Pharmacokinetics of a fipronil pour-on formulation and its efficacy against Dermacentor nitens (Acari: Ixodidae) in horses.
Abstract: The objective of this study was to standardize a stall-trial methodology for horses in order to evaluate the pharmacokinetics and efficacy of a 1 % fipronil pour-on formulation against Dermacentor nitens. Brazilian pony breed horses were housed in individual stalls within a covered barn and artificially infested with D. nitens larvae on alternate days from day -31 to -1 before treatment. The animals were treated on day 0 with a fipronil 1 % pour-on at a dose of 1 mg/Kg body weight. To determine the therapeutic efficacy, the number of engorged females naturally detached from control and treated groups was recorded for 29 days after treatment. To evaluate the persistent efficacy, further larvae infestations were performed on days 7, 14 and 21 after treatment and tick counts were recorded until day 50. The determination of fipronil and its metabolite fipronil sulfone concentration in the plasma was performed at times of 0, 4 h and on days 1, 2, 7, 12, 14, 15, 16, 21, 28, and 48 after treatment. The overall acaricidal efficacy was 91.83 % from day 1-29. The persistent efficacy was 99.69; 99.19 and 99.32 % against tick infestation challenges performed on days 7, 14 and 21, respectively. In plasma, the Cmax of fipronil was 0.71 ± 0.30 µg/mL on day 7 and 0.27 ± 0.06 µg/mL for fipronil sulfone on day 21. The implementation of a stall trial with horses enables the evaluation of the effectiveness of acaricides against all life stages of ticks without interference from environmental factors. The observed reduction in the number of detached, engorged ticks indicates that Fipronil 1 % pour-on is effective against all parasitic stages present on the animal: larvae, nymphs, and adults. Therefore, fipronil 1 % pour-on is both therapeutically and preventively effective against D. nitens in horses.
Copyright © 2025 Elsevier B.V. All rights reserved.
Publication Date: 2025-12-08 PubMed ID: 41385898DOI: 10.1016/j.vetpar.2025.110674Google Scholar: Lookup
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Summary
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Overview
- This study developed a stall-trial method to test how a 1% fipronil pour-on treatment is absorbed in horses and how effectively it controls the tick species Dermacentor nitens.
- The research demonstrated that the treatment was both therapeutically and preventively effective against larvae, nymphs, and adult ticks on treated horses.
Study Objective and Design
- The primary goal was to standardize a stall-trial methodology to evaluate both the pharmacokinetics (how the drug moves through the horse’s body) and efficacy of a 1% fipronil pour-on formulation against Dermacentor nitens ticks.
- Brazilian pony horses were used, housed individually in covered stalls to control environmental variables.
- These horses were experimentally infested with larvae of D. nitens on alternating days from day -31 up to day -1 before treatment, ensuring all animals had tick exposure prior to treatment.
- On day 0, horses received the fipronil pour-on dose at 1 mg per kilogram of body weight.
Measurement of Treatment Efficacy
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Therapeutic efficacy:
- Involved counting the number of engorged female ticks that naturally detached from both treated and control horses over 29 days post-treatment.
- This measure indicates how well the treatment kills ticks already on the animals.
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Persistent efficacy:
- New larval infestations were performed on days 7, 14, and 21 after treatment to test protection over time.
- Tick counts were recorded up to day 50 to measure how long the treatment remained effective.
Pharmacokinetic Analysis
- Blood plasma samples were collected at various times: before treatment (time 0), 4 hours after, then on days 1, 2, 7, 12, 14, 15, 16, 21, 28, and 48.
- Concentrations of fipronil and its active metabolite fipronil sulfone were measured in plasma.
- Fipronil reached its peak concentration (Cmax) around day 7 with an average of 0.71 ± 0.30 µg/mL.
- Fipronil sulfone peaked later on day 21 with an average concentration of 0.27 ± 0.06 µg/mL.
Results: Efficacy Against Ticks
- The overall acaricidal (tick-killing) efficacy from day 1 to day 29 was approximately 91.83%, indicating a strong immediate effect after treatment.
- Persistent efficacy against tick challenges was:
- 99.69% on day 7 post-treatment
- 99.19% on day 14 post-treatment
- 99.32% on day 21 post-treatment
- These high percentages illustrate sustained protection against new larval infestations for at least three weeks.
Significance of the Stall Trial Methodology
- Housing horses individually in stalls allowed detailed control of tick infestations and minimized outside environmental factors that might affect results.
- This method enabled evaluation of the treatment efficacy against all parasitic stages of the tick—larvae, nymphs, and adults—present on the animals.
- The reduction in detached, engorged ticks demonstrated the treatment’s effectiveness in killing ticks at multiple lifecycle stages.
Conclusions
- The study validated a reliable stall-trial method for testing acaricide efficacy in horses under controlled conditions.
- The 1% fipronil pour-on formulation demonstrated strong therapeutic and preventive efficacy against Dermacentor nitens ticks.
- This formulation can significantly reduce tick infestation burden on horses, protecting animal health over a sustained period after application.
Cite This Article
APA
da Silva Rocha MB, Avelar BR, Martins Dos Santos GC, Ferreira TP, de Sousa Vieira T, de Oliveira GF, Gomes BT, Klafke GM, Correia TR, Cid YP, Scott FB.
(2025).
Pharmacokinetics of a fipronil pour-on formulation and its efficacy against Dermacentor nitens (Acari: Ixodidae) in horses.
Vet Parasitol, 342, 110674.
https://doi.org/10.1016/j.vetpar.2025.110674 Publication
Researcher Affiliations
- Programa de pós-graduação em Ciências Veterinárias, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil.
- Programa de pós-graduação em Ciências Veterinárias, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil. Electronic address: barbararauta@ufrrj.br.
- Programa de pós-graduação em Ciências Veterinárias, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil.
- Departamento de Parasitologia Animal, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil.
- Programa de pós-graduação em Ciência Animal, Zootechnics Institute, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil.
- Programa de pós-graduação em Ciências Veterinárias, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil; Departamento de Parasitologia Animal, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil.
- Departamento de Parasitologia Animal, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil.
- Programa de pós-graduação em Ciências Veterinárias, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil; Instituto de Pesquisas Veterinárias Desidério Finamor, Estrada do Conde, 6000, Eldorado do Sul, RS 92990-000, Brazil.
- Programa de pós-graduação em Ciências Veterinárias, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil; Departamento de Parasitologia Animal, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil.
- Programa de pós-graduação em Ciências Veterinárias, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil; Departamento de Ciências Farmacêuticas, Instituto de Ciências Biológicas e da Saúde, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil.
- Programa de pós-graduação em Ciências Veterinárias, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil; Departamento de Parasitologia Animal, Instituto de Veterinária, Universidade Federal Rural do Rio de Janeiro, BR 465, km 7, Seropédica, RJ 23897-000, Brazil.
MeSH Terms
- Animals
- Horses
- Pyrazoles / pharmacokinetics
- Pyrazoles / administration & dosage
- Pyrazoles / therapeutic use
- Pyrazoles / blood
- Horse Diseases / drug therapy
- Horse Diseases / parasitology
- Tick Infestations / veterinary
- Tick Infestations / drug therapy
- Dermacentor / drug effects
- Female
- Acaricides / pharmacokinetics
- Acaricides / administration & dosage
- Acaricides / therapeutic use
- Male
- Insecticides / pharmacokinetics
- Insecticides / administration & dosage
- Larva / drug effects
Conflict of Interest Statement
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
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