CLINICAL USE

Insomnia (short-term treatment)

DOSE IN NORMAL RENAL FUNCTION

5–10 mg at night

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 764.9
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 92.5
  • %Excreted unchanged in urine &nbsp &nbsp : Negligible (56% as active metabolites)
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp : 0.34–0.54 (depends on age)
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp : Average: 2.4/ Increased

    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

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp: Not dialysed. Dose as in normal renal function

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

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Antibacterials: metabolism accelerated by rifampicin
  • Antipsychotics: enhanced sedative effects
  • Antivirals: concentration increased by ritonavir (risk of extreme sedation and respiratory depression) – avoid concomitant use

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    First pass metabolism by liver is 35% Clearance is reduced in renal impairment .