From the Guidelines
Paliperidone is an atypical antipsychotic primarily indicated for the treatment of schizophrenia in adults and adolescents (12 years and older), schizoaffective disorder in adults, and acute treatment of manic and mixed episodes associated with bipolar I disorder. The medication works by blocking dopamine D2 receptors and serotonin 5-HT2A receptors in the brain, helping to regulate neurotransmitter activity that contributes to psychotic symptoms. Common side effects of paliperidone include:
- Extrapyramidal symptoms (movement disorders like tremor, rigidity, and akathisia) as reported in 1, where the proportion of patients reporting EPS-related TEAEs during the AC/CT phases was higher in the paliperidone ER group
- Weight gain
- Increased prolactin levels which may cause sexual dysfunction and gynecomastia
- Sedation
- Dizziness
- Orthostatic hypotension More serious adverse effects can include:
- Metabolic changes (hyperglycemia, dyslipidemia)
- QT interval prolongation which may increase risk of arrhythmias
- Neuroleptic malignant syndrome
- Tardive dyskinesia with long-term use It's worth noting that, as discussed in 1 and 1, atypical antipsychotics like paliperidone are generally better tolerated than traditional antipsychotic medications, with a lower risk for extrapyramidal symptoms, but they can have other significant side effects, such as weight gain. Paliperidone requires dose adjustment in patients with renal impairment as it is primarily excreted unchanged in urine, and the medication is available in both oral extended-release tablets and long-acting injectable formulations, with the latter being beneficial for patients with adherence concerns.
From the FDA Drug Label
Paliperidone is an atypical antipsychotic agent indicated for Treatment of schizophrenia Treatment of schizoaffective disorder as monotherapy and as an adjunct to mood stabilizers and/or antidepressants.
The indications of Paliperidone are:
- Treatment of schizophrenia in adults and adolescents (ages 12 to 17)
- Treatment of schizoaffective disorder as monotherapy and as an adjunct to mood stabilizers and/or antidepressants in adults
The side effects of Paliperidone include:
- Extrapyramidal symptoms
- Tachycardia
- Akathisia
- Somnolence
- Dyspepsia
- Constipation
- Weight increased
- Nasopharyngitis
- Nervous system disorders
- Gastrointestinal disorders 2 2 2
From the Research
Indications of Paliperidone
- Paliperidone is indicated for the acute and maintenance treatment of schizophrenia in adults in the US and the EU 3.
- It is also approved for the treatment of schizoaffective disorder, as demonstrated by its efficacy in two 6-week, randomized, double-blind, placebo-controlled trials 4.
- The medication has shown significant improvements in psychopathology, functioning, and relapse in patients with schizophrenia when compared with placebo 5, 6.
Side Effects of Paliperidone
- Common side effects of paliperidone include headache, tremor, dizziness, insomnia, nausea, akathisia, dyspepsia, hypertonia, somnolence, and sedation 4, 6.
- Extrapyramidal symptoms, such as parkinsonism, occurred in approximately a quarter of patients treated with higher doses of paliperidone ER (9 and 12 mg/day) in 6-week trials 3.
- Paliperidone has been associated with an increased risk of hyperprolactinemia, particularly in women 5, 7.
- The medication may also cause weight gain, with clinically significant gains in bodyweight seen in 15% of patients treated with paliperidone ER during the extension phase of placebo-controlled trials 3.
- Paliperidone has a relatively low risk of pro-arrhythmic potential and little effect on plasma glucose, lipid, or insulin levels 3, 6.