Afoxolaner


Afoxolaner is an insecticide and acaricide that belongs to the isoxazoline chemical compound group. It is used to kill fleas and ticks in small animals.

Mechanism

Alfoxolander is a GABA receptor antagonist, which stops chloride transmission in nerves and muscles resulting in paralysis with the paralysis resulting in death for the insect. Alfoxolaner is more selective for GABA repectors in insects than mammals making it safe to give to an animal in amounts that are still lethal to insects.
Selectivity for insect over mammalian GABA-receptors has been demonstrated for other isoxazolines. The selectivity might be explained by the number of pharmacological differences that exist between GABA-gated chloride channels of insects and vertebrates.

Use

Afoxolaner is given orally and is then rapidly distributed into the systemic circulation, when a tick or flea feeds on the blood of the host it ingests the afoxolaner and becomes paralysed. Thus fleas and ticks must first feed on the host for the drug to be effective. Afoxolaner has been given up to five times the therapeutic dose without causing intoxication.

Legal status

The marketing authorization was granted by the European [Medicines Agency] in February 2014, for Nexgard, and in January 2015, for Nexgard Spectra.

Brand names

Afoxolaner is the active ingredient of the veterinary medicinal products Nexgard, Frontpro, and Nexgard Spectra. They are indicated for the treatment and prevention of flea infestations, and the treatment and control of tick infestations in dogs and puppies for one month.