Paliperidone extended-release tablet is indicated for:

• Schizophrenia, including acute treatment and prevention of recurrence
• Schizoaffective disorder, as monotherapy or in combination with antidepressants or mood stabilizers

Paliperidone is a psychotropic agent belonging to the benzisoxazole derivative class. It is the major active metabolite of risperidone. Paliperidone acts primarily as a centrally active dopamine type 2 (D2) receptor antagonist and serotonin type 2 (5-HT2A) receptor antagonist. It also shows antagonistic activity at α1 and α2 adrenergic receptors and H1 histaminergic receptors, which may contribute to some of its clinical effects. It has no significant affinity for cholinergic muscarinic receptors or β1 and β2 adrenergic receptors.

Schizophrenia:

• Adults: Initial dose is 6 mg/day. Recommended dose is 3–12 mg/day, Maximum dose is 12 mg/day.
• Adolescents (Weight <51 kg): Initial dose is 3 mg/day, Recommended dose is 3–6 mg/day, Maximum dose is 6 mg/day.
• Adolescents (Weight ≥51 kg): Initial dose is 3 mg/day, Recommended dose is 3–12 mg/day, Maximum dose is 12 mg/day.

Schizoaffective disorder: adults Initial dose is 6 mg/day. Recommended dose is 3–12 mg/day, Maximum dose is 12 mg/day.

Paliperidone extended release tablet can be taken with or without food. It must be swallowed whole with the aid of liquids. Tablets should not be chewed, divided or crushed.

• Paliperidone should be used with caution in combination with other centrally acting drugs and alcohol. It may antagonize the effect of Levodopa and other dopamine agonists.
• Because of its potential to induce orthostatic hypotension, an additive effect may be observed when Paliperidone is administered with other agents that also cause this condition.
• Strong CYP3A4/P-glycoprotein (P-gp) inducers: The dose of Paliperidone may need to be increased when a strong inducer of both CYP3A4 and P-gp (e.g., carbamazepine) is co-administered. Conversely, upon discontinuation of the inducer, dose reduction of Paliperidone may be required.
• Co-administration of divalproex sodium increases the Cmax and AUC of Paliperidone by approximately 50%. Dose adjustment may be required based on clinical evaluation.

The most common adverse reactions of Paliperidone include tachycardia, akathisia, somnolence, tremor, dystonia, cogwheel rigidity, anxiety, weight gain, dyspepsia, constipation, nasopharyngitis, etc.

Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Paliperidone should be used during pregnancy only if the potential benefits justify the potential risk to the fetus. Paliperidone is excreted in human breast milk. The benefits of breastfeeding should be weighed against the potential risks to the infant.

Caution should be exercised in patients with cardiovascular disease, QT prolongation, neuroleptic malignant syndrome, tardive dyskinesia, hyperglycemia, dyslipidemia, obesity, hyperprolactinemia, leukopenia, neutropenia, agranulocytosis, seizures, and risk of cognitive or motor impairment.

Pediatric use: Safety and effectiveness in schizophrenia have not been established in patients under 12 years of age. In schizoaffective disorder, safety and effectiveness have not been established in patients under 18 years of age.

Overdose data are limited. There is no specific antidote. In case of overdose, general supportive and symptomatic treatment should be provided.

Atypical neuroleptic drugs

Store in a cool, dry place away from light. Keep out of reach of children.