Generic
Paliperidone
8 brands available in the market
At a glance
Paliperidone is an atypical antipsychotic used for schizophrenia and schizoaffective disorder. It blocks dopamine D2 and serotonin 5HT2A receptors to improve mood, thoughts and behavior.
Description
Paliperidone is the major active metabolite of risperidone. It is a centrally active dopamine Type 2 (D2) antagonist 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.
Indications
- Schizophrenia (acute treatment and recurrence prevention)
- Schizoaffective disorder (monotherapy or with antidepressants/mood stabilizers)
Therapeutic class
Atypical Neuroleptic Drugs
Pharmacological class
Atypical Antipsychotic
Pharmacology
Paliperidone blocks dopamine D2 and serotonin 5HT2A receptors to control psychosis symptoms. It also blocks α1, α2 adrenergic and H1 histaminergic receptors.
Mechanism of action
Controls schizophrenia and schizoaffective disorder symptoms by blocking dopamine and serotonin receptors.
Dosage
Adult Dose (Oral):
- Schizophrenia: 6 mg/day (initial); increase by 3 mg/day (at intervals >5 days); max 12 mg/day
- Schizoaffective disorder: 6 mg/day (initial); 3-12 mg/day; max 12 mg/day
Pediatric Dose (>51 kg): 3 mg/day (initial); 3-12 mg/day; max 12 mg/day
Pediatric Dose (<51 kg): 3 mg/day (initial); 3-6 mg/day; max 6 mg/day
Administration
- Swallow tablet whole; do not chew, crush or break
- Take at the same time each day (morning)
- May be taken with or without food
Missed dose
If you miss a dose, take it as soon as you remember; skip if it's almost time for next dose; do not double the dose.
Side effects
Common Side Effects:
- Tachycardia
- Akathisia
- Somnolence
- Tremor
- Dystonia
- Cogwheel rigidity
- Anxiety
- Weight increased
- Dyspepsia
- Constipation
- Nasopharyngitis
- Nystagmus
Precautions & warnings
- Do not stop suddenly (may worsen symptoms)
- Caution in CV disease, QT prolongation, NMS, tardive dyskinesia, hyperglycemia, dyslipidemia, obesity, hyperprolactinemia, leukopenia, neutropenia, agranulocytosis, seizures
- Caution while driving
- Avoid alcohol
- Monitor blood glucose regularly
Contraindications
- Hypersensitivity
Drug interactions
- Increased risk of QT prolongation with Class IA/III antiarrhythmics
- Additive effects with drugs causing orthostatic hypotension
- May antagonize effects of levodopa and other dopaminergics
- Carbamazepine decreases plasma levels
- Valproate increases plasma levels
Food interactions
Alcohol may cause excessive drowsiness; avoid.
Use in pregnancy
Use in Pregnancy: Paliperidone may be unsafe during pregnancy; animal studies show evidence of fetal harm.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Paliperidone is probably unsafe during breastfeeding; may pass into breast milk and harm the baby.
Pediatric use
Safety not established in children under 12 years for schizophrenia; under 18 years for schizoaffective disorder.
Geriatric use
Elderly may require dose adjustment.
Renal / hepatic impairment
Renal Impairment: CrCl 50-79: 3 mg/day (initial); max 6 mg/day; CrCl 10-49: 1.5 mg/day (initial); max 3 mg/day; CrCl <10: Not recommended.
Hepatic Impairment: Caution in severe liver disease; no dose adjustment in mild-moderate.
Overdose effects
Limited information on overdose; no specific antidote; symptomatic supportive measures.
Storage conditions
Store in a cool and dry place, away from light; keep out of reach of children.
Chemical structure
Paliperidone