Flavia Valladao Thiesen (1), Helena M.T. Barros (2,*), Mario Tannhauser
(2) and Semiramis L. Tannhauser (2)
(1) Center of Applied Toxicology, Pontificia Universidade Catolica do Rio Grande do Sul, Av. Ipiranga, 6681 -Predio 12, Porto Alegre, 90619-900 Brazil
(2) Division of Pharmacology, Fundacao Faculdade Federal de Ciencias Medicas de Porto Alegre, Sarmento Leite, 245-Porto Alegre, 90050-170 Brazil
(*) To whom correspondence should be addressed.
Abstract: Early assessment of neurological and behavioral effects is extremely valuable for early identification of intoxications because preventive measures can be taken against more severe or chronic toxic consequences. The time course of the effects of an oral dose of the anticholinesterase agent propoxur (8.3 mg/kg) was determined on behaviors displayed in the open-field and during an active avoidance task by rats and on blood and brain cholinesterase activity. Maximum inhibition of blood cholinesterase was observed within 30 min after administration of propoxur. The half-life of enzyme-activity recovery was estimated to be 208.6 min. Peak brain cholinesterase inhibition was also detected between 5 and 30 min of the pesticide administration, but the half-life for enzyme activity recovery was much shorter, in the range of 85 min. Within this same time interval of the enzyme effects, diminished motor and exploratory activities and decreased performance of animals in the active avoidance task were observed. Likewise, behavioral normalization after propoxur followed a time frame similar to that of brain cholinesterase. These data indicate that behavioral changes that occur during intoxication with low oral doses of propoxur may be dissociated from signs characteristic of cholinergic over-stimulation but accompany brain cholinesterase activity inhibition.
Keywords: Propoxur, Anticholinesterase agent, Behavioral toxicology, Pharmacokinetics, Cholinesterase