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Multiple‐dose halazepam kinetics
Author(s) -
Chung Menger,
Hilbert James M,
Gural Richard P,
Radwanski Elaine,
Symchowicz Samson,
Zampaglione Nicola
Publication year - 1984
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.1984.122
Subject(s) - kinetics , pharmacokinetics , clinical pharmacology , metabolite , plasma concentration , chemistry , absorption (acoustics) , pharmacology , active metabolite , steady state (chemistry) , medicine , chromatography , biochemistry , organic chemistry , materials science , physics , composite material , quantum mechanics
Halazepam is a benzodiazepine used in the management of anxiety disorders or short‐term relief of anxiety. Our study was undertaken to evaluate its steady‐state kinetics and those of its major active plasma metabolite N‐desalkylhalazepam. Eleven healthy men aged 19 to 35 yr were given oral, 40‐mg halazepam tablets every 8 hr for 14 days. Plasma samples were analyzed by gas chromatography to determine levels of halazepam and N‐desalkylhalazepam. Halazepam kinetics can best be described by a two‐compartment open model with first‐order absorption kinetics. The elimination phase t½s of halazepam and N‐desalkylhalazepam were 34.7 and 57.9 hr. Steady‐state levels were predictable from kinetic data and were reached by the third day for halazepam and by the eleventh day for N‐desalkylhalazepam. Clinical Pharmacology and Therapeutics (1984) 35 , 838–842; doi: 10.1038/clpt.1984.122