Description: Second Generation (Atypical) Antipsychotic
“ALERT: US Boxed Warning
Increased mortality in elderly patients with dementia-related psychosis:
Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Brexpiprazole is not approved for the treatment of patients with dementia-related psychosis.
Suicidal thoughts and behaviours:
Antidepressants increased the risk of suicidal thoughts and behaviour in patients aged 24 years and younger in short-term studies. Monitor closely for clinical worsening and for the emergence of suicidal thoughts and behaviours. The safety and efficacy of brexpiprazole have not been established in pediatric patients.”
CSA NA – FDA Approved – REMS (N) – Can Ship
How Does It Work
Brexpiprazole exhibits partial agonist activity for 5-HT1A and D2 receptors and antagonist activity for 5-HT2A receptors.
Indications For Use
Brexpiprazole, Rexulti is officially indicated as an adjunct therapy for major depressive disorder and for the treatment of schizophrenia. It is also sometimes prescribed off-label for agitation, aggression, and psychosis associated with severe dementia. (maybe used for other conditions not listed)
Before starting Brexpiprazole, Rexulti makes sure your physician is aware of any allergies or medications you currently take if you have cardiovascular disease, dementia, a history of seizures or are pregnant or breastfeeding. Brexpiprazole use has rarely been associated with severe side effects such as blood dyscrasias, cerebrovascular effects, CNS depression, dyslipidemia, esophageal dysmotility, increased risk of falls, impulse control disorders, neuroleptic malignant syndrome, orthostatic hypotension, suicidal ideation, weight gain, and temperature regulation issues.
This medication also requires regular bloodwork and follow up with your physician to monitor for adverse reactions
Major depressive disorder (adjunct to antidepressants): Oral: Initial: 0.5 mg or 1 mg once daily; titrate at weekly intervals based on response and tolerability to 1 mg once daily (if the initial dose is 0.5 mg), followed by 2 mg once daily; maximum daily dose: 3 mg.
Schizophrenia: Oral: Initial: 1 mg once daily for 4 days, titrate based on response and tolerability to 2 mg once daily for 3 days, followed by 4 mg on day 8; target dose: 2 to 4 mg/day; maximum daily dose: 4 mg.
Pharmacist Tips On Using
How to Take: Follow instructions provided by physician/pharmacy label, take consistently at same times each day unless otherwise directed, store at room temperature
You Need to Avoid: Operating heavy machinery or driving at least until you know how the medication affects you. Do not stop this medication suddenly, make sure your physician is aware and can create a tapering schedule so you can come off slowly and prevent any withdrawal symptoms. This medication has many drug interactions so ask your pharmacist before starting any over the counter medications or supplements.
Endocrine & metabolic: Increased serum triglycerides (<500 mg/dL: 8% to 13%; ≥500 mg/dL: <1%), weight gain (3% to 11%)
Nervous system: Akathisia (4% to 14%; dose related)
Note- this is not a complete list of side effects, only common ones
Frequently Asked Questions
- Why would my doctor give me an antipsychotic? Does this mean I am psychotic?
This medication can be used for many conditions outside of its original classification. It commonly is also used for nonpsychotic mood disorders, but this class of medication was given its name back when we knew a lot less about their capabilities.
- This medication has a lot of scary side effects, is it safe?
All medications have side effects however this medication works on a lot of different neurotransmitter receptors in the brain which can lead to a variety of intentional and unintentional effects. These are mostly dosage dependant and in lower doses the risk is minimal. In all cases, regular lab work will allow your physician to see if your blood sugar, cholesterol etc. start to move in the wrong direction so action can be taken before they become a problem.
- What are extrapyramidal reactions?
Blocking dopamine in the extrapyramidal system in the central nervous system that regulates posture and skeletal muscle tone may cause a variety of movement disorders. This can include dystonic reactions (muscular spasms, usually repetitive), akathisia (motor restlessness/uneasiness), pseudoparkinsonism (drug-induced Parkinsonism – tremor, rigidity, bradykinesia, etc.), tardive dyskinesia (involuntary complex muscle movements in lower face and extremities). These side effects are generally dose dependant and generally occur with long term use of medications that block dopamine. If any of these effects may be occurring, speak to your physician as soon as possible to discuss your options.
- What is Neuroleptic Malignant Syndrome?
NMS is a rare but serious reaction from a significant blockade of dopamine which can occur from antipsychotic medications or from being on high dosages of levodopa (dopamine analogue) and stopping suddenly. Presents initially as muscle cramps, tremors, fever, unstable blood pressure, and sudden changes in mental status. As it progresses over 8-40 hours it can lead to complications of rhabdomyolysis, hyperkalemia, kidney failure, or seizures. Seek medical attention immediately if this reaction is suspected.