Toxicokinetics of temephos after oral administration to adult male rats.

Temephos (Tem) is the larvicide of choice to control mosquito transmission of dengue, Zika, and chikungunya. The toxicokinetic and toxicological information of temephos is very limited. The aim of this work was to determine the toxicokinetics and dosimetry of temephos and its metabolites. Male Wistar rats were orally administered temephos (300 mg/kg) emulsified with saline solution and sacrificed over time after dosing. Temephos and its metabolites were analyzed in blood and tissues by high performance liquid chromatography-diode array detector. At least eleven metabolites were detected, including temephos-sulfoxide (Tem-SO), temephos-oxon (Tem-oxon), temephos-oxon-sulfoxide (Tem-oxon-SO), temephos-oxon-SO-monohydrolyzed (Tem-oxon-SO-OH), 4,4´-thiodiphenol, 4,4´-sulfinyldiphenol, and 4,4´-sulfonyldiphenol or bisphenol S (BPS). The mean blood concentrations of temephos were fitted to a one-compartment model for kinetic analysis. At 2 h, the peak was reached (t1/2 abs = 0.38 h), and only trace levels were detected at 36 h (t1/2 elim = 8.6 h). Temephos was detected in all tissues and preferentially accumulated in fat. Temephos-sulfone-monohydrolyzed (Tem-SO2-OH) blood levels remained constant until 36 h and gradually accumulated in the kidney. Tem-oxon was detected in the brain, liver, kidney, and fat. Clearance from the liver and kidney were 7.59 and 5.52 ml/min, respectively. These results indicate that temephos is well absorbed, extensively metabolized, widely distributed and preferentially stored in adipose tissue. It is biotransformed into reactive metabolites such as Tem-oxons, Tem-dioxons, and BPS. Tem-SO2-OH, the most abundant metabolite of temephos, could be used as an exposure biomarker for toxicokinetic modeling. These results could provide critical insight into the dosimetry and toxicity of temephos and its metabolites.

Resistance to temephos and deltamethrin in Aedes aegypti from Brazil between 1985 and 2017.

BACKGROUND: Aedes aegypti populations in Brazil have been subjected to insecticide selection pressures with variable levels and sources since 1967. Therefore, the Brazilian Ministry of Health (MoH) coordinated the activities of an Ae. aegypti insecticide resistance monitoring network (MoReNAa) from 1999 to 2012. OBJECTIVES: The objective of this study was to consolidate all information available from between 1985 and 2017 regarding the resistance status and mechanisms of Brazilian Ae. aegypti populations against the main insecticide compounds used at the national level, including the larvicide temephos (an organophosphate) and the adulticide deltamethrin (a pyrethroid). METHODS: Data were gathered from two sources: a bibliographic review of studies published from 1985 to 2017, and unpublished data produced by our team within the MoReNAa between 1998 and 2012. A total of 146 municipalities were included, many of which were evaluated several times, totalling 457 evaluations for temephos and 274 for deltamethrin. Insecticide resistance data from the five Brazilian regions were examined separately using annual records of both the MoH supply of insecticides to each state and the dengue incidence in each evaluated municipality. FINDINGS: Ae. aegypti resistance to temephos and deltamethrin, the main larvicide and adulticide, respectively, employed against mosquitoes in Brazil for a long time, was found to be widespread in the country, although with some regional variations. Comparisons between metabolic and target-site resistance mechanisms showed that one or another of these was the main component of pesticide resistance in each studied population. MAIN CONCLUSIONS: (i) A robust dataset on the assessments of the insecticide resistance of Brazilian Ae. aegypti populations performed since 1985 was made available through our study. (ii) Our findings call into question the efficacy of chemical control as the sole methodology of vector control. (iii) It is necessary to ensure that sustainable insecticide resistance monitoring is maintained as a key component of integrated vector management. (iv) Consideration of additional parameters, beyond the supply of insecticides distributed by the MoH or the diverse local dynamics of dengue incidence, is necessary to find consistent correlations with heterogeneous vector resistance profiles.

Avaliaçäo da açäo residual do larvicida temephós sobre o Aedes aegypti(Diptera, Culicidae)em diferentes tipos de recipientes / Evaluation of the residual action of the larvicide temephos over Aedes aegypti(Diptera-Culicidae)in different types of containers

A açäo residual do larvicida Temephós aegypti foi avaliada através do teste de duas concentraçöes do produto - 1 ppm(400mg/l) e (2 ppm(800mg/l) - distribuidas, respectivamente, em 06 diferentes recipientes - pneu, vaso de barro, bacia de alumínio, aquário de vidro, bacia de plástico e caixa de amianto -, todas com volume constante de 04 litros. Em cada recipiente, foram colocadas 20 larvas de 3§ estádio de Aedes aegypti, avaliadas após 24 horas de exposiçäo ao produto e em seguida retiradas da soluçäo. Essa mesma soluçäo foi mantida por 14 semanas e os testes repetidos a cada 07 dias. A mortalidade das larvas foi o critério utilizado para avaliar a açäo residual do larvicida. A eficácia foi de 100 por cento para os recipientes vaso de barro, bacia de alumínio, aquário de vidro, bacia de plástico e caixa de amianto, durante todo o período do teste, nas duas concentraçöes; no pneu, houve queda de 45 por cento na concentraçäo de 800mg/l a partir da 7ª semana, decrescendo a partir daí, até näo ocorrer mortalidade no último teste

Preliminary trials using abate to control Kabowra flies in the Rupununi, Guyana - abstract

Control of Simulium (called Kabowras in Guyana) black flies is usually directed to the larvae which breed in fast flowing waters. The purpose of the project was to determine the effectiveness of Abate Insecticide 200E in controlling Simulium sp., in a selected river in the Rupununi Savannah, Guyana. Two bioassays were carried out on the San Jose River near Lethem, Rupununi to determine the effective distance of Abate 200E at a concentration of 0.3 ppm during August, 1979 along a 2.4 km and 3.5 km stretch of the river. River discharge rates were calculated at a point of injection of the Abate. The volume of Abate required to give a concentration of 0.3 ppm when dispensed over approximatelty thirty minutes at the measured discharge was dripped into the stream. Counts of larvae on marked vegetation were made at several points before injection of Abate and four and nineteen hours after injection. The results of the first bioassay over 2.4 km showed at 57.8 percent drop in larvae four hours after injection of larvicide and a 99.3 percent drop within nineteen hours. Larval mortality was 97 percent at 2.4 km. Larval counts after the second Abate application two weeks later at 3.5 km showed a 52.8 percent drop after four hours and 96.1 percent after nineteen hours. Larval mortality was 100 percent at 2.7 km and 9.3 percent at 3.5 km. Larval counts were very low during the subsequent four weeks. Abate 200E at a concentration of 0.3 ppn was found to be effective in killing Simulium larvae over a distance of 3.5 km with a mortality of 93 percent nineteen hours after injection of larvicide. These trials should continue using lower concentrations of the larvicide (AU)