Nurses Compass
Drug Guide
Brexpiprazole
Classification
Therapeutic: Antipsychotic
Pharmacological: Serotonin-Dopamine Activity Modulator
FDA Approved Indications
- Schizophrenia in adults
- Major depressive disorder (adjunctive treatment)
Mechanism of Action
Brexpiprazole is a partial agonist at serotonin 5-HT1A and dopamine D2 receptors and an antagonist at serotonin 5-HT2A receptors. Its activity modulates neurotransmission, which helps in alleviating symptoms of schizophrenia and depression.
Dosage and Administration
Adult: For schizophrenia: 1 mg once daily, may be increased to 2-4 mg/day based on response. For adjunctive treatment of depression: 0.5-1 mg/day, may titrate up to 3 mg/day.
Pediatric: Not indicated for pediatric use.
Geriatric: Starting dose typically lower (e.g., 0.5 mg), with careful titration.
Renal Impairment: Use with caution; no specific dose adjustment established.
Hepatic Impairment: Use with caution; lower initial doses recommended.
Pharmacokinetics
Absorption: Well-absorbed orally with approximately 95% bioavailability.
Distribution: Highly protein-bound (~99%).
Metabolism: Extensively metabolized in the liver primarily via CYP3A4 and CYP2D6 enzymes.
Excretion: Eliminated mainly via feces (~73%) and urine (~23%).
Half Life: Approximately 91 hours (range 75-112 hours).
Contraindications
- Hypersensitivity to brexpiprazole or any component of the formulation.
Precautions
- Risk of metabolic syndrome, including weight gain, hyperglycemia, and lipid abnormalities.
- Potential for increased mortality in elderly patients with dementia-related psychosis.
- Monitor for suicidal thoughts or behaviors, especially in early treatment.
Adverse Reactions - Common
- Akathisia (Common)
- Headache (Common)
- Somnolence (Common)
- Extrapyramidal symptoms (Common)
Adverse Reactions - Serious
- Suicidal thoughts and behaviors (Serious)
- Neuroleptic malignant syndrome (Rare)
- Orthostatic hypotension (Rare)
- Hyperglycemia/diabetes (Serious)
Drug-Drug Interactions
- CYP3A4 inhibitors or inducers (affect brexpiprazole levels)
- Other CNS depressants (risk of sedation)
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor for improvements in psychotic symptoms, monitor metabolic parameters, assess for side effects.
Diagnoses:
- Risk for weight gain related to metabolic side effects
- Risk for extrapyramidal symptoms
- Risk for falls due to orthostatic hypotension
Implementation: Administer once daily, preferably at the same time each day. Monitor metabolic parameters regularly.
Evaluation: Assess symptom control, weight, glucose levels, lipid profile, and side effects periodically.
Patient/Family Teaching
- Take medication exactly as prescribed and do not discontinue abruptly.
- Report any signs of side effects such as uncontrollable movements, fever, or unusual thoughts.
- Maintain a healthy diet and exercise routine to help manage weight and metabolic side effects.
- Avoid alcohol and CNS depressants unless approved by healthcare provider.
Special Considerations
Black Box Warnings:
- Increased mortality in elderly patients with dementia-related psychosis.
Genetic Factors: Consider pharmacogenetic testing for CYP2D6 or CYP3A4 enzyme variants if inconsistency in response or side effects.
Lab Test Interference: May alter blood glucose, lipid levels, and weight.
Overdose Management
Signs/Symptoms: Drowsiness, sedation, agitation, tachycardia, hypotension, seizures.
Treatment: Supportive care, gastric lavage, activated charcoal. No specific antidote available.
Storage and Handling
Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F), away from moisture and light.
Stability: Stable for at least 24 months when stored properly.