Antiparasitic products, ectoparasiticides for systemic use, isoxazolines.

Fluralaner is an acaricide and an insecticide which has a high potency against poultry mites, mostly by exposure via feeding, i.e. it is systemically active against the 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 gamma-aminobutyric acid (GABA) receptors of flea and fly, dieldrin resistance does not affect fluralaner.

The onset of activity against Dermanyssus gallinae is within four hours of the mites starting to feed on treated chickens.

The treatment kills mites feeding on treated chickens and stops egg production from female mites for 15 days after the first administration of the product. This activity breaks the mite life cycle.

In vitro bio-assays show that fluralaner is effective against parasites having proven field resistance, including organophosphates, pyrethroids and carbamates.

As demonstrated in a multi-site EU field study performed in commercial egg production farms, elimination of mites from infested chickens following treatment is associated with a statistically significant improvement in behavioural parameters indicative of animal welfare (reduction of night-time activity and head scratching, head shaking and preening of own plumage at night and during day-time) as well as a reduction of blood corticosterone concentration.

After oral administration, fluralaner is absorbed rapidly from the medicated drinking water, reaching maximum plasma concentrations 36 hours after the first dose and 12 hours after the second dose. The bioavailability is high, with approximately 91% of the dose absorbed following oral administration. Fluralaner is highly bound to protein. Fluralaner is widely distributed throughout the body, with the highest concentrations reported in the liver and skin/fat. No significant metabolites are observed in chickens, and fluralaner is mainly eliminated via the hepatic route. The apparent elimination half-life is approximately 5 days following oral administration.

Fluralaner has been shown to be very persistent in soil under both, aerobic and anaerobic conditions. Fluralaner degrades in aquatic sediment under anaerobic conditions while it has been shown to be very persistent under aerobic conditions.