Albendazole Grapefruit juice

Nagy J, Schipper HG, Koopmans RP, Butter JJ, Van Boxtel CJ, Kager PA. Effect of grapefruit juice or cimetidine coadministration on albendazole bioavailability. Am J Trop Med Hyg 2002 66(3) 260-263. 

GRAPEFRUIT JUICE ALBENDAZOLE T plasma levels of albendazole by nearly threefold. Risk of toxic effects of albendazole Albendazole is metabolized by intestinal CYP3A4, which is inhibited by grapefruit juice Monitor for toxic effects of albendazole... 

The poor intestinal absorption of albendazole, which may be enhanced by a fatty meal, contributes to difficulties in predicting its therapeutic response in echinococcosis. The effect of cimetidine co-administration on the systemic availability of albendazole has been studied in six healthy men (42). After an overnight fast, a single oral dose of albendazole (10 mg/kg) was administered on an empty stomach with water, a fatty meal, grapefruit juice, or grapefruit juice plus cimetidine. The systemic availability of albendazole was reduced by cimetidine. There were no adverse events. These results are consistent with presystemic metabolism of albendazole by CYP3A4. 

Grapefruit juice increases the plasma levels of albendazole. 

Grapefruit juice increased albendazole sulfoxide levels by about threefold and shortened its half-life by 46%. When albendazole was given with grapefruit juice and cimetidine the peak plasma level was reduced from 760 to 410 micrograms/L. However, the level achieved with cimetidine and grapefruit juice was still greater than that achieved when albendazole was given with water. 

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