Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:3.1.1.8 (cholinesterase)
12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Anaesthetic agents for day-case surgery ideally should have a short duration of action. This study was designed to compare the efficacy and safety of mivacurium and vecuronium for healthy adults undergoing dental day-case surgery. Thirty fit healthy adult patients (ASA I or II) randomly received either mivacurium 0.15 mg kg-1 (n = 15) or vecuronium 0.1 mg kg-1 (n = 15). Anaesthesia included propofol, fentanyl, nitrous oxide and isoflurane. Maximum depression of T1 was greater in the vecuronium group (99.8%) than in the mivacurium group (98.3%). There was no difference between grade of intubation at 2 min between the two groups, although patients receiving vecuronium had a more profound block at the time of intubation than those who received mivacurium (89.2% vs. 78.9%). Recovery to 10% T1 was faster in the mivacurium group (11.2 min vs. 33.1 min). All patients in the vecuronium group received neostigmine at the termination of surgery. The neostigmine evoked recovery index in the vecuronium group (4.39 min) was less than the spontaneous recovery index in the mivacurium group (6.78 min). One patient in the mivacurium group had a low plasma cholinesterase concentration (0.43 ku L-1); recovery times however, fell within the 95% confidence intervals (CI) for the group. There was no correlation between cholinesterase levels and recovery time. Mivacurium may be the more appropriate agent for dental day-case surgery because it has a shorter duration of action and does not generally require antagonism with an anticholinesterase.
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PMID:Mivacurium or vecuronium for muscular relaxation in day-case surgery. 946

Mivacurium is a short acting non-depolarising neuromuscular blocking agent. Short duration of action is due to a rapid hydrolysis by plasma cholinesterase (CHe). The duration of neuromuscular blockade can be prolonged by an abnormal variant of CHe. We report a case of a newborn with neuromuscular blockade for a duration of 8 hours following mivacurium 0.2 mg.kg-1. CHe activity values were not contributive for the diagnosis. The diagnosis was obtained with molecular study showing the new-born homozygocity. The whole family was heterozygous. This case emphasises the lack of precision of CHe activity measurement during the first 6 months of life.
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PMID:[Prolonged neuromuscular blockade with mivacurium in a newborn]. 975 Aug 10

Succinylcholine is the most important rapid-acting depolarizing muscle relaxant during anesthesia. Its desirable short duration of action is controlled by butyrylcholinesterase, the detoxifying enzyme. There are two reported cases of prolonged paralysis from succinylcholine in patients poisoned with the organophosphorus insecticides parathion and chlorpyrifos. The present study examines the possibility that other organophosphorus and methylcarbamate pesticides might also prolong succinylcholine action by inhibiting butyrylcholinesterase using mice treated intraperitoneally as a model and relating inhibition of blood serum hydrolysis of butyrylthiocholine to potentiated toxicity (mouse mortality). The organophosphorus plant defoliant tribufos (4 h pretreatment, 160 mg/kg) and organophosphorus plant growth regulator ethephon (1 h pretreatment, 200 mg/kg) potentiate the toxicity of succinylcholine by seven- and fourfold, respectively. Some other pesticides or analogs are more potent sensitizers for succinylcholine toxicity with threshold levels of 0.5, 1.0, 1.7, 8, 10, and 67 mg/kg for phenyl saligenin cyclic phosphonate, profenofos, methamidophos, tribufos, chlorpyrifos, and ethephon, respectively. Enhanced mortality from succinylcholine is generally observed when serum butyrylcholinesterase is inhibited 55-94%. Mivacurium, a related nondepolarizing muscle relaxant also detoxified by butyrylcholinesterase, is likewise potentiated by at least threefold on 4 hour pretreatment with tribufos (25 mg/kg) or profenofos (10 mg/kg).
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PMID:Organophosphorus pesticide-induced butyrylcholinesterase inhibition and potentiation of succinylcholine toxicity in mice. 989 Jan 96

The pharmacokinetics of 6 new neuromuscular blocking drugs are described. These are the aminosteroids pipecuronium bromide, rocuronium bromide and rapacuronium bromide (ORG-9487) and the benzylisoquinolinium diesters doxacurium chloride, mivacurium chloride and cisatracurium besilate. In healthy individuals, these drugs all have similar volumes of distribution. Their pharmacokinetics are influenced little by age or anaesthetic technique, but renal and hepatic disease may significantly alter their distribution and elimination. Pipecuronium resembles pancuronium in its pharmacokinetic and neuromuscular blocking profile, but is devoid of cardiovascular effects. It has a low clearance (0.16 L/h/kg) and long elimination half-life (120 minutes). It is largely eliminated through the kidney. Rocuronium has a similar pharmacokinetic profile to vecuronium but its onset of action is more rapid and duration of action slightly shorter. Its clearance (0.27 L/h/kg) is intermediate between those of pipecuronium and rapacuronium, but its elimination half-life is long (83 minutes). The pharmacokinetics of rocuronium are altered by renal and hepatic disease; the latter probably has the more significant effect. Rapacuronium has a rapid onset, and a bolus dose has a short duration of action. It has a high clearance (0.59 L/h/kg) but a long elimination half-life (112 minutes). Doxacurium has a pharmacokinetic and pharmacodynamic profile similar to pipecuronium. It has a high potency and is devoid of cardiovascular effects. In adults, it has a low clearance (0.15 L/h/kg) and long elimination half-life (87 minutes). Mivacurium is a mixture of 3 stereoisomers. It has a short to intermediate duration of action. It is hydrolysed by plasma cholinesterase. Inherited or acquired alterations in plasma cholinesterase activity are associated with changes in the pharmacokinetics and time course of action of mivacurium. The 2 active isomers (cis-trans and trans-trans) have a high clearance (4.74 L/h/kg) and very short elimination half-lives (approximately 2 minutes). Cisatracurium is the 1R-cis 1'R-cis isomer of atracurium. It has similar pharmacokinetics and pharmacodynamics to atracurium. It is mainly broken down by Hofmann (non-enzymatic) degradation. Cisatracurium has an intermediate clearance (0.3 L/h/kg) and short elimination half-life (26 minutes). Hepatic and renal disease have little effect on its pharmacokinetics.
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PMID:Clinical pharmacokinetics of the newer neuromuscular blocking drugs. 1022 67

Mivacurium is metabolized by plasma cholinesterase (PCHE). Metoclopramide inhibits PCHE in vitro and in vivo. We have assessed the effect of metoclopramide on duration of action of mivacurium and measured PCHE at baseline and at the time of maximal block. In a randomized, double-blind study, 30 patients received metoclopramide 0.15 mg kg-1 i.v. or saline, followed by propofol anaesthesia and mivacurium 0.15 mg kg-1. Using a TOF-Guard accelerometer, times to recovery of TI to 25%, 75% and 90% were 13.4, 19.3 and 21.9 min in the saline group and 17.8, 25.3 and 28.8 min in the metoclopramide group (P < 0.01, P < 0.05, P < 0.05, respectively). There were no differences in onset time or recovery index between the groups. PCHE activity at the time of maximum block decreased within each group (P < 0.01) but there was no difference between groups. In a second biochemical study of eight patients, a small decrease in PCHE activity was detected after metoclopramide 0.15 mg kg-1, but before administration of mivacurium (P < 0.025). We conclude that metoclopramide prolongs the duration of action of mivacurium.
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PMID:Influence of metoclopramide on plasma cholinesterase and duration of action of mivacurium. 1047 19

Mivacurium is mainly metabolized by plasma cholinesterase, whereas atracurium is removed by Hofman elimination. The purpose of this study was to compare the infusion rate of atracurium and mivacurium in maintaining surgical relaxation, and to compare their recovery indices between parturients and non-pregnant women. Muscle relaxation was maintained by the continuous infusion of relaxants to retain the first response of train-of-four (TOF) at 5% of control. When mivacurium was used, Bolus-T5 (duration from the end of mivacurium bolus injection to 5% single twitch recovery) was measured. After discontinuing the infusion, the recovery index was measured. The infusion rate of mivacurium, not atracurium, was significantly lower in parturients and Bolus-T5 of parturients was significantly longer than that of non-pregnant women. There was no significant difference in the recovery indices of both relaxants. The authors concluded that the infusion rate of mivacurium in maintaining muscle relaxation in parturients should be reduced compared to the rate in non-pregnant women and measuring Bolus-T5 may be helpful in determining the infusion rate to maintain muscle relaxation.
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PMID:The infusion rate of mivacurium or atracurium for cesarean section compared with gynecological procedures. 1048 41

Mivacurium is a short-acting, nondepolarizing neuromuscular blocking agent hydrolyzed by plasma cholinesterase. Because it allows fast recovery, it is a commonly used muscle relaxant for patients undergoing short surgical procedures. We report the case of a 5-year-old boy who underwent outpatient inguinal herniorraphy and developed unexpected prolonged neuromuscular block after the use of mivacurium. He required mechanical ventilation support in the intensive care unit because he could not attain adequate muscle power 1 hour after termination of anesthesia; the muscular paralysis persisted for 5 hours after the bolus dose of 0.3 mg/kg mivacurium. Subsequent investigation revealed an extremely low plasma cholinesterase concentration (115 U/L), and this was later determined to be a congenital condition. This is the first reported case of cholinesterase deficiency diagnosed as a result of general anesthesia in Taiwan.
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PMID:Prolonged neuromuscular block with mivacurium in a patient with cholinesterase deficiency. 1096 12

Mivacurium is a benzylisoquinolone, choline-like, non-depolarizing muscle relaxant. Its onset of action is similar to that of atracurium but its duration of action is shorter (approximately 10-15 minutes). Mivacurium is metabolized by plasma cholinesterases at approximately 70% of the rate of metabolism of suxamethonium. Deficiency or abnormality of plasma cholinesterase may cause the duration of action of both suxamethonium and mivacurium to be greatly prolonged. We describe a case of prolonged mivacurium paralysis after day surgery. Laboratory investigations showed a genetic tendency toward abnormal cholinesterase levels, but markedly depressed cholinesterase activity was suggestive of additional acquired causes. This patient had a history of liver disease, malnutrition and anticholinesterase use, which we believe were the most significant factors involved.
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PMID:Prolonged paralysis following mivacurium administration. 1207 46

Mivacurium is a short-acting neuromuscular blocking drug, ideal for short surgical procedures. The brief duration of action depends on rapid hydrolysis by plasma cholinesterase. An inherited or acquired deficiency of plasma cholinesterase can prolong the effect of mivacurium. We present an unusual case of unanticipated postoperative apnea following mivacurium administration, as a result of acquired plasma cholinesterase deficiency, in a patient with previous uneventful exposure to both mivacurium and suxamethonium (succinylcholine).
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PMID:Prolonged neuromuscular blockade as a result of malnutrition-induced pseudocholinesterase deficiency. 1498 58

The interaction between mivacurium and magnesium sulphate was investigated in a group of parturients undergoing caesarean section under general anaesthesia. Thirty parturients were studied; 10 normotensive controls (group NT), 10 hypertensive controls (group HT) and 10 hypertensives who received magnesium sulphate (group HTM). At induction group HT received 30 microg/kg of alfentanil and group HTM 10 microg/kg of alfentanil and 30 or 60 mg/kg of magnesium sulphate. Neuromuscular function was monitored by electromyography. Mivacurium 0.15 mg/kg was given after 60% recovery of T1 following succinylcholine. Magnesium concentrations and plasma cholinesterase activity were significantly elevated in group HTM (1.57 +/- 0.53 mmol/1 and 4.60 +/- 1.27 kU/1) compared with group HT (0.71 +/- 0.18 mmol/1 and 3.44 +/- 0.97 kU/1) and group NT (0.60 +/- 0.07 mmol/1 and 2.86 +/- 0.82 kU/1) (P < 0.005). Time to maximal recovery, and time from 25-75% of maximal recovery from mivacurium, were significantly prolonged in group HTM (60.9 +/- 15.3 min and 16.8 +/- 5.6 min) compared with group HT (34.9 +/- 7.6 min and 7.6 +/- 3.6 min) and group NT (37.4 +/- 14.4 min and 8.5 +/- 3.4 min) (P < 0.01). Time to 25% recovery was prolonged in group HTM (35.1 +/- 7.4 min) compared with the other two groups (HT: 21.6 +/- 6.4 min and NT: 22.8 +/- 10.2 min) (P < 0.01). Whilst the duration of action of mivacurium, determined by electromyography, is prolonged by subtherapeutic serum magnesium concentrations, of the available non-depolarizing relaxants mivacurium would seem to be most appropriate for caesarean section.
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PMID:Mivacurium for caesarean section in hypertensive parturients receiving magnesium sulphate therapy. 1532 Dec 40


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