Pharmacokinetics of moxidectin and doramectin in goats

Escudero, Elisa; Cárceles, C. M.; Diaz, M.S; Sutra, J.F.; Galtier, P.; Alvinerie, M.

doi:10.1053/rvsc.1998.0304

Cited by 58 publications

(42 citation statements)

References 15 publications

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“…The verified value was 78.5 ± 12.7 ng day mL -1 , which is similar to that reported by Dupuy et al 27 in lambs (73.26 ± 25.60 ng day mL -1 ) and smaller than the reported by Escudero et al 28 in goats of the Murciano-Granadina breed (136 ng day mL -1 ), with body weight between 31 and 45.8 kg, and 1.5 to 3 years old. The lower area under the curve values obtained in the present study, when compared with Escuredo et al, 28 may be related to the minor body fat storage in lambs when compared to adult animals. 29 Previous studies have also shown that the PK of endectocides presents variability according to the specie.…”

Section: Pharmacokinetic Study Of Moxidectinsupporting

confidence: 87%

“…MOX elimination half-life time value was 9.0 ± 3.8 days. Thus, the elimination half-life of MOX in lambs was similar than the values reported for male cattle, body weight between 180 and 210 kg, 10 months old (14.5 ± 1.2 days) and adult goats (9.9 ± 1.1 days ), 28,30 that received the same dose by the same route of exposure. The deposit of MOX in adipose tissue functions as a reservoir for the drug, releasing it gradually into the bloodstream and contributing for its long half-life elimination and, consequently, to the persistence of the molecule activity on target parasites.…”

supporting

confidence: 79%

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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: Pharmacokinetic Study Of Moxidectinsupporting

confidence: 87%

supporting

confidence: 79%

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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“…Por conseguinte é suspeitado que RA pareça emergir rapidamente em nematóides infectando cabras, que conseqüentemente podem ser transferidos para as ovelhas (Escudero et al 1999). Isto já tem acontecido para nematóides resistentes para levamisole e benzimidazoles (Conder & Campbell 1995) e possivelmente para lactonas macrocíclicas (Escudero et al 1999).…”

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Sensibilidade dos nematóides gastrintestinais de caprinos a anti-helmínticos na mesorregião do Sertão Paraibano

Rodrigues

Athayde²,

Rodrigues³

et al. 2007

Pesq. Vet. Bras.

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Evalu-Evalu-EvaluEvalu-Evaluation of the efficacy of antihelmintics to control gastrointestinal nematodes in goats ation of the efficacy of antihelmintics to control gastrointestinal nematodes in goats ation of the efficacy of antihelmintics to control gastrointestinal nematodes in goats ation of the efficacy of antihelmintics to control gastrointestinal nematodes in goats ation of the efficacy of antihelmintics to control gastrointestinal nematodes in goats raised in the state of P raised in the state of P raised in the state of P raised in the state of P raised in the state of Paraíba araíba araíba araíba araíba.] Sensibilidade dos nematóides gastrintestinais de caprinos a anti-helmínticos na mesorregião do sertão paraibano. Pesquisa Veterinária Brasileira 27 (4) The objective was to evaluate conventional and alternative anthelminthic action on the sensibility of gastrointestinal nematodes in goats. Hundred and twenty goats of both sexes were distributed into 10 groups of 24 animals each (12 males and 12 females) and submitted to treatments of specific anthelminthic composition. The commercial drugs used were moxidectin 0.2%, albendazole, levamisol chlorhydrate, ivermectin and an aqueous extract of the purgative potato (Operculina hamiltonii). The reduction test was applied through egg counts per gram of feces and larval culture to evaluate resistance. The fecal samples were collected in the day when medication was accomplished (day base), at 7, 14 and 21 days after treatment. The following results for the reduction of Trichostrongyloidea eggs were obtained: Treatment of the females with Moxidectina reduced the egg counts to 92.8, 88.7 and 89.8%, of the males to 92.6, 96.2 and 98.1%; with Levamisol of the females to 96, 97.1 and 91%, of the males to 85.7, 94,2 and 100%; with Albendazol of the females 65, 60.3 and 75.4%, of the males 88.8, 88.8 and 55.5%; with Ivermectin of the females to 92.2, 68.6 and 70.6%, of the males to 41.7, 73.6 and 59.7%; and with the purgative potato of the females to 31.8, 34.1 and 49.4%, of the males to 61.5, 80.7 and 50%. In larval culture Haemonchus, followed by Bunostomum, Trichostrongylus, and Oesophagostomum, were identified even after treatments.

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“…Ces différences ont été observées par de nombreux auteurs chez la plupart des autres espèces animales (3,9,12). Elles peuvent être expliquées par les propriétés physico-chimiques propres à chaque principe parental, associées à la nature de la formulation.…”

Section: Figure 1 : éVolution Des Concentrations Plasmatiques De Doraunclassified

Propriétés cinétiques et thérapeutiques des lactones macrocycliques endectocides, doramectine et moxidectine, chez le bovin N’Dama (<em>Bos taurus</em>) au Gabon

Bengone-Ndong¹,

Adjomo-Mba²,

Mabika-Moussavou

et al. 2010

Rev. Elev. Med. Vet. Pays Trop.

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La cinétique plasmatique et l’efficacité de la doramectine et de la moxidectine ont été étudiées chez le bovin de race taurine N’Dama après administration sous-cutanée à la dose recommandée pour les bovins (0,2 mg/kg). Les valeurs du temps de demi-absorption ont montré une absorption significativement plus rapide de la moxidectine (0,05 jour pour la moxidectine contre 1,7 jour pour la doramectine). Les concentrations maximales obtenues n’ont pas été statistiquement différentes, mais elles ont été atteintes plus rapidement avec la moxidectine (0,3 jour) qu’avec la doramectine (4,8 jours). L’exposition, mesurée par l’aire sous la courbe, a été plus importante pour la doramectine (458 ng.jour/ml) que pour la moxidectine (159 ng.jour/ml), alors que la moxidectine a semblé plus rémanente. Les deux molécules ont présenté une efficacité de 100 p. 100 entre les quinzième et trentième jours qui ont suivi le traitement. Ces résultats sont comparables à ceux obtenus chez les autres races taurines de bovins. La doramectine et la moxidectine peuvent donc être recommandées dans la lutte contre les parasitoses gastro-intestinales de la vache N’Dama en région tropicale humide.

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Pharmacokinetics of moxidectin and doramectin in goats

Cited by 58 publications

References 15 publications

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

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

Sensibilidade dos nematóides gastrintestinais de caprinos a anti-helmínticos na mesorregião do Sertão Paraibano

Propriétés cinétiques et thérapeutiques des lactones macrocycliques endectocides, doramectine et moxidectine, chez le bovin N’Dama (<em>Bos taurus</em>) au Gabon

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