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)

To evaluate the effects of exploratory laparotomy on cellular and biochemical parameters of blood and peritoneal fluid, an experiment was conducted using 10 Iranian cross-bred male goats. Approximately 10 ml of blood and 1-1.5 ml of peritoneal fluid were collected from all animals prior to operation for estimation of control values. Exploratory laparotomy was performed under local analgesia. Blood and peritoneal fluid samples were collected at 24, 48, 72 and 96 h after exploratory laparotomy. The results revealed that after exploratory laparotomy, the number of white blood cells and the percentage and absolute number of neutrophils and band neutrophils significantly increased (P < 0.05). However, the percentage of lymphocytes decreased significantly (P < 0.05). The concentrations of blood urea nitrogen significantly increased (P < 0.05). Furthermore, following the operation, the percentage and absolute number of neutrophils in the peritoneal fluid significantly increased (P < 0.05). In contrast, the percentage of lymphocytes in the peritoneal fluid decreased significantly (P < 0.05). The concentration of protein in the peritoneal fluid increased significantly (P < 0.05).
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PMID:Evaluation of cellular and biochemical parameters of blood and peritoneal fluid following exploratory laparotomy in the goat. 1084 63

Clinicophysiological, haematological and biochemical effects of xylazine (0.05mgkg(-1)) and medetomidine (0.01mgkg(-1)) were studied in nine adult goats after lumbosacral subarachnoid administration. The onset of analgesia by xylazine and medetomidine was observed in 9.11+/-1.07 and 8.66+/-2.37min (mean+/-S.E.), respectively. Both alpha(2)-agonists produced moderate analgesia of hind quarter, perineum and flank, mild ataxia and sedation. The duration of analgesia after xylazine administration was 134.44+/-8.87min and that after medetomidine was 158.33+/-9.96min (mean+/-S.E.). Xylazine and medetomidine induced significant (p<0.05) decrease in heart rate, respiratory rate and hypothermia. Haemoglobin (Hb), packed cell volume (PCV) and total leukocyte count (TLC) decreased significantly. Changes in the physiological and haematological parameters were transient in nature. Xylazine and medetomidine produced a significant (p<0.05) increase in creatinine and glucose levels. However, these parameters fluctuated within normal range and started to recover within 120min. However, serum urea nitrogen (SUN), serum chloride, sodium and potassium did not show any significant change. The effects produced by xylazine and medetomidine were however, comparable at these dose levels. The study indicates that xylazine at 0.05mgkg(-1) and medetomidine at 0.01mgkg(-1) did not induce any serious alteration in the physiological, haematological and biochemical parameters and can be safely used in inducing hind quarter, flank and perineal analgesia in goats.
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PMID:Physiologic and biochemical effects of subarachnoidally administered xylazine and medetomidine in goats. 1102 38

A study of the effect of transposition of the internal nitrogen atom for the adjacent benzylic carbon atom in delta-selective agonists such as BW373U86 (1) and SNC-80 (2) has been undertaken. It was shown that high-affinity, fully efficacious, and delta opioid receptor-selective compounds can be obtained from this transposition. In addition to the N,N-diethylamido group needed as the delta address, the structural features identified to promote delta receptor affinity in the set of compounds studied included a cis relative stereochemistry between the 3- and 4-substituents in the piperidine ring, a trans-crotyl or allyl substituent on the basic nitrogen, the lack of a 2-methyl group in the piperidine ring, and either no substitution or hydroxyl substitution in the aryl ring not substituted with the N,N-diethylamido group. Structural features found to be important for mu affinity include hydroxyl substitution in the aryl ring, the presence of a 2-methyl group in a cis relative relationship to the 4-amino group as well as N-substituents such as cyclopropylmethyl. It was also determined that mu receptor affinity could be increased while maintaining delta receptor affinity, especially when hydroxyl-substituted compounds are considered. Additionally, it was discovered that the somewhat lower mu/delta selectivities observed for the piperidine compounds relative to the piperazine-based ligands appear to arise as a consequence of the carbon-nitrogen transposition which imparts an overall lower delta and higher mu affinity to the piperidine-based ligands. This higher affinity for the mu receptor, apparently intrinsic to the piperidine-based compounds, suggests that ligands of this class will more easily be converted to mu/delta combination agonists compared to the piperazine ligands such as 1. This is particularly important since analogues of 1, which show both mu- and delta-type activity, are now recognized as important for their strong analgesia and cross-canceling of many of the side effects found in agonists operating exclusively from either the delta or mu opioid receptor.
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PMID:Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl)arylamino]-N,N-diethylbenzamides. 1130 Aug 79

We sought in this prospective study to use a multimodal approach to reduce stress and improve recovery in patients undergoing major surgery. During an initial study period, 30 patients were randomly allocated to receive general anesthesia (GA; Group 1) or a combination of GA and intraoperative thoracic epidural analgesia (TEA; Group 2) when undergoing radical cystectomy. Parenteral nutrition was provided for 5 days after surgery. During the second period, 15 patients were treated with a multimodal approach (Group 3) consisting of intraoperative GA and TEA, postoperative patient-controlled TEA, early oral nutrition, and enforced mobilization. Data for plasma and urine catecholamines, plasma cortisol, the nitrogen balance, the postoperative inflammatory nutrition index, pain relief, fatigue, sleep, overnight recovery, recovery of bowel function, and mobilization were recorded up to the fifth postoperative day. Plasma concentrations of catecholamines and cortisol were comparable in all patients, but those in Group 3 had lower levels of urinary catecholamine excretion. Protein intake was more effective with parenteral nutrition. Nitrogen balances were less negative, and the postoperative inflammatory nutrition index score increased significantly in the traditional groups but not in Group 3. Multimodally treated patients reported less fatigue and better overnight recovery. Along with improved pain relief, recovery of bowel function, and ambulation, there were no differences in the postoperative complication rates among the three groups. The multimodal approach reduced stress and improved metabolism and recovery after radical cystectomy.
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PMID:Multimodal perioperative management--combining thoracic epidural analgesia, forced mobilization, and oral nutrition--reduces hormonal and metabolic stress and improves convalescence after major urologic surgery. 1172 57

A laryngeal mask airway (LMA) and epidural analgesia were used for anesthetic management of microwave coagulo-necrotic therapy for multiple hepatoma in a 76-year-old male with a giant bulla and liver cirrhosis. Since bleeding times, PT and APTT were within normal limits, an epidural catheter was inserted between Th9 and 10 interspaces in operating room. After preoxygenation, general anesthesia was induced with propofol 120 mg. After insertion of a LMA, anesthesia was maintained under spontaneous breathing with sevoflurane (1-1.5%) in about 45% oxygen and nitrogen. During the operation, 2% lidocaine was injected continuously into the epidural space. Continuous epidural injection of 2% lidocaine was found to be very effective for obtaining abdominal muscle relaxation and perioperative pain management. Postoperative chest X ray did not show any signs of rupture of the giant bulla, and any neurological abnormalities due to the epidural hematoma were not encountered. We could reduce the risk of rupture of a giant bulla during general anesthesia using a LMA and epidural analgesia.
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PMID:[Anesthetic management of a patient with a giant bulla and liver cirrhosis using a laryngeal mask airway and epidural analgesia]. 1145 73

Vanilloid receptor subunit 1 (VR1) appears to play a critical role in the transduction of noxious chemical and thermal stimuli by sensory nerve endings in peripheral tissues. Thus, VR1 antagonists are useful compounds to unravel the contribution of this receptor to pain perception, as well as to induce analgesia. We have used a combinatorial approach to identify new, nonpeptidic channel blockers of VR1. Screening of a library of trimers of N-alkylglycines resulted in the identification of two molecules referred to as DD161515 [N-[2-(2-(N-methylpyrrolidinyl)ethyl]glycyl]-[N-[2,4-dichlorophenethyl]glycyl]-N-(2,4-dichlorophenethyl)glycinamide] and DD191515 [[N-[3-(N,N-diethylamino)propyl]glycyl]-[N-[2,4-dichlorophenethyl]glycyl]-N-(2,4-dichlorophenethyl)glycinamide] that selectively block VR1 channel activity with micromolar efficacy, rivaling that characteristic of vanilloid-related inhibitors. These compounds appear to be noncompetitive VR1 antagonists that recognize a receptor site distinct from that of capsaicin. Intraperitoneal administration of both trialkylglycines into mice significantly attenuated thermal nociception as measured in the hot plate test. It is noteworthy that these compounds eliminated pain and neurogenic inflammation evoked by intradermal injection of capsaicin into the animal hindpaw, as well as the thermal hyperalgesia induced by tissue irritation with nitrogen mustard. In contrast, responses to mechanical stimuli were not modified by either compound. Modulation of sensory nerve fibers excitability appears to underlie the peptoid analgesic activity. Collectively, these results indicate that blockade of VR1 activity attenuates chemical and thermal nociception and hyperalgesia, supporting the tenet that this ionotropic receptor contributes to chemical and thermal sensitivity and pain perception in vivo. These trialkylglycine-based, noncompetitive VR1 antagonists may likely be developed into analgesics to treat inflammatory pain.
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PMID:Attenuation of thermal nociception and hyperalgesia by VR1 blockers. 1185 30

The present study was designed to evaluate the analgesic, sedative and haemodynamic effects of spinally administered romifidine in goats. Ten female healthy goats weighing 14-18 kg were randomly divided into two groups, I and II, of five animals each. Romifidine was administered spinally at rates of 50 and 75 microg/kg body weight in the animals of groups I and II, respectively, into the lumbosacral space. The treatments were compared based on their effects on analgesia, sedation, ataxia, heart rate, respiratory rate, rectal temperature, mean arterial pressure, central venous pressure, electrocardiogram and haemato-biochemical parameters. The objective parameters were analysed statistically using paired t-test and Duncan's multiple range test. Depth of analgesia was measured by recording the response to pin prick at different regions and was graded on a scale from 0 to 3. Moderate to complete analgesia was recorded at perineum and flank in both groups. Sedation was moderate in both groups. Ataxia was observed in all the animals but it was more pronounced in group II. Heart rate decreased significantly (P < 0.01) in both groups. A decrease in respiration rate was also recorded in both groups but it was more significant (P < 0.01) and for longer duration in group II as compared to group I. A slight increase in rectal temperature was also observed in both groups. Mean arterial pressure decreased and central venous pressure increased significantly (P < 0.01) in both groups but changes were more pronounced in group II. Electrocardiogram changes in group I included bradycardia, increased QT interval and increased or biphasic T wave but in animals of group II, in addition to these changes, occasional sinus dysrhythmia, increased PR interval and second-degree heart block were also recorded. Haemoglobin and packed cell volume decreased non-significantly in both groups. A significant (P < 0.01) increase in blood glucose and non-significant changes in plasma proteins, urea nitrogen and creatinine were recorded in both groups. The results of the study revealed that romifidine at the rate of 50 microg/kg could produce moderate to complete analgesia of perineum and flank after spinal administration into the lumbosacral space in goats. The analgesia could not be enhanced further by increasing the dose of romifidine up to 75 microg/kg, however, ataxia and cardiopulmonary and haemodynamic side-effects became more apparent.
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PMID:Analgesic, sedative and haemodynamic effects of spinally administered romifidine in female goats. 1191 23

The ethanolic rhizome extract of Kaempferia galanga L. (Zingiberaceae) was studied by conventional pharmacological methods including the Hippocratic screening test, and acute and subacute toxicities in rats. The hexane fraction was tested for dermal irritation in rabbits. The ethanolic extract, when tested by the Hippocratic screening test, demonstrated signs that indicated CNS depression such as a decrease in motor activity and respiratory rate, and a loss of screen grip and analgesia. In the acute toxicity test, oral administration of 5 g/kg of Kaempferia galanga produced neither mortality nor significant differences in the body and organ weights between controls and treated animals. Moreover, both gross abnormalities and histopathological changes were not comparatively detectable between all controls and treated animals of both sexes. In subacute toxicity studies, no mortality was observed when varying doses of 25, 50 or 100 mg/kg of ethanolic Kaempferia galanga extract were administered orally per day for a period of 28 days. There were no significant differences in the body and organ weights between controls and treated animals of both sexes. Hematological analysis showed no differences in any of the parameters examined (WBC count, platelet, hematocrit and hemoglobin estimation) in either the control or treated groups of both sexes. However, the differential leukocyte counts showed a slight but significant decrease of lymphocyte count in the 50 and 100 mg/kg male rat groups. In the blood chemistry analysis, no significant change occurred in the blood chemistry parameters, including glucose, creatinine, blood urea nitrogen (BUN), aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (Alk-P), total protein and albumin of both sexes. Pathologically, neither gross abnormalities nor histopathological changes were observed. No sign of irritation was observed during the dermal irritation test of the hexane fraction of Kaempferia galanga.
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PMID:Toxicity of crude rhizome extract of Kaempferia galanga L. (Proh Hom). 1501 2

Controlled-release oral formulations of oxycodone and morphine are both suitable analgesics for moderate to severe pain. They were compared in cancer-pain patients randomized to double-blind treatment with controlled-release oxycodone (n = 48) or controlled-release morphine (n = 52) every 12 h for up to 12 days. Stable analgesia was achieved by 83% of controlled-release oxycodone and 81% of controlled-release morphine patients in 2 days (median). Following titration to stable analgesia, pain intensity (0=none to 3=severe) decreased from baseline within each group (p </= 0.005), from 1.9 (0.1) to 1.3 (0.1), mean (SE), with controlled-release oxycodone, and from 1.6 (0.1) to 1.0 (0.1) with controlled-release morphine (no significant between-group differences). Typical opioid adverse experiences were reported in both groups. Hallucinations were reported only with controlled-release morphine (n = 2). Visual analog scores (VAS) for 'itchy' and 'scratchin' were lower with controlled-release oxycodone (p </= 0.044), as was peak-to-trough fluctuation in steady-state plasma concentration (p = 0.004). The correlation between plasma concentration and dose was stronger (p = 0.026) for oxycodone (0.7) than morphine (0.3). The relationship between pain intensity (VAS) and plasma concentration was more positive for oxycodone (p = 0.046). There was a positive relationship between morphine-6-glucuronide concentrations and urea nitrogen and creatinine levels (p = 0.001). Controlled-release oxycodone was as effective as controlled-release morphine in relieving chronic cancer-related pain, and as easily titrated to the individual's need for pain control. While adverse experiences were similar, controlled-release oxycodone was associated with less itching and no hallucinations. Controlled-release oxycodone provides a rational alternative to controlled-release morphine for the management of moderate to severe cancer-related pain.
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PMID:Controlled-release oxycodone compared with controlled-release morphine in the treatment of cancer pain: a randomized, double-blind, parallel-group study. 1510 84

Intraspinal pentazocine, 1.5 mg/kg, produced sufficient analgesia and moter block in 50 cases of abdominal total hysterectomy. Pentazocine, a derivative of benzomorphans, shares some common characteristics with local anesthetics in the chemical structure. Both agents have an aromatic ring and an intermediate chain, in common, which connects the former to nitrogen moiety, and the local anesthetic action was anticipated. The onset of the sensory block was 3.2 +/- 0.9 (mean +/- SD) min, and the maximum level was T10 and T4 with mean level of T6. The onset of motor weakness at the knee was 4.1 +/- 1.9 min, and the duration was 108 +/- 10.5 min.
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PMID:Spinal anesthesia with pentazocine for total abdominal hysterectomy. 1523 41


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