Pro: Oximes should be used routinely in organophosphate poisoning.
acetylcholinesterase
obidoxime
organophosphate poisoning
oximes
pralidoxime
Journal
British journal of clinical pharmacology
ISSN: 1365-2125
Titre abrégé: Br J Clin Pharmacol
Pays: England
ID NLM: 7503323
Informations de publication
Date de publication:
12 2022
12 2022
Historique:
revised:
25
10
2021
received:
05
08
2021
accepted:
02
11
2021
pubmed:
14
1
2022
medline:
18
11
2022
entrez:
13
1
2022
Statut:
ppublish
Résumé
In poisoning with organophosphorus compounds (OP), patients can only profit from the regeneration of acetylcholinesterase, when the poison load has dropped below a toxic level. Every measure that allows an increase of synaptic acetylcholinesterase (AChE) activity at the earliest is essential for timely termination of the cholinergic crisis. Only drug-induced reactivation allows fast restoration of the inhibited AChE. Obidoxime and pralidoxime have proved to be able to reactivate inhibited cholinesterase thereby saving life of poisoned animals. A plasma level of obidoxime or pralidoxime allowing reactivation in humans poisoned by OP can be adjusted. There is no doubt that obidoxime and pralidoxime are able to reactivate OP-inhibited AChE activity in poisoned patients, thereby increasing AChE activity and contributing substantially to terminate cholinergic crisis. Hence, a benefit may be expected when substantial reactivation is achieved. A test system allowing determination of red blood cell AChE activity, reactivatability, inhibitory equivalents and butyrylcholinesterase activity is available for relatively low cost. If any reactivation is possible while inhibiting equivalents are present, oxime therapy should be maintained. In particular, when balancing the benefit risk assessment, obidoxime or palidoxime should be given as soon as possible and as long as a substantial reactivation may be expected.
Substances chimiques
pralidoxime
P7MU9UTP52
Oximes
0
Obidoxime Chloride
3HXR312Z9M
Acetylcholinesterase
EC 3.1.1.7
Cholinesterase Reactivators
0
Butyrylcholinesterase
EC 3.1.1.8
Cholinesterase Inhibitors
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
5064-5069Informations de copyright
© 2022 The Authors. British Journal of Clinical Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.
Références
Grob D, Garlick WL, Harvey AM. The toxic effects in man of the anticholinesterase insecticide parathion (p-nitrophenyl diethyl thionophosphate). Johns Hopkins Hosp Bull. 1950;87:106-129.
Holmstedt B. Pharmacology of organophosphorus cholinesterase inhibitors. Pharmacol Rev. 1959;11:567-688.
Grob D, Lilienthal JL, Harvey AM, et al. The administration of di-isopropyl fluorophosphate (DFP) to man. I. Effect on plasma and erythrocyte cholinesterase; general systemic effects; use in study of hepatic function and erythropoiesis; and some properties of plasma cholinesterase. Johns Hopkins Hosp. Bull. 1947;81:217-244.
Eddleston M. Novel clinical toxicology and pharmacology of organophosphorus insecticide self-poisoning. Annu Rev Pharmacol Toxicol. 2019;59(1):341-360.
Eyer P. The role of oximes in the management of organophosphorus pesticide poisoning. Toxicol Rev. 2003;22(3):165-190.
Willems J, Belpaire FM. Anticholinesterase poisoning: an overview of pharmacotherapy. In: Ballantyne B, Marrs TC, eds. Clinical and experimental toxicology of organophosphates and carbamates. Oxford: Butterworth Heinemann; 1992:543-554.
Grubic Z, Sketelj J, Klinar B, et al. Recovery of acetylcholinesterase in the diaphragm, brain, and plasma of the rat after irreversible inhibition by soman: A study of cytochemical localization and molecular forms of the enzyme in the motor end plate. J Neurochem. 1981;37(4):909-916.
Grob D, Harvey JC. Effects in man of the anticholinesterase compound sarin (isopropyl methyl phosphonofluoridate). J Clin Invest. 1958;37(3):350-368.
Sidell FR, Groff WA. The reactivatibility of cholinesterase inhibited by VX and sarin in man. Toxicol Appl Pharmacol. 1974;27(2):241-252.
Brank M, Zajc-Kreft K, Kreft S, Komel R, Grubic Z. Biogenesis of acetylcholinesterase is impaired, although its mRNA level remains normal, in the glucocorticoid-treated rat skeletal muscle. Eur J Biochem. 1998;251(1-2):374-381.
Thiermann H, Mast U, Klimmek R, et al. Cholinesterase status, pharmacokinetics and laboratory findings during obidoxime therapy in organophosphate poisoned patients. Hum Exp Toxicol. 1997;16(8):473-480.
Eyer F, Meischner V, Kiderlen D, et al. Human parathion poisoning. A toxicokinetic analysis. Toxicol Rev. 2003;22(3):143-163.
Philippa E. Factors influencing organophosphate toxicity in humans. In: Karalliedde L, Feldman S, Henry J, et al., eds. Organophosphates and Health. London: Imperial College Press; 2001:61-81.
Willems JL, de Bisschop HC, Verstraete AG, et al. Cholinesterase reactivation in organophosphorus poisoned patients depends on the plasma concentrations of the oxime pralidoxime methylsulphate and of the organophosphate. Arch Toxicol. 1993;67(2):79-84.
Boelcke G, Butigan N, Davar H, Erdmann W, Gaaz J, Nenner M. New experiences in the toxicologically controlled therapy of an unusually serious poisoning with nitrostigmine (E605 forte). Dtsch Med Wochenschr. 1970;95(50):2516-2521.
Mahieu P, Hassoun A, van Binst R, Lauwerys R, Deheneffe Y. Severe and prolonged poisoning by fenthion. Significance of the determination of the anticholinesterase capacity of plasma. Journal of Toxicology. Clin Toxicol. 1982;19(5):425-432.
Braeckman RA, Godefroot MG, Blondeel GM, Belpaire FM, Willems JL. Kinetic analysis of the fate of methyl parathion in the dog. Arch Toxicol. 1980;43(4):263-271.
Eigenberg DA, Pazdernik TL, Doull J. Hemoperfusion and pharmacokinetic studies with methamidophos in the rat. Fundam Appl Toxicol. 1983;3(6):496-501.
Eigenberg DA, Pazdernik TL, Doull J. Hemoperfusion and pharmacokinetic studies with parathion and paraoxon in the rat and dog. Drug Metab Dispos. 1983;11(4):366-370.
Peña-Egido MJ, Rivas-Gonzalo JC, Mariño-Hernandez EL. Toxicokinetics of parathion in the rabbit. Arch Toxicol. 1988;61(3):196-200.
Nielsen P, Friis C, Gyrd-Hansen N, Kraul I. Disposition of parathion in neonatal and young pigs. Pharmacol Toxicol. 1991;69(4):233-237.
Thiermann H, Szinicz L, Eyer F, et al. Modern strategies in therapy of organophosphate poisoning. Toxicol Lett. 1999;107(1-3):233-239.
Noort D, Benschop HP, Black RM. Biomonitoring of exposure to chemical warfare agents: A review. Toxicol Appl Pharmacol. 2002;184(2):116-126.
Hrabetz H, Thiermann H, Felgenhauer N, et al. Organophosphate poisoning in the developed world - a single centre experience from here to the millennium. Chem Biol Interact. 2013;206(3):561-568.
Kamat SR, Heera S, Potdar PV, Shah SV, Bhambure NM, Mahashur AA. Bombay experience in intensive respiratory care over 6 years. J Postgrad Med. 1989;35(3):123-134.
Dive A, Mahieu P, van Binst R, et al. Unusual manifestations after malathion poisoning. Hum Exp Toxicol. 1994;13(4):271-274.
Worek F, Thiermann H, Szinicz L, Eyer P. Kinetic analysis of interactions between human acetylcholinesterase, structurally different organophosphorus compounds and oximes. Biochem Pharmacol. 2004;68(11):2237-2248.
Worek F, Thiermann H, Wille T. Oximes in organophosphate poisoning: 60 years of hope and despair. Chem Biol Interact. 2016;259(Pt B):93-98.
Worek F, Thiermann H, Wille T. Organophosphorus compounds and oximes: A critical review. Arch Toxicol. 2020;94(7):2275-2292.
Eyer P, Kiderlen D, Meischner V, et al. The current status of oximes in the treatment of OP poisoning - comparing two regimes. Clin Toxicol. 2003;41(4):441-443.
Herkert NM, Lallement G, Clarençon D, Thiermann H, Worek F. Comparison of the oxime-induced reactivation of rhesus monkey, swine and guinea pig erythrocyte acetylcholinesterase following inhibition by sarin or paraoxon, using a perfusion model for the real-time determination of membrane-bound acetylcholinesterase activity. Toxicology. 2009;258(2-3):79-83.
Herkert NM, Aurbek N, Eyer P, Thiermann H, Worek F. Comparative study of oxime-induced reactivation of erythrocyte and muscle AChE from different animal species following inhibition by sarin or paraoxon. Toxicol Lett. 2010;194(3):94-101.
Herkert NM, Thiermann H, Worek F. In vitro kinetic interactions of pyridostigmine, physostigmine and soman with erythrocyte and muscle acetylcholinesterase from different species. Toxicol Lett. 2011;206(1):41-46.
Gonder S, Seeger T, Worek F, et al. Interspecies differences in pharmacotherapy of peripheral respiratory arrest after exposure with tabun. Naunyn-Schmiedeberg's Arch Pharmacol. 2009;379(Suppl 1):69.
Worek F, Aurbek N, Wille T, Eyer P, Thiermann H. Kinetic analysis of interactions of paraoxon and oximes with human, Rhesus monkey, swine, rabbit, rat and guinea pig acetylcholinesterase. Toxicol Lett. 2011;200(1-2):19-23.
Worek F, Reiter G, Eyer P, Szinicz L. Reactivation kinetics of acetylcholinesterase from different species inhibited by highly toxic organophosphates. Arch Toxicol. 2002;76(9):523-529.
Luo C, Tong M, Chilukuri N, Brecht K, Maxwell DM, Saxena A. An in vitro comparative study on the reactivation of nerve agent-inhibited guinea pig and human acetylcholinesterases by oximes. Biochemistry. 2007;46(42):11771-11779.
Clement JG, Erhardt N. In vitro oxime-induced reactivation of various molecular forms of soman-inhibited acetylcholinesterase in striated muscle from rat, monkey and human. Arch Toxicol. 1994;68(10):648-655.
Aurbek N, Thiermann H, Szinicz L, Eyer P, Worek F. Analysis of inhibition, reactivation and aging kinetics of highly toxic organophosphorus compounds with human and pig acetylcholinesterase. Toxicology. 2006;224(1-2):91-99.
Thiermann H, Aurbek N, Worek F. Treatment of nerve agent poisoning. In: Franz W, John J, Horst T, eds. Chemical warfare toxicology: Management of poisoning. Cambridge, UK: The Royal Society of Chemistry; 2016:1-42.
Willems JL. In: Szinicz L, Eyer P, Klimmek R, eds. Pralidoxime methylsulphate in the treatment of organophosphorus poisoning. Heidelberg, Berlin, Oxford: Spektrum Akademischer Verlag; 1996:69-73.
Thiermann H, Worek F, Kehe K. Limitations and challenges in treatment of acute chemical warfare agent poisoning. Chem Biol Interact. 2013;206(3):435-443.
Sundwall A. Minimum concentrations of N-methylpyridinium-2-aldoxime methane sulphonate (P2S) which reverse neuromuscular block. Biochem Pharmacol. 1961;8(4):413-417.
Anderson JM, Petersson KJ, Friberg LE, Worek F, Thiermann H, Buckley NA. Acute Organophosphorus poising in humans: A PK model for chlorpyrifos. Toxicol Lett. 2012;211:S173.
Eyer P, Thiermann H, Worek F, et al. The role of atropine and oximes in the treatment of organophosphorus insecticide poisoning. Clin Toxicol. 2005;43(5):447-448.
Eyer F, Worek F, Eyer P, et al. Obidoxime in acute organophosphate poisoning: 1 - clinical effectiveness. Clin Toxicol. 2009;47(8):798-806.
Eddleston M, Buckley NA, Eyer P, Dawson AH. Management of acute organophosphorus pesticide poisoning. Lancet. 2008;371(9612):597-607.
Herkert NM, Freude G, Kunz U, Thiermann H, Worek F. Comparative kinetics of organophosphates and oximes with erythrocyte, muscle and brain acetylcholinesterase. Toxicol Lett. 2012;209(2):173-178.
Massoulié J, Pezzementi L, Bon S, Krejci E, Vallette FM. Molecular and cellular biology of cholinesterases. Prog Neurobiol. 1993;41(1):31-91.
Herkert NM, Eckert S, Eyer P, et al. Identical kinetics of human erythrocyte and muscle acetylcholinesterase with respect to carbamate pre-treatment, residual activity upon soman challenge and spontaneous reactivation after withdrawal of the inhibitors. Toxicology. 2008;246(2-3):188-192.
Thiermann H, Szinicz L, Eyer P, et al. Correlation between red blood cell acetylcholinesterase activity and neuromuscular transmission in organaphosphate poisoning. Chem Biol Interact. 2005;157158:345-347.
Thiermann H, Zilker T, Eyer F, Felgenhauer N, Eyer P, Worek F. Monitoring of neuromuscular transmission in organophosphate pesticide-poisoned patients. Toxicol Lett. 2009;191(2-3):297-304.
Worek F, Szinicz L, Eyer P, et al. Evaluation of oxime efficacy in nerve agent poisoning: Development of a kinetic-based dynamic model. Toxicol Appl Pharmacol. 2005;209(3):193-202.
Eyer F, Eyer P. Enzyme-based assay for quantification of paraoxon in blood of parathion poisoned patients. Hum Exp Toxicol. 1998;17(12):645-651.
Thiermann H, Eyer F, Felgenhauer N, et al. Pharmacokinetics of obidoxime in patients poisoned with organophosphorus compounds. Toxicol Lett. 2010;197(3):236-242.
Eyer P, Worek F, Thiermann H, Eddleston M. Paradox findings may challenge orthodox reasoning in acute organophosphate poisoning. Chem Biol Interact. 2010;187(1-3):270-278.
Eddleston M, Eyer P, Worek F, et al. Pralidoxime in acute organophosphorus insecticide poisoning-a randomised controlled trial. PLoS Med. 2009;6(6):e1000104.
Namba T, Hiraki K. PAM (pyridine-2-aldoxime methiodide) therapy for alkylphosphate poisoning. Jama. 1958;166(15):1834-1839.
Besser R, Weilemann LS, Gutmann L. Efficacy of obidoxime in human organophosphorus poisoning: Determination by neuromuscular transmission studies. Muscle Nerve. 1995;18(1):15-22.
Seeger T, Niessen KV, Langer P, et al. Restoration of nerve agent inhibited muscle force production in human intercostal muscle strips with HI 6. Toxicol Lett. 2011;206(1):72-76.
Thiermann H, Worek F, Eyer P, Eyer F, Felgenhauer N, Zilker T. Obidoxime in acute organophosphate poisoning: 2 - PK/PD relationships. Clin Toxicol. 2009;47(8):807-813.
Sidell FR. Nerve Agents. In: Zajtchuck R, Bellamy RF, eds. Textbook of military medicine: Medical aspects of chemical and biological warfare. United States of America: Office of The Surgeon General, Department of the Army; 1997 Chapter 5.
Thiermann H, Seeger T, Gonder S, et al. Assessment of neuromuscular dysfunction during poisoning by organophosphorus compounds. Chem Biol Interact. 2010;187(1-3):265-269.
Pawar KS, Bhoite RR, Pillay CP, Chavan SC, Malshikare DS, Garad SG. Continuous pralidoxime infusion versus repeated bolus injection to treat organophosphorus pesticide poisoning: A randomised controlled trial. Lancet. 2006;368(9553):2136-2141.
Thiermann H, Szinicz L, Eyer P, Felgenhauer N, Zilker T, Worek F. Lessons to be learnt from organophosphorus pesticide poisoning for the treatment of nerve agent poisoning. Toxicology. 2007;233(1-3):145-154.
Worek F, Backer M, Thiermann H, et al. Reappraisal of indications and limitations of oxime therapy in organophosphate poisoning. Hum Exp Toxicol. 1997;16(8):466-472.
Amend N, Langgartner J, Siegert M, et al. A case report of cholinesterase inhibitor poisoning: Cholinesterase activities and analytical methods for diagnosis and clinical decision making. Arch Toxicol. 2020;94(6):2239-2247.
Amend N, Niessen KV, Seeger T, Wille T, Worek F, Thiermann H. Diagnostics and treatment of nerve agent poisoning-current status and future developments. Ann N Y Acad Sci. 2020;1479(1):13-28.
Worek F, Eyer P, Aurbek N, Thiermann H. Kinetic analysis of oxime interactions with acetylcholinesterase as a basis for the evaluation of oxime efficacy in organophosphate poisoning. CBC. 2010;6(1):16-22.
Worek F, Thiermann H, Szinicz L. Reactivation and aging kinetics of human acetylcholinesterase inhibited by organophosphonylcholines. Arch Toxicol. 2004;78(4):212-217.
Cochran R, Kalisiak J, Küçükkilinç T, et al. Oxime-assisted acetylcholinesterase catalytic scavengers of organophosphates that resist aging. J Biol Chem. 2011;286(34):29718-29724.
Worek F, Schilha M, Neumaier K, et al. On-site analysis of acetylcholinesterase and butyrylcholinesterase activity with the ChE check mobile test kit-Determination of reference values and their relevance for diagnosis of exposure to organophosphorus compounds. Toxicol Lett. 2016;249:22-28.
Aurbek N, Thiermann H, Worek F. Kinetic in vitro analysis of the eligibility of plasma butyrylcholinesterase as therapeutic marker in oxime-treated organophosphorus poisoning. Naunyn-Schmiedeberg's Arch Pharmacol. 2009;379(Suppl 1):69.
Bartling A, Worek F, Szinicz L, Thiermann H. Enzyme-kinetic investigation of different sarin analogues reacting with human acetylcholinesterase and butyrylcholinesterase. Toxicology. 2007;233(1-3):166-172.
Zujalovic B, Mayer B, Hafner S, Balling F, Barth E. AChE-activity in critically ill patients with suspected septic encephalopathy: a prospective single-centre study. BMC Anesthesiol. 2020;20(1):287. https://doi.org/10.1186/s12871-020-01204-6