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This study was undertaken to determine the serum pharmacokinetic parameters of loprazolam, a new benzodiazepine hypnotic, in elderly subjects and to compare these with the kinetics of the drug as determined by quantitative EEG analysis. In addition, a 14-day study was undertaken to determine the steady-state serum levels achieved in this population with repeated drug administration. The study was conducted on 16 male and female subjects between the ages of 62 and 72 years, randomly assigned to two groups treated with 0.5 or 1.0 mg of loprazolam. The serum half-life of loprazolam was found to be 5 hours, and the peak serum concentration was reached after 2 hours. Quantitative EEG changes were observed after 30 minutes suggesting rapid access of the drug into the nervous system. Quantitative EEG changes were evident for 9.5 hours, suggesting the persistent effects of an active metabolite. The 14-day study indicated that loprazolam did not accumulate with continued use.
M Mamelak, and
P Bunting, and
H Galin, and
V Price, and
A Csima, and
T Young, and
D Klein, and
J R Pelchat
August 1985,
British journal of clinical pharmacology,
M Mamelak, and
P Bunting, and
H Galin, and
V Price, and
A Csima, and
T Young, and
D Klein, and
J R Pelchat
August 1987,
Xenobiotica; the fate of foreign compounds in biological systems,
M Mamelak, and
P Bunting, and
H Galin, and
V Price, and
A Csima, and
T Young, and
D Klein, and
J R Pelchat
November 1990,
Archives of neurology,
M Mamelak, and
P Bunting, and
H Galin, and
V Price, and
A Csima, and
T Young, and
D Klein, and
J R Pelchat
January 1986,
Biopharmaceutics & drug disposition,
M Mamelak, and
P Bunting, and
H Galin, and
V Price, and
A Csima, and
T Young, and
D Klein, and
J R Pelchat
April 1988,
Journal of clinical pharmacology,
M Mamelak, and
P Bunting, and
H Galin, and
V Price, and
A Csima, and
T Young, and
D Klein, and
J R Pelchat
July 1985,
Xenobiotica; the fate of foreign compounds in biological systems,
M Mamelak, and
P Bunting, and
H Galin, and
V Price, and
A Csima, and
T Young, and
D Klein, and
J R Pelchat
January 2001,
Drugs under experimental and clinical research,
M Mamelak, and
P Bunting, and
H Galin, and
V Price, and
A Csima, and
T Young, and
D Klein, and
J R Pelchat
December 1988,
British journal of clinical pharmacology,
M Mamelak, and
P Bunting, and
H Galin, and
V Price, and
A Csima, and
T Young, and
D Klein, and
J R Pelchat
January 1999,
Biopharmaceutics & drug disposition,
M Mamelak, and
P Bunting, and
H Galin, and
V Price, and
A Csima, and
T Young, and
D Klein, and
J R Pelchat
May 1985,
British journal of clinical pharmacology,
