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Lack of Interaction between Tolcapone and Tolbutamide in Healthy Volunteers
Author(s) -
Jorga Karin M.,
Fotteler Bärbel,
Gasser Rodolfo,
Banken Ludger,
Birnboeck Herbert
Publication year - 2000
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/00912700022009161
Subject(s) - tolbutamide , pharmacokinetics , placebo , pharmacology , cyp2c9 , drug interaction , drug , cyp2d6 , medicine , cytochrome p450 , metabolism , insulin , alternative medicine , pathology
To assess the effect of tolcapone (an inhibitor of cytochrome P450 [CYP] 2C9 in vitro) on the pharmacokinetics and hypoglycemic effect of the CYP 2C9 substrate tolbutamide, 12 healthy male volunteers were randomized to receive a single dose of tolbutamide 500 mg plus either placebo or tolcapone 200 mg after an overnight fast and 30 minutes after the start of a 6.5‐hour 5% glucose infusion (150 mL/h). The participants crossed over to receive the alternative regimen after a washout period of at least 7 days. Tolcapone had no effect on the pharmacokinetics of tolbutamide or its metabolites and did not influence the effect of tolbutamide on plasma glucose concentrations. No serious adverse events or abnormal laboratory results or vital signs were reported. In conclusion, clinically relevant drug‐drug interactions between tolcapone and tolbutamide when given together in clinical practice appear unlikely.