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]
Clinical data | |
---|---|
Pronunciation | /ˌflʊərəˈlænər/ FLOOR-ə-LAN-ər |
Trade names | Bravecto |
Other names |
|
Routes of administration | By mouth (chewable tablets) |
ATCvet code |
|
Legal status | |
Legal status | |
Pharmacokinetic data | |
Bioavailability | 20–27%;[1] reduced in the fasted state[2] |
Elimination half-life | 9.3–16.2 days[3] |
Identifiers | |
IUPAC name
| |
CAS Number | |
PubChem CID | |
ChemSpider | |
UNII | |
KEGG | |
ChEMBL | |
ECHA InfoCard | 100.215.812 |
Chemical and physical data | |
Formula | C22H17Cl2F6N3O3 |
Molar mass | 556.29 g·mol−1 |
3D model (JSmol) | |
Chirality | Racemic mixture |
SMILES
| |
InChI
|
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, RKA; Nuernberger, MC (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, 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 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.
This article is issued from
Wikipedia.
The text is licensed under Creative
Commons - Attribution - Sharealike.
Additional terms may apply for the media files.