Fluralaner (AH252723)
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Product Description
Fluralaner is a systemic insecticide and acaricide belonging to the isoxazoline class, widely used in veterinary medicine to control fleas and ticks in pets such as dogs and cats, and in livestock. It acts as a GABA-gated chloride channel antagonist, disrupting the nervous system of parasites, leading to paralysis and death. Fluralaner is marketed under the brand name Bravecto and is administered orally or topically, providing long-lasting protection for up to 12 weeks per dose. It is effective against various ectoparasites, including Ixodes, Rhipicephalus, and Ctenocephalides. The compound is approved by the FDA and EMA for veterinary use and is considered safe for dogs and cats when used as directed, though it should not be used in species without established safety data. Fluralaner is a white to off-white crystalline solid with synonyms such as Bravecto, AH252723, A-1443, and A1443. It is classified as hazardous, with potential to cause skin irritation, serious eye damage, and harm if swallowed or inhaled. Environmental precautions are necessary to prevent release into waterways due to its potential aquatic toxicity. Recent studies have explored its mechanism of action, showing that it antagonizes GABA receptors by interacting with key residues in the activated state of the receptors.
Mechanism of Action
Fluralaner acts as a GABA-gated chloride channel antagonist, disrupting the nervous system of parasites, leading to paralysis and death. It targets the γ-aminobutyric acid (GABA) receptors in arthropods, blocking the chloride channels and causing hyperexcitation and convulsion in the insects.
Uses
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Veterinary Medicine:
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Fleas and Ticks: Fluralaner is widely used to control fleas and ticks in pets such as dogs and cats, and in livestock.
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Poultry Red Mite (PRM): Effective in controlling Dermanyssus gallinae in poultry, providing long-lasting protection and improving production efficiency.
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Sarcoptic Mange: Demonstrated efficacy in treating Sarcoptes scabiei in various mammal species, including koalas, wombats, rabbits, and black bears.
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Lyme Disease Prevention: Used in rodent-targeted baiting to reduce the density of Borrelia burgdorferi-infected Ixodes scapularis ticks in peri-urban settings.
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Administration
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Oral Administration: Given as flavored chewable tablets or oral solutions.
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Topical Application: Applied as spot-on solutions directly to the skin.
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Baiting: Used in baits for small mammals to reduce tick infestations.
Properties
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Molecular Formula: C₂₂H₁₇Cl₂F₆N₃O₃
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Molecular Weight: 556.3 g/mol
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IUPAC Name: 4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl]-2-methyl-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]benzamide
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Class: Isoxazoline
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Appearance: White to off-white crystalline solid
Safety and Regulatory Status
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FDA and EMA Approval: Approved for veterinary use by the FDA and EMA.
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Safety Profile: Considered safe for dogs, cats, and other target animals when used as directed. No withdrawal period required for eggs in poultry.
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Toxicity: Low acute toxicity in mammals, but highly toxic to invertebrates. Environmental precautions are necessary to prevent release into waterways.
Environmental and Public Health Considerations
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Integrated Pest Management: Fluralaner can be part of integrated pest management strategies, reducing the density of infected ticks and improving public health in endemic regions.
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Resistance Management: Care should be taken to avoid overuse to prevent the development of resistance in parasite populations.