Weak inhibitors protect cholinesterases from strong inhibitors (paraoxon): in vitro effect of tiapride

Weak and reversible inhibitors of cholinesterases, when administered before potent organophosphorus inhibitors (pretreatment), have the ability, to a certain extent, to protect enzymes from inhibition. Such a protective effect was demonstrated in vitro for metoclopramide and ranitidine. The putative mode of protective action of these substances is, when administered in excess, competition for the active site of the enzyme with the more potent organophosphate. The present paper presents results using another benzamide with weak cholinesterase inhibitory properties: tiapride (TIA).

[1]  G. Petroianu Organophosphate poisoning: the lesser-known face of a toxidrome. , 2005, European journal of emergency medicine : official journal of the European Society for Emergency Medicine.

[2]  K. Arafat,et al.  Weak Inhibitors Protect Cholinesterases from Stronger Inhibitors (Dichlorvos): In Vitro Effect of Tiapride , 2005, International journal of toxicology.

[3]  K. Arafat,et al.  In vitro protection of plasma cholinesterases by metoclopramide from inhibition by mipafox , 2004, Journal of applied toxicology : JAT.

[4]  R. Hoffman,et al.  Nerve Agents: A Comprehensive Review , 2004, Journal of intensive care medicine.

[5]  A. Saleh,et al.  In vitro protection of red blood cell acetylcholinesterase by metoclopramide from inhibition by organophosphates (paraoxon and mipafox) , 2003, Journal of applied toxicology : JAT.

[6]  A. Saleh,et al.  Metoclopramide protection of cholinesterase from paraoxon inhibition. , 2003, Veterinary and human toxicology.

[7]  M. Eddleston,et al.  Oximes in acute organophosphorus pesticide poisoning: a systematic review of clinical trials. , 2002, QJM : monthly journal of the Association of Physicians.

[8]  H. Cheng,et al.  The power issue: determination of KB or Ki from IC50. A closer look at the Cheng-Prusoff equation, the Schild plot and related power equations. , 2001, Journal of pharmacological and toxicological methods.

[9]  G. Petroianu,et al.  High‐dose intravenous paraoxon exposure does not cause organophosphate‐induced delayed neuropathy (OPIDN) in mini pigs , 2001, Journal of applied toxicology : JAT.

[10]  A. Woolf,et al.  Combined evidence-based literature analysis and consensus guidelines for stocking of emergency antidotes in the United States. , 2000, Annals of emergency medicine.

[11]  T. Marrs,et al.  EVALUATION OF ANTIDOTES FOR POISONING BY ORGANOPHOSPHORUS PESTICIDES , 2000 .

[12]  J. Peter,et al.  Organic Insecticides , 2000, Anaesthesia and intensive care.

[13]  L. Karalliedde Organophosphorus poisoning and anaesthesia , 1999, Anaesthesia.

[14]  P. Eyer,et al.  Improved determination of acetylcholinesterase activity in human whole blood. , 1999, Clinica chimica acta; international journal of clinical chemistry.

[15]  A. Petroianu,et al.  Control of blood pressure, heart rate and haematocrit during high‐dose intravenous paraoxon exposure in mini pigs , 1998, Journal of applied toxicology : JAT.

[16]  H. Schild,et al.  SOME QUANTITATIVE USES OF DRUG ANTAGONISTS , 1997, British journal of pharmacology and chemotherapy.

[17]  J. Jeyaratnam Acute pesticide poisoning: a major global health problem. , 1994, World health statistics quarterly. Rapport trimestriel de statistiques sanitaires mondiales.

[18]  D. Faulds,et al.  Tiapride. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in geriatric agitation. , 1993, Drugs & aging.

[19]  E. Rey,et al.  Pharmacokinetics of tiapride and absolute bioavailability of three extravascular forms. , 1982, International journal of clinical pharmacology, therapy, and toxicology.

[20]  J. Fontaine,et al.  The effects of substituted benzamides on frog rectus abdominis. , 1980, European journal of pharmacology.

[21]  D. Grob,et al.  Poisoning due to organophosphate insecticides. Acute and chronic manifestations. , 1971, The American journal of medicine.

[22]  W G ZIJLSTRA,et al.  Standardization of hemoglobinometry. II. The hemiglobincyanide method. , 1961, Clinica chimica acta; international journal of clinical chemistry.

[23]  K. Courtney,et al.  A new and rapid colorimetric determination of acetylcholinesterase activity. , 1961, Biochemical pharmacology.

[24]  K. Arafat,et al.  Weak inhibitors protect cholinesterases from strong inhibitors (paraoxon): in vitro effect of ranitidine , 2005, Journal of applied toxicology : JAT.

[25]  M. Eddleston,et al.  Oximes for acute organophosphate pesticide poisoning (Review) , 2005 .

[26]  N. Buckley,et al.  Oximes for acute organophosphate pesticide poisoning. , 2005, The Cochrane database of systematic reviews.

[27]  G. Petroianu,et al.  In vitroprotection of plasma cholinesterases by metoclopramide from inhibition by paraoxon: METOCLOPRAMIDE IN ORGANOPHOSPHATE (PARAOXON) POISONING , 2003 .

[28]  G. Petroianu,et al.  In vitro protection of plasma cholinesterases by metoclopramide from inhibition by paraoxon , 2003, Journal of applied toxicology : JAT.

[29]  F. Sidell,et al.  PRETREATMENT FOR NERVE AGENT EXPOSURE , 1999 .

[30]  T. Namba Cholinesterase inhibition by organophosphorus compounds and its clinical effects. , 1971, Bulletin of the World Health Organization.