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oxime, poisoning, organophosphate

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https://www.readbyqxmd.com/read/29129799/post-exposure-treatment-with-the-oxime-rs194b-rapidly-reactivates-and-reverses-advanced-symptoms-of-lethal-inhaled-paraoxon-in-macaques
#1
Yvonne J Rosenberg, Jerry Wang, Tara Ooms, Narayanan Rajendran, Lingjun Mao, Xiaoming Jiang, Jonathan Lees, Lori Urban, Jeremiah Romper, Yadire Sepulveda, Yan-Jye Shyong, Palmer Taylor
Fatalities from organophosphate (OP) insecticide result from both occupational and deliberate exposure; significantly impacting human health. Like nerve agents, insecticides are neurotoxins which target and inhibit acetylcholinesterases (AChE) in central and peripheral synapses in the cholinergic nervous system. Post-exposure therapeutic countermeasures generally include administration of atropine with a pyridinium aldoximes e.g. pralidoxime, to reactivate the OP-inhibited AChE. However, commonly used oximes inefficiently cross the blood brain barrier and are rapidly cleared and their benefit is debated...
November 9, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/29062551/in-vitro-cysteine-reactivates-organophosphate-insecticide-dichlorvos-inhibited-human-cholinesterases
#2
Hamidreza Mohammadi, Jafar Jalilian, Mohammad Y Karimi, Seyed V Shetab-Boushehri
OBJECTIVES: Organophosphate (OP) pesticides inhibit both red blood cell (RBC) and plasma cholinesterases (ChEs). Oximes, especially pralidoxime (2-PAM), are widely used as antidotes to treat OP poisoning. In addition, N-acetylcysteine (NAC) is sometimes used as an adjuvant antidote. The current study aimed to assess the feasibility of using NAC as a single therapeutic agent for OP poisoning in comparison to in vitro 2-PAM. METHODS: This study was carried out at the Razi Drug Research Center of Iran University of Medical Sciences, Tehran, Iran, between April and September 2014...
August 2017: Sultan Qaboos University Medical Journal
https://www.readbyqxmd.com/read/28743514/precision-cut-lung-slices-as-test-system-for-candidate-therapeutics-in-organophosphate-poisoning
#3
Julia Herbert, Horst Thiermann, Franz Worek, Timo Wille
Standard therapeutic options in organophosphate (OP) poisoning are limited to the administration of atropine and oximes, a regimen often lacking in efficacy and applicability. Treatment alternatives are needed, preferably covering a broad spectrum of OP intoxications. Although recent research yielded several promising compounds, e.g. bioscavengers, modulators of the muscarinic acetylcholine (ACh) receptor or bispyridinium non-oximes, these substances still need further evaluation, especially regarding effects on the potentially lethal respiratory symptoms of OP poisoning...
August 15, 2017: Toxicology
https://www.readbyqxmd.com/read/28722512/in-silico-and-in-vitro-evaluation-of-two-novel-oximes-k378-and-k727-in-comparison-to-k-27-and-pralidoxime-against-paraoxon-ethyl-intoxication
#4
Maria Arshad, Muhammad Qaiser Fatmi, Kamil Musilek, Alamdar Hussain, Kamil Kuca, Georg Petroianu, Huba Kalasz, Syed Muhammad Nurulain
Organophosphate (OP) poisoning is a major global health issue; while compounds from this group have been used intensively over the last century, an effective antidote is still lacking. Oxime-type acetylcholinesterase (AChE) reactivators are used to reactivate the OP inhibited AChE. Pralidoxime is the only US Food and Drug Administration approved oxime for therapeutic use but its efficacy has been disappointing. Two novel oximes (K378 and K727) were investigated in silico and in vitro and compared with an experimental oxime (kamiloxime; K-27) and pralidoxime...
August 4, 2017: Toxicology Mechanisms and Methods
https://www.readbyqxmd.com/read/28693885/post-exposure-treatment-with-the-oxime-rs194b-rapidly-reverses-early-and-advanced-symptoms-in-macaques-exposed-to-sarin-vapor
#5
Yvonne J Rosenberg, Lingjun Mao, Xiaoming Jiang, Jonathan Lees, Limin Zhang, Zoran Radic, Palmer Taylor
Organophosphate (OP) nerve agents and pesticides trigger a common mechanism of neurotoxicity resulting from critical targeting and inhibition of acetylcholinesterases (AChE) in central and peripheral synapses in the cholinergic nervous system. Therapeutic countermeasures have thus focused on either administering an oxime post-exposure, that can rapidly reactivate OP-inhibited AChE, or by preventing OP poisoning through administering pre-exposure treatments that scavenge OPs before they inhibit their physiological AChE targets...
August 25, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28652853/protection-studies-of-new-bis-quaternary-2-hydroxyimino-n-pyridin-3yl-acetamide-derivatives-hnk-series-oximes-against-acute-poisoning-by-dichlorvos-ddvp-in-swiss-albino-mice
#6
Pravin Kumar, Devyani Swami, Hitendra N Karade, Manindar Singh, Anupma Tiwari, Kshetra Pal Singh
The available antidotal therapy against acute poisoning by organophosphates involves the use of atropine alone or in combination with one of the oximes, e.g. 2-PAM, Obidoxime, TMB-4 or HI-6. Each of these oximes has some limitation, raising the question of the universal antidotal efficacy against poisoning by all OPs/nerve agents. In the present study, newly synthesized bis quaternary 2-(hydroxyimino)-N-(pyridin-3yl) acetamide derivatives (HNK-series) oximes were evaluated for their antidotal efficacy against DDVP intoxicated Swiss mice, in terms of the Protection Index (PI) and AChE reactivation in brain and serum...
December 2016: Interdisciplinary Toxicology
https://www.readbyqxmd.com/read/28296779/efficacy-of-fresh-packed-red-blood-transfusion-in-organophosphate-poisoning
#7
RANDOMIZED CONTROLLED TRIAL
Hang-Xing Bao, Pei-Jian Tong, Cai-Xia Li, Jing Du, Bing-Yu Chen, Zhi-Hui Huang, Ying Wang
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...
March 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/27896325/utilization-of-plasmapheresis-for-organophosphate-intoxication-a-case-report
#8
Nezihat Rana Disel, Ayca Acikalin, Zeynep Kekec, Ahmet Sebe
Organophosphate (OP) compounds are extremely toxic chemicals that may be absorbed via skin, conjunctiva, gastrointestinal and respiratory systems. Treatment of OP poisoning is a critical and aggressive process which includes decontamination, antidote administration (atropin and oximes), mechanical ventilation support and extracorporeal elimination procedures if needed. Here we present a young female patient who was unintentionally poisoned by an OP (trichlorfon) after using it to moisture her skin. The importance of this patient is the dermal disease that makes her unprotective to dermal exposure of chemicals and application of plasmapheresis to treat her poisoning...
June 2016: Turkish Journal of Emergency Medicine
https://www.readbyqxmd.com/read/27830420/organophosphate-hydrolyzing-enzymes-as-first-line-of-defence-against-nerve-agent-poisoning-perspectives-and-the-road-ahead
#9
REVIEW
A R Satvik Iyengar, Abhay H Pande
Nerve agents (NAs) are extremely neurotoxic synthetic organophosphate (OP) compounds exploited as weapons of mass destruction in terrorist attacks and chemical warfare. Considering the current world scenario, there is a persistent threat of NA-exposure to military personals and civilians. Various prophylactic and post-exposure treatments (such as atropine and oximes) available currently for NA-poisoning are inadequate and unsatisfactory and suffer from severe limitations. Hence, developing safe and effective treatment(s) against NA-poisoning is a critical necessity...
December 2016: Protein Journal
https://www.readbyqxmd.com/read/27396356/in-vitro-characterization-of-pralidoxime-transport-and-acetylcholinesterase-reactivation-across-mdck-cells-and-stem-cell-derived-human-brain-microvascular-endothelial-cells-bc1-hbmecs
#10
Erin Gallagher, Il Minn, Janice E Chambers, Peter C Searson
BACKGROUND: Current therapies for organophosphate poisoning involve administration of oximes, such as pralidoxime (2-PAM), that reactivate the enzyme acetylcholinesterase. Studies in animal models have shown a low concentration in the brain following systemic injection. METHODS: To assess 2-PAM transport, we studied transwell permeability in three Madin-Darby canine kidney (MDCKII) cell lines and stem cell-derived human brain microvascular endothelial cells (BC1-hBMECs)...
July 11, 2016: Fluids and Barriers of the CNS
https://www.readbyqxmd.com/read/27371941/limitations-in-current-acetylcholinesterase-structure-based-design-of-oxime-antidotes-for-organophosphate-poisoning
#11
REVIEW
Andrey Kovalevsky, Donald K Blumenthal, Xiaolin Cheng, Palmer Taylor, Zoran Radić
Acetylcholinesterase (AChE; EC 3.1.1.7), an essential enzyme of cholinergic neurotransmission in vertebrates, is a primary target in acute nerve agent and organophosphate (OP) pesticide intoxication. Catalytically inactive OP-AChE conjugates formed between the active-center serine and phosphorus of OPs can, in principle, be reactivated by nucleophilic oxime antidotes. Antidote efficacy is limited by the structural diversity of OP-AChE conjugates resulting from differences in the structure of the conjugated OP, the different active-center volumes they occupy when conjugated to the active-center serine of AChE, and the distinct chemical characteristics of both OPs and oximes documented in numerous X-ray structures of OP-conjugated AChEs...
August 2016: Annals of the New York Academy of Sciences
https://www.readbyqxmd.com/read/27212759/a-study-of-effectiveness-of-fresh-frozen-plasma-in-organophosphorous-compound-poisoning-in-reducing-length-of-intensive-care-unit-stay-and-in-reducing-need-for-tracheostomy
#12
V P Dayananda, B Bhaskara, G N P Pateel
BACKGROUND: The main stay of treatment in organophophosphorous [OP] poisoning is with atropine, oximes and supportive therapy. Despite the therapy, no improvement in mortality and morbidity. Fresh frozen plasma [FFP] a source of serum cholinesterase act as bio-scavenger to neutralise organophosphate toxins to improve the patients out come. METHODS: The prospective study was conducted in 80 patients with acute OP poisoning. Patients with moderate to severe grade of OP poisoning with serum cholinesterase level <1000 IU/L were included in the study...
May 2016: Anesthesia, Essays and Researches
https://www.readbyqxmd.com/read/27191504/structures-of-paraoxon-inhibited-human-acetylcholinesterase-reveal-perturbations-of-the-acyl-loop-and-the-dimer-interface
#13
Matthew C Franklin, Michael J Rudolph, Christopher Ginter, Michael S Cassidy, Jonah Cheung
Irreversible inhibition of the essential nervous system enzyme acetylcholinesterase by organophosphate nerve agents and pesticides may quickly lead to death. Oxime reactivators currently used as antidotes are generally less effective against pesticide exposure than nerve agent exposure, and pesticide exposure constitutes the majority of cases of organophosphate poisoning in the world. The current lack of published structural data specific to human acetylcholinesterase organophosphate-inhibited and oxime-bound states hinders development of effective medical treatments...
September 2016: Proteins
https://www.readbyqxmd.com/read/27138243/synthesis-and-in-vitro-reactivation-screening-of-imidazolium-aldoximes-as-reactivators-of-sarin-and-vx-inhibited-human-acetylcholinesterase-hache
#14
Rahul Sharma, Bhanushree Gupta, Arvind Kumar Sahu, Jyotiranjan Acharya, Manmohan L Satnami, Kallol K Ghosh
Post-treatment of organophosphate (OP) poisoning involves the application of oxime reactivator as an antidote. Structurally different oximes are widely studied to examine their kinetic and mechanistic behavior against OP-inhibited cholinesterase enzyme. A series of structurally related 1,3-disubstituted-2-[(hydroxyiminomethyl)alkyl]imidazolium halides (5a-5e, 9a-9c) were synthesized and further evaluated for their in-vitro reactivation ability to reactivate sarin- and VX-inhibited human acetylcholinesterase (hAChE)...
November 25, 2016: Chemico-biological Interactions
https://www.readbyqxmd.com/read/27129421/novel-bifunctional-hybrid-small-molecule-scavengers-for-mitigating-nerve-agents-toxicity
#15
Gabriel Amitai, Rellie Gez, Lily Raveh, Nira Bar-Ner, Ettie Grauer, Shira Chapman
The antidotal treatment of organophosphates (OP) nerve agents (NA) poisoning is based on anticholinergics (e.g. atropine) combined with oxime reactivators (e.g. 2PAM) of acetylcholinesterase (AChE). This treatment is symptomatic and does not degrade the OP. New small-molecule OP scavengers were developed as bifunctional hybrids. Their molecular design was based on combining a nucleophile that directly degrades OP with a moiety that reactivates OP-inhibited AChE. The OP degrading moiety is either benzhydroxamic acid (BHA) or 4-pyridinehydroxamic acid (4PHA) coupled via (CH2)n, (n = 1 or 3) to 2PAM...
November 25, 2016: Chemico-biological Interactions
https://www.readbyqxmd.com/read/27125761/oximes-in-organophosphate-poisoning-60-years-of-hope-and-despair
#16
Franz Worek, Horst Thiermann, Timo Wille
The high number of annual fatalities following suicidal poisoning by organophosphorus (OP) pesticides and the recent homicidal use of the chemical warfare nerve agent sarin against civilian population in Syria underlines the continuous threat by these highly toxic agents. The need for an effective treatment of OP poisoning resulted in the implementation of a combination therapy with the muscarinic receptor antagonist atropine and an oxime for the reactivation of OP-inhibited acetylcholinesterase (AChE). Since the invention of the first clinically used oxime pralidoxime (2-PAM) in the 1950s ongoing research attempted to identify more effective oximes...
November 25, 2016: Chemico-biological Interactions
https://www.readbyqxmd.com/read/27125569/mechanistic-studies-of-new-oximes-reactivators-of-human-butyryl-cholinesterase-inhibited-by-cyclosarin-and-sarin
#17
Willian E Amaral de Lima, Ander Francisco, Elaine F F da Cunha, Zoran Radic, Palmer Taylor, Tanos C C França, Teodorico C Ramalho
Butyryl cholinesterase (BChE) has been seen as a key enzyme in the search for new strategies in the treatment of poisoning by organophosphates (OPs), since human BChE (HssBChE), complexed with the appropriate oxime, can be a suitable scavenger and deactivator for OPs in the blood stream. However, the efficacy of HssBChE is limited by its strict stoichiometric scavenging, slow reactivation, and propensity for aging. The improvement of the reactivation rate by new and more efficient oximes could contribute to mitigate this problem and increase the HssBChE efficiency as scavenger...
May 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/27102179/efficacy-of-recommended-prehospital-human-equivalent-doses-of-atropine-and-pralidoxime-against-the-toxic-effects-of-carbamate-poisoning-in-the-hartley-guinea-pig
#18
Matthew K Brittain, Kevin G McGarry, Robert A Moyer, Michael C Babin, David A Jett, Gennady E Platoff, David T Yeung
PURPOSE: Aldicarb and methomyl are carbamate pesticides commonly implicated in human poisonings. The primary toxic mechanism of action for carbamate poisoning is cholinesterase (ChE) inhibition. As such, it is logical to assume that the currently accepted therapies for organophosphate poisoning (muscarinic antagonist atropine and the oxime acetylcholinesterase reactivator pralidoxime chloride [2-PAM Cl]) could afford therapeutic protection. However, oximes have been shown to be contraindicated for poisoning by some carbamates...
May 2016: International Journal of Toxicology
https://www.readbyqxmd.com/read/27101948/oxime-mediated-in-vitro-reactivation-kinetic-analysis-of-organophosphates-inhibited-human-and-electric-eel-acetylcholinesterase
#19
Arvind Kumar Sahu, Rahul Sharma, Bhanushree Gupta, Kamil Musilek, Kamil Kuca, Jyotiranjan Acharya, Kallol K Ghosh
Organophosphate (OP)-based pesticides and nerve agents are highly toxic compounds which interrupt the catalytic mechanism of acetylcholinesterase (AChE) by phosphorylating the hydroxyl moiety of serine residue. The inhibited enzyme can be reactivated by the nucleophilic action of oxime reactivators. To analyze the effect of different AChE sources on reactivation efficacy of reactivators, several in vivo studies have carried out using variety of AChE sources like pig, rat and monkey. Investigations on species differences provide a better insight for the development of new reactivators...
June 2016: Toxicology Mechanisms and Methods
https://www.readbyqxmd.com/read/26899146/emergence-of-catalytic-bioscavengers-against-organophosphorus-agents
#20
REVIEW
Patrick Masson, Sofya V Lushchekina
Bioscavengers are an effective alternative approach for pre- and post-exposure treatments of nerve agent (NA) poisoning. Bioscavengers are natural or recombinant enzymes, reactive proteins, and antibodies that neutralize NAs before they reach their physiological targets. They are administered by injection (protein or gene delivery vector) and react with NAs in the bloodstream. Other ways of delivery can be used: inhalation for pulmonary delivery, topical creams for skin protection, etc. Operational bioscavengers must be producible at low cost, not susceptible to induce immune response and adverse effects, and stable in the bloodstream, upon storage, and under field conditions...
November 25, 2016: Chemico-biological Interactions
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