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Clinical Pharmacokinetics

, Volume 6, Issue 2, pp 89–105 | Cite as

Clinical Pharmacokinetics of Oxazepam and Lorazepam

  • David J. Greenblatt
Article

Summary

Oxazepam and lorazepam are 3-hydroxy benzodiazepine derivatives used as sedatives and anxiolytics. The major metabolic pathway for both compounds involves conjugation to glucuronic acid at the 3-position, followed by urinary excretion of the inactive glucuronide metabolite.

Oxazepam has been administered to humans by the oral route only. Usual ranges for kinetic parameters are: elimination half-life, 5 to 15 hours; volume of distribution, 0.6 to 2.0L/kg; clearance, 0.9 to 2.0ml/min/kg. Age and liver disease have a minimal influence on oxazepam kinetics, but renal disease is associated with a prolonged half-life and increased volume of distribution.

Typical kinetic values for lorazepam are: elimination half-life, 8 to 25 hours; volume of distribution, 1.0 to 1.3L/kg; clearance, 0.7 to 1.2ml/min/kg. Lorazepam clearance is somewhat reduced in old age, but liver disease has a minimal effect on clearance. Oral and intramuscular lorazepam are rapidly absorbed, with systemic availability averaging 90 % or more.

Both oxazepam and lorazepam are extensively bound to plasma protein, but the free fraction for lorazepam (8 to 12%) is greater than that for oxazepam (2 to 4%).

Keywords

Cimetidine Clinical Pharmacokinetic Oxazepam Disulfiram Acute Viral Hepatitis 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© ADIS Press Australasia Pty Ltd. 1981

Authors and Affiliations

  • David J. Greenblatt
    • 1
  1. 1.Division of Clinical Pharmacology, Departments of Psychiatry and MedicineTufts University School of Medicine and New England Medical Center HospitalUSA

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