Fluphenazine
Fluphenazine.JPG

Fluphenazine

CLINICAL USE

Antipsychotic:Mania, schizophrenia and other psychoses Short-term use for anxiety, psychomotor agitation, excitement and violent or dangerously impulsive behaviour

DOSE IN NORMAL RENAL FUNCTION

Oral:Mania, schizophrenia and other psychoses: 2–20 mg daily in 2–3 divided dosesShort-term use for anxiety, psychomotor agitation, excitement and violent or dangerously impulsive behaviour: 1–2 mg twice dailyDeep IM:Schizophrenia and other psychoses: 12.5– 100 mg every 14–35 days

PHARMACOKINETICS

  • Molecular weight                           :437.5, 510.4 (as hydrochloride), (591.8 as decanoate)
  • %Protein binding                           :>90
  • %Excreted unchanged in urine     : 20
  • Volume of distribution (L/kg)       :10
  • half-life – normal/ESRD (hrs)      :14.7 (6–9 days after IM)

    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 a low 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      :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 plasma level of tricyclics; possibly increased risk of ventricular arrhythmias and antimuscarinic side effectsAnticonvulsant: antagonises anticonvulsant effect
  • Antimalarials: avoid concomitant use with artemether/lumefantrine
  • Antipsychotics: increased risk of ventricular arrhythmias with pimozide – avoid concomitant use; avoid concomitant use of depot formulations with clozapine (cannot be withdrawn quickly if neutropenia occurs)
  • Antivirals: concentration possibly increased with ritonavirAnxiolytics and hypnotics: increased sedative effects
  • 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 useAvoid concomitant use with drugs that prolong the QT interval

    ADMINISTRATION

    Reconstition

    Route

    Oral, IM

    Rate of Administration

    Comments





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