Fluralaner

한글명:Fluralaner

카스 번호864731-61-3

상품명:Fluralaner

CBNumberCB13164799

포뮬러 무게0

MOL 파일Mol file

화학적 성질

밀도	1.51±0.1 g/cm3(Predicted)
저장 조건	Store at -20°C
용해도	DMSO:150.0(Max Conc. mg/mL);269.65(Max Conc. mM) Ethanol:25.0(Max Conc. mg/mL);44.94(Max Conc. mM)
산도 계수 (pKa)	12.50±0.46(Predicted)
물리적 상태	결정성 고체
InChIKey	MLBZKOGAMRTSKP-UHFFFAOYSA-N
SMILES	C(NCC(=O)NCC(F)(F)F)(=O)C1=CC=C(C2CC(C3=CC(Cl)=CC(Cl)=C3)(C(F)(F)F)ON=2)C=C1C

그림문자(GHS)

Fluralaner 화학적 특성, 용도, 생산

개요
Fluralaner (INN) is a systemic insecticide and acaricide that is administered orally. The U.S. Food and Drug Administration (FDA) approved it under the trade name Bravecto for flea treatment in dogs in May 2014. The EU approved the drug in February 2014. Australia approved it for the treatment and prevention of ticks and fleas on dogs in January 2015.
용도
Fluralaner(864731-61-3) is a novel systemically administered insecticidal and acaricidal compound that provides long-acting efficacy after oral administration to dogs. Fluralaner belongs to a new class of compounds, the isoxazolines. A field study has shown that a single fluralaner dose administered orally to dogs provides at least twelve weeks of flea- and tick-control. The long duration of activity offers a more convenient treatment over monthly flea and tick control treatments with a potential compliance advantage, reducing the risk of vector-transmitted diseases.
Indications
Fluralaner is an insecticide and acaricide used to treat Sarcoptes scabiei var. canis infestation in dogs. Flea treatment. A possible anti-malarial found to kill disease-spreading mosquitoes when they bite treated people.
부작용
Most pets have very few side effects from fluralaner, provided it is given according to label recommendations and at the prescribed interval (or for off-label use, according to your veterinarian's directions). Side effects may include vomiting, diarrhea, decreased appetite, or flaky skin.
vcahospitals.com
Overdosage
No adverse reactions were observed following oral administration to puppies aged 8–9 weeks and weighing 2.0–3.6 kg treated with overdoses of up to 5 times the maximum recommended dose (56 mg, 168 mg and 280 mg fluralaner/kg bodyweight) on three occasions at shorter intervals than recommended (8-week intervals).
There were no findings on reproductive performance and no findings of concern on offspring viability when fluralaner was administered orally to Beagle dogs at overdoses of up to 3 times the maximum recommended dose (up to 168 mg/kg bodyweight of fluralaner).
The veterinary medicinal product was well tolerated in Collies with a deficient multidrug-resistanceprotein 1 (MDR1 -/-) following single oral administration at 3 times the recommended dose (168 mg/kg bodyweight). No treatment-related clinical signs were observed.
Drug interactions
Fluralaner is highly bound to plasma proteins and might compete with other highly bound drugs such as non-steroidal anti-inflammatory drugs (NSAIDs) and the cumarin derivative warfarin. Incubation of fluralaner in the presence of carprofen or warfarin in dog plasma at maximum expected plasma concentrations did not reduce the protein binding of fluralaner, carprofen or warfarin.
During clinical field testing, no interactions between Bravecto chewable tablets for dogs and routinely used veterinary medicinal products were observed.
Mode of action
Fluralaner is an inhibitor of the arthropod nervous system. It inhibits γ-aminobutyric acid (GABA)-gated chloride channels (GABAA receptors) and L-glutamate-gated chloride channels (GluCls). Potency of fluralaner is comparable to fipronil (a related GABA-antagonist insecticide and acaricide).

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