Timing of Rexulti (Brexpiprazole) Administration
Rexulti should be taken once daily at any time of day, with or without food, as the medication does not require specific timing for optimal efficacy.
Administration Guidelines
- Rexulti is administered once daily with no specific time-of-day requirement 1, 2, 3
- The medication can be taken with or without food, providing flexibility for patient convenience 1
- For schizophrenia, the recommended target dose is 2-4 mg/day taken once daily 2
- For major depressive disorder (as adjunctive therapy), the recommended dose is 2 mg once daily 2, 3
Dosing Titration Approach
- Brexpiprazole should be titrated to target doses rather than started at full therapeutic dose 2
- The gradual titration helps minimize adverse effects, particularly akathisia, which occurs in 5.5% of schizophrenia patients and 8.6% of MDD patients 2
Practical Considerations
- Unlike some medications that require morning or evening dosing, brexpiprazole's pharmacokinetic profile allows for flexible timing 1
- Patients should select a consistent time each day to maintain steady medication adherence
- The relatively low incidence of activating and sedating adverse effects means timing does not need to be adjusted based on side effect profile 1
Important Clinical Context
- Brexpiprazole displays lower intrinsic activity at D2 receptors compared to aripiprazole, which contributes to its lower propensity for activation-related adverse events 1, 4
- The drug has stronger antihistaminic activity than other dopamine partial agonists, which may provide mild sedative effects but does not necessitate bedtime dosing 4
- Weight gain appears modest in short-term studies, though more outliers with ≥7% body weight increase were noted in 52-week safety studies 2