Aripiprazole

CLINICAL USE

Atypical antipsychotic for the treatment of
schizophrenia

DOSE IN NORMAL RENAL FUNCTION

10–30 mg daily

PHARMACOKINETICS

Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
448.4

%Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
>99

%Excreted unchanged in urine &nbsp &nbsp :
<1

Volume of distribution (L/kg) &nbsp &nbsp &nbsp :
4.9

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

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 :
Dose as in normal renal function

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:
Not dialysed. Dose as in normal renal function

HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :
Not dialysed. Dose as in normal renal function

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

CAV/VVHD &nbsp &nbsp &nbsp:
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

–

Route

Oral

Rate of Administration

–

Comments

–

OTHER INFORMATION

Hepatic metabolism and elimination

Can cause QT prolongation

Tags: post-by-auto-php