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)

A series of dermorphin-like compounds were injected intracerebroventricularly in the rat to assess in vivo their effects on intestinal motility and analgesia. In vitro they were tested by binding assay using 3H-naloxone as radioligand or by guinea pig ileum bioassay. The synthetic peptides were less potent than dermorphin in inhibiting intestinal transit and in producing analgesia, or even inactive up to doses 30 times the dermorphin ED50. This reduction in pharmacological activity was coupled with a decrease in binding potency. The 3H-naloxone binding studies in the absence or presence of Na+ indicated that Na+ reduced the interaction of dermorphin and its analogs with brain opiate receptors. Only the dibenzyl derivative was slightly affected by sodium, suggesting a dual action for this peptide, as confirmed by preliminary data from guinea pig ileum bioassay.
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PMID:Central pharmacological activities and opiate receptor binding studies of some dermorphin analogs. 300 17

Previous studies have reported that elevation of the pH of local anaesthetics is associated with enhanced quality and duration of block. This study investigated the effect, on time to onset and duration of analgesia, of pH adjustment of 0.25 per cent bupivacaine immediately prior to injection into the epidural space in parturients. Addition of 0.1 ml of 8.4 per cent sodium bicarbonate to 20 ml of 0.25 per cent bupivacaine consistently raised the pH of the local anaesthetic from 5.65 to 7.26 (mean values). Thirty parturients received an epidural injection of 8 ml of pH-adjusted 0.25 per cent bupivacaine and a control group of 30 parturients received 8 ml of the standard commercial preparation of 0.25 per cent bupivacaine. Elevation of the pH of the local anaesthetic significantly increased the speed of onset of analgesia from 6.0 minutes to 3.2 minutes and the duration of analgesia was significantly lengthened from 79.4 minutes to 96.5 minutes. There was no significant influence on time to peak effect, nor on mean maternal plasma levels of bupivacaine.
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PMID:Effect of pH-adjustment of bupivacaine on onset and duration of epidural analgesia in parturients. 302 Dec 99

Bupivacaine and chloroprocaine have proven to be valuable local anesthetics for a variety of surgical and obstetrical situations. Bupivacaine is particularly useful as a long acting agent which provides excellent sensory analgesia particularly during labor with minimal blockade of motor fibers. The 0.75% solution is useful for epidural surgical anesthesia since it does result in a decrease in onset time and a more marked motor blockade. In recent years, this agent has been reported to cause rapid cardiovascular collapse in some patients. Cardiotoxicity associated with bupivacaine is related not to the concentration employed but to the total dosage administered as a rapid intravenous injection. The careful administration of this agents to avoid an accidental intravenous injection should not preclude the use of 0.75% bupivacaine for epidural anesthesia in surgical patients. This concentration is not recommended in obstetrical cases. Chloroprocaine is valuable as a rapid onset, short duration local anesthetic with a low potential for systemic toxicity. The 3% solution is particularly useful for providing a rapid onset of action. In recent years, localized neural irritation has occurred in some patients in whom large amounts of this agent were administered epidurally or intrathecally. The local neural toxicity of chloroprocaine solutions is referably to the low pH and the inclusion of sodium bisulfite in these particular solutions. The toxicity of chloroprocaine solutions is related to total dosage rather than the concentration of solution employed. Careful administration of chloroprocaine epidurally in order to avoid accidental subarachnoid injection should preclude the possibility of local neural toxicity.
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PMID:Is there a need for chloroprocaine 3% and bupivacaine 0.75%? 305 87

Experimental data has shown that sodium valproate has analgesic properties in animals, probably by way of the increase in cerebral and spinal gamma amino-butyric acid (GABA) it induces. A study was therefore designed to assess this analgesia in man in the postoperative period. A first open study was carried out on 12 consenting patients, who were each given 15 mg.kg-1 sodium valproate intravenously over 20 min. A significant decrease in pain intensity, measured by an analogic visual scale, was seen from the 20th min up to the 140th min. A controlled double-blind study was then carried out; it included three groups of 13 patients each. Patients in group 1 were given placebo (5% dextrose); group 2 patients were given 15 mg.kg-1 sodium valproate intravenously over 20 min, and group 3 patients 2 mg.kg-1 ketoprofen intravenously over 20 min also. There was no difference in the pain intensity profile of groups 1 and 2: sodium valproate was no more efficient than placebo in relieving postoperative pain. However, ketoprofen gave a prompt and effective analgesic effect. The clinical data obtained with sodium valproate in man during the postoperative period stand in contrast with the promising animal results. Sodium valproate cannot be recommended for the treatment of postoperative pain.
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PMID:[Comparative study of sodium valproate and ketoprofen in the treatment of postoperative pain]. 314 23

Haemodynamic, respiratory, metabolic and endocrine investigations were performed in a total number of 124 patients, divided into four different groups, during opiate anaesthesia for neurosurgical operations in order to characterize general effects of nimodipine, a calcium channel blocking agent with a preferential cerebrovascular action. These studies led to the following conclusions: Nimodipine is a vasodilator drug with a hypotensive action, which is especially obvious in hypertensive patients and in combination with similarly acting agents, such as sodium nitroprusside or nitroglycerin. This vascular hypotensive effect may be also enhanced by combined cardiodepressive activity if nimodipine is applied together with inhaled anaesthetics, such as halothane or isoflurane. Nimodipine as well as other vasodilator drugs may lead to increased pulmonary shunting in patients with artificial ventilation, which, however, can be reduced by adequate positive end-exspiratory pressure. With high doses the decrease of oxygen extraction and consumption, seen with nimodipine, is accompanied by a moderate rise of lactate. Determination of stress hormones did not reveal analgesia potentiation of nimodipine, as has been assumed in other studies.
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PMID:Interactions between nimodipine and general anaesthesia--clinical investigations in 124 patients during neurosurgical operations. 314 99

Serotonin can induce analgesia when injected directly into the brain, but analgesia after peripheral administration has been more difficult to show. The pentobarbital anesthetized mouse (PAM) model, developed to alleviate some of the problems involved in the measurement of tail flick latency, was used to assess the action of peripherally administered serotonin. Mice were anesthetized with about 65 mg/kg of sodium pentobarbital IP and their tail flick latencies measured while they were in stage III anesthesia. In these anesthetized mice, IP serotonin induced a significant analgesia that was much more robust than that found in awake mice. The analgesic effect was dose-dependent from 0.25 mg/kg to 10 mg/kg but was not blocked by the antiopiate naltrexone. Of several psychotropic agents tested, only amitriptyline, mianserin, and trazodone had significant effects on analgesia in the PAM model. The analgesic effect of serotonin was reproduced by the 5HT2 agonist DOI and totally blocked by the 5HT2 antagonist NPP. These results show the utility of the PAM model in studying nonopiate analgesia and suggest that the analgesic action of serotonin is mediated primarily through the 5HT2 receptor.
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PMID:Mediation of serotonin-induced analgesia by the 5HT2 receptor in the pentobarbital anesthetized mouse model. 322 81

A randomized, single-blind, parallel study involving 100 adults was performed to compare the efficacy and safety of naproxen sodium with that of pirprofen in the treatment of moderate to severe pain after orthopaedic surgery. Fifty patients received 550 mg of naproxen sodium initially and 275 mg every 6 h thereafter, and 50 received 400 mg of pirprofen every 8 h until either their pain was completely relieved or the 3-day trial ended. Patients who required additional analgesia were given 500 mg of paracetamol 2 h after administration of the test medication. Both medications significantly relieved post-operative pain, and there were no statistically significant differences in efficacy between the groups. Six patients receiving naproxen sodium and two patients receiving pirprofen withdrew from the study because of lack of efficacy. Thirteen patients receiving naproxen sodium recorded 17 adverse events and 13 patients receiving pirprofen recorded 20 adverse events, again with no statistically significant differences between groups. Six patients in each group withdrew from the study because of these adverse events. Naproxen sodium and pirprofen were equally safe and effective in relieving post-operative pain following musculoskeletal surgery.
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PMID:The comparative efficacy of naproxen sodium and pirprofen in the treatment of post-operative pain. 330 58

Peri-operative blood loss was compared in a prospective, randomized double-blind study between two groups of patients undergoing transurethral prostatectomy (TURP) under spinal (subarachnoid) analgesia: the first received the non-steroidal anti-inflammatory drug diclofenac sodium, the second group received placebo. The total blood loss and the blood loss per gram of prostate resected did not differ significantly. Some 80% of patients were completely pain free at 8 and 24 h post-operation, and low pain scores recorded by the remaining 20% of patients supported the conclusion that TURP performed under spinal analgesia is not commonly associated with severe post-operative pain.
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PMID:Peri-operative blood loss and non-steroidal anti-inflammatory drugs: an investigation using diclofenac in patients undergoing transurethral resection of the prostate. 332 84

This study investigated the potential analgesic effects of medial hypothalamic stimulation (HS) on a measure of nocifensive behavior (tail-flick test (TF] in awake rats, and potential inhibitory effects of identical HS on spinal dorsal horn neuronal responses to noxious skin heating in the same animals anesthetized with sodium pentobarbital. Sixty-five male Sprague-Dawley rats implanted with a bipolar stimulation electrode in histologically verified medial hypothalamic sites were tested behaviorally for TF suppression during HS (100 ms trains at 100 Hz, 3/s, 100-1100 microA) in 2-4 consecutive weekly test sessions. Thirty-three of these rats were then used in electrophysiological experiments to record responses of 36 dorsal horn units to noxious skin heating (48-54 degrees C, 10 s/2 min) of the hindfoot pad in the absence of and during HS. Behaviorally, 31/65 rats had no TF suppression at the highest HS intensity tested (1100 microA), 24/65 rats exhibited aversive behavior or motor activity which disallowed reliable TF testing, and only 10/65 rats showed TF suppression in at least one test session. In electrophysiological experiments, the heat-evoked responses of 25/36 dorsal horn units were inhibited to at least 50% of control during HS. The responses of 11 units remained at 65-100% of the control responses during HS of up to 1100 microA. In rats demonstrating TF suppression, 4/7 units were inhibited. In rats with no TF suppression, 10/15 units were inhibited, and in rats showing aversive behavior, 11/14 units were inhibited by HS. These data indicate that although HS suppresses spinal nociceptive neurons, it does not cause reliable TF suppression in unanesthetized rats and bring into question the often-held assumption that stimulation-evoked descending inhibition of spinal nociceptive neurons implies behavioral analgesia.
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PMID:Medial hypothalamic stimulation suppresses nociceptive spinal dorsal horn neurons but not the tail-flick reflex in the rat. 334 22

Aneurysm of the descending thoracic or thoracoabdominal aorta was repaired in 12 cases during simple aortic cross-clamping. The regimen for anaesthesia and general monitoring is presented. It includes thoracic epidural analgesia with intravenous general anaesthesia, use of a double-lumen endotracheal tube, continuous registration of ECG, body temperature, urinary output, systemic and pulmonary arterial pressures and central venous pressure, and intermittent measurement of pulmonary capillary wedge pressure (PCWP), cardiac output, blood gases and haemoglobin. Mannitol (25-40 g) is infused prior to aortic cross-clamping, and infusion of sodium nitroprusside and possibly nitroglycerin is begun just before clamping to control left ventricular afterload and preload. Sodium bicarbonate is given to maintain positive base excess. Before declamping, ventilation is increased by 50% and rapid infusion of blood, plasma and crystalloids is begun in order to raise PCWP by 3-5 mmHg. The clamp is gradually released, and small doses of vasopressor may be required to stabilize the circulation. The operation was uncomplicated in 11 cases, but a patient with ruptured aneurysm died of myocardial infarction.
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PMID:Anaesthesia in surgery for aneurysm of the descending thoracic or thoracoabdominal aorta. 335 96


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