-micrograms dose. We conclude that 30 micrograms of epidural sufentanil is preferable to the higher dose with regard to both respiratory and nonrespiratory side effects. Even with the lower dose, monitoring of ventilation is advisable for a minimum of 2 h.
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PMID:Respiratory effects of epidural sufentanil after cesarean section. 153 6

We have compared the performance of the Baxter disposable with the Graseby electronic patient-controlled analgesia system in 30 patients following major gynaecological surgery. Patients were allocated randomly to receive analgesia via the Baxter or Graseby device for postoperative pain relief. There were no significant differences between the two groups with regard to postoperative pain relief or sedation as measured by visual analogue scale. Requirements for antiemetic drugs and patient acceptability were similar. Mean (SEM) morphine demanded over 30 h was 35.7 (6.6) in the Graseby group and 35.1 (8.5) in the Baxter group.
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PMID:Electronic and disposable patient-controlled analgesia systems. A comparison of the Graseby and Baxter systems after major gynaecological surgery. 153 90

The results from 44 experiments performed on 13 rats with chronically implanted lumbar subarachnoid catheters are reported. ICI 197 067 produced dose-dependent segmental analgesic effects when measurement of electrical current threshold for pain was used as the nociceptive test. Ten microliters of intrathecal ICI 197 067 (0.06 mg ml-1; 1.5 nmol) caused a significant rise in the current threshold for pain in the tail of 1.56 +/- 0.04 x control (mean +/- SEM) but no significant change in pain threshold in the neck (1.03 +/- 0.03 x control). By contrast, simultaneous measurements of tail-flick latency in these animals revealed no significant rise in pain thresholds using this nociceptive test. Intraperitoneally administered naloxone produced a dose-dependent suppression of the spinally mediated analgesic effect produced by ICI 197 067; the ED50 for this effect was 0.79 mumol kg-1, a value very close to the ED50 for naloxone antagonism of ketocyclazocine spinally mediated analgesia. We conclude that ICI 197 067 produces spinally mediated analgesia by binding to spinal-cord kappa-opioid receptors.
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PMID:Analgesia mediated by spinal kappa-opioid receptors. 165 58

Laparoscopic cholecystectomy is rapidly becoming the preferred therapy for symptomatic cholelithiasis. It was our impression that the necessary traction exerted on the gallbladder during this procedure would frequently lead to intraoperative perforation with bile leak. We sought to determine prospectively the incidence of gallbladder perforation during laparoscopic cholecystectomy and to ascertain whether or not intraoperative bile leak resulted in overt complications. Laparoscopic cholecystectomy was performed successfully on 250 patients between November 1989 and December 1990. Gallbladder perforation occurred in 80 patients (32%). Compared with those without a bile leak, there was a larger percentage of men (p < 0.05), and the average weight was greater (p < 0.01) in those developing a bile leak. Operating time was significantly longer in patients with gallbladder perforation (mean +/- SEM, 104 +/- 4 min) than in those without a bile leak (94 +/- 3 min, p < 0.01), presumably because of the increased time spent irrigating the abdomen and retrieving gallstones. There was no difference in postoperative serum liver enzymes, amount or type of analgesia administered, interval to return to work or to full activity, or the development of postoperative infections. A wound infection requiring antibiotic therapy developed in only one patient who had not suffered a bile leak. The incidence of bile leak during the performance of laparoscopic cholecystectomy is therefore appreciable, occurring in approximately a third of our patients. Gallbladder perforation does not lead to any other adverse complications and should not cause the surgeon to convert to an open cholecystectomy.
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PMID:Does intraoperative gallbladder perforation influence the early outcome of laparoscopic cholecystectomy? 166 95

Eight patients (7 men and 1 woman, 45-68 yr old) scheduled to undergo thoracotomy were given, preoperatively, 15 micrograms sufentanil in the lumbar intrathecal space for a study of cerebrospinal fluid (CSF) and plasma kinetics of sufentanil. Multiple samples of plasma and CSF from the lumbar region were obtained through indwelling catheters for 12 h and analyzed for sufentanil by radioimmunoassay. Pharmacokinetic parameters were derived by noncompartmental analysis. In plasma, the maximal concentration of sufentanil appeared after 0.65 +/- 0.17 h (mean +/- SEM). No equilibrium was reached between the sufentanil concentration in CSF and plasma, but the CSF/plasma concentration ratio declined from approximately 140 at 2 h to about 15 at 10 h. Extrapolation indicates that another 10 h would be required before the concentration in CSF would equal that in plasma. The mean residence time (MRT) of sufentanil in CSF was 0.92 +/- 0.08 h and in plasma was 6.8 +/- 0.6 h. The volume of distribution at steady state (Vss) in the subarachnoid compartment was 1.54 +/- 0.39 ml/kg, and the clearance from the CSF was 27 +/- 5 microliters.kg-1.min-1. The intrathecal administration of 15 micrograms sufentanil at the beginning of the operation did not produce analgesia that lasted into the postoperative period. Most patients had urinary retention, but none experienced any serious complications. This study demonstrates that the lipophilic opioid sufentanil undergoes rapid clearance from CSF and absorption to plasma after intrathecal administration. These pharmacokinetic characteristics are slower for the less lipophilic opioids meperidine and morphine. The rapid pharmacokinetics of sufentanil explain its rapid onset of action and short-lasting effects.
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PMID:The CSF and plasma pharmacokinetics of sufentanil after intrathecal administration. 167 23

Nineteen patients undergoing elective gastrointestinal surgery were randomised to receive recombination human growth hormone (n = 9) or placebo (n = 10) for the first five postoperative days. All received epidural analgesia and total parenteral nutrition during the same period (energy supply 125% of basal metabolic rate, mean nitrogen (+/- SEM) 5.7 (+/- 0.1) g/m2). Nitrogen and potassium retention was induced in the growth hormone group compared with the placebo group (cumulative nitrogen balance 4.1 (+/- 1.1) g/m2 in the growth hormone group and -3.1 (+/- 1.8) g/m2 in the placebo group, p less than 0.01; cumulative potassium balance 80.8 (+/- 4.7) mmol/m2 in the growth hormone group and 43.1 (+/- 11.4) mmol/m2 in the placebo group, p less than 0.01). In the growth hormone group, serum glucose concentrations increased each evening and mean serum albumin concentrations were reduced throughout the period; the morning pulse rates were decreased, and the patients gained weight compared with the placebo group.
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PMID:Nitrogen retention caused by growth hormone in patients undergoing gastrointestinal surgery with epidural analgesia and parenteral nutrition. 167 77

The incidence, character and treatment of backache associated with epidural anesthesia (EA) using 3% chloroprocaine (2-CP, Nesacaine-MPF) were observed in ten volunteers undergoing a study of the effects of EA upon plasma catecholamines. Three levels of epidural analgesia were sequentially sought, T10, T4 and C8, in ascending order. Each block was allowed to fully dissipate prior to the next injection. For the first, second and third injections, 15-20 ml, 25-35 ml and 52-60 ml, respectively, of 3% 2-CP were injected via an epidural catheter. Mean total volume of 2-CP injected was 103 ml (range, 92-115 ml) over seven hours. Back pain was first reported after as little as 15 ml (mean +/- SEM, 24.0 +/- 3.9 ml; range, 15-45 ml). The pain was described as a dull ache deep in the lumbar back, ranging in severity from mild to severe. No profound spasm of the erector spinae muscles was observed. Mean verbal analog scale pain scores after regression of the first, second and third blocks were 2.2, 4.3 and 6.5, respectively. Epidural fentanyl (100-200 micrograms) was effective in providing rapid relief of the pain. Large doses or possibly repeated injections of epidural Nesacaine-MPF are associated with an increased incidence and severity of postanesthesia lumbar back pain.
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PMID:Back pain after epidural anesthesia with chloroprocaine in volunteers: preliminary report. 183 45


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