Apomorphine hydrochloride

CLINICAL USE


Treatment of refractory motor fluctuations in
Parkinson’s disease

DOSE IN NORMAL RENAL FUNCTION


3–30 mg daily in divided doses (maximum
single dose 10 mg); infusion: 1–4 mg/hour
during waking hours
Maximum dose 100 mg daily

PHARMACOKINETICS


  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    312.8
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    90
  • %Excreted unchanged in urine &nbsp &nbsp :
    <2
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
    2–19
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
    29.1–36.9 minutes

    DOSE IN RENAL IMPAIRMENT


    GFR (mL/MIN)


  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function.
    Start with 1 mg
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function.
    Start with 1 mg
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function. Start with 1 mg

    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 :
    Unlikely to be dialysed. Dose as in
    GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:
    Unlikely to be dialysed. Dose as in
    GFR 10 to 20 mL/min

    IMPORTANT DRUG INTERACTIONS


    Potentially hazardous interactions with other drugs

  • Nitrates: enhanced hypotensive effect
  • Antihypertensives: enhanced hypotensive

    effect

    ADMINISTRATION


    Reconstition



    Route


    SC

    Rate of Administration


    1–4 mg/hour

    Comments


    Change site every 4 hours for SC

    administration

    OTHER INFORMATION

  • Pre-treatment with domperidone is

    required for at least 2 days before and at
    least 3 days after treatment

  • Bioavailability by subcutaneous

    administration is 17–18%

  • Most of dose is excreted in the urine as

    active metabolites

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