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)

Anti-writhing assays to detect analgesia or specific activity against selected agonists were performed on albino mice. Acetylcholine Cl, bradykinin triacetate, phenylquinone, and serotonin creatinine sulfate were used as agonists. 10 compounds, including 5 standard analgetics, were tested against each agonist. Attempts to study histamine phosphate as an agonist were not successful. Results of these investigations showed satisfactory analgetic acitivity for codeine phosphate and acteyl salicylic acid (ASA) in all assays. weaker analgetics displayed varying degrees of activity depending on the agonist tested. Acute oral toxicities were determined for the 10 test compounds and the analgetic ED50 vs the LD50 of each compound was compared. The data confirmed the nonspecificity for writhing assays as well as a variability in activity of the test compounds against the various agonist.
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PMID:Comparative analgetic testing of various compounds in mice using writhing techniques. 58 70

Blood urea content and the serum concentrations of sodium, creatinine, uric acid, glutamic oxaloacetic transaminase (g.o.t.), glutamic pyruvate transaminase (g.p.t.) and bilirubin were measured before delivery, on the 2nd and 3rd days and on the 5th day after delivery. In two groups of mothers, one receiving nitrous oxide analgesia and the other a combination of nitrous oxide and methoxyflurane, blood urea and serum sodium and g.o.t. were increased following labour and nitrous oxide analgesia; s.g.p.t. was increased only in the late post-partum period. Serum sodium, creatinine, uric acid, urea, g.o.t. and g.p.t. increased following exposure to methoxyflurance. The increase in serum sodium, uric acid and urea was dose-dependent. Capillary concentrations of uric acid in the neonates showed dose-dependent changes in response to methoxyflurane.
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PMID:Influence of methoxyflurane-nitrous oxide analgesia during childbirth on renal and hepatic function. 58 3

Two postoperative cardiopulmonary bypass patients who had pancreatitis within a two week period provided the impetus for pursuing this study. Amylase-creatinine clearance ratios (ACCR) were measured in a series of ten thoracic surgery patients: six coronary artery bypass patients with cardiopulmonary bypass (cardiac group), and four exploratory thoracotomy patients (pulmonary group). These ratios were obtained in the preoperative, recovery room, and postoperative periods. Comparisons were made among the following data: clinical history, pre- and postoperative medications, intraoperative vital signs, drugs, and anesthetics. The preoperative mean ACCR was 3.34 per cent. All cardiac patients had a significantly elevated ACCR in the recovery room with a mean of 17.36 per cent (p less than 0.05). The ACCR had returned to preoperative levels by the second postoperative day in five of six cases. There were no elevated ACCR levels in the pulmonary group. All patients were asymptomatic for pancreatitis. The intraoperative course of the cardiac patients involved four common factors, besides cardiopulmonary bypass, which were not present in the pulmonary group. These similarities included transfusion of citrated fresh whole blood activated by calcium chloride, hypotension treated with ephedrine, administration of mannitol, and intraoperative morphine analgesia. The mechanisms of increased amylase secretion by calcium chloride or ephedrine administration and transient sphincter of Oddi constriction by morphine or the alpha-adrenergic response of ephedrine are considered with the theoretical implications toward pancreatitis. The background and significance of the ACCR are also analyzed, especially in association with the osmotic diuresis of mannitol and a subsequent low urine creatinine level.
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PMID:Eelvated postoperative renal clearance of amylase without pancreatitis after cardiopulmonary bypass. 84 59

Methoxyflurane (MOF) administration for conscious analgesia during vaginal delivery (range 5 to 70 min, mean 23 min) or for anesthesia following delivery of the infant at cesarean section (range 25 to 70 min, mean 44 min) was studied in 18 healthy parturients. Serum ionic fluoride increased significantly in both groups 2 hours after discontinuing MOF with peak concentrations of 11.2 and 14.1 mumol/L in the vaginal delivery and cesarean section groups, respectively. Individual peak serum ionic fluoride levels in the 2 groups of 21 and 25 mumol/L were well below reported levels for subclinical toxicity. Significant ionic fluoride elevations in fetal umbilical venous blood (mean 5.3 mumol/L) were measured in the vaginal-delivery group. Maternal urinary ionic fluoride and oxalate were elevated 24 and 48 hours postpartum. BUN, creatinine, urine volume, and urine osmolality remained within normal range. These data indicate that hazardous elevations of serum ionic fluoride with subsequent renal dysfunction are unlikely following low-dose MOF administration for vaginal delivery or cesarean section.
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PMID:Methoxyflurane biotransformation and renal function following methoxyflurane administration for vaginal delivery or cesarean section. 94 23

1. The pharmacokinetics, cardio-respiratory effects and analgesic effects of intravenous morphine-6-glucuronide were studied in 20 cancer patients with pain. Four different dose levels (0.5, 1, 2, and 4 mg 70 kg-1) were studied. Plasma concentrations of morphine-6-glucuronide were measured for 12 h after dosing. Pulse rate, respiratory rate and blood pressure were monitored, and pain relief was measured using two rating scales and a visual analogue scale. 2. The mean elimination half-life (+/- s.d.) of morphine-6-glucuronide was 3.2 +/- 1.6 h. The mean AUC standardised to a dose of 1 mg 70 kg-1 was 390 +/- 263 nmol l-1 h. Mean morphine-6-glucuronide clearance was 96 +/- 38 ml min-1. There was a direct relationship between morphine-6-glucuronide plasma clearance and calculated creatinine clearance (r = 0.81, P less than 0.001). 38 +/- 22% of the dose of morphine-6-glucuronide was recovered unchanged in the urine in 24 h. No morphine or morphine-3-glucuronide was detected in the plasma or urine of any patient after morphine-6-glucuronide treatment. 3. Morphine-6-glucuronide exerted a useful analgesic effect in 17/19 assessable patients for periods ranging between 2 and 24 h. No correlation was observed between dose or plasma morphine-6-glucuronide concentrations, and duration or degree of analgesia. No clinically significant changes in cardio-respiratory parameters were observed. No patients reported sedation or euphoria. Nausea and vomiting were notably absent in all cases. 4. Morphine-6-glucuronide is an effective and well-tolerated analgesic. It is likely that the majority of the therapeutic benefit of morphine is mediated by morphine-6-glucuronide.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:The analgesic activity of morphine-6-glucuronide. 141 74

Morphine-6-glucuronide is a metabolite of morphine that binds to the opioid receptor and is analgesic in animals and humans. Although accumulation of morphine-6-glucuronide in patients with renal insufficiency has been implicated in morphine toxicity, the contribution of the metabolite to morphine analgesia in patients with normal renal function has not been established. To evaluate this contribution, we repeatedly sampled blood and assessed effects during and after a loading infusion with morphine (mean duration, 168 minutes) in 14 patients with chronic pain, all of whom had normal serum creatinine levels. Plasma concentrations of morphine and morphine-6-glucuronide were assayed by use of high performance liquid chromatography with electrochemical detection. Patients were divided into three groups on the basis of the molar concentration ratio of morphine-6-glucuronide:morphine from the start of the infusion until 240 minutes later: Group 1 (n = 5) had a mean ratio greater than or equal to 0.7:1; group 2 (n = 4) had a mean ratio less than 0.7:1 but greater than or equal to 0.4:1; and group 3 (n = 5) had a mean ratio less than 0.4:1. Time-effect plots revealed that average and peak relief were greater in group 1 than group 2 and greater in group 2 than group 3. For all patients, mean morphine-6-glucuronide:morphine ratio throughout the study was significantly correlated with mean pain relief (r = 0.611, p less than 0.02). These data suggest that morphine-6-glucuronide contributes to morphine analgesia in patients with normal renal function. The role of the metabolite should be considered when morphine is used clinically.
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PMID:The metabolite morphine-6-glucuronide contributes to the analgesia produced by morphine infusion in patients with pain and normal renal function. 156 12

We have studied the efficacy of a continuous i.v. infusion of diclofenac 2 mg kg-1/24 h given for 2 days after major thoracic surgery in 30 patients in a double-blind, placebo-controlled, parallel-group design. The patients were able to obtain additional pain relief as on demand morphine boluses. In the diclofenac group, the consumption of morphine was reduced by 60% during the first and by 76% during the second day after operation compared with the control group. Overall, analgesia was also superior in the diclofenac group. Arterial oxygenation was significantly greater and the arterial PCO2 increased less during the first day after operation in the diclofenac group compared with the control group. Diclofenac had no significant effect compared with placebo on blood loss or on any bleeding or platelet test. Urine output was significantly less during the first day after operation in the diclofenac group compared with the control group, but was normal on the second day after operation; plasma creatinine concentrations were unchanged. I.v. diclofenac infusion combined with opioids delivered via a patient-controlled analgesia device seems a valuable method of pain relief after thoracic surgery in patients in whom more invasive techniques, such as extradural local anaesthetics and opioids, cannot be used. However, non-steroidal anti-inflammatory drugs should be used cautiously, if at all, in patients who are at risk of acute renal failure.
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PMID:IV diclofenac in post-thoracotomy pain. 164 35

Telazol was evaluated as an anesthetic for rabbits. Two groups of five rabbits each were injected intramuscularly with 32 or 64 mg/kg of Telazol, and the depth and duration of anesthesia period monitored. At both doses, the righting reflex was lost within 2 minutes postinjection. Animals in both groups responded to noxious stimuli for the duration of the anesthesia. Hematology and urinalyses were performed daily for 7 days postinjection. Hematologic parameters remained unchanged in both groups. In the high-dose group, blood urea nitrogen and serum creatinine levels increased 1 day postinjection and continued steadily throughout the week. Elevations in urine protein and the presence of casts correlated with this increase. In the low-dose group, blood urea nitrogen and creatinine levels increased and protein was present in the urine of four of five rabbits beginning approximately 5 days postinjection. Histologically, severe renal tubular necrosis was evident 7 days postinjection in all high-dose rabbits and in three rabbits in the low-dose group. Our results indicate that Telazol does not produce analgesia in rabbits and is nephrotoxic at both 32 and 64 mg/kg. We conclude that Telazol is contraindicated for use in rabbits.
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PMID:Anesthetic and nephrotoxic effects of Telazol in New Zealand white rabbits. 166 43

Total intravenous anesthesia with droperidol, fentanyl, and ketamine (FK) was administered to 56 pediatric surgical patients ranging in ages from 5 to 15 years to evaluate their hemodynamics during anesthesia, post-operative hepatic as well as renal functions, and post-operative sedation as well as analgesia. These data were compared with those of the patients who underwent almost the same surgical procedures under enflurane-N2O anesthesia. The post-operative s-GOT, s-GPT, BUN, creatinine levels were not elevated significantly as compared with pre-operative levels in the FK group. As compared with those patients who received enflurane anesthesia, the blood pressure in the FK groups was higher by 15-30 mmHg, but it was stable during anesthesia without any complications. Their post-operative sedation and analgesia were better in the FK group than in the enflurane group and the complications such as nausea and vomiting were observed less frequently in the FK patients than in the patients who received anesthesia with ketamine alone reported in literatures. The data described above suggest that this method of anesthesia deserves further detailed clinical trials for pediatric patients.
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PMID:[Clinical study on total intravenous anesthesia with droperidol, fentanyl and ketamine--13. Application for pediatric patients]. 177 May 77

Factors which might affect paracetamol disposition have been studied in a heterogenous group of patients in need of mild analgesia in an intensive care unit. Following oral administration of 1 g of paracetamol, plasma and urinary concentrations of the parent compound and metabolites were assessed by HPLC. The renal clearance of paracetamol was significantly correlated with urine flow (r = 0.84) and creatinine clearance (r = 0.77), but not with urine pH. Metabolite output was diminished in patients with reduced renal function. Despite the heterogeneity of patients and the diversity of drug treatment, the urine to plasma paracetamol concentration ratio appeared remarkably constant in patients with normal renal function (9.8 +/- 2.7). It is concluded that the metabolite to paracetamol ratio may only be regarded as a measure of the drug metabolizing capacity in subjects with normal renal function, if factors influencing urine volume and paracetamol absorption are standardized.
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PMID:Paracetamol test: modification by renal function, urine flow and pH. 225 60


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