Oral pharmacokinetic profile of fipronil and efficacy against flea and tick in dogs.

Autor: Dos Santos GCM; Post graduation Program of Veterinary Science, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Scott FB; Animal Parasitology Department, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Campos DR; Post graduation Program of Veterinary Science, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Magalhães VS; Animal Parasitology Department, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Borges DA; Post graduation Program of Veterinary Science, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Miranda FR; Post graduation Program of Veterinary Science, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Alves MCC; Post graduation Program of Veterinary Science, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Pereira GA; Post graduation Program of Veterinary Science, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Moreira LO; Post graduation Program of Veterinary Science, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Lima EAS; Post graduation Program of Veterinary Science, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Rocha MBDS; Post graduation Program of Veterinary Science, Veterinary Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil., Cid YP; Pharmaceutical Science Department, Health and Biological Science Institute, Federal Rural University of Rio de Janeiro, Seropédica, RJ, Brazil.
Jazyk: angličtina
Zdroj: Journal of veterinary pharmacology and therapeutics [J Vet Pharmacol Ther] 2022 Jan; Vol. 45 (1), pp. 23-33. Date of Electronic Publication: 2021 Jul 31.
DOI: 10.1111/jvp.13004
Abstrakt: Fipronil (FIP) is an ectoparasiticide of the phenylpyrazole class, used in veterinary medicine in topical form. Supported by evidence of uncontrolled human exposure to FIP and environmental damage caused by commercially available formulations, its use by oral administration has become promising. The effectiveness of FIP against the flea Ctenocephalides felis felis and the tick Rhipicephalus sanguineus and its pharmacokinetics and main active metabolite, fipronil sulfone (SULF) were evaluated after single oral administration of tablets in three different doses (2, 4, and 6 mg/kg) in dogs. Through the plasma concentration curves, it was possible to observe that the FIP showed rapid absorption and metabolization and slow elimination. The values of C max (β = 0.7653) and AUC 0- t (β = 0.3209) did not increase proportionally with increasing dose. At 48 h after treatment, doses of 4 mg/kg (AUC 0- t  = 442.39 ± 137.35 µg/ml*h) and 6 mg/kg (AUC 0- t  = 421.32 ± 102.84 µg/ml*h) provided 100% and 99% efficacy against fleas, and 95% and 98% against ticks, respectively. The estimated EC 90 of FIP +SULF was 1.30 µg/ml against C. felis felis and 2.16 µg/ml against R. sanguineus. The correlation between the FIP pharmacokinetic and efficacy data demonstrated its potential for oral administration in the form of tablets for the control of ectoparasites in dogs, as a safer alternative for animals, humans, and the environment, aligned with the One Health concept.
(© 2021 John Wiley & Sons Ltd.)
Databáze: MEDLINE
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