Rexulti Dosage/Direction for Use

Posology: Schizophrenia (Adults and Pediatric Patients 13 to 17 Years): Adults: The recommended starting dose for brexpiprazole is 1 mg once daily on days 1 to 4.
The recommended target dose range is 2 mg to 4 mg once daily.
Based on the patient's clinical response and tolerability the brexpiprazole dose can be titrated to 2 mg once daily on day 5 through day 7 and then to 4 mg on day 8.
The maximum recommended daily dose is 4 mg.
Pediatric Patients 13 to 17 Years: The recommended starting dosage for brexpiprazole is 0.5 mg once daily on days 1 to 4.
The recommended target dose range is 2 mg to 4 mg once daily.
Based on the patient's clinical response and tolerability the brexpiprazole dose can be titrated to 1 mg once daily on day 5 through day 7, then to 2 mg on day 8.
Weekly dose increases can be made in 1 mg increments.
The maximum recommended daily dosage is 4 mg.
Switching from other antipsychotics to brexpiprazole: When switching from other antipsychotics to brexpiprazole gradual cross-titration should be considered, with gradual discontinuation of the previous treatment while brexpiprazole treatment is initiated.
Switching to other antipsychotics from brexpiprazole: When switching to other antipsychotics from brexpiprazole, no gradual cross-titration is needed, the new antipsychotic should be initiated in its lowest dose while brexpiprazole is discontinued. It should be considered that plasma concentration of brexpiprazole will decline gradually and will be completely washed out in 1 to 2 weeks.
Major Depressive Disorder (Adults): The recommended starting dose for brexpiprazole as adjunctive treatment is 0.5 mg or 1 mg once daily.
Titrate to 1 mg once daily, then up to the target dosage of 2 mg once daily. Dosage increases should occur at weekly intervals based on the patient's clinical response and tolerability.
The maximum recommended daily dosage is 3 mg.
Periodically reassess to determine the continued need and appropriate dosage for treatment.
Agitation Associated with Dementia Due to Alzheimer's Disease: The recommended starting REXULTI dosage for the treatment of agitation associated with dementia due to Alzheimer's disease is 0.5 mg taken once daily on Days 1 to 7. Increase the dosage on Days 8 through 14 to 1 mg once daily, and on Day 15 to 2 mg once daily. The recommended target dose is 2 mg once daily. The dosage can be increased to the maximum recommended daily dosage of 3 mg once daily after at least 14 days, based on clinical response and tolerability.
Special populations: Elderly: The safety and efficacy of brexpiprazole in the treatment of schizophrenia in patients aged 65 years and older have not been established (see Precautions and Pharmacology: Pharmacokinetics under Actions). It is not possible to advise on a minimum effective/safe dose in this population.
The total number of REXULTI-treated patients 65 years of age and older in the clinical studies for agitation associated with dementia due to Alzheimer's disease was 448 (86%) including 170 (33%) patients 65 to 74 years of age, 228 (44%) patients 75 to 84 years of age, and 50 (10%) patients 85 years of age and older (see Pharmacology: Pharmacokinetics under Actions).
In clinical studies of REXULTI for the treatment of agitation associated with dementia due to Alzheimer's disease did not include sufficient numbers of younger adult patients to determine if patients 65 years of age and older respond differently than younger adult patients.
Renal impairment: The maximum recommended dose in patients with moderate to severe impaired renal function is reduced to 3 mg once daily for patients with schizophrenia, and 2 mg once daily for patients with MDD or agitation associated with dementia due to Alzheimer's disease (see Pharmacology: Pharmacokinetics under Actions).
Hepatic impairment: The maximum recommended dose in patients with moderate to severe hepatic impairment (Child Pugh score ≥7) is reduced to 3 mg once daily for patients with schizophrenia, and 2 mg once daily for patients with MDD or agitation associated with dementia due to Alzheimer's disease (see Pharmacology: Pharmacokinetics under Actions).
CYP2D6 poor metabolisers: Dosing modifications to half the recommended doses is required for patients with known CYP2D6 poor metaboliser status. Further dosing modifications to a quarter of the recommended dose is required for known CYP2D6 poor metabolisers while taking strong or moderate CYP3A4 inhibitors (see Interactions and Pharmacology: Pharmacokinetics under Actions).
Dose adjustments due to interactions: Dose adjustments should be made in patients taking concomitant strong CYP3A4 inhibitors/inducers or strong CYP2D6 inhibitors. If the CYP3A4 inhibitor/inducers or CYP2D6 inhibitor is withdrawn, the dose may need to be returned to the original dose (see Interactions). In case of adverse reactions despite dose adjustments of REXULTI, the necessity of concomitant use of REXULTI and CYP2D6 or CYP3A4 inhibitor should be reassessed. (See Table 6.)

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Patients taking strong CYP3A4 inducers: If brexpiprazole is used concomitantly with strong CYP3A4 inducers (e.g. rifampicin), in a patient stabilised on brexpiprazole it is necessary to titrate the daily dose of brexpiprazole stepwise up to double the recommended dose over the course of 1 to 2 weeks. Thereafter, if according to clinical response, further dose adjustments are required, the dose may be increased up to a maximum of three times the recommended daily dose. Daily dose must not exceed 12 mg when brexpiprazole is used concomitantly with strong CYP3A4 inducers. Twice daily divided dosing of brexpiprazole is preferable as once daily dosing results in high peak to trough fluctuation (see Interactions).
CYP3A4 inducers exert their effect in a time-dependent manner, and may take at least 2 weeks to reach maximal effect after introduction. Conversely, on discontinuation, CYP3A4 induction may take at least 2 weeks to decline.
Pediatric population: Schizophrenia: Safety and effectiveness of REXULTI for treatment of schizophrenia have been established in pediatric patients 13 years of age and older. Use of REXULTI in this population is supported by evidence from adequate and well-controlled studies in adults with schizophrenia, pharmacokinetic data from adults and pediatric patients, and safety data in pediatric patients 13 to 17 years of age.
Major Depressive Disorder and agitation associated with dementia due to Alzheimer's disease: The safety and efficacy of brexpiprazole in children and adolescents aged less than 18 years have not been established. No data are available.
Method of administration: Oral use.
The film-coated tablets can be taken with or without food.