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[PMID]:28296779
[Au] Autor:Bao HX; Tong PJ; Li CX; Du J; Chen BY; Huang ZH; Wang Y
[Ad] Endereço:aFirst Clinical Medical College of Zhejiang Chinese Medical University bZhejiang Provincial Hospital of TCM cDepartment of Laboratory Medicine, Zhejiang Provincial People's Hospital, People's Hospital of Hangzhou Medical College dDepartment of Transfusion, Zhejiang Provincial People's Hospital, People's Hospital of Hangzhou Medical College, Hangzhou eInstitute of Neuroscience and Institute of Hypoxia Medicine, Wenzhou Medical University, Wenzhou fDepartment of Transfusion, Lishui People's Hospital, Lishui, Zhejiang, China.
[Ti] Título:Efficacy of fresh packed red blood transfusion in organophosphate poisoning.
[So] Source:Medicine (Baltimore);96(11):e6375, 2017 Mar.
[Is] ISSN:1536-5964
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The mortality rate caused by organophosphate (OP) poisoning is still high, even the standard treatment such as atropine and oxime improves a lot. To search for alternative therapies, this study was aimed to investigate the effects of packed red blood cell (RBC) transfusion in acute OP poisoning, and compare the therapeutic effects of RBCs at different storage times.Patients diagnosed with OP poisoning were included in this prospective study. Fresh RBCs (packed RBCs stored less than 10 days) and longer-storage RBCs (stored more than 10 days but less than 35 days) were randomly transfused or not into OP poisoning patients. Cholinesterase (ChE) levels in blood, atropine usage and durations, pralidoxime durations were measured.We found that both fresh and longer-storage RBCs (200-400 mL) significantly increased blood ChE levels 6 hours after transfusion, shortened the duration for ChE recovery and length of hospital stay, and reduced the usage of atropine and pralidoxime. In addition, fresh RBCs demonstrated stronger therapeutic effects than longer-storage RBCs.Packed RBCs might be an alternative approach in patients with OP poisoning, especially during early stages.
[Mh] Termos MeSH primário: Transfusão de Eritrócitos/métodos
Intoxicação por Organofosfatos/terapia
[Mh] Termos MeSH secundário: Doença Aguda
Atropina/uso terapêutico
Reativadores da Colinesterase/uso terapêutico
Colinesterases/sangue
Feminino
Lavagem Gástrica
Seres Humanos
Masculino
Intoxicação por Organofosfatos/tratamento farmacológico
Compostos de Pralidoxima/uso terapêutico
Estudos Prospectivos
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Cholinesterase Reactivators); 0 (Pralidoxime Compounds); 7C0697DR9I (Atropine); EC 3.1.1.8 (Cholinesterases); P7MU9UTP52 (pralidoxime)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170410
[Lr] Data última revisão:
170410
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:170316
[St] Status:MEDLINE
[do] DOI:10.1097/MD.0000000000006375


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[PMID]:28106328
[Au] Autor:Driant T; Nachon F; Ollivier C; Renard PY; Derat E
[Ad] Endereço:Sorbonne Universités, UPMC UNIV Paris 06, Institut Parisien de Chimie Moléculaire, UMR CNRS 8232, Case 229, 4 Place Jussieu, 75252, Paris Cedex 05, France.
[Ti] Título:On the Influence of the Protonation States of Active Site Residues on AChE Reactivation: A QM/MM Approach.
[So] Source:Chembiochem;18(7):666-675, 2017 Apr 04.
[Is] ISSN:1439-7633
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Acetylcholinesterase (AChE), an enzyme of the serine hydrolase superfamily, is a mediator of signal transmission at cholinergic synapses by catalyzing acetylcholine cleavage into acetate and choline. This enzyme is vulnerable to covalent inhibition by organophosphate compounds (like VX). Covalent inhibition of AChE does not revert spontaneously. Known reactivator compounds have limited action in restoring catalytic activity. QM/MM simulations of VX-inhibited AChE reactivation by pralidoxime (2-PAM), a classical reactivator, were performed. These afforded a broad view of the effect of protonation states of active-site residues, and provide evidence for the role of Glu202, which needs to be protonated for reactivation to occur. In situ deprotonation of 2-PAM for both protonation states of Glu202 showed that His447 is able to deprotonate 2-PAM with the assistance of Glu202. Because the active site of serine hydrolases is highly conserved, this work provides new insights on the interplay between the catalytic triad residues and this glutamate, newly identified as protonatable.
[Mh] Termos MeSH primário: Acetilcolinesterase/química
Reativadores da Colinesterase/química
[Mh] Termos MeSH secundário: Domínio Catalítico
Inibidores da Colinesterase/química
Simulação por Computador
Ácido Glutâmico/química
Histidina/química
Modelos Químicos
Estrutura Molecular
Organofosfatos/química
Compostos Organotiofosforados/química
Compostos de Pralidoxima/química
Prótons
Teoria Quântica
Serina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Cholinesterase Inhibitors); 0 (Cholinesterase Reactivators); 0 (Organophosphates); 0 (Organothiophosphorus Compounds); 0 (Pralidoxime Compounds); 0 (Protons); 3KX376GY7L (Glutamic Acid); 452VLY9402 (Serine); 4QD397987E (Histidine); 9A4381183B (VX); EC 3.1.1.7 (Acetylcholinesterase); P7MU9UTP52 (pralidoxime); S45M750QSH (tabun)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170919
[Lr] Data última revisão:
170919
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170121
[St] Status:MEDLINE
[do] DOI:10.1002/cbic.201600646


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[PMID]:27765719
[Au] Autor:Hudson JS; Abode-Iyamah K; Nagahama Y; Reddy CG
[Ad] Endereço:Department of Neurological Surgery, University of Iowa Hospitals and Clinics, Iowa City, Iowa, USA. Electronic address: joseph-hudson@uiowa.edu.
[Ti] Título:Accidental Intrathecal Injection of Ionic Contrast: Case Report and Review of the Literature.
[So] Source:World Neurosurg;97:757.e1-757.e9, 2017 Jan.
[Is] ISSN:1878-8769
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Ionic contrast, if accidentally injected into the intrathecal space during routine imaging studies or interventional procedures, may significantly interfere with neuronal activity, potentially causing ascending tonic-clonic seizure syndrome and even death. As a result, ionic contrast is strictly contraindicated for intrathecal use. Rapid recognition of the condition followed by prompt management, typically involving aggressive cerebrospinal fluid (CSF) drainage, is critical to improving patient outcome. Lumbar drain has previously been well described as a management strategy. CASE DESCRIPTION: We present a case of accidental intrathecal injection of an ionic contrast agent, iothalamate meglumine, in a patient undergoing cervical epidural steroid injection. This patient was managed successfully with drainage of CSF using an external ventricular drain alone. CONCLUSION: Our literature review and analysis of the previously published cases demonstrate that aggressive CSF drainage is essential to improve outcomes, and in some cases an external ventricular drain alone may be effectively used.
[Mh] Termos MeSH primário: Encefalopatias/induzido quimicamente
Iotalamato de Meglumina/efeitos adversos
Erros de Medicação/efeitos adversos
Erros de Medicação/prevenção & controle
Doenças da Coluna Vertebral/induzido quimicamente
Derivação Ventriculoperitoneal
[Mh] Termos MeSH secundário: Encefalopatias/diagnóstico
Encefalopatias/prevenção & controle
Drenagem/instrumentação
Drenagem/métodos
Medicina Baseada em Evidências
Feminino
Seres Humanos
Injeções Espinhais/efeitos adversos
Iotalamato de Meglumina/administração & dosagem
Meia-Idade
Compostos de Pralidoxima/administração & dosagem
Compostos de Pralidoxima/efeitos adversos
Doenças da Coluna Vertebral/diagnóstico
Doenças da Coluna Vertebral/prevenção & controle
Resultado do Tratamento
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Pralidoxime Compounds); P7MU9UTP52 (pralidoxime); XUW72GOP7W (Iothalamate Meglumine)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170911
[Lr] Data última revisão:
170911
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:161022
[St] Status:MEDLINE


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[PMID]:26972668
[Au] Autor:Calas AG; Dias J; Rousseau C; Arboléas M; Touvrey-Loiodice M; Mercey G; Jean L; Renard PY; Nachon F
[Ad] Endereço:Institut de Recherche Biomédicale des Armées, Brétigny-sur-Orge Cédex, France; COGNition and ACtion Group, UMR 8257, CNRS-MD-UPV, Centre universitaire des Saints-Pères, Paris, France. Electronic address: guilhem.calas@irba.fr.
[Ti] Título:An easy method for the determination of active concentrations of cholinesterase reactivators in blood samples: Application to the efficacy assessment of non quaternary reactivators compared to HI-6 and pralidoxime in VX-poisoned mice.
[So] Source:Chem Biol Interact;267:11-16, 2017 Apr 01.
[Is] ISSN:1872-7786
[Cp] País de publicação:Ireland
[La] Idioma:eng
[Ab] Resumo:Organophosphorus nerve agents, like VX, are highly toxic due to their strong inhibition potency against acetylcholinesterase (AChE). AChE inhibited by VX can be reactivated using powerful nucleophilic molecules, most commonly oximes, which are one major component of the emergency treatment in case of nerve agent intoxication. We present here a comparative in vivo study on Swiss mice of four reactivators: HI-6, pralidoxime and two uncharged derivatives of 3-hydroxy-2-pyridinaldoxime that should more easily cross the blood-brain barrier and display a significant central nervous system activity. The reactivability kinetic profile of the oximes is established following intraperitoneal injection in healthy mice, using an original and fast enzymatic method based on the reactivation potential of oxime-containing plasma samples. HI-6 displays the highest reactivation potential whatever the conditions, followed by pralidoxime and the two non quaternary reactivators at the dose of 50 mg/kg bw. But these three last reactivators display equivalent reactivation potential at the same dose of 100 µmol/kg bw. Maximal reactivation potential closely correlates to surviving test results of VX intoxicated mice.
[Mh] Termos MeSH primário: Análise Química do Sangue/métodos
Barreira Hematoencefálica/efeitos dos fármacos
Substâncias para a Guerra Química/toxicidade
Reativadores da Colinesterase/sangue
Compostos Organotiofosforados/toxicidade
Oximas/farmacologia
Compostos de Pralidoxima/farmacologia
Compostos de Piridínio/farmacologia
[Mh] Termos MeSH secundário: Acetilcolinesterase/química
Acetilcolinesterase/metabolismo
Animais
Barreira Hematoencefálica/metabolismo
Eritrócitos/citologia
Eritrócitos/enzimologia
Meia-Vida
Seres Humanos
Injeções Intraperitoneais
Masculino
Camundongos
Oximas/metabolismo
Compostos de Pralidoxima/metabolismo
Substâncias Protetoras/metabolismo
Substâncias Protetoras/farmacologia
Compostos de Piridínio/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Chemical Warfare Agents); 0 (Cholinesterase Reactivators); 0 (Organothiophosphorus Compounds); 0 (Oximes); 0 (Pralidoxime Compounds); 0 (Protective Agents); 0 (Pyridinium Compounds); 9A4381183B (VX); EC 3.1.1.7 (Acetylcholinesterase); HUV88P6SJS (asoxime chloride); P7MU9UTP52 (pralidoxime)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170328
[Lr] Data última revisão:
170328
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160315
[St] Status:MEDLINE


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[PMID]:28102531
[Au] Autor:Droste DJ; Shelley ML; Gearhart JM; Kempisty DM
[Ad] Endereço:Environmental Compliance Officer, Marine Corps Installation Command, 3000 Marine Corps, Pentagon, Washington, District of Columbia.
[Ti] Título:A systems dynamics approach to the efficacy of oxime therapy for mild exposure to sarin gas.
[So] Source:Am J Disaster Med;11(2):89-118, 2016.
[Is] ISSN:1932-149X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The use of nerve agents such as sarin is as much a threat today as any other time in our history. The events in Syria in 2013 are proof of this. "The Obama administration asserted Sunday for the first time that the Syrian government used the nerve gas sarin to kill more than 1,400 people (August 21, 2013) in the world's gravest chemical weapons attack in 25 years." With these recent events clear in our mind, we must focus on the horrific nature of these chemical agents to devise a strategy that will enable first responders to counteract these insidious chemicals. This paper presents research on a physiologically based pharmacokinetic model to determine whether the current treatment protocol prescribed by the Center for Disease Control (CDC) and the US Army is effective in treating victims suffering from acute exposure symptoms. The model was used to determine what treatment should be used for victims suffering from mild exposure symptoms. The results indicate that the current CDC and US Army treatment is effective, but treatment with oxime therapy was not effective in alleviating symptoms of mild exposure. By applying these results, an effective treatment protocol was developed.
[Mh] Termos MeSH primário: Antídotos/farmacocinética
Substâncias para a Guerra Química/farmacocinética
Intoxicação por Organofosfatos/tratamento farmacológico
Oximas/farmacocinética
Sarina/farmacocinética
[Mh] Termos MeSH secundário: Antídotos/uso terapêutico
Centers for Disease Control and Prevention (U.S.)
Substâncias para a Guerra Química/envenenamento
Seres Humanos
Modelos Teóricos
Oximas/uso terapêutico
Guias de Prática Clínica como Assunto
Compostos de Pralidoxima/uso terapêutico
Sarina/envenenamento
Análise de Sistemas
Estados Unidos
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antidotes); 0 (Chemical Warfare Agents); 0 (Oximes); 0 (Pralidoxime Compounds); B4XG72QGFM (Sarin); P7MU9UTP52 (pralidoxime)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:170629
[Lr] Data última revisão:
170629
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170120
[St] Status:MEDLINE


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[PMID]:28043418
[Au] Autor:Lin CC; Hung DZ; Chen HY; Hsu KH
[Ad] Endereço:Department of Emergency Medicine, Chang Gung Memorial Hospital at Linkou, Chang Gung University College of Medicine, Taoyuan, Taiwan; College of Medicine, Chang Gung University, Taoyuan, Taiwan.
[Ti] Título:The effectiveness of patient-tailored treatment for acute organophosphate poisoning.
[So] Source:Biomed J;39(6):391-399, 2016 Dec.
[Is] ISSN:2320-2890
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: To determine a new pralidoxime (PAM) treatment guideline based on the severity of acute organophosphate intoxication patients, APACHE II score, and dynamic changes in serum butyrylcholinesterase (BuChE) activity. METHODS: This is a randomization trial. All patients received supportive care measurements and atropinization. Each enrolled patient was treated with 2 gm PAM intravenously as the loading dose. The control group was treated according to the WHO's recommended PAM regimen, and the experimental group was treated according to their APACHE II scores and dynamic changes in BuChE activity. If a patient's APACHE II score was ≧26 or there was no elevation in BuChE activity at the 12th hour when compared to the 6th, doses of 1 g/h PAM (i.e., doubled WHO's recommended PAM regimen) were given. The levels of the serum BuChE and red blood cells acetylcholinesterase and the serum PAM levels were also measured. RESULTS: Forty-six organophosphate poisoning patients were enrolled in this study. There were 24 patients in the control group and 22 patients in the experimental group. The hazard ratio of death in the control group to that of the experimental group was 111.51 (95% CI: 1.17-1.613.45; p = 0.04). The RBC acetylcholinesterase level was elevated in the experimental group but was not in the control group. The experimental group did not exhibit a higher PAM blood level than did the control group. CONCLUSION: The use of PAM can be guided by patient severity. Thus, may help to improve the outcomes of organophosphate poisoning patients.
[Mh] Termos MeSH primário: Acetilcolinesterase/metabolismo
Intoxicação por Organofosfatos/tratamento farmacológico
Compostos de Pralidoxima/uso terapêutico
[Mh] Termos MeSH secundário: Doença Aguda
Adulto
Idoso
Eritrócitos/efeitos dos fármacos
Feminino
Seres Humanos
Masculino
Meia-Idade
Resultado do Tratamento
[Pt] Tipo de publicação:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
[Nm] Nome de substância:
0 (Pralidoxime Compounds); EC 3.1.1.7 (Acetylcholinesterase); P7MU9UTP52 (pralidoxime)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170104
[St] Status:MEDLINE


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[PMID]:28043415
[Au] Autor:Walton EL
[Ad] Endereço:Staff Writer at the Biomedical Journal, 56 Dronningens Gate, 7012 Trondheim, Norway. Electronic address: ewalton86@gmail.com.
[Ti] Título:Pralidoxime and pesticide poisoning: A question of severity?
[So] Source:Biomed J;39(6):373-375, 2016 Dec.
[Is] ISSN:2320-2890
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In this issue of the Biomedical Journal, we highlight new data supporting the use of pralidoxime in the treatment of cases of organophosphate poisoning, which also suggest that WHO treatment guidelines should be updated. We also learn about a modified surgical technique to repair severe spinal injuries, as well as new insight into the structure of human adenovirus that could inform vaccine development.
[Mh] Termos MeSH primário: Intoxicação por Organofosfatos/tratamento farmacológico
Praguicidas/farmacologia
Compostos de Pralidoxima/uso terapêutico
[Mh] Termos MeSH secundário: Seres Humanos
[Pt] Tipo de publicação:EDITORIAL; INTRODUCTORY JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Pesticides); 0 (Pralidoxime Compounds); P7MU9UTP52 (pralidoxime)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170104
[St] Status:MEDLINE


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[PMID]:27494215
[Au] Autor:Berberich JA; Stouch TR; Manepalli S; Esposito EX; Madura JD
[Ad] Endereço:Department of Chemical, Paper and Biomedical Engineering, College of Engineering and Computing, Miami University , 64 P Engineering Building, 650 East High Street, Oxford, Ohio 45056, United States.
[Ti] Título:Biological Testing of Organophosphorus-Inactivated Acetylcholinesterase Oxime Reactivators Identified via Virtual Screening.
[So] Source:Chem Res Toxicol;29(9):1534-40, 2016 Sep 19.
[Is] ISSN:1520-5010
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:There is a pressing need for new therapeutics to reactivate covalently inactivated acetylcholinesterase (AChE) due to exposure to organophosphorus (OP) compounds. Current reactivation therapeutics (RTs) are not broad-spectrum and suffer from other liabilities, specifically the inability to cross the blood-brain-barrier. Additionally, the chemical diversity of available therapeutics is small, limiting opportunities for structure-activity relationship (SAR) studies to aid in the design of more effective compounds. In order to find new starting points for the development of oxime-containing therapeutic reactivators and to increase our base of knowledge, we have employed a combination of computational and experimental procedures to identify additional compounds with the real or potential ability to reactivate AChE while augmenting and complementing current knowledge. Computational methods were used to identify previously uninvestigated oxime-containing molecules. Experimentally, six compounds were found with reactivation capabilities comparable to, or exceeding, those of 2-pralidoxime (2-PAM) against a panel of AChE inactivated by paraoxon, diisopropylfluorophosphate (DFP), fenamiphos, and methamidophos. One compound showed enhanced reactivation ability against DFP and fenamiphos, the least tractable of these OPs to be reactivated.
[Mh] Termos MeSH primário: Acetilcolinesterase/química
Acetilcolinesterase/metabolismo
Simulação por Computador
Compostos Organofosforados/química
Oximas/química
[Mh] Termos MeSH secundário: Bases de Dados de Compostos Químicos
Ativação Enzimática/efeitos dos fármacos
Eritrócitos/enzimologia
Seres Humanos
Estrutura Molecular
Compostos Organofosforados/farmacologia
Oximas/farmacologia
Compostos de Pralidoxima/química
Compostos de Pralidoxima/farmacologia
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Organophosphorus Compounds); 0 (Oximes); 0 (Pralidoxime Compounds); EC 3.1.1.7 (Acetylcholinesterase)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170714
[Lr] Data última revisão:
170714
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160806
[St] Status:MEDLINE
[do] DOI:10.1021/acs.chemrestox.6b00198


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[PMID]:27450532
[Au] Autor:Karade HN; Raviraju G; Acharya BN; Valiveti AK; Bhalerao U; Acharya J
[Ad] Endereço:Process Technology Development Division, Defence Research & Development Establishment, Jhansi Road, Gwalior 474002, India.
[Ti] Título:Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE).
[So] Source:Bioorg Med Chem;24(18):4171-4176, 2016 Sep 15.
[Is] ISSN:1464-3391
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Previously (Karade et al., 2014), we have reported the synthesis and in vitro evaluation of bis-pyridinium derivatives of pyridine-3-yl-(2-hydroxyimino acetamide), as reactivators of sarin and VX inhibited hAChE. Few of the molecules showed superior in vivo protection efficacy (mice model) (Kumar et al., 2014; Swami et al., 2016) in comparison to 2-PAM against DFP and sarin poisoning. Encouraged by these results, herein we report the synthesis and in vitro evaluation of isonicotinamide derivatives of pyridine-3-yl-(2-hydroxyimino acetamide) (4a-4d) against sarin and VX inhibited erythrocyte ghost hAChE. Reactivation kinetics of these compounds was studied and the determined kinetic parameters were compared with that of commercial reactivators viz. 2-PAM and obidoxime. In comparison to 2-PAM and obidoxime, oxime 4a and 4b exhibited enhanced reactivation efficacy toward sarin inhibited hAChE while oxime 4c showed far greater reactivation efficacy toward VX inhibited hAChE. The acid dissociation constant and IC50 values of these oximes were determined and correlated with the observed reactivation potential.
[Mh] Termos MeSH primário: Acetamidas/química
Aminopiridinas/química
Reativadores da Colinesterase/química
Niacinamida/análogos & derivados
Niacinamida/química
Oximas/química
[Mh] Termos MeSH secundário: Acetamidas/síntese química
Aminopiridinas/síntese química
Inibidores da Colinesterase/química
Reativadores da Colinesterase/síntese química
Membrana Eritrocítica/enzimologia
Seres Humanos
Cinética
Niacinamida/síntese química
Cloreto de Obidoxima/química
Compostos Organotiofosforados/química
Oximas/síntese química
Compostos de Pralidoxima/química
Sarina/química
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Acetamides); 0 (Aminopyridines); 0 (Cholinesterase Inhibitors); 0 (Cholinesterase Reactivators); 0 (Organothiophosphorus Compounds); 0 (Oximes); 0 (Pralidoxime Compounds); 25X51I8RD4 (Niacinamide); 3HXR312Z9M (Obidoxime Chloride); 9A4381183B (VX); B4XG72QGFM (Sarin); P7MU9UTP52 (pralidoxime)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170812
[Lr] Data última revisão:
170812
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160725
[St] Status:MEDLINE


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[PMID]:27432237
[Au] Autor:Snider TH; Babin MC; Jett DA; Platoff GE; Yeung DT
[Ad] Endereço:Battelle, USA.
[Ti] Título:Toxicity and median effective doses of oxime therapies against percutaneous organophosphorus pesticide and nerve agent challenges in the Hartley guinea pig.
[So] Source:J Toxicol Sci;41(4):511-21, 2016.
[Is] ISSN:1880-3989
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Anticholinesterases, such as organophosphorus pesticides and warfare nerve agents, present a significant health threat. Onset of symptoms after exposure can be rapid, requiring quick-acting, efficacious therapy to mitigate the effects. The goal of the current study was to identify the safest antidote with the highest therapeutic index (TI = oxime 24-hr LD50/oxime ED50) from a panel of four oximes deemed most efficacious in a previous study. The oximes tested were pralidoxime chloride (2-PAM Cl), MMB4 DMS, HLö-7 DMS, and obidoxime Cl2. The 24-hr median lethal dose (LD50) for the four by intramuscular (IM) injection and the median effective dose (ED50) were determined. In the ED50 study, male guinea pigs clipped of hair received 2x LD50 topical challenges of undiluted Russian VX (VR), VX, or phorate oxon (PHO) and, at the onset of cholinergic signs, IM therapy of atropine (0.4 mg/kg) and varying levels of oxime. Survival was assessed at 3 hr after onset clinical signs. The 3-hr 90th percentile dose (ED90) for each oxime was compared to the guinea pig pre-hospital human-equivalent dose of 2-PAM Cl, 149 µmol/kg. The TI was calculated for each OP/oxime combination. Against VR, MMB4 DMS had a higher TI than HLö-7 DMS, whereas 2-PAM Cl and obidoxime Cl2 were ineffective. Against VX, MMB4 DMS > HLö-7 DMS > 2-PAM Cl > obidoxime Cl2. Against PHO, all performed better than 2-PAM Cl. MMB4 DMS was the most effective oxime as it was the only oxime with ED90 < 149 µmol/kg against all three topical OPs tested.
[Mh] Termos MeSH primário: Antídotos/farmacologia
Substâncias para a Guerra Química/toxicidade
Inibidores da Colinesterase/toxicidade
Reativadores da Colinesterase/farmacologia
Intoxicação por Organofosfatos/tratamento farmacológico
Compostos Organotiofosforados/toxicidade
Oximas/farmacologia
Praguicidas/toxicidade
[Mh] Termos MeSH secundário: Animais
Antídotos/toxicidade
Atropina/farmacologia
Reativadores da Colinesterase/toxicidade
Relação Dose-Resposta a Droga
Cobaias
Dose Letal Mediana
Masculino
Antagonistas Muscarínicos/farmacologia
Cloreto de Obidoxima/farmacologia
Cloreto de Obidoxima/toxicidade
Intoxicação por Organofosfatos/etiologia
Oximas/toxicidade
Compostos de Pralidoxima/farmacologia
Compostos de Pralidoxima/toxicidade
Compostos de Piridínio/farmacologia
Compostos de Piridínio/toxicidade
Fatores de Tempo
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antidotes); 0 (Chemical Warfare Agents); 0 (Cholinesterase Inhibitors); 0 (Cholinesterase Reactivators); 0 (Muscarinic Antagonists); 0 (Organothiophosphorus Compounds); 0 (Oximes); 0 (Pesticides); 0 (Pralidoxime Compounds); 0 (Pyridinium Compounds); 0 (S-(N,N-diethylaminoethyl) isobutyl methylphosphothiolate); 120103-35-7 (HLo 7); 3HXR312Z9M (Obidoxime Chloride); 61444-84-6 (N,N'-monomethylenebis(pyridiniumaldoxime)); 7C0697DR9I (Atropine); 9A4381183B (VX); P7MU9UTP52 (pralidoxime)
[Em] Mês de entrada:1704
[Cu] Atualização por classe:170410
[Lr] Data última revisão:
170410
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160720
[St] Status:MEDLINE
[do] DOI:10.2131/jts.41.511



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