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At least 829 records · Page 46Linked to original sources
PubMed1984

Effect of a muscle relaxant, chlorphenesin carbamate, on the spinal neurons of rats.

The effects of chlorphenesin carbamate (CPC) and mephenesin on spinal neurons were investigated in spinal rats. CPC (50 mg/kg i.v.) inhibited the mono-(MSR) and poly-synaptic reflex (PSR), the latter being more susceptible than the former to CPC depression. Mephenesin also inhibited MSR and PSR, though the effects were short in duration. CPC had no effect on the dorsal root potential evoked by the stimulation of the dorsal root, while mephenesin reduced the dorsal root-dorsal root reflex. The excitability of motoneuron was reduced by the administration of CPC or mephenesin. The excitability of primary afferent terminal was unchanged by CPC, while it was inhibited by mephenesin. Neither CPC nor mephenesin influenced the field potential evoked by the dorsal root stimulation. Both CPC and mephenesin had no effect on the synaptic recovery. These results suggest that both CPC and mephenesin inhibit the firing of motoneurons by stabilizing the neuronal membrane, while mephenesin additionally suppresses the dorsal root reflex and the excitability of the primary afferent terminal. These inhibitory actions of CPC on spinal activities may contribute, at least partly, to its muscle relaxing action.

Action Potentials↗
PubMed1998

[The relationship between maintenance dose of vecuronium and the recovery time from the muscle relaxation].

We investigated the relationship between maintenance bolus dose of vecuronium bromide (Vb) and the recovery time measured by TOF Guard in patients anesthetized with isoflurane (1.2-2.0%)-N2O-O2 (GOI group, n = 19) and epidural anesthesia (2% mepivacaine) plus isoflurane (0.5%)-N2O-O2 (EPI group, n = 14). In both groups, anesthesia was induced with propofol 2 mg.kg-1 and Vb 0.1 mg.kg-1 and ventilation was controlled to keep end tidal CO2 between 35-40 mmHg. When the muscle relaxation recovered to 25% of train-of four ratio (TOFR), doses of Vb 0.06, 0.04 or 0.02 mg.kg-1 were administered. Recovery time to TOFR 25% at each Vb dose (T 0.06, T 0.04 and T 0.02 respectively) was observed. T 0.02, T 0.04 and T 0.06 in GOI group were 36.7 +/- 3.2, 50.7 +/- 4.3 and 60.7 +/- 5.02 min (mean +/- SE), respectively and those in EPI group were 42.6 +/- 2.53, 52.2 +/- 2.51 and 59.9 +/- 3.22 min, respectively. There were no significant differences in the recovery time between these two groups. In both groups, although the recovery time to TOFR 25% was prolonged significantly in proportion to the increasing doses of Vb, the increase did not correlate with the dose of Vb. We suggest that frequent administration of Vb 0.02 mg.kg-1 decreases the total amount of Vb to keep TOFR within 25%.

Aged↗
PubMed1985

[Interaction of the calcium antagonists nifedipine and nisoldipine with the nondepolarizing muscle relaxant vecuronium bromide in an vivo rat preparation].

The interaction of two orally administered Ca-channel blockers, the dihydropyridines nisoldipine and nifedipine, with the non-depolarizing muscle relaxant, vecuronium bromide, was tested in the indirectly stimulated tibialis anterior muscle of anesthetized and ventilated Sprague-Dawley rats. In both the nisoldipine and the nifedipine group, depression of twitch tension and duration of vecuronium-induced neuromuscular blockade was potentiated when compared with a control group. The possible clinical relevance of these findings is discussed.

Animals↗
PubMed1987

Activity of some benzodiazepine receptor ligands with reduced sedative and muscle relaxant properties on stress-induced electrocorticogram arousal in sleeping rats.

Arousal of the electrocorticogram induced by intermittent footshocks in sleeping rats was originally developed to detect hypnotic compounds. A modified shortened protocol is described in which a 2.5-hr nonstressed control period is followed by drug or vehicle administration and a further 5.5-hr recording of the electrocorticogram in the presence of intermittent footshock. The arousal induced by the footshock is reversed by the benzodiazepine chlordiazepoxide and by agents that displace brain benzodiazepine binding but that do not possess the muscle relaxant and sedative properties of benzodiazepines (CL218872, premazepam, ZK91296, RU 43028, and CGS9896). Nonstressed arousal during normal waking was reduced to only a small extent by chlordiazepoxide or any of the other agents tested, suggesting that the footshock-induced arousal is sensitive to the anxiolytic properties of such agents.

Animals↗
PubMed1975

The effect of carbon dioxide on the neuromuscular and haemodunamic effects of AH 8265, a new non-depolarizing muscle relaxant.

The influence of carbon dioxide on the neuromuscular and haemodynamic effects of AH 8165, a new non-depolarizing muscle relaxant, was determined in nine healthy patients before the onset of minor elective surgery. Five patients (hypocapnic, group I) were maintained at an arterial Pco2 ranging from 25 to 31 mm Hg; four patients (hypercapnic, group II) at a Cco2 from 54 to 57 mm Hg. AH 8165 0.25 MG/KG (one-quarter of the dose required for intubation) was given by rapid central venous injection. Haemodynamic responses were similar in the two groups; there were increases in heart rate ranging from 45 to 60 per cent, increases in mean arterial pressure of 17 - 20 percent, and increases in cardiac output of 22-32 per cent. The intensity of neuromuscular blockade of the forearm muscles after AH 8165 was similar in the two groups, and there was no significant difference in recovery rates; group I patients were 80 percent recovered in 36.6 min. group II patients in 47.3 min. It was concluded that the activity of AH 8165 was not influenced by moderate changes in respiratory acid base status.

Acid-Base Equilibrium↗
PubMed1987

Dissociation between calcium influx blockage and smooth muscle relaxation by nifedipine in spontaneously hypertensive rats.

Aortic smooth muscle isolated from spontaneously hypertensive rats (SHR) and normotensive, age-matched Wistar Kyoto rats (WKY) was precontracted by potassium chloride. The relaxant effect of nifedipine (NIF) was much more pronounced in SHR than in WKY, while the relaxation produced by nitroglycerin (NTG) was similar in both tissues. EC50s were (in - log [M]) NIF:SHR 13.1 +/- 0.4 and WKY 9.4 +/- 0.2 (p less than 0.05); NTG:SHR 7.35 +/- 0.3 and WKY 7.26 +/- 0.18 (NS). Aortas from SHR were less sensitive to the contractile effect of Ca2+ than their WKY controls (EC50 was 3.18 +/- 0.03 in WKY and 2.76 +/- 0.13 in SHR, p less than 0.05). The relaxant effect of NIF was dissociated from its effect on Ca2+ influx in SHR aortas. NIF 10(-10) M relaxed the muscle by 100% without producing Ca2+ influx blockage, and NIF 10(-9) and 10(-8) M induced Ca2+ influx blockage while the muscle continued in the relaxed state. Chemically skinned aortic fibers from SHR were less sensitive to the contractile effect of Ca2+ than their normotensive (NR) controls (pCa for EC50 was 5.91 +/- 0.05 in SHR and 6.20 +/- 0.03 in NR, p less than 0.05). NIF 10(-10) M depressed the contractile response to Ca2+ significantly more in SHR than in NR skinned fibers (pCa for EC50 for 5.62 +/- 0.09 in SHR and 6.07 +/- 0.07 in NR, p less than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)

Animals↗
PubMed1985

[Addition of muscle relaxants to intravenous regional anesthesia].

Nine volunteers received two intravenous regional anaesthetics in the right arm. The first anaesthetic was performed with plain 0.25% lignocaine (dose 1 ml/kg body weight), the second with the same volume of lignocaine, with the addition of 0.5 mg pancuronium-Bromide. Latency for onset of the following was measured in both groups: 1. analgesia, 2. cold sensation, 3. warm sensation, 4. touch, 5. motor blockade. As expected, the addition of pancuronium had no influence on sensory blockade, however, motor block was significantly stronger, faster in onset, and longer in duration. Significant systemic side effects after pancuronium were not observed. No pancuronium was found in flame photometry plasma studies. On the basis of these investigations, one can recommend, for I.V.R.A., a relatively large volume of dilute local anaesthetic solution and, to achieve better muscle relaxation, the addition of 0.5 mg of pancuronium.

Adult↗
PubMedDate not supplied

Reduced duration of muscle relaxation with rocuronium in a normocalcemic hyperparathyroid patient.

PURPOSE: To report a case of reduced duration of action of rocuronium in a patient with normocalcemic hyperparathyroidism (HPT). CLINICAL FEATURES: A 56-yr-old patient with primary HPT, who had had surgical resection of three and a half parathyroid glands nine months previously, was referred to our institution for further investigation of a persistent increase in parathyroid hormone. Preoperatively, the patient had a normal serum ionized and total calcium. The patient was diagnosed with a persistent parathyroid adenoma and was scheduled for an elective parathyroidectomy. General anesthesia was induced with iv propofol, fentanyl and succinylcholine. Intraoperatively, anesthesia was maintained with nitrous oxide in oxygen, and isoflurane. Neuromuscular blockade was attained using incremental doses of rocuronium. The average duration of 0.15 mg x kg(-1) incremental doses of rocuronium was 5.9 min (expected: 13-18 min), and that of 0.2 mg x kg(-1) was ten minutes (expected: 19-23 min). CONCLUSION: Primary HPT even in the absence of hypercalcemia may result in resistance to competitive blockade by rocuronium. It suggests that primary HPT may cause acetylcholine receptor up-regulation resulting in hyposensitivity to non-depolarizing muscle relaxants.

Androstanols↗
PubMed2002

Dissociation of human thalamic and cortical SEP gating as revealed by intrathalamic recordings under muscle relaxation.

'Gating' refers to a reduction of cortical somatosensory evoked potentials (SEP) under multiple simultaneous afferent inputs. This study used the opportunity for intrathalamic recordings in patients with movement disorders to clarify to what extent cortical SEP gating is preceded by thalamic gating. Recordings were performed in 10 patients, narcotised by intravenous propofol when receiving implantation of a therapeutic deep brain stimulator system. SEP were elicited by an 8.1-Hz median nerve stimulation at twice motor threshold and were recorded simultaneously from both intrathalamic and scalp electrodes before and after the application of the depolarising muscle blocker succinylcholine which eliminated both the background muscular tone and the repetitive muscle twitches caused by the median nerve stimulation. Peripheral compound action potentials recorded at the upper arm remained unchanged after complete muscle relaxation, proving a continuously effective nerve stimulation. In contrast, the primary cortical SEP component (N20) was significantly increased under succinylcholine (+17%). This cortical release from gating was not paralleled, however, by an increased thalamic response; rather, the primary thalamic response (P16) showed a slight (-9%) but highly significant amplitude reduction. As the recordings were performed in narcotised patients, any potentially variable attentional bias on part of the subjects can be excluded as confounding factor when comparing the two experimental conditions with vs. without reafferent somatosensory inflow. Thus, given the high signal-to-noise ratio of intrathalamically recorded SEP, the present study shows a distinct thalamo-cortical dissociation with the primary somatosensory cortex representing the predominant level exhibiting SEP gating.

Action Potentials↗
PubMed1982

Effects of various catecholamine receptor antagonists, muscle relaxation and physical hindrance on shuttlebox self-stimulation.

Certain drugs, particularly clozapine and clonidine, have been reported to increase selectively the latency to initiate brain stimulation (the ON latency) in a shuttlebox test of self-stimulation, suggesting a preferential attenuation of the "reward" component. The pharmacological selectivity of this reported effect was systematically evaluated. At doses that blocked bar-pressing self-stimulation, metoclopramide (3 mg/kg), prazosin (3 mg/kg) clonidine (0.1mg/kg), clozapine (3 mg/kg)and haloperidol (0.3 mg/kg), all elevated the ON latency to a greater extent than the OFF latency. Methocarbamol (200 mg/kg), and a muscle relaxant, also elevated the ON latency preferentially but the magnitude of this preferential effect was smaller than that produced by the other drugs. A hurdle in the center of the shuttlebox increased the ON and OFF latencies nonselectively. The shuttlebox procedure does not clearly discriminate among various substances that interfere with noradrenergic or dopaminergic neurotransmission, but the common profile produced by the these substances is distinguishable to some degree from simple motor disruption.

Adrenergic alpha-Antagonists↗
PubMed2000

Use of the intubating laryngeal mask airway: are muscle relaxants necessary?

BACKGROUND: The intubating laryngeal mask airway (ILMA) is designed to facilitate blind tracheal intubation. The effect of a muscle relaxant on the ability to perform tracheal intubation through the ILMA device has not been previously evaluated. This randomized, double-blind, placebo-controlled study was designed to evaluate rocuronium, 0.2 or 0.4 mg/kg administered intravenously, on the success rate and incidence of complications associated with ILMA-assisted tracheal intubation. METHODS: A total of 75 healthy patients were induced with propofol 2 mg/kg and fentanyl 1 microg/kg intravenously. After insertion of the ILMA device, patients were administered either saline, rocuronium 0.2 mg/kg, or rocuronium 0.4 mg/kg in a total volume of 5 ml. At 90 s after administration of the study drug, tracheal intubation was attempted using a disposable polyvinyl tube. If unsuccessful, a reusable silicone tube was tried. In addition to recording the time and number of attempts required to secure the airway, the incidence of complications during placement of the tracheal tube and removal of the ILMA were noted. RESULTS: Tracheal intubation was successful in 76-96% of the patients. The overall success rates and times required to secure the airway were similar in all three treatment groups. The high-dose rocuronium group experienced less patient movement (8 vs. 28 and 48%) and coughing (12 vs. 20 and 52%) than the low-dose rocuronium and saline groups, respectively. Use of rocuronium was also associated with a dose-related decrease in the requirement for supplemental bolus doses of propofol during intubation and removal of the ILMA device. CONCLUSIONS: Use of rocuronium did not significantly improve the success rate in performing tracheal intubation through the ILMA. However, it produced dose-related decreases in coughing and movement after tracheal intubation and reduced difficulties associated with removal of the ILMA device.

Adult↗
PubMed1995

Allometry of pharmacokinetics and pharmacodynamics of the muscle relaxant metocurine in mammals.

We investigated the effects of body size on the pharmacokinetics and pharmacodynamics of the renally cleared muscle relaxant metocurine. We hypothesized that pharmacokinetics of the drug would change allometrically in proportion to physiological time [infinity Mb0.25, where Mb is body mass] and that pharmacodynamics would be independent of size because of the highly conserved structure of the acetylcholine receptor. Metocurine effects during general anesthesia were examined in 17 rats, 8 cats, 6 dogs, 5 pigs, 7 sheep, and 12 horses. Allometric analysis demonstrated size dependence for pharmacokinetics, which were affected by physiological time (Mb0.25). Pharmacodynamics were size independent, except for the value for effect compartment concentration associated with 50% twitch paralysis (IC50). Data from individual species had a bimodal distribution that was significant: pigs and sheep were more sensitive than other large species, and their IC50 appeared size independent. IC50 was size dependent in more active species (horse, dog, cat, rat). Although the mechanism is unknown, we speculate that this trend might relate to receptor density within the end plate. Thus pharmacokinetics changed in proportion to physiological time, and pharmacodynamics were in part size independent.

Anesthesia, General↗
PubMed1991

[Determinations of steroidal muscle relaxants and their metabolites].

Pancuronium, vecuronium and pipecuronium are quaternary ammonium steroidal neuromuscular blocking agents. These drugs are typical nondepolarizing muscle relaxants. The steroidal compounds and/or their metabolites have been determined using mass spectrometry or gas chromatography. In this review, these analytical methods and application of the methods to pharmacokinetics are introduced.

Androstane-3,17-diol↗
PubMed1980

The effect of the steroid muscle relaxant pipecurium bromide on the acetylcholinesterase activity of red blood cells in vitro.

The acetylcholinesterase (AchE) inhibitory effect of a muscle relaxant 2 beta,16 beta-bis-(4'-dimethyl-1'-piperazino)-3 alpha,17 beta-diacetoxy-5 alpha-androstane dibromide (pipecurium bromide, RGH-1106, Arduan), was studied in vitro. The inhibition of AchE activity of human red blood cells, expressed as pI50, was 3.99, whereas that of serum cholinesterase (ChE) was 4.33. The AchE inhibitor action was reversible. The inhibition was not influenced by the combined administration of promethazine or atropine. The combined effect of pipecurium bromide and of some other diamino-azasteroid agent proved to be additive. Pipecurium bromide showed mixed-type inhibitory effect both on AchE and ChE.

Acetylcholinesterase↗