Aripiprazole Lauroxil: Uses, Side Effects, Dosage - Drugvu

ℹ️ Compiled from public regulatory records · Last regulator revision: January 28, 2025🚩 Report this page

Aripiprazole Lauroxil

Active ingredient

Sold as ARISTADA

US FDA

Drug class: -
Availability: Prescription only
Routes: Intramuscular
Markets covered: 1
Products on record: 1
FDA reports (12 mo): 230

Overview

Aripiprazole Lauroxil is an active pharmaceutical ingredient. The information below is compiled per regulator from the product labels on record, with direct links to the original documents.

Regulatory status by market

Market	Regulator	Products	Last revision
US United States	FDA	1	January 28, 2025

USUnited States· FDA

1 product

Uses

USOfficial regulatory label· revised January 28, 2025[1]

1 INDICATIONS AND USAGE ARISTADA is indicated for the treatment of schizophrenia in adults [see Clinical Studies ( 14 )]. ARISTADA is an atypical antipsychotic indicated for the treatment of schizophrenia in adults ( 1 ).

How to take

Sources & citations

[1]FDA DailyMed · 17a8d11b-73b0-48… · revised January 28, 2025 [PDF]
[2]OpenFDA adverse-event reports (US), 12 months ending June 4, 2026.

Information on this page is compiled from public regulatory records. Drugvu is not affiliated with any regulator or pharmaceutical manufacturer. This is not medical advice. Always consult a qualified healthcare professional.

1 ). 1 ).
There are two options for initiating treatment with ARISTADA:
Option #1: Administer one injection of 675 mg of ARISTADA INITIO ® and one 30 mg dose of oral aripiprazole in conjunction with the first ARISTADA injection. 1 ). 1 ). 1 ). 2 ). 4 ). 1 Recommended Dosage ARISTADA is only to be administered as an intramuscular injection by a healthcare professional.
For patients who have never taken aripiprazole, establish tolerability with oral aripiprazole prior to initiating treatment with ARISTADA. Due to the half-life of oral aripiprazole, it may take up to 2 weeks to fully assess tolerability.
Refer to the prescribing information of oral aripiprazole for the recommended dosage and administration of the oral formulation.
There are two ways to initiate treatment with ARISTADA:
Option #1: Administer one intramuscular injection of ARISTADA INITIO 675 mg (in either the deltoid or gluteal muscle) and one dose of oral aripiprazole 30 mg in conjunction with the first ARISTADA injection. The first ARISTADA injection may be administered on the same day as ARISTADA INITIO or up to 10 days thereafter.
See the ARISTADA INITIO prescribing information for additional information regarding administration of ARISTADA INITIO. Avoid injecting both ARISTADA INITIO and ARISTADA concomitantly into the same deltoid or gluteal muscle.
Option #2:
Administer 21 consecutive days of oral aripiprazole in conjunction with the first ARISTADA injection. Depending on individual patient's needs, treatment with ARISTADA can be initiated at a dose of 441 mg, 662 mg or 882 mg administered monthly, 882 mg administered every 6 weeks or 1064 mg administered every 2 months.
3 )].
Table 1:
ARISTADA Dosing Frequency and Site of Injection Dose Dosing Frequency Site of Intramuscular Injection 441 mg Monthly Deltoid or Gluteal 662 mg Monthly Gluteal 882 mg Monthly or every 6 weeks Gluteal 1064 mg Every 2 months Gluteal Use the following ARISTADA doses for patients who are stabilized on oral aripiprazole, as shown in Table 2 .
1 )]. Adjust the ARISTADA dose as needed. 3 )]. 2 Missed Doses When a dose of ARISTADA is missed, administer the next injection of ARISTADA as soon as possible. Depending on the time elapsed since the last ARISTADA injection, supplement the next ARISTADA injection as recommended in Table 3 below.
Table 3:
Recommendation for Concomitant Supplementation Following Missed Doses of ARISTADA Dose of Patient's Last ARISTADA Injection Length of Time Since Last Injection a The patient should supplement with the same dose of oral aripiprazole as when the patient began ARISTADA (see Table 2 ).
3 Early Dosing The recommended ARISTADA dosing interval is monthly for the 441 mg, 662 mg and 882 mg doses, every 6 weeks for the 882 mg dose, or every 2 months for the 1064 mg dose and should be maintained. In the event of early dosing, an ARISTADA injection should not be given earlier than 14 days after the previous injection.
4 Dose Adjustments for CYP450 Considerations Refer to the prescribing information for oral aripiprazole for recommendations regarding dosage adjustments due to drug interactions, for the first 21 days when the patient is taking 21 days of oral aripiprazole concomitantly with the first dose of ARISTADA.
Avoid initiating ARISTADA treatment with ARISTADA INITIO in patients requiring dose adjustments. Once stabilized on ARISTADA, refer to the dosing recommendations below for patients taking strong CYP2D6 inhibitors, strong CYP3A4 inhibitors, or strong CYP3A4 inducers: No dosage changes recommended for ARISTADA, if CYP450 modulators are added for less than 2 weeks.
Make dose changes to ARISTADA if CYP450 modulators are added for greater than 2 weeks (see Table 4 ).
Table 4:
ARISTADA Dose Adjustments with Concomitant CYP450 Modulator Use Concomitant Medicine Dose Change for ARISTADA a a For the 882 mg dose administered every 6 weeks and the 1064 mg administered every 2 months, the next lower strength should be 441 mg administered monthly.
Strong CYP3A4 Inhibitor Reduce the dose of ARISTADA to the next lower strength. No dosage adjustment is necessary in patients taking 441 mg ARISTADA, if tolerated.
For patients known to be poor metabolizers of CYP2D6 :
Reduce dose to 441 mg from 662 mg, 882 mg, or 1064 mg. No dosage adjustment is necessary in patients taking 441 mg ARISTADA, if tolerated. Strong CYP2D6 Inhibitor Reduce the dose of ARISTADA to the next lower strength. No dosage adjustment is necessary in patients taking 441 mg ARISTADA, if tolerated.
For patients known to be poor metabolizers of CYP2D6 :
No dose adjustment required. Both Strong CYP3A4 Inhibitor and Strong CYP2D6 Inhibitor Avoid use for patients at 662 mg, 882 mg, or 1064 mg dose. No dosage adjustment is necessary in patients taking 441 mg ARISTADA, if tolerated. CYP3A4 Inducers No dose adjustment for 662 mg, 882 mg, or 1064 mg dose; increase the 441 mg dose to 662 mg.
5 Important Administration Instructions The kit contains a syringe containing ARISTADA sterile aqueous extended-release injectable suspension and 2 or 3 safety needles depending on dose (a 2-inch 20 gauge needle with yellow needle hub, a 1 ½-inch 20 gauge needle with yellow needle hub, and a 1-inch 21 gauge needle with green needle hub (441 mg kit only)) for intramuscular injection.
All materials should be stored at room temperature. A | 5 mL syringe containing ARISTADA sterile aqueous extended-release injectable suspension B | 20 gauge needle, 2-inch with yellow needle hub C | 20 gauge needle, 1½-inch with yellow needle hub D | 21 gauge needle, 1-inch with green needle hub 1.
TAP and vigorously SHAKE the syringe. 1a. Tap the syringe at least 10 times to dislodge any material which may have settled. 1b. Shake the syringe vigorously for a minimum of 30 seconds to ensure a uniform suspension. If the syringe is not used within 15 minutes, shake again for 30 seconds.
2. SELECT the injection needle. 2a. Select injection site. 2b. Select needle length based on injection site. For patients with a larger amount of subcutaneous tissue overlaying the injection site muscle, use the longer of the needles provided.
1 )] 3. ATTACH the injection needle. Attach the appropriate needle securely with a clockwise twisting motion. Do NOT overtighten. Overtightening could lead to needle hub cracking. 4. PRIME the syringe to remove air. 4a. Bring the syringe into upright position and tap the syringe to bring air to the top.
4b. Depress the plunger rod to remove air until a few drops are released. It is normal to see small air bubbles remaining in the syringe. 5. Inject in a RAPID and CONTINUOUS manner. Product requires a RAPID injection. Do not hesitate. Administer the entire content intramuscularly.
Do not inject by any other route. 6. DISPOSE of the needle. Cover the needle by pressing the safety device. Dispose of used and unused items in a proper waste container. Figure Figure Figure Figure Figure Figure Figure Figure

Side effects & warnings

USOfficial regulatory label· Adverse reactions· revised January 28, 2025[1]

1 ). To report SUSPECTED ADVERSE REACTIONS, contact Alkermes, Inc. gov/medwatch . 1 Clinical Studies Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
ARISTADA Patient Exposure ARISTADA has been evaluated for safety in 1180 adult patients in clinical trials in schizophrenia. Commonly Observed Adverse Reactions The most common adverse reaction (incidence ≥5% and at least twice the rate of placebo in patients treated with ARISTADA) was akathisia.
Adverse Reactions Occurring at an Incidence of 2% or More in ARISTADA-Treated Patients Adverse reactions associated with the use of ARISTADA (incidence of 2% or greater, rounded to the nearest percent and ARISTADA incidence greater than placebo) that occurred are shown in Table 8 .
Table 8:
Adverse Reaction in 2% or More of ARISTADA-Treated Patients and That Occurred at Greater Incidence than in the Placebo-Treated Patients in the 12-Week, Placebo-Controlled, Fixed-Dose Schizophrenia Trial Adverse Reaction System Organ Class Preferred Term Placebo N=207 (%) Aripiprazole Lauroxil 441 mg N=207 (%) 882 mg N=208 (%) General disorders and administration site conditions Injection site pain 2 3 4 Investigations Increased weight 1 2 2 Increased blood creatine phosphokinase 0 2 1 Nervous system disorders Akathisia 4 11 11 Headache 3 3 5 Psychiatric disorders Insomnia 2 3 4 Restlessness 1 3 1 In an open label pharmacokinetic study, the adverse reactions associated with the use of 441 mg monthly, 882 mg every 6 weeks, and 1064 mg every 2 months were similar across the dose groups.
Injection Site Reactions Injection site reactions were reported by 4% of patients treated with 441 mg ARISTADA and 5% of patients treated with 882 mg ARISTADA compared to 2% of patients treated with placebo. Most of these were injection site pain (3%, 4% and 2% in the 441 mg ARISTADA, 882 mg ARISTADA and placebo groups, respectively) and most were associated with the first injection, and decreased with each subsequent injection to less than or equal to 1% for both doses of ARISTADA and placebo.
Other injection site reactions (induration, swelling and redness) occurred at less than 1%. In an open label pharmacokinetic study evaluating 441 mg monthly, 882 mg every 6 weeks, and 1064 mg every 2 months, injection site reactions were similar across the dose groups.
Extrapyramidal Symptoms In the 12-week schizophrenia efficacy study [see Clinical Studies ( 14 )] , for ARISTADA-treated patients, the incidence of other EPS-related events, excluding akathisia and restlessness, was 5% and 7% for patients on 441 mg and 882 mg, respectively, versus 4% for placebo-treated patient ( Table 9 ).
Table 9:
Incidence of EPS Compared to Placebo ARISTADA Adverse Reaction Term Placebo N=207 (%) 441 mg N=207 (%) 882 mg N=208 (%) Akathisia 4 11 11 Restlessness 1 3 1 Other EPS 4 5 7 Dystonia 1 2 2 Parkinsonism 3 3 4 Dystonia Symptoms of dystonia, prolonged abnormal contractions of muscle groups, may occur in susceptible individuals during the first few days of treatment.
Dystonic symptoms include: spasm of the neck muscles, sometimes progressing to tightness of the throat, swallowing difficulty, difficulty breathing, and/or protrusion of the tongue. While these symptoms can occur at low doses, they occur more frequently and with greater severity with high potency and at higher doses of first generation antipsychotic drugs.
An elevated risk of acute dystonia is observed in males and younger age groups. Other Adverse Reactions Observed in Clinical Studies The following listing does not include reactions: 1) already listed in previous tables or elsewhere in labeling, 2) for which a drug cause was remote, 3) which were so general as to be uninformative, 4) which were not considered to have significant clinical implications, or 5) which occurred at a rate equal to or less than placebo.
Cardiac – angina pectoris, tachycardia, palpitations Gastrointestinal disorders – constipation, dry mouth General disorders – asthenia Musculoskeletal – muscular weakness Nervous system disorders – dizziness Psychiatric disorders – anxiety, suicide Adverse Reactions Reported in Clinical Trials with Oral Aripiprazole The following is a list of additional adverse reactions that have been reported in clinical trials with oral aripiprazole and not reported above for ARISTADA.
2 Postmarketing Experience The following adverse reactions have been identified during post-approval use of oral aripiprazole. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or to establish a causal relationship to drug exposure: occurrences of allergic reaction (anaphylactic reaction, angioedema, laryngospasm, pruritus/urticaria, or oropharyngeal spasm), pathological gambling, hiccups, blood glucose fluctuation, oculogyric crisis, drug reaction with eosinophilia and systemic symptoms (DRESS), and fecal incontinence.

USOfficial regulatory label· Warnings and precautions· revised January 28, 2025[1]

2 ).
Potential for Dosing and Medication Errors :
Substitution and dispensing errors between ARISTADA and ARISTADA INITIO could occur. 3 ). 4 ). 5 ). 6 ). 7 ). 8 ).
Leukopenia, Neutropenia, and Agranulocytosis :
Perform complete blood counts in patients with a history of a clinically significant low white blood cell (WBC) count. 10 ). 11 ). 12 ). 1 Increased Mortality in Elderly Patients with Dementia-related Psychosis Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death.
7 times the risk of death in placebo-treated patients. 6% in the placebo group. , pneumonia) in nature. Observational studies suggest that, similar to atypical antipsychotic drugs, treatment with conventional antipsychotic drugs may increase mortality.
The extent to which the findings of increased mortality in observational studies may be attributed to the antipsychotic drug as opposed to some characteristic(s) of the patients is not clear. 2 )]. 2 Cerebrovascular Adverse Reactions, Including Stroke In placebo-controlled trials with risperidone, aripiprazole, and olanzapine in elderly patients with dementia, there was a higher incidence of cerebrovascular adverse reactions (cerebrovascular accidents and transient ischemic attacks) including fatalities compared to placebo-treated patients.
1 )]. 3 Potential for Dosing and Medication Errors Medication errors, including substitution and dispensing errors, between ARISTADA and ARISTADA INITIO could occur. 1 )] . 3 )]. 4 Neuroleptic Malignant Syndrome A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) may occur in association with antipsychotic drugs, including ARISTADA.
Clinical manifestations of NMS are hyperpyrexia, muscle rigidity, altered mental status, and evidence of autonomic instability (irregular pulse or blood pressure, tachycardia, diaphoresis, and cardiac dysrhythmia). Additional signs may include elevated creatine phosphokinase, myoglobinuria (rhabdomyolysis), and acute renal failure.
The diagnostic evaluation of patients with this syndrome is complicated. ) and untreated or inadequately treated extrapyramidal signs and symptoms (EPS). Other important considerations in the differential diagnosis include central anticholinergic toxicity, heat stroke, drug fever, and primary central nervous system pathology.

This is not medical advice. Consult a qualified healthcare professional.