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)

Nociceptin is a preferred endogenous ligand for the orphan opioid receptor-like 1 (ORL1) receptor. Central administration of nociceptin showed various pharmacological effects on analgesia, cardiovascular and renal responses, food intake, and so on. In the present study, we investigated the effect of nociceptin injected into the central nervous system (CNS) on gastric acid secretion in the perfused stomach of urethane-anesthetized rats. Injection of nociceptin (0.55-5.52 nmol per rat) into the fourth cerebroventricle stimulated gastric acid secretion and the secretion was inhibited in atropine-treated (1 mg/kg, i.v.) and vagotomized rats. The secretion induced by nociceptin (1.65 nmol) was not inhibited by the central injection of naloxone (275 nmol, a non-selective antagonist of opioid receptors). The secretion was significantly inhibited by the central injection of [Phe(1)psi(CH(2)-NH)Gly(2)]nociceptin-(1-13)-NH(2) ([F/G]nociceptin-(1-13), 0.21 nmol, an antagonist of ORL1 receptor), although [F/G]nociceptin-(1-13) alone at higher doses (2.10 and 7.31 nmol) markedly stimulated gastric acid secretion. In the 0-40 min period, the secretion induced by nociceptin was inhibited at least partially by CompB (68.8 nmol, a nonpeptidic antagonist of ORL1 receptor). Injection of nociceptin (5.52 nmol) into the lateral cerebroventricle also stimulated the secretion. Injection of nociceptin did not modify gastric acid secretion stimulated by 2-deoxy-D-glucose (200 mg/kg, i.v.). In conclusion, nociceptin injected into the CNS stimulated gastric acid secretion in rats via the ORL1 receptors and through mechanisms involving the vagus nerve.
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PMID:Gastric acid secretion stimulated by centrally injected nociceptin in urethane-anesthetized rats. 1200 27

Four enkephalin analogues (Tyr-D-Thr-Gly-Phe-Leu-Ser-CONH(2), 1, and the related O-linked glycopeptides bearing the monosaccharide beta-glucose, 2, the disaccharide beta-maltose, 3, and the trisaccharide beta-maltotriose, 4) were synthesized, purified by HPLC, and biophysical studies were conducted to examine their interactions with membrane model systems. Glycopeptide 2 has been previously reported to penetrate the blood-brain barrier (BBB), and produce potent analgesia superior to morphine in mice (J. Med. Chem.2000, 43, 2586-90 and J. Pharm. Exp. Ther. 2001, 299, 967-972). The parent peptide and its three glycopeptide derivatives were studied in aqueous solution and in the presence of micelles using 2-D NMR, CD, and molecular mechanics (Monte Carlo studies). Consistent with previous conformational studies on cyclic opioid agonist glycopeptides, it was seen that glycosylation did not significantly perturb the peptide backbone in aqueous solution, but all four compounds strongly associated with 5-30 mM SDS or DPC micelles, and underwent profound membrane-induced conformational changes. Interaction was also observed with POPC:POPE:cholesterol lipid vesicles (LUV) in equilibrium dialysis experiments. Although the peptide backbones of 1-4 possessed random coil structures in water, in the presence of the lipid phase they each formed a nearly identical pair of structures, all with a stable beta-turn motif at the C-terminus. Use of spin labels (Mn(2+) and 5-DOXYL-stearic acid) allowed for the determination of the position and orientation of the compounds relative to the surface of the micelle.
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PMID:Glycopeptide-membrane interactions: glycosyl enkephalin analogues adopt turn conformations by NMR and CD in amphipathic media. 1273 23

According to the traditional usage of the plant for antiinflammation and analgesia, Leucas aspera was tested for its prostaglandin (PG) inhibitory and antioxidant activities. The extract showed both activities, i.e., inhibition at 3 x 10(-4) g/ml against PGE(1)- and PGE(2)-induced contractions in guinea pig ileum and a 1, 1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging effect. The separation guided by the activities in these dual assay methods provided eight lignans and four flavonoids, LA-1- -12, among which LA-1- -7 and LA-10- -12 were identified as nectandrin B, meso-dihydroguaiaretic acid, macelignan, acacetin, apigenin 7-O-[6"-O-(p-coumaroyl)-beta-D-glucoside], chrysoeriol, apigenin, erythro-2-(4-allyl-2, 6-dimethoxyphenoxy)-1-(4-hydroxy-3-methoxyphenyl)propan-1-ol, myristargenol B, and machilin C, respectively. LA-8 was determined to be (-)-chicanine, the new antipode of the (+) compound, by spectroscopic methods including CD and ORD. Chiral-HPLC analysis of LA-9 showed that it was a mixture of two enantiomers, (7R, 8R)- and (7S, 8S)-licarin A. All of these components were first isolated from L. aspera. PG inhibition was observed in LA-1, LA-2, and LA-5, and antioxidant activity in LA-1- -3 and LA-8- -12.
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PMID:Separation of Leucas aspera, a medicinal plant of Bangladesh, guided by prostaglandin inhibitory and antioxidant activities. 1273 64

OBJECTIVES: To update information about available neonatal pain assessment and pain relief methods.METHOD: Medical literature review of the past 10 years, including textbooks, general reviews, systematic reviews, prospective, randomized controlled studies, retrospective works and case studies. Literature was reviewed based on the author clinical and scientific experience regarding pain evaluation and treatment.RESULTS: Lack of verbal expression of pain is one of the major impediments to adequate pain relief in the neonatal period. Nowadays, several valid pain assessment tools are available, including the analysis of the neonate facial features and multidimensional tools, as NIPS, CRIES, and PIPP. Non-pharmacological pain relief can be achieved by non-nutritive suction and suction of dextrose water. Neonatal analgesia, in general, includes de the use of paracetamol, opioids and local anesthetics. Opioids remain the main resource for acute pain treatment in the neonatal intensive care unit. Sedatives are important agents to decrease patient activity and restlessness, but they do not relieve pain.CONCLUSION: Based on medical, ethical, and humanitarian grounds, neonatal pain should be considered and treated.
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PMID:[Assessing and treating pain in the newborn] 1468 35

In a randomized double-blind study, 40 healthy women undergoing elective caesarean section with spinal anaesthesia received either 0.3 mg diamorphine or saline with bupivacaine 0.5% in 8% dextrose. The study recorded time to the first morphine demand delivered by patient-controlled analgesia (PCA), and total morphine requirement over 24 h. In addition pain, sedation, and pruritus were assessed by non-graduated visual analogue scores (VAS). Six patients in the diamorphine group required no postoperative morphine. The median (interquartile range) time to first morphine demand was significantly longer in the diamorphine group at 340 min (127, never used), than in the control group at 80 min (53, 159) (P 0.0006, 95% confidence interval for the difference between the medians is 60 to 1235 min). The use of PCA morphine over 24 h was significantly less in the diamorphine group than in the controls. The medians (interquartile ranges) were 5 (0, 36) mg vs 45 (26, 72) mg (P 0.0045, 95% confidence interval for the difference between the medians is 12 to 46 mg). In the diamorphine group, postoperative VAS for pain was significantly lower at 2 h and 3 h both at rest (P 0.0003, 0.003) and on moving (P 0.009, 0.002), at 8 h on moving (P 0.01), and at 12 and 24 h at rest (P 0.005, 0.029). Significantly more women suffered pruritus in the diamorphine group for the first 12 h after surgery (P 0.01).
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PMID:A double-blind assessment of the analgesic sparing effect of intrathecal diamorphine (0.3 mg) with spinal anaesthesia for elective caesarean section. 1532 Dec 58

Healthy women who underwent caesarean section under spinal anaesthesia were studied to determine the extent of postoperative analgesia and side-effects produced by low doses of intrathecal morphine. Patients were randomly allocated to receive, in double-blind fashion, 0 mg (group 1: control group), 0.05 mg (group 2), 0.1 mg (group 3), or 0.2 mg (group 4) of morphine, with 10 mg tetracaine in 10% dextrose 2.5 ml. (n = 20 x 4 groups). The effect of intrathecal morphine was examined in terms of the duration until the first supplemental analgesic was needed and the numbers of the doses within the first postoperative 48 h. Pain relief was significantly greater in groups 3 and 4 than in group 1. The incidence of nausea, vomiting and pruritus increased in a dose-dependent manner. No patient developed respiratory depression. Our results suggest that postoperative analgesia lasts more than 24 h with 0.1 mg or 0.2 mg of intrathecal morphine. Since the incidence of side-effects was higher at 0.2 mg, 0.1 mg may be the optimum dose for caesarean section.
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PMID:Low dose intrathecal morphine and pain relief following caesarean section. 1563 59

Hysteroscopic endometrial ablation (HEA) was introduced in the 1980s to treat menorrhagia. Its use required additional training, surgical expertise and specialized equipment to minimize emergent complications such as uterine perforations, thermal injuries and excessive fluid absorption. To overcome these difficulties and concerns, thermal balloon endometrial ablation (TBEA) was introduced in the 1990s. Four hot liquid balloons have been introduced into clinical practice. All systems consist of a catheter (4-10mm diameter), a silicone balloon and a control unit. Liquids used to inflate the balloons include internally heated dextrose in water (ThermaChoice, 87 degrees C), and externally heated glycine (Cavaterm, 78 degrees C), saline (Menotreat, 85 degrees ) and glycerine (Thermablate, 173 degrees C). All balloons require pressurization from 160 to 240 mmHg for treatment cycles of 2 to 10 minutes. Prior to TBEA, preoperative endometrial thinning, including suction curettage, is optional. Several RCTs and cohort studies indicate that the advantages of TBEA include portability, ease of use and short learning curve. In addition, small diameter catheters requiring minimal cervical dilatation (5-7 mm) and short duration of treatment cycles (2-8 min) allow treatment under minimal analgesia/anesthesia requirements in a clinic setting. Following TBEA serious adverse events, including thermal injuries to viscera have been experienced. To minimize such injuries some surgeons advocate the use of routine post-dilatation hysteroscopy and/or ultrasonography to confirm correct intrauterine placement of the balloon prior to initiating the treatment cycle. After 10 years of clinical practice, TBEA is thought to be the preferred first-line surgical treatment of menorrhagia in appropriately selected candidates. Economic modeling also suggested that TBEA may be more cost-effective than HEA.
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PMID:Second-generation endometrial ablation technologies: the hot liquid balloons. 1754 85

Ketorolac is a nonopioid, anti-inflammatory drug commonly used for postoperative analgesia. Its effectiveness has been previously documented in various orthopedic procedures and more recently in spinal surgery. It remains uncertain if ketorolac has an effect on wound healing. The purpose of this study was to determine if the use of postoperative ketorolac induced deleterious effects on wound healing in a simulated spinal surgery incision using a rat model. A 4-cm dorsal midline incision was made and closed in 36 rats. Rats were divided into 3 groups: (1) 5 mg/kg ketorolac given every 6 hours for 24 hours; (2) 5 mg/kg ketorolac given every 6 hours for 48 hours; and (3) control group given dextrose 5% in water every 6 hours for 48 hours. On postoperative day 14, sutures were removed. Wounds were removed and loaded to failure in tension. The mean+/-SD loads to failure were 9.8+/-1.8 N for group 1, 9.0+/-2.4 N for group 2, and 9.5+/-4.5 N for group 3. The differences among the 3 groups were not statistically significant (P>.05). The use of ketorolac in the immediate postoperative period produces no increased risk of wound complications in this rat model.
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PMID:The effects of postoperative ketorolac on wound healing in a rat model. 1990 87

Surgical injury provokes a stress response that leads to a catabolic state and, when prolonged, interferes with the postoperative recovery process. This study tests the impact of 2 nutrition support regimens on protein and glucose metabolism as part of an integrated approach in the perioperative period incorporating epidural analgesia in 18 nondiabetic patients undergoing colorectal surgery. To test the hypothesis that parenteral amino acid infusion (amino acid group, n = 9) maintains glucose homeostasis while maintaining normoglycemia and reduces proteolysis compared with infusion of dextrose alone (DEX group, n = 9), glucose and protein kinetics were measured before and on the second day after surgery using a stable isotope tracer technique. Postoperatively, the rate of appearance of glucose was higher (P < .001) and blood glucose increased more (P < .001) in the DEX group than in the amino acid group. The postoperative increase in the appearance of leucine from protein breakdown tended to be greater (P = .077) in the DEX group. We conclude that perioperative infusion of a nutrition support regimen delivering amino acids alone maintains blood glucose homeostasis and normoglycemia and tends to have a suppressive effect on protein breakdown compared with infusion of dextrose alone.
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PMID:Glucose and protein kinetics in patients undergoing colorectal surgery: perioperative amino acid versus hypocaloric dextrose infusion. 2042 61

Antinociceptive effect and safety of sub-arachnoid (SAB) midazolam is well established in animals and human beings. In this randomized, prospective placebo control clinical study, we investigated the addition of 2.5mg midazolam to bupivacaine on the quality of surgical anaesthesia and duration of first analgesic in the post operative period after lower uterine caesarean section (LUCS). Sixty ASA I or II pregnant women scheduled for elective lower uterine caesarean section were selected for the study. The patients were randomly allocated to receive 2ml of 0.5% hyperbaric bupivacaine with either 0.5ml of 5% dextrose in aqua or 2.5 mg (0.5ml) midazolam. The duration of first analgesic demand, quality of anaesthesia, haemodynamic changes and neonatal condition were assessed. The duration of analgesia (the time interval in minutes between the sub-arachnoid injection and the first analgesic demand by the patient) was significantly longer in the Group II than Group I (197min vs. 112min; p<0.001). The quality of surgical anaesthesia was excellent or good throughout the surgical procedure in 90% (n = 27) of the patients in Group II (p = 0.01). Systolic Blood pressure was significantly lower in the group I at 10 min and 20 min after administration of SAB than group II (p = 0.005 and p = 0.007) but comparable at other times. Sedation level, Apgar score was comparable in both groups. No neurological deficit or other significant adverse effects were recorded. The addition of midazolam with hyperbaric low dose bupivacaine in SAB significantly improves the quality of surgical anaesthesia and prolongs the duration of analgesia without any adverse effects.
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PMID:Prolonged analgesia by adding midazolam and hyperbaric bupivacaine in subarachnoid block for lower uterine caesarian section. 2095 2


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