Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0011570 (depression)
 172,036 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The pharmacokinetics of pethidine has been studied in 12 patients subjected to major intraabdominal surgery. Pethidine and norpethine were analyzed in plasma samples collected during anesthesia and during patient-controlled administration of small intravenous doses of pethidine in the early postoperative period. A second study on the pharmacokinetics of pethidine was performed on the 3-5th postoperative day. The plasma clearance of pethidine was significantly lower in the preoperative study (8.9 +/- 1.8 ml x kg x min-1) compared with the postoperative study (12.0 +/- 3.1 ml x kg x min-1). Volume of distribution (Vd) was not significantly influenced, being 4.25 +/- 1.72 l x kg-1 peroperatively and 3.14 +/- 0.84 l x kg-1 postoperatively. Elimination half-life decreased from 5.91 +/- 3.57 h peroperatively to 3.25 +/- 1.40 h postoperatively. The kinetics of pethidine in the postoperative study agreed with pethidine kinetics reported for healthy volunteers. The fraction of unbound pethidine decreased from 0.26 +/- 0.1 peroperatively to 0.18 +/- 0.1 postoperatively. Norpethidine, a metabolite of pethidine, has been claimed to be responsible for several side effects like respiratory depression and convulsions during pethidine therapy. No side effect attributable to norpethidine was observed in the self-administration period. Norpethidine plasma concentrations did not exceed 500 ng/ml. The altered pethidine pharmacokinetics during anesthesia and the ensuing postoperative hours and the interindividual differences of the disposition of the drug strongly suggest that pethidine should be given by individualized regimens in surgical patients.
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PMID:Pharmacokinetics of pethidine during anaesthesia and patient-controlled analgesic therapy. 695 38

Pethidine 50 mg, fentanyl 100 microgram and morphine 2 mg administered to the extradural space, were compared in the treatment of pain following surgery. All three drugs produced a rapid decrease in pain scores as assessed using a visual linear analogue, morphine being the least effective. Fentanyl had a relatively short duration of action (2 h), whereas morphine appeared to be the longest acting. It is suggested that the best relief of pain would be obtained by incremental doses given extradurally. All drugs produced an increase in sedation, but there was no respiratory depression as assessed by PaCO2 measurement.
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PMID:Extradural opioids for postoperative analgesia. A double-blind comparison of pethidine, fentanyl and morphine. 702 74

The pain-relieving effect of a single extradural dose of pethidine 25 mg with and without adrenaline was studied in 20 healthy women during labour. The study was open regarding the effects of pethidine but double-blind regarding the addition of adrenaline. In 14 of 19 women good or excellent analgesia was achieved for a period of 50-160 min. Pethidine with adrenaline 25 micrograms was not more effective than pethidine alone. Eight of the 14 women showed signs of regional analgesia to pin-prick and temperature discrimination. The patients had small (45-188 ng ml-1) concentrations of pethidine in plasma. In eight patients the plasma concentrations of pethidine were maintained for at least 1.5 h. Extradural pethidine thus induces analgesia of short and variable duration. Repeated doses may be needed, resulting in accumulation of the drug in plasma with the risk of respiratory depression in mother or child.
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PMID:Extradural pethidine with and without adrenaline during labour: wide variation in effect. 706 38

Data collected by the Quebec Board of Physicians show that during the 5 years from 1974 to 1978 the prevalence of addiction to opiates among Quebec physicians was 2.8/1000. The physician addicts had greater mobility and a higher attrition rate than their peers. The typical addict was male, a general practitioner and married. He often suffered from pain, fatigue, overwork, and financial and marital difficulties. His addiction had begun at approximately 35 years of age and had become evident about 3 1/2 years later. Meperidine was the preferred opiate. Some of the physicians lost their licences to practise for variable periods of time; for these the prognosis was gloomy. Depression was the main psychiatric disorder diagnosed.
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PMID:Drug addiction among Quebec physicians. 707 90

Pethidine (100 mg) was administered i.m. to women in labor at different times before delivery. The interval before respiration in the newborn became sustained was shorter if pethidine was given less than one hour before delivery. The respiratory rate of the newborn increased after naloxone injection in 40 per cent of the cases, mostly when intrauterine exposure to pethidine exceeded one hour. The plasma concentrations of pethidine and norpethidine were measured in mother and newborn. The concentrations in the umbilical vein and artery indicted a continuous net transfer of pethidine from mother to fetus for approximately two hours. This correlated with the clinical finding of maximal neonatal depression 2-3 hours after maternal injection. The concentrations of norpethidine increased with a longer time interval between injection and delivery, but were probably too low to have any effect on the newborn. Neonatal depression seems to be related to the amount of unmetabolized pethidine that has been transferred from mother to fetus but not to norpethidine as had been suspected earlier.
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PMID:Neonatal depression after obstetrical analgesia with pethidine. The role of the injection-delivery time interval and of the plasma concentrations of pethidine and norpethidine. 721 Dec 35

Meperidine 1 mg kg-1 and pentazocine 0.3 mg kg-1 were administered epidurally to investigate their effect on vesical function in twenty American Society of Anesthesiologists Classification I (ASA-1) adult males. Cystometry was performed before and 45 minutes following epidural administration of meperidine and pentazocine. There was no significant change in maximum cystometric capacity, detrusor pressure at which detrusor reflex occurred and in vesical compliance following epidural administration of meperidine in ten patients and also in ten patients who received epidural pentazocine. The mean onset of analgesia after epidural administration of meperidine was 8 minutes which lasted for more than 360 minutes whereas mean onset of analgesia after epidural administration of pentazocine was 4 minutes which lasted for more than 360 minutes. There was no significant change in heart rate, blood pressure and respiratory rate after epidural administration of either meperidine or pentazocine. None of the subjects in either of the groups experienced any difficulty in passing urine, frequency or urgency of micturition. Side-effects like nausea, vomiting, pruritus and respiratory depression were not observed. It is concluded that epidural administration of meperidine 1 mg kg-1 or pentazocine 0.3 mg kg-1 produces significant analgesia of faster onset without altering vesical function as documented, both subjectively by voiding symptoms and objectively by cystometry.
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PMID:Analgesic and urodynamic effects of epidural meperidine and pentazocine--a comparative study. 771 90

Hydroxyzine is frequently used to tranquilize chronic obstructive pulmonary disease patients, who may be concomitantly receiving narcotic analgesics. Therefore, its effect alone and in combination with meperidine on arterial blood gases and ventilation at rest were evaluated in 44 patient volunteers, who gave informed consent. Hydroxyzine, 1.5 mg/kg i.v. caused no significant decrease in PaO2 and pH, no increase in PaCO2 at 5, 10, 20, 30 and 60 min post-infusion (n = 13, mean age = 63.4 years). Meperidine, 1.5 mg/kg i.v. caused a significant (p < 0.001) reduction in PaO2 for 20 min with concomitant increase in PaCO2 (n = 14; mean age = 49.4 years). The combination of the same doses of hydroxyzine with meperidine i.v. caused no greater decrease in PaO2 or in pH or increase in PaCO2 than did meperidine alone (n = 17; mean age = 52.6 years), indicating no greater ventilatory depression with the combination than with meperidine alone. The lack of significant pH decreases at 30 and 60 min further corroborates no potentiation of meperidine by hydroxyzine. In conclusion, hydroxyzine, even when given through the i.v. route in excess of the maximum i.m. therapeutic dose, caused no changes in PaO2, PaCO2 or pH in chronic obstructive pulmonary disease patients. Therefore, its i.m. administration resulting in lower blood levels than i.v., is not likely to cause ventilatory depression. Furthermore, hydroxyzine caused no potentiation of the ventilatory depression induced by meperidine, hence hydroxyzine may be safely employed in combination with meperidine.
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PMID:Effect of hydroxyzine and meperidine on arterial blood gases in patients with chronic obstructive pulmonary disease. 846 9

The respiratory and analgesic effects of i.v. meperidine, tramadol and their correlation with plasma concentrations of meperidine, tramadol and O-demethyltramadol were determined. Forty-eight patients after total hip or knee replacement were randomly distributed into 3 groups (n = 16 each). At the time of analgesia request, they received in a double-blind manner, i.v. single doses of 100 mg meperidine, 100 mg tramadol, or saline. Thirty minutes after treatment, patients who requested additional analgesia were rescued with 75 mg diclofenac and morphine as required. Patients were evaluated at the time of analgesia request and at set intervals during 4 h. Meperidine induced sedation (p < 0.05), respiratory depression (tidal volume, p < 0.047; respiratory rate, p < 0.004; % O2 Sat, p < 0.036), and hypercapnia (PaCO2, p < 0.002). Incidence of nausea and vomiting was higher with tramadol (p < 0.02). For the first 30 min, meperidine produced lower pain intensity scores than tramadol or saline (p < 0.05). At this time, 14/16 patients on saline, 8/16 on meperidine and 11/16 on tramadol were rescued. Onset for meperidine analgesia was 10 min and > 30 min for tramadol. Both opioids produced similar degree of analgesia in patients who were not rescued. A negative correlation (r = -0.99) between analgesia and tramadol concentrations and a poor positive correlation (r = +0.54) with O-demethyltramadol (a metabolite of tramadol) was observed. Pain intensity differences correlated negatively with meperidine plasma concentrations during the first 30 min (r = -0.97) and positively thereafter (r = +0.92). In the present study, meperidine and tramadol produced comparable analgesia, with a different time course profile, but meperidine induced sedation and respiratory depression while tramadol did not.
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PMID:Respiratory and analgesic effects of meperidine and tramadol in patients undergoing orthopedic surgery. 873 73

Tramadol is a centrally acting opioid with a low affinity for mu-opioid receptors, which has been claimed not to depress respiration as do the classic opioids. The respiratory effects of intravenous (i.v.) pethidine (0.6 mg kg-1) and tramadol (0.6 mg kg-1) were compared in 36 ASA Grade I-II patients in a placebo-controlled double-blind study. After induction of anaesthesia with propofol followed by suxamethonium-facilitated endotracheal intubation, the patients spontaneously breathed halothane in 70% nitrous oxide and oxygen via a non-rebreathing valve. Inspiratory and expiratory oxygen, and end-tidal carbon dioxide concentrations (PETCO2), tidal volume (VT), minute volume of ventilation (MV) and respiratory rate were monitored by a side-stream spirometry at an end-tidal halothane of 0.3%. The recordings were collected before surgery. Pethidine caused significant respiratory depression seen as an increase in fractional inspiratory-expiratory oxygen difference and PETCO2 and as a decrease in MV and respiratory rate. However, the effects of tramadol were similar to those of a placebo. Tidal volume was not affected by any study drug. In conclusion, tramadol 0.6 mg kg-1 was shown not to be associated with respiratory depression, unlike equipotent dose of pethidine in this setting.
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PMID:Comparison of respiratory effects of tramadol and pethidine. 952 44

The traditional view of opioids held that the individual opioid agonists shared the same mechanism of action, differing only in their potency and pharmacokinetic properties. However, recent advances in opioid receptor pharmacology have made this view obsolete. Distinguishing features of the synthetic opioid agonists are related, at least in part, to variation in affinity and intrinsic efficacy at multiple opioid receptors. Respiratory depression is the opioid adverse effect most feared by anaesthesiologists. Specific kappa-receptor agonists produce analgesia with little or no respiratory depression. There are a number of commercially available kappa-receptor partial agonist drugs, the so-called agonist-antagonist or nalorphine-like opioids, which appear to have a limited effect on breathing. Within the series of fentanyl analogues there are differences in behaviour towards particular opioid receptors and there is evidence for subtle differences in respiratory depressant effects. Pethidine (meperidine) causes histamine release and myocardial depression, while the fentanyl analogues do not. Pethidine has atropine-like effects on heart rate, while fentanyl analogues reduce heart rate by a vagomimetic action. Severe bradycardia or even asystole is possible with fentanyl analogues, especially in conjunction with the vagal stimulating effects of laryngoscopy. Fentanyl analogues often produce minor reductions in blood pressure, and occasionally severe hypotension by centrally mediated reduction in systemic vascular resistance. Muscle rigidity and myoclonic movement occurs frequently during induction of anaesthesia with larger doses of opioids. Fentanyl and alfentanil have been reported to produce localised temporal lobe electrical seizure activity in patients with complex partial epilepsy. There are probably fewer biliary effects with agonist-antagonist opioids than the agonist opioids. The mechanism of adverse effects after spinal administration is distinctly different for morphine, which is very water soluble, compared with more lipid-soluble opioids. The systemic absorption of morphine after intrathecal or epidural administration is very slow, resulting in long duration of analgesia and low plasma concentrations, while lipid-soluble opioids are rapidly absorbed into the circulation and redistributed to the brain. The serotonin syndrome may result from coadministration of pethidine, dextromethorphan, pentazocine or tramadol with monoamine oxidase inhibitors (MAOIs) or selective serotonin (5-hydroxytryptamine; 5-HT) reuptake inhibitors (SSRIs). There are clinically important interactions between opioids and hypnosedatives, resulting in synergistic effects on sedation, breathing and blood pressure.
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PMID:Adverse effects of opioid agonists and agonist-antagonists in anaesthesia. 974 65


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