Safety of concurrent treatment of dogs with fluralaner (Bravecto™) and milbemycin oxime - praziquantel

Walther, Feli M; Fisara, Petr; Allan, Mark J; Roepke, Rainer K. A.; Nuernberger, Martin C

doi:10.1186/s13071-014-0481-y

Cited by 7 publications

(1 citation statement)

References 4 publications

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“…by inhibition of MDR1-mediated fluralaner efflux by the premedication via drug-drug interaction. However, fluralaner was shown to be safe when administered concurrently with milbemycin oxime + praziquantel [22].…”

Section: Discussionmentioning

confidence: 99%

Suspected neurological toxicity after oral application of fluralaner (Bravecto®) in a Kooikerhondje dog

et al. 2019

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Background Although the new isoxazoline drug fluralaner (Bravecto®) is generally well tolerated in dogs, adverse drug reactions involving neurological dysfunction occurred in individual dogs. However, most of these cases are documented inadequately and none of them is reported and discussed in the literature. As isoxazoline drugs target neuronal chloride channels with a clear preference for invertebrates, they are considered to have a good safety profile. However, pharmacodynamic effects in the nervous system of vertebrates cannot be ruled out completely. Case presentation A seven-month-old female Kooikerhondje dog was treated with Bravecto® at the recommended dose. About 24 h after administration, the dog exhibited signs of neurological toxicity, including generalized ataxia, myoclonic jerks, tremor of head and body, muscle twitching and oral dysphagia. All symptoms were transient and the dog fully recovered without any treatment after 10 h. Conclusion This case report describes transient occurrence of neurological dysfunction after administration of Bravecto®. It may help to better classify adverse drug reactions after application of isoxazoline drugs and documents a good prognosis even after occurrence of severe neurological dysfunction in the present case. Electronic supplementary material The online version of this article (10.1186/s12917-019-2016-4) contains supplementary material, which is available to authorized users.

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Section: Discussionmentioning

confidence: 99%

Suspected neurological toxicity after oral application of fluralaner (Bravecto®) in a Kooikerhondje dog

et al. 2019

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Fluralaner activity against life stages of ticks using Rhipicephalus sanguineus and Ornithodoros moubata IN in vitro contact and feeding assays

Williams

Zoller

Roepke

et al. 2015

Parasites & Vectors

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BackgroundFluralaner is a novel isoxazoline eliciting both acaricidal and insecticidal activity through potent blockage of GABA- and glutamate-gated chloride channels. The aim of the study was to investigate the susceptibility of juvenile stages of common tick species exposed to fluralaner through either contact (Rhipicephalus sanguineus) or contact and feeding routes (Ornithodoros moubata).MethodsFluralaner acaricidal activity through both contact and feeding exposure was measured in vitro using two separate testing protocols. Acaricidal contact activity against Rhipicephalus sanguineus life stages was assessed using three minute immersion in fluralaner concentrations between 50 and 0.05 μg/mL (larvae) or between 1000 and 0.2 μg/mL (nymphs and adults). Contact and feeding activity against Ornithodoros moubata nymphs was assessed using fluralaner concentrations between 1000 to 10−4 μg/mL (contact test) and 0.1 to 10−10 μg/mL (feeding test). Activity was assessed 48 hours after exposure and all tests included vehicle and untreated negative control groups.ResultsFluralaner lethal concentrations (LC50, LC90/95) were defined as concentrations with either 50%, 90% or 95% killing effect in the tested sample population. After contact exposure of R. sanguineus life stages lethal concentrations were (μg/mL): larvae - LC50 0.7, LC90 2.4; nymphs - LC50 1.4, LC90 2.6; and adults - LC50 278, LC90 1973. After exposure of O. moubata nymphs to fluralaner lethal concentrations were (μg/mL): contact exposure - LC50 720, LC95 1133; and feeding exposure- LC50 0.00007, LC95 0.09.ConclusionsFluralaner demonstrates potent in vitro acaricidal activity against all life stages of the brown dog tick, R.sanguineus. The testing of fluralaner contact and feeding routes using O. moubata nymphs demonstrates a high acaricidal activity in both exposure routes.

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A quantitative evaluation of the extent of fluralaner uptake by ticks (Ixodes ricinus, Ixodes scapularis) in fluralaner (BravectoTM) treated vs. untreated dogs using the parameters tick weight and coxal index

et al. 2015

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BackgroundFluralaner is a new antiparasitic drug that was recently introduced as BravectoTM chewable tablets for the treatment of tick and flea infestations in dogs. Most marketed tick products exert their effect via topical application and contact exposure to the parasite. In contrast, BravectoTM delivers its acaricidal activity through systemic exposure. Tick exposure to fluralaner occurs after attachment to orally treated dogs, which induces a tick-killing effect within 12 h. The fast onset of killing lasts over the entire treatment interval (12 weeks) and suggests that only marginal uptake by ticks is required to induce efficacy. Three laboratory studies were conducted to quantify the extent of uptake by comparison of ticks’ weight and coxal index obtained from BravectoTM-treated and negative-control dogs.MethodsThree studies were conducted using experimental tick infestation with either Ixodes ricinus or Ixodes scapularis after oral administration of fluralaner to dogs. All studies included a treated (BravectoTM chewable tablets, MSD Animal Health) and a negative control group. Each study had a similar design for assessing vitality and weighing of ticks collected from dogs of both groups. Additionally, in one study the coxal index (I. ricinus) was calculated as a ratio of tick’s ventral coxal gap and dorsal width of scutum. Tick weight data and coxal indices from BravectoTM-treated and negative-control groups were compared via statistical analysis.ResultsTicks collected from BravectoTM-treated dogs weighed significantly less (p ≤ 0.0108) than ticks collected from negative-control dogs, and their coxal index was also significantly lower (p < 0.0001). The difference in tick weights was demonstrated irrespective of the tick species investigated (I. ricinus, I. scapularis). At some assessments the mean tick weights of BravectoTM-treated dogs were significantly lower than those of unfed pre-infestation (baseline) ticks. The demonstrated tick-killing efficacy was in the range of 94.6 – 100 %.ConclusionsTick weights and coxal indices confirm that a minimal uptake results in a sufficient exposure of ticks to fluralaner (BravectoTM) and consequently in a potent acaricidal effect.

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Safety of concurrent treatment of dogs with fluralaner (Bravecto™) and milbemycin oxime - praziquantel

Cited by 7 publications

References 4 publications

Suspected neurological toxicity after oral application of fluralaner (Bravecto®) in a Kooikerhondje dog

Suspected neurological toxicity after oral application of fluralaner (Bravecto®) in a Kooikerhondje dog

Fluralaner activity against life stages of ticks using Rhipicephalus sanguineus and Ornithodoros moubata IN in vitro contact and feeding assays

A quantitative evaluation of the extent of fluralaner uptake by ticks (Ixodes ricinus, Ixodes scapularis) in fluralaner (BravectoTM) treated vs. untreated dogs using the parameters tick weight and coxal index

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