It is an atypical antipsychotic agent indicated for the ? acute and maintenance treatment of schizophrenia (1.1) ? acute treatment of schizoaffective disorder as monotherapy (1.2) ? acute treatment of schizoaffective disorder as an adjunct to mood stabilizers and/or antidepressants
Atypical neuroleptic drugs
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.
For schizophrenia: 6 mg extended-release tablet administered in the morning with or without food. Initial dose titration is not required. Some patients may benefit from either higher doses up to 12 mg/day,or a lower dose of 3 mg/day. If clinical assessment warrants,increase the dose at increments of 3 mg/day at intervals of more than 5 days. Maximum recommended dose is 12 mg/day. ? For schizoaffective disorder: 6 mg extended-release tablet administered in the morning with or without food. Initial dose titration is not required. Some patients may benefit from lower or higher doses within the recommended dose range of 3 to 12 mg once daily. If clinical assessment warrants,increase the dose at increments of 3 mg/day at intervals of more than 4 days. Maximum recommended dose is 12 mg/day. ? Tablet should be swallowed whole and should not be chewed,divided,or crushed. ? Patients may notice tablet-shaped shell in their stool.
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.
Known hypersensitivity to paliperidone,risperidone,or to any components in the formulation
Tachycardia,and akathisia in the schizophrenia trials,and extrapyramidal symptoms,somnolence,dyspepsia, constipation,weight increased,and nasopharyngitis
Use of first generation antipsychotic drugs during the last trimester of pregnancy has been associated with extrapyramidal symptoms in the neonate. These symptoms are usually self- limited. It is not known whether paliperidone,when taken near the end of pregnancy,will lead to similar neonatal signs and symptoms. Nursing Mothers: Paliperidone is excreted in human breast milk. The known benefits of breastfeeding should be weighed against the unknown risks of infant exposure to paliperidone.
Overdose of Paliperidone is limited; there is no specific antidote to Paliperidone. If overdose occurs general supportive and symptomatic measures should be employed.
Store in a cool and dry place, away from light. Keep out of reach of children.
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