CLINICAL USE

Antipsychotic for schizophrenia and other psychoses

DOSE IN NORMAL RENAL FUNCTION

Schizophrenia and paranoid psychoses: Oral: 20–30 mg daily in divided doses; maximum 150 mg daily Maintenance:

  • 20 to 50     : mg daily Deep IM: 200–500 mg every 1–4 weeks Maximum: 600 mg weekly Acute psychoses: (Clopixol Acuphase) Deep IM: 50–150 mg, repeated if required after 2–3 days Maximum 400 mg per course

    PHARMACOKINETICS

  • Molecular weight                           : 401 (443 as acetate), (473.9 as hydrochloride), (555.2 as decanoate)
  • %Protein binding                           : 98
  • %Excreted unchanged in urine     : Minimal (
  • 10 to 20
  • % unchanged drug and metabolites)

  • Volume of distribution (L/kg)       :
  • 10 to 20     :
  • half-life – normal/ESRD (hrs)      : 20–24

    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 50% of the dose and titrate slowly

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                : Not dialysed. Dose as in GFR <10 mL/min
  • HD                     : Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux   : Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD      : Not dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Anaesthetics: enhanced hypotensive effects
  • 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
  • Antidepressants: increased level of tricyclics
  • Anti-epileptics: anticonvulsant effect antagonised
  • Antimalarials: avoid concomitant use with artemether/lumefantrine
  • Antipsychotics: avoid concomitant use of clozapine with depot preparations in case of neutropenia
  • Antivirals: concentration possibly increased with ritonavir Anxiolytics and hypnotics: increased sedative effects
  • Sibutramine: increased risk of CNS toxicity – avoid concomitant use Avoid concomitant use with drugs that prolong the QT interval

    ADMINISTRATION

    Reconstition

    Route

    Oral, IM

    Rate of Administration

    Comments

    OTHER INFORMATION

    May cause hypotension and excessive sedation Increased CNS sensitivity in renally impaired patients – start with small doses as can accumulate Peak levels occur 3–6 hours after oral administration .the liver. It can be used in renal failure at normal doses with caution.

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