Drug Guide
Paliperidone Palmitate
Classification
Therapeutic: Antipsychotic, Schizophrenia treatment
Pharmacological: Atypical antipsychotic, long-acting injectable
FDA Approved Indications
- Schizophrenia in adults
Mechanism of Action
Paliperidone is an antagonist at dopamine D2 and serotonin 5-HT2A receptors, which helps modulate neurotransmission and reduce psychotic symptoms.
Dosage and Administration
Adult: Initially, 234 mg on day 1 and 156 mg 7 days later, then maintenance doses of 39-234 mg once monthly for Invega Sustenna, every 3 months for Invega Trinza, and every 6 months for Invega Hafyera. Dose adjustments based on clinical response.
Pediatric: Not approved for pediatric use.
Geriatric: Use cautiously; adjust dosing as needed considering hepatic and renal function.
Renal Impairment: Use with caution; no dose adjustment necessary for mild to moderate impairment. Limited data available.
Hepatic Impairment: Use cautiously; no specific adjustment recommended.
Pharmacokinetics
Absorption: Long-acting injectable with sustained release.
Distribution: Extensively bound to plasma proteins (~74%).
Metabolism: Partially metabolized by CYP3A4 and CYP2D6.
Excretion: Primarily excreted in urine (approximately 59%), with the remainder in feces.
Half Life: Invega Hafyera: approximately 126 days (steady state after multiple doses). Invega Trinza: approximately 87 days.
Contraindications
- Hypersensitivity to paliperidone or related compounds.
Precautions
- History of cardiovascular disease, cerebrovascular disease, orthostatic hypotension, seizures, or conditions that could be exacerbated by dopamine blockade.
- Use cautiously in elderly patients with dementia-related psychosis due to increased mortality risk.
Adverse Reactions - Common
- Injection site pain (Common)
- Weight gain (Common)
- Akathisia (Common)
- Somnolence (Common)
Adverse Reactions - Serious
- Neuroleptic malignant syndrome (Rare)
- QT prolongation leading to arrhythmias (Rare)
- Orthostatic hypotension (Rare)
Drug-Drug Interactions
- CNS depressants
- Other QT prolonging agents, Antihypertensives, Drugs affecting CYP3A4
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor mental status, mood, and behavior. Check for signs of EPS or TD. Assess for orthostatic hypotension.
Diagnoses:
- Risk for falls
- Imbalanced nutrition: less than body requirements
Implementation: Administer deep IM injection; ensure patient is monitored post-injection for adverse effects. Educate patient on injection schedule.
Evaluation: Evaluate symptom control and monitor for adverse reactions.
Patient/Family Teaching
- Do not stop medication abruptly.
- Report any unusual movements, fever, or signs of infection.
- Be aware of ingestion side effects like weight gain and drowsiness.
- Attend scheduled injections and follow-up appointments.
Special Considerations
Black Box Warnings:
- Increased mortality in elderly patients with dementia-related psychosis.
Genetic Factors: No specific genetic contraindications but monitor for individual adverse reactions.
Lab Test Interference: Potential for increased prolactin levels, which can affect menstrual cycles and bone density.
Overdose Management
Signs/Symptoms: Sedation, hypotension, extrapyramidal symptoms, seizures.
Treatment: Supportive care, activated charcoal if early, and symptomatic treatment. No specific antidote.
Storage and Handling
Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F).
Stability: Stable for the duration specified on packaging when stored properly.