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Contents

   



(Top)
  


1 Mode of action  




2 Research  




3 References  













Fluralaner






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From Wikipedia, the free encyclopedia
  

This is an old revision of this page, as edited by Throughthemind (talk | contribs)at13:49, 1 December 2023 (Reword). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.
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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
  • US DailyMed: Fluralaner
    • Routes of
    administration    		By mouth
    ATCvet code
    Legal status
    Legal status
    • AU: S5 (Caution)
  • CA: ℞-only
  • US: ℞-only
  • EU: Rx-only
  • Rx-only; OTC (RU)[1]
    • 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

    CAS Number
    PubChem CID
    ChemSpider
    UNII
    KEGG
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard100.215.812 Edit this at Wikidata
    Chemical and physical data
    FormulaC22H17Cl2F6N3O3
    Molar mass556.29 g·mol−1
    3D model (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, an oral solution is available as Exzolt.[12]

    Mode of action

    Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls).[13] Potency of fluralaner is comparable to fipronil (a related GABA-antagonist insecticide and acaricide).[14]

    Research

    Fluralaner is being investigated to determine its ability to reduce the incidence of mosquito-borne diseases,[15] as well as bed bugs.[16][17]

    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.
  • ^ Walther FM, Allan MJ, Roepke RK, Nuernberger MC (March 2014). "The effect of food on the pharmacokinetics of oral fluralaner in dogs". Parasites & Vectors. 7 (1): 84. doi:10.1186/1756-3305-7-84. PMC 3975707. PMID 24598049.
  • ^ "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.
  • ^ "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.
  • ^ Walther FM, Allan MJ, Roepke RK, Nuernberger MC (March 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 3975339. PMID 24606886.
  • ^ Ranjan S, Young D, Sun F (July 2018). "A single topical fluralaner application to cats and to dogs controls fleas for 12 weeks in a simulated home environment". Parasites & Vectors. 11 (1): 385. doi:10.1186/s13071-018-2927-0. PMC 6029119. PMID 29970135.
  • ^ 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.
  • ^ "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.
  • ^ 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.
  • ^ "MSD Animal Health receives EU approval for Bravecto". 19 February 2014. Archived from the original on 27 March 2019. Retrieved 3 Nov 2014.
  • ^ "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.
  • ^ Imrie, Paul (2020-06-24). "Backyard poultry red mite treatment launches". Vet Times. Retrieved 2023-12-01.
  • ^ 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". Insect Biochemistry and Molecular Biology. 45: 111–124. doi:10.1016/j.ibmb.2013.11.009. PMID 24365472.
  • ^ 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): 91–95. doi:10.1002/ps.3768. PMID 24591229.
  • ^ Miglianico M, Eldering M, Slater H, Ferguson N, Ambrose P, Lees RS, et al. (July 2018). "Repurposing isoxazoline veterinary drugs for control of vector-borne human diseases". Proceedings of the National Academy of Sciences of the United States of America. 115 (29): E6920–E6926. Bibcode:2018PNAS..115E6920M. doi:10.1073/pnas.1801338115. PMC 6055183. PMID 29967151.
  • ^ Murez, Cara (1 December 2022). "Two veterinary drugs may help eliminate bedbugs". United Press International, Inc. Retrieved 3 December 2022.
  • ^ Sheele, Johnathan M. (2020). "A Preliminary Report Showing Spinosad and Fluralaner Are Able to Incapacitate Cimex lectularius L., the Common Bed Bug". Cureus. 12 (4): e7529. doi:10.7759/cureus.7529. PMC 7198093. PMID 32377477. S2CID 216501793. Retrieved 3 December 2022.{{cite journal}}: CS1 maint: unflagged free DOI (link)
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    ●This page was last edited on 1 December 2023, at 13:49 (UTC).
    ●This version of the page has been revised. Besides normal editing, the reason for revision may have been that this version contains factual inaccuracies, vandalism, or material not compatible with the Creative Commons Attribution-ShareAlike License.


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