Influence of diet on the pattern of gastrointestinal biotransformation of netobimin and albendazole sulphoxide in sheep

Virkel, G.; Lifschitz, Adrián Luis; Pis, A.; Lanusse, Carlos

doi:10.1007/bf03190008

Cited by 13 publications

(13 citation statements)

References 23 publications

(16 reference statements)

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“…It has been shown that the gastrointestinal micro¯ora is very active in reductive biotransformation reactions of foreign compounds, particularly those containing sulphoxide groups (Renwick et al 1986). Sheep and cattle ruminal and intestinal contents sulphoreduce the BZDsulphoxide derivatives (ABZSO, oxfendazole) to form the respective thioethers (ABZ and fenbendazole) (Lanusse et al 1992;Virkel et al 1999). Xenobiotic metabolism in parasites seems to be predominantly reductive and hydrolytic (Douch and Buchanan 1979).…”

Section: Discussionmentioning

confidence: 99%

Comparative metabolism of albendazole and albendazole sulphoxide by different helminth parasites

2001

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Albendazole (ABZ) is a broad-spectrum benzimidazole anthelmintic widely used in human and veterinary medicine. The aim of the current work was to characterise the sulphoxidative metabolism of ABZ, and the sulphoreduction of ABZ sulphoxide (ABZSO), by microsomal (Ms) and cytosolic (Cyt) fractions of three different helminth species: Fasciola hepatica, Moniezia expansa and Ascaris suum. After the incubation assays, parasite material was analysed by HPLC to characterise the metabolic product formed. Both the Ms and Cyt fractions of the three parasites studied were able to oxidise ABZ into ABZSO in a non-enantioselective fashion. Oxidation of ABZ was greater in the Ms fraction of the trematode (50%) than in both cestode (19%) and nematode (14%) parasites. Only the incubation of ABZSO with both subcellular fractions of M. expansa generated ABZ as a metabolic product. The results obtained here indicate that helminths have the capacity to biotransform benzimidazole compounds; however, this metabolic activity differs qualitatively and quantitatively among helminth species.

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Section: Discussionmentioning

confidence: 99%

Comparative metabolism of albendazole and albendazole sulphoxide by different helminth parasites

2001

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“…Although the liver is the main site for the biotransformation of xenobiotic compounds, drug metabolism also takes place in extra‐hepatic tissues such as the gastrointestinal tract, which may contribute to reduce the systemic availability of orally administered compounds (Rowland, 1986; Vynckier & Debackere, 1993). The anthelmintics netobimin (an albendazole prodrug) and ABZSO have been shown to suffer extensive biotransformation in ruminal (Virkel et al. , 1999) and intestinal (Lanusse et al.…”

Section: Discussionmentioning

confidence: 99%

“…, 1992) contents collected from sheep and cattle. Those metabolic conversions are mediated by the digestive microflora and both the type of diet (Virkel et al. , 1999) and the antibacterial effect of monensin (Virkel et al.…”

Section: Discussionmentioning

confidence: 99%

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Moxidectin and ivermectin metabolic stability in sheep ruminal and abomasal contents

Lifschitz

Virkel

Ballent

et al. 2005

Vet Pharm & Therapeutics

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The oral administration of macrocyclic lactones to sheep leads to poorer efficacy and shorter persistence of the antiparasitic activity compared to the subcutaneous treatment. Gastrointestinal biotransformation occurring after oral treatment to ruminant species has been considered as a possible cause of the differences observed between routes of administration. The current work was addressed to evaluate on a comparative basis the in vitro metabolism of moxidectin (MXD) and ivermectin (IVM) in sheep ruminal and abomasal contents. Both compounds were incubated under anaerobic conditions during 2, 6 and 24 h in ruminal and abomasal contents collected from untreated adult sheep. Drug concentrations were measured by high-performance liquid chromatography with fluorescence detection after sample clean up and solid phase extraction. Neither MXD nor IVM suffered metabolic conversion and/or chemical degradation after 24-h incubation in ruminal and abomasal contents collected from adult sheep. Unchanged MXD and IVM parent compounds represented between 95.5 and 100% of the total drug recovered in the ruminal and abomasal incubation mixtures compared with those measured in inactive control incubations. The partition of both molecules between the solid and fluid phases of both sheep digestive contents was assessed. MXD and IVM were extensively bound (>90%) to the solid material of both ruminal and abomasal contents collected from sheep fed on lucerne hay. The results reported here confirm the extensive degree of association to the solid digestive material and demonstrates a high chemical stability without evident metabolism and/or degradation for both MXD and IVM in ruminal and abomasal contents.

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“…The influence of the type of feed (lucerne hay diet or concentrate-based diet) was shown in vitro by Virkel et al (1999) who examined the biotransformation of the pro-drug netobimin (NTB) to ABZ and ABZSO by the ruminal fluid obtained from sheep fed hay or concentrates. The biotransformation was found to be more efficient in ruminal fluid obtained from sheep fed a concentrate diet.…”

Section: Albendazole (Abz)mentioning

confidence: 99%

Effect of composition and quality of diet and feeding time on the kinetics and efficacy of some anthelmintic drugs: A mini-review

Ali

2004

Acta Veterinaria Hungarica

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This article reviews the literature dealing with the effects of composition and quality of diet and feeding time on the pharmacokinetics and efficacy of some anthelmintic drugs in ruminants. Studies have suggested that greater availability, and therefore improved anthelmintic activity, is possible through temporary feed restriction. It is also recommended that anthelmintic drugs should not be given to animals whilst they are maintained on large feed intakes, particularly of lush pasture that promotes rapid gastric transit, as this may reduce drug availability and anthelmintic efficacy. Generally, feeding animals low-quality fibrous diets reduces the passage rate of digesta and allows more time for absorption of several anthelmintic drugs and their metabolites from the gut. Some kinetic data of drugs given to animals on such diets may be slightly different, but this does not necessarily indicate alteration of the dosages of the anthelmintic drug. Nonetheless, due consideration should be given to anthelmintic dosages under various dietary regimes if optimum efficacy is to be achieved at all times.

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Influence of diet on the pattern of gastrointestinal biotransformation of netobimin and albendazole sulphoxide in sheep

Cited by 13 publications

References 23 publications

Comparative metabolism of albendazole and albendazole sulphoxide by different helminth parasites

Comparative metabolism of albendazole and albendazole sulphoxide by different helminth parasites

Moxidectin and ivermectin metabolic stability in sheep ruminal and abomasal contents

Effect of composition and quality of diet and feeding time on the kinetics and efficacy of some anthelmintic drugs: A mini-review

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