Brexpiprazole

Antipsychotic Drug

Drug class: Atypical antipsychotic

Brexpiprazole (Rexulti)（中文：銳思定）

Common Strengths of Brexpiprazole Tablet

Brexpiprazole tablets are available in the following strengths:

• 0.25 mg

• 0.5 mg

• 1 mg

• 2 mg

• 3 mg

• 4 mg

Drug Trade Names of Brexpiprazole Tablet

Rexulti is the trade name for Brexpiprazole:

Drug Usage

Brexpiprazole is used for:

• Treatment of schizophrenia
• Adjunctive treatment of major depressive disorder (MDD)
• Treatment of agitation associated with dementia due to Alzheimer's disease

Mechanism of Action

Brexpiprazole acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and as an antagonist at serotonin 5-HT2A receptors. It modulates dopaminergic and

serotonergic activity to improve symptoms of schizophrenia and depression

Route of Administration

Brexpiprazole is administered orally in the form of tablets or liquid solution.

Dosages

• Schizophrenia (Adults): Initial dose of 1 mg once daily, titrated to 2 mg on Day 5 to 7, and up to 4 mg by Day 8. Target dose: 2 to 4 mg daily. Maximum dose: 4 mg/day.

• Depression (Adults): Initial dose of 0.5 mg or 1 mg once daily, titrated to 2 mg daily. Maximum dose: 3 mg/day.
• Pediatric Schizophrenia (13-17 years): Initial dose of 0.5 mg once daily, titrated to 1 mg on Day 5 to 7, and up to 2 mg by Day 8. Maximum dose: 4 mg/day.

For patients with moderate to severe renal impairment, the dosage of brexpiprazole should be reduced to a maximum of 3 mg per day for schizophrenia and 2 mg per day for MDD.

No adjustment is needed for mild renal impairment.

Side Effects

Frequency	Adverse reactions
Common	Weight gain
	Akathisia (feeling of restlessness, constant urge to move)
	Headache
	Drowsiness/sleepiness
	Dizziness
	Nausea
	Constipation
	Indigestion/heartburn
	Increased appetite
	Fatigue/tiredness
	Tremor
	Stuffy or runny nose
Uncommon	Neuroleptic malignant syndrome (high fever, muscle stiffness, confusion)
	Tardive dyskinesia (uncontrolled muscle movements)
	High blood sugar/diabetes
	Orthostatic hypotension (dizziness when standing up)
	Seizures
	Low white blood cell count
	Difficulty swallowing
	Suicidal thoughts or behaviors (especially in young adults)
	Compulsive behaviors (gambling, sexual urges, binge eating)
	Cognitive impairment
	Impaired body temperature regulation
	Stroke in elderly patients with dementia-related psychosis
	Allergic reactions (rash, itching, difficulty breathing)

Pharmacokinetics

• Absorption
  • Peak plasma concentration within 4 hours.
• Metabolism
  • Primarily metabolized by CYP3A4 and CYP2D6.
• Excretion
  • 25% in urine and 46% in feces. Terminal elimination half-life is approximately 91 hours.

Initial effects: Some patients may begin to see improvements within 1 to 2 weeks of starting treatment.

Full Therapeutic Effects: The best results are typically observed after 4 to 6 weeks for schizophrenia and major depressive disorder (MDD) For agitation associated with

dementia due to Alzheimer's disease, significant results may be seen in about 12 weeks.

Drug Precautions

Increased risk in elderly patients

• Should not be used to treat dementia-related psychosis in older adults due to increased risk of stroke and death
• May cause drowsiness, dizziness, and difficulty swallowing in elderly patients, increasing the risk of falls and choking

Suicidal thoughts in young people

• May increase the risk of suicidal thoughts in young people under 24 years old, especially in the first few months of treatment or with dose changes
• Close monitoring is required for children/teens taking aripiprazole

Use cautiously in patients with a history of seizures or with conditions that lower the seizure threshold.

Dysphagia

• Esophageal dysmotility and aspiration associated with antipsychotic drug use
• Use cautiously in patients at risk for aspiration pneumonia

Monitoring Requirements

• Regular monitoring of blood sugar levels, weight, and signs of extrapyramidal symptoms
• Perform complete blood count (CBC) in patients with pre-existing low white blood cell count (WBC) or history of drug-induced leukopenia/neutropenia
• Monitor heart rate and blood pressure and warn patients with known cardiovascular or cerebrovascular disease, and risk of dehydration or syncope

Drug Interactions

• Avoid strong CYP3A4 inducers and inhibitors

FAQ

How Should I Take the Tablet?

• Take brexpiprazole once daily with or without food, at the same time each day.

What should I avoid while taking brexpiprazole?

• Avoid alcohol, and activities requiring alertness until you know how the medication affects you. Avoid overheating and dehydration

What Happens if I Miss a Dose?

• Take the missed dose as soon as you remember unless it is almost time for your next dose. Do not double doses.