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PubMed1987

Combined effects of succinylcholine and calcium on membrane-bound acetylcholinesterase activity.

The effects of succinylcholine and calcium (Ca2+), alone and together, on membrane-bound acetylcholinesterase ("true-type" cholinesterase) were examined using human erythrocyte ghosts to elucidate the combined pharmacological activity of succinylcholine and calcium in in vivo system. Succinylcholine inhibited the acetylcholinesterase by a mixed style. Calcium alone exhibited an inhibitory effect on the enzyme, but a biphasic effect together with succinylcholine: marked restoration of the enzyme activity at calcium concentrations lower than 6 mM and depression at its higher concentrations. It is suggested that calcium induces a conformational change of the enzyme protein leading to the altered binding capacity of succinylcholine. In anesthetic practice, therefore, the use of calcium may not be indicated for the treatment of SCh phase II block.

Journal Article↗
PubMed1983

Succinylcholine apnoea: attempted reversal with anticholinesterases.

Anticholinesterases were administered in an attempt to antagonize prolonged neuromuscular blockade following the administration of succinylcholine in a patient later found to be homozygous for atypical plasma cholinesterase. Edrophonium 10 mg, given 74 min after succinylcholine, when train-of-four stimulation was characteristic of phase II block, produced partial antagonism which was not sustained. Repeated doses of edrophonium to 70 mg and neostigmine to 2.5 mg did not antagonize or augment the block. Spontaneous respiration recommenced 200 min after succinylcholine administration. It is concluded that anticholinesterases are only partially effective in restoring neuromuscular function in succinylcholine apnoea despite muscle twitch activity typical of phase II block.

Adult↗
PubMed1983

Neuromuscular blockade in infants following intramuscular succinylcholine in two or five per cent concentration.

This study determined the characteristics of the neuromuscular block which followed intramuscular succinylcholine 4 mg . kg-1 in 20 infants during halothane anaesthesia. The infants were divided into two groups of ten; the first received succinylcholine in two percent solution and the second in five per cent solution. The mean maximum depression of the first twitch of the train-of-four (T1) was 89.7 +/- 5.0 per cent in 4.0 +/- 0.6 min, and the mean full recovery of T1 occurred in 15.6 +/- 0.9 min after injection. The maximum block achieved and the onset and recovery times were not affected by the concentration used. Depolarizing block, with equal depression of all twitches of the train-of-four was observed during the onset of neuromuscular blockade. During recovery, phase II block, as determined by a train-of-four ratio (T4/T1) of 0.5 or less, occurred frequently at T1 recovery of 25-50 per cent, but was not associated with prolonged paralysis. It is concluded that the onset time of 4 min for intramuscular succinylcholine 4 mg . kg-1 may be too long for emergency use in infants, and no improvement is obtained by increasing the concentration of injected succinylcholine from two to five per cent.

Adjuvants, Anesthesia↗
PubMed1983

ORG NC45 for short intra-abdominal operations: a comparison with succinylcholine.

ORG NC45 was compared with succinylcholine to produce muscle relaxation for short, intra-abdominal operations in 40 patients during nitrous oxide-oxygen-enflurane anaesthesia. Intubating conditions after ORG NC45, 100 micrograms/kg, were similar to those after succinylcholine 1 mg/kg, although this was achieved at a mean time of 229.9 +/- 10.8 sec compared with 129.8 +/- 14.2 sec after succinylcholine. Muscle relaxation during surgery, mean duration 32.5 minutes, was provided in the succinylcholine group with an infusion and in the ORG NC45 group by repeated boluses, 10 micrograms/kg, which were required in four patients. At the end of surgery ORG NC45 was antagonized with atropine, 17 micrograms/kg, and neostigmine, 36 micrograms/kg, which were repeated in two patients. Postoperative recovery of neuromuscular function was indistinguishable between the two groups. We conclude that ORG NC45 is a suitable relaxant for short, intra-abdominal operations if sufficient time, three to four minutes, is allowed to produce good intubating conditions.

Adult↗
PubMed1994

Succinylcholine and vecuronium blockade of the diaphragm, laryngeal and limb muscles in the anaesthetized goat.

The purpose of the study was to compare the response of the cricoarytenoideus dorsalis muscle (CD) to neuromuscular blocking drugs with those of the thyroarytenoideus (TA), diaphragm (DI) and ulnaris lateralis (UL) muscles. Evoked electromyographic response to indirect supramaximal stimulation at 1 Hz was monitored in ten adult goats under thiopentone-halothane anaesthesia. The onset time and duration of neuromuscular blockade after intravenous administration of 500 micrograms.kg-1 of succinylcholine or 4 micrograms.kg-1 of vecuronium were determined. Times to 100% paralysis in CD, TA, DI and UL after succinylcholine were (mean +/- SD) 39 +/- 11, 39 +/- 11, 42 +/- 8 and 57 +/- 8 seconds, respectively; the corresponding times for vecuronium were 5.6 +/- 2.3, 4.6 +/- 1.7, 6.0 +/- 1.9 and 9.6 +/- 1.7 min. The order of recovery to 25% spontaneous EMG activity was TA, CD, DI and UL after succinylcholine (durations: 9.7 +/- 3.6, 11.0 +/- 3.0, 15.3 +/- 1.3 and 22.0 +/- 1.2 min, respectively) but DI, CD, TA and UL after vecuronium (durations: 31.9 +/- 18.6, 35.2 +/- 19.5, 47.1 +/- 19.9 and 71.7 +/- 16.1 minutes, respectively). Thus, as in the diaphragm and thyroarytenoideus muscles, onset time and duration of succinylcholine or vecuronium blockade were shorter in the abductor muscle of the glottis, cricoarytenoideus dorsalis, than in the limb muscle.

Action Potentials↗
PubMed1988

Myalgia in outpatient surgery: comparison of atracurium and succinylcholine.

We studied 60 outpatients randomly divided into two groups. Anesthesia was induced with fentanyl 1.5 micrograms.kg-1 plus thiopentone 5-7 mg.kg-1. Patients in Group I were intubated with the aid of succinylcholine 1.5 mg.kg-1 after pre-treatment with d-tubocurarine 0.05 mg.kg-1. Group II received atracurium 350 micrograms.kg-1 three minutes after a priming dose of 50 micrograms.kg-1. Anesthesia was maintained with isoflurane 1-2 per cent in a mixture of nitrous oxide 60 per cent and oxygen 40 per cent. No supplemental doses of fentanyl or atracurium were given. Intubation conditions were satisfactory for all patients in both groups. There was no significant difference in intubation score between the two groups. The incidence of myalgia was 76 per cent in the succinylcholine group compared to 23 per cent in the atracurium group (p less than 0.005). Fifty per cent of the patients in the succinylcholine group had myalgia necessitating bed rest or analgesics compared to 23 per cent in the atracurium group (p less than 0.05). We conclude that atracurium is a suitable neuromuscular relaxant for outpatient surgery and that myalgia is a major morbidity factor in this population that can be reduced by the use of atracurium instead of succinylcholine.

Adolescent↗
PubMed1986

Shortened action of succinylcholine in individuals with cholinesterase C5 isozyme.

To test the possibility that individuals with and without plasma cholinesterase C5 isozyme have differences in neuromuscular sensitivity to succinylcholine chloride, we examined the effects of succinylcholine in these two groups of patients. Sera from 491 adult patients were examined for presence of the plasma cholinesterase C5 isozyme by use of electrophoresis with polyacrylamide; 24 were positive for the C5 isozyme. Plasma cholinesterase activity and duration of action of succinylcholine were measured in 12 C5 positive patients and 18 C5 negative patients, all of whom had the normal cholinesterase genotype. C5 positive patients had 30.1 per cent higher mean plasma cholinesterase activity than C5 negative patients. The duration of neuromuscular blockade, measured by the first twitch height evoked by train-of-four stimulation, was significantly shorter in C5 positive patients than C5 negative patients. The C5 positive individuals had shorter duration of action of succinylcholine than C5 negative individuals.

Adult↗
PubMed1986

Serum potassium following succinylcholine in patients with brain tumours.

Serum potassium levels were measured in 15 patients with brain tumours between 3-7 cm diameter, during thiopentone/70 per cent N2O in O2 anaesthesia, with mask ventilation controlled to maintain a constant end-tidal CO2 concentration. Potassium levels were determined one minute before and one and ten minutes after administration of succinylcholine 1.0 mg X kg-1 IV. No statistically significant increase in serum potassium occurred following succinylcholine, nor were there any ECG changes associated with succinylcholine administration. Use of succinylcholine in patients with brain tumours does not appear to cause elevation of serum potassium levels or ECG changes.

Adult↗
PubMed1995

Speed and ease of tracheal intubation: priming with mivacurium compared with succinylcholine.

This study examined the efficacy of mivacurium priming (0.015 mg.kg-1) with five minutes between the priming and intubating doses by comparing the effects of one, two and three times the ED95 dose (0.075 mg.kg-1) of mivacurium after priming (Groups 1, 2 and 3, respectively), with a saline prime and 2 x ED95 mivacurium (Group 4) or 1 mg.kg-1 dose of succinylcholine (Group 5). The time from the intubating dose injection to intubation was measured and intubating conditions were rated on a five-point scale with 4 being optimal and 0 being failure. Mean times (+/- SEM) in seconds between the administration of the intubating dose and tracheal intubation were: 106.4 +/- 5.1, 89.6 +/- 6.7, 81.9 +/- 2.7, 169.9 +/- 7.8 and 82.9 +/- 3.5 for Groups 1-5 respectively. The times for Group 2 (2 x ED95 with priming), Group 3 (3 x ED95 with priming) and Group 5 (succinylcholine with saline) were shorter than the times of Groups 1 (1 x ED95 with priming) and 4 (2 x ED95 with saline) P < 0.05. Mean intubating condition scores (+/- SD) for the five groups respectively were 3.1 +/- 0.6, 3.4 +/- 0.6, 3.5 +/- 0.5, 3.2 +/- 0.6 and 3.8 +/- 0.4. Scores for Groups 2, 3 and 5 were higher than those of Group 1 (P < 0.05). The data demonstrated that (1) priming with mivacurium shortens the intubation time and is accompanied by good intubating conditions with doses 2x and 3x ED95, and (2) intubating times and conditions similar to those achieved with succinylcholine can be obtained using mivacurium 2x (total dose 0.150 mg.kg-1) or 3 x ED95 (total dose 0.215 mg.kg-1) with a five-minute priming interval. Priming provides an alternative technique in those clinical circumstances where succinylcholine is contraindicated.

Adult↗
PubMed1987

Decreasing post-succinylcholine myalgia in outpatients.

The effectiveness of four pretreatment regimens in decreasing succinylcholine-induced myalgias was studied in healthy outpatients undergoing general anaesthesia for ambulatory surgery. Four hundred and forty adult females were randomly assigned to one of four pretreatment groups. Three hundred and ninety-five patients completed the study. One of the following pretreatments was given prior to injection of 1.5 mg X kg-1 of succinylcholine: normal saline IV three minutes and again immediately prior to succinylcholine; 0.06 mg X kg-1 d-tubo-curarine (dTc) IV three minutes prior and normal saline IV immediately prior; normal saline IV three minutes prior and 1.5 mg X kg-1 lidocaine IV immediately prior; 0.06 mg X kg-1 dTc IV three minutes prior and 1.5 mg X kg-1 lidocaine IV immediately prior. Fasciculations after injection of succinylcholine were observed and recorded. Patients were contacted by telephone 40-48 hours postoperatively and questioned about the presence of muscle pains. These pains, if present, were graded either mild or moderate to severe. The patients in the two dTc-containing groups exhibited less fasciculations than patients in the other two experimental groups. The dTc-lidocaine group had a lower incidence of moderate to severe fasciculations than in any of the other three groups. Patients in the dTc, lidocaine, and dTc-lidocaine experimental groups reported a higher incidence of absence of muscle pain and a lower incidence of moderate-severe pain than did patients in the saline group. The dTc-lidocaine group had more patients without myalgia and less patients with moderate to severe myalgias than any of the other groups.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1987

Comparison of atracurium and succinylcholine for electroconvulsive therapy in a patient with atypical plasma cholinesterase.

Succinylcholine 2-5 mg or atracurium 10-15 mg were given on five separate occasions to a 24-year-old, 64 kg woman homozygous for atypical plasma cholinesterase who was undergoing electroconvulsive therapy (ECT). Atracurium blockade was reversed with atropine, 0.6 mg and edrophonium, 35 mg. Train-of-four stimulation was applied to the ulnar nerve and the force of contraction of the adductor pollicis muscle was recorded. Doses producing 90 per cent first twitch blockade were 2.5 and 15 mg for succinylcholine and atracurium respectively. The onset of action was 6 min for both relaxants, and time to 90 per cent first twitch recovery was 20 min for succinylcholine and 16 min for the atracurium-edrophonium combination. It is concluded that the use of atracurium in these patients does not offer marked advantages over small doses of succinylcholine.

Adult↗
PubMed1999

Onset of neuromuscular block at the masseter and adductor pollicis muscles following rocuronium or succinylcholine.

PURPOSE: To compare the onset time of two different rocuronium doses (0.6 and 0.9 mg x kg(-1)) and succinylcholine (1.5 mg x kg(-1), preceeded by 0.06 mg x kg(-1) rocuronium) at the masseter and the adductor pollicis muscle. METHODS: In a randomized study, 60 ASA I or II adult women, 18-65 yr of age, were anesthetized with propofol and fentanyl and nitrous oxide in oxygen. Neuromuscular monitoring was performed using acceleromyography simultaneously on the masseter and adductor pollicis. Onset time was measured at both muscles using supramaximal 0.1 Hz single twitch stimulation (square-wave pulse 0.2 msec duration). RESULTS: In all patients, complete neuromuscular block occurred at the masseter and adductor pollicis muscles. Lag-time and onset time were faster at the masseter that at the adductor pollicis muscle in both rocuronium-groups (P < 0.01) and in the succinylcholine-group (P < 0.01). Furthermore, onset time was more rapid after 0.9 mg x kg(-1) rocuronium (65 +/- 7 s) than after succinylcholine (83 +/- 19 sec) at the AP (P < 0.05), but did not differ at the masseter (33 +/- 6 vs 36 +/- 7 sec). CONCLUSIONS: Following rocuronium and succinylcholine, onset time is faster at the masseter than at the adductor pollicis muscle.

Adolescent↗
PubMed2002

[Plasma cholinesterase variations as a result of prolonged neuromuscular blockade. Review and problems encountered in two cases of prolonged neuromuscular blockade after muscle relaxation with succinylcholine as compared to mivacurium].

Succinylcholine and mivacurium are degraded more slowly in patients with a qualitatively or quantitatively reduced plasma cholinesterase and are therefore known for inducing a prolonged postoperative apnea. Perioperative laboratory screening even including plasma cholinesterase activity testing will not prevent this due to a possible aberration only in the qualitative cholinesterase activity. This is illustrated by introducing two cases reports of prolonged apnea after administration of mivacurium or succinylcholine. The pathophysiology of plasma cholinesterase is reviewed including genetically determined variants and the degradation pathways of mivacurium and succinylcholine. Only extensive laboratory chemical tests are sufficient to prevent this possible complication. Due to the rare incidence there is no evidence for recommending these laboratory investigations in all patients. Once prolonged apnea occurs following the administration of mivacurium or succinylcholine the best choice is ongoing ventilation combined with a sufficient sedation.

Apnea↗
PubMedDate not supplied

Comparative effects of (+)- and (-)-isomers of propranolol and INPEA on (+)-tubocurarine- and succinylcholine-induced neuromuscular blockade.

The effects of the (+)- and (-)-isomers of propranolol and INPEA on the neuromuscular blocking action of (+)-tubocurarine and succinylcholine were studied in the tibialis anterior-peroneal nerve preparation of the rabbit and the isolated phrenic nerve-diaphragm preparation of the rat. (+)-Tubocurarine-induced neuromuscular blockade was intensified by (+)- and (-)-isomers of INPEA whereas it was unaffected by isomers of propranolol in both preparations. In the rabbit tibialis anterior-peroneal nerve preparation, only the (-)-isomers of propranolol and INPEA increased the duration of succinylcholine-induced neuromuscular blockade without affecting its magnitude. Higher doses of both (+)- and (-)-isomers of propranolol and INPEA potentiated succinylcholine-induced blockade in the rat phrenic nerve-diaphragm preparation. The results obtained indicate that only the increase in duration of succinylcholine-induced blockade with beta-adrenoceptor blockers can be related to beta-blocking property of these compounds.

Animals↗
PubMed1990

Genetic variants of human serum cholinesterase influence metabolism of the muscle relaxant succinylcholine.

People with genetic variants of cholinesterase respond abnormally to succinylcholine, experiencing substantial prolongation of muscle paralysis with apnea rather than the usual 2-6 min. The structure of usual cholinesterase has been determined including the complete amino acid and nucleotide sequence. This has allowed identification of altered amino acids and nucleotides. The variant most frequently found in patients who respond abnormally to succinylcholine is atypical cholinesterase, which occurs in homozygous form in 1 out of 3500 Caucasians. Atypical cholinesterase has a single substitution at nucleotide 209 which changes aspartic acid 70 to glycine. This suggests that Asp 70 is part of the anionic site, and that the absence of this negatively charged amino acid explains the reduced affinity of atypical cholinesterase for positively charged substrates and inhibitors. The clinical consequence of reduced affinity for succinylcholine is that none of the succinylcholine is hydrolyzed in blood and a large overdose reaches the nerve-muscle junction where it causes prolonged muscle paralysis. Silent cholinesterase has a frame shift mutation at glycine 117 which prematurely terminates protein synthesis and yields no active enzyme. The K variant, named in honor of W. Kalow, has threonine in place of alanine 539. The K variant is associated with 33% lower activity. All variants arise from a single locus as there is only one gene for human cholinesterase (EC 3.1.1.8). Comparison of amino acid sequences of esterases and proteases shows that cholinesterase belongs to a new family of serine esterases which is different from the serine proteases.

Amino Acid Sequence↗
PubMedDate not supplied

Mivacurium as an alternative to succinylcholine during outpatient laparoscopy.

STUDY OBJECTIVES: To compare (1) the adequacy of conditions for tracheal intubation; (2) the onset, depth, clinically effective duration, and recovery profile; and (3) adverse effects associated with mivacurium as an alternative to succinylcholine during general (endotracheal) anesthesia for outpatient laparoscopy. DESIGN: A randomized, controlled clinical trial. SETTING: Barnes Hospital Outpatient Surgery Center. PATIENTS: Sixty healthy consenting ASA physical status I or II adult female outpatients. INTERVENTIONS: Following a standardized thiopental sodium-alfentanil induction, patients were randomly assigned to one of three groups: Group I-alfentanil-nitrous oxide (N2O)-succinylcholine; Group II-alfentanil-N2O-mivacurium; Group III-enflurane-N2O-mivacurium. MEASUREMENTS AND MAIN RESULTS: Neuromuscular blockade was measured by electromyography of the stimulated adductor pollicis muscle contraction. Tracheal intubation was attempted after achieving 70% or greater blockade and was graded on a four-point scale. Onset and recovery were more rapid with succinylcholine than with mivacurium. The clinically effective duration of action of mivacurium was not significantly different in the enflurane-N2O group compared with the alfentanil-N2O group. Side effects with mivacurium included flushing and occasional wheezing. CONCLUSIONS: Mivacurium 0.15 mg/kg given intravenously provided good to excellent conditions for tracheal intubation in 2 to 3 minutes. This dose provided a clinically effective duration of action of 20 to 25 minutes, and the residual blockade was readily reversible with neostigmine. Mivacurium did not, however, offer any apparent advantage over succinylcholine in this outpatient population.

Adult↗
PubMedDate not supplied

Neuromuscular effects of succinylcholine following different pretreatments.

STUDY OBJECTIVE: To study the neuromuscular effects (onset, intensity, and duration of block) of succinylcholine following different pretreatments. DESIGN: Randomized open study. SETTING: University-affiliated hospital. PATIENTS: Fifty ASA physical status I and II adult inpatients undergoing elective ophthalmic surgery. INTERVENTIONS: Succinylcholine 0.5 mg/kg was administered after no pretreatment or after pretreatment with d-tubocurarine 0.05 mg/kg intravenously (IV) 3 minutes before, chlorpromazine 0.1 mg/kg i.v. 3 minutes before, alpha-tocopherol (vitamin E) 600 mg in three divided doses orally at 6-hour intervals, or aspirin 600 mg orally 1 hour before in groups of ten patients each. MEASUREMENTS AND MAIN RESULTS: Neuromuscular block by stimulation of the ulnar nerve at the wrist by application of train-of-four stimuli at 2 Hz every 12 seconds and recording the force of contraction of the adductor pollicis muscle. There was no significant difference in the time to occurrence of maximum block (49 to 53 seconds), reappearance of the twitch response (254 to 307 seconds), or complete recovery of twitch response (532 to 607 seconds) between the groups receiving no pretreatment and those pretreated with chlorpromazine, alpha-tocopherol, or aspirin. However, the time to maximum block (71 seconds) was significantly longer and the time to reappearance of the response (172 seconds) was significantly shorter (both p < 0.05) in the d-tubocurarine pretreated group in comparison with the control group. The time to complete recovery (420 seconds) also was shorter but not significantly different. CONCLUSIONS: Of the pretreatments used, only d-tubocurarine interferes with the neuromuscular blocking effects of succinylcholine. Chlorpromazine, which attenuates the muscle pains as well as the increase in creatine kinase and can be administered with the same convenience, may be a better pretreatment in the prevention of side effects of succinylcholine.

Adolescent↗
PubMedDate not supplied

Calcium channel blockers do not enhance increases in plasma potassium after succinylcholine in humans.

STUDY OBJECTIVE: To determine whether chronic calcium channel blocker therapy exaggerates the rise in plasma potassium concentration ([K+]) after succinylcholine administration. DESIGN: Prospective clinical study. SETTING: University and Veterans Affairs hospitals. PATIENTS: 36 ASA physical status III and IV male patients: 21 patients taking chronic calcium channel blockers and 15 patients not receiving calcium channel blockers, all of whom were scheduled for inpatient surgical procedures with general anesthesia. INTERVENTIONS: In all patients, anesthesia was induced with high-dose opioids plus a sedative-hypnotic, and intubation was facilitated with 1 to 1.5 mg/kg succinylcholine without nondepolarizing neuromuscular blocker pretreatment. MEASUREMENTS AND MAIN RESULTS: Plasma [K+] was measured prior to induction and 1, 3, 5, 8, 11, and 15 minutes after succinylcholine was administered. A modest average peak rise of 0.5 mEq/L in plasma [K+] was observed, but there were no differences between patients who were or were not receiving calcium channel blockers. CONCLUSIONS: Patients receiving chronic calcium channel blocker therapy are at no greater risk of hyperkalemia after succinylcholine than those not taking such medications.

Anesthesia, Intravenous↗