Paliperidone Palmitate

What it is and how it works

Mechanism of Action Paliperidone is the major active metabolite of risperidone. The mechanism of action of paliperidone in schizophrenia is unclear. However, the drug's therapeutic effect in schizophrenia could be mediated through a combination of central dopamine Type 2 (D 2 ) and serotonin Type 2 (5HT 2A ) receptor antagonism.

Indications

Paliperidone Extended-Release Tablets are an atypical antipsychotic agent indicated for Treatment of schizophrenia Adults: Efficacy was established in three 6-week trials and one maintenance trial. Adolescents (ages 12–17): Efficacy was established in one 6-week trial. Treatment of schizoaffective disorder as monotherapy and as an adjunct to mood stabilizers and/or antidepressants. Efficacy was established in two 6-week trials in adult patients. Schizophrenia Paliperidone Extended-Release Tablets are indicated for the treatment of schizophrenia . The efficacy of Paliperidone Extended-Release Tablets in schizophrenia was established in three 6-week trials in adults and one 6-week trial in adolescents, as well as one maintenance trial in adults. Schizoaffective Disorder Paliperidone Extended-Release Tablets are indicated for the treatment of schizoaffective disorder as monotherapy and an adjunct to mood stabilizers and/or antidepressant therapy . The efficacy of Paliperidone Extended-Release Tablets in schizoaffective disorder was established in two 6-week trials in adults.

Dosage and administration (summary)

Initial Dose Recommended Dose Maximum Dose Schizophrenia - adults 6 mg/day 3 – 12 mg/day 12 mg/day Schizophrenia-adolescents Weight < 51 kg 3 mg/day 3 – 6 mg/day 6 mg/day Weight ≥ 51 kg 3 mg/day 3 – 12 mg/day 12 mg/day Schizoaffective disorder - adults 6 mg/day 3 – 12 mg/day 12 mg/day Tablet should be swallowed whole and should not be chewed, divided, or crushed. Schizophrenia Adults The recommended dose of Paliperidone Extended-Release Tablets for the treatment of schizophrenia in adults is 6 mg administered once daily. Initial dose titration is not required.

Contraindications

Paliperidone Extended-Release Tablets are contraindicated in patients with a known hypersensitivity to either paliperidone or risperidone, or to any of the excipients in the Paliperidone Extended-Release Tablets formulation. Hypersensitivity reactions, including anaphylactic reactions and angioedema, have been reported in patients treated with risperidone and in patients treated with paliperidone. Paliperidone is a metabolite of risperidone.

Warnings and precautions

Cerebrovascular Adverse Reactions: An increased incidence of cerebrovascular adverse reactions (e.g. stroke, transient ischemic attack, including fatalities) has been seen in elderly patients with dementia-related psychoses treated with atypical antipsychotics. Neuroleptic Malignant Syndrome: Manage with immediate discontinuation of drug and close monitoring. QT Prolongation: Increase in QT interval, avoid use with drugs that also increase QT interval and in patients with risk factors for prolonged QT interval. Tardive Dyskinesia: Discontinue drug if clinically appropriate.

Pregnancy

Pregnancy Risk Summary Neonates exposed to antipsychotic drugs during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms following delivery ( see Clinical Considerations ).

Storage and supply

Storage and Handling Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) . Protect from moisture. Keep out of reach of children.

Source: Paliperidone (Paliperidone) — US FDA prescribing information, 2026-04-30, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.