Efficacious Oxime for Organophosphorus Poisoning: A
Minireview
Syed M Nurulain
Department of Pharmacology and Therapeutics, Faculty of
Medicine and Health Sciences, United Arab Emirates
University, PO Box 17666, AlAin, United Arab Emirate
For correspondence:
E-mail:
nurulain@uaeu.ac.ae
Tel: 009713-7137141
Received: 18 August
2010 Revised
accepted: 27 April 2011
Tropical
Journal of Pharmaceutical Research, June 2011;
10(3):
341-349
doi:
10.4314/tjpr.v10i3.10
Abstract
Oximes are well known as
acetylcholinesterase reactivators and are used in
organophosphorus poisoning to reactivate inhibited
acetylcholinesterase. Therapeutically available oximes,
namely, pralidoxime (2-PAM), obidoxime, trimedoxime and
Hagedorn oxime (HI-6), have no broad-spectrum activity
against structurally different kinds of organophosphorus
anticholinesterases. The widely used oxime, 2-PAM, is
least effective. The focus of the review is to find an
oxime that is broad spectrum and superior to the
presently available oximes for the treatment of
organophosphorus poisoning. Numerous oxime-based
reactivators have been synthesized - in laboratories in
Croatia, United States of America, Israel and most
recently in Czech Republic. Some experimental oximes
synthesized in Czech Republic and named as K-series of
oximes have been found promising. Among them, K-27 and
K-48 have higher or comparable efficacy to all available
oximes though it is not effective against all
organophosphorus (OP) nerve agents. They are also
efficacious in pretreatment protocol for OP
anticholinesterases. K-27 oxime is a promising candidate
to replace therapeutically available oximes with respect
to insecticide/pesticide organophosphorus poisoning. K27
and K48 may be candidates to replace the only approved
pretreatment drug, pyridostigmine, in military combat
medicine for OP nerve agent.
Keywords:
K-oximes, K-27 and K-48
oxime, Bispyridinium aldoxime, Acetylcholinesterase
reactivators, OPC poisoning.