Introduction

Name

• Fluralaner.

Class of drug

• Ectoparasiticides for systemic use.
• Isoxazoline.
• Systemic insecticide and acaricide.

Description

Chemical name

• 4-[(5R)-5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-1,2-oxazol-3-yl]-2-methyl-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]benzamide.

Molecular formula

• C₂₂H₁₇Cl₂F₆N₃O₃.

Molecular weight

• 556.28 g/mol.

Physical properties

• Chewable tablet: light to dark brown tablet with a smooth or slightly rough surface and circular shape. Some marbling, speckles or both may be visible.
• Spot-on solution: clear, colorless to yellow solution.
• Oral solution: yellow.

Storage requirements

• Shelf-life as packaged for sale: 2 years.
• Do not store above 30°C/86°F.
• Pipettes should be kept in the outer packaging to prevent solvent loss or moisture uptake. The sachets should only be opened immediately prior to use.

Uses

Indications

• Not licensed for use in rabbits although it has been successfully used to eliminate:
  • Psoroptes cuniculi mites Psoroptes cuniculi.
  • Sarcoptic scabiei var. cuniculi Sarcoptes scabiei.

 Efficacy against other ectoparasites

• Used to eliminate Psoroptes cuniculi mites off license. One off dose given and eliminated the mites in 12 days. A residual effect was also noted and there were no signs of recurrence of P. cuniculi mites for the duration of the 90-day study.
• Was found to be effective in the treatment of severe sarcoptic mange in pet rabbits when administered orally and no additional topical or systemic medications were needed. Clinical recovery occurred within 30 days of fluralaner administration in one study on rabbits with severe sarcoptic manage. Parasitological cure occurred within 45 days of fluralaner administration in the same study.
• In another study by day 14 post-oral dosing, only one rabbit out of the 12 had persistent clinical signs of sarcoptic mange but had a negative skin scrape. By day 21 all rabbits had negative skin scrapings, and all showed no clinical signs. There was no recurrence of the clinical signs or positive skin scrapings for the duration of the 90-day study period.
• Was found to be effective in eliminating sarcoptic mange in rabbits when administered topically in combination with moxidectin. This resulted in 100% eradication of mites and complete resolution of all skin lesions within 21 days. Recurrence was not observed 90 days post-treatment.

Administration

Pharmacokinetics

Precautions

Interactions

with other drugs

• None known.
• Theoretical competition with other highly bound drugs, eg non-steroidal anti-inflammatory drugs (NSAIDs). However, protein binding of fluralaner, carprofen or warfarin was not reduced in an in vitro study in dog plasma using the maximum expected plasma concentrations.
• No interactions with routinely used veterinary medicinal products in dogs during clinical field trials.
• Data not available for the rabbit, further research is required.

Adverse Reactions

Further Reading

Publications

Refereed Papers

• Recent references from PubMed and VetMedResource.
• D’Ovidio D & Santoro D (2022) Efficacy of a spot-on combination of fluralaner plus moxidectin (Bravecto plus) against naturally acquired Sarcoptes scabiei infestation in 10 pet rabbits: Retrospective case series. Vet Derm WileyOnline.
• Singh S K, Jaiswal A K, Kumari S et al (2022) Therapeutic effects of oral fluralaner in pet rabbits with severe sarcoptic mange (Sarcoptes scabiei). Vet Parasitol 304, 109693 PubMed.
• D’Ovidio D & Santoro D (2021) Efficacy of Fluralaner in the Treatment of Sarcoptic Mange (Sarcoptes scabiei) in 12 Pet Rabbits, Topics Comp Anim Med 43, 100528 SciDirect.
• Sojka P A (2018) Isoxazolines. J Exotic Pet Med 27 (2), 118-122 VetMedResource.
• Sheinberg G, Romero C, Heredia R et al (2017) Use of oral fluralaner for the treatment of Psoroptes cuniculi in 15 naturally infested rabbits. Vet Derm 28 (4), 393-396 PubMed.
• Zhao C & Casida J E (2014) Insect γ-aminobutyric acid receptors and isoxazoline insecticides: toxicological profiles relative to the binding sites of [³H]fluralaner, [³H]-4'-ethynyl-4-n-propylbicycloorthobenzoate, and [³H]avermectin. J Agric Food Chem 62 (5), 1019-1024 PubMed.

Other sources of information

• Merck Animal Health (2022) Bravecto. Website: www.bravecto.com.
• Varga M & Paterson S (2021) Dermatologic Diseases of Rabbits. In: Ferrets, Rabbits and Rodents Clinical Medicine and Surgery. 4th edn. Eds: Quesenberry K E, Orcutt C J, Mans C & Carpenter J W. Elsevier, USA. pp 220-232.
• US Food and Drugs Administration (2014) Bravecto - Freedom of Information Summary. Website: https://animaldrugsatfda.fda.gov.
• European Medicines Agency (online) Bravecto - Summary of Product Characteristics. Website: www.ema.europa.eu (pdf download).
• European Medicines Agency (online) CVMP Assessment Report for Bravecto. Website: www.ema.europa.eu (pdf download).

Organisation(s)

• American Association of Veterinary Parasitologists (AAVP). Website: www.aavp.org.
• Companion Animal Parasite Council (CAPC). Website: www.capcvet.org.
• European Scientific Counsel Companion Animal Parasites (ESCCAP). Website: www.esccap.org.
• European Veterinary Parasitology College (EBVS). Website: www.eurovetpar.org.