Pharmacokinetic profile and efficacy against Ctenocephalides felis felis and Rhipicephalus sanguineus administered orally in Beagles dogs
Phenylpyrazoles, Oral, Pharmacokinetics, Dose, Efficacy, Ectoparasites.
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 as a medicine for oral administration has become promising. The effectiveness of FIP against the flea Ctenocephalides felis felis and the tick Rhipicephalus sanguineus and its pharmacokinetics and its main active metabolite, fipronil sulfone (SULF), were evaluated after oral administration of tablets in three different doses (2, 4 and 6 mg/kg) in Beagle dogs, in a single treatment. Through the plasma concentration curves it was possible to observe that the FIP showed rapid absorption and metabolization and slow elimination. The values of Cmax (β = 0.7653) and AUC0-t (β = 0.3209) did not increase proportionally with increasing dose. At 48h after treatment, doses of 4 mg/kg (AUC0-t = 442.39 ± 137.35 µg/mL*h) and 6 mg/kg (AUC0-t = 421.32 ± 102.84 µg/mL*h) provided 100% and 99% efficacy for fleas and 95% and 98% for ticks, respectively. The estimated EC90 for FIP + SULF was 1.30 µg/mL for C. felis felis and 2.16 µg/mL for R. sanguineus. The correlation of the FIP pharmacokinetic and efficacy data demonstrated its potential to be administered orally in the form of tablets for the control of ectoparasites in dogs, as a safer alternative for animals, humans and environment, aligned with the One Health concept.