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with pimozide – avoid concomitant use; avoid concomitant use of depot formulations with clozapine (cannot be withdrawn quickly if neutropenia occurs)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

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Route

Oral, IM

Rate of Administration

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