Aripiprazole

CLINICAL USE

Atypical antipsychotic for the treatment of
schizophrenia

DOSE IN NORMAL RENAL FUNCTION

10–30 mg daily

PHARMACOKINETICS

  • Molecular weight                           :
    448.4
  • %Protein binding                           :
    >99
  • %Excreted unchanged in urine     :
    <1
  • Volume of distribution (L/kg)       :
    4.9
  • half-life – normal/ESRD (hrs)      :
    75 (146 in poor
    metabolisers)/
    Unchanged

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Dose as in normal renal function
  • <10           :
    Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :
    Not dialysed. Dose as in normal renal function
  • HD                     :
    Not dialysed. Dose as in normal renal function
  • HDF/high flux   :
    Unlikely to be dialysed. Dose as in
    normal renal function
  • CAV/VVHD      :
    Not dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Anaesthetics: enhanced hypotensive effect
  • Analgesics: increased risk of convulsionswith tramadol; enhanced hypotensive and
    sedative effects with opioids
    Antihypertensives: may enhance

    antihypertensive effect

  • Alcohol and other CNS drugs: increasedsedation and other related side effects
  • Anti-arrhythmics: increased risk ofventricular arrhythmias with anti-
    arrhythmics that prolong the QT interval
  • Antibacterials: concentration possiblyreduced by rifabutin and rifampicin –
    increase dose of aripiprazole
  • Antidepressants: fluoxetine and paroxetinepossibly inhibit metabolism – reduce dose
    of aripiprazole; concentration possibly
    reduced by St John’s wort – increase
    aripiprazole dose; increased concentration
    of tricyclics
  • Anti-epileptics: antagonises anticonvulsanteffect; concentration reduced by
    carbamazepine and possibly reduced by
    phenytoin, phenobarbital and primidone –
    increase dose of aripiprazole
    Antifungals: metabolism inhibited by

    ketoconazole and possibly by itraconazole
    reduce dose of aripiprazole

  • Antimalarials: avoid concomitant use withartemether/lumefantrine
  • Antivirals: metabolism possibly inhibitedby amprenavir, atazanavir, indinavir,
    lopinavir, nelfinavir, ritonavir and
    saquinavir – reduce dose of aripiprazole;
    concentration possibly reduced by
    efavirenz and nevirapine – increase dose
    of aripiprazole
  • Anxiolytics and hypnotics: increasedsedative effects
    S
  • ibutramine: increased risk of CNStoxicity – avoid concomitant use

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Hepatic metabolism and elimination

    Can cause QT prolongation

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