Afoxolaner
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| Clinical data | |
|---|---|
| Pronunciation | ay-FOX-oh-LAN-ər |
| Trade names | NexGard |
| Routes of administration |
By mouth (chewables) |
| ATCvet code | QP53BE01 (WHO) |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 74% (Tmax = 2–4 hours)[1] |
| Biological half-life | 14 hours[1] |
| Excretion | Biliary (major route) |
| Identifiers | |
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| Synonyms | 4-[(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 |
| CAS Number | 1093861-60-9 |
| PubChem (CID) | 25154249 |
| ChemSpider | 28651525 |
| UNII | 02L07H6D0U |
| KEGG | D10361 |
| ChEMBL | CHEMBL2219412 |
| Chemical and physical data | |
| Formula | C26H17ClF9N3O3 |
| Molar mass | 625.88 g·mol−1 |
| 3D model (Jmol) | Interactive image |
| Chirality | Racemic mixture |
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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]
See also[edit]
References[edit]
- ^ 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.
- ^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 70" (PDF). World Health Organization. pp. 276–7. Retrieved 14 November 2016.
- ^ "NexGard (afoxolaner) Chewables. Full Prescribing Information" (PDF). Frontline Vet Labs, a Division of Merial, Inc. Duluth, GA 30096-4640 USA. Retrieved 14 November 2016.
- ^ 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.
- ^ 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. - ^ 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.
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