CLINICAL USE


Treatment of Parkinson’s disease

DOSE IN NORMAL RENAL FUNCTION

1 mg daily

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :267.3 (as mesilate)
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :60–70
  • %Excreted unchanged in urine &nbsp &nbsp : <1
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :243 litres
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :0.6–2/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

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unknown dialysability. Dose as in normal renal function
  • HDF/high flux &nbsp :Likely to be dialysed. Dose as in normal renal function
  • CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Analgesics: avoid concomitant use with dextromethorphan; avoid concomitant use with pethidine (risk of serious adverse reactions) – allow at least 14 days before starting pethidine
  • Antidepressants: avoid concomitant use with other MAOIs (can lead to hypertensive crisis) – allow at least 14 days before starting a MAOI; avoid concomitant use with fluoxetine and fluvoxamine; allow 5 weeks between stopping fluoxetine and starting rasagiline; allow 14 days between stopping rasagiline and starting fluoxetine or fluvoxamine; increased CNS toxicity with SSRIs and tricyclics
  • Sympathomimetics: concomitant use is not recommended

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

    Rasagiline is an irreversible selective inhibitor of monoamine oxidase type B.