Pharmacokinetics of albendazole in man

Marriner, S. E.; Dl, Morris; Dickson, Brian; Bogan, J. A.

doi:10.1007/bf00608219

Cited by 180 publications

(122 citation statements)

References 11 publications

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“…As expected from previous data on oral albendazole and mebendazole disposition [4,12] high interindividual variability in bioavailability was seen. While single dose administration of the potent CYP3A inhibitor ritonavir did not result in changes in albendazole and mebendazole plasma concentrations in most of the patients, long term administration led to a significant decrease in benzimidazoles systemic exposure.…”

Section: Discussionsupporting

confidence: 84%

“…Changes in AUC 0-24 and C max were chosen as primary endpoints. Sample size calculation was based upon the following considerations: (i) the extent of interindividual variability in albendazole pharmacokinetics in healthy volunteers [4], (ii)…”

Section: Power Calculationmentioning

confidence: 99%

“…After oral administration, albendazole and mebendazole are poorly absorbed in the intestinal tract, mainly due to limited solubility [4]. Furthermore, benzimidazoles undergo extensive intestinal and hepatic bioconversion, adding to the low systemic exposures with these compounds [5,6].…”

Section: Introductionmentioning

confidence: 99%

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Effect of ritonavir on the pharmacokinetics of the benzimidazoles albendazole and mebendazole: an interaction study in healthy volunteers

Corti

Heck

Rentsch

et al. 2009

Eur J Clin Pharmacol

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Effect of ritonavir on the pharmacokinetics of the benzimidazoles albendazole and mebendazole: an interaction study in healthy volunteers Abstract BACKGROUND: Benzimidazoles are often used concomitantly with protease inhibitors in patients with helminthic disease and HIV infection. Low bioavailability and extensive first-pass metabolism make benzimidazoles prone to pharmacokinetic drug interactions. The aim of the present study was to investigate potential drug interactions between the benzimidazoles albendazole and mebendazole and the potent CYP3A4 inhibitor ritonavir. METHODS: Sixteen healthy volunteers were administered a single oral dose of 1,000 mg mebendazole or 400 mg albendazole (2 x n = 8). AUC, C(max), and t(1/2) of mebendazole, albendazole, and albendazole sulfoxide were studied in absence and after short-term (2 doses) and long-term (8 days) treatment with ritonavir 200 mg bid. RESULTS: Pharmacokinetic parameters of albendazole and mebendazole were not changed by short-term administration of ritonavir. However, long-term administration of ritonavir resulted in significant changes in albendazole and mebendazole disposition, with a significant decrease in AUC(0-24) (27 and 43% of baseline for albendazole and mebendazole, respectively) and C(max) (26 and 41% of baseline, respectively). CONCLUSION: The AUC(0-24) of benzimidazoles decreased after long-term use of ritonavir, while no changes in pharmacokinetic profiles were observed under short-term administration. These findings might help to optimize benzimidazole efficacy when used in combination with protease inhibitors.

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Section: Discussionsupporting

confidence: 84%

Section: Power Calculationmentioning

confidence: 99%

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Effect of ritonavir on the pharmacokinetics of the benzimidazoles albendazole and mebendazole: an interaction study in healthy volunteers

Corti

Heck

Rentsch

et al. 2009

Eur J Clin Pharmacol

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“…[13][14][15] In contrast, in one study no increase in C max was demonstrated when albendazole was combined with a fatty meal. 16 The interindividual variability in these studies was great. Therefore, it is unclear whether increasing the albendazole dose results in a linear increase of albendazole bioavailability, although a proportional increase of ABZSX concentration was reported after administration of a 50% greater dose of albendazole.…”

Section: Introductionmentioning

confidence: 93%

Effect of dose increase or cimetidine co-administration on albendazole bioavailability.

Schipper¹,

Koopmans²,

Nagy³

et al. 2000

The American Journal of Tropical Medicine and Hygiene

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Abstract. The low bioavailability of albendazole affects the therapeutic response in patients with echinococcosis. Cimetidine co-administration is reported to improve bioavailability. To analyze the assumed dose-dependent bioavailability of albendazole, we administered 5 to 30 mg/kg albendazole to 6 male volunteers in a randomized cross-over study. To assess the effect of cimetidine (10 mg/kg twice daily), the drug was given with albendazole (20 mg/kg). A dose-dependent bioavailability was not observed. This was due to inter-individual variability of the maximal concentration (C max 38%-72%) of albendazole sulphoxide (ABZSX), the active metabolite of albendazole. C max was 0.21 Ϯ 0.14 mg/L after 5 mg/kg and 0.39 Ϯ 0.19 mg/L after 30 mg/kg albendazole (P ϭ 0.217). Cimetidine tended to decrease C max by 52% (P ϭ 0.109) and significantly inhibited ABZSX breakdown as indicated by the prolongation of ABZSX elimination half-life from 7.4 Ϯ 3.3 hr to 19.0 Ϯ 11.7 hr (P ϭ 0.028). Remarkably, the inter-individual variability of C max was significantly lower during cimetidine co-administration: 14% versus 72%.

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“…However in field studies, using a pulse release formulation delivering 750 mg of oxfendazole, no evidence of any effects of oxfendazole on the rate of dung degradation or on the numbers or weight of earthworms in the pasture were found [119]. According to McKellar [81], the benzimidazoles have relatively short residence times following single oral administration and very low concentrations are passed in the faeces within 36 h (thiabendazole), 96 h (albendazole) or 168 h (oxfendazole, fenbendazole) after administration [73][74][75]118]. The fenbendazole bolus delivers 67-103 mg of fenbendazole per animal per day with prophylactic activity for 140 days [89].…”

Section: Concentration Stability and Activity Of Anthelmintics In Thmentioning

confidence: 99%

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

2002

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-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

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Pharmacokinetics of albendazole in man

Cited by 180 publications

References 11 publications

Effect of ritonavir on the pharmacokinetics of the benzimidazoles albendazole and mebendazole: an interaction study in healthy volunteers

Effect of ritonavir on the pharmacokinetics of the benzimidazoles albendazole and mebendazole: an interaction study in healthy volunteers

Effect of dose increase or cimetidine co-administration on albendazole bioavailability.

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

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