Canis ISSN: 2398-2942

Spinosad

Synonym(s): Comfortis®, Trifexis®

Contributor(s): Linda Horspool

Introduction

Name

  • IUPAC
  • CAS

Class of drug

  • Spinosyn - mixture of spinosyns A and D.
  • Macrolides (non-antibacterial) containing a unique tetracyclic ring system with two sugar derivatives (forosamine and rhamnose sugars) attached through ether linkages.

Description

Chemical name

  • Spinosyn A: 2-((6-deoxy-2,3,4-tri-O-methyl-a-L- mannopyranosyl)oxy)-13-(((5- dimethylamino)tetrahydro-6-methyl- 2H-pyran-2-yl)oxy)-9-ethyl- 2,3,3a,5a,5b,6,9,10,11,12,13,14,16a,16 b-tetradecahydro-14-methyl-1H-as- indaceno(3,2-d)oxacyclododecin-7,15- dione.
  • Spinosyn D: 2-((6-deoxy-2,3,4-tri-O-methyl-a-L- mannopyranosyl)oxy)-13-(((5- dimethylamino)tetrahydro-6-methyl- 2H-pyran-2-yl)oxy)-9-ethyl- 2,3,3a,5a,5b,6,9,10,11,12,13,14,16a,16 b-tetradecahydro-4,14-dimethyl-1H-as- indaceno(3,2-d)oxacyclododecin-7,15- dione.

Molecular formula

  • Spinosyn A C42H67NO16.
  • Spinosyn D C41H65NO16.

Molecular weight

  • Spinosyn A 731.98.
  • Spinosyn D 746.00.

Physical properties

Property Spinosyn A Spinosyn D
Water Solubility (at 25°c, pH7) 235 ppm 0.332 ppm
Octanol-water Partition Coefficient (log P, pH7) 4.0 4.5
Photolysis half-life 23 hours 20 hours
  • Product as packaged for sale:
    • Chewable tablets.
    • Flavored with artificial beef flavor.
    • Unscored tan to brown, or speckled, round, flat, bevelled edge tablets, plain on one side and debossed on the other.

Storage requirements

  • Product as packaged for sale:
    • Room temperature (between 9 and 25 °C).
    • Keep the blister pack in the outer carton.

Uses

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Indications

  • Ectoparasiticide. Insecticide. Adulticide.
  • Treatment of flea infestations (Ctenocephalides felis Ctenocephalides felis ) and prevention of re-infestation for up to 4 weeks.
  • Can be used as part of a treatment strategy for the control of flea-allergy dermatitis (FAD) Skin: flea bite hypersensitivity.

Administration

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Pharmocokinetics

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Precautions

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Interactions

with other drugs

  • Spinosad has been shown to be a substrate for P-glycoprotein (PgP). Spinosad could therefore interact with other PgP-substrates (for example, digoxin Digoxin , doxorubicin Doxorubicin ). This could lead to enhanced adverse reactions and/or compromised efficacy.
  • Concomitant use of spinosad with extra-label high dose ivermectin Ivermectin has led to some dogs experiencing trembling/twitching, salivation/drooling, seizures, ataxia, mydriasis, blindness and disorientation.
  • Spinosad has a different binding site from other nicotinic or GABAergic insecticides, such as neonicotinides (imidacloprid Imidacloprid or nitenpyram), phenylpyrazoles (fipronil Fipronil ), milbemycins Milbemycin oxime , avermectins (eg selamectin Selamectin ) or cyclodienes.

Adverse Reactions

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Further Reading

Publications

Refereed papers

  • Recent references from VetMedResource and PubMed.
  • Dryden M W, Payne P A, Smith V, Berg T C, Lane M (2013)Efficacy of selamectin, spinosad, and spinosad/milbemycin oxime against the KS1 Ctenocephalides felis flea strain infesting dogs.Parasit Vectors6, 80PubMed.
  • Dryden M W, Ryan W G, Bell M, Rumschlag A J, Young L M, Snyder D E (2013)Assessment of owner-administered monthly treatments with oral spinosad or topical spot-on fipronil/(S)-methoprene in controlling fleas and associated pruritus in dogs.Vet Parasitol191, 340-346PubMed.
  • Paarlberg T E, Wiseman S, Trout C M, Kee E A, Snyder D E (2013)Safety and efficacy of spinosad chewable tablets for treatment of flea infestations of cats.J Am Vet Med Assoc242, 1092-1098PubMed.
  • Snyder D E, Meyer K A, Wiseman S, Trout C M, Young D R (2013)Speed of kill efficacy and efficacy of flavored spinosad tablets administered orally to cats in a simulated home environment for the treatment and prevention of cat flea (Ctenocephalides felis) infestations.Vet Parasitol196, 492-496PubMed.
  • MacKay C S, Mattoon J S, Roberts G D, Tucker R L, Morimoto T R, Mealey K L (2012)Evaluation of the biliary and brain distribution of technetium Tc 99m sestamibi in healthy dogs with the ABCB1 wildtype genotype before and after treatment with spinosad.Am J Vet Res73, 814-820PubMed.
  • Ross D H, Arther R G, von Simson C, Doyle V, Dryden M W (2012)Evaluation of the efficacy of topically administered imidacloprid + pyriproxyfen and orally administered spinosad against cat fleas (Ctenocephalides felis): Impact of treated dogs on flea life stages in a simulated home environment.Parasit Vectors5, 192PubMed.
  • Schnitzler B, Hayes B, Wiseman S, Snyder D E (2012)Confirmation of the efficacy of a combination tablet of spinosad and milbemycin oxime against naturally acquired infections of canine intestinal nematode parasites.Vet Parasitol184, 279-283PubMed.
  • Snyder D E, Wiseman S (2012)Dose confirmation and non-interference evaluations of the oral efficacy of a combination of milbemycin oxime and spinosad against the dose limiting parasites, adult cat flea (Ctenocephalides felis) and hookworm (Ancylostoma caninum), in dogs.Vet Parasitol23(184), 284-290PubMed.
  • Wolken S, Franc M, Bouhsira E, Wiseman S, Hayes B, Schnitzler B, Jacobs D E (2012)Evaluation of spinosad for the oral treatment and control of flea infestations on dogs in Europe.Vet Rec170, 99PubMed.
  • Beugnet F, Doyle V, Murray M, Chalvet-Monfray K (2011)Comparative efficacy on dogs of a single topical treatment with the pioneer fipronil/(S)-methoprene and an oral treatment with spinosad against Ctenocephalides felis.Parasite18, 325-331PubMed.
  • Blagburn B L, Young D R, Moran C, Meyer J A, Leigh-Heffron A, Paarlberg T, Zimmermann A G, Mowrey D, Wiseman S, Snyder D E (2010)Effects of orally administered spinosad (Comfortis) in dogs on adult and immature stages of the cat flea (Ctenocephalides felis).Vet Parasitol168,312-317PubMed.
  • Sherman J G, Paul A J, Firkins L D (2010)Evaluation of the safety of spinosad and milbemycin 5-oxime orally administered to Collies with the MDR1 gene mutation.Am J Vet Res71, 115-119PubMed.
  • Franc M, Bouhsira E (2009)Evaluation of speed and duration of efficacy of spinosad tablets for treatment and control of Ctenocephalides canis (Siphonaptera: Pulicidae) infestations in dogs.Parasite16, 125-128PubMed.
  • Robertson-Plouch C, Baker K A, Hozak R R, Zimmermann A G, Parks S C, Herr C, Hart L M, Jay J, Hutchens D E, Snyder D E (2008)Clinical field study of the safety and efficacy of spinosad chewable tablets for controlling fleas on dogs.Vet Ther9, 26-36PubMed.

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