CLINICAL PHARMACOKINETICS OF LORAZEPAM - REVIEW

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  • 1 January 1978
    • journal article
    • review article
    • Vol. 39  (10) , 16-23
Abstract
The clinical [human] pharmacokinetics of lorazepam, a 3-hydroxy,1,4-benzodiazepine, indicate that it is rapidly and readily absorbed, reaching peak concentrations in the blood proportional to the dose approximately 2 h after oral administration. Blood levels decline thereafter, with an elimination half-life of about 12 h. Conjugation with glucuronic acid to form inactive lorazepam glucuronide is the major metabolic pathway. Of the administered dose, 70-75% is excreted as the glucuronide conjugate in the urine. On multiple-dose regimens, steady state blood levels directly proportional to the daily dose occur within 2-3 days and are maintained after several months of continuous treatment. The active drug and the glucuronide conjugate are completely eliminated from the blood within 1 wk following the last dose. [Lorazepam, like other 1,4-benzodiazepines, has clinically demonstrable anti-anxiety effects.].

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