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Pharmacological particulars
Pharmacotherapeutic group: Ectoparasiticides for systemic use.
ATCvet code: QP53B E02
Pharmacodynamic properties
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.
The onset of efficacy is within 8 hours for fleas (C. felis) and 12 hours for ticks (I. ricinus).
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 particulars
Fluralaner is readily absorbed from the topical administration site into the hair, skin and subjacent tissues, from where it is slowly absorbed into the vascular system. A plateau is seen in plasma between 7 and 63 days post administration, after which concentrations decline slowly. The prolonged persistence and slow elimination from plasma (t1/2 = 21 days) and the lack of extensive metabolism provide effective concentrations of fluralaner for the duration of the inter-dosing interval. Unchanged fluralaner is excreted in faeces and to a very low extent in urine.