Influence of P-glycoprotein inhibition on secretion of ivermectin and doramectin by milk in lactating sheep

Antonić, Jan; Grabnar, Iztok; Milčinski, Luka; Škibin, Andrej; Süssinger, Adica; Pogačnik, M.; Cerkvenik-Flajs, Vesna

doi:10.1016/j.vetpar.2011.03.002

Cited by 5 publications

(1 citation statement)

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“…1 The parasiticide agents allowed for controlling endo and ecto-parasites in sheep, the macrocyclic lactones, have been widely employed over the world because of its high efficiency and broad-spectrum activity. 2 The moxidectin (MOX) (Figure 1), semisynthetic derivative of nemadectin, is a macrocyclic lactone obtained by the fermentation of Streptomyces cyanogriseus. 3 In the last decade MOX has emerged in sheep flocks in Brazil due to its efficacy against a wide variety of nematodes and arthropod parasites, even at extremely low doses.…”

Section: Introductionmentioning

confidence: 99%

Determination of Moxidectin in Serum by Liquid Chromatography-Tandem Mass Spectrometry and Its Application in Pharmacokinetic Study in Lambs

Baptista¹,

Fernandes²,

Gilaverte³

et al. 2016

Journal of the Brazilian Chemical Society

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The widespread use of moxidectin (MOX), a parasiticide used in the sheep breeding, has induced the parasite resistance in Brazilian farms. As a consequence, the farmers often increase the dose and frequency of drug utilization, and disregards safety of meat or milk. In order to establish adequate therapeutic treatment it is necessary to know the pharmacokinetics of the drug in the animal's body. Thus, high performance liquid chromatography-electrospray ionization-tandem mass spectrometry (HPLC-ESI-MS/MS) method was developed for the determination of MOX in serum lamb. Serum samples were treated with acetonitrile to precipitate proteins. A clean up by dispersive extraction in solid phase (SPE-d), using primary/secondary amine (PSA) and C18 sorbents, followed by freezing was performed. Method validation presented precision (coefficient of variation) and accuracy (recovery%) between 1.7-6.7 and 80.0-107.3%, respectively. The limit of quantification (LOQ) of the method was 2.0 ng mL -1 and a linear response was obtained over a range of 2.0 to 100 ng mL -1 . This method was successfully applied to the determination of MOX in serum from suffolk lamb to evaluate the pharmacokinetic profile. Keywords: serum lamb, moxidectin, veterinary drug, pharmacokinetic, LC-MS/MS IntroductionThe infections with gastrointestinal nematodes have constituted major obstacle to the expansion of the sheep industry in Brazil. The gastrointestinal parasitism is associated with physiological changes in animals, such as bowel dysfunction and nutritional stress that result in decreased body condition, lower weight gain and death of animals. Among the most important parasites that affect sheep flocks we can highlight the Haemonchus contortus. The parasiticide agents allowed for controlling endo and ecto-parasites in sheep, the macrocyclic lactones, have been widely employed over the world because of its high efficiency and broad-spectrum activity.2 The moxidectin (MOX) (Figure 1), semisynthetic derivative of nemadectin, is a macrocyclic lactone obtained by the fermentation of Streptomyces cyanogriseus. 3 In the last decade MOX has emerged in sheep flocks in Brazil due to its efficacy against a wide variety of nematodes and arthropod parasites, even at extremely low doses. 4 However, similarly as occurred with other drugs, indiscriminate use of MOX could induce parasite resistance, affecting the efficiency of the drug.5 Actually, similarly to ivermectin and the benzimidazole, parasite resistance against MOX has been reported in Brazil. 6 As an action of parasite resistance control, alternatives have been studied in order to minimize the spread of animal diseases and the damage to the breeding and may be referred: correct management and grazing, proper sheep nutrition, selection of resistant animals, biological control, use of vaccines, herbal medicine and/or the use of techniques for assessing the degree of infection. 7Chromatographic methods for the determination of MOX in plasma from different species (alpacas, cattle, horses, pig, rabbit and s...

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Section: Introductionmentioning

confidence: 99%