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Temephos, an organophosphate larvicide for residential use: a review of its toxicity

Juan Pablo Martínez-Mercado, Adolfo Sierra‐Santoyo, Francisco Alberto Verdín-Betancourt, Aurora Elizabeth Rojas‐García, Betzabet Quintanilla‐Vega

2022Critical Reviews in Toxicology18 citationsDOI

Abstract

Temephos (O,O,O',O′-tetramethyl O,O′-thiodi-p-phenylene bis(phosphorothioate)) is a larvicide belonging to the family of organophosphate pesticides used for the control of different vectors of diseases, such as dengue, Zika, chikungunya, and dracunculiasis. The aim of this review was to discuss the available published information about temephos toxicokinetics and toxicity in mammals. Temephos is quickly absorbed in the gastrointestinal tract, distributed to all organs, and then it accumulates mainly in adipose tissue. It is metabolized by S-oxidation, oxidative desulfuration, and hydrolysis reactions, with the possible participation of cytochrome P450 (CYP). Temephos is mainly eliminated by feces, whereas some of its metabolites are eliminated by urine. The World Health Organization classifies it as class III: slightly dangerous with a NOAEL (no-observed adverse effect level) of 2.3 mg/kg/day for up to 90 days in rats, based on brain acetylcholinesterase (AChE) inhibition. A LOAEL (lowest observable adverse effect level) of 100 mg/kg/day for up to 44 days in rats was proposed based on cholinergic symptoms. However, some studies have shown that temephos causes toxic effects in mammals. The inhibition of the enzyme acetylcholinesterase (AChE) is one of its main demonstrated effects; however, this larvicide has also shown genotoxic effects and some adverse effects on male reproduction and fertility, as well as liver damage, even at low doses. We performed an extensive review through several databases of the literature about temephos toxicokinetics, and we recommend to revisit current assessment of temephos with the new available data.

Topics & Concepts

ToxicodynamicsAcetylcholinesteraseLarvicideToxicokineticsOrganophosphateToxicologyToxicityPharmacologyNo-observed-adverse-effect levelCarbamateIvermectinPharmacokineticsPesticideAedes aegyptiMedicineBiologyVeterinary medicineInternal medicineEnzymeLarvaBiochemistryAgronomyBotanyPesticide Exposure and ToxicityCholinesterase and Neurodegenerative DiseasesEnvironmental Toxicology and Ecotoxicology