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Plasma pharmacokinetic profile of fluralaner (Bravecto™) and ivermectin following concurrent administration to dogs.

Walther FM, Allan MJ, Roepke RK - Parasit Vectors (2015)

Bottom Line: Blood plasma samples were collected at multiple post-treatment time points over a 12-week period for fluralaner and ivermectin plasma concentration analysis.Concurrent administration of fluralaner and ivermectin does not alter the pharmacokinetics of either compound.Based on the plasma pharmacokinetic profile and the clinical observations, there is no evident interaction between fluralaner and ivermectin, and co-administration does not increase the risk of ivermectin associated neurotoxicity.

View Article: PubMed Central - PubMed

Affiliation: Merck Animal Health, 2 Giralda Farms, Madison, NJ, USA. feli.walther@merck.com.

ABSTRACT

Background: Fluralaner is a novel systemic ectoparasiticide for dogs providing immediate and persistent flea, tick and mite control after a single oral dose. Ivermectin has been used in dogs for heartworm prevention and at off label doses for mite and worm infestations. Ivermectin pharmacokinetics can be influenced by substances affecting the p-glycoprotein transporter, potentially increasing the risk of ivermectin neurotoxicity. This study investigated ivermectin blood plasma pharmacokinetics following concurrent administration with fluralaner.

Findings: Ten Beagle dogs each received a single oral administration of either 56 mg fluralaner (Bravecto™), 0.3 mg ivermectin or 56 mg fluralaner plus 0.3 mg ivermectin/kg body weight. Blood plasma samples were collected at multiple post-treatment time points over a 12-week period for fluralaner and ivermectin plasma concentration analysis. Ivermectin blood plasma concentration profile and pharmacokinetic parameters Cmax, tmax, AUC∞ and t½ were similar in dogs administered ivermectin only and in dogs administered ivermectin concurrently with fluralaner, and the same was true for fluralaner pharmacokinetic parameters.

Conclusions: Concurrent administration of fluralaner and ivermectin does not alter the pharmacokinetics of either compound. Based on the plasma pharmacokinetic profile and the clinical observations, there is no evident interaction between fluralaner and ivermectin, and co-administration does not increase the risk of ivermectin associated neurotoxicity.

No MeSH data available.


Related in: MedlinePlus

Mean ivermectin plasma concentration (± standard deviation) in dogs following oral administration (0.3 mg/kg BW) alone or concurrently with fluralaner (56 mg/kg BW)
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Fig1: Mean ivermectin plasma concentration (± standard deviation) in dogs following oral administration (0.3 mg/kg BW) alone or concurrently with fluralaner (56 mg/kg BW)

Mentions: The plasma concentration versus time profile of ivermectin was comparable in dogs administered ivermectin only and in dogs administered ivermectin concurrently with fluralaner (Fig. 1). Similarly, the plasma concentration versus time profile of fluralaner was comparable in dogs administered fluralaner only and in dogs administered fluralaner concurrently with ivermectin (Fig. 2). The pharmacokinetic parameters of both, ivermectin and fluralaner, were also comparable across groups (Tables 2 and 3), with no statistical significant differences between groups.Fig. 1


Plasma pharmacokinetic profile of fluralaner (Bravecto™) and ivermectin following concurrent administration to dogs.

Walther FM, Allan MJ, Roepke RK - Parasit Vectors (2015)

Mean ivermectin plasma concentration (± standard deviation) in dogs following oral administration (0.3 mg/kg BW) alone or concurrently with fluralaner (56 mg/kg BW)
© Copyright Policy - OpenAccess
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC4595236&req=5

Fig1: Mean ivermectin plasma concentration (± standard deviation) in dogs following oral administration (0.3 mg/kg BW) alone or concurrently with fluralaner (56 mg/kg BW)
Mentions: The plasma concentration versus time profile of ivermectin was comparable in dogs administered ivermectin only and in dogs administered ivermectin concurrently with fluralaner (Fig. 1). Similarly, the plasma concentration versus time profile of fluralaner was comparable in dogs administered fluralaner only and in dogs administered fluralaner concurrently with ivermectin (Fig. 2). The pharmacokinetic parameters of both, ivermectin and fluralaner, were also comparable across groups (Tables 2 and 3), with no statistical significant differences between groups.Fig. 1

Bottom Line: Blood plasma samples were collected at multiple post-treatment time points over a 12-week period for fluralaner and ivermectin plasma concentration analysis.Concurrent administration of fluralaner and ivermectin does not alter the pharmacokinetics of either compound.Based on the plasma pharmacokinetic profile and the clinical observations, there is no evident interaction between fluralaner and ivermectin, and co-administration does not increase the risk of ivermectin associated neurotoxicity.

View Article: PubMed Central - PubMed

Affiliation: Merck Animal Health, 2 Giralda Farms, Madison, NJ, USA. feli.walther@merck.com.

ABSTRACT

Background: Fluralaner is a novel systemic ectoparasiticide for dogs providing immediate and persistent flea, tick and mite control after a single oral dose. Ivermectin has been used in dogs for heartworm prevention and at off label doses for mite and worm infestations. Ivermectin pharmacokinetics can be influenced by substances affecting the p-glycoprotein transporter, potentially increasing the risk of ivermectin neurotoxicity. This study investigated ivermectin blood plasma pharmacokinetics following concurrent administration with fluralaner.

Findings: Ten Beagle dogs each received a single oral administration of either 56 mg fluralaner (Bravecto™), 0.3 mg ivermectin or 56 mg fluralaner plus 0.3 mg ivermectin/kg body weight. Blood plasma samples were collected at multiple post-treatment time points over a 12-week period for fluralaner and ivermectin plasma concentration analysis. Ivermectin blood plasma concentration profile and pharmacokinetic parameters Cmax, tmax, AUC∞ and t½ were similar in dogs administered ivermectin only and in dogs administered ivermectin concurrently with fluralaner, and the same was true for fluralaner pharmacokinetic parameters.

Conclusions: Concurrent administration of fluralaner and ivermectin does not alter the pharmacokinetics of either compound. Based on the plasma pharmacokinetic profile and the clinical observations, there is no evident interaction between fluralaner and ivermectin, and co-administration does not increase the risk of ivermectin associated neurotoxicity.

No MeSH data available.


Related in: MedlinePlus