Medical treatment of acute poisoning with organophosphorus and carbamate pesticides

Jokanović, Milan

doi:10.1016/j.toxlet.2009.07.025

Cited by 195 publications

(134 citation statements)

References 41 publications

Supporting

Mentioning

130

Contrasting

Unclassified

Order By: Relevance

“…This inhibition leads to accumulation of the neurotransmitter acetylcholine, causing interruption of nervous impulses in the synapses (Eyer 2003). Exposure to even small amounts of an OPs compound can be fatal; death is generally caused by respiratory failure (Jokanović 2009).…”

Section: Introductionmentioning

confidence: 99%

Potential cytotoxic effect of Anilofos by using Allium cepa assay

et al. 2014

View full text Add to dashboard Cite

Cytogenetic effects of Anilofos which was widely used in agriculture, was evaluated in Allium cepa root meristematic cells. In the Allium root growth inhibition test EC 50 value was determined 50 ppm and 1/29 EC 50 (25 ppm), EC 50 (50 ppm) and 2 9 EC 50 (100 ppm) concentrations of Anilofos were applied to onion roots. A negative and positive control were used in the experiment in parallel. According to results mitotic index decreased with increasing the Anilofos concentrations in all application groups and each exposure time, while disturbed anaphase-telophase, choromosome laggard(s), stickiness and anaphase bridge(s) were observed. In anaphase-telophase cells, c-metaphase, disturbed nucleus and binuclear cells were observed in other anomalies. The results were also analyzed statistically by using Dunnett t test (2-tailed) and all concentrations of Anilofos were found significant.

show abstract

Section: Introductionmentioning

confidence: 99%

Potential cytotoxic effect of Anilofos by using Allium cepa assay

et al. 2014

View full text Add to dashboard Cite

show abstract

“…Increased ACh overstimulates muscarinic and nicotinic receptors, resulting in peripheral muscarinic (salivation, lacrymation, nausea, bradycardia, bronchosecretion), nicotinic (skeletal muscle fasciculations, diaphragm and intercostal paralysis) and central (muscle tremors, convulsions, coma and respiratory depression) manifestations that lead to death [7][8][9] . Current antidotal regimens approved for human treatment of OP poisoning consist of a combination of muscarinic receptor antagonists (atropine), anticonvulsants (benzodiazepines) and AChE reactivators (oximes), such as obidoxime, 2-PAM, TMB-4 and HI-6 10,11 . These oximes have a high affinity for AChE and have strong nucleophilic character.…”

Section: Introductionmentioning

confidence: 99%

In vitro evaluation of neutral oximes as reactivators of parathion-inhibited electric eel acetylcholinesterase

et al. 2017

View full text Add to dashboard Cite

Organophosphorus (OP) compounds are irreversible inhibitors of acetylcholinesterase (AChE) commonly used as pesticides and, unfortunately, as nerve agents in terrorist attacks. These compounds are highly soluble easily crossing the blood-brain barrier (BBB). Clinically, oximes such as pralidoxime and obidoxime are used for the reactivation of AChE. These oximes are not effective to reactivate AChE inhibited by different OPs besides the fact that they are permanently charged and do not readily cross the BBB. This work evaluated the ability of ten neutral oximes to reactivate parathion-inhibited eel AChE. Because oximes can bind to AChE as reversible inhibitors, this property was also evaluated, with pralidoxime (2-PAM) used as a reference compound. Unlike 2-PAM, which inhibited AChE in a concentration-dependent way, neutral oximes did not follow the linear order of AChE inhibition. Neutral ligands can present affinity for the periferic anionic site (PAS) site. Neutral oximes 1 and 2 (200 µM) reactivated parathion-inhibited eel AChE by 9 per cent and 11 per cent, respectively; but neither of them surpassed the reactivation efficacy of 2-PAM (25 per cent). Neutral oximes 1 and 2 reactivated AChE at a safe concentration for humans. Both neutral oximes 1 and 2 are good non-quaternary moieties for the synthesis of conjugates with enhanced reactivation potency and BBB penetration.Keywords: Acetylcholinesterase; Eel AChE; Reactivator; Oxime; Pralidoxime; Parathion RESEARCH PAPERDefence Life Science Journal, Vol. 2, No. 3, July 2017, pp. 363-369, DOI : 10.14429 LIMA, et al.: DEf. LIfE SCI. J., VOL. 2, NO. 3, JULy 2017, DOI : 10.14429/dlsj.2.10730 or allosteric) 14 . Although approved as antidotes, these oximes are not sufficiently effective to reactivate AChE inhibited by the different OPs 15,16 . The mono-quaternary oxime 2-PAM is very efficient in reactivating AChE inhibited with sarin or VX 17 but is not effective against tabun or soman 18 . Obidoxime is the most potent and most efficacious oxime in reactivating AChE inhibited by various classes of OP insecticides and tabun, but was inferior to oxime HI-6 against soman, sarin, cyclosarin and VX 19. A significant drawback to these oximes is they are permanently charged and do not readily cross the blood brain barrier (BBB) 20 . As a result, they show only limited activity in the CNS, which is a major target of OPs. Thus, effective reactivators as antidotes are increasingly needed against a broader spectrum of nerve agents 21 . Introducing non-quaternary organic compounds has been a novel method of efficiently penetrate the BBB for reactivation of brain AChE 22. Non-charged oximes have previously been developed with improved BBB penetration [23][24][25][26][27][28][29] and sufficient reactivation of AChE inhibited by nerve agents and insecticides 24,30 . Even with improved BBB penetration and reactivation of AChE, the specific oxime structures with superior reactivating potency to those in use remain unknown.The work proposed here evaluated the ability of...

show abstract

“…Carbamate compounds are generally called anticholinesterases. In the presence of inhibitors, acetylcholinesterase becomes progressively inhibited and is not further capable of hydrolyzing acetylcholine to choline and acetic acid (Jokanovic 2009;Jokanovic and Maksimovic 1997). The acute toxicity of the different carbamates ranges from highly toxic to only slightly toxic or non-toxic (IPCS 1986).…”

Section: Introductionmentioning

confidence: 99%

Mutagenic and cytotoxic activities of benfuracarb insecticide

et al. 2014

View full text Add to dashboard Cite

Benfuracarb is a carbamate insecticide used to control insect pests in vegetables and it has anti-acetylcholinesterase activity lower than other carbamates. Cytotoxic effects of benfuracarb were evaluated by using root growth inhibition (EC 50 ), mitotic index (MI), and mitotic phase determinations on the root meristem cells of Allium cepa and mutagenic effects were determined in Salmonella typhymurium Ames test by TA98 and TA100 strains with and without metabolic activation. In Allium test, 1 % DMSO was used as negative control group and 10 ppm MMS was used as positive control group. 75 ppm concentration of benfuracarb was found as EC 50 . In MI and mitotic phases determination study, 37.5, 75 and 150 ppm doses of benfuracarb were used. Dose-dependent cytotoxic activity was found by root growth inhibition and MI studies. It was identified that mitotic inhibition activity of benfuracarb was higher than 10 ppm MMS. In Ames test, mutagenic activity was not observed and over 200 lg/plate of benfuracarb was determined as cytotoxic to S. typhymurium strains. Benfuracarb can be called as ''mitotic inhibitor'' but not called as mutagen.

show abstract

Medical treatment of acute poisoning with organophosphorus and carbamate pesticides

Cited by 195 publications

References 41 publications

Potential cytotoxic effect of Anilofos by using Allium cepa assay

Potential cytotoxic effect of Anilofos by using Allium cepa assay

In vitro evaluation of neutral oximes as reactivators of parathion-inhibited electric eel acetylcholinesterase

Mutagenic and cytotoxic activities of benfuracarb insecticide

Contact Info

Product

Resources

About