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At least 19 recordsLinked to original sources

Effect of antacids on the plasma concentration of phenoperidine.

The effect of antacids on the plasma concentration of phenoperidine was studied in six volunteers. All subjects received the same dose of phenoperidine (15 micrograms kg-1) on different occasions in the presence, and absence of, an antacid preparation. In control studies, secondary peaks in the plasma concentration of phenoperidine were invariably observed; these were entirely eliminated, or modified substantially, by the concurrent administration of antacids. In the latter conditions, plasma concentrations of phenoperidine were greater during the first 20 min, and the area under the plasma concentration--time curve between 0 and 20 min was significantly greater than in control studies. In contrast, the plasma clearance of the drug was almost identical in control conditions and during treatment with antacids. After the oral administration of phenoperidine to two subjects, the systemic bioavailability of the drug was 9.9% and 13.9% respectively.

Administration, Oral

Pharmacokinetics of phenoperidine in patients undergoing cardiopulmonary bypass.

Phenoperidine concentrations were studied, using radioimmunoassay, in five patients submitted to coronary artery bypass graft surgery. Administration of phenoperidine consisted of a 5-mg bolus dose followed by constant infusion of 5 mg h-1. Before cardiopulmonary bypass, phenoperidine concentrations were stable in an individual patient, but there was a large scatter between patients. The concentrations decreased immediately following the start of the bypass, but this decrease was short. During cardiopulmonary bypass, the phenoperidine concentrations increased progressively and were greater at the end of the bypass than before it. The increase in concentration continued following the discontinuation of bypass. The ratios of change of the observed results were in accord with a theoretical evaluation, although the observed concentrations were all greater than those calculated, except at one point. This difference in phenoperidine concentration is probably related to an alteration of liver plasma flow. Haemodilution as a result of the priming of the cardiopulmonary bypass circuit played only a transient role.

Adult

A comparison of diazepam and phenoperidine in premedication for upper gastrointestinal endoscopy: a randomized double blind controlled study.

A variety of agents are used as premedication for upper gastrointestinal endoscopy (U.G.E.). To our knowledge, no double blind studies have been performed to compare their value. In this study phenoperidine (2 mg i.v.) was compared with diazepam (t mg i.v.) in 200 consecutive patients undergoing elective U.G.E. The study was randomized and double blind in regard to both endoscopists and patients. All patients were given atropine (0.4 mg i.v.) and a throat spray with 2% amethocaine. Patients who needed supplemental medication were given diazepam and excluded from final analysis. A graded questionnaire was recorded by endoscopists and patients after U.G.E., and a further anonymous questionnaire was returned by patients four days later. Statistical analysis revealed that phenoperidine was superior at facilitating intubation and providing more relaxation as judged by the endoscopist. Patient questionnaires, four days after U.G.E., indicated less distress during intubation and examination with phenoperidine. Nausea, vomiting, amnesia and phlebitis were uncommon after either phenoperidine or diazepam.

Clinical Trials as Topic

Influence of bolus doses of phenoperidine on intracranial pressure and systemic arterial pressure in traumatic coma.

The effects of bolus doses of phenoperidine 1-2 mg i.v. either alone, or combined with pancuronium 2-4 mg, were investigated in seven patients in traumatic coma. Phenoperidine alone significantly reduced mean arterial pressure (MAP) by a mean (+/- SEM) of 13.2 (+/- 2.8) mm Hg. Overall there was no significant change in intracranial pressure (ICP) despite the decreases in MAP and, consequently, cerebral perfusion pressure (CPP) decreased (14.0 +/- 2.4 mm Hg) on all but one occasion. In some instances these decreases were considerable (maximum 38 mm Hg). Similar results were obtained when phenoperidine was combined with pancuronium. These findings suggest that the bolus administration of phenoperidine and probably other opiates should be avoided in traumatic coma.

Adolescent

[Hemodynamic effects of equipotent doses of phenoperidine and fentanyl in man].

The haemodynamic effects of phenoperidine and fentanyl were studied in ten patients with craniocerebral trauma who presented no surgical indications. They were all mechanically ventilated with a constant tidal volume and rate and their cardiovascular state was stable. The patients were given 5 gamma/kg of fentanyl intravenously; the haemodynamic measurements were performed at two mn interval for 20 mn. Three hours later, the patients were given 30 gamma/kg of phenoperidine intravenously and the haemodynamic measurements were performed similarly. Phenoperidine and fentanyl had the same effects: a significant fall in heart rate, mean arterial pressure and cardiac index without any change in pulmonary wedge pressure. These changes do not dangerously alter the haemodynamic condition of the patients and thus are not a contra-indication to the general use of phenoperidine and fentanyl in anaesthetic practice and in intensive care.

Adult

Plasma concentration and metabolism of phenoperidine in man.

The plasma concentrations of phenoperidine were measured in five patients during general anaesthesia. The concentration of the drug decreased rapidly between 2 and 40 min and then declined more slowly. Detectable concentrations of phenoperidine were present in plasma for at least 3 h. In the five patients, the distribution half-life of the drug ranged from 3.19 to 14.23 min and the elimination half-life from 47.31 to 162.30 min. Unchanged phenoperidine and two identified metabolites (pethidine and norpethidine) were present in urine.

Adjuvants, Anesthesia

Elimination of phenoperidine in liver disease.

The disposition and elimination of phenoperidine was studied in five normal subjects, and in six patients with hepatic disease. Plasma concentrations of phenoperidine were generally higher in patients with hepatic dysfunction. Secondary peaks were observed between 15 and 105 min (particularly in patients with liver disease). In the patients the terminal half-life of phenoperidine was prolonged by approximately 50%, mainly because of a decrease in the clearance of the drug. There was little or no change in the total apparent volume of distribution. However, the differences between normal subjects and patients with hepatic disease were not statistically significant. The results suggest that slight or moderate impairment of hepatic function does not significantly affect the kinetics of the drug, and that modification of its dosage may not be required.

Adult

Intracranial pressure after phenoperidine.

The problem of sedating patients requiring prolonged controlled ventilation has recently received considerable attention. Various therapeutic regimes are available and there appears to be a general move away from the use of muscle relaxants towards sedative drugs. Phenoperidine is a popular agent for this purpose. One survey from a district general hospital reported that 66% of their ventilated intensive therapy unit patients received phenoperidine, either alone or as part of a sedation regime. However, enthusiasm for its use must be tempered by recent reports of cardiovascular collapse following its administration. We wish to report a case of intracranial hypertension following the use of phenoperidine in a ventilated patient with a severe head injury.

Blood Pressure

[Anesthesia with continuous infusion of alfatesine and phenoperidine. Uses in anesthesia of aged subjects in visceral surgery].

Anaesthesia was administered to one hundred and fifty eight patients by continuous infusion of a mixture of Alfatesine and phenoperidine. The patients were divided on two groups: group A consisted in 96 patients undergoing abdominal surgery and group B of 62 cases of various types of surgery, mainly orthopedics. The average age was 63 years (range 16-96). The operative risk scored 6 or more in 71 cases. The length of operation averaged 151 minutes (S.D. +/- 15). The mixture made of alfadione 25 ml and phenoperidine 5 mg in a glucose 5 per cent 250 ml solution was administered by mechanical pump. The induction dose was 50 ml of the mixture for patients under 50 years (rate 10 ml per minute), 40 ml per patients from 50 to 70 years (5 ml per minute), and 30 ml for patients over 70 years (5 ml per minute). The maintenance dose was adjusted to weight and age and ranged from 0,11 to 0,15 ml/kg/h for alfadione and from 0,022 to 0,030 mg/kg/h for phenoperidine. Routine tracheal intubation and artificial ventilation were performed in group A. The results are studied in relation to the effectiveness of the anaesthesia mixture, its side effects and influence on recovery. Generally, the results are good and emphasize the value of the technic in abdominal surgery for elderly patients. The methods of application are discussed in terms of medical background.

Adult

Influence of anaesthetic technique on postoperative pain. A comparison of anaesthetic supplementation with halothane and with phenoperidine.

Fifty male patients undergoing elective surgery for duodenal ulcer received either phenoperidine or halothane 0.5% for the supplementation of anaesthesia. The patients in the phenoperidine group required the first postoperative dose of analgesic later and had lower pain scores in the first 2 h after operation. In the course of the 1st, 2nd and 3rd days, the two groups of patients showed a similar pattern after operation with regard to pain scores, vital capacity impairment and oxygen tension measurements.

Adolescent

Blood loss in total hip replacement: extradural v. phenoperidine analgesia.

The effects of phenoperidine and extradural analgesia on blood loss during and after total hip replacement were compared in 41 patients randomly divided into two statistically comparable groups. Mean blood loss in patients who received phenoperidine was 1065 +/- 316 ml and in patients who received extradural analgesia with 0.5% bupivacaine with adrenaline 1:200 000 it was 650 +/- 277 ml (p less than 0.001). There was no significant difference in postoperative blood loss between the two groups. The reduction in blood loss resulting from the extradural block may prove beneficial in decreasing the hazard and cost of blood transfusions and in facilitating autologous transfusion.

Aged

Pharmacokinetics of phenoperidine in anaesthetized patients undergoing general surgery.

The pharmacokinetics of phenoperidine have been studied in five anaesthetized patients receiving a 2-mg bolus dose i.v. Plasma concentrations were measured using a sensitive radioimmunoassay method. The distribution of phenoperidine was described according to a two-compartment open model. The mean distribution half-life (T1/2 alpha) for the five patients was short (2.2 min); the mean elimination half-life (T1/2 beta) was 193 min. The mean whole body clearance was 22 ml min-1 kg-1 and the apparent steady state distribution volume (VSS) was 5.7 litre kg-1. Secondary concentration peaks occurred in all patients; in two patients these were substantial and occurred 80 min after injection.

Anesthesia, General

Double-blind comparison of the efficacy of extradural diamorphine, extradural phenoperidine and i.m. diamorphine following caesarean section.

A randomized, double-blind study of the efficacy, duration of action and side effects of three analgesic regimens following Caesarean section is described. Patients received i.m. diamorphine 5 mg, extradural phenoperidine 2 mg or extradural diamorphine 5 mg. Analgesia was of rapid onset in all groups, as judged by reductions in linear analogue pain scores and rank pain scores. Time to next analgesia was significantly greater after extradural phenoperidine (5.96 h) and extradural diamorphine (8.39 h) than after i.m. diamorphine (3.40 h) (P less than 0.001). Itching was reported on direct questioning by 50% of patients in the extradural groups. No serious side effects were reported. Factors affecting the disposition of extradurally administered diamorphine are discussed.

Adult

Effect of urine pH on the elimination of phenoperidine.

The effect of urine pH on the plasma concentration and elimination of phenoperidine and its main metabolites was studied in six volunteers. The clearance of unchanged phenoperidine in acid urine was significantly greater than in neutral or alkaline urine. By contrast, the elimination of its basic metabolites was enhanced in uncontrolled or alkaline urine. Other pharmacokinetic parameters were not significantly affected.

Adult

[Phenoperidine and operative common bile duct pressure (author's transl)].

The pressure variations registered in the common bile duct, after injection of phenoperidine (0,033 mg/kg) during sixteen anaesthesias performed for cholecystectomy, showed no significant modifications. In one case a spasm of the common bile duct was observed before analgesic administration which induced no change in the biliary pressure, an inhalation of amyl nitrite made it possible to affirm the functional character of the anomaly. The analgesic anaesthesia using phenoperidine, method chosen for high-risk patients, is compatible with bile duct surgery without risk of bringing about unnecessary surgical procedures.

Adult

Comparative study of cardiovascular, neurological and metabolic side effects of 8 narcotics in dogs. Pethidine, piritramide, morphine, phenoperidine, fentanyl, R 39 209, sufentanil, R 34 995. II. Comparative study on the epileptoid activity of the narcotics used in high and massive doses in curarised and mechanically ventilated dogs.

The experimental design, described in part I, was again used here. The electrocortical activity was registered with an EEG amplifier using a bipolar derivation of needle electrodes fixed in the scalp of a dog in the fronto-occipital position. In this situation the convlusion threshold for the 8 substances is as follows: pethidine 20 mg.kg-1 I.V., piritramide 30, morphine 180, phenoperidine 4, R 39 209 5, fentanyl 4, sufentanil 4 and R 34 995 10 mg.kg-1 I.V. Comparing the I.V. doses producing severe convulsions with the doses necessary for deep surgical analgesia a safety margin of neurological toxicity was calculated. This was for pethidine 2.2, for piritramide 6.6, for phenoperidine 16, for R 39 209 62.5, for morphine 72, for fentanyl 160, for sufentanil 1 000 and for R 34 995 10 000. It is concluded that for pure narcotics there exists an inverse relationship between analgesic potency and neurological toxicity which is always accompanied by a hyperactivity of the automatic nervous system. Factors modifying the convulsive level of the narcotics are still under investigation. In the meanwhile it can be stated that the association of a strong narcotic with flunitrazepam, droperidol or etomidate will increase the convulsion threshold of the morphinomimetics.

Acidosis

Simultaneous determination of pethidine (meperidine), phenoperidine, and norpethidine (normeperidine), their common metabolite, by gas chromatography with selective nitrogen detection.

This article describes a selective gas chromatographic method for the resolution and quantification of phenoperidine and its two metabolites, pethidine (meperidine) and norpethidine (normeperidine). Drugs and SKF 525 A, the internal standard, are separated from plasma by solvent extraction under alkaline conditions. They are chromatographed on a 3% OV-17 Chromosorb Q glass column and detected with a nitrogen-phosphorous detector. Linearity is observed in the study range (5-200 ng/ml). No interference by endogenous substances is noted.

Cholinesterase Inhibitors

[Neuroplegia and extracorporeal circulation. Comparison between combinations of droperidol-phenoperidine and chlorprothixene-dextromoramide in cardiac surgery].

After a quick review of the physiopathology of extra-corporeal circulation, the value of the use of neuroplegic drugs in cardiac surgery is recalled by means of pharmacological arguments. The experimental differences existing between the combinations droperidol - phenoperidine and chlorportixene - dextromoramide, on the rate of flow and on the pressure of the perfusion, and on the esophago-rectal thermic gradients during E.C.C. is then demonstrated. Statistic calculation confirmed the superiority of chlorprotixene in the realm of tissue perfusion during E.C.C. under hypothermia.

Adult