Brexpiprazole (Dosage)

Brexpiprazole is an antipsychotic drug used in the treatment of some mental illnesses such as schizophrenia or depression. Its metabolism is mainly through CYP2D6, so knowing the metabolizer profile can help to better adjust the dose and minimize the risk of adverse effects.

Brexpiprazole is a second-generation or atypical antipsychotic medication whose mechanism of action is to change the actions of chemicals in the brain.

Brexpiprazole is used to treat the symptoms of schizophrenia and is also prescribed along with other medications to treat major depressive disorders (MDD) in adults.

MECHANISM OF ACTION

The mechanism of action of brexpiprazole in the treatment of MDD or schizophrenia is unknown. However, the efficacy of brexpiprazole may be mediated through the combination of partial agonist activity at serotonin 5-HT1A and dopamine D2 receptors and antagonist activity at serotonin 5-HT2A receptors. Likewise, brexpiprazole presents high affinity (subnanomolar) for these receptors, in addition to the alpha1B/2C receptors of norepinephrine.

SIDE EFFECTS

Headache, constipation, heartburn, tiredness, uncontrollable shaking of a part of the body, dizziness, feeling unsteady, or difficulty maintaining balance. Other side effects that may also occur but in a less present form are: rash, hives, itching, swelling of the eyes, face, mouth, lips, tongue, throat, hands, feet, ankles, or lower legs, difficulty breathing or swallowing, seizures, difficulty breathing, sore throat, cough, chills and other signs of infection, fever, sweating, confusion, irregular or rapid heart rate and severe muscle stiffness, unusual and uncontrolled movements of the face or body, falls.

Some young people have thoughts of suicide when they first start taking an antidepressant. Stay alert to changes in your mood or symptoms. Brexpiprazole is not approved for use in anyone under 18 years of age.

BRAND NAME

  • Rexulti ®

Genes analyzed

CYP2D6

Bibliography

Beunk L, Nijenhuis M, Soree B, et al. Dutch Pharmacogenetics Working Group (DPWG) guideline for the gene-drug interaction between CYP2D6, CYP3A4 and CYP1A2 and antipsychotics. Eur J Hum Genet. 2024 Mar;32(3):278-285.

Ishigooka J, Iwashita S, Higashi K, et al . Pharmacokinetics and Safety of Brexpiprazole Following Multiple-Dose Administration to Japanese Patients With Schizophrenia. J Clin Pharmacol. 2018 Jan;58(1):74-80.

Maeda K, Sugino H, Akazawa H, et al . Brexpiprazole I: in vitro and in vivo characterization of a novel serotonin-dopamine activity modulator. J Pharmacol Exp Ther. 2014 Sep;350(3):589-604.

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