Fluralaner
![]() | |
Clinical data | |
---|---|
Pronunciation | FLOOR-ə-LAN-ər |
Trade names | Bravecto |
Routes of administration | By mouth (chewable tablets) |
ATCvet code | QP53BE02 (WHO) |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Bioavailability | 20–27%;[1] reduced in the fasted state[2] |
Biological half-life | 9.3–16.2 days[3] |
Identifiers | |
| |
Synonyms |
|
CAS Number | 864731-61-3 |
PubChem (CID) | 25144319 |
ChemSpider | 29398949 |
UNII | WSH8393RM5 |
KEGG | D10402 |
ChEMBL | CHEMBL2364610 |
Chemical and physical data | |
Formula | C22H17Cl2F6N3O3 |
Molar mass | 556.29 g·mol−1 |
3D model (Jmol) | Interactive image |
Chirality | Racemic mixture |
| |
|
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 its use for sale as a flea and tick control treatment.
Mode of action
Fluralaner is an inhibitor of the arthropod nervous system.[3] Fluralaner inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABACls) and L-glutamate-gated chloride channels (GluCls).[8] Potency of fluralaner is comparable to fipronil (a phenylpyrazole ectoparasiticide).[9]
See also
References
- 1 2 "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" (PDF). Parasites & Vectors. 7 (1): 84. doi:10.1186/1756-3305-7-84. PMC 3975707
. Retrieved 14 November 2016.
- 1 2 "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.
- ↑ 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" (PDF). Insect Biochemistry and Molecular Biology. 45: 111–24. doi:10.1016/j.ibmb.2013.11.009. PMID 24365472. Retrieved 14 November 2016.
- ↑ 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 - version of the 11/14/2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.