Paliperidone is an atypical antipsychotic that is a major active metabolite of risperidone (5-hydroxyrisperidone), approved for use in the US in 2006 as daily oral extended-release tablets and 1-month or 3-month LAI formulations
[28][29][30]. Paliperidone ER is indicated for treatment of schizophrenia in adults and adolescents ages 12–17
[28]. It is available in 1.5 mg, 3 mg, 6 mg, 9 mg and 12 mg
[28]. The LAI form of paliperidone is indicated for the treatment of schizophrenia or schizoaffective disorder in adults as monotherapy or in conjunction with mood stabilizers, only after tolerance to oral paliperidone or risperidone has been demonstrated
[29][30]. The 3-month injectable is to be used only after successful administration of the 1-month LAI
[30]. The 1-month LAI is available in dosages of 39 mg, 78 mg, 117 mg, 156 mg, or 234 mg and the 3-month injectable is available in the higher dosages of 273 mg, 410 mg, 546 mg, or 819 mg
[29][30]. Contraindications to the use of paliperidone include previous hypersensitivity reactions to paliperidone or risperidone
[28][29][30]. Paliperidone, like all antipsychotics, is contraindicated for use in elderly patients with dementia-related psychosis, holding a boxed warning for increased mortality in this population
[28][29][30]. Adverse events of paliperidone are consistent with other atypical antipsychotics due to dopamine blockade and effects at other neurotransmitter receptors. These include cerebrovascular disease (in the elderly), neuroleptic malignant syndrome, QT prolongation, extrapyramidal symptoms, tardive dyskinesia, weight gain, dyslipidemia, hyperglycemia, hyperprolactinemia, orthostatic hypotension, leukopenia, cognitive impairment and seizures
[28][29][30]. No teratogenic effects have been demonstrated, but there is increased risk for EPS and/or withdrawal symptoms in neonates exposed during pregnancy
[28][29][30]. Coadministration of paliperidone ER tablets or LAI with risperidone has not been studied
[28][29][30].