Paliperidone

CLINICAL USE

Atypical antipsychotic for schizophrenia

DOSE IN NORMAL RENAL FUNCTION

3–12 mg once daily

PHARMACOKINETICS

Molecular weight :426.5

%Protein binding :74

%Excreted unchanged in urine : 59

Volume of distribution (L/kg) :487 litres

half-life – normal/ESRD (hrs) :23/51

DOSE IN RENAL IMPAIRMENT

GFR (mL/MIN)

50–80 3 mg once daily and increase according to response30–50 3 mg once daily and increase according to response10–30 3 mg alternate days, increasing to 3 mg daily according to response

<10 : 3 mg alternate days, increasing to 3 mg daily according to response. Use with caution

DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

CAPD :Unknown dialysability. Dose as in GFR <10 mL/min

HD :Unknown dialysability. 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 GFR=10–30 mL/min

IMPORTANT DRUG INTERACTIONS

Potentially hazardous interactions with other drugs

Anaesthetics: enhanced hypotensive effect

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

Antidepressants: increases concentration of tricyclics (possibly increased risk of ventricular arrhythmias)

Antimalarials: avoidance of antipsychotics advised by manufacturer of artemether/lumefantrine

Atomoxetine: increased risk of ventricular arrhythmias with atomoxetine

Anti-epileptics: antagonise anticonvulsant effect (convulsive threshold lowered)

Antivirals: concentration possibly increased by ritonavir

Sibutramine: increased risk of CNS toxicity – manufacturer of sibutramine advises avoid concomitant use

ADMINISTRATION

Reconstition

–

Route

Oral

Rate of Administration

–

Comments

–

OTHER INFORMATION

Clearance is reduced by 71% in ERF

Contraindicated (by manufacturer) in patients with GFR <10 mL/min, due to lack of experience.

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