Aripiprazole lauroxil

ARISTADA is indicated for the treatment of schizophrenia in adults. ARISTADA is an atypical antipsychotic indicated for the treatment of schizophrenia in adults.

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 D 2 and serotonin 5-HT 1A receptors and antagonist activity at 5-HT 2A receptors.

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. Dosing regimen adjustments may be required for missed doses.

ARISTADA is contraindicated in patients with a known hypersensitivity reaction to aripiprazole. Hypersensitivity reactions have ranged from pruritus/urticaria to anaphylaxis. Known hypersensitivity to aripiprazole

Boxed warning (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. ARISTADA is not approved for the treatment of patients with dementia-related psychosis. Cerebrovascular Adverse Reactions in Elderly Patients with Dementia-Related Psychosis: Increased incidence of cerebrovascular adverse reactions (e.g., stroke, transient ischemia attack, including fatalities). Potential for Dosing and Medication Errors: Substitution and dispensing errors between ARISTADA and ARISTADA INITIO could occur. Do not substitute ARISTADA INITIO for ARISTADA. Neuroleptic Malignant Syndrome: Manage with immediate discontinuation and close monitoring. Tardive Dyskinesia: Discontinue if clinically appropriate.

The following are discussed in more details in other sections of the labeling: Increased Mortality in Elderly Patients with Dementia-related Psychosis Cerebrovascular Adverse Reactions, Including Stroke Neuroleptic Malignant Syndrome Tardive Dyskinesia Metabolic Changes Pathological Gambling and Other Compulsive Behaviors Orthostatic Hypotension Falls Leukopenia, Neutropenia, and Agranulocytosis Seizures Potential for Cognitive and Motor Impairment Body Temperature Regulation Dysphagia Most commonly observed adverse reaction with ARISTADA (incidence ≥5% and at least twice that for placebo) was akathisia.

Drugs Having Clinically Important Interactions with ARISTADA Table 10: Clinically Important Drug Interactions with ARISTADA Strong CYP3A4 Inhibitors and CYP2D6 Inhibitors Clinical Impact: The concomitant use of oral aripiprazole with strong CYP3A4 or CYP2D6 inhibitors increased the exposure of aripiprazole compared to the use of oral aripiprazole alone. Intervention: With concomitant use of ARISTADA with a strong CYP3A4 inhibitor or CYP2D6 inhibitor for more than 2 weeks, reduce the ARISTADA dose. Examples: itraconazole, clarithromycin, quinidine, fluoxetine, paroxetine Strong CYP3A4 Inducers Clinical Impact: The concomitant use of oral aripiprazole and carbamazepine decreased the exposure of aripiprazole compared to the use of oral aripiprazole alone. Intervention: With concomitant use of ARISTADA with a strong CYP3A4 inducer for more than 2 weeks consider increasing the ARISTADA dose.

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).