Pharmacokinetics of combination antiparasitic drug preparation for dogs and cats in the form of spot-on solution

Abstract

Objective: The object of the study was to examine the major pharmacokinetic parameters after a single application of a complex drug preparation for veterinary use based on fipronil, praziquantel, moxidectin, and pyriproxyfen in cats and dogs. Materials and Methods: For dogs, the drug preparation was administered spot-on solution in the following dosage of active pharmaceutical substances: fipronil 27.0 mg/kg body weight (bwt), praziquantel 10.8 mg/kg bwt, moxidectin 6.75 mg/kg bwt, and pyriproxyfen 5.4 mg/kg bwt; for cats, the dosage was the following: fipronil 43.2 mg/kg bwt, praziquantel 17.28 mg/kg bwt, moxidectin 4.32 mg/kg bwt, and pyriproxyfen 8.64 mg/kg bwt. The blood samples were taken from dogs and cats. The principle of the method for determining praziquantel, trans-4-hydroxypraziquantel, pyriproxyfen, and fipronil in serum samples was chromatographed in a high-pressure liquid chromatograph with detection by means of a mass-spectrometric detector. The moxidectin content of the blood was detected by high-performance liquid chromatography. Results: The drug preparation active substances: praziquantel, fipronil, and moxidectin are absorbed into the blood of dogs and cats. The penetration of praziquantel into the systemic circulation and further into organs and tissues was proved. After topical administration, moxidectin is absorbed and distributed systemically and is slowly removed from the plasma, which manifests itself in detectable concentrations of moxidectin in the blood for 1 month. Conclusion: The present results of pharmacokinetic investigations may promote to the determination of effective therapy strategy and prophylaxis of parasitic diseases in dogs and cats.

Evaluation of the Acaricidal Effectiveness of Fipronil and Phoxim in Field Populations of Dermanyssus gallinae (De Geer, 1778) from Ornamental Poultry Farms in Italy

“…The use of fipronil, a progenitor of the phenylpyrazole class, against Dermanyssus in addition to being prohibited is rather empirical. In fact, even if used as an insecticide in agriculture and against ectoparasites, including ticks, in pets such as dog and cats [35,36], there is little evidence in the literature regarding its in vitro effectiveness against Dermanyssus, and there are conflicting data. In an in vitro study, Kim et al [37] tested fipronil as a pure substance by calculating how many milligrams of molecule were present in one cm 2 of filter paper in contact with the mites.…”

A dirofilariasis mouse model for heartworm preclinical research

“…For future pharmacological investigations, to fully enable characterisation of interactions between sex and the drug pharmacokineticpharmacodynamic (PK-PD) relationship, it would be useful to assess whether D. immitis are able to develop within female NSG mice. In natural hosts, injectable formulations of moxidectin are proven to mediate 100% preventative efficacies [37].The substantial yet incomplete moxidectin responses in our NSG/NXG model may reflect full efficacy evolves over an extended time-period, particularly considering that this ML depots in fatty subcutaneous tissues and delivers a long-tail of systemic exposure, detectable over one month [57,58]. Alternatively, an immunopharmacological mode-of-action involving disruption of immunosuppressive parasite secretions and an activated host-immune response has been proffered as one rationale why filarial larvae are differentially sensitive to ML-drugs at physiological levels in vitro vs in vivo [59].…”

Arachnoentomoses of domestic carnivores and effectiveness of insacar total in dogs otodectosis

“…The results obtained by us on the age dynamics of aphanipterosis agree with the data obtained by Zhemchueva G. V. (figure 4). Due to the fact that arachno myiosis of domestic carnivores are quite widespread in the Russian Federation, as well as in cross-border territories, the problem of finding highly effective drugs for their treatment is very relevant [9].…”