Drug Guide
Aripiprazole Lauroxil
Classification
Therapeutic: Antipsychotic, Long-acting injectable
Pharmacological: Atypical antipsychotic, D2 dopamine receptor partial agonist
FDA Approved Indications
- Schizophrenia in adults
- Maintenance treatment of schizophrenia
Mechanism of Action
Aripiprazole Lauroxil is a prodrug of aripiprazole, which acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors, and an antagonist at 5-HT2A receptors, modulating neurotransmission involved in psychosis.
Dosage and Administration
Adult: Initial dose of 441 mg administered as a single injection, adjustable based on response, then maintenance doses typically ranging from 441 mg monthly. For Aristada Initio, 675 mg intramuscularly once, followed by compatible doses.
Pediatric: Not approved for pediatric use.
Geriatric: Use with caution; no specific dose adjustments provided.
Renal Impairment: Adjust dosage based on clinical response; specific guidelines not established.
Hepatic Impairment: No specific adjustments recommended but monitor for adverse effects.
Pharmacokinetics
Absorption: Well absorbed after IM injection.
Distribution: Sparse protein binding (~99%).
Metabolism: Extensively metabolized by CYP3A4 and CYP2D6 enzymes to active metabolites.
Excretion: Primarily via feces (~54%) and urine (~24%).
Half Life: Approximately 54 days due to depot formulation.
Contraindications
- Hypersensitivity to aripiprazole or excipients.
Precautions
- Risk of suicidal thoughts, cardiovascular disease, neuroleptic malignant syndrome, impulse control problems, orthostatic hypotension, elderly patients with dementia-related psychosis are at increased risk of death.
Adverse Reactions - Common
- Injection site pain (Common)
- Akathisia (Common)
- Somnolence (Common)
- Dizziness (Common)
Adverse Reactions - Serious
- Neuroleptic malignant syndrome (Uncommon)
- Extrapyramidal symptoms (Uncommon)
- QT prolongation (Uncommon)
- Suicidal thoughts (Uncommon)
Drug-Drug Interactions
- CYP3A4 inhibitors or inducers (e.g., ketoconazole, rifampin) which can alter aripiprazole levels.
Drug-Food Interactions
- Avoid alcohol and CNS depressants.
Drug-Herb Interactions
N/ANursing Implications
Assessment: Monitor for effectiveness, adverse effects, injection site reactions, mental status, and metabolic parameters.
Diagnoses:
- Risk for falls
- Imbalanced nutrition: less than body requirements
- Risk for metabolic syndrome
Implementation: Administer IM injections as ordered, observe for adverse reactions, counsel about potential side effects.
Evaluation: Assess for symptom improvement, side effects, and adherence.
Patient/Family Teaching
- Instruct on importance of adherence to injection schedule.
- Report any abnormal movements, severe dizziness, or allergic reactions.
- Avoid alcohol and CNS depressants.
- Be aware of signs of worsening depression or suicidal thoughts.
Special Considerations
Black Box Warnings:
- Increased risk of death in elderly patients with dementia-related psychosis.
- Suicide-related events in young adults.
Genetic Factors: CYP2D6 metabolizer status may affect drug levels.
Lab Test Interference: May cause false-positive results for catecholamine metabolites.
Overdose Management
Signs/Symptoms: Dizziness, drowsiness, agitation, seizure, coma.
Treatment: Supportive care; no specific antidote. Consider activated charcoal if ingestion occurred recently; provide supportive measures and monitor vital signs; use benzodiazepines for agitation if needed.
Storage and Handling
Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F). Keep in original container until use.
Stability: Stable under recommended storage conditions until expiration date.