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Serum and Quantitative Electroencephalographic Pharmacokinetics of Loprazolam in the Elderly
Author(s) -
Mamelak Mortimer,
Bunting Peter,
Galin Howard,
Price Victoria,
Csima Adele,
Young Trevor,
Klein Dwora,
Pelchat Jocelyn R.
Publication year - 1988
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 - 10.1002/j.1552-4604.1988.tb03162.x
Subject(s) - pharmacokinetics , medicine , pharmacology , electroencephalography , psychiatry
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.