Fluoxetine

CLINICAL USE

SSRI antidepressant:Depressive illness Bulimia nervosa Obsessive compulsive disorder

DOSE IN NORMAL RENAL FUNCTION

20–60 mg daily depending on indication

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :345.8 (as hydrochloride)

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :94.5

%Excreted unchanged in urine &nbsp &nbsp :

<10 &nbsp &nbsp &nbsp &nbsp &nbsp :

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :20–40

half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :Acute dosing: 24–72/UnchangedChronic dosing: 4–6 days/Increased

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

20 to 50 &nbsp &nbsp : Dose as in normal renal function

10 to 20 &nbsp &nbsp : Dose as in normal renal function

<10 &nbsp &nbsp &nbsp &nbsp &nbsp : Use low dose, or on alternate days and increase according to response

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR <10 mL/min

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Not dialysed. Dose as in GFR <10 mL/min

HDF/high flux &nbsp :Not dialysed. Dose as in GFR <10 mL/min

CAV/VVHD &nbsp &nbsp &nbsp:Not dialysed. Dose as in GFR=

10 to 20 &nbsp &nbsp : mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Analgesics: increased risk of bleeding with aspirin and NSAIDs; risk of CNS toxicity increased with tramadol

Anti-arrhythmics: increased flecainide concentration

Anticoagulants: effect of coumarins possibly enhanced

Antidepressants: avoid concomitant use with MAOIs and moclobemide, increased risk of toxicity; avoid concomitant use with St John’s wort; possibly enhanced serotonergic effects with duloxetine; can increase tricyclics antidepressant concentration; increased agitation and nausea with tryptophan

Anti-epileptics: antagonism (lowered convulsive threshold); concentration of carbamazepine and phenytoin increased

Antimalarials: avoid concomitant use with artemether/lumefantrine

Antipsychotics: concentration of haloperidol, clozapine, risperidone, sertindole and zotepine increased; possibly inhibit aripiprazole metabolism – reduce aripiprazole dose

Antivirals: concentration possibly increased by ritonavir

Ciclosporin: may increase ciclosporin concentration

Dopaminergics: increased risk of hypertension and CNS excitation with selegiline – avoid concomitant use; increased risk of CNS toxicity with rasagiline – avoid concomitant use5HT 1 agonist: increased risk of CNS toxicity with sumatriptan; possibly increased risk of serotonergic effects with frovatriptan

Lithium: increased risk of CNS effects (lithium toxicity reported)

Sibutramine: increased risk of CNS toxicity – avoid concomitant use

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

–

Comments

OTHER INFORMATION

Accumulation may occur in patients with severe renal failure during chronic treatment (metabolites are excreted renally)

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