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In vitro protection of plasma cholinesterases by metoclopramide from inhibition by paraoxon

✍ Scribed by G. Petroianu; F. Kühn; C. Thyes; V. Ewald; A. Missler

Publisher
John Wiley and Sons
Year
2003
Tongue
English
Weight
107 KB
Volume
23
Category
Article
ISSN
0260-437X

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✦ Synopsis

Abstract

Metoclopramide (MCP) is a dopamine receptor antagonist and serotonine receptor agonist widely used as an antiemetic and gastric prokinetic drug. In addition MCP is a reversible inhibitor of cholinesterases from human central nervous system and blood. MCP may have a cholinesterase protective effect against inhibition by organophosphates.

The purpose of the study was to quantify “in vitro” by means of the IC~50~‐shift the extent of MCP conferred protection, using paraoxon (POX) as an inhibitor. POX is a widely used organophospate responsible for a large number of accidental or suicidal exposures.

Cholinesteratic activities (ChE) (with acetyl‐thiocholine (A) and butyryl‐thiocholine (B) as substrates) in human plasma were measured photometrically in the presence of different POX concentrations and IC~50~ was calculated. Determinations were repeated in the presence of increasing MCP concentrations. It appears that the shift induced by the presence of MCP increases with the MCP concentration in a linear manner.

In the presence of a clinically easily achievable plasma concentration of 1 µM MCP the IC~50~ of POX for ChE ‘shifts’ by a factor of ≈2–3. The protective effect of metoclopramide on cholinesterases could be of practical relevance in the treatment of paraoxon poisoning. We conclude that in vivo testing of MCP as an organophosphate protective agent is warranted. Copyright © 2003 John Wiley & Sons, Ltd.

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