CLINICAL USE


Benzodiazepine:Hypnotic

DOSE IN NORMAL RENAL FUNCTION

5–10 mg at bedtime; elderly (or debilitated) 2.5–5 mg

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :281.3
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :87
  • %Excreted unchanged in urine &nbsp &nbsp : <5
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :2
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :24–30/Unchanged

    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 : Dose as in normal renal function. Start with small doses

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unlikely to be dialysed. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unlikely to be 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:Unlikely to be dialysed. Dose as in normal renal function

    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 of nitrazepam inhibited, increased sedative effectsSodium oxybate: enhanced effects of sodium oxybate – avoid

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Mild to moderate renal insufficiency does not alter the kinetics of nitrazepamCKD 5 patients will be more susceptible to adverse effects (drowsiness, sedation, unsteadiness).