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 establish the relationships between epidural sufentanil analgesia and respiratory effects and to determine the pharmacokinetics of the drug, 22 adult patients undergoing thoracotomy were put into a randomized, double-blind study and received either 30, 50, or 75 micrograms per dose in 20 ml normal saline solution. Repeated doses were given on request for the 24-hour study period. There was a weak but significant nonlinear correlation between length of effective analgesia and the cumulative dose of the drug (r = 0.26, p less than 0.001). In 12 of 22 patients, the maximal length of effective analgesia was reached before the last dose and the effect tended to taper off thereafter. The mean maximal length of effective analgesia was 4.69 +/- 0.32 hours (mean +/- SEM), whereas the length of effective analgesia with the last dose was only 3.34 +/- 0.46 hours (p less than 0.0005). There was a significant correlation between the peak serum concentrations of sufentanil during the dose interval and the length of effective analgesia (r = 0.44, p less than 0.0001). Area under the concentration-time curve was proportional to the size of the epidural dose, and with all three doses tested there was a gradual accumulation of sufentanil in the serum. Mean time-to-peak concentration (tmax) increased with repeated doses (p less than 0.05). Mean serum concentration of sufentanil during periods of slow respiratory rate (0.47 +/- 0.05 ng/ml) was significantly higher than during episodes without adverse respiratory effects (0.37 +/- 0.05 ng/ml, p less than 0.05). The above data suggest that an important part of the analgesic and adverse effects of sufentanil are mediated centrally, after this opioid is absorbed systemically.
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PMID:Relationship between the pharmacokinetics and the analgesic and respiratory pharmacodynamics of epidural sufentanil. 252 72

Six groups of ten women each in active labor at term had epidural catheters placed in the usual manner and received a 3 mL test dose of 2% lidocaine with epinephrine. Groups 1-6 received, respectively, 5, 10, 20, 30, 40 and 50 micrograms of sufentanil diluted to 10 mL with normal saline. Significantly effective analgesia was provided at all sufentanil doses studied, with pain scores decreasing from 8.1 +/- 0.2 at baseline to 2.9 +/- 0.3 at 10 minutes and 1.1 +/- 0.2 at 30 minutes (mean +/- SEM, average for all groups). The duration of analgesia showed a significant (p less than 0.05) relation to sufentanil dose, increasing from 79.1 +/- 11.3 minutes (5-micrograms group) to 137.8 +/- 17.2 minutes (50-micrograms group). There were no serious maternal side effects, although ten patients developed pruritus, four became dizzy, two experienced mild sedation, and one had transient hypotension. No neonatal side effects occurred. Maternal serum sufentanil levels remained below the sensitivity of the assay, or 0.1 ng/ml.
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PMID:Epidural sufentanil for analgesia for labor and delivery. 257 52

Experimental data and anecdotal clinical observations have shown that clonidine, an alpha 2-agonist, has a marked analgesic effect. We investigated clonidine-induced analgesia in response to nociceptive stimuli. On 2 different days 7 normal volunteers received either placebo or clonidine (200 micrograms) orally according to a cross-over, double-blind, randomized, placebo-controlled design. Analgesia was assessed by measurement of the subjective (VAS) and objective (R III reflex) pain thresholds. A close correlation was observed between subjective and objective pain thresholds (r = 0.88, y = 0.2 + 1.2 x). Clonidine increased the objective threshold by 21% (+6.2 mA, SEM 2.4) and the subjective threshold by 10% (+2.4 mA, SEM 1.3). Drug effect was rapid (peak between 90 and 120 min) and overall analgesia lasted up to 4 hours. Side effects were a moderate fall in blood pressure, sedation and dryness of the mouth. A single oral dose of clonidine induces significant analgesia. These results suggest that clonidine is potentially a worthwhile drug for pain treatment which deserves further clinical investigation.
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PMID:[Analgesic effects of an oral dose of clonidine]. 261 77

The purpose of this study was to compare the effectiveness and safety of etidocaine and bupivacaine for postoperative analgesia after laparoscope sterilization. The study was performed in 22 healthy patients who received either one per cent etidocaine, 2 mg.kg-1, or bupivacaine 1.5 mg.kg-1 in a double-blind, randomized fashion. The local anaesthetic was dropped onto the fallopian tubes from uterus to fimbriae before tubal occlusion. To establish safety, blood concentrations of the parent drug and its metabolites were measured before application and at 1, 3, 6, 10, 15, 30, 60 and 120 min. The mean peak concentrations were 501.8 +/- 71.3 (SEM) for etidocaine with a range of 225 to 905 ng.ml-1. For bupivacaine, the mean peak concentration was 468 +/- 73.8 SEM with a range from 191 to 1005 ng.ml-1. The mean values are one eighth of the toxic convulsive dose for humans. Etidocaine was metabolized at a faster rate than bupivacaine with a rapid appearance of 2-amino-2'-butyroxylidide (ABX). The bupivacaine metabolite 2,6-pipecoloxylidide (PPX) was detected in low concentrations in the 60-minute samples. We conclude that the topical application of either etidocaine or bupivacaine is a safe procedure in the doses and concentrations used during general anaesthesia for laparoscopic tubal banding.
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PMID:Topical bupivacaine and etidocaine analgesia following fallopian tube banding. 267 20

In a randomized study, 94 patients with term pregnancies underwent augmentation of labor with either continuous or pulsed (every 8 minutes) intravenous oxytocin infusion. There were no significant differences with respect to the maternal characteristics, cervical dilatation and effacement, induction-to-labor interval, induction-to-delivery interval, cesarean section rate, analgesia for labor, or low Apgar scores. No hyperstimulation was noted in either group. In each group, 20% of the patients had dysfunctional labor patterns, with coupling and tripling of the uterine contractions. The mean +/- SEM oxytocin administered in the pulsed-infusion group was significantly lower than that in the continuous-infusion group (2.1 +/- 0.4 versus 4.1 +/- 0.4 mU/minute; P less than .001). The mean +/- SEM total amount of oxytocin administered was 1300 +/- 332 mU for the pulsed group and 1803 +/- 302 mU for the continuous group, indicating that lower amounts of oxytocin were required for pulsed administration. Our study demonstrates that pulsatile administration of oxytocin is similar in efficacy to our standard continuous oxytocin infusion and requires a lower total amount and rate of oxytocin administered, which may afford a greater margin of safety.
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PMID:Pulsatile administration of oxytocin for augmentation of labor. 268 76

The effects of intrathecal midazolam and fentanyl on electrical current threshold for pain were measured using stimulating electrodes in the neck and tail of rats with chronically implanted lumbar subarachnoid catheters. This involved the measurement of the minimum current (50 Hz 2 ms pulses 0-5 mA), which made the rat squeak when applied alternately to electrodes at each skin site. The responses measured in milliamperes were expressed as a number of times control readings. Equieffective doses of both midazolam and fentanyl produced a significant increase in electrical threshold for pain in the tail (mean +/- SEM 3.14 +/- 0.51 and 2.89 +/- 0.35: P less than 0.05; Wilcoxon sum rank test) in the absence of any change in the neck (mean +/- SEM 1.28 +/- 0.13 and 0.96 +/- 0.12, NS), thus demonstrating a spinal effect. Fentanyl caused a significant simultaneous increase in tail flick latency (mean +/- SEM 67.8 +/- 20.1%, P less than 0.05), but midazolam did not (mean +/- SEM 4.22 +/- 2.76%, NS). Intraperitoneal injections of naloxone (0.25 mg/kg) blocked the response to fentanyl in both tests and did not affect the response to midazolam. Intraperitoneal flumazenil (5 mg/kg) blocked the midazolam antinociceptive effect but did not affect the response to fentanyl in either test. Tail withdrawal in response to non-noxious stimulation was preserved in all animals with spinal analgesia, indicating that myelinated afferent and efferent pathways were still functioning. Righting reflex, coordination, motor power, and alertness were also preserved in the presence of both drugs. Both drugs caused spinally mediated antinociceptive effects that were qualitatively different.
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PMID:Intrathecal midazolam and fentanyl in the rat: evidence for different spinal antinociceptive effects. 271 11

The frequency and severity of oxyhemoglobin desaturation was compared in 49 patients receiving epidural morphine, 5 mg (n = 21); patient-controlled analgesia (PCA) using meperidine (n = 20); or intramuscular (im) meperidine (n = 8) for postoperative analgesia following elective cesarean section performed with epidural anesthesia. Oxygen saturation (SpO2) was monitored for 24 h using a pulse oximeter; data were continuously collected and stored every 30 s via an interface connected to a computer. For analysis purposes, SpO2 was divided into five categories: 96-100%, 91-95%, 86-90%, 81-85%, and less than or equal to 80%. Although SpO2 remained above 95% for the majority of the monitored period, patients in all groups experienced periods of desaturation. PCA patients spent the longest cumulative time with SpO2 between 91 and 95%, 231 +/- 49 min (mean +/- SEM), compared with only 112 +/- 30 min and 152 +/- 42 min for the epidural and im groups, respectively (P less than 0.05 vs. epidural group). PCA patients also spent longest with SpO2 at 86-90% (19 +/- 10 min, vs. 6 +/- 3 and 0.5 +/- 0.3 min for the epidural and im groups, respectively), although this difference was not statistically significant. Severe desaturation episodes, defined as SpO2 less than or equal to 85% for more than 30 s, occurred in 71% of patients in the epidural group, 30% in the PCA group, and 63% in the im group (P less than 0.05 PCA vs. epidural and im).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Oxyhemoglobin saturation following cesarean section in patients receiving epidural morphine, PCA, or im meperidine analgesia. 272 36

Epidurally administered clonidine has been reported to produce postoperative analgesia. To assess the efficacy, safety, and appropriate dose of epidural clonidine for postoperative analgesia, clonidine (range, 100-900 micrograms in 100-micrograms increments) was injected in 22 patients following abdominal surgery or total knee arthroplasty (TKA). Clonidine produced analgesia, as measured by change in verbal pain scores and supplemental iv morphine usage. The largest doses examined (700-900 micrograms) produced complete pain relief for 5.0 +/- 0.8 h (mean +/- SEM; range 2-11 h), without other sensory or motor blockade. Clonidine also produced dose dependent decreases in blood pressure, being less following small (100-300 micrograms) and large (700-900 micrograms) doses than following intermediate (400-600 micrograms) doses. Six patients required iv ephedrine for treatment of blood pressure decrease of greater than 30%. Clonidine decreased heart rate 10-30% and produced transient sedation. Oxyhemoglobin saturation, serum glucose, and arterial blood gas tensions were not altered by clonidine, whereas there was a small (28%) dose-independent decrease in serum cortisol following clonidine injection. Clonidine was absorbed in a dose-dependent manner into the systemic circulation, with plasma concentrations 0.1-3.3 ng/ml 1 h following injection. These results suggest that hemodynamic depression and short-lasting analgesia may limit the usefulness of bolus epidural clonidine analgesia in the postoperative setting.
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PMID:Epidural clonidine analgesia following surgery: phase I. 281 56

We have studied combinations of alfentanil and propofol for total i.v. anaesthesia in 24 severely burned patients. No inhalation agents were used. After a loading dose of alfentanil 100 micrograms kg-1, the intraoperative requirement was 1.24 (SEM 0.7) micrograms kg-1 min-1, and after a propofol induction dose of 2 mg kg-1 the maintenance rate was 100 micrograms kg-1 min-1. Initial hypotension occurred after induction of anaesthesia, but during the operation, cardiovascular variables were stable. After adequate antagonism of neuromuscular block, respiratory depression persisted in three patients when the two agents were discontinued simultaneously; this was not seen when alfentanil was discontinued 15 min before propofol. Quality of recovery was good, and satisfactory postoperative analgesia was present in the majority of patients 2 h after operation. This study indicates that total i.v. anaesthesia with a combination of alfentanil and propofol appears to be satisfactory in burned patients.
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PMID:Alfentanil and propofol infusions for surgery in the burned patient. 281 18

To test the hypothesis that segmental thoracic extradural block causes sympathetic denervation caudally beyond dermatomes rendered analgesic, we have measured regional skin temperatures in six conscious dogs after upper thoracic, mid thoracic, and lumbar extradural injection of 0.5% bupivacaine 0.5, 1 and 2 ml cumulatively (total dose: 3.5 ml) given at 45-min intervals. Dogs were studied at constant ambient and rectal temperatures. Upper thoracic extradural injections resulted in a significant increase in skin temperatures on both the front (+1.4 (SEM 0.2) degrees C) and hind paw (+1.4 (0.3) degrees C), while the area of analgesia was confined to the upper trunk. With lumbar extradural injection, skin temperatures increased significantly (+2.0 (0.5) degrees C) on the lower extremities only. Mid thoracic injection significantly increased both front (+2.4 (0.9) degrees C) and hind paw (+2.2 (0.6) degrees C) skin temperatures, but decreased temperatures on the thorax (-0.9 (0.2) degrees C) and abdomen (-1.0 (0.2) degrees C), reversing the normal temperature gradient along the body axis. Irrespective of the injection site, skin temperatures on the trunk failed to increase or even decreased significantly. These data suggest that small doses of local anaesthetics applied to the extradural space of conscious dogs cause increased lower extremity skin temperatures caudal to areas unresponsive to pinprick stimulation when injected at a high thoracic level, and decreased trunk skin temperature even in analgesic areas, so that skin temperature measurements are unlikely to reflect purely sympathetic efferent activity on the trunk. Upper thoracic segmental extradural analgesia induced a decrease in sympathetic tone distal to the area of analgesia.
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PMID:Effects of segmental thoracic extradural analgesia on sympathetic block in conscious dogs. 281 26


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