Fluazuron orally administered to guinea pigs: pharmacokinetic and efficacy against Amblyomma sculptum

Abstract

Background: Brazilian spotted fever (BSF), the most lethal tick-borne disease in the Western Hemisphere, is caused by the bacterium Rickettsia rickettsii and transmitted by the bite of Amblyomma sculptum. Capybaras are considered primary hosts of this tick and amplifier hosts of R. rickettsii, generating new infected lineages of A. sculptum in BSF-endemic areas. To define a possible treatment regimen for controlling the tick A. sculptum in capybaras, the aim of this study was to establish an effective fluazuron (FLU) dose to control A. sculptum larvae in artificially infested guinea pigs. Methods: In Study I (pharmacokinetic and pharmacodynamic analysis), 24 guinea pigs were divided into four equal groups: control group (CG; untreated) and treated groups receiving FLU administered by gavage in three doses: G1—1 mg/kg, G2—5 mg/kg and G3—10 mg/kg, once a day for 15 days (d0 to d + 14). Blood samples were collected from the animals of the treated groups before and at d + 1, + 2, + 4, + 7, + 15 and + 21. The guinea pigs were artificially infested at d + 7 with A. sculptum larvae, and specimens were recovered at d + 11 to d + 14 and kept in a climatized chamber for 14 days. In Study II (evaluation of pharmacokinetic parameters), one group of eight animals received FLU administered by gavage in a single dose of 10 mg/kg, and blood samples were collected before and on day 0 (8 h after treatment), + 1, + 4, + 7, + 15, + 21 and + 28 after single FLU administration. FLU was analyzed in plasma samples by high-performance liquid chromatography with ultraviolet detection. Results: FLU plasma concentrations increased quickly, indicating rapid absorption, and decreased slowly. Some larvae from all treated groups exhibited morphological and behavioral changes. FLU interfered in molting, and the efficacy obtained was 100% for all treated groups. Conclusions: The results offer promising perspectives for the development of a palatable feed cube containing FLU for free-living capybaras to control A. sculptum and also to prevent BSF in areas where capybaras have been shown to play a primary role.