Vergiftungen mit esteraseblockierenden Insecticiden aus der Gruppe der organischen Phosphorsäure-Ester (E 605 und Verwandte)

Erdmann, W. D.; Lendle, L.

doi:10.1007/978-3-642-94724-7_3

Cited by 16 publications

(2 citation statements)

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“…For equal degrees of enzyme reactivation the quantity of pyridine-2-aldoxime methiodide required when a di-isopropylphosphoryl group is involved, as for instance in poisoning with dyflos (di-isopropyl phosphorofluoridate), is 20 to 30 times higher than that necessary for the treatment of poisoning with parathion, ethyl pyrophosphate (TEPP) or paraoxon where a diethylphosphoryl group is involved. The dose of pyridine-2-aldoxime methiodide used and recommended by Namba and Hiraki (1958) Since organophosphorus insecticides are used widely and cases of poisoning have frequently been reported (Pribilla, 1955;Holmes and Gaon, 1956;Conley, 1957;Maresch, 1957;Erdmann and Lendle, 1958;Namba and Hiraki, 1958;Quinby and Lemmon, 1958) (Hobbiger, 1957b). Reactivation was studied in the Warburg apparatus, allowing 30 min.…”

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Protection Against Lethal Organophosphate Poisoning by Quaternary Pyridine Aldoximes

Hobbiger

Sadler

1959

British Journal of Pharmacology and Chemotherapy

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The effect of 18 pyridinium aldoximes on diethylphosphoryl-acetocholinesterase in vitro and the protection against lethal poisoning by ethyl pyrophosphate (TEPP) in mice pretreated with 0.095 m.mole/kg. of these oximes was investigated. Monoximes and dioximes of polymethylenebispyridinium compounds were studied in greater detail since they were up to 22 times more potent than pyridine-2-aldoxime methiodide (2-hydroxyiminomethyl-N-methylpyridinium iodide) in reactivating diethylphosphoryl-acetocholinesterase in vitro and protected mice against lethal poisoning by up to 15 LD100 of ethyl pyrophosphate. These oximes were also up to 52 times more potent than pyridine-2-aldoxime methiodide in reactivating di-isopropylphosphorylacetocholinesterase in vitro and were effective in preventing lethal poisoning by dyflos (di-isopropyl phosphorofluoridate). The antidotal action against diethyl phosphostigmine (Ro 3-0340) was even greater than that against ethyl pyrophosphate. Some of the most effective oximes had antidotal actions in poisoning by ethyl pyrophosphate, diethyl phosphostigmine and dyflos when given in 0.0095 m.mole/kg. and this effect was enhanced by 1 mg./kg. atropine sulphate. In vivo reactivation of diethylphosphoryl-acetocholinesterases by 0.0095 or 0.095 m.mole/kg. of oximes of polymethylenebispyridinium compounds was demonstrated in blood but not in brain. Atropine-like and neuromuscular blocking activities were studied on isolated organs and protection against lethal doses of neostigmine and related anticholinesterases were also investigated. Some of the oximes of polymethylenebispyridinium compounds have, relative to pyridine-2-aldoxime methiodide, a higher therapeutic ratio in mice and considerably greater water-solubility. The possible advantages to be gained from their use in preference to pyridine-2-aldoxime methiodide are discussed.The interaction between anticholinesterases of the organophosphate type and acetocholinesterase (also often referred to as true cholinesterase or acetylcholinesterase) yields phosphorylated acetocholinesterase which is enzymatically inactive and in many instances has a half-life ranging from several days to weeks. While cholinesterase is in a phosphorylated form acetylcholine accumulates and thus the administration of organophosphates is followed by muscarinic and nicotinic symptoms of acetylcholine poisoning.

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Protection Against Lethal Organophosphate Poisoning by Quaternary Pyridine Aldoximes

Hobbiger

Sadler

1959

British Journal of Pharmacology and Chemotherapy

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“…Due to the wide spread and the easy access to the substance a large number of acute intoxications caused by accidental poisoning or deliberate poisoning to commit suicide are seen [2]. OPC toxicologically act as blocking agents for cholinesterases (ChE) and lead to endogenic acetylcholine overflow, which results in hyperactivity of the peripheral and central cholinergic system [3]. Acute symptoms of poisoning result from these effects.…”

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Effect of Organophosphorus Compound Intoxication on Auditory Brainstem Response in Mini Pigs

Bergler¹,

Juncker²,

Petroianu

et al. 1996

ORL

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Organophosphorus compounds (OPC) are widely used as insecticides and cause a high number of acute and chronic intoxications in man. Their toxico logical properties lead among others to disturbances of the central nervous system. Hearing disturbances have been reported after chronic exposure to OPC, and changes in bioelectric brain activity have been observed during the acute state of intoxication. The EEG showed no characteristic alterations. We performed a threshold auditory brainstem response (ABR) in 12 mini pigs before, during and after paraoxon (a typical OPC) intoxication with a high dose of 27 mg/kg BW. During the application of paraoxon we saw a prolongation of the interpeak latencies Jewett I-V of approximately 1 ms. A threshold shift of 10–20 dB was seen in 8 animals. After the application, while the systemic effect of the paraoxon intoxication was still apparent, the threshold shift disappeared except for 2 animals and the prolongation of the interpeak latencies could not be observed any more. No characteristic signs of paraoxon intoxication could be seen in the ABR after the application was completed. Acute intoxication with an OPC only leads to temporary, limited hearing impairment and increased interpeak latency. We could not observe characteristic changes in the ABR corresponding to the state of intoxication.

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Acetylcholin-Esterase

Engelhard¹,

Nenner²,

Prchal³

1967

Angew. Chem.

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Abhangigkeit von deren Zusammensetzung studieren. Auch heterogene Reaktionen in elektrochemischen ZeIlen lassen sich so gut verfolgen. Fragen zur Elektronen-und Raumstruktur gasformiger Molekule konnen rnit der Massenspektrometrie nicht unmittelbar angegangen werden. Allerdings hat die Massenspektrometrie zur Identifizierung von Partikeln bei Molekularstrahlexperimenten im magnetischen oder elektrischen Feld schon vie1 beigetragen [1471. Vielversprechend sind Kombinationen optischer mit massenspektrometrischen Untersuchungen unter Einbeziehnng von Mikrowellen-und Matrix-Techniken [1481, desgleichen Kombinationen mit

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Vergiftungen mit esteraseblockierenden Insecticiden aus der Gruppe der organischen Phosphorsäure-Ester (E 605 und Verwandte)

Cited by 16 publications

References 130 publications

Protection Against Lethal Organophosphate Poisoning by Quaternary Pyridine Aldoximes

Protection Against Lethal Organophosphate Poisoning by Quaternary Pyridine Aldoximes

Effect of Organophosphorus Compound Intoxication on Auditory Brainstem Response in Mini Pigs

Acetylcholin-Esterase

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