Modesto(Paliperidone)
Therapeutic Group: Antipsychotic
Presentation
Modestoâ„¢ XR 3: Each extended release tablet contains Paliperidone USP 3 mg.
Modestoâ„¢ XR 6: Each extended release tablet contains Paliperidone USP 6 mg.
Description
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.
Indications
Paliperidone XR is indicated for-
• Schizophrenia, including acute treatment and recurrence prevention
• Treatment of schizoaffective disorder as monotherapy and in combination with antidepressants or mood stabilizers
Dosage & Administration
• Schizophrenia-adults Initial dose is 6 mg/day. Recommended dose is 3-12 mg/day, Maximum dose is 12 mg/day
• Schizophrenia-adolescents (Weight < 51kg) Initial dose is 3 mg/day, Recommended dose is 3-6 mg/day, Maximum dose is 6 mg/day
• Schizophrenia-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
• Paliperidone XR 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.
Side Effects
The most common adverse reactions of Paliperidone are tachycardia, akathisia, somnolence, tremor, dystonia, cogwheel rigidity, anxiety, weight increased, dyspepsia, constipation, nasopharyngitis etc.
Precautions
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 Pregnancy & Lactation
Pregnancy: 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.
Lactation: Paliperidone is excreted in human breast milk. The known benefits of breastfeeding should be weighed against the unknown risks of infant exposure to Paliperidone.
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.
Drug Interaction
• 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 for inducing orthostatic hypotension, an additive effect may be observed when Paliperidone is administered with other therapeutic agents that have this potential.
• Strong CYP3A4/P-glycoprotein (P-gp) inducers: It may be necessary to increase the dose of Paliperidone when a strong inducer of both CYP3A4 and P-gp (e.g., carbamazepine) is co-administered. Conversely, on discontinuation of the strong inducer, it may be necessary to decrease the dose of Paliperidone.
• Co-administration of divalproex sodium increased Cmax and AUC of Paliperidone by approximately 50%. Adjust dose of Paliperidone if necessary based on clinical assessment.
Over Dose
Overdose of Paliperidone is limited; there is no specific antidote to Paliperidone. If overdose occurs general supportive and symptomatic measures should be employed.
Storage
Do not store above 300 C. Keep away from light and out of the reach of children.
Commercial Pack
Modestoâ„¢ XR 3: Each box contains 3 blister strips of 10 tablets.
Modestoâ„¢ XR 6: Each box contains 3 blister strips of 10 tablets.