Aripiprazole lauroxil

What is Aripiprazole lauroxil?

• Aripiprazole lauroxil (ARISTADA) is an atypical antipsychotic used to treat adults with schizophrenia.

What are the uses of this medicine?

• This medicine is used to treat schizophrenia in adults.

How does this medicine work?

• Aripiprazole lauroxil is a prodrug of aripiprazole.
• Following intramuscular injection, aripiprazole lauroxil is likely converted by enzyme-mediated hydrolysis to N-hydroxymethyl aripiprazole, which is then hydrolyzed to aripiprazole.
• The mechanism of action of aripiprazole in schizophrenia is unknown.
• However, efficacy could be mediated through a combination of partial agonist activity at dopamine D2 and serotonin 5-HT1A receptors and antagonist activity at 5-HT2A receptors.

Who Should Not Use this medicine ?

This medicine caanot be used in patients:

• with a known hypersensitivity reaction to aripiprazole.

What drug interactions can this medicine cause?

• With concomitant use of ARISTADA with a strong CYP3A4 inhibitor(eg: itraconazole, clarithromycin, quinidine, fluoxetine, paroxetine) or CYP2D6 inhibitor for more than 2 weeks, reduce the ARISTADA dose.
• With concomitant use of ARISTADA with a strong CYP3A4 inducer (eg: carbamazepine, rifampin) for more than 2 weeks consider increasing the ARISTADA dose.
• Due to its alpha adrenergic antagonism, aripiprazole has the potential to enhance the effect of certain antihypertensive agents (carvedilol, lisinopril, prazosin).
• The intensity of sedation was greater with the combination of oral aripiprazole and lorazepam as compared to that observed with aripiprazole alone. The orthostatic hypotension observed was greater with the combination as compared to that observed with lorazepam alone. Monitor sedation and blood pressure. Adjust dose accordingly.

Is this medicine FDA approved?

• It was approved for use in the United States in 2015.

How should this medicine be used?

Recommended Dosage:

• Administer ARISTADA by intramuscular injection in the deltoid (441 mg dose only) or gluteal (441 mg, 662 mg, 882 mg or 1064 mg) muscle by a healthcare professional.
• For patients naïve to aripiprazole, establish tolerability with oral aripiprazole prior to initiating treatment with ARISTADA

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.
• Option -2: Administer 21 consecutive days of oral aripiprazole in conjunction with the first ARISTADA injection.

• ARISTADA can be initiated at a dose of 441 mg, 662 mg or 882 mg administered monthly, 882 mg dose every 6 weeks, or 1064 mg dose every 2 months.
• Dose adjustments are required for 1) known CYP2D6 poor metabolizers and 2) for patients taking CYP3A4 inhibitors, CYP2D6 inhibitors, or CYP3A4 inducers for more than 2 weeks.

Administration

• Follow your ARISTADA treatment schedule exactly as your healthcare provider tells you to.
• Each ARISTADA is an injection given by your healthcare provider into the muscle (intramuscular) of your arm or buttock.

There are 2 ways to start treatment with ARISTADA:

• Option 1: You will receive 1 dose of ARISTADA INITIO in combination with a single dose of oral aripiprazole. You may also receive your first injection of ARISTADA on the same day you receive ARISTADA INITIO or up to 10 days after you receive ARISTADA INITIO.
• Option 2: After your first injection of ARISTADA, you will take oral aripiprazole for 21 days in a row (consecutive).
• You should not miss a dose of ARISTADA. If you miss a dose for some reason, call your healthcare provider right away to discuss what you should do next.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Extended-release injectable suspension: 441 mg, 662 mg, 882 mg or 1064 mg single-dose pre-filled syringe

This medicine is available in fallowing brand namesː

• ARISTADA

What side effects can this medication cause?

The most common side effects of this medicine include:

• restlessness or feeling like you need to move (akathisia)

ARISTADA may cause serious side effects, including:

• Increased risk of death in elderly people with dementia-related psychosis
• Cerebrovascular problems (including stroke) in elderly people with dementia-related psychosis that can lead to death.
• Neuroleptic malignant syndrome (NMS), a serious condition that can lead to death
• Uncontrolled body movements (tardive dyskinesia)
• Problems with your metabolism

What special precautions should I follow?

• Do not drive a car, operate hazardous machinery, or do other dangerous activities until you know how ARISTADA affects you. ARISTADA may affect your judgment, thinking or motor skills.
• Avoid becoming too hot or dehydrated while you receive ARISTADA.
• Do not exercise too much.
• In hot weather, stay inside in a cool place if possible.
• Stay out of the sun.
• Do not wear too much clothing or heavy clothing.
• Drink plenty of water.
• Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. 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). ARISTADA is not approved for the treatment of patients with dementia-related psychosis.
• Substitution and dispensing errors between ARISTADA and ARISTADA INITIO could occur. Do not substitute ARISTADA INITIO for ARISTADA.
• A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) may occur in association with antipsychotic drugs, including ARISTADA. Manage with immediate discontinuation and close monitoring.
• Tardive Dyskinesia, syndrome of potentially irreversible, involuntary, dyskinetic movements may develop in patients treated with antipsychotic drugs. Discontinue if clinically appropriate.
• Atypical antipsychotic drugs have been associated with metabolic changes that include hyperglycemia/diabetes mellitus, dyslipidemia, and weight gain. Monitor for hyperglycemia, dyslipidemia, and weight gain.
• Post-marketing case reports suggest that patients can experience intense urges, particularly for gambling, and the inability to control these urges while taking aripiprazole. Consider dose reduction or stopping the medication if a patient develops such urges.
• Aripiprazole may cause orthostatic hypotension. Monitor heart rate and blood pressure and warn patients with known cardiovascular or cerebrovascular disease, and risk of dehydration or syncope.
• Events of leukopenia and neutropenia have been reported temporally related to antipsychotic agents. Agranulocytosis has also been reported. Perform complete blood counts in patients with a history of a clinically significant low white blood cell (WBC) count. Consider discontinuation if clinically significant decline in WBC in the absence of other causative factors.
• Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold.

What to do in case of emergency/overdose?

• Sympotms of overdosage with oral aripiprazole overdosage (alone or in combination with other substances) include vomiting, somnolence, and tremor.
• Other clinically important signs and symptoms observed in one or more patients with aripiprazole overdoses (alone or with other substances) include acidosis, aggression, aspartate aminotransferase increased, atrial fibrillation, bradycardia, coma, confusional state, convulsion, blood creatine phosphokinase increased, depressed level of consciousness, hypertension, hypokalemia, hypotension, lethargy, loss of consciousness, QRS complex prolonged, QT prolonged, pneumonia aspiration, respiratory arrest, status epilepticus, and tachycardia.

Management of Overdosage

• In case of overdosage, call the Poison control center immediately at 1-800-222-1222.

Can this medicine be used in pregnancy?

• Limited published data on aripiprazole use in pregnant women are not sufficient to inform any drug-associated risks for birth defects or miscarriage.
• There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ARISTADA during pregnancy. For more information, contact the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit

http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/.

Can this medicine be used in children?

• Safety and effectiveness of ARISTADA in patients <18 years of age have not been evaluated.

What are the active and inactive ingredients in this medicine?

• Active ingredient: aripiprazole lauroxil
• Inactive ingredients: sorbitan monolaurate, polysorbate 20, sodium chloride, sodium phosphate dibasic anhydrous, sodium phosphate monobasic dihydrate and water for injection

Who manufactures and distributes this medicine?

• Manufactured and marketed by: Alkermes, Inc., 852 Winter Street, Waltham

What should I know about storage and disposal of this medication?

• Store at room temperature 20°C to 25°C (68°F to 77°F) with excursions permitted between 15°C and 30°C (between 59°F and 86°F).

• Dailymed label info on Aripiprazole lauroxil
• FDA Aripiprazole lauroxil

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