General Information
Manufacturer: Otsuka America Pharmaceutical
Medical Name: Brexpiprazole
Purpose: Rexulti is an atypical antipsychotic medication used to treat several conditions.
Possible Side Effects
| Side Effect | MDD Trials (%) | Schizophrenia Trials (%) |
|---|---|---|
| Akathisia (inability to sit still) | 9% | 6% |
| Weight gain | 7% | 4% |
| Headache | 7% | >5% (exact % varies) |
| Somnolence (sleepiness/drowsiness) | 5% | >5% (exact % varies) |
| Insomnia (trouble sleeping) | Not specified (NS) | >5% (exact % varies) |
| Restlessness | 3% | NS |
| Fatigue | 3% | NS |
| Nasopharyngitis (stuffy/runny nose) | 4% | >5% (exact % varies) |
| Tremor | 4% | 3% |
| Dizziness | 3% | NS |
| Note: In long-term studies, weight gain was a more significant issue, with up to 30% of patients experiencing a 7% or greater increase in body weight. | ||
Serious but Less Common Side Effects
- Neuroleptic Malignant Syndrome (NMS): A rare but potentially fatal condition characterized by high fever, stiff muscles, confusion, and changes in pulse, blood pressure, and heart rate.
- Tardive Dyskinesia (TD): Uncontrolled, repetitive body movements (e.g., in the face, tongue, or limbs) that may not go away even after stopping the medication.
- Metabolic Changes: Increased blood sugar (hyperglycemia), diabetes, and high cholesterol/triglyceride levels are possible.
- Compulsive Urges: Unusual and uncontrollable urges, such as gambling, binge eating, or shopping.
- Orthostatic Hypotension: A drop in blood pressure when standing up quickly, which can lead to dizziness, lightheadedness, fainting, and falls.
- Increased Risk of Suicidal Thoughts and Behaviors: Especially in children, adolescents, and young adults (up to age 24) when used as an antidepressant.
- Increased Risk of Death in Elderly Dementia Patients: Rexulti is not approved for psychosis related to dementia (without agitation) due to an increased risk of stroke and death.
- Low White Blood Cell Count: Can increase the risk of infection.
- Seizures.
- Difficulty Swallowing.
Contraindications
- Rexulti (brexpiprazole) is contraindicated in patients with a known hypersensitivity to brexpiprazole or any of its components. Reactions can include rash, facial swelling, hives (urticaria), and a severe allergic reaction (anaphylaxis).
- Furthermore, there are several serious safety concerns and conditions where Rexulti is generally not recommended or should be used with extreme caution due to increased risks:
- Boxed Warnings
- Elderly patients with dementia-related psychosis: Rexulti is not approved for treating psychosis in elderly patients with dementia due to an increased risk of death (often from cardiovascular or infectious causes, such as pneumonia) and stroke.
Preconditions and Warnings
- Cardiovascular and Cerebrovascular Disease: Use with caution in patients with a history of heart attack (myocardial infarction), ischemic heart disease, heart failure, or stroke, as the drug can cause orthostatic hypotension (a sudden drop in blood pressure upon standing).
- Metabolic Abnormalities: Rexulti can cause metabolic changes, including high blood sugar (hyperglycemia) and diabetes, increased fat levels (cholesterol and triglycerides) in the blood, and weight gain. Patients with pre-existing diabetes or high cholesterol require close monitoring.
- Blood Disorders: Patients with a history of a low white blood cell count (leukopenia or neutropenia) should have their blood counts monitored. Rexulti should be discontinued if a clinically significant decline in white blood cells occurs.
- Seizures: Rexulti should be used with caution in patients with a history of seizures or with conditions that may lower the seizure threshold.
- Liver or Kidney Impairment: Dosage adjustments are recommended for patients with moderate to severe liver or kidney problems.
- Difficulty Swallowing (Dysphagia): The medication has been associated with esophageal dysmotility and aspiration, so caution is advised for patients at risk for aspiration pneumonia.
- Compulsive Behaviors: Rexulti has been linked to new or increased intense, uncontrollable urges, such as pathological gambling, sexual urges, or binge eating. Dose reduction or discontinuation may be necessary if these occur.
- Pregnancy and Breastfeeding: Rexulti is not recommended during the third trimester of pregnancy due to the risk of abnormal muscle movements or withdrawal symptoms in the newborn. It is unknown if it passes into breast milk.