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PubMed1998

Interactions between P-glycoprotein substrates and other cationic drugs at the hepatic excretory level.

1. In the present study it was tested whether known P-glycoprotein (P-gp) substrates/MDR reversal agents interact with small (type 1) and bulky (type 2) cationic drugs at the level of biliary excretion in the rat isolated perfused liver model (IPRL). The studies were performed with model compounds tri-n-butylmethylammonium (TBuMA) (a relatively small type 1 organic cation), rocuronium (Roc) (a bulky type 2 organic cation) and the classical P-gp substrate doxorubicin (Dox). 2. Inhibitors were given in a 4 fold molar excess to the substrate studied. To minimize an interaction of the substrates at the hepatic uptake level, the competing compounds were added when over 55% to 85% of the administered dose of the model compounds had been removed from the perfusate and taken up by the liver. 3. We found a mutual interaction between TBuMA and procainamidethobromide (PAEB), both type 1 cationic compounds during biliary excretion. Interestingly, type 2 compounds, such as rocuronium, clearly inhibited type 1 cationic drugs as well as Dox secretion into bile, whereas type 1 compounds did not significantly inhibit type 2 drug excretion into bile. The type 1 cations PAEB and TBuMA only moderately inhibited Dox biliary excretion. Dox did not inhibit the biliary excretion of the type 2 agent rocuronium whereas rocuronium reduced Dox biliary excretion by 50% compared to controls. 4. MDR substrates/reversal agents like verapamil, quinine, quinidine and vinblastine strongly reduced both type 1 and type 2 organic cation excretion into bile. Dox secretion into bile was also profoundly reduced by these drugs, vinblastine being the most potent inhibitor in general. 5. The lack of mutual inhibition observed in some combinations of substrates may indicate that major differences in affinity of the substrates for a single excretory system exist. Alternatively, multiple organic cation transport systems with separate substrate specificities may be involved in the biliary excretion of amphiphilic drugs. Furthermore, the present study revealed a clear positive correlation between the lipophilicity of the potential inhibitors studied and their respective inhibitory activity on the biliary excretion of the model drugs investigated. 6. Our data are compatible with a potential involvement of P-glycoprotein in the hepatobiliary excretion of doxorubicin as well as of some type 1 and type 2 organic cations. Furthermore we postulate that the hydrophobic properties of the amphiphilic cationic drugs studied play a crucial role in the accommodation of these agents by P-glycoprotein and/or other potential cationic drug carrier proteins in the canalicular membrane.

ATP Binding Cassette Transporter, Subfamily B, Mem↗
PubMed2000

Adenosine potentiation of neuromuscular blocking agents in guinea-pigs.

We have investigated the effects of adenosine i.v. on neuromuscular block induced by rocuronium, vecuronium and pipecuronium in an in vivo guinea-pig sciatic nerve-tibialis anterior preparation. The ED50 of each neuromuscular blocker was determined from cumulative log dose-response regression lines (n = 14). In separate experiments, adenosine 0.1 mg kg-1 min-1 or the same volume of 0.9% NaCl was given i.v. via a constant infusion and the ED50 of each neuromuscular blocking agent was then administered (n = 24). Adenosine 0.1 mg kg-1 min-1 increased significantly maximal block induced by the ED50 of these neuromuscular blockers (55-72%, 49-73% and 60-96%, respectively, for rocuronium, vecuronium and pipecuronium; P < 0.05). Time to maximal block after rocuronium was significantly prolonged by adenosine (1.4-2.1 min; P < 0.05) and time to maximal block after vecuronium and pipecuronium was unchanged by adenosine. Time to maximal recovery of twitch tension after administration of the ED50 of all neuromuscular blocking agents was prolonged significantly by adenosine (4.5-10.7 min, 8.2-15.8 min and 47.0-128.7 min, respectively, for rocuronium, vecuronium and pipecuronium; P < 0.05). We conclude that continuous infusion of adenosine 0.1 mg kg-1 min-1 potentiated the effects of neuromuscular blocking agents in this in vivo guinea-pig preparation.

Adenosine↗
PubMed1999

Assessing neuromuscular block at the larynx: the effect of change in resting cuff pressure and a comparison with video imaging in anesthetized humans.

UNLABELLED: Neuromuscular block (NMB) at the larynx has been assessed by measuring the cuff pressure (CP) in an endotracheal tube (ETT) placed between the vocal cords. In this study, we evaluated the decrease in resting cuff pressure (RCP) after the administration of rocuronium and the effect of this decrease on the assessment of NMB, and we compared CP measurement with an alternative technique, video imaging (VI). In 20 patients, NMB was determined at the hand by mechanomyography and at the larynx initially by CP and subsequently by VI, recording images using a fiberoptic bronchoscope via a laryngeal mask. Train-of-four stimuli were applied at both sites. After baseline measurements, the ETT was replaced, and rocuronium was infused to achieve a steady-state 50% (n = 10) or 75% (n = 10) block at the hand. CP measurements were recorded before and after restoration of RCP to prerocuronium pressure, followed by further VI measurements. The mean RCP decreased from 21 +/- 4 to 12 +/- 5 mm Hg after rocuronium. At 50% block at the hand, the CP estimate of block at the larynx with reduced RCP was 62% +/- 18%, and that after restoring RCP was 29% +/- 13%; VI estimated 27% +/- 14% block. At 75% block at the hand, CP and VI estimated 52% +/- 11% and 46% +/- 9% block, respectively (RCP maintained). We conclude that RCP decreases after the administration of rocuronium, that restoring RCP significantly alters CP estimates of NMB, and that VI is in agreement with CP measurement if RCP is maintained at prerelaxant values. IMPLICATIONS: In this study, we show that a muscle relaxant-induced decrease in resting tension at the larynx may confound the assessment of neuromuscular block by cuff pressure measurement. The preliminary data suggest that video imaging may provide a suitable alternative to cuff pressure measurement to assess neuromuscular block at the larynx.

Adult↗
PubMed1999

The effects of antagonizing residual neuromuscular blockade by neostigmine and glycopyrrolate on nausea and vomiting after ambulatory surgery.

UNLABELLED: The effects of neostigmine on the incidence of postoperative nausea and vomiting (PONV) are controversial. In this study, we evaluated the effects of neostigmine and glycopyrrolate on the incidence of PONV and the need for antiemetics in patients undergoing ambulatory surgery. One hundred healthy patients undergoing outpatient surgical procedures were included in the study. A standardized anesthetic technique was used for all patients. Patients were randomized to receive either mivacurium (n = 50) or rocuronium (n = 50) to achieve muscle paralysis. Bolus doses of mivacurium 2-4 mg or rocuronium 5-10 mg were administered to maintain one or two twitches of the train-of-four stimulation of the ulnar nerve at the wrist. After surgery, residual neuromuscular blockade was reversed with neostigmine 2.5 mg i.v. and glycopyrrolate 0.5 mg i.v. only if clinically deemed necessary (i.e., fade on train-of-four stimulation, inadequate tidal volume, reduced hand grip, or inability to maintain head lift). The incidence of PONV and the need for antiemetics were recorded in the post-anesthesia care unit (PACU), in the phase II unit, and 24 h after surgery. We compared patients who received neostigmine (n = 40) for reversal of residual neuromuscular blockade with those who did not (n = 60). More patients receiving rocuronium required reversal drugs than those receiving mivacurium (68% vs 10%). There were no differences in the incidence of nausea (18% vs 15%), vomiting (8% vs 12%), and the need for antiemetics (13% in both the groups) in the PACU between patients who received neostigmine and those who did not. In addition, the duration of PACU stay and the time to home-readiness were also similar between the groups. We conclude that, compared with rocuronium, the use of mivacurium decreases the need for reversal drugs. In addition, reversal of residual neuromuscular blockade with neostigmine does not increase the incidence of PONV or the need for antiemetic medications in patients undergoing ambulatory surgery. IMPLICATIONS: In this study, we showed that the incidence of postoperative nausea and vomiting and the need for antiemetics do not increase with the use of neostigmine and glycopyrrolate for reversal of residual muscle paralysis.

Adult↗
PubMed1999

The pulmonary first-pass uptake of five nondepolarizing muscle relaxants in the pig.

BACKGROUND: It is not known whether the lungs influence the early pharmacokinetics of muscle relaxants and, if they do, whether differences in pulmonary uptake contribute to the differences in potency and/or onset time among muscle relaxants. Because the lungs are uniquely positioned, receive the entire cardiac output, have a large capillary surface area, and can temporarily store various basic drugs, the authors determined whether substantial pulmonary first-pass uptake of muscle relaxants occurs. METHODS: In 14 pigs, rocuronium, vecuronium, Org 9487, Org 7617, or d-tubocurarine were administered simultaneously with indocyanin green within 1 s into the right ventricle, and then arterial blood was sampled every 1.2 s (in the first min). The tibialis muscle response was registered mechanomyographically. RESULTS: The maximum block was 93% (68-100% [median and range]). Onset times ranged from 83 s (78-86 s) for rocuronium to 182 s (172-192 s) for d-tubocurarine. Fraction-versus-time outflow curves showed that the peak of muscle relaxants and indocyanin green occurred almost simultaneously. Pulmonary first-pass retention was negligible. The retention of muscle relaxants at 95% passage of indocyanin green was -9% (-31 to 18%). The difference in the mean transit time between muscle relaxant and indocyanin green was 1.0 (0.8 to 1.4), 0.2 (-0.8 to 0.3), 0.3 (0.2 to 0.4), 0.5 (0.2 to 1.3), and -2.2 s for rocuronium, vecuronium, Org 9487, Org 7617, and d-tubocurarine, respectively. CONCLUSIONS: There is no substantial pulmonary first-pass uptake of rocuronium, vecuronium, Org 9487, Org 7617, or d-tubocurarine in pigs. Therefore, differences in pulmonary first-pass uptake do not contribute to the differences in potency and/or onset time among muscle relaxants.

Androstanols↗
PubMed2002

Impact of shorter-acting neuromuscular blocking agents on fast-track recovery of the cardiac surgical patient.

BACKGROUND: Residual paralysis associated with the use of long-acting muscle relaxants can delay recovery from anesthesia and surgery. The authors tested the hypothesis that use of shorter-acting neuromuscular blocking agents is associated with reductions in tracheal extubation times and intensive care unit (ICU) length of stay in patients undergoing cardiac surgery with cardiopulmonary bypass. METHODS: One hundred ten patients scheduled for elective coronary artery bypass grafting or single valve surgery were randomized prospectively to receive either pancuronium or rocuronium intraoperatively. Anesthetic management and muscle relaxant maintenance dosing were standardized. In the ICU, the time required to wean ventilatory support, the duration of tracheal intubation, and length of stay were recorded. Subjects were asked to quantify generalized muscle weakness as they awakened in the ICU and again after tracheal extubation. RESULTS: Complete data were collected on 51 patients in the pancuronium group and 52 patients in the rocuronium group. No differences were found between the groups in anesthetic, surgical, or ICU management. Significant increases in the duration of weaning of ventilatory support were observed in patients who received pancuronium (median, 180 min; range, 50-780 min) compared with the rocuronium group (median, 110 min; range, 45-250 min). Tracheal extubation was significantly delayed in the pancuronium group (median, 500 min; range, 240-1,305 min) compared with the rocuronium group (median, 350 min; range, 210-1,140 min). Subjects in the pancuronium group experienced more mild to severe weakness in the ICU. However, the choice of muscle relaxant did not influence ICU length of stay. CONCLUSION: The use of shorter-acting neuromuscular blocking agents in patients undergoing cardiac surgery with cardiopulmonary bypass is associated with reductions in tracheal extubation times and symptoms of residual paresis.

Adult↗
PubMed2004

Muscle weakness after muscle relaxants: an audit of clinical practice.

Residual muscle weakness after general anaesthesia, assessed using handgrip strength, was audited in a teaching hospital. The relationships between residual weakness, the use of muscle relaxants and patient characteristics were examined. Handgrip strength was measured preoperatively, one hour postoperatively and one day postoperatively using a hand dynamometer in 151 patients having general anaesthesia. Forty-nine patients received no muscle relaxant, 34 patients received vecuronium and 68 received rocuronium. Patients were managed by their anaesthetist according to that anaesthetist's clinical choice. All patients who received muscle relaxants received neostigmine. One hour postoperatively, there was a decline in handgrip strength of 16% for the no relaxant group, 24% for vecuronium and 29% for rocuronium. The degree of weakness for the relaxant groups was unrelated to age (P=0.89) but was strongly influenced by the patient's sex. Almost all of the increased weakness with relaxants was found in the female patients. The mean decline in handgrip strength in the male patients who received either vecuronium or rocuronium was similar to that seen when relaxants had not been used (P=0.40). One hour postoperatively, female patients showed a marked decrease in handgrip strength after both vecuronium and rocuronium (32% and 34% respectively, combined P=0.01). These results suggest that in usual clinical practice at our institution, female patients are more likely to have residual weakness after muscle relaxants.

Age Factors↗
PubMed2001

Choice of the muscle relaxant for rapid-sequence induction.

Muscle relaxants are given as part of a rapid-sequence induction to facilitate tracheal intubation. Among all the muscle relaxants available, succinylcholine is the only one with a fast (approximately equal to 1 min) onset and a fast recovery. Therefore it is still the most frequently used muscle relaxant for rapid-sequence induction despite its well-known side-effects. The short duration of action of succinylcholine is, however, no substitute for aggressive airway management in the case of an unexpectedly difficult intubation in order to prevent life-threatening hypoxia. A preoperative assessment of the airway is mandatory in any patient and may indicate the need for using intubation techniques without a muscle relaxant. Rocuronium in large doses (i.e. > or = 1 mg kg-1) is an alternative to succinylcholine in a classical rapid-sequence setting under relatively light anaesthesia. With respect to rapid tracheal intubation, the timing and priming principles offer little advantage over the use of rocuronium in doses of 0.6 mg kg-1 in combination with an appropriate induction technique (i.e. including an opioid) or over the use of larger doses of rocuronium (> or = 1.0 mg kg-1) under relatively light anaesthesia, and may even be potentially harmful. In contrast to rocuronium, the use of rapacuronium in a rapid-sequence setting has been associated with dose-dependent respiratory side-effects that limit its usefulness in doses higher than 1.5 mg kg-1 for this indication.

Androstanols↗
PubMed2001

The new neuromuscular blocking agents: do they offer any advantages?

The pharmacodynamics and pharmacokinetics of the two most recent aminosteroid neuromuscular blocking drugs to become available, rapacuronium bromide (Org 9487) and rocuronium bromide are reviewed. Two new classes of drug with neuromuscular blocking properties, the bis-tetrahydroisoquinolinium chlorofumarates and the tropinyl diester derivatives are introduced. Comparisons between these drugs and mivacurium and cisatracurium are made. Rapacuronium 1.5 mg kg(-1) (ED95 1 mg kg(-1)), produces maximal neuromuscular block in 54 s. Time to recovery of the train-of-four ratio to 0.7 is achieved within 20 min after neostigmiine 0.05 mg kg(-1) given at 2 min. The plasma clearance of rapacuronium is 7-8 ml kg(-1) min(-1). Rapacuronium undergoes hepatic metabolism: no prolongation of effect has been reported after a single bolus or a short infusion in patients with hepatic or renal failure. Org 9488 is the 3-desacetyl metabolite of rapacuronium, which has neuromuscular blocking properties. Its much lower clearance (1.28 ml kg(-1) min(-1)) and plasma equilibration constant (0.105 min(-1)) may limit the prolonged use of rapacuronium. Rocuronium given at 2xED95 produces maximal neuromuscular block in 1 min. Spontaneous recovery of the train-of-four ratio to 0.7 takes over 40 min. Rocuronium has a plasma clearance of 4 ml kg(-1) min(-1). Its pharmacodynamics are altered in hepatic and renal disease. A number of anaphylactoid reactions to rocuronium have been reported recently. The bis-tetrahydroisoquinolinium chlorofumarate GW280430A has an ED95 of 0.19 mg kg(-1). Given at three times this dose, onset of neuromuscular block occurs within 100 s; the duration of block is 8-9 min. Following a 2 h infusion, the recovery index does not seem to be increased. Early studies suggest that this drug has no adverse cardiovascular or respiratory side-effects. The tropinyl diester derivative G-1-64 will produce 80-90% neuromuscular block in less than 2 min using 3xED80. Ninety per cent recovery of the first twitch of the train-of-four occurs after 5-7 min using one ED80. A recovery index of less than 2 min has been reported in rats. All the tropinyl diesters appear to produce vagal block.

Aged↗
PubMed2004

Identification and quantitation of six non-depolarizing neuromuscular blocking agents by LC-MS in biological fluids.

A liquid chromatography-electrospray-mass spectrometry technique for the screening and determination of five non-depolarizing neuromuscular blocking agents (NDBAs), atracurium and its product of degradation/metabolite laudanosine, rocuronium, pancuronium, vecuronium, and mivacurium has been developed using ambenonium as the internal standard (I.S.). Samples were acidified upon reception by adding 20 micro L 0.5M H(2)SO(4) to 500 micro L of biofluid. Sample preparation consisted of simple blood purification and/or protein precipitation using 1 mL I.S. in acetonitrile. Chromatographic separation was carried out on an X-TERRA trade mark column along with a gradient of acetonitrile in 2mM ammonium formate (pH 3). Detection was carried out in the positive selected ion monitoring mode, targeting one quantitation ion and one confirmation ion per compound. The limit of quantitation was 2.5 micro g/L for mivacurium and laudanosine, 5 micro g/L for rocuronium and pancuronium and 10 micro g/L for atracurium and vecuronium in serum (i.e., in the range of, or less than, therapeutic levels). The technique was found to be linear between the respective LOQs and 2000 micro g/L, with correlation coefficients higher than 0.999 in all matrices. Intra- and interday precision and accuracy in serum fulfilled the international criteria. This method was employed for the investigation of a case of suicide by infusion of drugs. Laudanosine, the metabolite or degradation product of both atracurium and cisatracurium, and rocuronium were found in urine and whole blood, at supratherapeutic concentrations in the latter (rocuronium: 1.53 and 2.18 mg/L, laudanosine: 8.86 and 0.31 mg/L, respectively), and even therapeutic concentrations would have been lethal in the absence of respiratory assistance.

Chromatography, High Pressure Liquid↗
PubMed2000

Emergency department use of neuromuscular blocking agents in children.

There is no ideal neuromuscular blocking agent with a rapid onset and ultra-short duration of action with a good safety profile in children. Rocuronium, vecuronium, rapacuronium, and succinylcholine are currently the neuromuscular blocking agents most suitable for children who require RSI in ED settings. Succinylcholine is the only agent with rapid onset and ultra-short duration of action; however, it has many potential side effects, of which some (albeit rare) may be fatal. In select situations, some emergency physicians may decide that the benefits of succinylcholine outweigh the risks; however, others may choose a nondepolarizing agent as their drug of choice for RSI. Rocuronium has an excellent safety profile and a rapid onset of action similar to succinylcholine. Despite a longer duration of action, rocuronium is the preferred agent for RSI in children by many physicians. For EDs that do not have access to rocuronium, vecuronium is frequently the agent of choice for RSI in children. Despite its longer onset of action and recovery, its side effects are minimal when compared to succinylcholine. If further studies confirm the safety profile of rapacuronium, its rapid onset and short duration of action will likely make it the neuromuscular blocking agent of choice for RSI.

Attitude of Health Personnel↗
PubMed2006

Association of oculocardiac reflex and postoperative nausea and vomiting in strabismus surgery in children anesthetized with halothane and nitrous oxide.

BACKGROUND: Postoperative nausea and vomiting (PONV) occurs frequently after strabismus surgery. The controversy still exists regarding the association of PONV and the oculocardiac reflex (OCR). A recent study has proven that rocuronium attenuates OCR. If these two occurrences are dependent, it is expected that with the diminution of OCR, occurrence of PONV will also be reduced. The goal of this randomized, controlled study was to prove an association between OCR and PONV by attenuating OCR with 0.4 mg x kg(-1) of rocuronium and subsequently diminishing PONV if these occurrences are associated. METHODS: A total of 119 ASA 1 children, aged between 3 and 10, undergoing surgery of the medial rectus muscle, were randomly assigned to two groups. In group R (n = 59), 0.4 mg x kg(-1) of rocuronium was administered i.v. before intubation. Group C (controls, n = 60) received no muscle relaxant. The anesthesia was induced and maintained with halothane and N(2)O/O(2) (50/50%). Chi-squared test, Fisher's exact test, t-test, and anova were used for statistical analysis; P-value <0.05 was considered statistically significant. RESULTS: There were no differences between groups regarding patients' characteristics as well as endtidal halothane and duration of surgery and anesthesia. The occurrence of OCR was different between groups (R: 16/59, 27.1%, C: 28/60, 46.7%; P = 0.027), but not the occurrence of PONV (R: 27/59, 45.8%, C: 28/60, 46.7%; P = 0.921). There was an equal number of patients with PONV and bradycardias in both groups (R: 4/27 vs C: 4/28; P = 0.858), whereas there was different, but statistically insignificant distribution of patients (R: 3/27 vs C: 10/28; P = 0.086) with PONV and arrhythmias other than bradycardia. However, simultaneous occurrence of total OCR and PONV in the 24-h period was not different between the two groups (P = 0.964). CONCLUSIONS: Rocuronium (0.4 mg x kg(-1)) attenuates the occurrence of OCR, but with the reduced occurrence of OCR we were not able to attenuate the occurrence of PONV, therefore the association of OCR and PONV in strabismus surgery in children anesthetized with halothane and nitrous oxide remains unclear, and if there is a link between the two, it could be related to arrhythmias and not bradycardia.

Anesthesia↗
PubMed2001

Transcranial Doppler ultrasonography with induction of anesthesia and neuromuscular blockade in surgical patients.

STUDY OBJECTIVES: To evaluate the cerebral vascular effects of cis-atracurium and rocuronium given after thiopental induction of anesthesia. DESIGN: Randomized, single-blinded study. SETTING: University-affiliated hospital. PATIENTS: 39 adult ASA physical status I and II patients undergoing nonintracranial procedures. INTERVENTIONS: Patients received intravenously (IV), either saline placebo, cis-atracurium, or rocuronium after induction of general anesthesia with thiopental sodium. MEASUREMENTS: The right middle cerebral artery was insonated using a pulsed-wave range-gated transcranial Doppler, and data were recorded at preinduction, immediately postinduction, at injection of the study drug, and at 15-second intervals for 3 minutes thereafter. The variables recorded for each subject included the systolic, diastolic, and mean flow velocity, as well as pulsality index, systolic, diastolic, and mean arterial blood pressure (MAP), and end-tidal carbon dioxide concentration. MAIN RESULTS: No significant differences between the groups were present in the postanesthetic induction maximal or minimal mean flow velocity. CONCLUSIONS: cis-Atracurium and rocuronium, administered after thiopental, do not produce clinically relevant changes in cerebral blood flow velocity.

Adolescent↗
PubMed2004

An investigation of non-depolarizing muscle relaxants on embryonic development in cultured rat embryos.

BACKGROUND AND OBJECTIVE: We have investigated the toxic and teratogenic effects of certain non-depolarizing muscle relaxants on embryonic development in cultured rat embryos. METHODS: Rat embryos of 9.5 days were explanted and cultured in vitro for 48 h in rat serum. Whole rat serum was used as a culture medium for the control group while different concentrations of atracurium, cis-atracurium, rocuronium and mivacurium were added to rat serum for the experimental groups. Dose-dependent effects of these agents on embryonic developmental parameters were compared using morphological and biochemical methods. Each embryo was evaluated for the presence of any malformations. RESULTS: When compared to the control embryos, the muscle relaxants significantly decreased all growth and developmental parameters dose dependently with an increase in overall dismorphology. Among these malformations, maxillary deformity was most frequently observed. These effects were observed in much lower doses with atracurium and cis-atracurium compared to those with rocuronium and mivacurium. CONCLUSIONS: Our results suggest that non-depolarizing muscle relaxants cause dose-dependent toxicity on rat embryos at concentrations much greater than those in clinical practice. Although, these agents seems to have a low potential for causing developmental toxicity during organogenesis, because of the lower toxic effects observed with rocuronium and mivacurium, these agents may be preferred when recurrent administrations are necessary for parturients.

Abnormalities, Drug-Induced↗
PubMed1999

Investigation of fading responses induced by non-depolarising muscle relaxants in the evoked EMG of the gastrocnemius muscle of the cat.

BACKGROUND: During partial neuromuscular blockade indirect repetitive nerve stimulation causes fade in the response of the muscle. We studied the intensity of the fade induced by intravenous administration of three steroidal muscle relaxants, and investigated the mechanism of fade by comparing with results obtained during partial blockade with animal toxins and vesamicol. METHODS: In 60 cats, we measured the fade in the compound action potentials of the gastrocnemius muscle evoked by repetitive sciatic nerve stimulation at 100 Hz during partial neuromuscular blockade with rocuronium, vecuronium, pancuronium, alpha-bungarotoxin, mu-conotoxin and vesamicol, respectively. RESULTS: Profound fade was induced by all three non-depolarising muscle relaxants (rocuronium=vecuronium<pancuronium) and by vesamicol, in contrast to alpha-bungarotoxin and mu-conotoxin which induced no fading. CONCLUSION: Our results suggest that non-depolarising muscle relaxant-induced fade is caused by an inhibitory effect on acetylcholine release. Pancuronium seems to have a higher potency of presynaptic inhibition of acetylcholine release than both rocuronium and vecuronium.

Acetylcholine↗
PubMed2001

Postoperative residual block after intermediate-acting neuromuscular blocking drugs.

The frequency and duration of postoperative residual neuromuscular block on arrival of 150 patients in the recovery ward following the use of vecuronium (n = 50), atracurium (n = 50) and rocuronium (n = 50) were recorded. Residual block was defined as a train-of-four ratio of <0.8. An additional group of 10 patients received no neuromuscular blocking drugs during anaesthesia. The incidence of postoperative residual neuromuscular block was 64%, 52% and 39% after the use of vecuronium, atracurium and rocuronium, respectively. Similar numbers of patients were not able to maintain a sustained head or leg lift for 5 s on arrival in the recovery ward. The mean [range] times to attaining a train-of-four ratio of > or =0.8 after arrival in the recovery ward were 9.2 [1-61], 6.9 [1-24] and 14.7 [1.5-83] min for vecuronium, atracurium and rocuronium, respectively. None of the 10 patients who did not receive neuromuscular blocking drugs had train-of-four ratios <0.8 on arrival in the recovery ward. It is concluded that a large proportion of patients arrive in the recovery ward with a train-of-four ratio <0.8, even with the use of intermediate-acting neuromuscular blocking drugs. Although the residual block is relatively short lasting, it may occasionally be prolonged, requiring close observation and monitoring of such patients in the recovery ward.

Adolescent↗
PubMed2000

Economic aspects of different muscle relaxant regimens.

OBJECTIVE: At a time of cost reduction in medical care efforts to manage the ever-increasing costs of new pharmaceutical drugs become increasingly important. Costs of four different muscle relaxant regimens including the new intermediate-acting neuromuscular blocking drugs (NMBD) cisatracurium and rocuronium will be analyzed. METHODS: Eighty patients undergoing laparoscopic cholecystectomy were prospectively studied. All patients received standardized general anaesthesia with desflurane/fentanyl. Muscle relaxation was achieved with atracurium, cisatracurium, vecuronium, or rocuronium with 20 patients in each group. Intraoperatively muscle relaxants were added to maintain two twitches of the train-of-four (TOF) assessment. RESULTS: There were no differences among the four groups regarding biometric data, duration of surgery and anesthesia, number of patients with reversal of neuromuscular blockade, and time of extubation. Length of stay in the postanesthesia care unit (PACU) and the incidence of side effects were similar in all groups. Total costs of used drugs were significantly lowest in the atracurium-treated patients (per patient: 18.27 Euro) and significantly highest in the cisatracurium group (26.71 Euro) compared with the other groups (vecuronium: 22.61 Euro; rocuronium: 22.63 Euro). CONCLUSION: It is summarized that the use of cisatracurium was associated with higher costs compared to a standard muscle relaxant regimen using atracurium, whereas patient outcome was the same in all study groups. The routine use of the newer NMBDs can only be justified economically, if considerable improvements to clinical practice can be demonstrated.

Adult↗
PubMed1996

[New muscle relaxants].

Mivacurium is a short-acting nondepolarising muscle relaxant of the benzylisoquinoline type undergoing rapid breakdown by plasma cholinesterase. With 2.5 fold ED95, tracheal intubation can be accomplished within 2-3 min following injection. The ensuing DUR 25% (i.e. time from injection to 25% recovery of control twitch tension) is three times as long as with succinylcholine and about half as long as with equipotent doses of atracurium and vecuronium. The principal side effects of mivacurium are facial flushing and a transient fall in blood pressure due to a moderate histamine release following doses of 3-4 times the ED95. In patients with end stage liver or renal disease as well as in patients with atypical plasma cholinesterase the duration of action of mivacurium is prolonged. Rocuronium is a steroidal non-depolarising neuromuscular blocking agent chemically related to vecuronium. Compared with the latter, rocuronium is less potent, has a shorter onset of action, and no cumulative effects. Adequate intubating conditions are achieved within 60 to 90 s after i.v. injection of twice the ED95. Its elimination from the blood occurs primarily via liver uptake, while renal elimination is about 10 to 30%. Slight vagolytic effects are reported following injection of 0.6 mg/kg rocuronium, while histamine release is unlikely to occur. Atracurium is a mixture of ten stereoisomers. One of them, cis-atracurium, is five times as potent as the chiral mixture while having a similar pharmacodynamic and kinetic profile. It does not cause significant histamine release or clinically relevant cardiovascular effects at doses up to 8 times the ED95. Laudanosine release seems to be less with cis-atracurium than with atracurium.

Androstanols↗