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Pharmacological particulars
ATCvet code: QP53BE02.
Pharmacotherapeutic group
Ectoparasiticides for systemic use.
Fluralaner is an acaricide and insecticide. It is efficacious against ticks (Ixodes spp., Dermacentor spp. and Rhipicephalus sanguineus), fleas (Ctenocephalides spp.), Demodex canis mites and sarcoptic mange (Sarcoptes scabiei var. canis) on the dog.
Fluralaner reduces the risk of infection with Babesia canis canis via transmission by Dermacentor reticulatus by killing the ticks within 48 hours, before disease transmission occurs.
Fluralaner reduces the risk of infection with D. caninum via transmission of Ctenocephalides felis by killing the fleas before disease transmission occurs.
The onset of effect is within 8 hours of attachment for fleas (C. felis) and 12 hours of attachment for I. ricinus and 48 hours for D. reticulatus ticks. The onset of acaricidal efficacy against I. hexagonus ticks was demonstrated 7 days after treatment.
Fluralaner has a high potency against ticks and fleas by exposure via feeding, i.e. it is systemically active on target parasites.
Fluralaner is a potent inhibitor of parts of the arthropod nervous system by acting antagonistically on ligand-gated chloride channels (GABA-receptor and glutamate-receptor).
In molecular on-target studies on insect GABA receptors of flea and fly, fluralaner is not affected by dieldrin resistance.
In in vitro bio-assays, fluralaner is not affected by proven field resistances against amidines (tick), organophosphates (tick, mite), cyclodienes (tick, flea, fly), macrocyclic lactones (sea lice), phenylpyrazoles (tick, flea), benzophenyl ureas (tick), pyrethroids (tick, mite) and carbamates (mite).
The product contributes towards the control of the environmental flea populations in areas to which treated dogs have access.
Newly emerged fleas on a dog are killed before viable eggs are produced. An in vitro study also demonstrated that very low concentrations of fluralaner stop the production of viable eggs by fleas.
The flea life cycle is broken due to the rapid onset of action and long-lasting efficacy against adult fleas on the animal and the absence of viable egg production.
Pharmacokinetic properties
Following oral administration, fluralaner is readily absorbed reaching maximum plasma concentrations within 1 day. Food enhances the absorption. Fluralaner is systemically distributed and reaches the highest concentrations in fat, followed by liver, kidney and muscle. The prolonged persistence and slow elimination from plasma (t1/2 = 12 days) and the lack of extensive metabolism provide effective concentrations of fluralaner for the duration of the inter-dosing interval. Individual variation in Cmax and t1/2 was observed. The major route of elimination is the excretion of unchanged fluralaner in faeces (~90% of the dose). Renal clearance is the minor route of elimination.