Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Rocuronium”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 379 records · Page 21Linked to original sources
PubMed1994

Onset and duration of action and hemodynamic effects of rocuronium bromide under balanced and volatile anesthesia.

The onset and duration of action, and hemodynamic effects of rocuronium bromide 0.6 or 0.9 mg kg-1 were studied in 4 groups of 10 patients each during anesthesia with nitrous oxide in oxygen and fentanyl or halothane. Neuromuscular block was monitored using mechanomyography and train-of-four (TOF) stimulation. The mean time to onset of complete neuromuscular block was 55 s with the 0.6 mg kg-1 dose during both anesthetic techniques. The times to recovery of T1 (first response in the TOF stimulation) to 25 and 90% of control and to the recovery of the TOF ratio to 0.7 were 36, 45 and 54 min respectively during narcotic anesthesia, and 35, 54 and 58 min during halothane anesthesia. Complete block with the 0.9 mg kg-1 dose occurred in 50, and 52 s respectively in the fentanyl and halothane groups. The recovery of T1 to 25% occurred in 49 and 52 min, to 90% in 66 and 71 min and to TOF ratio of 0.7 in 72 and 79 min respectively during balanced and halothane anesthesia. There were no significant changes in heart rate or mean arterial pressure during the 5 min following administration of either dose of rocuronium during balanced or halothane anesthesia. A separate group of 10 patients received 0.9 mg kg-1 of rocuronium during anesthesia with nitrous oxide, oxygen and isoflurane. Complete block occurred in an average time of 45 s in these patients with 25% recovery of T1 in 53 min.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1995

Pharmacokinetics of rocuronium bromide in patients with and without renal failure.

We studied the onset and duration of action and pharmacokinetics of rocuronium bromide during anaesthesia with nitrous oxide, fentanyl and isoflurane after a single bolus dose of rocuronium (0.6 mg kg-1) in nine patients with chronic renal failure requiring regular haemodialysis, and in nine healthy control patients. Blood samples were collected over 390 min and concentrations of rocuronium and its putative metabolites measured using HPLC. Onset time for maximum block and duration of clinical relaxation (DUR25) were 61 (SD 25.0) s and 65 (16.4) s, 55 (26.9) min and 42 (9.3) min, respectively, for patients with and without renal failure. The time for train-of-four ratio to return spontaneously to 0.7 was 99 (41.1) min and 73 (24.2) min, respectively, in the two groups. None of these differences was significant. The pharmacokinetic data were best described by a three-exponential equation. There were significant differences between patients with and without renal failure in the rates of clearance (2.5 (1.1) mL kg-1 min-1 and 3.7 (1.4) mL kg-1 min-1, respectively) and the mean residence times (97.1 (48.7) min and 58.3 (9.6) min) (P < 0.05). The differences in other kinetic parameters were not significant.

Androstanols↗
PubMed1995

1 x ED90 dose of rocuronium bromide: tracheal intubation conditions and time-course of action.

The intubation conditions and time-course of action of a 0.3 mg kg-1 bolus of rocuronium were studied under alfentanil/propofol and fentanyl/thiopentone/enflurane anaesthesia. Forty healthy patients were randomly allocated to induction of anaesthesia with either alfentanil 20 micrograms kg-1 and propofol 2.0-2.5 mg kg-1, or fentanyl 3 micrograms kg-1 and thiopentone 4-6 mg kg-1. Approximately 5 min later, after calibration of mechanomyography, an i.v. bolus of 0.3 mg kg-1 rocuronium was administered. Laryngoscopy and tracheal intubation were attempted when maximum block occurred. Intubation was completed successfully in 39 patients. The passage of the tube was rated good or excellent in 18/20 (alfentanil/propofol group) and 18/19 patients in the other group. The times of onset were 65 s and 69 s, respectively. It is concluded that a 1 x ED90 dose of rocuronium will rapidly provide good or excellent intubation conditions in the majority of cases.

Adolescent↗
PubMed1998

Characterization of the uptake of rocuronium and digoxin in human hepatocytes: carrier specificity and comparison with in vivo data.

Mechanisms of drug transport in the liver have been investigated predominantly in rodents. Most of the in vitro drug research in the liver is performed in liver preparations of animals. The results of such experiments frequently are discussed in relation to anticipated metabolic profiles in man, but these extrapolations are often inappropriate because of large interspecies differences in drug metabolism. In the present study, the mechanisms and specificity of the uptake of the organic cation rocuronium and the cardiac glycoside digoxin were investigated in human hepatocytes and were compared with results obtained in rat hepatocytes. The extraction ratio for the intact liver was calculated from the measured uptake rates of the compounds in the human cells in vitro and compared with published in vivo data. The initial hepatic extraction ratio, calculated from the in vitro uptake data for digoxin and rocuronium, very well reflected the initial extraction ratio for distribution in the liver in vivo in man. Uptake of 100 microM rocuronium was inhibited by 40 microM K-strophantoside (80% inhibition), and although not significantly, by 160 microM procainamide ethobromide, whereas no inhibitory effect was found in the presence of 160 microM taurocholic acid. In a previous study in rat hepatocytes, marked inhibition of digoxin uptake by quinine and only minimal inhibition by the diastereomer quinidine was demonstrated, showing clear stereoselectivity in transport inhibition. Unexpectedly, the uptake of digoxin in human hepatocytes was not inhibited significantly by quinidine or quinine, which indicates clear species differences. This is the first study to investigate the uptake mechanisms of organic cations and cardiac glycosides in human hepatocytes in some detail. The results show that uptake characteristics of drugs found in rats can not be extrapolated directly to humans.

Androstanols↗
PubMed2002

Liquid chromatography/mass spectrometric bioanalysis of a modified gamma-cyclodextrin (Org 25969) and Rocuronium bromide (Org 9426) in guinea pig plasma and urine: its application to determine the plasma pharmacokinetics of Org 25969.

A sensitive and specific liquid chromatography/mass spectrometry (LC/MS) method has been developed and validated for the quantification of the modified gamma-cyclodextrin Org 25969 and Rocuronium bromide (Roc or Org 9426) in the plasma and urine of guinea pigs. The assay was linear and reproducible over the range 25-10000 ng/mL for both compounds. The lowest limit of quantification (LLOQ) for both compounds in urine was 25 ng/mL. In plasma, the LLOQ was 25 ng/mL for Org 9426 and 50 ng/mL for Org 25969. The inter- and intra-day variation was lower than 20%. The physicochemical properties of both compounds imposed different modes of extraction from plasma. The modified gamma-cyclodextrin was extracted by trifluoroacetic acid (TFA) precipitation while Rocuronium was extracted by acetonitrile precipitation. Both compounds were quantified in urine by direct injection onto the column. The LC/MS analyses of Org 25969 and Org 9426 were performed using two different assay conditions. It was not possible to quantify the complex of cyclodextrin and Roc as it dissociated on the LC column. The use of LC/MS conferred great advantage to the quantification of both Org 25969 and Org 9426, as they were not chromogenic enough to afford the sensitivity and specificity required for the assay.

Androstanols↗
PubMed1992

Rocuronium (ORG 9426) neuromuscular blockade at the adductor muscles of the larynx and adductor pollicis in humans.

The effects of rocuronium, 0.25 or 0.5 mg.kg-1, were measured simultaneously on the adductor muscles of the larynx and adductor pollicis in 14 adult patients. Anaesthesia was induced and maintained with propofol and fentanyl. Tracheal intubation was performed without muscle relaxants. The recurrent laryngeal and ulnar nerves were both stimulated supramaximally, at the notch of the thyroid cartilage and at the wrist respectively, using train-of-four stimulation. The laryngeal response was evaluated by measuring the pressure change in the cuff of a tracheal tube positioned between the vocal cords. Onset time, intensity of blockade and duration of action were less at the larynx than at the adductor pollicis. After rocuronium, 0.25 mg.kg-1, the onset time (interval between injection and maximal T1 blockade) was 1.6 +/- 0.1 min and 3.0 +/- 0.3 min (mean +/- SEM) at the laryngeal muscles and adductor pollicis, respectively (P less than 0.01 between muscles). Maximum blockade was 37 +/- 8% and 69 +/- 8%, respectively (P less than 0.05), and time to 90% T1 recovery was 7 +/- 1 min and 20 +/- 4 min, respectively (P less than 0.05). With 0.5 mg.kg-1, the onset time was also more rapid at the vocal cords (1.4 +/- 0.1 min) than at the adductor pollicis (2.4 +/- 0.2 min, P less than 0.001). Maximum blockade was 77 +/- 5% and 98 +/- 1%, respectively (P less than 0.01), and time to 90% T1 recovery was 22 +/- 3 min and 37 +/- 4 min, respectively (P less than 0.01).(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1994

Characterization of transport in isolated human hepatocytes. A study with the bile acid taurocholic acid, the uncharged ouabain and the organic cations vecuronium and rocuronium.

The uptake and efflux of three categories of substrates were measured in isolated human hepatocytes and compared to those in rat hepatocytes. In addition, the extent to which the in vitro experiments quantitatively reflect liver function in vivo in both species was investigated. The anionic bile acid taurocholic acid was taken up by isolated human hepatocytes at a considerably lower rate than observed in isolated rat hepatocytes. Taurocholic acid uptake both in human hepatocytes and in liver plasma membrane vesicles showed sodium dependency. The uptake rate of taurocholic acid in isolated hepatocytes of both species was quantitatively compatible with the reported liver clearance of the bile acid in vivo. Ouabain uptake rate in isolated human hepatocytes was lower than in rat hepatocytes. This species difference was in accordance with pharmacokinetic studies in vivo on hepatic clearance of ouabain in man and rat. Uptake of vecuronium into human hepatocytes was about a factor of 10 lower than that in rat hepatocytes. Uptake into and efflux from human hepatocytes was comparable for the two short acting muscle relaxants vecuronium and rocuronium. Since distribution to the liver is considered to be a major factor in termination of action of vecuronium and rocuronium these observations were in line with the human pharmacokinetic profiles. In conclusion, the uptake rate of the studied model compounds in human hepatocytes appeared to be lower than that in rat hepatocytes. These observed transport rates reflected the relative hepatic transport rates observed in these species in the intact organism, but the absolute values in both species for some substrates may have been somewhat lower than calculated from in vivo data. It is concluded that transport studies in isolated hepatocytes are suitable for comparative drug transport studies, but are less precise in the prediction of quantitative membrane transport.

Androstanols↗
PubMed1995

Pharmacokinetics and pharmacodynamics of rocuronium at the vocal cords and the adductor pollicis in humans.

The pharmacokinetic-pharmacodynamic relationship of rocuronium at the laryngeal adductor muscles and the adductor pollicis was determined in eight patients during general anesthesia. Rocuronium was administered as an infusion at a rate of 100 micrograms.kg-1.min-1 over 5 minutes. The half-life of transport between plasma and biophase (effect compartment) was significantly shorter at the adductor laryngeal muscles (2.7 +/- 0.6 minutes, mean +/- SD) than at the adductor pollicis (4.4 +/- 1.5 minutes, p = 0.003). The concentration in the effect compartment producing 50% of the maximum effect was significantly greater at the adductor laryngeal muscles (1424 +/- 148 micrograms.L-1) than at the adductor pollicis (823 +/- 157 micrograms.L-1, p = 0.0001). The shorter onset of neuromuscular blockade at the laryngeal muscles than at the adductor pollicis may be explained by a faster transfer rate at the laryngeal adductor muscles neuromuscular junction than at the adductor pollicis neuromuscular junction.

Adult↗
PubMed2002

Presynaptic inhibitory effects of rocuronium and SZ1677 on [3H]acetylcholine release from the mouse hemidiaphragm preparation.

It has been shown that nondepolarizing muscle relaxants may have effects on nicotinic acetylcholine receptors (nAChRs) other than those located on the skeletal muscle: some of them possess inhibitory effects on neuronal nAChRs [Anesth. Analg. 59 (1980) 935; Trends Pharmacol. Sci. 9 (1988) 16; Pharmacol. Ther. 73 (1997) 75]. It was shown that, e.g. (+)-tubocurarine and pancuronium are able to inhibit ACh release from the axon terminals of hemidiaphragm preparations and produce tetanic fade indicating their presynaptic effect. In this study rocuronium, a nondepolarizing steroidal muscle relaxant with shorter onset of action, and SZ1677 [1-(3alpha-hydroxy-17beta-acetyloxy)-2beta-(1.4-dioxa-8-azaspiro-[4,5]-dec-8-yl)-(5alpha-androstane-16beta-yl)-1-(2-propenyl) pyrrolidinium bromide], a short-acting muscle relaxant [Ann. New York Acad. Sci. 757 (1995b) 84] inhibited the release of ACh in response to axonal stimulation, while alpha-bungarotoxin failed to reduce the stimulation evoked release of ACh and did not produce tetanic fade. These results indicate that in addition to their postsynaptic effect, rocuronium and SZ1677 have presynaptic inhibitory effects on neuronal nAChRs at the neuromuscular junction. The finding that alpha-bungarotoxin does not inhibit the release and does not produce tetanic fade indicates that it possesses affinity only for the postsynaptic muscle nAChRs.

Acetylcholine↗
PubMed1999

Cardiac effects of non-depolarizing neuromuscular blocking agents pancuronium,vecuronium, and rocuronium in isolated rat atria.

Pancuronium, vecuronium, and rocuronium produce different cardiac effects. Using spontaneously beating right and electrically stimulated left rat atria, while measuring developed force, effective refractory period, and heart rate, we determined and compared the concentration-dependent cardiac effects of the compounds. The preparations were exposed to five progressively increasing concentrations of these compounds (10(-9), 10(-8), 10(-7), 10(-6), and 10(-5) mol/L). Pancuronium increased heart rate; vecuronium and rocuronium produced positive inotropic effects; and vecuronium shortened refractoriness. These effects may be the result of a blockade of the M2 muscarinic receptors. However, the concentrations required to produce changes were higher than those observed in patients under neuromuscular blockade.

Androstanols↗
PubMed2000

The relationship between rate of administration of an intubating dose of rocuronium and time to 50% and 90% block at the adductor pollicis muscle.

OBJECTIVE: To determine the relationship between the rate of rocuronium injection and the onset time of neuromuscular block. METHODS: After intravenous induction, 60 female patients (ASA I-II) were assigned randomly into 3 groups for rocuronium administration within 1-15, 15-30 or 30-60 seconds. Acceleromyography of the thumb was performed using train-of-four (TOF) stimulation. Times to 50% and 90% twitch depression of the first twitch of the TOF stimulation (T1) were recorded. RESULTS: Injection time significantly influences time to 50% relaxation, but not time to 90% relaxation. Body mass index is negatively correlated with time to 50% and 90% relaxation. CONCLUSIONS: We conclude that rate of injection influences only the initial phase of development of the block and that slower injection times do not significantly affect time to 90% relaxation at the adductor pollicis muscle.

Adolescent↗
PubMed2002

Postoperative muscle paralysis after rocuronium: less residual block when acceleromyography is used.

BACKGROUND: Residual muscle paralysis after anesthesia is common after pancuronium, but less common following the intermediate-acting drugs vecuronium and atracurium. Therefore, many anesthetists do not monitor neuromuscular function when using an intermediate-acting agent. The purpose of this prospective, randomised and double-blind study was to establish the incidence and degree of postoperative residual block following the use of rocuronium in patients not monitored with a nerve stimulator, and to compare it with results obtained in patients monitored using acceleromyography (AMG). METHODS: During propofol/opioid anesthesia, 120 adult patients were randomised to two groups, one monitored with AMG, the other using only clinical criteria without a nerve stimulator. Postoperatively, TOF-ratio was measured with mechanomyography; a TOF-ratio < 0.80 indicated residual muscle paralysis. RESULTS: Residual muscle paralysis was found in 10 patients in the group without neuromuscular monitoring (16.7%) (95% confidence interval, 12-21%) and in two patients in the AMG-monitored group (3%) (95% CI, 0-8%); (P = 0.029, Fisher's exact test). Time from end of surgery to tracheal extubation was significantly longer in the AMG-monitored group (12.5 min) than in the group not monitored with AMG (10 min). CONCLUSION: Clinical evaluation of recovery of neuromuscular function does not exclude significant residual paralysis following the intermediate-acting muscle relaxant rocuronium, but the problem of residual block can be minimized by use of AMG.

Adolescent↗
PubMed2002

Resistance to rocuronium in a child with Schwartz-Jampel syndrome type 1 B.

In Schwartz-Jampel syndrome micrognathia and jaw muscle rigidity may result in difficult or impossible tracheal intubation. Since the dose-response relationship to muscle relaxants is unknown in this rare disease we assessed by mechanomyography the neuromuscular response to the rocuronium in a two-year-old child with Schwartz-Jampel syndrome (SJS) Type 1 B. Rocuronium's dose-response curve was markedly shifted (3.5-fold dose) to the right when compared to healthy children and intubation conditions were improved. This resistance to NDMR may result from a lower acetylcholine degradation rate suggested as being the consequence of mutation of the gene encoding perlecan (HSPG2) in SJS. Thus, considerably higher doses of NDMR than usual may be required for facilitation of tracheal intubation in patients with SJS. Since evidence for genetic heterogeneity of SJS exists we also recommend incremental doses of a rapidly acting NDMR with continuous monitoring of neuromuscular function so as to assess the optimum relaxant dose.

Androstanols↗
PubMed1995

Histamine-release haemodynamic changes produced by rocuronium, vecuronium, mivacurium, atracurium and tubocurarine.

We have examined the effects of different benzyl-isoquinolinium and steroidal neuromuscular blocking compounds on plasma concentrations of histamine, heart rate and arterial pressure in surgical patients. A single, rapid (5-s) bolus of mivacurium 0.2 mg kg-1, atracurium 0.6 mg kg-1, tubocurarine 0.5 mg kg-1, vecuronium 0.1 mg kg-1 or rocuronium 0.6 mg kg-1 was administered to 75 patients (n = 15 in each group). Anaesthesia was induced with thiopentone 6 mg kg-1 i.v. and maintained with isoflurane and 70% nitrous oxide in oxygen. Venous blood samples were obtained before induction, 1 min after thiopentone and 1, 3 and 5 min after administration of the neuromuscular blocking drug. Mivacurium, atracurium and tubocurarine caused 370%, 234% and 252% increases in plasma histamine concentrations at 1 min, respectively. Corresponding values at 3 min were 223%, 148% and 157%, respectively. These changes were significant (P < 0.01) at 1 and 3 min. In contrast, the rocuronium and vecuronium groups had no significant changes in either plasma histamine concentrations or haemodynamic variables.

Adolescent↗
PubMed1996

Is recovery of neuromuscular transmission complete after the use of neostigmine to antagonize block produced by rocuronium, vecuronium, atracurium and pancuronium?

To test if recovery of neuromuscular transmission is complete after the use of neostigmine under standardized conditions, we have measured adductor pollicis mechanical activity in response to 0.1 Hz (twitch height), train-of-four (TOF) and 100 Hz (RF 100 Hz) ulnar nerve stimulations. We studied 56 adult anaesthetized (thiopentone, fentanyl, nitrous oxide in oxygen) patients, allocated randomly to one of four groups (n = 14) to receive rocuronium (group Roc), vecuronium (group Vec), atracurium (group Atr) or pancuronium (group Pan). Recovery of neuromuscular transmission was studied for 15 min after neostigmine 40 micrograms kg-1 was given at 25% recovery of twitch height. Fifteen minutes after antagonism, the TOF ratio was 0.91 (SEM 0.01), 0.88 (0.02) and 0.92 (0.01) (ns), and RF 100 Hz was 0.78 (0.01), 0.79 (0.02) and 0.78 (0.01) (ns) respectively, in patients in groups Roc, Vec and Atr, respectively. In patients in group Pan, TOF ratio and RF 100 Hz were only 0.76 (0.01) and 0.33 (0.04) respectively (P < 0.01, one-way analysis of variance, Duncan's multiple classification range tests). In contrast with pancuronium, antagonism of rocuronium-, vecuronium- and atracurium-induced neuromuscular blocks produced a similar high degree of recovery of neuromuscular transmission.

Adult↗
PubMed1997

Neuromuscular effects of rocuronium in patients receiving beta-adrenoreceptor blocking, calcium entry blocking and anticonvulsant drugs.

We have studied the onset and duration of action of rocuronium 0.6 mg kg-1 in patients receiving therapy for more than 1 month with beta-receptor blocking drugs (n = 16), calcium entry blocking drugs (n = 17) or anticonvulsant drugs (n = 14) and compared these data with those from a control group (n = 27). Anaesthesia comprised fentanyl, propofol infusion and nitrous oxide in oxygen. Neuromuscular block was monitored by measuring the force of contraction of the adductor pollicis muscle in response to train-of-four (TOF) stimulation. There were no significant differences in onset times between the four groups (mean 62-76 s). Mean times to 25% recovery of T1 (first response in the TOF) and of the TOF ratio of 0.7 were 38 (SD 15) and 58 (22) min, 36 (8) and 61 (19) min, 40 (11) and 68 (22) min, and 25 (6) and 35 (9) min in the control, beta-blocker, calcium entry blocker and anticonvulsant groups, respectively (P < 0.01 between the anticonvulsant and other groups). We conclude that chronic therapy with anticonvulsant drugs reduces the duration of action of rocuronium.

Adolescent↗
PubMed1997

Pharmacokinetics and pharmacokinetic-dynamic modelling of rocuronium in infants and children.

We have determined the pharmacokinetics and pharmacokinetic-pharmacodynamic relationship of rocuronium in infants and children. We studied infants (n = 5, 0.1-0.8 yr) and children (n = 5, 2.3-8 yr), ASA II, in the ICU while undergoing artificial ventilation under i.v. anaesthesia with an arterial cannula in situ and the EMG of the adductor pollicis muscle was monitored. Rocuronium 0.06 (infants) and 0.09 (children) mg kg-1 min-1 was given i.v. over +/- 5 min until 85% neuromuscular block was obtained. Arterial blood samples were obtained over 240 min. Plasma concentrations were measured by HPLC. Pharmacokinetic-dynamic variables were calculated using the Sheiner model and the Hill equation. Statistical analysis was performed using the Mann-Whitney U test (P < 0.05). The mean administered dose was 0.32 (SD 0.08) mg kg-1 and 0.4 (0.1) mg kg-1 for infants and children, respectively. Infants differed from children in plasma clearance (4.2 (0.4) vs 6.7 (1.1) ml min-1 kg-1), distribution volume at steady state (231 (32) vs 165 (44) ml kg-1), mean residence time (56 (10) vs 26 (9) min), concentration in the effect compartment at 50% block (1.2 (0.4) vs 1.7 (0.4) mg litre-1) and the slope of the concentration-effect relationship (5.7 (1.3) vs 3.9 (0.5)). Calculated mean ED90 values were 0.26 and 0.34 mg kg-1 for infants and children, respectively. The time course of neuromuscular block after equipotent doses did not differ.

Aging↗
PubMed1999

Spontaneous or neostigmine-induced recovery after maintenance of neuromuscular block with Org 9487 (rapacuronium) or rocuronium following an initial dose of Org 9487.

We have examined spontaneous and neostigmine-induced recovery after an initial dose of Org 9487 1.5 mg kg-1 followed by three repeat doses of Org 9487, a 30-min infusion of Org 9487 or two incremental doses of rocuronium. Mean clinical duration after incremental doses of Org 9487 0.5 mg kg-1 increased from 12.3 (SD 3.4) min to 14.0 (4.0) and 15.9 (5.9) min (P < 0.01), and after rocuronium from 14.4 (5.2) min to 19.2 (5.9) min (P < 0.01). Times for spontaneous recovery from a T1 of 25% to a TOF ratio of 0.8 after the last bolus dose of Org 9487 and after a 30-min infusion were 72.4 (16.5) and 66.1 (26.9) min compared with 36.7 (15.8) min in the group receiving reocuronium. These times were significantly reduced to 9.9 (4.5), 8.6 (6.1) and 5.7 (2.5) min, respectively, after neostigmine administration at a T1 of 25% (P < 0.05). We conclude that administration of Org 9487 by repeat bolus doses or infusion was associated with slow spontaneous recovery but neostigmine administration resulted in adequate recovery in less than 10 min.

Androstanols↗