Peer-reviewed veterinary case report
How afoxolaner kills fleas and ticks on dogs after one pill
By Shoop, Wesley L et al.·Published in Veterinary parasitology·2014·DuPont Crop Protection, United States·View original on PubMed →
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Original publication title: Discovery and mode of action of afoxolaner, a new isoxazoline parasiticide for dogs.
- Species:
- dog
Plain-English summary
A dog was treated with a new oral medication called afoxolaner to help get rid of fleas and ticks. After giving the dog a dose of 2.5 mg per kilogram of body weight, the medication was found to be very effective, keeping the blood levels high enough to fight off these parasites for over a month. Afoxolaner works by blocking certain channels in the parasites that are essential for their nervous system function, which helps to eliminate them. Overall, the treatment showed a good safety profile and was successful in controlling flea and tick infestations.
People also search for: dog flea treatment afoxolaner · how to get rid of ticks on dogs · safe flea medication for dogs
Abstract
Afoxolaner is an isoxazoline compound characterized by a good safety profile and extended effectiveness against fleas and ticks on dogs following a single oral administration. In vitro membrane feeding assay data and in vivo pharmacokinetic studies in dogs established an afoxolaner blood concentration of 0.1-0.2 μg/ml to be effective against both fleas (Ctenocephalides felis) and ticks (Dermacentor variabilis). Pharmacokinetic profiles in dogs following a 2.5mg/kg oral dosage demonstrated uniform and predictable afoxolaner plasma concentrations above threshold levels required for efficacy for more than one month. Dose ranging and a 5-month multi-dose experimental study in dogs, established that the 2.5mg/kg oral dosage was highly effective against fleas and ticks, and produced predictable and reproducible pharmacokinetics following repeated dosing. Mode of action studies showed that afoxolaner blocked native and expressed insect GABA-gated chloride channels with nanomolar potency. Afoxolaner has comparable potency between wild type channels and channels possessing the A302S (resistance-to-dieldrin) mutation. Lack of cyclodiene cross-resistance for afoxolaner was confirmed in comparative Drosophila toxicity studies, and it is concluded that afoxolaner blocked GABA-gated chloride channels via a site distinct from the cyclodienes.
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Search related cases →Original publication on PubMed: https://pubmed.ncbi.nlm.nih.gov/24631502/