Paliperidone

Drug Approvals

(US Adopted Name, rINN)

Drug Approvals

(US Adopted Name, rINNM)

Profile

Paliperidone is a benzisoxazole derivative and is the major active metabolite of the atypical antipsychotic risperidone. It is reported to be an antagonist at dopamine D₂, serotonin (5-HT₂), adrenergic (α₁ and α₂), and histamine (H1) receptors. It is used in the treatment of schizophrenia.

The recommended oral dose of paliperidone is 6 mg once daily as a modified-release preparation doses may range from 3 to 12 mg daily. US licensed product information recommends that dose increases are made in small steps of 3 mg at intervals of more than 5 days.

For details of dose reductions in patients with renal impairment, see below.

Paliperidone palmitate is being developed as a long-acting intramuscular formulation.

Administration in renal impairment.

The plasma concentrations of paliperidone are increased in patients with renal impairment. The usual oral daily dosage (see above) should therefore be adjusted according to creatinine clearance (CC). In the UK, licensed product information recommends the following doses:

• CC 50 to 80 mL/minute: initially 3 mg once daily, may be increased thereafter according to response and tolerance
• CC 30 to 50 mL/minute: 3 mg once daily
• CC 10 to 30 mL/minute: initially 3 mg on alternate days which may be increased thereafter to 3 mg once daily after clinical reassessment

However, US licensed product information recommends the following maximum doses:

• CC 50 to 80 mL/minute: 6 mg once daily
• CC 10 to 50 mL/minute: 3 mg once daily

Paliperidone has not been studied in patients with a CC of less than 10 mL/minute UK product information does not recommend its use in such patients.

Proprietary Preparations

Czech Republic: Invega

France: Invega

Portugal: Invega

United Kingdom: Invega

USA: Invega