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Method for the medicinal prophylaxis of cholinesterase inhibitor intoxication, and active substances and medicaments suitable therefor

A cholinesterase and inhibitor technology, which is applied in the field of pharmacy of organic phosphorus compounds causing poisoning and active components, can solve the problem that physostigmine cannot be approved as a drug and the like

Inactive Publication Date: 2006-03-01
LTS LOHMANN THERAPIE-SYST AG +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, its disadvantage is that physostigmine cannot be approved as a drug

Method used

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  • Method for the medicinal prophylaxis of cholinesterase inhibitor intoxication, and active substances and medicaments suitable therefor
  • Method for the medicinal prophylaxis of cholinesterase inhibitor intoxication, and active substances and medicaments suitable therefor
  • Method for the medicinal prophylaxis of cholinesterase inhibitor intoxication, and active substances and medicaments suitable therefor

Examples

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Embodiment

[0073] In order to show the binding of (S)-N-ethyl-N-methyl-3-[1-(dimethylamino)ethyl]-phenylaminomethyl ester (compound (1)) and scopolamine Preventive properties, protective effects were tested in studies using piglets as an animal model. Plasma levels of both active ingredients in animals were adjusted to fall within ranges corresponding to use in humans.

[0074] In a preliminary trial, 6 mg of (S)-N-ethyl-N-methyl-3-[1-(dimethylamino)ethyl]-phenylaminomethyl ester bitartrate was administered orally in capsule form Piglets (12 kg each) were dosed at random. This caused a 20-40% inhibition of cholinesterase in the blood 2 hours after administration. This range corresponds to the target and inhibition to be achieved in humans. In this context, it must be considered that lower doses are required in humans to achieve better absorption of the active agent. Based on blood cholinesterase inhibitors measured in humans, it can be assumed that treatment with 3 mg BID (ie, a two-...

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Abstract

The present invention discloses (S)-N-ethyl-N-methyl-3-[1-(dimethylamino)ethyl]-phenylcarbamate (1) or one or Various active substances are used for the prophylactic protection of individuals against intoxication by cholinesterase inhibitors.

Description

technical field [0001] The present invention relates to a method for the pharmaceutical prophylaxis of poisoning by cholinesterase inhibitors, especially those of the class of organophosphorus compounds. The invention also relates to active ingredients and medicaments suitable as prophylactic drugs / compositions for such intoxications, in particular medicaments comprising active ingredients from the phenylcarbamate group. The invention also includes the use of said active ingredient for the prevention of said intoxication. Background technique [0002] Compounds having a cholinesterase-inhibiting effect are used on the one hand as insecticides and fungicides for the protection of agricultural crops and, on the other hand, certain compounds of this type are suitable as combat agents or gases in warfare or in terrorist attacks. Whereas the toxic effect in the latter case is deliberate, human poisoning by insecticides or fungicides can be attributed to improper handling, especi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/325A61K31/46
CPCA61K31/46A61K31/325A61P39/02A61P43/00A61K2300/00A61K31/27
Inventor 弗兰克·比彻托马斯·希勒弗兰克·西奥博尔德阿哈龙·莱维
Owner LTS LOHMANN THERAPIE-SYST AG
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