Fluralaner
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]
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Pronunciation | /ˌflʊərəˈlænər/ FLOOR-ə-LAN-ər |
Trade names | Bravecto |
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Routes of administration | By mouth (chewable tablets) |
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Pharmacokinetic data | |
Bioavailability | 20–27%;[1] reduced in the fasted state[2] |
Elimination half-life | 9.3–16.2 days[3] |
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ECHA InfoCard | 100.215.812 |
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Formula | C22H17Cl2F6N3O3 |
Molar mass | 556.29 g·mol−1 |
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Chirality | Racemic mixture |
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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]
See also
References
- "Bravecto (fluralaner) for the Treatment and Prophylaxis of Arachnoenthomoses in Dogs. Full Prescribing Information" (PDF) (in Russian). Intervet GesmbH. 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. 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.
- 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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