Afoxolaner

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Afoxolaner
Afoxolaner structure.svg
Clinical data
Pronunciation/ˌfɒksˈlænər/ ay-FOK-soh-LAN-ər
Trade namesNexGard
Synonyms4-[(5RS)-5-(5-Chloro-α,α,α-trifluoro-m-tolyl)-4,5-dihydro-5-(trifluoromethyl)-1,2-oxazol-3-yl]-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]naphthalene-1-carboxamide
Routes of
administration
By mouth (chewables)
ATCvet code
Legal status
Legal status
Pharmacokinetic data
Bioavailability74% (Tmax = 2–4 hours)[1]
Elimination half-life14 hours[1]
ExcretionBiliary (major route)
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
Chemical and physical data
FormulaC26H17ClF9N3O3
Molar mass625.88 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture

Afoxolaner (INN)[2] is an insecticide and acaricide used in dogs. It is indicated for the treatment and prevention of flea infestations, and the treatment and control of tick infestations in dogs and puppies 8 weeks of age and older, weighing 4 pounds (~1.8 kilograms) of body weight or greater. It is given once a month.[3]

Unlike most other flea treatments which are applied topically to the animal's coat, afoxolaner is administered orally in meat-flavoured tablets, and poisons fleas once they start feeding. It is used either alone or as a combination treatment with milbemycin oxime.[4][5][6]

The US FDA reports[7] that drugs in this class (isoxazolines) can have adverse neurologic effects on some dogs, such as muscle tremors, ataxia, and seizures.

See also[edit]

References[edit]

  1. ^ a b c "Frontline NexGard (afoxolaner) for the Treatment and Prophylaxis of Ectoparasitic Diseases in Dogs. Full Prescribing Information" (PDF) (in Russian). Sanofi Russia. Retrieved 14 November 2016.
  2. ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 70" (PDF). World Health Organization. pp. 276–7. Retrieved 14 November 2016.
  3. ^ "NexGard (afoxolaner) Chewables. Full Prescribing Information" (PDF). Frontline Vet Labs, a Division of Merial, Inc. Duluth, GA 30096-4640 USA. Retrieved 14 November 2016.
  4. ^ Shoop, WL; Hartline, EJ; Gould, BR; Waddell, ME; McDowell, RG; Kinney, JB; Lahm, GP; Long, JK; Xu, M; Wagerle, T; Jones, GS; Dietrich, RF; Cordova, D; Schroeder, ME; Rhoades, DF; Benner, EA; Confalone, PN (2 April 2014). "Discovery and Mode of Action of Afoxolaner, a New Isoxazoline Parasiticide for Dogs" (PDF). Veterinary Parasitology. 201 (3–4): 179–89. doi:10.1016/j.vetpar.2014.02.020. PMID 24631502. Retrieved 14 November 2016.
  5. ^ Beugnet, F; deVos, C; Liebenberg, J; Halos, L; Fourie, J (25 August 2014). "Afoxolaner Against Fleas: Immediate Efficacy and Resultant Mortality After Short Exposure on Dogs" (PDF). Parasite. 21: 42. doi:10.1051/parasite/2014045. PMC 4141545. PMID 25148564. Retrieved 14 November 2016.
  6. ^ Beugnet, F; Crafford, D; de Vos, C; Kok, D; Larsen, D; Fourie, J (15 August 2016). "Evaluation of the Efficacy of Monthly Oral Administration of Afoxolaner plus Milbemycin Oxime (NexGard Spectra®, Merial) in the Prevention of Adult Spirocerca lupi Establishment in Experimentally Infected Dogs" (PDF). Veterinary Parasitology. 226: 150–61. doi:10.1016/j.vetpar.2016.07.002. PMID 27514901. Retrieved 14 November 2016.
  7. ^ Medicine, Center for Veterinary. "CVM Updates - Animal Drug Safety Communication: FDA Alerts Pet Owners and Veterinarians About Potential for Neurologic Adverse Events Associated with Certain Flea and Tick Products". www.fda.gov. Retrieved 2018-09-22.