Drug Guide
Paliperidone
Classification
Therapeutic: Antipsychotic, Mood Stabilizer
Pharmacological: Atypical Antipsychotic
FDA Approved Indications
- Schizophrenia in adults and adolescents (ages 12 and older)
- Schizoaffective disorder in adults
Mechanism of Action
Paliperidone is an atypical antipsychotic that primarily acts as an antagonist at dopamine D2 and serotonin 5-HT2A receptors, which helps to balance neurotransmitters in the brain and reduce psychotic symptoms.
Dosage and Administration
Adult: Starting dose is typically 6 mg once daily, titrated up to 12 mg as needed based on response and tolerability.
Pediatric: Approved for adolescents 12 and older; doses vary based on individual response.
Geriatric: Use with caution; start at lower doses due to increased sensitivity.
Renal Impairment: Reduce dose in patients with moderate to severe renal impairment.
Hepatic Impairment: No dose adjustment needed for mild to moderate hepatic impairment.
Pharmacokinetics
Absorption: Well absorbed orally, bioavailability approximately 100%.
Distribution: Begins within an hour of administration, widely distributed.
Metabolism: Minimal hepatic metabolism; primarily excreted unchanged in urine.
Excretion: Excreted mainly through urine, with some fecal elimination.
Half Life: Approximately 23 hours, allowing for once-daily dosing.
Contraindications
- Hypersensitivity to paliperidone or any components of the formulation.
Precautions
- Use cautiously in patients with cardiovascular disease, cerebrovascular disease, or a history of seizures.
- Risk of metabolic syndrome; monitor weight, glucose, and lipid levels.
- Evaluate for extrapyramidal symptoms and tardive dyskinesia.
Adverse Reactions - Common
- Akathisia (Occasional)
- Headache (Common)
- Sleep disturbance (Common)
- Dizziness (Common)
- Sedation (Common)
Adverse Reactions - Serious
- Neuroleptic Malignant Syndrome (Rare)
- Extrapyramidal Symptoms (Uncommon)
- QT prolongation (Uncommon)
- Hyperglycemia / Diabetes Mellitus (Less common)
- Leukopenia / Neutropenia (Rare)
Drug-Drug Interactions
- Other central nervous system depressants, medications prolonging QT interval, drugs affecting renal function.
Drug-Food Interactions
- High-fat meals may delay absorption.
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor mental status, risk of falls, metabolic parameters, cardiovascular status, weight, glucose, lipids, and signs of extrapyramidal symptoms.
Diagnoses:
- Risk for falls, related to dizziness or sedation.
- Impaired skin integrity, related to possible sedation or orthostatic hypotension.
Implementation: Administer once daily, monitor for side effects, educate patient about potential adverse effects, especially signs of metabolic changes and movement disorders.
Evaluation: Assess efficacy of symptom control and monitor for side effects regularly.
Patient/Family Teaching
- Take medication exactly as prescribed.
- Report any signs of movement issues, fever, or severe side effects promptly.
- Maintain regular follow-up appointments for metabolic monitoring.
- Advise against abrupt discontinuation.
Special Considerations
Black Box Warnings:
- Increased risk of mortality in elderly patients with dementia-related psychosis.
Genetic Factors: Potential genetic predisposition to tardive dyskinesia and metabolic adverse effects.
Lab Test Interference: May affect blood glucose and lipid measurements.
Overdose Management
Signs/Symptoms: Dizziness, tachycardia, sedation, extrapyramidal symptoms, hypotension, sedation.
Treatment: Supportive care, monitor cardiac function, and provide symptomatic treatment. Dialysis is not effective for drug removal.
Storage and Handling
Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F).
Stability: Stable under recommended storage conditions; check expiration date regularly.