Lormetazepam

CLINICAL USE

Benzodiazepine:Insomnia (short-term use)

DOSE IN NORMAL RENAL FUNCTION

0.5–1.5 mg at night

PHARMACOKINETICS

  • Molecular weight                           :335.2
  • %Protein binding                           :85
  • %Excreted unchanged in urine     : <6 (86 as metabolites)
  • Volume of distribution (L/kg)       :4.6
  • half-life – normal/ESRD (hrs)      :11–16/Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Dose as in normal renal function. Start with small doses
  • <10           : Dose as in normal renal function. Start with small doses

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Not dialysed. Dose as in GFR <10 mL/min
  • HD                     :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux   :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD      :Unknown dialysability. Dose as in GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antibacterials: metabolism possibly increased by rifampicin
  • Antipsychotics: increased sedative effects
  • Antivirals: concentration possibly increased by ritonavirDisulfiram: metabolism inhibited, increased sedative effectsSodium oxybate: enhanced effect – avoid concomitant use

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Increased CNS sensitivity in renal impairmentLong-term use may lead to dependence and withdrawal symptoms in certain patientsThe half-life of the glucuronide metabolite is increased in renal impairment

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