Entecavir

CLINICAL USE


Treatment of chronic hepatitis B infection

DOSE IN NORMAL RENAL FUNCTION

500 mcg daily; 1000 mcg daily in lamivudine-refractory patients

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :295.3
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :13
  • %Excreted unchanged in urine &nbsp &nbsp : 75
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :Large
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :128–149

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

    30–50 250 mcg daily; 500 mcg daily in lamivudine-refractory patients10–30 150 mcg daily; 300 mcg daily in lamivudine-refractory patients
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : 50 mcg daily; 100 mcg daily in lamivudine-refractory patients

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:0.3% dialysed. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :13% dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp :Dialysed. Dose as in GFR
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Likely to be 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