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)

1. Single doses (500 and 1000 mg) of both buffered aspirin and aspirin tablets were compared with placebo in a randomised double-blind trial of parallel design in patients with postoperative pain after third molar surgery. 2. Only buffered aspirin 500 mg provided significant pain relief (P = 0.016) during the 5 h investigation period. 3. A significant correlation (P = 0.004) was observed between overall pain scores after the various aspirin treatments and aspirin esterase activity. 4. Buffered aspirin preparations afforded a slight advantage over aspirin tablets in the control of postoperative pain after third molar surgery. However, the duration of analgesia was short (approximately 2 h). 5. Aspirin esterase activity appears to be an important determinant of the drug's efficacy in postoperative dental pain.
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PMID:An evaluation of buffered aspirin and aspirin tablets in postoperative pain after third molar surgery. 157 68

Blood coagulation and fibrinolysis were studied in 20 premenopausal women undergoing abdominal hysterectomy under general anaesthesia (GA) or high epidural analgesia (EDA). As expected, the adrenocortical stress response was suppressed in the EDA group. The Factor VIII complex (F VIII:C, F VIII R:Ag = von Willebrand factor), known to be related to adrenocortical activity and/or vessel wall reactivity, was found to increase less in the EDA group. With regard to all the other variables analysed there were no significant differences between the groups. With both anaesthetic procedures activation of coagulation could be demonstrated by a decrease in prekallikrein, F X and antithrombin as well as by an increase in fibrinopeptide A levels. A decrease in plasminogen and alpha 2-antiplasmin suggested activation of the fibrinolytic system and a decrease in prekallikrein and kallikrein inhibition activity (C-1-esterase inhibitor) an activation of the kallikrein system. In this study only the differences in F VIII complex could explain the previously reported higher thromboembolic frequency after GA as compared to EDA.
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PMID:Per- and postoperative changes in coagulation and fibrinolytic variables during abdominal hysterectomy under epidural or general anaesthesia. 373 76

Changes in the peripheral blood leucocyte count, lymphocyte subpopulations, and in 'in vitro' responses of lymphocytes to phytohaemagglutinin and tuberculin after induced labour were investigated in 10 normal parturients and their newborns. Every other parturient was given segmental epidural analgesia at level T 10-12 for pain relief during the first stage of labour. The remaining mothers served as controls. The results of blood samples taken from the mothers before induction of labour and from the newborns immediately after delivery served as basal values against which the results of samples drawn on the 1st and on the 5th day following delivery were compared. A significant (p less than 0.05) increase from the basal values in the total leucocyte count after delivery was found only in those mothers not given epidural analgesia and in their newborns. Similarly, a significant (p less than 0.01) decrease in the T cell count characterized by both E rosette formation and acid alpha-naphthyl acetate esterase staining was found in the peripheral blood only in the mothers (but not the newborns) without epidural analgesia. The differences between the research groups were not, however, significant. The lymphocyte response to phytohaemagglutinin on the 1st and on the 5th day after delivery was also significantly (p less than 0.05) lower in the newborns of the mothers not given epidural analgesia than in those of the mothers given it. The present results show that the depression induced by the stress of parturition in some parameters of cell-mediated immunity of mothers and newborns can be at least partly prevented by using segmental epidural analgesia.
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PMID:Effect of segmental epidural analgesia on changes in peripheral blood leucocyte counts, lymphocyte subpopulations, and in vitro transformation in healthy parturients and their newborns. 660 64

Remifentanil is a newly synthesized 4-anilido-piperidine with an ester side chain susceptible to esterase metabolism. We evaluated the safety, analgesic efficacy, and pharmacokinetics of remifentanil in 48 male volunteers. Volunteers were randomized to receive increasing doses of remifentanil, alfentanil, or placebo. Analgesic efficacy was evaluated by increasing tolerance to a spring-loaded rod measured at the tibia and sternum at multiple time points. Respiratory depression was measured by changes in arterial blood gas tensions and peripheral hemoglobin oxygen saturation. Hemodynamics were continuously monitored by means of an intra-arterial catheter. Both remifentanil and alfentanil produced a dose-dependent increase in analgesia and respiratory depression. Remifentanil was 20 to 30 times more potent (milligram to milligram) than alfentanil when assessed by either analgesic efficacy or respiratory measures. The pharmacokinetics of remifentanil were best described by a biexponential decay curve. Remifentanil had a small volume of distribution of 0.39 (SD, +/- 0.25) L/kg (alfentanil, 0.52 +/- 2 L/kg), with a rapid distribution phase of 0.94 (SD, +/- 0.57) min and an extremely short elimination half-life of 9.5 (SD, +/- 4) min compared with an elimination half-life of alfentanil of 58 (SD, +/- 7.6) min. The t1/2 ke0 (half-time for equilibration between plasma and the effect compartment) of remifentanil for analgesia was calculated as 1.3 min. Thus, remifentanil appears to have a pharmacologic profile similar to other potent mu agonists, but with exceptionally short-lasting pharmacokinetics, which is likely to make it a very useful opioid for clinical practice.
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PMID:Preliminary pharmacokinetics and pharmacodynamics of an ultra-short-acting opioid: remifentanil (GI87084B). 1203 62

Current trends toward outpatient surgery and closed loop computer controlled drug administration have created a demand for short acting anaesthetic agents. Such agents not only provide the anaesthetist with rapid patient recovery after completion of the procedure, but also with almost immediate intra-operative control over the anaesthetic state of the patient. Shorter acting anaesthetic agents are being developed in several therapeutic areas including volatile anaesthetics, neuromuscular blockers as well as injectable anaesthetics. In the injectable anaesthetic area, propofol has been introduced and offers some significant advantages over the previously existing induction agents. Remifentanil is a novel member in the family of the 4-anilidopiperidine opioid analgesics which also include the traditional agents fentanyl, alfentanil, and sufentanil. Remifentanil undergoes widespread extrahepatic metabolism by blood and tissue nonspecific esterases, resulting in an extremely rapid clearance. Because of its unique metabolic pathway among this group of drugs, remifentanil represents a new pharmacokinetic class of opioids which is named esterase metabolised opioid (EMO). Rapid biotransformation to minimally active metabolites results in short and predictable duration of action with no accumulation of effect on repeated dosing or with continuous infusion. Clinical experiences presented so far indicate that remifentanil can be safely administered in different anaesthetic regimens as well as in the great variety of patients including children and patients with renal, hepatic or cardiovascular diseases. However, its use also presents the anaesthetist with a significant challenge. If remifentanil is the only opioid analgesic administered during anaesthesia, it must be remembered that shortly after the end of the surgical procedure, the patient will not benefit from opioid-based analgesia. This problem must be addressed if remifentanil is to be used for procedures associated with significant postoperative pain. Reducing the infusion rate of remifentanil to analgesic doses suitable for the postoperative pain management or immediate administration of longer acting opioids at the end of anaesthesia might solve this problem. At present it is difficult to predict precisely the future ranking of remifentanil. However, the unique pharmacokinetic profile of remifentanil should make it useful in the various surgical settings and in all circumstances where precise control over the analgesic state are desirable.
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PMID:[Is remifentanil an ideal opioid for anesthesiologic management in the 21st century?]. 908 16

Patient-controlled intravenous remifentanil was used to provide analgesia in labour for three thrombocytopaenic women. The most successful regimen comprised a patient-demand bolus of 0.5 microg x kg(-1) with a lockout period of 2-3 min, allowing for a successful demand with each contraction. There was an initial period during which the patient learned to anticipate the next contraction and to deliver a bolus about 30 s beforehand; subsequently the remifentanil provided excellent analgesia, with a range of consumption of 426-1050 microg x h(-1). Apart from one episode of maternal sedation and fetal heart rate decelerations resulting from an excessive demand bolus, mothers and neonates tolerated the remifentanil without sequelae. Owing to rapid metabolism by tissue esterase, the use of remifentanil allows adequate doses of opioid to be administered to the mother to achieve good analgesia, without its accumulation in the fetus.
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PMID:Patient-controlled analgesia using remifentanil in the parturient with thrombocytopaenia. 1099 44

In a prospective study, from September 2000 to September 2001, all ureteroscopies ( n=140) were performed under local and intravenous patient controlled analgesia using continuous infusion of remifentanil (Ultiva). The dosage of 0.15 micro g/kg/min was adapted to changing intraoperative pain (range 0.08-0.30 micro g/kg/min). Preoperative sedation with midazolam 2 mg was given 5 min prior to ureteroscopy. The efficacy of monitored anesthesia care ("Big MAC") was quantified by the patient using a visual analogue pain scale. A total of 97.1% (136/140) of the procedures were performed and finished under remifentanil. Only four male patients underwent conversion to general anesthesia due to insufficient analgesia. All but one patient would choose remifentanil again for first line anesthesia. Significant differences in pain scale values were noticed for male/female patients and ureteroscopies above/below the iliac vessel crossing. Side effects were rare being mainly hypoxic events (pO(2)<90% in 5.1%). Indication, intraoperative procedure, average surgery time (24 min), complications and primary success rate (96.6/90/63.3% stone free for distal/mid/proximal ureter, respectively) did not differ from the control group under general anesthesia. Ureteroscopies with remifentanil are safe, universally applicable because of refifentanil's organ independent esterase metabolism and as effective as general anesthesia. There is no need for PACU stay for patients due to the ultra-short drug half-life, and therefore remifentanil is cost effective and perfect in an outpatient setting.
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PMID:[Ureteroscopy under intravenous analgesia with remifentanil]. 1510 11

Remifentanil is an esterase-metabolized ultra-short acting mu-agonist opioid with a rapid clearance. The aim of this study was to determine the efficacy of remifentanil infusion for the short-lasting, but painful, transvaginal puncture for oocyte retrieval. Eighty consenting adult women (ASA I and II) aged 30.5 +/- 5 years and with a body weight of 69.1 +/- 9.1 kg were enrolled in this prospective study. After an oral premedication with 7.5 mg midazolam, all patients received 3 l/min oxygen. Subsequently, the remifentanil infusion was started with a rate of 0.3 microg/kg/min. Remifenanil doses were adjusted as needed for painless puncture and sufficient oxygen saturation in steps of 0.05 microg/kg/min. Dosage requirements, blood pressure, heart rate, oxygen saturation (pulse oxymetry, SaO2) and the level of analgesia were recorded every 3 minutes. Follicular aspiration lasted 11.8 +/- 4.1 min and the time of remifentanil infusion was 18.7 +/- 4.6 min. Dosage requirements of remifentanil were 0.3 microg/kg/min in 48.7% of all patients, but 27.8% needed only 0.25 microg/kg/min and 16.6% needed only 0.2 microg/kg/min. However, 4.2% of patients needed 0.35 microg/kg/min and 2.7% of all cases needed 0.4 microg/kg/min. Vital parameters remained nearly unchanged. Oxygen saturation decreased significantly from 99.2 +/- 0.7% to 98.2 +/- 2.4% after 3 min and to 94.9 +/- 7.2% after 10 min. Nine women showed motoric reactions to puncture. In many cases, the infusion of remifentanil after premedication with midazolam provided a suitable and satisfying anaesthesia for oocyte retrieval. Some patients, however, showed motoric reactions to vaginal puncture, while in other cases significant and clinical relevant decreases in Hb-oxygen saturation occurred. Therefore, we no longer carry out remifentanil infusion for transvaginal oocyte retrieval. We now prefer a remifentanil infusion of 0.2 microg/kg/min and propofol (1 mg/kg initially with intermittent doses of 0.5 mg/kg) combined with assisted ventilation by mask.
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PMID:[Remifentanil analgesia for aspiration of follicles for oocyte retrieval]. 1531 58

Angioneurotic oedema is a rare disease caused by Cl esterase inhibitor deficiency. Hereditary angioneurotic oedema includes type I (quantitative and functional) deficiency and type 11 (functional) deficiency. Its prophylactic treatment during pregnancy, based on danazol therapy if the fetus is male, may avoid acute attacks of generalized or laryngeal oedema. It must be instituted before delivery and carried into the postpartum period. If the fetus is female, epsilon aminocaproic acid may be used. The acquired form of angioneurotic oedema can be due to antibodies to C1 esterase inhibitor. A prophylactic therapy is not well established, but high doses of corticosteroids are recommended. Operative delivery is best avoided when possible. Regional analgesia is indicated for labour or caesarean section to prevent pain and stress and to avoid the difficulties associated with laryngeal oedema and tracheal intubation. In the treatment of an acute attack, Cl esterase inhibitor concentrates (1500 units) may be given i.v. We present two cases, one of hereditary and one of acquired angioneurotic oedema, both presenting during pregnancy and both delivered vaginally under epidural analgesia with successful outcome.
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PMID:Parturition and angioneurotic oedema. 1532 Nov 58

Remifentanil (Ultiva), a fentanyl derivative, is an ultra-short acting, nonspecific esterase-metabolised, selective mu-opioid receptor agonist, with a pharmacodynamic profile typical of opioid analgesic agents. Notably, the esterase linkage in remifentanil results in a unique and favourable pharmacokinetic profile for this class of agent. Adjunctive intravenous remifentanil during general anaesthesia is an effective and generally well tolerated opioid analgesic in a broad spectrum of patients, including adults and paediatric patients, undergoing several types of surgical procedures in both the inpatient and outpatient setting. Remifentanil is efficacious in combination with intravenous or volatile hypnotic agents, with these regimens generally being at least as effective as fentanyl- or alfentanil-containing regimens in terms of attenuation of haemodynamic, autonomic and somatic intraoperative responses, and postoperative recovery parameters. The rapid offset of action and short context-sensitive half-time of remifentanil, irrespective of the duration of the infusion, makes the drug a valuable opioid analgesic option for use during balanced general inhalational or total intravenous anaesthesia (TIVA) where rapid, titratable, intense analgesia of variable duration, and a fast and predictable recovery are required.
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PMID:Remifentanil: a review of its use during the induction and maintenance of general anaesthesia. 1611 80


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