Human tolerance of flumecinol (Zixoryn, RGH-3332), its regime and dosage in healthy volunteers.
The enzyme inductive effect of flumecinol (Zixoryn, RGH-3332), a new hepatic enzyme inducer, was studied in healthy volunteers. The dosages employed were as follows: 25, 50, 100, 200, 400, 600 and 800 mg single doses; and during a 7-day period single doses of 50 mg daily, and doses of 200, 300 and 400 mg three times daily. The intensity of enzyme induction was measured by the following parameters: antipyrine metabolic clearance, D-glucaric acid excretion, menthol loading, and total serum bilirubin. The minimal and optimal inductive doses of flumecinol were determined. A single dose of 600 mg of flumecinol is recommended at intervals of 7 days. This dosage also induces the first and the second phases of reactions. The induction effect becomes manifest after 24 hours. Its peak is reached between 48 and 96 hours, and the inductive activity ceases between 216 and 408 hours.
D000328:Adult; D000983:Antipyrine / Q000378:metabolism; D001559:Benzhydryl Compounds / Q000008:administration & dosage / Q000009:adverse effects* / Q000494:pharmacology; D001663:Bilirubin / Q000378:metabolism; D004334:Drug Administration Schedule; D004790:Enzyme Induction / Q000187:drug effects*; D005260:Female; D005937:Glucaric Acid / Q000378:metabolism; D005965:Glucuronates / Q000378:metabolism; D006801:Humans; D008297:Male; D008610:Menthol
D001559:Benzhydryl Compounds; D005965:Glucuronates; D008610:Menthol; C016914:flumecinol; D005937:Glucaric Acid; D001663:Bilirubin; D000983:Antipyrine