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Contents

   



(Top)
  


1 Mode of action  




2 See also  




3 References  













Fluralaner






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From Wikipedia, the free encyclopedia
  

This is an old revision of this page, as edited by 172.116.23.135 (talk)at04:44, 3 September 2020 (→‎Mode of action). The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.
(diff) ← Previous revision | Latest revision (diff) | Newer revision → (diff)
Fluralaner
Clinical data
Pronunciation/ˌflʊərəˈlænər/ FLOOR-ə-LAN-ər
Trade namesBravecto
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
Routes of
administration		By mouth (chewable tablets)
ATCvet code
Legal status
Legal status
  • 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] 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 it for the treatment and prevention of ticks and fleas on dogs in January 2015.[8]

    Mode of action

    Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls).[9] Potency of fluralaner is comparable to fipronil (a related GABA-antagonist insecticide and acaricide).[10] yes

    See also

    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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  • ^ "Bravecto (fluralaner) Flavored Chews for Dogs. Prescribing Information" (PDF). Intervet, Inc., a subsidiary of Merck & Company, In. 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. 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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  • ^ Lee, J (21 May 2014). "New Flea/Tick Medication by Merck Just Approved: Bravecto". Retrieved 3 November 2014.
  • ^ "MSD Animal Health receives EU approval for Bravecto". 19 February 2014. Retrieved 3 Nov 2014.
  • ^ "Agricultural and Veterinary Chemicals" (PDF). Australian Pesticides and Veterinary Medicines Authority. 10 February 2015. Retrieved 14 February 2019.
  • ^ 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: 111–24. 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): 91–5. doi:10.1002/ps.3768. PMID 24591229.
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    • Retrieved from "https://en.wikipedia.org/w/index.php?title=Fluralaner&oldid=976479091"
    Categories: 
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    ●This page was last edited on 3 September 2020, at 04:44 (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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