Mechanism of Action: although the mechanism of action of brexpiprazole in the treatment of MDD and schizophrenia is unclear, the efficacy of brexpiprazole may be attributed to partial agonist activity at serotonin 1A and dopamine D2 receptors, and antagonist activity at serotonin 2A receptors. –DrugBank
Indications: brexpiprazole is indicated as adjunctive therapy to antidepressants for the treatment of major depressive disorder in adults. It is also indicated for the treatment of schizophrenia in patients 13 years of age and older. -DrugBank
Interactions: There are 536 drugs known to interact with Rexulti (brexpiprazole), along with 14 disease interactions, and 4 alcohol/food interactions. Of the total drug interactions, 106 are major, 427 are moderate, and 3 are minor. –Drugs.com
Food Interactions
- Avoid St. John’s Wort. This herb induces the CYP3A metabolism of brexpiprazole and may reduce its serum concentration. The dose of Brexpiprazole should be doubled if administered with St. John’s wort.
- Drink plenty of fluids.
- Take with or without food.
-Drug Bank
Dosing Forms:
Usual Adult Dose for Schizophrenia:
- Initial dose: 1 mg orally once a day on Days 1 through 4
- Titration regimen: Based on clinical response and tolerability, titrate to 2 mg once a day on Days 5 to 7, then to 4 mg once a day on Day 8.
- Maintenance dose: 2 to 4 mg orally once a day
- Maximum dose: 4 mg/day
Usual Adult Dose for Depression:
- Initial dose: 0.5 mg to 1 mg orally once a day
- Titration regimen: Based on clinical response and tolerability, dose increases should be done at weekly intervals; titrate to 1 mg once a day, then up 2 mg once a day.
- Maintenance dose: 2 mg orally once a day
- Maximum dose: 3 mg/day
Comment: Healthcare providers should periodically reassess the need for maintenance treatment.
Pros
- Only need to take the medication once a day
- Less likely to cause weight gain, high cholesterol, or high blood sugar compared with other similar medications
- Less likely to cause movement side effects compared to some other antipsychotics
Cons
- Can be expensive because it’s only available as a brand-name medication (which is why I have yet to prescribe it)
- Not recommended for use in pregnancy
- Your healthcare provider might need to adjust your dose several times before you find one that works best for you
Side-Effects:
- Common side effects: Fidgeting (9%), Weight gain (7%), Headache (7%), Sleepiness (5%), Tremor (4%), Common cold (4%), Larger appetite (3%), Fatigue (3%), Dizziness (3%), Restlessness (3%), Anxiety (3%)
Heartburn (3%), Diarrhea (3%), Constipation (2%) - Other side effects: Blurry vision, Nausea, Dry mouth, Stomach pain, Passing Gas, Urinary tract infection, Muscle pain, Strange dreams, Difficulty sleeping, Excessive sweating
–Good RX
Additional Information
Official Medication Website: Rexulti (Brexpiprazole)
- Brexpiprazole (Rexulti) – Uses, Dosing, Side Effects –Drug Talk (YouTube Video)
- Treating major depressive disorder after limited response to an initial agent –MD Edge (above graphic)
