Background: Fluralaner is a novel systemic insecticide and acaricide. The purpose of these studies was to\r\ninvestigate the pharmacokinetic properties of fluralaner in Beagle dogs following single oral or intravenous\r\n(i.v.) administration.\r\nMethods: Following the oral administration of 12.5, 25 or 50 mg fluralaner/kg body weight (BW), formulated as\r\nchewable tablets or i.v. administration of 12.5 mg fluralaner/kg BW, formulated as i.v. solution to 24 Beagles, plasma\r\nsamples were collected until 112 days after treatment. Plasma concentrations of fluralaner were measured using\r\nHPLC-MS/MS. Pharmacokinetic parameters were calculated by non-compartmental methods.\r\nResults: After oral administration, maximum plasma concentrations (Cmax) were reached within 1 day on average.\r\nFluralaner was quantifiable in plasma for up to 112 days after single oral and i.v. treatment. The apparent half-life\r\nof fluralaner was 12ââ?¬â??15 days and the mean residence time was 15ââ?¬â??20 days. The apparent volume of distribution of\r\nfluralaner was 3.1 L/kg, and clearance was 0.14 L/kg/day.\r\nConclusions: Fluralaner is readily absorbed after single-dose oral administration, and has a long elimination half-life,\r\nlong mean residence time, relatively high apparent volume of distribution, and low clearance. These pharmacokinetic\r\ncharacteristics help to explain the prolonged activity of fluralaner against fleas and ticks on dogs after a single oral dose.
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