Aripiprazole

CLINICAL USE

Atypical antipsychotic for the treatment of schizophrenia

DOSE IN NORMAL RENAL FUNCTION

10–30 mg daily

PHARMACOKINETICS

Molecular weight : 448.4

%Protein binding : >99

%Excreted unchanged in urine : <1

Volume of distribution (L/kg) : 4.9

half-life – normal/ESRD (hrs) : 75 (146 in poor metabolisers)/ Unchanged

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 : Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD : Not dialysed. Dose as in normal renal function

HD : Not dialysed. Dose as in normal renal function

HDF/high flux : Unlikely to be dialysed. Dose as in normal renal function

CAV/VVHD : Not 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 opioids Antihypertensives: may enhance antihypertensive effect

Alcohol and other CNS drugs: increased sedation and other related side effects

Anti-arrhythmics: increased risk of ventricular arrhythmias with anti- arrhythmics that prolong the QT interval

Antibacterials: concentration possibly reduced by rifabutin and rifampicin – increase dose of aripiprazole

Antidepressants: fluoxetine and paroxetine possibly inhibit metabolism – reduce dose of aripiprazole; concentration possibly reduced by St John’s wort – increase aripiprazole dose; increased concentration of tricyclics

Anti-epileptics: antagonises anticonvulsant effect; concentration reduced by carbamazepine and possibly reduced by phenytoin, phenobarbital and primidone – increase dose of aripiprazole Antifungals: metabolism inhibited by ketoconazole and possibly by itraconazole reduce dose of aripiprazole

Antimalarials: avoid concomitant use with artemether/lumefantrine

Antivirals: metabolism possibly inhibited by amprenavir, atazanavir, indinavir, lopinavir, nelfinavir, ritonavir and saquinavir – reduce dose of aripiprazole; concentration possibly reduced by efavirenz and nevirapine – increase dose of aripiprazole

Anxiolytics and hypnotics: increased sedative effects S

ibutramine: increased risk of CNS toxicity – avoid concomitant use

ADMINISTRATION

Reconstition

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Route

Oral

Rate of Administration

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Comments

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OTHER INFORMATION

Hepatic metabolism and elimination Can cause QT prolongation

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

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