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Interaction of cimetidine with oxazepam, lorazepam, and flurazepam

Interaction of cimetidine with oxazepam, lorazepam, and flurazepam

  1. Ilsa
    Abstract: The influence of cimetidine coadministration, 300 mg every 6 hours, on the
    kinetics of single oral doses of oxazepam (30 mg), lorazepam (2mg), and flurazepam
    (30 mg) was evaluated in healthy volunteers. Cimetidine had no significant effect on
    the peak plasma concentration orthe time of peak concentration for either oxazepam,
    lorazepam, or desalkylflurazepam (formed from flurazepam). Cimetidine likewise did
    not alter the elimination half-life of oxazepam (9.4 hours) or lorazepam (11.6 hours),
    and did not change total AUC for lorazepam. Oxazepam AUC was increased an
    average of 10 per cent by cimetidine (P < 0.02). In contrast, cimetidine prolonged
    desalkylflurazepam elimination half-life (141 vs. 94 hours, P< 0.1) and increased AUG
    an average of 65 per cent (P< 0.05). Thus, cimetidine has little or no influence on the
    absorption or disposition of oxazepam and lorazepam, two benzodiazepines biotrans-
    formed by glucuronide conjugation. However, cimetidine slows the elimination of
    flurazepam’s metabolite, desalkylflurazepam, which is biotransformed by oxidation.