Clinical pharmacokinetics of lorazepam. IV. Long-term oral administration

J Clin Pharmacol. 1977 Aug-Sep;17(8-9):495-500. doi: 10.1002/j.1552-4604.1977.tb05642.x.

Abstract

Fifteen healthy male volunteers received long-term daily treatment with oral lorazepam at doses as high as 10 mg per day for a period of 26 weeks. Steady-state plasma concentrations of lorazepam and its glucuronide metabolite were measured in all subjects at least every two weeks. At daily doses of 6 mg per day, the mean steady-state lorazepam level was 88 ng/ml and that of lorazepam glucuronide was 170 ng/ml. Mean levels among seven subjects who received 10 mg per day were 164 and 266 ng/ml, respectively. Lorazepam concentrations fluctuated from week to week despite constant dosage, but there was no evidence of systematic variation. Mean steady-state lorazepam levels were highly correlated with daily dose in mg/kg, but were not related to age. Lorazepam was not detected in any plasma samples drawn one week after discontinuation of treatment.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Administration, Oral
  • Adult
  • Age Factors
  • Anti-Anxiety Agents / blood*
  • Glucuronates / blood
  • Humans
  • Kinetics
  • Lorazepam / administration & dosage
  • Lorazepam / adverse effects
  • Lorazepam / blood*
  • Male
  • Middle Aged
  • Time Factors

Substances

  • Anti-Anxiety Agents
  • Glucuronates
  • Lorazepam