Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:3.1.1.7 (acetylcholinesterase)
 28,390 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Atracurium besylate, a nondepolarizing neuromuscular blocking agent, was administered by infusion to 10 cats that were anesthetized with isoflurane and oxygen to allow transplantation of a myocutaneous flap. Five of the cats were given cyclosporine (20 mg/kg of body weight, PO q 12 h in divided doses) for 2 days prior to anesthesia, and prednisolone (0.25 mg/kg, PO) on the morning of surgery. The other 5 cats were not given either drug. Neuromuscular blockade was assessed, using the train-of-four stimulation, and throughout surgery, the infusion rate was adjusted to maintain the first-twitch response (T1) at 90 to 95% depression from baseline. At completion of surgery, atracurium was discontinued, and the infusion rate and the time for recovery (the time for the train-of-four ratio to increase from 50 to 75%) were recorded. Once the train-of-four ratio had been stable for 10 minutes, edrophonium (0.5 mg/kg), a cholinesterase inhibitor, was administered IV, and neuromuscular blockade was monitored for another 10 minutes. Mean (+/- SD) duration of the atracurium infusion was 302.1 +/- 70.5 minutes for the control group and was 323.9 +/- 61.7 minutes for the cats given cyclosporine and prednisolone. In the cats of the control group, the infusion rate required to induce 90 to 95% T1 depression from baseline was 3.7 +/- 0.7 micrograms/kg/min. This rate was not significantly different from that of 2.8 +/- 1.2 micrograms/kg/min in cats given cyclosporine and prednisolone. Significant difference in recovery time was not evident between the control group and the treated group (6.4 +/- 4.5 minutes vs 6.2 +/- 2.5 minutes).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Atracurium administration, as an infusion, to induce neuromuscular blockade in clinically normal and temporarily immune-suppressed cats. 225 41

A 69 year old man receiving echothiophate eye drops for glaucoma was given a controlled infusion of succinylcholine during elective surgery for incisional hernia. Neuromuscular blockade was assessed by the measurement of the force of contraction of the adductor pollicis muscle. Only 9.5 mg succinylcholine were required for tracheal intubation and 1.1 mg/min for maintenance. When the infusion was stopped, recovery of neuromuscular transmission was rapid and uneventful. Plasma cholinesterase activity was 62 per cent below normal, but the enzyme was qualitatively normal. Thus, muscle relaxation can be achieved safely with a succinylcholine infusion in patients with decreased plasma cholinesterase activity if neuromuscular function is closely monitored.
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PMID:Controlled succinylcholine infusion in a patient receiving echothiophate eye drops. 728 94

Mivacurium is a short-acting nondepolarizing muscle relaxant (NDPMR) with a benzyl-isoquinoline structure and rapid, spontaneous reversal. It is hydrolyzed by cholinesterase in plasma and its chemical structure favors histamine release, leading to cutaneous or cardiovascular symptoms, particularly when the dose is increased or when the drug is injected rapidly. Both duration of effect and reversal of mivacurium are less dose dependent than they are with intermediate-duration NDPMRs. In adults the recommended dose for intubation (2 to 3 times the ED95) induces clinically effective blockade lasting 15 to 25 minutes, with spontaneous recovery occurring 10 to 20 minutes later. In children two to 12 years old given the same dose, duration of action is shorter and reversal occurs more rapidly. These properties reduce the likelihood of antagonizing the residual neuromuscular blockade. The duration of successive doses is similar and continuous infusion does not affect reversal. Neuromuscular blockade may be prolonged in patients with low plasma cholinesterase activity, particularly in individuals who are homozygous for the atypical plasma cholinesterase gene. Monitoring is therefore recommended when mivacurium is used. Provided patients have normal plasma cholinesterase activity, mivacurium is indicated for interventions that are short or of unpredictable duration when rapid reversal of neuromuscular blockade is required, or whenever anticholinesterase agents must be avoided.
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PMID:[Mivacurium]. 964 62

Mivacurium- pancuronium combination proved to be more potent than either drug given alone. The goal of this study was to evaluate the safety and efficacy of this combination in elderly group and its correlation to plasma butyryl cholinesterase (Bche) activity. Forty patients, ASA I or II scheduled for elective open cholecystectomy were allocated into two groups of twenty patients each: young group (18- 55 years) and elderly group (60-75 years). Anesthesia was induced with midazolam, fentanyl, and propofol then maintained with isoflurane and opioid supplementation. Neuromuscular blockade (NMB) was monitored by train-of-four (TOF) stimulation of the ulnar nerve. After calibration, NMB was achieved by 16 microg kg(-1) pancuronium followed by 32 microg kg(-1) mivacurium. The following parameters were recorded: The onset time, clinical duration, recovery index and the total dose of mivacurium and pancuronium together with hemodynamic data. Three blood samples for Bche activity were collected: before pancuronium injection, 3 min. and 30 min. afterwards in both groups. The onset time and the recovery index of NMB were comparable in both groups. The duration of action was significantly prolonged in elderly group (49.8 +/- 10.48 min.) compared to young one (37.13 +/- 7.81 min.). The total dose of mivacurium was significantly less in the elderly group (22.56 +/- 2.39 microg kg(-1) hr(-1)) when compared to the young group (25.78 +/- 3.05 microg kg(-1) hr(-1)). For all patients, the preoperative Bche activity was within the normal range. After pancuronium injecttion, it showed a significant reduction in both groups at three and thirty minutes except a non significant value in young at thirty minutes. This reduction showed a significantly higher percent change in the elderly group (30.37 +/- 22.01) than the young group (8.60 +/- 19.19) at thirty minutes. There were significant intra operative variations in the percent changes of hemodynamic data compared to the preoperative values, yet, still within the clinically acceptable range. So, the use of a small dose of pancuronium followed by a small dose of mivacurium with a ratio of 1:2 can produce synergism without affecting either the recovery profile of mivacurium or the clinical hemodynamic stability even in the elderly group.
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PMID:Role of cholinesterase activity on pharmacodynamics of mivacurium preceded by pancuronium in elderly and young adults. 1758 May 81

Neuromuscular blockade, induced by neuromuscular blocking agents, has allowed prescribed immobility, improved surgical exposure, optimal airway management conditions, and facilitated mechanical ventilation. However, termination of the effects of neuromuscular blocking agents has, until now, remained limited. A novel cyclodextrin encapsulation process offers improved termination of the paralytic effects of aminosteroidal non-depolarizing neuromuscular blocking agents. Sugammadex sodium is the first in a new class of drug called selective relaxant binding agents. Currently, in clinical trials, sugammadex, a modified gamma cyclodextrin, has shown consistent and rapid termination of neuromuscular blockade with few side effects. The pharmacology of cyclodextrins in general and sugammadex in particular, together with the results of current clinical research are reviewed. The ability of sugammadex to terminate the action of neuromuscular blocking agents by direct encapsulation is compared to the indirect competitive antagonism of their effects by cholinesterase inhibitors. Also discussed are the clinical implications that extend beyond fast, effective reversal, including numerous potential perioperative benefits.
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PMID:Discovery, development, and clinical application of sugammadex sodium, a selective relaxant binding agent. 1992 Aug 93

Neuromuscular blockade plays an important role in the safe management of patient airways, surgical field improvement, and respiratory care. Rapid-sequence induction of anesthesia is indispensable to emergency surgery and obstetric anesthesia, and its purpose is to obtain a stable airway, adequate depth of anesthesia, and appropriate respiration within a short period of time without causing irritation or damage to the patient. There has been a continued search for new neuromuscular blocking drugs (NMBDs) with a rapid onset of action. Factors that affect the onset time include the potency of the NMBDs, the rate of NMBDs reaching the effect site, the onset time by dose control, metabolism and elimination of NMBDs, buffered diffusion to the effect site, nicotinic acetylcholine receptor subunit affinity, drugs that affect acetylcholine (ACh) production and release at the neuromuscular junction, drugs that inhibit plasma cholinesterase, presynaptic receptors responsible for ACh release at the neuromuscular junction, anesthetics or drugs that affect muscle contractility, site and methods for monitoring neuromuscular function, individual variability, and coexisting disease. NMBDs with rapid onset without major adverse events are expected in the next few years, and the development of lower potency NMBDs will continue. Anesthesiologists should be aware of the use of NMBDs in the management of anesthesia. The choice of NMBD and determination of the appropriate dosage to modulate neuromuscular blockade characteristics such as onset time and duration of neuromuscular blockade should be considered along with factors that affect the effects of the NMBDs. In this review, we discuss the factors that affect the onset time of NMBDs.
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PMID:Factors that affect the onset of action of non-depolarizing neuromuscular blocking agents. 2922 15