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At least 19 recordsLinked to original sources
PubMed1979

Meperidine and normeperidine levels following meperidine administration during labor. I. Mother.

Because of the unavailability of sensitive analytic techniques, the pharmacokinetics of meperidine have not been clearly delineated in obstetric patients during labor. Moreover, the production of the active meperidine metabolite--normeperidine--has not been investigated. By means of gas chromatographic and mass spectrometric techniques, these characteristics of meperidine metabolism were evaluated in 23 pregnant patients in the present study. The data show that the disappearance curve and pharmacokinetic constants for meperidine are similar to those previously reported for nonpregnant subjects. In regard to normeperidine, the data indicate that it is produced within ten minutes after meperidine injection, increases rapidly for the next 20 minutes, and then slowly increases throughout labor. The results enumerate the pharmacokinetic constants of meperidine in obstetric patients and describe the appearance of normeperidine, the active meperidine metabolite, following meperidine administration during labor.

Adult↗
PubMed1979

Meperidine and normeperidine levels following meperidine administration during labor. II. Fetus and neonate.

The time interval between the administration of meperidine to laboring patients and delivery may affect neonatal status, but sophisticated analytic techniques have not been used to determine the exposure of the fetus to meperidine at various drug-delivery intervals. By means of gas chromatography and mass spectrometry, the concentrations of meperidine and normeperidine (the principle metabolite of meperidine) were quantitated in the umbilical cord venous and arterial plasma at delivery and in the urine of the neonate for three days postpartum. Following 50 mg. of meperidine administered intravenously during labor, fetal exposure to meperidine was highest two to three hours after maternal medication while fetal exposure to normeperidine was highest four hours or more after medication. We conclude from this study that there is a definite but nonlinear relationship between the drug-delivery interval and the amount of meperidine and normeperidine an infant receives; and that the drug-delivery intervals resulting in maximum fetal exposure reported here correspond with those resulting in maximum neonatal depression reported by others.

Chromatography, Gas↗
PubMed1976

Effects of intravenous meperidine and meperidine with promethazine on uterine activity and fetal heart rate during labor.

A prospective study of the effects of the i.v. injection of 75 mg meperidine, alone or combined with 25 mg promethazine, was conducted by continuous and direct monitoring of the fetus and of intrauterine pressure. The study was carried out in 16 primiparas and 24 multiparas in active spontaneous labor with cervical dilatation of 3 to 4 cm. Administration of meperidine and of meperidine with promethazine was associated with an increase in uterine activity of 31 to 45% (Montevideo units), respectively. The most marked effects were on the amplitude of the uterine contractions. There was no significant change in uterine tone. A tetanic response was recorded in two patients who vomited after the administration of meperidine with promethazine and was followed by slowing of the fetal heart rate. In no other cases were there significant changes in fetal heart rate. Except for the latter two patients, no adverse effect of meperidine or of meperidine with promethazine on the fetal heart rate was noted. The condition of the newborns at birth was excellent in all but three cases, in two of which maternal amniotic infection and high fever were present.

Female↗
PubMed1975

The bioavailability of meperidine using urine assays for meperidine and normeperidine.

The results of a two-way crossover trial of two commercial preparations of meperidine hydrochloride in 24 healthy volunteers is reported. The urinary excretion patterns resulting from dosing with the two preparations were followed for 48 hours, and the urine concentrations of meperidine and a major metabolite, normeperidine, were determined by gas liquid chromatography. Statistical analysis of the data showed no significant difference between the urine concentrations of meperidine and normeperidine produced by either preparation, and the preparations are of comparable bioavailability. The use of the urinary excretion pattern and concentrations represents a rapid, accurate, and quantitative method for determining the bioavailability of different preparations of meperidine hydrochloride.

Adult↗
PubMed1976

Meperidine metabolites: identification of N-hydroxynormeperidine and a hydroxy-methoxy derivative of meperidine in biological fluids.

Gas chromatographic and gas chromatographic-mass spectrometric techniques were used to identify non-acidic metabolites of meperidine (N-methyl-4-phenyl-4-carbethoxypiperidine) excreted in human, rat, and guinea pig urine. Following enzymic hydrolysis N-hydroxynormeperidine was identified in the urine of all three species in addition to the expected metabolites normeperidine and meperidine N-oxide. In rat urine the p-hydroxyphenyl metabolite of meperidine was present in appreciable amounts. Also present in small quantity was a new phenolic metabolite of meperidine containing both hydroxyl and O-methoxyl substituents in the phenyl ring of the parent drug. The latter two metabolites were excreted as conjugates in the rat.

Adult↗
PubMed1975

Two mechanisms for the meperidine block of action potential production in frog's skeletal muscle; non-specific and opiate drug receptor mediated blockade.

The effects of meperidine and naloxone, and their interaction effects on action potential production in frog's sartorius muscle fibres, were studied with intracellular micro-electrode techniques. 1. Meperidine, a narcotic analgesic drug, depressed the rate of rise, the rate of fall and the amplitude of the action potentials. 2. At a meperidine concentration of 0-35 mM, the depression in the action potential maximum rate of rise followed a diphasic time course. At first there was a rapid reduction in the maximum rate of rise which was levelling off at about 60% of control 60-90 min after drug application. This was followed by the second phase during which there was an initial rapid decrease in the maximum rate of rise and all surface fibres were inexcitable by 180 min. 3. The addition of naloxone, a narcotic antagonist, in low concentrations (3 X 10(-5) to 3 X 10(-4) mM) at 70-90 min blocked the second phase of the meperidine-induced depression. 4. With lower concentrations of meperidine (0-18 and 0-07 mM) the depression usually developed more slowly (up to 6 hr with the latter dose) and the addition of low naloxone concentrations partially antagonized the effects of meperidine. However, under no conditions was it possible to completely antagonize the effects of meperidine by the addition of naloxone. 5. A linear relation was found between action potential amplitude and the action potential maximum rate of fall. 6. Meperidine caused a shift in the relation of rate of fall against amplitude to higher action potential amplitudes, indicating that the drug inhibited the increase in potassium conductivity (gK) associated with the falling phase of the action potential. 7. When low naloxone concentrations antagonized the effects of meperidine on the rate of rise and restored action potential amplitudes to control levels, the effect of meperidine on the maximum rate of fall was not antagonized. 8. Larger naloxone concentrations (1-5 X 10(-2) mM or more) depressed the action potential rate of rise but did not alter the relation between action potential amplitude and the maximum rate of fall. 9. It is proposed that meperidine blocks action potential production by two mechanisms: (i) a non-specific mechanism in which the increases in both gNa and gK ar depressed and (ii) an opiate drug receptor mediated mechanism causing a specific depression of gNa. 10. The impression gained from the results is that there are opiate drug receptors located on the inner surface of the muscle membrane associated with the 'sodium channels' and that drug activation of these receptors by either meperidine or high naloxone concentrations interferes with the opening of the 'sodium channels' normally produced by membrane depolarization.

Action Potentials↗
PubMedDate not supplied

Comparison of methotrimeprazine and meperidine as components of balanced anesthesia.

Methotrimeprazine (MTM) (0.5 mg/kg) and meperidine (1.5 mg/kg) was administered to four groups of 10 patients each. Two of these groups (I and II) received MTM or meperidine 12 minutes before, two other groups (III and IV), 3 minutes after, induction of thiopental anesthesia. N2O-O2 was administered after thiopental induction, and fractional doses of meperidine and muscle relaxants were used as required for maintenance of anesthesia. The preliminary administration of MTM or meperidine decreased the induction dose of thiopental by about 60 percent. When administered before thiopental, both had similar effects on heart rate, but whereas MTM moderately decreased, meperidine moderately increased systolic and diastolic blood pressure MTM had little or no effect on respiratory rate, which was significantly depressed by meperidine. When given after an induction dose of thiopental, the circulatory effects of MTM and meperidine were similar. Respiratory measurements were little affected by MTM but were markedly depressed by meperidine. The mug/kg/min maintenance doses of meperidine were about the same in the four groups. Postanesthetic recovery of consciousness was delayed in the two MTM groups. The incidence of postoperative nausea and vomiting was less in the MTM than in the meperidine groups. MTM appears to have several advantages over meperidine as a component of balanced anesthesia, but is not desirable if rapid postanesthetic recovery or early ambulation is important. Its use is indicated in patients in whom even transient respiratory depression is undesirable and in those in whom prolonged postoperative sedation is desired.

Adolescent↗
PubMedDate not supplied

[Administration of lysine acetylsalicylate and meperidine in acute postoperative pain].

INTRODUCTION: Postoperative analgesia is insufficiently done due, among others, to the undesirable effects of analgesic agents. OBJECTIVE: The aim of this study was to analyze the effects of the simultaneous administration of opiates (meperidine) and AINES (lysine acetylsalicylate, ASL). MATERIAL AND METHODS: We studied 160 patients during the immediate postoperative phase. All of them underwent programmed surgery with the same general anesthetic technique. Patients were allocated into 8 groups of treatment: A) ASL 900 mg and 1.800 mg/8 h, B) ASL 900 mg and 3.600 mg/8 h, C) ASL 900 mg and meperidine 100 mg/8 h, D) ASL 900 mg and 1.800 mg/8 h together with meperidine 100 mg/8 h, E) meperidine 50 mg and ASL 1.800 mg/8 h, F) meperidine 50 mg and ASL 3.600 mg/8 h, G) meperidine 50 mg and 100 mg/8 h, and H) meperidine 50 mg and 100 mg/8 h together with ASL 1.800 mg/8 h. The effects of analgesic agents were evaluated on the basis of patient's appreciation of the degree of pain and relief and on the basis of an observer who did not know the therapeutic regime administered. Results were compared according to the analysis of variance in a graded factorial design. A p value less than 0.05 was considered significant. RESULTS: The degree of pain was significantly lower in groups C, D, G and H (specially in G and H) than in the remaining groups, but there were no significant differences between them. The lowest pain relief was observed in groups A, B, E and F. The highest attenuation of pain was achieved in groups G and H. The highest attenuation of pain was achieved in groups G and H. The observer considered that the two latter groups were those with the highest pain relief, followed by groups C and D. The remaining patients failed to show appreciable improvement. Nausea and vomiting only occurred in some patients after administration of a bolus of meperidine. There were no other secondary effects. CONCLUSIONS: The best degree of postoperative analgesia is achieved after administration of continuous infusion of meperidine 100 mg/8 h. Simultaneous infusion of ASL 1.800 mg/8 h did not improve the analgesia obtained with a bolus of 900 mg of ASL nor with a bolus of 50 mg of meperidine. Secondary effects were only nausea and vomiting and coincided with the administration of a bolus of meperidine.

Adult↗
PubMed1976

The production and characterization of antibodies reactive with meperidine.

Meperidinic acid was converted to O-meperidinyl-glycollic acid and covalently attached to bovine serum albumin. Rabbits injected with this conjugate produced antibodies reactive with meperidine which were measured by the ammonium sulfate method. The specificities of these antisera were studied by competitive inhibition of the binding of 100 pmol/ml of 3H-meperidine to antibody by the prior addition of increasing concentrations of various unlabeled compounds. The concentrations in nanomoles per milliliter of various unlabeled opiods required to inhibit 3H-meperidine binding by 50% (I50) were: meperidine, 0.08; O-meperidinyl-glycollic acid, 1.7; methadone, 580; heroin, 1750; codeine, 2600; and morphine, 4200. Several psychopharmacologically active compounds were found to have I50 values comparable to the nonmeperidine opioids: hydroxyzine. HCl, 460; propoxyphene, 4,500; diazepam, 6,500; and cocaine, 10,800. The metabolites of meperidine exhibited the following I50 values: normeperidine, 0.7; meperidinic acid and normeperidinic acid, 210. A radioimmunoassay for meperidine which employs this antiserum was shown to be approximately 100 times more sensitive than the spectrophotometric method of Burns et al. (J. Pharmacol. Exp Ther. 114: 289-293, 1955). In this assay only normeperidine and some of the meperidine congeners might be expected to interfere with the measurement of meperidine. The degree of normeperidine interference was shown to be comparable to that present in the existing assay method.

Animals↗
PubMed1976

The production and characterization of antibodies reactive with meperidine.

Meperidinic acid was converted to O-meperidinyl-glycollic acid and covalently attached to bovine serum albumin. Rabbits injected with this conjugate produced antibodies reactive with meperidine which were measured by the ammonium sulfate method. The specificities of these antisera were studied by competitive inhibition of the binding of 100 pmol/ml of 3H-meperidine to antibody by the prior addition of increasing concentrations of various unlabeled compounds. The concentrations in nanomoles per milliliter of various unlabeled opiods required to inhibit 3H-meperidine binding by 50% (I50) were: meperidine, 0.08; O-meperidinyl-glycollic acid, 1.7; methadone, 580; heroin, 1750; codeine, 2600; and morphine, 4200. Several psychopharmacologically active compounds were found to have I50 values comparable to the nonmeperidine opioids: hydroxyzine-HC1, 460; propoxyphene, 4,500; diazepam, 6,500; and cocaine, 10,800. The metabolites of meperidine exhibited the following I50 values: normeperidine, 0.7; meperidinic acid and normeperidinic acid, 210. A radioimmunoassay for meperidine which employs this antiserum was shown to be approximately 100 times more sensitive than the spectrophotometric method of Burns et al. (J. Pharmacol. Exp. Ther. 114:289-293, 1955). In this assay only normeperidine and some of the meperidine congeners might be expected to interfere with the measurement of meperidine. The degree of normeperidine interference was shown to be comparable to that present in the existing assay method.

Animals↗
PubMed1992

Clinical and pharmacokinetic aspects of the combination of meperidine and prilocaine for spinal anaesthesia.

The aim of this study was to determine whether the addition of a small dose of prilocaine could augment the spinal block induced by meperidine and affect intrathecal meperidine pharmacokinetic behaviour. Spinal anaesthesia was performed in 60 men scheduled for endoscopic resection of a prostatic adenoma or bladder tumour under spinal anaesthesia. They were allocated randomly to receive either 1 mg.kg-1 meperidine (Group 1, n = 30), or 1 mg.kg-1 meperidine plus 0.5 mg.kg-1 prilocaine (Group 2, n = 30). Blood samples were collected prior to and for 24 hr after spinal injection in 24 patients (12 in each group). Plasma meperidine levels were assayed by gas chromatography. Complete motor block was achieved in all Group 2 patients, but was incomplete in seven of Group 1 (P less than 0.05). The onset of both motor and sensory blocks was shorter (P less than 0.01) in Group 2 and the duration was longer (P less than 0.05). Coadministration of prilocaine modifies meperidine pharmacokinetic behaviour. The area under curve was 48% greater (P less than 0.01) and Cmax was higher in Group 2 than in Group 1, 145.8 +/- 42.2 vs 107 +/- 20.5 ng.ml-1 (P less than 0.001). No evidence of respiratory depression was noted in any of the patients. Despite the increase in plasma meperidine concentrations, no side effects were observed. The plasma concentrations remained at one third to one sixth the levels reported to induce a respiratory depression. It is concluded that the addition of prilocaine to meperidine improves motor and sensory block during surgery and alters meperidine kinetics without producing major side effects.

Aged↗
PubMedDate not supplied

Patient-controlled analgesia with epidural meperidine after elective cesarean section.

BACKGROUND AND OBJECTIVES: We report the first controlled analysis of the use of patient-controlled epidural meperidine. This randomized, prospective study compares the efficacy and safety of patient-controlled epidural meperidine to conventional intramuscular meperidine for the management of postoperative pain after elective cesarean delivery. METHODS: After delivery, 60 patients were randomly assigned to receive either conventional intramuscular meperidine therapy or epidural meperidine by a patient-controlled analgesia pump, which was programmed to deliver bolus doses in addition to a continuous background infusion. RESULTS: Patients in the patient-controlled epidural analgesia group used significantly less meperidine in the first 24 hours after surgery (p < 0.05) and had significantly lower visual analog pain scores (p < 0.05) from three hours postoperatively until study completion at 24 hours. Patients in the patient-controlled epidural analgesia group ambulated sooner (19 +/- 7.8 versus 29.2 +/- 2.2 hours, p < 0.005) and cared for their infants earlier (4.6 +/- 0.9 versus 8.1 +/- 6.8 hours, p < 0.05) than patients receiving intramuscular meperidine. One patient developed a respiratory rate of four breaths per minute, 25 minutes after receiving 75 mg epidural meperidine in the operating room. This was treated with intravenous naloxone. No other serious side effects occurred in either group. Both groups were similar with regard to minor intraoperative and postoperative side effects. CONCLUSIONS: Patient-controlled epidural meperidine after cesarean delivery more effectively manages postoperative pain than conventional intramuscular use. The technique is preferred by both patients and nursing staff and can be used in the ward setting with appropriate organization and education. Respiratory depression, if it occurs, should present early after epidural bolus administration.

Adult↗
PubMed1978

Neonatal neurobehavior in the first 48 hours of life: effect of the administration of meperidine with and without naloxone in the mother.

The early neonatal neurobehavioral scale was administered to three groups of newborns at 2, 4, and 24 hours of age. Group 1 consisted of 28 babies whose mothers had received no narcotics during labor, group 2 of 33 babies whose mothers had received meperidine hydrochloride alone during labor, and group 3 of 40 babies whose mothers had received meperidine followed by 0.4 mg of naloxone hydrochloride intravenously approximately 15 minutes before delivery. Babies who were not exposed to meperidine showed a statistically significantly greater percentage of high scores than those exposed to meperidine alone for all items on the neurobehavioral scale at 2 and 4 hours and for all items except tone and Moro response at 24 hours. Similarly, babies whose mothers had received meperidine and naloxone showed a significantly greater percentage of high scores than those whose mothers had received meperidine alone at 2 hours of age. At 4 hours a difference was found for tone and rooting and at 24 hours for overall score, placing, and total decrement score. It is concluded that naloxone given intravenously to the mother reverses the effect of meperidine on neonatal neurobehavior for approximately two hours after birth. At 4 and 24 hours, however, the neurobehavior of neonates exposed to meperidine and naloxone is depressed almost as much as that of babies exposed to meperidine alone.

Child Behavior↗
PubMed1978

The effect of phenobarbital on the metabolism of meperidine in normal volunteers.

Phenobarbital has been observed clinically to alter the metabolism of meperidine, with resultant enhanced toxicity. In order to determine if this effect occurs consistently, 12 health volunteers were entered into a two-way, crossover study comparing the pharmacokinetics and metabolism of meperidine after pretreatment with both phenobarbital and placebo. Phenobarbital pretreatment had no significant effect on serum levels or the half-life of meperidine. However, phenobarbital pretreatment resulted in a decrease in the cumulative excretion of meperidine and an increase in the cumulative excretion of the N-demethylated metabolite normeperidine. Similarly, phenobarbital pretreatment resulted in a decrease in meperidinic acid and increase in normeperidinic acid. In addition, phenobarbital pretreatment also significantly altered the hepatic clearance of meperidine, indicating an increase in the hepatic N-demethylation of meperidine. Since normeperidine has been reported to be less efficacious and more toxic than meperidine, this reported interaction may be important clinically, especially with repeated doses.

Adult↗
PubMed1979

Urinary excretion of meperidine by the fetal lamb.

The renal excretion of meperidine by the fetus was determined in five chronic, unanesthesized fetal lamb preparations. Chronic indwelling catheters were implanted in the maternal aorta and vena cava, the fetal aorta, amniotic sac and allantoic sac. Via laparotomy, two catheters were implanted in the fetal bladder; the urachus and urethra were ligated. After intravenous administration of 2.5 mg/kg to the mother, meperidine rapidly appears in fetal urine. Approximately 0.02 to 0.05% of the maternal dose was excreted into fetal urine as unchanged meperidine in 300 min. The elimination half-life of meperidine in the fetus is 32.6 +/- 3.7 min when calculated from the urinary excretion rates, and 28.6 +/- 3.9 min when estimated from the plasma decay curve. The renal clearance of meperidine by the fetus ranged from 2.8 to 16.7 ml/min. Although the urachus and urethra were ligated, meperidine is found in samples of amniotic and allantoic fluid, indicating that the drug can diffuse across the placental membranes from the mother into these fluids. We have demonstrated that renal elimination of meperidine is a route of drug elimination by the fetus. These data support a pharmacokinetic model that describes the disposition of meperidine in the maternal-fetal unit by use of a two-compartment open model with elimination from both maternal and fetal compartments.

Animals↗
PubMed1977

Meperidine effects on schedule-controlled responding.

The effect of meperidine were studied on responding by pigeons under a multiple fixed-ratio, fixed-interval schedule of food presentation. Low doses of meperidine (0.3-3 mg/kg) generally increased and higher doses decreased responding under the fixed-interval component of the multiple schedule. The responding under the fixed-ratio component was usually unaffected by low doses and decreased by doses greater than 3 mg/kg of meperidine. Naloxone (1 mg/kg) antagonized the rate increases in the fixed-interval component; however, no dose of naloxone (1-56 mg/kg) or cyclazocine (0.1-3 mg/kg) antagonized the rate decreases produced by meperidine under either schedule component. The effects of morphine and meperidine were compared in two birds treated daily with methadone. In a bird maintained on a daily dose of 120 mg/kg (p.o.) of methadone, there was a 10-fold shift of the dose-effect curve for morphine but no shift of the meperidine dose-effect curve. In a bird maintained on a daily dose of 30 mg/kg (p.o.) of methadone, there was a 3- to 5-fold shift of the morphine dose-effect curve, but again no shift of the meperidine dose-effect curve. Thus, the rate-decreasing effects of meperidine were not antagonized by narcotic antagonists, nor did they show cross-tolerance to methadone.

Animals↗
PubMed1978

Clinical effects of meperidine in hospitalized medical patients.

Of 26,294 hospitalized medical patients monitored in a drug surveillance program, 366 (1.4%) received meperidine orally and 3268 (12.4%) received meperidine parenterally during one or more admissions. Neoplastic disease was the most common category of primary diagnosis (43%) among oral recipients; among parenteral recipients cardiovascular and neoplastic diseases (23% each) were most common. Oral meperidine was prescribed almost exclusively (93%) for pain relief, whereas the parenteral drug also had substantial use (41%) as a diagnostic and preoperative adjunct. Oral meperidine was judged by attending physicians to have provided unsatisfactory pain relief in 22% of recipients, while parenteral meperidine was rated unsatisfactory in 11%. The drug was less effective in patients with a primary diagnosis of neoplastic disease than in patients with other primary diagnoses. Minor gastrointestinal disturbances were the most commonly reported adverse reactions among oral meperidine recipients (2.7%); among parenteral recipients central nervous system effects were most common (1.2%). Seven recipients had life-threatening adverse reactions. However, only two of these were judged definitely related to meperidine, and in both instances other drugs were also definitely implicated. Adverse reactions were dose related.

Administration, Oral↗
PubMed1992

Comparison of the efficacy and safety of ketorolac and meperidine in the relief of dental pain.

A single-dose, randomized, double-blind study of parallel design was conducted to determine the analgesic efficacy and safety of ketorolac tromethamine in patients who experience moderate or severe pain after the surgical removal of three or more third molars, one of which was a bony-impacted mandibular molar. Meperidine hydrochloride was used as the control analgesic. In this 8-hour study, assessments were made of pain intensity, pain relief, and overall rating of the medication in 145 patients, each of whom had received an intramuscular injection of 10 mg, 30 mg, or 90 mg of ketorolac, or 50 mg or 100 mg of meperidine. The summed pain intensity and total pain relief scores showed that, at 3 and 8 hours, the effectiveness of 30 mg of ketorolac was similar to that of 90 mg ketorolac and that both of these doses were significantly more efficacious than 10-mg ketorolac, 50-mg meperidine, or 100-mg meperidine. Patients who received 30 mg or 90 mg of ketorolac gave the study medication significantly higher ratings overall than did patients who received 50 mg or 100 mg of meperidine. Significantly fewer patients treated with ketorolac reported adverse events in comparison with those treated with meperidine (17% and 59%, respectively), which suggests that it possesses a better therapeutic index than meperidine. Thus, ketorolac appears to represent an important advance in analgesic therapy.

Analgesics↗