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Clinical Pharmacology and Therapeutics Aug 1981Plasma concentrations and urinary excretion of meperidine and its metabolite normeperidine were determined after intravenous and oral administration to 11 men; five men... (Comparative Study)
Comparative Study
Plasma concentrations and urinary excretion of meperidine and its metabolite normeperidine were determined after intravenous and oral administration to 11 men; five men had hepatic cirrhosis and six were normal. Systemic clearance of meperidine was smaller and bioavailability and half-life greater in the cirrhotic patients than in the normal subjects. Plasma concentrations and 24-hr urinary excretion of normeperidine was lower and persistence of normeperidine in plasma longer in the patients with cirrhosis. The route of administration did not alter the fraction of normeperidine generated from meperidine. The results suggest that in patients requiring repeated meperidine dosage the drug should be taken parenterally rather than orally to allow maximal analgesia and minimal formation of normeperidine. Patients with cirrhosis may be relatively protected from normeperidine toxicity because of impaired formation, but the risk of cumulative toxicity may be greater than in normal subjects because of slower elimination of the metabolite and greater sensitivity to the effects of narcotics on the central nervous system.
Topics: Administration, Oral; Adult; Biotransformation; Dealkylation; Humans; Injections, Intravenous; Kinetics; Liver Cirrhosis, Alcoholic; Male; Meperidine; Middle Aged
PubMed: 7249503
DOI: 10.1038/clpt.1981.146 -
American Journal of Ophthalmology Apr 1962
Topics: Cataract; Cataract Extraction; Humans; Lens, Crystalline; Meperidine; Preoperative Care
PubMed: 13893311
DOI: 10.1016/0002-9394(62)91991-8 -
Obstetrics and Gynecology Mar 1982A study of meperidine metabolism was undertaken in 21 normal parturients at term. Meperidine, 50 mg intravenously, was the sole analgesic agent used during the...
A study of meperidine metabolism was undertaken in 21 normal parturients at term. Meperidine, 50 mg intravenously, was the sole analgesic agent used during the intrapartum period. Maternal and cord blood assessment for meperidine and normeperidine was done by gas chromatography-mass spectrophotometry. Most maternal sera showed a typical meperidine elimination curve. A secondary rise in maternal meperidine 30 to 180 minutes after injection was found in 4 patients. One patient showed a significant alteration in normeperidine appearance. These data add further validity to the hypothesis that the pregnant woman can metabolize meperidine by several pathways.
Topics: Adolescent; Adult; Anesthesia, Intravenous; Anesthesia, Obstetrical; Cholinesterase Inhibitors; Chromatography, Gas; Female; Fetal Blood; Humans; Meperidine; Postpartum Period; Pregnancy; Time Factors
PubMed: 7200592
DOI: No ID Found -
Pharmacology, Biochemistry, and Behavior Jun 1982The effects of meperidine and normeperidine were determined alone and after pretreatment with 10 mg/kg of diazepam on the tail-withdrawal measure of analgesia in rats....
The effects of meperidine and normeperidine were determined alone and after pretreatment with 10 mg/kg of diazepam on the tail-withdrawal measure of analgesia in rats. Lethal doses of normeperidine were determined alone and in combination with three doses of diazepam, and lethal doses of meperidine were determined along and in combination with 10 mg/kg of diazepam. Diazepam potentiated the analgesic effects of meperidine and increased the dose of normeperidine necessary to produce lethality.
Topics: Animals; Diazepam; Dose-Response Relationship, Drug; Drug Interactions; Male; Meperidine; Nociceptors; Rats; Rats, Inbred Strains; Seizures
PubMed: 7111343
DOI: 10.1016/0091-3057(82)90061-2 -
Journal of Korean Medical Science Sep 1989Recently several reports have described the usefulness of meperidine as the sole agent for spinal anesthesia. In this study, meperidine 50mg mixed with 10% dextrose...
Recently several reports have described the usefulness of meperidine as the sole agent for spinal anesthesia. In this study, meperidine 50mg mixed with 10% dextrose 0.5ml was used for the spinal anesthetic agent for Cesarean section in 182 cases. The subarachnoid injection of meperidine resulted in anesthesia similar to that noted with the intrathecal administration of local anesthetics. Sensory and motor blockades in all patients with meperidine spinal anesthesia were obtained. Prolonged analgesic effect (453.7 +/- 158.1 minutes) and rapid motor recovery (75.9 +/- 17.2 minutes) were obtained. Side effects included nausea (49 patients), hypotension (95 patients) and pruritus (30 patients). Hypotension was easily treated with rapid hydration and ephedrine. Eighteen patients complained of mild pain during the last period of operation. At birth, all newborns cried immediately and the mean Apgar scores were 9.8 +/- 0.4 at one minute and 10 at 5 minutes. It is concluded that meperidine, which has advantages such as rapid motor recovery, prolonged postoperative analgesia, and mild complications which may be easily treated, can serve as a good alternative agent for spinal anesthesia for Cesarean section.
Topics: Adult; Anesthesia, Epidural; Anesthesia, Obstetrical; Cesarean Section; Female; Humans; Infant, Newborn; Injections, Spinal; Meperidine; Middle Aged; Pregnancy
PubMed: 2631746
DOI: 10.3346/jkms.1989.4.3.135 -
Psychopharmacology 1993Meperidine is a mu opiate agonist that is frequently used to treat pain. We examined in healthy volunteers (N = 10) the effects of intravenous meperidine (0, 0.25, 0.5,... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
Meperidine is a mu opiate agonist that is frequently used to treat pain. We examined in healthy volunteers (N = 10) the effects of intravenous meperidine (0, 0.25, 0.5, and 1.0 mg/kg) on mood and psychomotor performance. A randomized, placebo-controlled, crossover design was used in which subjects were injected with meperidine or saline in a double-blind fashion. Subjects completed several subjective effects questionnaires commonly used in abuse liability testing studies before drug injection and at periodic intervals for up to 5 h after drug injection. Subjects also completed several psychomotor tests. Meperidine produced a constellation of subjective effects in a dose-related fashion, including increases in ratings of "sedated," "coasting or spaced out" and "feel drug effect" ratings. Many of the drug's subjective effects persisted up to 4 or 5 h after administration of the 1.0 mg/kg dose. Drug liking ratings assessed on a visual analog scale were increased after meperidine injection in about half of the subjects (P = 0.09). Eye-hand coordination was affected slightly by meperidine but other indices of psychomotor functioning were unaffected. Miosis increased in a dose-related fashion. Other physiological parameters, such as vital signs, were not affected by meperidine. We conclude that meperidine in healthy volunteers has robust and long-lasting effects on mood, but may have weaker effects on psychomotor performance.
Topics: Adult; Affect; Behavior; Cross-Over Studies; Dose-Response Relationship, Drug; Double-Blind Method; Female; Hemodynamics; Humans; Injections, Intravenous; Male; Meperidine; Psychomotor Performance; Pupil
PubMed: 7870968
DOI: 10.1007/BF02244946 -
Clinical Pharmacology and Therapeutics Nov 1981The presystemic metabolism of meperidine to normeperidine was examined in four healthy men before, during, and 3 wk after phenytoin. The results from the two control...
The presystemic metabolism of meperidine to normeperidine was examined in four healthy men before, during, and 3 wk after phenytoin. The results from the two control periods were similar. Meperidine systemic clearance rose from 1017 +/- 225 ml/min (mean +/- SD) to 1280 +/- 130 ml/min during phenytoin dosing (P less than 0.01). Meperidine elimination half-life fell from 6.4 +/- 1.0 hr to 4.3 +/- 0.4 hr during phenytoin dosing (P less than 0.05). Bioavailability fell from 0.61 +/- 0.08 to 0.43 +/- 0.14 (P less than 0.07). Meperidine volume of distribution, renal clearance, and protein binding did not change. The normeperdine area under the blood concentration-time curve from 0 to 24 hr after intravenous meperidine rose from 385 +/- 105 ng/hr/ml-1 to 589 +/- 108 ng/hr/ml-1 during phenytoin dosing (P less than 0.01); after oral meperidine it rose from 592 +/- 50 ng/hr/ml-1 to 738 +/- 178 ng/hr/ml-1. Normeperidine renal clearance was approximately four times that of meperidine, but was not altered by phenytoin. Because analgesia relates to meperidine blood concentrations, patients on long-term phenytoin therapy may require more frequent parenteral doses and larger and more frequent oral doses than usual.
Topics: Adult; Drug Interactions; Humans; Male; Meperidine; Metabolic Clearance Rate; Phenytoin
PubMed: 7297025
DOI: 10.1038/clpt.1981.220 -
American Journal of Obstetrics and... Nov 1980The uptake of meperidine by the brain of the fetal lamb was investigated by determining the concentration of meperidine in the fetal brachiocephalic artery and sagittal...
The uptake of meperidine by the brain of the fetal lamb was investigated by determining the concentration of meperidine in the fetal brachiocephalic artery and sagittal vein after intravenous and intramuscular administration to the mother. A positive arteriovenous gradient across the fetal brain existed for 10 minutes after intravenous administration, and for 20 to 25 minutes after intramuscular administration, thus indicating the uptake of meperidine by the fetal brain. The peak concentration of unbound meperidine in the fetal brain, as estimated from the plasma concentration of free meperidine at equilibrium, was three to four times greater after intravenous administration than after intramuscular administration. The findings suggest that, during labor, the route of administration of meperidine will determine the time course of meperidine in the fetal brain and, consequently, the time action of effects seen in the neonate. The lag time required for plasma-brain equilibration may explain the lack of correlation between the incidence of neonatal respiratory depression and the levels of meperidine in the cord after intramuscular administration.
Topics: Animals; Blood-Brain Barrier; Brain; Female; Fetus; Injections, Intramuscular; Injections, Intravenous; Maternal-Fetal Exchange; Meperidine; Pregnancy; Sheep; Time Factors
PubMed: 7425023
DOI: No ID Found -
Anaesthesia and Intensive Care Oct 1998
Topics: Adjuvants, Anesthesia; Anesthesia, Spinal; Humans; Injections, Spinal; Meperidine
PubMed: 9807625
DOI: No ID Found -
British Journal of Anaesthesia Jul 1954
Topics: Humans; Meperidine; Phlebitis
PubMed: 13172374
DOI: 10.1093/bja/26.4.260