Paliperidone
Generic Name: Paliperidone
Brand Names: Invega
Paliperidone is an atypical antipsychotic available in oral and long-acting injectable forms for schizophrenia and schizoaffective disorder.
Drug Class
Atypical Antipsychotic (Second-Generation Antipsychotic — Benzisoxazole Derivative)
Pregnancy
Based on human data, antipsychotics used during the third trimester can cause extrapyramidal symptoms and withdrawal in neonates. No adequate controlled studies. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Enroll in the National Pregnancy Registry for Atypical Antipsychotics if exposed during pregnancy.
Available Forms
Extended-release tablet (Invega): 1.5 mg, 3 mg, 6 mg, 9 mg, Injectable suspension — monthly (Invega Sustenna): 39 mg, 78 mg, 117 mg, 156 mg, 234 mg, Injectable suspension — every 3 months (Invega Trinza): 273 mg, 410 mg, 546 mg, 819 mg, Injectable suspension — every 6 months (Invega Hafyera): 1,092 mg, 1,560 mg
What It's Used For
Dosage Quick Reference
These are general dosage guidelines. Your doctor will determine the appropriate dose for your specific situation.
| Condition | Starting Dose | Maintenance Dose |
|---|---|---|
| Schizophrenia (oral) | 6 mg once daily in the morning | 3–12 mg once daily |
| Schizoaffective Disorder (oral) | 6 mg once daily in the morning | 6–12 mg once daily |
| Schizophrenia (monthly injection — Invega Sustenna) | 234 mg IM deltoid on day 1, then 156 mg IM deltoid on day 8 | 39–234 mg IM monthly (deltoid or gluteal) |
Side Effects
Common Side Effects:
- Extrapyramidal symptoms (akathisia, dystonia, parkinsonism)
- Somnolence
- Tachycardia
- Headache
- Weight gain
- Injection site reactions (LAI)
Serious Side Effects:
- Tardive dyskinesia
- Neuroleptic malignant syndrome
- QT prolongation
- Metabolic syndrome
- Hyperprolactinemia (galactorrhea, amenorrhea, gynecomastia)
- Orthostatic hypotension
Drug Interactions
- Strong CYP3A4/P-gp inducers (carbamazepine, rifampin, St. John's wort) — Decrease paliperidone levels and may reduce efficacy. Increase paliperidone dose if co-administered; reassess when inducer is discontinued.
- Antihypertensives — Paliperidone can cause orthostatic hypotension, especially during initial titration. Additive effects with blood pressure-lowering medications.
- QT-prolonging agents (amiodarone, moxifloxacin, class IA/III antiarrhythmics) — Paliperidone may prolong the QTc interval. Avoid co-administration with other QT-prolonging drugs when possible.
- Levodopa / dopamine agonists — Paliperidone, as a dopamine D2 antagonist, may counteract the effects of dopaminergic medications used for Parkinson disease. Avoid concurrent use.
- CNS depressants (alcohol, opioids, benzodiazepines) — Additive sedation and CNS depression. Use caution and monitor.
Additional Information
Paliperidone is an atypical antipsychotic medication used to treat schizophrenia and schizoaffective disorder. As the active metabolite of risperidone, it offers similar efficacy with a potentially different side effect profile and the convenience of long-acting injectable formulations.
Mechanism of Action
Paliperidone's antipsychotic effects are primarily mediated through:
- Dopamine D2 receptor antagonism: Core mechanism for treating positive symptoms
- Serotonin 5-HT2A receptor antagonism: Contributes to improved tolerability and efficacy for negative symptoms
Additional receptor activities include:
- Alpha-1 adrenergic antagonism (contributes to orthostatic hypotension)
- Histamine H1 antagonism (contributes to sedation and weight gain)
- No significant anticholinergic activity
Available Formulations
Oral Extended-Release (Invega):
- Tablets: 1.5 mg, 3 mg, 6 mg, 9 mg
- Uses OROS osmotic delivery system; do not crush, chew, or divide
Long-Acting Injectable (Monthly - Invega Sustenna):
- 39 mg, 78 mg, 117 mg, 156 mg, 234 mg prefilled syringes
Long-Acting Injectable (Every 3 Months - Invega Trinza):
- 273 mg, 410 mg, 546 mg, 819 mg prefilled syringes
- Requires stabilization on monthly injection first
Long-Acting Injectable (Every 6 Months - Invega Hafyera):
- 1092 mg, 1560 mg prefilled syringes
- Requires stabilization on monthly injection first
Medical Uses
FDA-Approved Indications:
- Schizophrenia in adults and adolescents (12-17 years, oral only)
- Schizoaffective disorder as monotherapy or adjunct to mood stabilizers/antidepressants
Long-acting injectables improve adherence and reduce relapse risk in patients with schizophrenia.
Dosing Guidelines
Oral (Schizophrenia):
- Adults: 6 mg once daily in the morning; range 3-12 mg daily
- Adolescents: 3 mg once daily; may increase to 6-12 mg daily
- Maximum: 12 mg daily (adults), 12 mg daily (adolescents with weight ≥51 kg)
Monthly Injectable (Invega Sustenna):
- Initiation: 234 mg IM deltoid day 1, then 156 mg IM deltoid day 8
- Maintenance: 39-234 mg monthly (deltoid or gluteal)
Schizoaffective Disorder:
- Similar dosing to schizophrenia
- May use as monotherapy or with mood stabilizers
Important Safety Information
Black Box Warnings:
- Increased mortality in elderly patients with dementia-related psychosis
- Not approved for dementia-related psychosis
Contraindications:
- Known hypersensitivity to paliperidone or risperidone
Warnings and Precautions:
- Tardive dyskinesia
- Neuroleptic malignant syndrome
- QT prolongation
- Hyperprolactinemia
- Metabolic changes (weight gain, hyperglycemia, dyslipidemia)
- Orthostatic hypotension
- Leukopenia/neutropenia
- Seizures
Drug Interactions
- QT-prolonging drugs: Avoid combination
- Dopamine agonists (levodopa): Antagonistic effects
- Strong CYP3A4/P-gp inducers (carbamazepine, rifampin): May decrease paliperidone levels
- Antihypertensives: Additive hypotensive effects
- CNS depressants: Additive sedation
Note: Unlike risperidone, paliperidone has minimal CYP2D6 metabolism.
Special Populations
- Renal Impairment:
- CrCl 50-79: Max 6 mg/day oral; adjust injectable accordingly
- CrCl 10-49: Max 3 mg/day oral; injectable not recommended
- CrCl <10: Not recommended
- Hepatic Impairment: No adjustment for mild to moderate; not studied in severe
- Pregnancy: May cause extrapyramidal symptoms in neonates
- Elderly: Start with lower doses; avoid in dementia-related psychosis
Frequently Asked Questions
Questions to Ask Your Doctor
Consider discussing these topics at your next appointment:
- ✓Is a long-acting injectable form a better option for me than daily oral medication?
- ✓How will we monitor my metabolic health (weight, blood sugar, cholesterol) on this medication?
- ✓What symptoms of tardive dyskinesia or EPS should I watch for?
- ✓Does paliperidone interact with any of my current medications?
- ✓What should I expect during the initial titration period?
Related Health Conditions
This medication is commonly used to treat or manage the following conditions:
Medical Disclaimer: This information is for educational purposes only and should not be considered medical advice. Always consult with your healthcare provider before starting, stopping, or changing any medication. Your doctor can provide personalized recommendations based on your specific health condition and medical history.
Related Medications
Other medications in the same category
Questions About This Medication?
Talk to your doctor or pharmacist about whether Paliperidone is right for you.
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