Home Drug Guide Pimavanserin Tartrate

Drug Guide

Generic Name

Pimavanserin Tartrate

Brand Names Nuplazid

Classification

Therapeutic: Antipsychotic, central nervous system

Pharmacological: Selective 5-HT2A receptor inverse agonist

FDA Approved Indications

Parkinson's disease psychosis

Mechanism of Action

Pimavanserin selectively targets 5-HT2A receptors as an inverse agonist, modulating serotonin activity implicated in psychosis without affecting dopaminergic receptors, thereby reducing hallucinations and delusions in Parkinson's disease psychosis.

Dosage and Administration

Adult: 34 mg once daily, with or without food.

Pediatric: Not approved for pediatric use.

Geriatric: Similar dosing as adults, but caution in elderly with hepatic impairment.

Renal Impairment: Use caution; no specific dosage adjustments established.

Hepatic Impairment: No specific recommendations, but monitor closely due to hepatic metabolism.

Pharmacokinetics

Absorption: Rapid absorption, peak plasma concentration in about 2 hours.

Distribution: Widely distributed; high plasma protein binding.

Metabolism: Metabolized primarily via CYP3A4; minimal CYP2D6 involvement.

Excretion: Excreted mainly in feces; minimal urinary excretion.

Half Life: Approximately 57 hours, allowing for once-daily dosing.

Contraindications

Hypersensitivity to pimavanserin or any component of the formulation.

Precautions

Use with caution in patients with QT prolongation, history of seizures, or those taking other QT-prolonging drugs. Monitor for falls and cognitive impairment, especially in elderly.

Adverse Reactions - Common

∑Headache (Common)
Confusion (Common)
Peripheral edema (Common)
Nausea (Common)

Adverse Reactions - Serious

QT prolongation, resulting in risk of torsades de pointes (Serious, requires monitoring)
Falls, leading to injury (Serious)
Psychosis or worsening of symptoms (Serious)

Drug-Drug Interactions

CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase pimavanserin levels.
CYP3A4 inducers (e.g., carbamazepine, rifampin) may decrease levels.

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor patient's mental status, for hallucinations, delusions, and behavioral changes. ECG monitoring for QT interval if indicated.

Diagnoses:

Risk for falls due to sedation or hypotension.
Risk for electrolyte imbalances affecting QT interval.

Implementation: Administer as prescribed. Monitor for adverse reactions, especially QT prolongation.

Evaluation: Assess for improvement in psychosis symptoms and monitor for adverse effects.

Patient/Family Teaching

Do not operate heavy machinery until accustomed to effects.
Report any side effects such as prolonged QT interval, fainting, or worsening hallucinations.
Follow prescribed dosing schedule.
Avoid abrupt discontinuation.

Special Considerations

Black Box Warnings:

QT prolongation and potential for arrhythmias.
Use with caution in elderly patients due to increased risk of death (generally included in antipsychotics).

Genetic Factors: CYP3A4 polymorphisms may affect drug levels.

Lab Test Interference: None known.

Overdose Management

Signs/Symptoms: Dizziness, hypotension, sleepiness, seizures, or prolonged QT interval.

Treatment: Supportive care, ECG monitoring, and management of symptoms. Activated charcoal if ingestion was recent. No specific antidote.

Storage and Handling

Storage: Store at room temperature between 20°C to 25°C (68°F to 77°F).

Stability: Stable until the expiration date on the package.