The partition and fate of soluble and digesta particulate associated oxfendazole and its metabolites in the gastrointestinal tract of sheep

Hennessy, D.R.; Ali, D.N.; Tremain, S.A.

doi:10.1016/0020-7519(94)90079-5

Cited by 40 publications

(26 citation statements)

References 24 publications

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“…Furthermore, the potential anti-inflammatory activity of ABC-1 could be beneficial in treating chronic infections, such as those found in the CF lung, where it is thought that host inflammation is responsible for much of the host cell damage observed (20). In addition, benzimidazoles have low toxicity (16,39). We have determined that omeprazole does not possess significant antibiofilm activity under the conditions we examined (data not shown), suggesting ABC-1 has novel properties not found in the benzimadazoles used clinically.…”

Section: Discussionmentioning

confidence: 99%

Identification of a Novel Benzimidazole That Inhibits Bacterial Biofilm Formation in a Broad-Spectrum Manner

Sambanthamoorthy

Gokhale

Lao

et al. 2011

Antimicrob Agents Chemother

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Bacterial biofilm formation causes significant industrial economic loss and high morbidity and mortality in medical settings. Biofilms are defined as multicellular communities of bacteria encased in a matrix of protective extracellular polymers. Because biofilms have a high tolerance for treatment with antimicrobials, protect bacteria from immune defense, and resist clearance with standard sanitation protocols, it is critical to develop new approaches to prevent biofilm formation. Here, a novel benzimidazole molecule, named antibiofilm compound 1 (ABC-1), identified in a small-molecule screen, was found to prevent bacterial biofilm formation in multiple Gram-negative and Gram-positive bacterial pathogens, including Pseudomonas aeruginosa and Staphylococcus aureus, on a variety of different surface types. Importantly, ABC-1 itself does not inhibit the growth of bacteria, and it is effective at nanomolar concentrations. Also, coating a polystyrene surface with ABC-1 reduces biofilm formation. These data suggest ABC-1 is a new chemical scaffold for the development of antibiofilm compounds.

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Section: Discussionmentioning

confidence: 99%

Identification of a Novel Benzimidazole That Inhibits Bacterial Biofilm Formation in a Broad-Spectrum Manner

Sambanthamoorthy

Gokhale

Lao

et al. 2011

Antimicrob Agents Chemother

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“…The bioavailability of sulfide benzimidazoles is markedly reduced in ruminants which have had unrestricted access to food compared with those given restricted access prior to treatment. This is thought to be associated with adsorbence on to, and passage of, particulate associated drug in the digestive tract (Hennessy et al, 1994). The opposite is true in the dog (McKellar et al, 1993) in which coadministration with food increases the bioavailability of the benzimidazole by up to three times.…”

mentioning

confidence: 96%

“…The bioavailability of sulfide benzimidazoles is markedly reduced in ruminants which have had unrestricted access to food compared with those given restricted access prior to treatment. This is thought to be associated with adsorbence on to, and passage of, particulate associated drug in the digestive tract (Hennessy et al, 1994 OH-FBZ, hydroxy-fenbendazole; HPLC, high performance liquid chromatography; FBZSO-1, the first enantiomer of oxfendazole; FBZSO-2, the second enantiomer of oxfendazole; AUC, area under the plasma concentration time curve; AUMC, area under the first moment curve; MRT, mean residence time; r, recovery; FMO, flavin-containing monooxygenase. …”

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confidence: 99%

Fenbendazole Pharmacokinetics, Metabolism, and Potentiation in Horses

McKellar

Gökbulut²,

Muzandu³

et al. 2002

Drug Metab Dispos

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ABSTRACT:The present study was designed to describe the pharmacokinetics and fecal excretion of fenbendazole (FBZ) and fenbendazole sulphoxide (FBZSO) and their metabolites in horses, to investigate the effects which concurrent feeding has on the absorption and pharmacokinetics of FBZ, and to determine the effect of coadministration of the metabolic inhibitor piperonyl-butoxide on the in vivo pharmacokinetics and in vitro liver microsomal metabolism of sulfide and sulfoxide benzimidazoles. The effect of piperonyl-butoxide on the enantiomeric genesis of the sulfoxide moiety was also investigated. Following administration of FBZSO and FBZ, the fenbendazole sulphone metabolite predominated in plasma, and the C max and area under the plasma curve (AUC) values for each moiety were larger (P < 0.001) following FBZSO than FBZ. In feces the administered parent molecule predominated. The combined AUC for active benzimidazole moieties following oral administration of FBZ (10 mg/kg) in horses was almost 4 times as high in unfed horses (2.19 g ⅐ h/ml) than in fed horses (0.59 g ⅐ h/ml), and coadministration of piperonyl-butoxide significantly increased the AUC and C max of active moieties following intravenous administration of FBZSO and oral administration of FBZ. When FBZSO was administered i.v. as a racemate, the first enantiomer of oxfendazole (FBZSO-1) predominated in plasma, however, following coadministration with piperonyl-butoxide, the second enantiomer of oxfendazole (FBZSO-2) predominated for 10 h. Piperonyl-butoxide significantly reduced the oxidative metabolism of FBZSO and FBZ in equine liver microsomes and altered the ratio of enantiomers FBZSO-1/FBZSO-2 from >4:1 to 1:1. It is concluded that in horses efficacy of FBZSO and FBZ could be improved by administration to unfed animals and coadministration with piperonyl-butoxide.Helminth parasites produce pathological changes in the horse including diarrhea (Mair et al., 1990), rapid progressive weight loss (Love, 1992), functional disorders of the intestine (Ogbourne and Duncan, 1977), and colic and pathological changes in the mesenteric arteries (Duncan and Dargie, 1975).Large strongyles (Strongylus vulgaris, Strongylus edentatus, Strongylus equinus) migrate from the gastrointestinal tract through viscera and blood vessels where orally administered anthelmintics with low bioavailability are ineffective. The small strongyles (Cyathostominae) may become inhibited within the large intestinal mucosa at the early third and fourth larval stages, which are largely recalcitrant to available anthelmintics. The selection of anthelmintic resistant populations has increased since phenothiazine resistance was first recognized in horses in 1961 (Drudge and Elam, 1961). Selection of resistance to anthelmintics has developed rapidly in the horse (Love et al., 1989) probably because the epidemiology of equine parasites is less seasonal than that of ruminant parasites. Horses are consequently treated frequently throughout the year even in temperate climates thus exerting great se...

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“…Adequate fibre in the ruminoreticulum is a prerequisite for normal rumination to occur and when the ruminoreticulum becomes devoid of ad equate fibre, rumino-reticular contractions cease l . 16 ). Thus the reduced rumino-reticular contractions support the radio graphic observations that the ruminoreticulum contents were predominantly fluid after withholding feed for 24 hours.…”

Section: Discussionmentioning

confidence: 93%

The effects of age, weaning, drench volume and yarding on ruminoreticulum bypass in sheep, with reference to the anthelmintic efficacy of benzimidazole drenches

Sargison

Stafford

West

1998

New Zealand Veterinary Journal

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The partition and fate of soluble and digesta particulate associated oxfendazole and its metabolites in the gastrointestinal tract of sheep

Cited by 40 publications

References 24 publications

Identification of a Novel Benzimidazole That Inhibits Bacterial Biofilm Formation in a Broad-Spectrum Manner

Identification of a Novel Benzimidazole That Inhibits Bacterial Biofilm Formation in a Broad-Spectrum Manner

Fenbendazole Pharmacokinetics, Metabolism, and Potentiation in Horses

The effects of age, weaning, drench volume and yarding on ruminoreticulum bypass in sheep, with reference to the anthelmintic efficacy of benzimidazole drenches

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