Cimetidine increases serum mebendazole concentrations. Implications for treatment of hepatic hydatid cysts.

Bekhti, A; Pirotte, Jean

doi:10.1111/j.1365-2125.1987.tb03186.x

Cited by 28 publications

(25 citation statements)

References 5 publications

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“…A better defined effect of cimetidine is the increase of concentrations of drugs that are metabolized by these CYP enzymes, such as mebendazole. 22 Therefore, the metabolism of ABZSX, which is also CYP dependent, may be inhibited by cimetidine co-administration and thereby increase the elimination half-life of ABZSX. In our study, a 2.6-fold prolongation of ABZSX elimination halflife was indeed observed after cimetidine co-administration.…”

Section: Discussionmentioning

confidence: 99%

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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Section: Discussionmentioning

confidence: 99%

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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show abstract

“…Mebendazole and albendazole are used orally, in patients who are under operative high risk and/or to prevent secondary hidatidosis [10,11,[17][18][19][20].…”

Section: Discussionmentioning

confidence: 99%

The Effect of Intraoperative Mebendazole-Albendazole Applications on the Hepatobiliary System

et al. 1995

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Caustic sclerosing cholangitis occurs with the use of scolicidal solutions in liver hydatid disease draining into the biliary system. In this study, we investigated the effectiveness of benzimidazole solutions, their in vitro scolicidal effects and the histopathological changes in the hepatobiliary system due to their intraoperative use. It was found that 5 mg% mebendazole and 1 mg% albendazole have strong scolicidal effects. In an in vivo study, under general anesthesia, 5% mebendazole in group I, 1 % albendazole in group II and normal saline in group III were injected into the biliary system of rabbits. Liver biochemical tests showed no significant changes. More elaborate ductal mucosal proliferation, ductal dilatation and periductal fibrosis were found in group I compared with group II in biopsies taken on the 60th day. The biopsies of group III were normal.

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“…In contrast, only few data are available on specific enzymes involved in the metabolism of mebendazole. Metabolites isolated from feces and urine as well as results of the aminopyrine breath test suggest the involvement of a keton reductase and different CYP isoforms [10,11]. Furthermore, interaction data in healthy volunteers indicate that the nonspecific cytochrome P450 (CYP) inhibitor cimetidine significantly increases mebendazole plasma levels [10,12], pointing towards an involvement of cytochrome P450 enzymes in mebendazole metabolism.…”

Section: Introductionmentioning

confidence: 99%

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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Cimetidine increases serum mebendazole concentrations. Implications for treatment of hepatic hydatid cysts.

Cited by 28 publications

References 5 publications

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

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

The Effect of Intraoperative Mebendazole-Albendazole Applications on the Hepatobiliary System

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

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