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 :345.8 (as hydrochloride)

%Protein binding :94.5

%Excreted unchanged in urine :

<10 :

Volume of distribution (L/kg) :20–40

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

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 : Use low dose, or on alternate days and increase according to response

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

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

10 to 20 : 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)

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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