Ivermectin in Senegalese Peulh Sheep: Influence of Sex on Plasma Disposition

Ndong, T. Bengone; Kane, Yaghouba; Diouf, E. H. M.; Alvinerie, M.

doi:10.1007/s11259-007-3522-6

Cited by 9 publications

(3 citation statements)

References 37 publications

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“…Gender influence on the in‐vivo disposition kinetics of these macrocyclic lactones has been observed in different animal species. In cattle and sheep the plasma levels of ivermectin after its subcutaneous administration were higher in females than males [15,16] . Similar sex‐dependent differences were observed for selamectin, a structurally‐related antiparasitic compound, in dogs [17] .…”

Section: Introductionsupporting

confidence: 57%

“…In addition, Ndong et al . [16] reported sex‐related differences in the bioavailability of ivermectin in Senegalese sheep, where the area under the curve (AUC) was 69% higher in females than males. The administration of selamectin, an avermectin topically applied to dogs, also showed a differential pharmacokinetic pattern between male and female, where systemic drug exposure was 93% higher in female compared with male Beagle dogs [17] .…”

Section: Discussionmentioning

confidence: 99%

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Gender-related differences on P-glycoprotein-mediated drug intestinal transport in rats

Ballent

Lifschitz

Virkel

et al. 2011

Journal of Pharmacy and Pharmacology

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Section: Introductionsupporting

confidence: 57%

Section: Discussionmentioning

confidence: 99%

Gender-related differences on P-glycoprotein-mediated drug intestinal transport in rats

Ballent

Lifschitz

Virkel

et al. 2011

Journal of Pharmacy and Pharmacology

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“…It has been recently reported that significantly larger (68.7%) AUC of IVM was observed in female sheep compared with male sheep after subcutaneous administration. 20 In a previous study, the effect of lipid ingestion on the kinetic disposition of MXD has been investigated in rabbits following oral administration at a dose rate of 0.3 mg/kg. 13 This study suggested that lipid administration increases the systemic availability of oral MXD.…”

Section: Discussionmentioning

confidence: 99%

Plasma dispositions of ivermectin, doramectin and moxidectin following subcutaneous administration in rabbits

et al. 2010

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This study evaluated the comparative plasma dispositions of ivermectin (IVM), doramectin (DRM) and moxidectin (MXD) following subcutaneous administration in rabbits. Fifteen New Zealand white rabbits were allocated into three groups of five animals each. The animals in each group received IVM, DRM or MXD by subcutaneous injection at a single dose of 0.3 mg/kg. Blood samples were collected at various times between 1 h and 40 days after treatment and the plasma samples were analysed by high-performance liquid chromatography using fluorescence detection. Moxidectin was absorbed faster from the injection site and reached the peak plasma concentration (C max ) significantly earlier than IVM and DRM. There was no significant difference in C max values among the three molecules, whereas the area under the concentration -time curves of DRM (258.40 ng.d/mL) and IVM (191.62 ng.d/mL) was significantly higher than that of MXD (83.17 ng.d/mL). The mean plasma residence time and terminal half-life (t 1/2lz ) were longer for DRM (7.52 and 4.48 days, respectively) and MXD (8.97 and 8.16 days, respectively) compared with IVM (4.73 and 2.75 days, respectively). Considering the pharmacokinetic parameters for the parent molecules, the persistence of DRM and MXD are significantly longer than IVM and this may have a positive effect on their efficacy in rabbits following subcutaneous administration or utility relating to interdosing interval. Avermectins and milbemycins have been used intensively to control parasites of animals, humans and crops worldwide. Both chemical groups are naturally derived 16-membered macrocyclic lactones 1 produced by the soil dwelling actinomycetes, Streptomyces spp. Milbemycins are structurally related to the avermectins and share physicochemical properties with avermectins. Avermectins and milbemycins have excellent activity against nematodes and have systemic activity against several pathogenic ectoparasites of domestic animals at low dosage rates. Due to the high activity of avermectins and milbemycins against both nematodes and arthropods, they are now classified as 'endectocides'.2 The pharmacokinetic behaviour of avermectins and milbemycins is significantly affected by route of administration, formulation of the drug, and interspecies and interindividual variation.2 These anthelmintics are highly lipophilic substances, and are extensively distributed throughout the body and slowly eliminated through tissues such as liver and fat.3 For this reason a larger volume of distribution (V d ) may be obtained for these compounds compared with other anthelmintics. 4 Rabbits are widely used as laboratory animals for animal experiments. Endectocides are used extralabelly to control particularly ectoparasites, such as mite and mange infestations in rabbits.5212 Pharmacokinetic behaviours of endectocides have been extensively studied in different animal species. Although kinetic dispositions of ivermectin (IVM) have been reported previously, 6,13 very little information is available on the plasma pharma...

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The effect of sheep breed, age, and gender on the pharmacokinetics and efficacy of monepantel, an amino-acetonitrile derivative

et al. 2009

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This analysis investigated the influence of breed and gender on the pharmacokinetics of monepantel, and influence of breed, age, and gender on its efficacy against gastrointestinal nematodes of sheep. In a comparison of pharmacokinetic profiles from two studies, Merino lambs had significantly greater maximum concentrations of monepantel and monepantel sulfone, and faster times to reach these concentrations than Dorset cross lambs. Males had a statistically greater area under the curve (0-504 h) than females for monepantel sulfone. The biological relevance of these relatively small differences is unclear because efficacy was not evaluated in these studies. For efficacy, a breed effect existed for some nematodes when sheep were treated at a sub-optimum dose (1.25 mg/kg). There were no gender effects between sheep infected with adult parasites and treated at 1.25 mg/kg but there were differences between females and males treated at this dose when infected with fourth-stage larvae of Haemonchus contortus, Teladorsagia circumcincta, Trichostrongylus colubriformis, and Cooperia curticei. There were no breed or gender differences for sheep treated at the recommended dose (2.5 mg/kg). There was a potential trend for declining efficacy with increasing animal age for fourth-stage Trichostrongylus axei. This analysis demonstrated that, similarly to what is observed with other anthelmintics, the pharmacokinetics and efficacy of monepantel can vary with factors like breed, age, and gender. Identifying these covariates is important for understanding inter-individual variability in drug response. While further investigation is warranted, correctly treating sheep at the recommended dose of 2.5 mg/kg appears to mitigate any associated risk.

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Ivermectin in Senegalese Peulh Sheep: Influence of Sex on Plasma Disposition

Cited by 9 publications

References 37 publications

Gender-related differences on P-glycoprotein-mediated drug intestinal transport in rats

Gender-related differences on P-glycoprotein-mediated drug intestinal transport in rats

Plasma dispositions of ivermectin, doramectin and moxidectin following subcutaneous administration in rabbits

The effect of sheep breed, age, and gender on the pharmacokinetics and efficacy of monepantel, an amino-acetonitrile derivative

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