CLINICAL USE

Nausea and vomiting Labyrinthine disorders Psychoses Severe anxiety

DOSE IN NORMAL RENAL FUNCTION

Oral: 5–10 mg 2–3 times daily Buccal: 1–2 tablets twice daily IM/IV: 12.5 mg (unlicensed IV) Psychoses: Oral: 75–100 mg daily, IM: 12.5–25 mg 2–3 times dailySevere anxiety: 15–20 mg daily by mouth, in divided doses; maximum 40 mg daily

PHARMACOKINETICS

  • Molecular weight                           :373.9
  • %Protein binding                           :96
  • %Excreted unchanged in urine     : Minimal
  • Volume of distribution (L/kg)       :23
  • half-life – normal/ESRD (hrs)      :6–9/–

    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 small doses, i.e. 6.25 mg IM or 5 mg orally

    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      :Unlikely to be dialysed. 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 opioidsAnti-arrhythmics increased risk of ventricular arrhythmias with anti-arrhythmics that prolong the QT interval, e.g. procainamide, disopyramide and amiodarone – avoid concomitant use with amiodarone
  • Antibacterials: increased risk of ventricular arrhythmias with moxifloxacin – avoid concomitant use
  • Antidepressants: increase concentrations and additive antimuscarinic effects, notably with tricyclics
  • Anti-epileptics: antagonised (convulsive threshold lowered)
  • 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 sotalolDesferrioxamine: avoid concomitant use
  • 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

    ADMINISTRATION

    Reconstition

    –

    Route

    IM, IV (unlicensed), oral, buccal

    Rate of Administration

    IM or IV over 3–4 minutes

    Comments

    Unlicensed IV administration methods: Either: dilute with water for injection —to 5 times its own volume, and administer slowly over not less than 5 minutes,Or dilute to 1 mg/mL and administer at —rate not greater than 1 mg/minute

    OTHER INFORMATION

    Increased CNS sensitivity in severe renal impairment.

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