CLINICAL USE

Antipsychotic for agitation and restlessness

DOSE IN NORMAL RENAL FUNCTION

Psychomotor agitation: 100–200 mg 4 times a dayAgitation and restlessness in elderly: 25–50 mg 4 times a day

PHARMACOKINETICS

As for chlorpromazine

  • Molecular weight                           :320.9
  • %Protein binding                           :95–98
  • %Excreted unchanged in urine     : <1
  • Volume of distribution (L/kg)       :7–20
  • half-life – normal/ESRD (hrs)      :23–37/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           : Start with low doses and titrate slowly

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unlikely to be dialysed. Dose as in GFR <10 mL/min
  • HD                     :Unlikely to be dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux   :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD      :Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Anaesthetics: enhanced hypotensive effect
  • Analgesics: increased risk of convulsions with tramadol; enhanced hypotensive and sedative effects with opioids
  • Anti-arrhythmics: increased risk of ventricular arrhythmias with anti-arrhythmics that prolong the QT interval – avoid concomitant use with amiodarone
  • Antibacterials: increased risk of ventricular arrhythmias with moxifloxacin – avoid concomitant use
  • Antidepressants: increased level of tricyclics (possibly increased risk of ventricular arrhythmias and antimuscarinic side effects)Anticonvulsant: antagonises anticonvulsant effect
  • Antimalarials: avoid concomitant use with artemether/lumefantrine
  • Antipsychotics: increased risk of ventricular arrhythmias with pimozide – avoid concomitant use
  • Antivirals: concentration possibly increased with ritonavirAnxiolytics and hypnotics: increased sedative effects
  • Atomoxetine: increased risk of ventricular arrhythmias
  • Beta-blockers: enhanced hypotensive effect; increased risk of ventricular arrhythmias with sotalol
  • Diuretics: enhanced hypotensive effect
  • Lithium: increased risk of extrapyramidal side effects and possibly neurotoxicity
  • Pentamidine: increased risk of ventricular arrhythmias
  • Sibutramine: increased risk of CNS toxicity – avoid concomitant use with drugs that prolong the QT interval

    ADMINISTRATION

    Reconstition

    Route

    Oral

    Rate of Administration

    Comments

    OTHER INFORMATION

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