ARISTADA (aripiprazole lauroxil) Injection – Treatment for Schizophrenia in Adults

ARISTADA is a long-acting injectable atypical antipsychotic formulated as an extended-release suspension for intramuscular use. It is approved for the treatment of schizophrenia in adult patients, providing sustained delivery of aripiprazole to help manage symptoms over monthly to bi-monthly dosing intervals.

ARISTADA is indicated for the treatment of schizophrenia in adults. It is administered by intramuscular injection by a healthcare professional, with dosing tailored to individual needs and prior treatment with oral aripiprazole to establish tolerability.

aripiprazole lauroxil

ARISTADA contains aripiprazole lauroxil, a prodrug that is converted into aripiprazole in the body. Aripiprazole modulates dopamine and serotonin receptor activity in the brain, which is thought to help regulate neurotransmitter pathways involved in schizophrenia.

Administration and Initiation

• Administered only by healthcare professionals via intramuscular injection into the deltoid (441 mg dose) or gluteal muscles (all doses).
• Patients new to aripiprazole must first tolerate oral aripiprazole before starting ARISTADA; this assessment may take up to 2 weeks.
• Two initiation methods exist:
• Option 1: One injection of ARISTADA INITIO 675 mg plus one 30 mg oral aripiprazole dose concurrently with first ARISTADA injection; first ARISTADA dose given the same day or up to 10 days later.
• Option 2: Start oral aripiprazole daily for 21 days together with the first ARISTADA injection.

Dosing Regimens

Dose Selection According to Oral Aripiprazole

Missed Doses

When a dose is missed, the next injection should be given as soon as possible. Depending on time since last injection, oral aripiprazole supplementation or ARISTADA INITIO injection may be required before resuming ARISTADA, as per specified time intervals and patient's last dose.

Drug Interaction Dose Adjustments

• No adjustment if CYP450 modulators are used for less than 2 weeks.
• If CYP3A4 or CYP2D6 inhibitors (strong) are used for >2 weeks, dose reduction to the next lower strength is recommended, except for some CYP2D6 poor metabolizers where specific adjustments apply.
• Concurrent strong inhibitors of both enzymes should be avoided at higher doses.
• CYP3A4 inducers require increasing the 441 mg dose to 662 mg; no adjustments needed for higher doses.

Known hypersensitivity to aripiprazole, including allergic reactions ranging from itching or rash to anaphylaxis.

Increased Mortality in Elderly with Dementia-Related Psychosis

Patients with dementia-related psychosis treated with antipsychotics have an increased risk of death. ARISTADA is not approved for this population.

Cerebrovascular Adverse Reactions

Elderly patients with dementia-related psychosis may have higher rates of stroke and transient ischemic attacks, including fatalities.

Neuroleptic Malignant Syndrome (NMS)

May cause potentially fatal NMS characterized by high fever, muscle rigidity, autonomic instability, altered mental status; requires immediate drug discontinuation and supportive care.

Tardive Dyskinesia

May develop involuntary, potentially irreversible movements. Use the lowest effective dose and monitor closely.

Metabolic Changes

Monitor for hyperglycemia, lipid changes, and weight gain.

Compulsive Behaviors

Pathological gambling and other compulsive behaviors have been reported; consider dose modification or drug discontinuation.

Orthostatic Hypotension

Monitor blood pressure and heart rate; caution in patients with cardiovascular risk or prone to dehydration.

Hematologic Effects

Monitor white blood cell counts in patients with a history of low counts; consider stopping if significant declines occur without other causes.

Seizures

Use cautiously in patients with seizure history or conditions lowering seizure threshold.

Cognitive and Motor Impairment

May impair ability to operate machinery or drive; caution advised.

Serious Side Effects

• Neuroleptic malignant syndrome (fever, muscle rigidity, autonomic instability)
• Tardive dyskinesia (involuntary movements)
• Cerebrovascular events (stroke, transient ischemic attacks)
• Hypersensitivity reactions ranging from rash to anaphylaxis

Common Side Effects

Not fully detailed in the source text.

Concomitant use of strong CYP3A4 inhibitors or strong CYP2D6 inhibitors requires dose adjustments of ARISTADA. Avoid combined use of strong inhibitors of both enzymes at higher ARISTADA doses. Use caution and adjust dose if CYP3A4 inducers are used chronically.

Store ARISTADA components at room temperature. The pre-filled syringe and needles included in the kit should be maintained as directed until use.