2001
DOI: 10.1046/j.1365-2885.2001.00320.x
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Albendazole sulphoxide enantiomeric ratios in plasma and target tissues after intravenous administration of ricobendazole to cattle

Abstract: The comparative concentration profiles of the (+) and (-) albendazole sulphoxide (ABZSO) enantiomers obtained in plasma and in selected target tissues/fluids after intravenous (i.v.) administration of a racemic formulation of ricobendazole (RBZ) to cattle were characterised. Fourteen Holstein calves received RBZ (racemic solution, 150 mg/mL) by i.v. administration at 7.5 mg/kg. Jugular blood samples were collected over 48 h post-treatment (plasma kinetic trial) and two animals were sacrificed at either 4, 12, … Show more

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Cited by 24 publications
(39 citation statements)
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“…Large quantities of ABZ were recovered from tissues of parasite location such as lung parenchyma and small intestinal mucosa in both sheep and cattle Cristofol et al, 2001). FBZ has been recovered in both target tissues following oral administration of OFZ to cattle (G. Virkel, L. Mottier, and C. Lanusse, unpublished observations).…”
Section: Virkel Et Almentioning
confidence: 95%
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“…Large quantities of ABZ were recovered from tissues of parasite location such as lung parenchyma and small intestinal mucosa in both sheep and cattle Cristofol et al, 2001). FBZ has been recovered in both target tissues following oral administration of OFZ to cattle (G. Virkel, L. Mottier, and C. Lanusse, unpublished observations).…”
Section: Virkel Et Almentioning
confidence: 95%
“…The (ϩ) ABZSO enantiomer predominates in plasma (Delatour et al, 1991;Cristofol et al, 2001) and in tissues of parasite location such as lung and GI mucosa (Cristofol et al, 2001), as well as in a target parasite such as the liver fluke Fasciola hepatica . For example, the (ϩ) ABZSO enantiomer represents 91% of the total ABZSO plasma area under the concentration versus time curve (AUC) in cattle and 86% in sheep (Delatour et al, 1991).…”
Section: Virkel Et Almentioning
confidence: 99%
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“…Moreover, the absorbed drug is more important for the efficacy against GI nematodes than unabsorbed drug passing down the GI tract [21]. Thus, the plasma concentration profiles of anthelmintically active BZD moieties reflect the pattern of exposure of worms in the GI tract (mucosas or lumen) as well in other tissues of parasite location such as liver or lung [20,22,23]. It has been recently shown that plasma profiles of ABZ metabolites correlate with those obtained in different tissues/fluids and in target parasites (Moniezia spp., Haemonchus spp.…”
Section: Resultsmentioning
confidence: 99%
“…1 Recently, pharmacokinetic studies have been published using an injectable form of the active sulphoxide metabolite of ABZ and the benefits of injectable forms of benzimidazoles have been discussed. [3][4][5][6] Ricobendazole (RBZ) or albendazole sulphoxide (Scheme 1) is reported as the active metabolite of ABZ. 1,[7][8][9] Following oral administration of ABZ 8,10 in sheep or its prodrug netobimin in cattle, 11 ABZ concentrations are either very low (0.05 mg/mL) or not detected in the plasma and systemic activity is attributed to the active sulphoxide metabolite.…”
Section: Introductionmentioning
confidence: 99%