Amisulpride

CLINICAL USE


Treatment of acute and chronic
schizophrenia

DOSE IN NORMAL RENAL FUNCTION


50–1200 mg daily (in divided doses if
>300 mg); varies according to indication

PHARMACOKINETICS


  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    369.5
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
    16
  • %Excreted unchanged in urine &nbsp &nbsp :
    50
  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
    5.8
  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :
    12/Unchanged

    DOSE IN RENAL IMPAIRMENT


    GFR (mL/MIN)


    30–60 Reduce dose by 50%
    10–30 Use a third of the dose.
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp :
    Use with caution. Start with
    minimum dose and increase
    according to patient’s response

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES


  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:
    Not dialysed. Dose as in
    GFR <10 mL/min

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

    IMPORTANT DRUG INTERACTIONS


    Potentially hazardous interactions with other drugs

  • Alcohol: may enhance CNS effects of

    alcohol

  • Anaesthetics: enhanced hypotensive effect
  • Analgesics: increased risk of convulsions

    with tramadol; enhanced hypotensive and
    sedative effects with opioids

  • Antiarrhythmics: increased risk of

    ventricular arrhythmias with antiarrhythmics that prolong the QT interval;
    avoid concomitant use with amiodarone,
    disopyramide and procainamide (risk of
    ventricular arrhythmias)

  • Antibacterials: avoid concomitant use with

    parenteral erythromycin (increased risk of
    ventricular arrhythmias)

  • Antidepressants: increased level of

    tricyclics

  • Antiepileptics: antagonises anticonvulsant

    effect

  • Antihypertensives: increased risk of

    hypotension

  • Antimalarials: avoid concomitant use with

    artemether/lumefantrine
    Antipsychotics: increased risk of

    ventricular arrhythmias with sertindole –
    avoid concomitant use

  • Antivirals: concentration possibly

    increased by ritonavir
    Anxiolytics & hypnotics: increased

    sedative effects

  • Atomoxetine: increased risk of ventricular

    arrhythmias

  • Beta-blockers: increased risk of ventricular

    arrhythmias with sotalol
    Diuretics: increased risk of ventricular

    arrhythmias due to hypokalaemia

  • Pentamidine: increased risk of ventricular

    arrhythmias – avoid

  • Sibutramine: increased risk of CNS

    toxicity – avoid concomitant use

    ADMINISTRATION


    Reconstition



    Route


    Oral

    Rate of Administration



    Comments



    OTHER INFORMATION


    Elimination half-life is unchanged in

    patients with renal insufficiency, while
    systemic clearance is reduced by a factor
    of 2.5–3. The area under the curve of
    amisulpride in mild renal failure is
    increased 2-fold, and almost 10-fold in
    moderate renal failure. Experience is
    limited and there is no data with doses
    >50 mg