Fluralaner

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Fluralaner
Clinical data
Pronunciation/ˌflʊərəˈlænər/ FLOOR-ə-LAN-ər
Trade namesBravecto, Exzolt
Other names
  • 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
License data
QP53BE02 (WHO)
Legal status
Legal status
Pharmacokinetic data
Bioavailability20–27%;[1] reduced in the fasted state[2]
Elimination half-life9.3–16.2 days[3]
Identifiers
  • (±)-4-[5-(3,5-Dichlorophenyl)-5-(trifluoromethyl)-4,5-dihydroisoxazol-3-yl]-2-methyl-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]benzamide
JSmol)
ChiralityRacemic mixture
  • Cc1cc(ccc1C(=O)NCC(=O)NCC(F)(F)F)C2=NOC(C2)(c3cc(cc(c3)Cl)Cl)C(F)(F)F
  • InChI=1S/C22H17Cl2F6N3O3/c1-11-4-12(2-3-16(11)19(35)31-9-18(34)32-10-21(25,26)27)17-8-20(36-33-17,22(28,29)30)13-5-14(23)7-15(24)6-13/h2-7H,8-10H2,1H3,(H,31,35)(H,32,34)
  • Key:MLBZKOGAMRTSKP-UHFFFAOYSA-N

Fluralaner (INN)[4] is a systemic insecticide and acaricide that is administered orally[5] or topically.[6] The U.S. Food and Drug Administration (FDA) approved it under the trade name Bravecto for flea treatment in dogs in May 2014[7] and Bravecto Plus as a topical treatment for cats in November 2019,[8] with warnings about possible side effects in both species.[9] The EU approved the drug in February 2014.[10] Australia approved it for the treatment and prevention of ticks and fleas on dogs in January 2015.[11] For treating mites in chickens, a solution for use in drinking water is available under the name Exzolt;[12] it was introduced by the EU in 2017.[13]

Mode of action

Fluralaner inhibits

γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls).[14] Potency of fluralaner is comparable to fipronil (a related GABA-antagonist insecticide and acaricide).[15]

Research

Fluralaner is being investigated to determine its ability to reduce the incidence of mosquito-borne diseases,[16] as well as bed bugs.[17][18]

References

  1. ^ a b "Bravecto (fluralaner) for the Treatment and Prophylaxis of Arachnoenthomoses in Dogs. Full Prescribing Information" (PDF) (in Russian). Intervet GesmbH. Archived from the original (PDF) on 17 May 2018. Retrieved 14 November 2016.
  2. PMID 24598049
    .
  3. ^ "Bravecto (fluralaner) Flavored Chews for Dogs. Prescribing Information" (PDF). Intervet, Inc., a subsidiary of Merck & Company, In. Archived from the original (PDF) on 27 March 2019. 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. Archived from the original (PDF) on November 14, 2016. Retrieved 14 November 2016.
  5. PMID 24606886
    .
  6. PMID 29970135
    .
  7. ^ Lee J (21 May 2014). "New Flea/Tick Medication by Merck Just Approved: Bravecto". Archived from the original on 15 June 2018. Retrieved 3 November 2014.
  8. ^ "BRAVECTO® PLUS (fluralaner and moxidectin topical solution) for Cats Receives Approval from US Food and Drug Administration". Merck Animal Health. 2019-11-15. Archived from the original on 2022-09-19. Retrieved 22 May 2021.
  9. ^ Center for Veterinary Medicine (2020-07-31). "Fact Sheet for Pet Owners and Veterinarians about Potential Adverse Events Associated with Isoxazoline Flea and Tick Products". FDA. Archived from the original on 2021-05-22. Retrieved 22 May 2021.
  10. ^ "MSD Animal Health receives EU approval for Bravecto". 19 February 2014. Archived from the original on 27 March 2019. Retrieved 3 Nov 2014.
  11. ^ "Agricultural and Veterinary Chemicals" (PDF). Australian Pesticides and Veterinary Medicines Authority. 10 February 2015. Archived (PDF) from the original on 19 September 2022. Retrieved 14 February 2019.
  12. ^ Imrie, Paul (2020-06-24). "Backyard poultry red mite treatment launches". Vet Times. Retrieved 2023-12-01.
  13. PMID 29197422
    .
  14. PMID 24365472
    .
  15. PMID 24591229
    .
  16. PMID 29967151
    .
  17. ^ Murez, Cara (1 December 2022). "Two veterinary drugs may help eliminate bedbugs". United Press International, Inc. Retrieved 3 December 2022.
  18. S2CID 216501793
    .
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