Fluralaner

Fluralaner
Clinical data
Pronunciation FLOOR-ə-LAN-ər
Trade names Bravecto
Routes of
administration		 By mouth (chewable tablets)
ATCvet code QP53BE02 (WHO)
Legal status
Legal status
Pharmacokinetic data
Bioavailability 20–27%;[1] reduced in the fasted state[2]
Biological half-life 9.3–16.2 days[3]
Identifiers
Synonyms
  • A1443, AH252723
  • 4-[(5RS)-5-(3,5-Dichlorophenyl)-4,5-dihydro-5-(trifluoromethyl)-1,2-oxazol-3-yl]-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]-o-toluamide
CAS Number 864731-61-3
PubChem (CID) 25144319
ChemSpider 29398949
UNII WSH8393RM5
KEGG D10402
ChEMBL CHEMBL2364610
Chemical and physical data
Formula C22H17Cl2F6N3O3
Molar mass 556.29 g·mol−1
3D model (Jmol) Interactive image
Chirality Racemic mixture

Fluralaner (INN)[4] is a systemic insecticide and acaricide that is administered orally.[5] The U.S. Food and Drug Administration (FDA) approved it under the trade name Bravecto for flea treatment in dogs in May 2014.[6] The EU approved the drug in February 2014.[7] Australia approved its use for sale as a flea and tick control treatment.

Mode of action

Fluralaner is an inhibitor of the arthropod nervous system.[3] Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABACls) and L-glutamate-gated chloride channels (GluCls).[8] Potency of fluralaner is comparable to fipronil (a phenylpyrazole ectoparasiticide).[9]

See also

References

  1. 1 2 "Bravecto (fluralaner) for the Treatment and Prophylaxis of Arachnoenthomoses in Dogs. Full Prescribing Information" (PDF) (in Russian). Intervet GesmbH. Retrieved 14 November 2016.
  2. ↑ Walther, FM; Allan, MJ; Roepke, RKA; Nuernberger, MC (2014). "The Effect of Food on the Pharmacokinetics of Oral Fluralaner in Dogs" (PDF). Parasites & Vectors. 7 (1): 84. doi:10.1186/1756-3305-7-84. PMC 3975707Freely accessible. Retrieved 14 November 2016.
  3. 1 2 "Bravecto (fluralaner) Flavored Chews for Dogs. Prescribing Information" (PDF). Intervet, Inc., a subsidiary of Merck & Company, In. Retrieved 14 November 2016.
  4. ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 69" (PDF). WHO Drug Information. 27 (1): 59. 2013. Retrieved 14 November 2016.
  5. ↑ Walther, FM; Allan, MJ; Roepke, RKA; Nuernberger, MC (2014). "Safety of Fluralaner Chewable Tablets (Bravecto™), a Novel Systemic Antiparasitic Drug, in Dogs After Oral Administration". Parasites & Vectors. 7 (1): 87. doi:10.1186/1756-3305-7-87. PMC 3975339Freely accessible. PMID 24606886.
  6. ↑ Lee, J (21 May 2014). "New Flea/Tick Medication by Merck Just Approved: Bravecto". Retrieved 3 November 2014.
  7. ↑ "MSD Animal Health receives EU approval for Bravecto". 19 February 2014. Retrieved 3 Nov 2014.
  8. ↑ Gassel, M; Wolf, C; Noack, S; Williams, H; Ilg, T (February 2014). "The Novel Isoxazoline Ectoparasiticide Fluralaner: Selective Inhibition of Arthropod γ-Aminobutyric Acid- and L-Glutamate-gated Chloride Channels and Insecticidal/Acaricidal Activity" (PDF). Insect Biochemistry and Molecular Biology. 45: 111–24. doi:10.1016/j.ibmb.2013.11.009. PMID 24365472. Retrieved 14 November 2016.
  9. ↑ Asahi, M; Kobayashi, M; Matsui, H; Nakahira, K (January 2015). "Differential Mechanisms of Action of the Novel γ-Aminobutyric Acid Receptor Antagonist Ectoparasiticides Fluralaner (A1443) and Fipronil". Pest Management Science. 71 (1): 91–5. doi:10.1002/ps.3768. PMID 24591229.
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