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

Schipper, H.G.; Koopmans, Richard P.; Nagy, Judit; Butter, Jan J.; Kager, Piet A.; Boxtel, C. J. van

doi:10.4269/ajtmh.2000.63.270

Cited by 63 publications

(53 citation statements)

References 22 publications

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“…Albendazole and mebendazole absorption is increased by fatty meals [4], and a pH-dependency has been postulated for albendazole absorption [27]. To evaluate the importance of variability in intestinal absorption on our findings, data were recalculated without the outliers with the highest AUC-values in the albendazole group (individual 3) and the mebendazole group (individual 9).…”

Section: Discussionmentioning

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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Section: Discussionmentioning

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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“…First, there is considerable inter-individual variability in the plasma concentration of PZQ and ASOX [26,52,53]. The exact mechanism of this variability in the plasma concentration of the drug is not clear but may include a gender factor -greater ASOX concentration in women than in men -and dominant expression of cytochrome P450 isoforms [54,55].…”

Section: Failure Of Anticysticercal Therapy: Possible Explanationsmentioning

confidence: 99%

Therapy for neurocysticercosis

Takayanagui

2004

Expert Review of Neurotherapeutics

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“…In order to improve bioavailability, liposome-entrapped formulations and emulsions of albendazole have been tested (Wen et al 1996 ;Chai et al 2004). The use of cimetidine is discouraged, since it increases intestinal absorption (Wen et al 1996 ;Schipper et al 2000), which in turn could result in toxic effects.…”

Section: E C H I N O C O C C U S: B I O L O G Y a N D D I S E A S Ementioning

confidence: 99%

Echinococcusmetacestodes as laboratory models for the screening of drugs against cestodes and trematodes

Hemphill¹,

Lundström‐Stadelmann²,

Scholl³

et al. 2009

Parasitology

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Among the cestodes, Echinococcus granulosus, Echinococcus multilocularis and Taenia solium represent the most dangerous parasites. Their larval stages cause the diseases cystic echinococcosis (CE), alveolar echincoccosis (AE) and cysticercosis, respectively, which exhibit considerable medical and veterinary health concerns with a profound economic impact. Others caused by other cestodes, such as species of the genera Mesocestoides and Hymenolepis, are relatively rare in humans. In this review, we will focus on E. granulosus and E. multilocularis metacestode laboratory models and will review the use of these models in the search for novel drugs that could be employed for chemotherapeutic treatment of echinococcosis. Clearly, improved therapeutic drugs are needed for the treatment of AE and CE, and this can only be achieved through the development of medium-to-high throughput screening approaches. The most recent achievements in the in vitro culture and genetic manipulation of E. multilocularis cells and metacestodes, and the accessability of the E. multilocularis genome and EST sequence information, have rendered the E. multilocularis model uniquely suited for studies on drug-efficacy and drug target identification. This could lead to the development of novel compounds for the use in chemotherapy against echinococcosis, and possibly against diseases caused by other cestodes, and potentially also trematodes.

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

Cited by 63 publications

References 22 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

Therapy for neurocysticercosis

Echinococcusmetacestodes as laboratory models for the screening of drugs against cestodes and trematodes

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