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Pharmacological particulars
Pharmacotherapeutic group: ectoparasiticides for systemic use, isoxazolines.
ATCvet code: QP53BE04
Pharmacodynamic properties
Lotilaner, a pure enantiomer from the isoxazoline class is active against fleas (Ctenocephalides felis and Ctenocephalides canis) the tick species Dermacentor reticulatus, Ixodes hexagonus, Ixodes ricinus and Rhipicephalus sanguineus as well as Demodex canis mites.
Lotilaner is a potent inhibitor of gamma–aminobutyric acid (GABA)-gated chloride channels, resulting in rapid death of ticks and fleas. In in vitro studies, the activity of lotilaner against some arthropod species was not affected by resistance to organochlorines (cyclodienes, e.g. dieldrin), phenylpyrazoles (e.g. fipronil), neonicotinoids (e.g. imidacloprid), formamidines (e.g. amitraz) and pyrethroids (e.g. cypermethrin).
For fleas, the onset of efficacy is within 4 hours of attachment for one month after product administration. Fleas on the animal prior to administration are killed within 6 hours.
For ticks, the onset of efficacy is within 48 hours of attachment for one month after product administration. Existing I. ricinus ticks on the animal prior to administration are killed within 8 hours.
The veterinary medicinal product kills existing and newly emerged fleas on dogs before they can lay eggs. Therefore, the product breaks the flea life cycle and prevents environmental flea contamination in areas to which the dog has access.
Pharmacokinetic particulars
Following oral administration, lotilaner is readily absorbed and peak blood concentration is reached within 4 hours. Lotilaner is approximately 10 times more bioavailable when administered with food. The terminal half-life is approximately 4 weeks (harmonic mean). This long terminal half-life provides effective blood concentrations for the entire duration of the inter- dosing interval.
The major route of elimination is biliary excretion and renal excretion is the minor route of elimination (less than 10% of the dose). Lotilaner is metabolized to a small extent into more hydrophilic compounds which are observed in faeces and urine.