Generic Name

Aripiprazole

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Classification

FDA Approved Indications

• Schizophrenia in adults and adolescents
• Bipolar I disorder in adults and pediatric patients aged 10 and older
• Major depressive disorder (adjunctive)
• Irritability associated with autism spectrum disorder in children aged 6 and older
• Tourettes disorder (short-term use)

Mechanism of Action

Aripiprazole acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and as an antagonist at serotonin 5-HT2A receptors. This modulation stabilizes neurotransmitter activity related to psychosis and mood disorders.

Dosage and Administration

Adult: Dosage varies by condition. For schizophrenia, typically starting at 10-15 mg once daily, titrated as needed. For bipolar disorder, usual starting dose is 15 mg daily.

Pediatric: Schizophrenia: 10-30 mg once daily; Bipolar disorder: 10-30 mg once daily, based on the specific indication and age.

Geriatric: Usually starting at the lower end of the dosing range, with careful monitoring.

Renal Impairment: Use with caution; dose adjustments may be necessary.

Hepatic Impairment: Start at lower doses; monitor closely.

Pharmacokinetics

Absorption: Well absorbed orally, with peak plasma concentrations within 3-5 hours.

Distribution: Highly protein bound (~99%), volume of distribution approximately 12 L/kg.

Metabolism: Extensively metabolized in the liver via CYP2D6 and CYP3A4 enzymes.

Excretion: Primarily excreted in feces (about 60%) and urine (about 25%).

Half Life: Approximately 75 hours (range 47-136 hours).

Contraindications

• None specific, but use cautiously in patients with hypersensitivity.

Precautions

• Use with caution in elderly patients with dementia-related psychosis due to increased risk of mortality.
• Monitor for metabolic side effects, including weight gain, hyperglycemia, and dyslipidemia.
• Assess for suicidality, especially in pediatric and young adult patients.

Adverse Reactions - Common

• Akathisia (frequent)
• Weight gain (common)
• Insomnia (common)
• Nausea (common)

Adverse Reactions - Serious

• Extrapyramidal symptoms (uncommon)
• Neuroleptic malignant syndrome (rare)
• QT prolongation (rare)
• Seizures (rare)

Drug-Drug Interactions

• CYP3A4 inhibitors or inducers (e.g., ketoconazole, rifampin) may alter aripiprazole levels.
• Other CNS depressants may enhance sedative effects.

Drug-Food Interactions

• Avoid grapefruit juice as it may increase plasma concentrations.

Drug-Herb Interactions

• St. John’s Wort may reduce aripiprazole levels.

Nursing Implications

Patient/Family Teaching

• Take medication exactly as prescribed.
• Report any concerning side effects such as movement changes or severe sedation.
• Maintain regular follow-up appointments for monitoring.
• Inform about potential metabolic side effects and lifestyle modifications needed.

Special Considerations

Black Box Warnings:

• Increased mortality in elderly patients with dementia-related psychosis.
• Suicidality risk in children, adolescents, and young adults.

Genetic Factors: CYP2D6 poor metabolizers may have higher plasma levels; consider dose adjustment.

Lab Test Interference: May affect blood glucose and lipid tests.

Overdose Management

Signs/Symptoms: Drowsiness, dizziness, agitation, tachycardia, vomiting, hallucinations, seizures.

Treatment: Supportive care, activated charcoal if ingestion is recent, and symptomatic treatment. No specific antidote.

Storage and Handling

Storage: Store at room temperature, 20-25°C (68-77°F). Keep container tightly closed.

Stability: Stable under recommended storage conditions for the duration of the labeled shelf life.