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Single and repeated dose kinetics of the hypnotic agent loprazolam in healthy volunteers.

Abstract：

:The pharmacokinetics of loprazolam have been studied in eight healthy male volunteers after single and repeated 2 mg oral doses taken at night, for eight nights. The absorption and disposition of unchanged drug (HPLC-GC assay) and receptor active benzodiazepine-type materials (radioreceptor assay) were examined after the first and eighth dose. Maximum levels of approximately 10 ng ml-1 (range 3.6 to 15.5 ng ml-1) were reached within about 2.5 h after dosing. The post-peak levels declined in a single exponential fashion with an overall mean +/- SD half-life of 7.06 +/- 1.98 h and total areas under the curve ranging from 35.9 to 189.0 ng ml-1 h. There were no statistical differences between the values for the first and eighth doses. There was no evidence to suggest that significant accumulation of parent drug or receptor active benzodiazepine-type materials had occurred, and it is concluded that the kinetics of loprazolam would allow repeated daily doses of 2 mg.

journal_name

Eur J Clin Pharmacol

journal_title

European journal of clinical pharmacology

authors

Stevens LA,Bevan CD,Salmon J,Krieger J,Perianu M,LeGo A

doi

10.1007/BF00542354

subject

Has Abstract

pub_date

1983-01-01 00:00:00

pages

651-5

issue

5

eissn

0031-6970

issn

1432-1041

journal_volume

25

pub_type

杂志文章

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