CLINICAL USE

Aid to smoking cessation

DOSE IN NORMAL RENAL FUNCTION

0.5 mg once daily for 3 days, 0.5 mg twice daily for 3 days, then 0.5–1 mg twice daily

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : 361.3 (as tartrate)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : <20
  • %Excreted unchanged in urine &nbsp &nbsp : 92
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp : 415 litres
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp : 24/Increased

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    Initial doses as for normal renal function, then maintenance doses of: 30–50 1 mg once or twice daily 10–30 1 mg once daily
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : 0.5–1 mg once daily

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp: Unknown dialysability. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp : Dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp : Dialysed. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp: Dialysed. Dose as in GFR=10–30 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • None known

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    – .