Serum and Quantitative Electroencephalographic Pharmacokinetics of Loprazolam in the Elderly

  title={Serum and Quantitative Electroencephalographic Pharmacokinetics of Loprazolam in the Elderly},
  author={Mortimer Mamelak and P. Bunting and Howard Galin and V Price and Adele C Csima and Trevor Young and Dwora Klein and Jocelyn R. Pelchat},
  journal={The Journal of Clinical Pharmacology},
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… 
Benzodiazepine hypnotics in the elderly
  • P. Cook
  • Psychology, Medicine
    Acta psychiatrica Scandinavica. Supplementum
  • 1986
Control studies in which subjects of different ages have received single doses of diazepam have consistently shown an increase in the response to benzodiazepines in the elderly which is not explained by the effects of disease or by altered plasma concentrations.
Impairment of memory and plasma flunitrazepam levels
Results indicate that higher concentrations were needed to impair attention than were required to impair memory, and there was a significant positive correlation between peak levels of flunitrazepam at night and impairment of night attention and explicit memory.
Pharmacokinetics of temazepam compared with other benzodiazepine hypnotics—some clinical consequences
In hypnotic treatment, the duration of drug action should be restricted to theduration of the night, hence a compound with a relatively short elimination half‐life may represent a more rational choice.


Single dose pharmacokinetics and pharmacodynamics of oral loprazolam in the elderly.
The results are compatible with previous evidence of increased 'sensitivity' to benzodiazepines in the elderly and suggest that a lower starting dose of loprazolam would be appropriate for older recipients.
Pharmacokinetics and pharmacodynamics following single and repeated nightly administrations of loprazolam, a new benzodiazepine hypnotic.
After repeated doses of loprazolam, there were no significant changes with respect to results after single doses in psychomotor function assessed objectively by critical flicker fusion threshold or choice reaction time, or in sleep quality or behaviour on awakening assessed subjectively by 10 cm analogue scales.
Hypnotic benzodiazepines: Relationship between sleep parameters and pharmacokinetics of loprazolam
No correspondence could be demonstrated, suggesting that the drug does not act directly on sleep systems and that its hypnotic effects may be indirect, secondary to anxiolytic effects or to deactivation of wake systems.
Quantitative pharmaco-EEG and performance after administration of brotizolam to healthy volunteers.
The activity of brotizolam (0.1 mg) is the minimal effective psychoactive dose with a tranquillizing effect, while 0.5 mg and to some extent 0.3 mg induce a sedative effect and may be regarded as hypnotic doses.
Diazepam absorption: Effect of antacids and food
Under the conditions of this study, coadministration of diazepam with antacids or a standard meal reduces the rate of absorption but does not reduce extent of absorption.
Pharmacokinetics and metabolism of various benzodiazepines used as hypnotics.
  • D. Breimer
  • Biology, Medicine
    British journal of clinical pharmacology
  • 1979
These considerations serve as a guide for a review of the kinetics and metabolism of various benzodiazepines and biopharmaceutical factors, such as those which promote a rapid rate of absorption, are important.
A clinical trial of a new hypnotic--loprazolam.
Loprazolam: an intermediate acting benzodiazepine. A review article.
  • G. Beaumont
  • Medicine
    The British journal of clinical practice
  • 1983
A clinical trial of a new hypnotic : Loprazo
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  • 1983