Metabolic disposition of ivermectin in swine

Chiu, Shuet Hing Lee; Sestokas, E.; Taub, Rae; Green, Marilyn L.; Baylis, Francis P.; Jacob, Theodore A.; Lu, Anthony Y. H.

doi:10.1021/jf00101a016

Cited by 37 publications

(40 citation statements)

References 5 publications

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“…Analysis by high-performance liquid chromatography (HPLC) of acetone extracts of feces showed that the major component in feces was the parent drug, and that the remainder of the radioactivity consisted of various ivermectin metabolites (Halley et al, 1989a). Based on both in vivo and in vitro metabolism studies (Chiu et al 1985;Chiu et al 1986;Miwa et al 1982); and a comparison of retention times on HPLC, the polar metabolites are believed to include the monosaccharides and aglycones of ivermectin, as well as ivermectin's 24-hydroxymethyl derivatives and the corresponding monosaccharides and aglycones. The druglike metabolites would most likely be the 3"-O-desmethyl derivatives (Chiu et al 1984;Chiu et al 1987).…”

Section: Excretion Of Ivermectinmentioning

confidence: 99%

Environmental Aspects of Ivermectin Usage in Livestock: General Considerations

Halley

Nessel

1989

Ivermectin and Abamectin

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Section: Excretion Of Ivermectinmentioning

confidence: 99%

Environmental Aspects of Ivermectin Usage in Livestock: General Considerations

Halley

Nessel

1989

Ivermectin and Abamectin

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“…They have a strong affinity for adipose tissue, which constitutes the main storage site for such drugs (Chiu et al 1986). …”

Section: Introductionmentioning

confidence: 99%

Assessment of a liposomal formulation of ivermectin in rabbit after a single subcutaneous administration

Bassissi¹,

Lespine²,

Alvinerie³

2005

Parasitol Res

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Ivermectin is a member of the macrocyclic lactone family widely used in livestock, pets, and humans as a potent parasiticide. Slight differences in formulation may change the plasma kinetics and efficacy of these compounds. The aim of the study is to evaluate the ability of a liposomal formulation of ivermectin to generate an efficient exposure of the animal to the drug. Ten rabbits were subcutaneously administered with 0.3 mg kg(-1) of ivermectin using Ivomec (n=5) or a liposomal formulation (n=5). The areas under serum concentration-time curve were similar after both treatments, indicating the same bioavailability for the two formulations. However, the liposomal formulation gave a higher C(max) value (33.33 ng ml(-1)) compared with Ivomec (20.82 ng ml(-1)) and a significantly faster absorption as indicated by the T(max) of 0.23 days compared with 1.13 days for the Ivomec formulation. The use of liposomal formulation shows promise as this system improves the efficacy of ivermectin and related drugs.

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“…The structures of these avermectins are shown in Figure 1 Extensive work has been published on the tissue distribution and metabolism of ivermectin in multiple species. [4][5][6][7][8][9][10][11] The metabolism of ivermectin is qualitatively similar in all species examined. It is only the ratios of the metabolites that differ.…”

Section: Ivermectinmentioning

confidence: 99%

“…12 Liver is a target tissue in all species for which ivermectin is approved in the United States. The half-lives of ivermectin MRs in liver for cattle, sheep, swine, and rats were calculated using a simple linear regression from data presented by Chiu et al [6][7][8]10,11 and Steel. 13 For goats, half-lives were estimated using data from an NRSP-7 Public Master File.…”

Section: Ivermectinmentioning

confidence: 99%

Interspecies considerations in the evaluation of human food safety for veterinary drugs

Craigmill

Cortright

2002

AAPS J

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Residues are composed of the parent drug and metabolites, and therefore interspecies comparisons must involve a consideration of comparative xenobiotic metabolism. The focus of this article will be the residue studies that are required to establish human food safety, and the interspecies pharmacokinetic differences and similarities that impact drug residues in animal-derived foods. To illustrate the factors that can complicate and assist these comparisons, 2 drugs will be examined in detail: ivermectin and fenbendazole. In addition, the activities of 2 US programs, the Food Animal Residue Avoidance Databank (FARAD) and the NRSP-7 (National Research Support Project Number 7) Minor Use Animal Drug Program will be presented, along with strategies that may be employed in the study of species differences.

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Metabolic disposition of ivermectin in swine

Cited by 37 publications

References 5 publications

Environmental Aspects of Ivermectin Usage in Livestock: General Considerations

Environmental Aspects of Ivermectin Usage in Livestock: General Considerations

Assessment of a liposomal formulation of ivermectin in rabbit after a single subcutaneous administration

Interspecies considerations in the evaluation of human food safety for veterinary drugs

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