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Bioorganic & Medicinal Chemistry Letters Nov 2015A series of pethidine analogs were synthesized and their affinities for the [(3)H]N-methyl-scopolamine (NMS) binding site on muscarinic acetylcholine receptors (mAChRs)...
A series of pethidine analogs were synthesized and their affinities for the [(3)H]N-methyl-scopolamine (NMS) binding site on muscarinic acetylcholine receptors (mAChRs) were determined using M1, M3 or M5 human mAChRs expressed by Chinese hamster ovary (CHO) cell membranes. Compound 6b showed the highest binding affinities at M1, M3 and M5 mAChRs (Ki=0.67, 0.37, and 0.38 μM, respectively).
Topics: Animals; CHO Cells; Cricetulus; Female; Humans; Ligands; Meperidine; Receptor, Muscarinic M1; Receptor, Muscarinic M3; Receptor, Muscarinic M5; Structure-Activity Relationship
PubMed: 26494260
DOI: 10.1016/j.bmcl.2015.10.029 -
British Journal of Anaesthesia Sep 1990We have examined the extraction ratios, net fluxes and clearances of pethidine by the liver, kidneys and hindquarters in sheep before, during and after continuous... (Comparative Study)
Comparative Study
We have examined the extraction ratios, net fluxes and clearances of pethidine by the liver, kidneys and hindquarters in sheep before, during and after continuous anaesthesia (70 min) with propofol or thiopentone. Before anaesthesia, the overall mean respective regional pethidine extraction ratios were 0.98 (SD 0.01), 0.20 (0.06) and 0.44 (0.13), the corresponding net fluxes were 47 (7), 5 (2) and 20 (10)% dose min-1 and the clearances 1.44 (0.22), 0.17 (0.07) and 0.80 (0.39) litre min-1. During propofol anaesthesia, arterial blood concentrations of pethidine approximately doubled (P less than 0.05), mean pethidine hepatic extraction ratio was unchanged, flux was increased to 145 (20)% and clearance decreased to 79 (10)% (P less than 0.05) of baseline values; mean pethidine renal extraction ratio, flux and clearance were 73 (34), 112 (43) and 69 (31)% of baseline values; mean hindquarter pethidine extraction ratio decreased to 65 (25)% (P less than 0.05) of baseline values. During thiopentone anaesthesia, arterial blood concentrations of pethidine approximately doubled (P less than 0.01), mean pethidine hepatic extraction ratio was 97 (2)% of baseline values and flux and clearance were unchanged, mean pethidine renal extraction ratios, flux and clearance decreased to 37 (21), 54 (18) and 27 (19)% (all P less than 0.05) of baseline values and mean pethidine hindquarter extraction ratio was 81 (20)% of baseline values. In spite of only modest changes in hepatic and renal blood flow during anaesthesia, blood concentrations of pethidine doubled and pethidine kinetics were disturbed for several hours after anaesthesia. Overall, however, the changes were of smaller magnitude and shorter duration than those that have been described for anaesthesia with the volatile anaesthetic agents.
Topics: Anesthesia, Intravenous; Animals; Blood Flow Velocity; Cardiac Output; Female; Kidney; Liver; Longitudinal Studies; Meperidine; Propofol; Sheep; Thiopental; Time Factors
PubMed: 2223366
DOI: 10.1093/bja/65.3.365 -
Agri : Agri (Algoloji) Dernegi'nin... Jul 2022Patients suffer notable levels of pain after lumbar spine surgery. The primary objective of this randomized clinical trial is to investigate the efficacy of erector... (Randomized Controlled Trial)
Randomized Controlled Trial
OBJECTIVES
Patients suffer notable levels of pain after lumbar spine surgery. The primary objective of this randomized clinical trial is to investigate the efficacy of erector spinae plane block (ESPB) on 24-h post-operative pain score of patients undergoing lumbar spine surgery. Cumulative opioid consumption and intraoperative bleeding were assessed as well.
METHODS
Adult patient candidates for elective lumbar spine surgery were randomly assigned to case (ESPB) and control (no ESPB) groups. The block was performed under ultrasound guidance in prone position after induction of general anesthesia. Both groups received the same anesthesia medication and technique. Post-operative pain score, number of patients requiring rescue analgesia (meperidine), total amount of post-operative rescue analgesic demand in the first 24 h, and intraoperative bleeding were recorded. To compare pain score variable in time span, the ANOVA repeated measure test was used. All the statistical tests were two tailed and p<0.05 considered as statistically significant.
RESULTS
In all time intervals, pain score in case group was significantly lower than control group. In case group, eight patients demanded rescue analgesic (40%) which was significantly lower than that in control group (15 patients [75%]) (p=0.025). Total amount of meperidine consumption was 57.50±45.95 in control group and 22.50±32.34 in case group (p=0.01) which was higher in control group and statistically significant.
CONCLUSION
ESPB reduces post-operative pain score and opioid consumption, while it does not affect intraoperative bleeding in lumbar spine surgery.
Topics: Adult; Analgesics, Opioid; Humans; Meperidine; Nerve Block; Pain, Postoperative; Ultrasonography, Interventional
PubMed: 35792689
DOI: 10.14744/agri.2021.04864 -
Cirugia Y Cirujanos 2024The aim of this study is to evaluate the effect of erector spinae plane block (ESPB) as a rescue therapy in the recovery room.
OBJECTIVE
The aim of this study is to evaluate the effect of erector spinae plane block (ESPB) as a rescue therapy in the recovery room.
MATERIALS AND METHODS
This single-center historical cohort study included patients who received either ESPB or intravenous meperidine for pain management in the recovery room. Patients' numeric rating scale (NRS) scores and opoid consumptions were evaluated.
RESULTS
One hundred and eight patients were included in the statistical analysis. Sixty-two (57%) patients received ESPB postoperatively (pESPB) and 46 (43%) patients were managed with IV meperidine boluses only (IV). The cumulative meperidine doses administered were 0 (0-40) and 30 (10-80) mg for the pESPB and IV groups, respectively (p < 0.001). NRS scores of group pESPB were significantly lower than those of Group IV on T30 and T60.
CONCLUSION
ESPB reduces the frequency of opioid administration and the amount of opioids administered in the early post-operative period. When post-operative rescue therapy is required, it should be considered before opioids.
Topics: Humans; Male; Female; Middle Aged; Pain, Postoperative; Nerve Block; Paraspinal Muscles; Adult; Meperidine; Analgesics, Opioid; Cohort Studies; Pain Measurement; Aged; Cholecystectomy; Anesthetics, Local; Retrospective Studies
PubMed: 38782375
DOI: 10.24875/CIRU.23000062 -
Anesthesia Progress 1988A rabbit tooth pulp antinociceptive model was used to investigate the effect of prior administration of diazepam or muscimol on the potency and duration of fentanyl and...
A rabbit tooth pulp antinociceptive model was used to investigate the effect of prior administration of diazepam or muscimol on the potency and duration of fentanyl and meperidine Potency experiments compared ED(50) values in all-or-none dose-response assays between both muscimol (0.25 mg/kg) and saline, and diazepam (1.5 mg/kg) and propylene glycol vehicle. An all-or-none effect was defined as doubling of voltage threshold to elicit a lick/chew evoked response. Duration experiments compared time (minutes) to 50% maximum possible effect (MPE) of an ED(90) dose of fentanyl (0.04 mg/kg) and to 50% and 20% MPE of an ED(98) dose of meperidine (17 mg/kg) 10 minutes after pretreatment with diazepam (1.5 mg/kg). Prior (10 minutes) injection of diazepam (1.5 mg/kg) increased the ED(50) value for meperidine (3.06 mg/kg) compared with its control (1.48 mg/kg), indicating a decrease in antinociceptive potency. The same dose of diazepam decreased the ED(50) value for fentanyl (1.1 μg/kg) compared with its control (13.1 μg/kg), indicating an increase in antinociceptive potency. Muscimol also had a similar effect on fentanyl (ED(50), 1.8 μg/kg) compared with saline control (ED(50), 13.8 μg/kg). Diazepam, vehicle, and muscimol by themselves had no effect on voltage thresholds to elicit a lick/chew response. Time to 50% MPE for diazepam-fentanyl was 38 minutes vs. 25 minutes for vehicle-fetanyl; time to 20% MPE for diazepam-meperidine was 38 minutes vs. 54 minutes for vehicle-meperidine (maximum percentage of MPE produced by diazepam-meperidine was 40% compared with 100% MPE for vehicle-meperidine). Percentages of MPE for diazepam-meperidine were significantly lower than those for vehicle-meperidine at all time intervals, whereas percentages of MPE for diazepam-fentanyl were significantly greater than those for vehicle-fentanyl over time.
Topics: Animals; Dental Pulp; Diazepam; Drug Therapy, Combination; Female; Fentanyl; Male; Meperidine; Muscimol; Rabbits
PubMed: 3250278
DOI: No ID Found -
Journal of Accident & Emergency Medicine Jul 2000Migraine can be a disabling condition for the sufferer. For the small number of patients who fail home therapy and seek treatment in an emergency department, there are a...
Migraine can be a disabling condition for the sufferer. For the small number of patients who fail home therapy and seek treatment in an emergency department, there are a number of therapeutic options. This paper reviews the evidence regarding the effectiveness and safety of the following therapies: the phenothiazines, lignocaine (lidocaine), ketorolac, the ergot alkaloids, metoclopramide, the "triptans", haloperidol, pethidine and magnesium. Based on available evidence, the most effective agents seem to be prochlorperazine, chlorpromazine and sumatriptan, each of which have achieved greater then 70% efficacy in a number of studies.
Topics: Analgesics, Opioid; Antipsychotic Agents; Emergency Service, Hospital; Emergency Treatment; Haloperidol; Humans; Meperidine; Migraine Disorders; Phenothiazines
PubMed: 10921808
DOI: 10.1136/emj.17.4.241 -
BMC Pregnancy and Childbirth Jul 2011Intramuscular pethidine is routinely used throughout the UK for labour analgesia. Studies have suggested that pethidine provides little pain relief in labour and has a... (Comparative Study)
Comparative Study Randomized Controlled Trial
BACKGROUND
Intramuscular pethidine is routinely used throughout the UK for labour analgesia. Studies have suggested that pethidine provides little pain relief in labour and has a number of side effects affecting mother and neonate. It can cause nausea, vomiting and dysphoria in mothers and can cause reduced fetal heart rate variability and accelerations. Neonatal effects include respiratory depression and impaired feeding. There are few large studies comparing the relative side effects and efficacy of different opioids in labour. A small trial comparing intramuscular pethidine with diamorphine, showed diamorphine to have some benefits over pethidine when used for labour analgesia but the study did not investigate the adverse effects of either opioid.
METHODS
The Intramuscular Diamorphine versus Intramuscular Pethidine (IDvIP) trial is a randomised double-blind two centre controlled trial comparing intramuscular diamorphine and pethidine regarding their analgesic efficacy in labour and their side effects in mother, fetus and neonate. Information about the trial will be provided to women in the antenatal period or in early labour. Consent and recruitment to the trial will be obtained when the mother requests opioid analgesia. The sample size requirement is 406 women with data on primary outcomes. The maternal primary outcomes are pain relief during the first 3 hours after trial analgesia and specifically pain relief after 60 minutes. The neonatal primary outcomes are need for resuscitation and Apgar Score <7 at 1 minute. The secondary outcomes are an additional measure of pain relief, maternal sedation, nausea and vomiting, maternal oxygen saturation, satisfaction with analgesia, whether method of analgesia would be used again, use of Entonox, umbilical arterial and venous pH, fetal heart rate, meconium staining, time from delivery to first breath, Apgar scores at 5 mins, naloxone requirement, transfer to neonatal intensive care unit, neonatal haemoglobin oxygen saturation at 30, 60, 90, and 120 mins after delivery, and neonatal sedation and feeding behaviour during first 2 hours.
DISCUSSION
If the trial demonstrates that diamorphine provides better analgesia with fewer side effects in mother and neonate this could lead to a change in national practice and result in diamorphine becoming the preferred intramuscular opioid for analgesia in labour.
TRIAL REGISTRATION
ISRCTN14898678Eudra No: 2006-003250-18, REC Reference No: 06/Q1702/95, MHRA Authorisation No: 1443/0001/001-0001, NIHR UKCRN reference 6895, RfPB grant PB-PG-0407-13170_IR5.
Topics: Analgesia, Obstetrical; Analgesics, Opioid; Apgar Score; Cardiotocography; Double-Blind Method; Feeding Behavior; Female; Heroin; Humans; Infant, Newborn; Injections, Intramuscular; Intensive Care, Neonatal; Labor Pain; Meperidine; Nausea; Oxygen; Patient Satisfaction; Pregnancy; Resuscitation; Vomiting
PubMed: 21740578
DOI: 10.1186/1471-2393-11-51 -
Beijing Da Xue Xue Bao. Yi Xue Ban =... Feb 2017To compare the pain control efficiency of continuous adductor canal block (ACB) and femoral nerve block (FNB) in total knee arthroplasty. (Clinical Trial)
Clinical Trial
OBJECTIVE
To compare the pain control efficiency of continuous adductor canal block (ACB) and femoral nerve block (FNB) in total knee arthroplasty.
METHODS
From April to September 2016, patients with severe knee osteoarthritis undergoing primary unilateral total knee arthroplasty (TKA) were prospectively observed, and all the patients were randomized received ultrasound-guided continuous ACB or FNB after surgery. Numeric pain rating scales(NPRS)pain scores in rest and activity 2, 6, 12, 24 and 48 h after surgery were collected, and the preoperative and postoperative quadriceps strength at 24 and 48 h were analyzed. Opioids consumption and anesthesia related adverse effects were also recorded.
RESULTS
In the study, 40 patients were enrolled, with 20 patients in each group, male:female=7:33, the age: (63.8±10.1) years, and the body mass index (BMI): (28.5±3.5) kg/m(2).The general conditions were comparable between the two groups. Though the rest pain 2 h after surgery [ACB=0.0(0,6), FNB=3.0(0,5), P=0.004] and activity pain 12 h post operation [ACB=3.0(3,0), FNB=5.5(0,10), P=0.004] were lower in ACB group compared with FNB group, there was no statistical difference in the other pain checking points between the two groups. The quadriceps strength 24 h and 48 h after surgery were(85.3±27.6) N and (80.0±30.1) N in ACB group, (69.0±29.4) N and (64.4±32.0) N in FNB group, both of them were declined by time. The exact data were higher in ACB group, however, there was no statistical difference between the two group by repeated measurements variance analysis(F=2.703, P=0.108).Four patients in ACB group and five in FNB acquired additional use of dolantin once (100 mg/per time) within 24 h. And among them, three patients acquired once dolantin in ACB, two in FNB, from 24 to 48 h postoperation. There were five patients who suffered nausea postoperation in ACB group, and one who reported xerostomia. Four patients in FNB had nausea with vomiting, and three experienced xerostomia. Deep vein thrombosis appeared in 2 patients in FNB group, but no one in ACB group.
CONCLUSION
Continuous ACB is not superior in pain control after TKA compared with FNB, and the quadriceps strength could be reserved more by this method, which performed early benefits in fast rehabilitation.
Topics: Aged; Analgesics, Opioid; Arthroplasty, Replacement, Knee; Comparative Effectiveness Research; Female; Femoral Nerve; Humans; Male; Meperidine; Middle Aged; Muscle Strength; Nerve Block; Pain Management; Pain, Postoperative; Postoperative Complications; Postoperative Nausea and Vomiting; Quadriceps Muscle; Treatment Outcome; Xerostomia
PubMed: 28203021
DOI: No ID Found -
The Israel Medical Association Journal... Mar 2002Visual interpretation of fetal heart rare monitoring is subject to intra- and inter-observer variability.
BACKGROUND
Visual interpretation of fetal heart rare monitoring is subject to intra- and inter-observer variability.
OBJECTIVE
To examine the effect of intrapartum administration of meperidine and promethazine on fetal heart activity measured objectively by a computerized system.
METHODS
Fourteen healthy women with normal pregnancies at term were studied during the active phase of labor. Fetal heart rate was recorded with the Oxford Sonicaid system 8000. Recordings were performed for 40 minutes prior to and after maternal intravenous administration of meperidine 50 mg with promethazine 25 mg.
RESULTS
The combination of meperidine and promethazine caused a significant decrease in the number of accelerations of 10 beats per minute (9.7 versus 2.6, P = 0.002) and 15 beats per minute (5.2 vs. 1.4, P = 0.003), time spent in episodes of high variation (14.8 vs. 2.0, P = 0.005) and short-term variation (7.8 vs. 5.0, P = 0.003). On the other hand there was an increase in the time spent in episodes of low variation (5.3 vs. 19.7, P = 0.009).
CONCLUSIONS
Maternal administration of meperidine with promethazine has a significant effect on FHR indices during the active phase of normal labor.
Topics: Adjuvants, Anesthesia; Computers; Drug Synergism; Female; Fetal Monitoring; Heart Rate, Fetal; Histamine H1 Antagonists; Humans; Labor, Obstetric; Meperidine; Pregnancy; Promethazine
PubMed: 11908257
DOI: No ID Found -
Medicinski Glasnik : Official... Feb 2021Aim To investigate analgesic effect of three different regimens of combination of analgesics administered to patients undergoing laparoscopic cholecystectomy. Methods... (Randomized Controlled Trial)
Randomized Controlled Trial
Comparison of analgesic efficacy of acetaminophen monotherapy versus acetaminophen combinations with either pethidine or parecoxib in patients undergoing laparoscopic cholecystectomy: a randomized prospective study.
Aim To investigate analgesic effect of three different regimens of combination of analgesics administered to patients undergoing laparoscopic cholecystectomy. Methods Patients undergoing laparoscopic cholecystectomy were randomly allocated to one of three groups on admission, depending of a prescribed post-operative analgesic regimen. Patients allocated to the group A received a combination of intravenous (IV) acetaminophen and intramuscular (IM) pethidine, patients in the group B received a combination of IV acetaminophen and IV parecoxib, and the patients of the group C received IV acetaminophen monotherapy. Analgesic therapy was administered at regular intervals. Pain was evaluated utilizing the numeric rating scale (NRS) at 5 time points: the first assessment was done at 45 minutes, the second, third, fourth and fifth at 2, 6, 12, and 24 hours post-administration, respectively. Postoperative pain intensity was measured by NRS within the groups and between the groups at each time they analysed using one-way repeat measured ANOVA and Post Hoc Test-Bonferroni Correlation. Results A total of 316 patients were enrolled. The analgesic regimens of groups A and B (combination regimens consisting of IV acetaminophen and intramuscular pethidine and IV acetaminophen and IV parecoxib, respectively) were found to be of equivalent efficacy (p=1.000). In contrast, patients in group C (acetaminophen monotherapy) had higher NRS scores, compared to both patients in groups A (p<0.01) and B (p<0.01). Conclusion This study confirms the notion of a significant opioid-sparing effect of parecoxib in postoperative pain management after laparoscopic cholecystectomy.
Topics: Acetaminophen; Analgesics; Cholecystectomy, Laparoscopic; Double-Blind Method; Humans; Isoxazoles; Meperidine; Pain Measurement; Pain, Postoperative; Prospective Studies
PubMed: 33155461
DOI: 10.17392/1245-21