Afoxolaner is an active ingredient, alone and in combination with milbemycin oxime, as an insecticide and an acaricide in dogs. Afoxolaner is also used for the treatment of sarcoptic and demodectic mange. It has a chemical structure of C26H17ClF9N3O3, with a molecular weight of 625.88.
The acute oral LD50 and dermal LD50 of afoxolaner in rats are >1,000 mg/kg and >2,000 mg/kg, respectively.
Afoxalaner is given to dogs and puppies (>8 weeks of age) orally has a chewable with a recommended dose of 2.7–7 mg/kg. The parasiticidal effect lasts for a month. It is rapidly absorbed with maximum blood levels within 2–12 hours, and a bioavailability of 74%. The half-life of afoxolaner is greater in Collies than in Beagles. Ninety-nine percent of absorbed afoxolaner may bind to blood proteins. Elimination half-life is 14 hours, and excretion of afoxolaner and its metabolites occurs primarily via the biliary route.
In general, afoxolaner is safe in dogs. At higher doses (100, 300, and 1,000 mg/kg, PO), afoxolaner produced a diuretic effect in rats, reduction in food consumption in rats and rabbits, and vomiting and diarrhea in dogs.
There is no specific antidote for afoxolaner poisoning in pets. Treatment rests with preventing further exposure and supportive measures. Gastric lavage and administration of activated charcoal are advised if the exposure is via accidental ingestion.
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