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Albendazole treatment of echinococcosis in humans: Effects on microsomal metabolism and drug tolerance
Author(s) -
Steiger Ursula,
Cotting Jacques,
Reichen Jürg
Publication year - 1990
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1990.38
Subject(s) - albendazole , pharmacology , echinococcosis , microsome , drug metabolism , gastroenterology , medicine , drug , chemistry , surgery , biochemistry , enzyme
We prospectively studied the effect of albendazole on microsomal reserve and on first‐pass activation to albendazole sulfoxide in patients with hydatid disease. An aminopyrine breath test was performed in 12 patients while they were receiving albendazole treatment and while they were not. Excretion of 14 CO 2 in breath averaged 0.70% · kg · mmol −1 ± 0.20% · kg · mmol −1 without treatment and 0.54% · kg · mmol −1 ± 0.14% · kg · mmol −1 with treatment ( p < 0.005). Plasma levels of albendazole sulfoxide were measured 4 hours after the morning dose during the first and second half of the 4‐week treatment cycles. In nine of the 12 patients albendazole sulfoxide levels decreased during the second half of the cycle by an average of 0.84 ± 0.76 μmol/L ( p < 0.02). Transaminase levels increased in 10 of the 12 patients during long‐term albendazole treatment, and major side effects, including hepatotoxicity, neutropenia, and alopecia, were observed in three patients. We conclude that albendazole partially inhibits microsomal enzyme function but induces its own metabolism. Hepatotoxicity and other possible severe side effects necessitate close therapeutic monitoring of patients who are given albendazole. Clinical Pharmacology and Therapeutics (1990) 47, 347–353; doi: 10.1038/clpt.1990.38