The effect of level of feed intake on the pharmacokinetic disposition and efficacy of ivermectin in sheep

Ali, D.N.; Hennessy, D.R.

doi:10.1111/j.1365-2885.1996.tb00018.x

Cited by 68 publications

(50 citation statements)

References 20 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Thus, drug efficacy can be improved by enhancing the concentration of MLs in the plasma and target tissues. Different physiological and pharmacological methods have been used to increase the systemic bioavailability of MLs, such as food restriction in sheep (Ali and Hennessy 1996), fasting in horses (Alvinerie et al 2000) and drug interference (Dupuy et al 2003). The possible involvement of the lymphatic route in the intestinal absorption of moxidectin led us to study the influence of lipid ingestion on the pharmacokinetic parameters of orally administered moxidectin.…”

Section: Discussionmentioning

confidence: 99%

Enhancement of oral moxidectin bioavailability in rabbits by lipid co-administration

2004

View full text Add to dashboard Cite

Moxidectin is a member of the macrocyclic lactone family of drugs widely used for the control of internal and external parasites. Because moxidectin is highly lipophilic, we suspect that lymphatic transport influences the intestinal absorption of oral formulations of the drug. We studied the influence of lipid coadministration on the pharmacokinetics of an oral formulation of moxidectin in rabbits. Ten rabbits were orally administered 0.3 mg kg À1 moxidectin with or without sunflower oil. Moxidectin and triglyceride were analyzed in plasma over 23 days. Sunflower oil coadministration significantly increased the area under the plasma concentration-time curve of moxidectin (98%, P<0.05) and prolonged its mean residence time from 1.52 days to 2.12 days (P<0.04). Simultaneously, an increase in plasma triglyceride was observed in response to oil administration. It is suggested that lipid administration increases the systemic availability of oral moxidectin by enhancing the extent of intestinal lymphatic transport of the drug. Lipid-based formulations should improve the bioavailability of moxidectin in rabbits.

show abstract

Section: Discussionmentioning

confidence: 99%

Enhancement of oral moxidectin bioavailability in rabbits by lipid co-administration

2004

View full text Add to dashboard Cite

show abstract

“…This explanation, however, is difficult to conciliate with our results, since the unabsorbed fraction of ingested ivermectin was fully recovered in the faeces of the lickers. Moreover, several studies argue for the stability of ivermectin in rumen fluids in cattle and sheep [3,6] and show that there is rather an extensive adsorption of ivermectin to the digesta particulates of the rumen [1]. Our model stipulates that the fraction of drug which is not absorbed in compartment GIT 1 will not be absorbed later in compartment GIT 2.…”

Section: Discussionmentioning

confidence: 99%

A pharmacokinetic model to document the actual disposition of topical ivermectin in cattle

et al. 2003

View full text Add to dashboard Cite

-Ivermectin is a worldwide-used antiparasitic drug largely administered to cattle as a topical formulation (pour-on). The actual plasma and faecal disposition of pour-on ivermectin in cattle was documented using an original pharmacokinetic model, and taking into account the oral ingestion of the topical drug following physiological licking as a secondary route of exposure. Six pairs of monozygotic twin cattle received successively one i.v. and two pour-on administrations of ivermectin at a 3-5-month interval. For one pour-on administration, the twins were separated into an unrestrained group and a group where self-and allo-licking were prevented. Ivermectin concentrations in the plasma and faeces were determined by HPLC. Licking resulted in a high intraand inter-individual variability of systemic exposure after topical application. By the means of pharmacokinetic modelling, we showed that 58-87% of the pour-on dose was ingested, while only 10% was absorbed percutaneously. Approximately 72% of the ingested ivermectin transited directly into the faeces, resulting in a 7-fold higher faecal excretion of the parent drug than in the non-lickers. We conclude that topical administration does not guarantee a controlled drug delivery in cattle. More importantly, the simulations revealed that non-treated cattle could get easily contaminated by allo-licking, raising the public health problem of unexpected drug residues in edible tissues.ivermectin / pour-on / cattle / licking behaviour / pharmacokinetics

show abstract

“…By seven days, the faecal residues account for 69% of the dose and 61-69% of these residues are present as the parent drug [40,76]. Other studies have shown 95% recovery of the total dose in the faeces of sheep seven days after intra-ruminal administration [2], two-thirds of this being recovered during the first two days [98]. The presence of ivermectin residues in sheep droppings after oral administration influenced the survival of fly and beetle larvae for less than a week after treatment, but such transient effects were unlikely to have a major impact on insect populations [113].…”

Section: Concentration Stability and Activity Of Anthelmintics In Thmentioning

confidence: 89%

Use of anthelmintics in herbivores and evaluation of risks for the non target fauna of pastures

2002

View full text Add to dashboard Cite

-The overall purpose of this paper was to review the major and most recent literature relating the effects of anthelmintics on dung breeding invertebrates and dung degradation. Faecal residues or metabolites of drugs belonging to the benzimidazole and levamisole/morantel groups are relatively harmless to dung fauna, on the contrary to other anthelmintics such as coumaphos, dichlorvos, phenothiazine, piperazine, synthetic pyrethroids, and most macrocyclic lactones which have been shown to be highly toxic for dung beetles (abamectin, ivermectin, eprinomectin, doramectin), among which moxidectin was the less toxic for dung beetles. To date, the detrimental impact upon non-target organisms has been considered acceptable in eradicating the parasites because of their economic importance to commercial livestock production. The consequences of routine treatments are discussed with consideration of the long-term consequences for cow pat fauna and sustainable pastureland ecology.anthelmintic / residue / dung beetle / Diptera / sustainable parasite control Résumé -Usage des anthelminthiques en élevage et évaluation des risques pour la faune non cible du pâturage. Cet article de synthèse passe en revue les travaux de la littérature les plus récents concernant les effets secondaires des principaux produits vétérinaires utilisés en routine sur la faune coprophage et sur la dégradation des excréments dans les pâturages. Les résidus (ou les métabolites) des groupes du benzimidazole et levamisole/morantel trouvés dans les excréments s'avèrent relativement peu toxiques pour la faune coprophage. Au contraire les anthelminthiques des groupes suivants s'avèrent hautement toxiques: coumaphos, dichlorvos, phénothiazine, pipérazine, pyréthroïdes de synthèse, et la plupart des lactones macrocycliques (abamectine, ivermectine, éprinomectine, doramectine), la moxidectine étant la moins toxique pour la faune coprophage. Jusqu'à présent, cet impact négatif a été considéré comme acceptable par les éleveurs et firmes pharmaceutiques en regard de l'importance économique du contrôle et/ou l'éradication des parasites. Les conséquences des traitements de routine sont discutées en considérant que l'absence de dégradation des bouses constatée 547

show abstract

The effect of level of feed intake on the pharmacokinetic disposition and efficacy of ivermectin in sheep

Cited by 68 publications

References 20 publications

Enhancement of oral moxidectin bioavailability in rabbits by lipid co-administration

Enhancement of oral moxidectin bioavailability in rabbits by lipid co-administration

A pharmacokinetic model to document the actual disposition of topical ivermectin in cattle

Use of anthelmintics in herbivores and evaluation of risks for the non target fauna of pastures

Contact Info

Product

Resources

About