CLINICAL USE


Benzodiazepine:Anxiolytic Insomnia

DOSE IN NORMAL RENAL FUNCTION

Anxiolytic: 15–30 mg 3 or 4 times a dayInsomnia: 15–50 mg at night

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :286.7
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :85–97
  • %Excreted unchanged in urine &nbsp &nbsp : <1

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :0.6–1.6

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :3–21/25–90

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Start at low dose and increase according to response

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Antibacterials: metabolism possibly increased by rifampicin
  • Antipsychotics: enhanced sedative effects
  • Antivirals: possibly increased concentration with ritonavir
    Sodium oxybate: enhanced effects of sodium oxybate – avoid
  • Ulcer-healing drugs: metabolism inhibited by cimetidine

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Protein binding decreased and volume of distribution increased in glucuronide metabolite accumulates in CKD 5; significance of this unknown.
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