Paliperidone is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives. Paliperidone is the major active metabolite of Risperidone. It is a centrally active dopamine Type 2 (D2) antagonist and with predominant serotonin Type 2 (5-HT2A) antagonist activity. It is also active as an antagonist at α1 and α2 adrenergic receptors and H1 histaminergic receptors, which may explain some of the other effects of the drug. It has no affinity for cholinergic muscarinic or β1-and β2-adrenergic receptors.

Paliperidone extended release tablet is indicated for-

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

Schizophrenia:

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

Administration

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.

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

Overdose Effects

Overdose of Paliperidone is limited; there is no specific antidote to Paliperidone. If overdose occurs general supportive and symptomatic measures should be employed.

Caution should be exercised when Paliperidone is prescribed in patients with known Cardiovascular diseases, QT prolongation, Neuroleptic malignant syndrome, Tardive dyskinesia, Hyperglycemia, Dyslipidemia, Obesity, Hyperprolactinemia, Leukopenia, Neutropenia, Agranulocytosis, Seizures, Potential for Cognitive & Motor impairment etc.

Use in Special Populations

Pediatric use: Safety and effectiveness in the treatment of schizophrenia not established in patients less than 12 years of age. Safety and effectiveness in the treatment of schizoaffective disorder not established in patients less than 18 years of age.

Pregnancy & Lactation

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 justifies the potential risk to the fetus. Paliperidone is excreted in human breast milk. The known benefits of breastfeeding should be weighed against the unknown risks of infant exposure to Paliperidone.