Abstract:
BACKGROUND:Reversible cholinesterase inhibitors, when given prophylactically before exposure to organophosphates, are able to decrease organophosphate-induced mortality. However, the efficacy of pyridostigmine, the only pre-treatment substance approved by the US Federal Drug Administration, is unsatisfactory. METHODS:In search of a better prophylactic compound, we determined in vivo the protection conferred by five cholinesterase inhibitors (ranitidine, physostigmine, tacrine, K-27 and pyridostigmine), which were administered in equitoxic dosage (1/4 of LD01) 30 minutes before exposure to the organophosphate dicrotophos. Efficacy was measured in rats by Cox analysis calculating the relative risk of death (RR), RR being 1 for the reference group which received dicrotophos and no prophylaxis. RESULTS:K-27 (RR=0.06), physostigmine (RR=0.15), pyridostigmine (RR=0.22) and tacrine (RR=0.28) significantly (p ≤ 0.05) reduced dicrotophos-induced mortality in comparison to the reference group (dicrotophos without pre-treatment), whereas ranitidine (RR=0.86) had no significant influence. The experimental oxime K-27, when given before dicrotophos exposure, conferred the best in vivo protection. This was significantly (p ≤ 0.05) more efficacious than pre-treatment with any other tested compound. The differences in efficacy between the second best compound, physostigmine, and the less efficacious substances (tacrine and pyridostigmine) were also statistically significant. CONCLUSION:These data indicate that K-27 can be considered a very efficacious prophylactic agent for organophosphate exposure.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Lorke DE,Nurulain SM,Hasan MY,Kuca K,Petroianu GAdoi
10.2174/1381612822666161027154303subject
Has Abstractpub_date
2017-01-01 00:00:00pages
3432-3439issue
23eissn
1381-6128issn
1873-4286pii
CPD-EPUB-79334journal_volume
23pub_type
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journal_title:Current pharmaceutical design
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