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)

Fifty-four ASA I and II children 1 to 10 yr of age undergoing strabismus surgery were randomized to receive in a double-blind fashion intravenous ketorolac (0.9 mg/kg), fentanyl (1 microgram/kg), or saline placebo (2 mL) during a standardized general anesthetic. Patients received no analgesic or antiemetics intraoperatively except for the study drug. Patients receiving ketorolac or placebo compared to fentanyl had a significantly lower incidence of postoperative vomiting in the day surgery unit (DSU) (P = 0.03) and overall (DSU plus home) (P = 0.005). The severity (number of episodes) of post-operative vomiting was significantly lower in the DSU, at home (first 24 h after hospital discharge), and overall for patients receiving ketorolac or placebo compared to fentanyl (P < 0.01). Postoperative pain scores and frequency of acetaminophen administration did not differ among the study groups, suggesting that the intraoperative use of ketorolac or fentanyl during pediatric strabismus surgery is unnecessary. No patients required fentanyl postoperatively, indicating that rectal acetaminophen administered in the postanesthesia recovery room provides sufficient analgesia for pediatric strabismus surgery. In conclusion, neither ketorolac nor fentanyl was associated with less postoperative vomiting or analgesic requirements compared to saline placebo administered during pediatric strabismus surgery. Fentanyl should be avoided, as it was associated with a significantly greater incidence of postoperative vomiting compared to ketorolac or placebo.
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PMID:The effects of ketorolac and fentanyl on postoperative vomiting and analgesic requirements in children undergoing strabismus surgery. 861 27

Opioid receptors have been demonstrated on sensory nerves in both inflamed and normal subcutaneous tissue but locally applied opioid agonists produce analgesia in inflamed tissue only. Inflammation confers a disruption of the perineurial barrier that can also be induced deliberately by hyperosmolar solutions. The present study examines at which stage of Freund's adjuvant-induced inflammation peripheral opioid analgesic effects become manifest and whether a perineurial defect contributes to the appearance of such effects. To this end we have monitored the temporal evolution of inflammatory signs (swelling, temperature, hyperalgesia) and of peripheral antinociceptive effects (by the paw pressure test) of mu-, delta-, and kappa-selective opioids. Using horseradish peroxidase histochemistry, the perineurial barrier was assessed in normal and inflamed tissue and following its artificial disruption by hyperosmolar saline and mannitol in vivo. Finally, we sought to elicit analgesia in normal tissue by the concomitant application of mannitol and receptor-selective opioids or by an extremely lipophilic opioid agonist (fentanyl). We found that peripheral opioid antinociception and perineurial leakage occur simultaneously at a very early stage (within 12 hr) of the inflammatory reaction and that both can be mimicked by the administration of hyperosmolar solutions in normal tissue. Fentanyl produced peripheral antinociception in noninflamed tissue that was potentiated by mannitol or inflammation. Our findings demonstrate that the perineurium is a crucial determinant for peripheral opioid analgesia and that the efficacy of locally applied hydrophilic or lipophilic neuromodulatory compounds can be improved dramatically by the concomitant modulation of perineurial permeability.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Perineurial defect and peripheral opioid analgesia in inflammation. 782 27

We have recently reported that, in SH-SY5Y cells, mu-opioid receptor occupancy activates phospholipase C via a pertussis toxin-sensitive G-protein. In the present study we have further characterized the mechanisms involved in this process. Fentanyl (0.1 microM) caused a monophasic increase in inositol 1,4,5-trisphosphate mass formation, with a peak (20.5 +/- 3.6 pmol/mg of protein) at 15 s. Incubation in Ca(2+)-free buffer abolished this response, while Ca2+ replacement 1 min later restored the stimulation of inositol 1,4,5-trisphosphate formation (20.1 +/- 0.6 pmol/mg of protein). In addition, nifedipine (1 nM-0.1 mM), an L-type Ca(2+)-channel antagonist, caused a dose-dependent inhibition of inositol 1,4,5-trisphosphate formation, with an IC50 of 60.3 +/- 1.1 nM. Elevation of endogenous beta/gamma subunits by selective activation of delta-opioid and alpha 2 adrenoceptors failed to stimulate phospholipase C. Fentanyl also caused a dose-dependent (EC50 of 16.2 +/- 1.0 nM), additive enhancement of carbachol-induced inositol 1,4,5-trisphosphate formation. In summary, we have demonstrated that in SH-SY5Y cells activation of the mu-opioid receptor allows Ca2+ influx to activate phospholipase C. However, the possible role of this mechanism in the process of analgesia remains to be elucidated.
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PMID:Mu-opioids activate phospholipase C in SH-SY5Y human neuroblastoma cells via calcium-channel opening. 783 76

The immunoregulatory effects of fentanyl and a fentanyl-related compound, OHM3295, were studied in mice. Male CD1 mice treated with a range of fentanyl doses (0.1-1.0 mg/kg, subcutaneously) showed suppression of splenic natural killer (NK) activity following 0.25-0.50 mg/kg fentanyl dose but not higher (0.75-1.0 mg/kg) or lower (0.1 mg/kg) doses. Fentanyl (0.01-32.0 mg/kg) also induced dose-related analgesia as measured by an increase in tail flick latency; these analgesic effects were antagonized by naltrexone (1.0-10.0 mg/kg). Pretreatment with naltrexone (1.0-3.2 mg/kg) resulted in significant suppression of splenic NK activity following fentanyl (10.0-32.0 mg/kg) administration. In comparison to fentanyl, OHM3295 (3.2-25.0 mg/kg) augmented splenic NK activity in a naltrexone-reversible manner. Similar to fentanyl, OHM3295 (1.0-32.0 mg/kg) also induced a naltrexone-sensitive, dose-related analgesia as measured by an increase in tail flick latency. These results with OHM3295 demonstrate a novel profile of effects which includes naltrexone-sensitive analgesic effects in the absence of immunosuppressive effects. In addition, this is the first reported case in which a compound with opioid analgesic effects has been shown to potentiate natural killer cytolytic activity following in vivo administration.
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PMID:OHM3295: a fentanyl-related 4-heteroanilido piperidine with analgesic effects but not suppressive effects on splenic NK activity in mice. 784 55

1. Vomiting and restlessness following ENT and eye surgery are undesirable, and may be related to the emetic and analgesic effects of any analgesic given to augment anaesthesia during surgery. 2. To rationalise the choice of analgesic for routine ENT surgery we examined the intraoperative, recovery and postoperative effects following the administration of either buprenorphine (3.0 to 4.5 micrograms kg-1), diclofenac (1 mg kg-1), fentanyl (1.5 to 2.0 micrograms kg-1), morphine (0.1 to 0.15 mg kg-1), nalbuphine (0.1 to 0.15 mg kg-1), pethidine (1.0 to 1.5 mg kg-1) or saline (as control) given with the induction of anaesthesia in 374 patients. A standardised anaesthetic technique with controlled ventilation using 0.6-0.8% isoflurane in nitrous oxide and oxygen was employed. The study population constituted 7 similar groups of patients. 3. Intraoperatively, their effects on heart rate and blood pressure, airway pressure and intraocular pressure, were similar. This implies, most surprisingly, that neither their analgesic nor their histamine releasing effects were clinically evident during surgery. By prolonging the time to extubation at the end of anaesthesia, only buprenorphine, fentanyl, morphine and pethidine provided evidence of intraoperative respiratory depression. 4. Postoperatively, buprenorphine was associated with severe respiratory depression, prolonged somnolence, profound analgesia and the highest emesis rate. Diclofenac exhibited no sedative, analgesic, analgesic sparing, emetic or antipyretic effects. Fentanyl provided no sedative or analgesic effects, but was mildly emetic. Morphine provided poor sedation and analgesia, delayed the requirement for re-medication and was highly emetic. Nalbuphine and pethidine produced sedation with analgesia during recovery, a prolonged time to re-medication and a mild emetic effect. None provided evidence, from analysis of postoperative re-medication times and analgesic consumption, of any pre-emptive analgesic effect. 5. We conclude that nalbuphine (mean dose 0.13 mg kg-1) and pethidine (mean dose 1.35 mg kg-1), given individually as a single i.v. bolus during induction of anaesthesia, are the most efficacious analgesics for routine in-patient ENT surgery.
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PMID:Analgesics and ENT surgery. A clinical comparison of the intraoperative, recovery and postoperative effects of buprenorphine, diclofenac, fentanyl, morphine, nalbuphine, pethidine and placebo given intravenously with induction of anaesthesia. 788 92

A questionnaire was sent to the pharmacies of 88 Finish hospitals with surgical departments to inquire about the consumption of opioids during 1990. Another questionnaire was sent to 480 members of the Finnish Society of Anaesthesiologists to ask how they administer opioids to adult patients. Answers were received from 95% of hospitals and 67% of anaesthetists. Dextropropoxyphene was the most common oral opioid and oxycodone was the most common parenteral opioid used in Finland. Parenteral opioids were consumed almost totally in the hospitals. The anaesthetists reported oxycodone to be the opioid of choice for premedication, postoperative pain and sedation of critically ill patients. Fentanyl was the opioid most commonly used intravenously during balanced anaesthesia and in epidural administration. Epidural opioids were administered by 77% of anaesthetists and patient-controlled analgesia (PCA) technique mostly for intravenous administration by 19%. Only 10% of Finnish anaesthetists were actively involved in the management of chronic pain; the methods they use are discussed. The majority of anaesthetists were satisfied with the currently available opioids.
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PMID:Opioids in anaesthesia: a questionnaire survey in Finland. 791 67

Pulsed dye laser is a new treatment for port-wine stains, congenital lesions in the cutaneous vascular plexus. We report our anesthetic experience with paediatric outpatients treated in the dermatology clinic. From April to November 1993, 48 ASA 1 children were anaesthetised for a total of 105 consecutive laser treatments. The youngest was eight months old, the oldest was 12 yrs old and most of the sessions (43%) were done for children aged from two to four years. Each received acetaminophen (10 mg.kg-1 p.o.) before treatment. A propofol infusion was chosen for anaesthesia to achieve early discharge and to reduce the incidence of postoperative emesis. The infusion was adjusted to maintain blood pressure within 20% of baseline and to keep the child immobile. The dose was progressively reduced during the procedure from 400 micrograms.kg-1.min-1 to 100 micrograms.kg-1.min-1. Fentanyl (2 micrograms.kg-1 i.v.) was added for analgesia. Respiration was spontaneous through a nasopharyngeal airway (air in oxygen 40%). Anaesthesia proceeded uneventfully in all cases and lasted for 15-30 min (63% of treatments), 30-45 min (28%) or 45-60 min (9%) according to the size of the lesion. The mean stay in the recovery room was 25.1 min and none of the patients experienced emesis. Our experience shows that general anaesthesia with propofol supplemented with fentanyl offers a rapid onset and awakening, a painless treatment and an immobile child. It is a safe solution to alleviate pain from repeated painful procedures even in small children under two years of age.
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PMID:Propofol for pulsed dye laser treatments in paediatric outpatients. 792 22

This study was done to compare the hemodynamics, serum catecholamine levels and postoperative analgesia in total intravenous anesthesia with inhalation anesthesia. Thirteen patients for elective upper abdominal surgery, aged from 40 to 75 years, were studied. In the total intravenous anesthesia group (TIVA group, 7 patients), anesthesia was induced with 0.3 mg.kg-1 midazolam and maintained with 0.68 mg.kg-1.hr-1 midazolam for 15 minutes followed by 0.125 mg.kg-1.hr-1. Fentanyl was also administered as necessary. In the inhalation anesthesia group (inhalation group, 6 patients), anesthesia was induced with 5 mg.kg-1 thiamylal and maintained with 0.5-2.0% enflurane and 66% nitrous oxide in oxygen. In the TIVA group, the blood pressure and heart rate were as stable as those in the inhalation group. The serum concentration of catecholamines in the TIVA group rose significantly 60 minutes after intubation, in particular, the serum epinephrine level was higher than in the inhalation group. The time for extubation, respiratory rate and PaCO2 were not different between the two groups. The postoperative analgesic duration in the TIVA group was significantly longer than that in the inhalation group. The elimination half-life of midazolam was 1.675 +/- 0.281 hours in the TIVA group. In this study, TIVA failed to suppress the elevation of serum catecholamine levels, but it achieved stable hemodynamics during upper abdominal surgery and enough postoperative analgesia without affecting the extubation time, the respiratory conditions and the elimination half-life of midazolam.
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PMID:Total intravenous anesthesia. Midazolam-fentanyl vs enflurane-nitrous oxide. 793 34

Forty-five patients undergoing circumcision were allocated randomly to one of three study groups to compare topical analgesia with dorsal nerve block using the midline or lateral approach. Pain scores, side effects and analgesic requirements were recorded after surgery. Patients who received topical analgesia required significantly more fentanyl and had higher pain scores at the 15-min observation period after operation. Fentanyl requirements and pain scores were similar in patients who received a dorsal nerve block using either the midline or lateral approach. The incidence of side effects after surgery was similar in all three groups.
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PMID:Post-circumcision analgesia: comparison of topical analgesia with dorsal nerve block using the midline and lateral approaches. 777 44

Opioids inhibit the voltage-dependent calcium channel conductance, which is one of the mechanisms of opioid analgesia on the opioid receptor. According to the hypothesis that calcium antagonists can potentiate the analgesic effect of opioids, we designed a study to investigate the effects of KB-2796, a new calcium channel blocker, on the antinociception of fentanyl at the level of the spinal cord in rats. PE-10 catheters were chronically implanted in the lumbar intrathecal space of the rats. Tail-flick test was used to assess the nociceptive sensitivity. Fentanyl (1 microgram) and KB-2796 (50, 150 or 250 micrograms) were tested individually as well as in combination. Dimethyl sulfoxide (10%) was used as a control. All drugs were injected intrathecally. Fentanyl alone produced a significant but short duration (15-30 minutes) of antinociception. KB-2796 by itself did not show any antinociception at any of the doses tested. However, when KB-2796 at the higher doses (150 and 250 micrograms) was administered with fentanyl, the antinociceptive effect was significantly (P < 0.05) enhanced over that of fentanyl alone from 30 to 180 minutes after the injection. In conclusion, our results suggest that KB-2796 potentiates the analgesic effect of fentanyl at the spinal level. These data also support our hypothesis that calcium channel blockers may involve in the antinociception of opioids.
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PMID:Enhancement of antinociceptive effect of fentanyl by KB-2796 at spinal level. 803 73


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