Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.1.1.8 (cholinesterase)
 12,691 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Preliminary disposition studies of the investigational, long-acting muscle relaxant doxacurium chloride (Nuromax) have demonstrated dual elimination by renal and hepatobiliary pathways, as well as slow hydrolysis by plasma cholinesterase. The present study compares the kinetics and dynamics of doxacurium in eight ASA physical status I or II elderly patients (67-72 yr of age) and eight ASA I or II young patients (22-49 yr of age). After institutionally approved written informed consent, kinetic and dynamic measurements were made after a 25-micrograms/kg bolus injection of doxacurium during 1.25 MAC nitrous oxide/oxygen/isoflurane anesthesia. Maximum twitch depression was similar in older patients (96.4% +/- 1.3%) to that in the young patients (96.6% +/- 1.8%). The time to achieve this level of block was significantly longer in the elderly than in the young (11.2 +/- 1.1 min versus 7.7 +/- 1.0 min, respectively). Recovery times to twitch heights of 5% and 25% of control tended to be prolonged and were more variable in the elderly (82.6 +/- 17.2 and 97.1 +/- 20.1 min, respectively) than in the young (54.8 +/- 9 and 67.5 +/- 8.2 min, respectively). Elimination half-life (96 +/- 20 min) and clearance (2.47 +/- 0.69 mL.kg-1.min-1) in the elderly patients were not statistically different from values found in the younger group. Volume of distribution at steady state in the elderly (220 +/- 80.2 mL/kg) was significantly larger than in the young (150 +/- 40.0 mL/kg).(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Pharmacokinetics and pharmacodynamics of doxacurium in young and elderly patients during isoflurane anesthesia. 214 83

Metals of the platinum group have found important application in technology and industry. Compounds of these metals display a broad spectrum of toxic effects on the organism. In persons dealing with them in the production, they induce allergic occupational diseases of the respiratory passages, dermatoses, affections of the eyes. Their resorptive chronic effect in experiment is characterized by reduction in the body mass of the animals and the content of haemoglobin in the blood, by disturbances of the protein-synthesizing function of the liver, decreased cholinesterase activity in the blood, impaired carbohydrate and lipid metabolism, reduced concentrating capacity of the liver, development of glomerulonephritis. Platinum and platinoids irritate mucous membranes and skin. They penetrate the organism through intact skin. Data on the distribution of the metals in the organs and on their elimination from the organism are reported. Toxicity of the metals of the platinum group is correlated with valence of the compounds and with electron structure. MAC for milling and condensation aerosols of poorly soluble compounds (metal and its oxides) are recommended at 0.1 mg/m3. For aerosols of all soluble compounds of platinum and platinoids, MAC of 0.001 mg/m3 are recommended.
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PMID:Industrial toxicology of metals of the platinum group. 671 73

Inhalation exposure to kuscide changed the function of the CNS, microcirculation, blood cholinesterase activity. Kuscide concentration 40 mg/m3 is toxic for rats, 4 mg/m3 is threshold, and 0.4 mg/m3 is nonactual. MAC of kuscide for working environment is 0.5 mg/m3.
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PMID:[Rationale for maximum permissible concentration of kuscide in the air of the work area in agriculture]. 802 70

In the event of mass destruction with nerve agents a number of victims can be expected to suffer from symptoms of cholinergic overstimulation due to intoxication as well as from physical trauma. Since previous studies have demonstrated that cholinesterase inhibitors may reverse general anaesthesia in humans this scenario raises the question of how these patients can be anaesthetised in order to enable surgical interventions. A likely reason for this reversal is a reduction of anaesthetic potency by acetylcholine as observed for volatile anaesthetics in vitro. In order to test whether a combination of cholinergic antagonists with general anaesthetics improves their potency, we investigated the effects of clinically relevant concentrations of atropine on sevoflurane potency in cortical and spinal slice cultures during cholinergic overstimulation. As the spinal cord and neocortex are important substrates for general anaesthetics cultured spinal and cortical tissue slices were obtained from embryonic and newborn mice, respectively. Drug effects were assessed by extracellular voltage recordings of spontaneous action potential activity. Application of acetylcholine elevated spontaneous activity in neocortical and spinal slices. Atropine (10 nM) reduced discharge rates and reversed the increase of spontaneous activity induced by acetylcholine. In the presence of acetylcholine and atropine sevoflurane caused a concentration-dependent decrease of neuronal activity in neocortical (EC(50)=0.35+/-0.33 MAC) and spinal slices (EC(50)=0.43+/-0.03 MAC). Comparing our results with previous studies which investigated the effects of acetylcholine on anaesthetic potency it is concluded that small concentrations of atropine increase sevoflurane potency in cortical networks during cholinergic overstimulation. Thus, in a clinical setting, we recommend that anaesthetic drugs should be co-applied with atropine for adequate performance of general anaesthesia.
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PMID:Atropine increases sevoflurane potency in cortical but not spinal networks during cholinergic overstimulation. 2000 96