【藥品性質提示】 根據 2019 AGS Beers Criteria，本藥品為【潛在不適當用藥 (PIM)】，不建議用於老年人 (除非用於思覺失調、雙極症、或化療止吐)。

思覺失調症 Schizophrenia
阿茲海默症 Alzheimer's disease (不適用PRN治療) <20240802>

Second Generation (Atypical) Antipsychotic
Brexpiprazole exhibits partial agonist activity for 5-HT1A and D2 receptors and antagonist activity for 5-HT2A receptors

Onset of action:
(Schizophrenia) Initial effects may be observed within 1 to 2 weeks of treatment with continued improvements through 4 to 6 weeks
Protein binding:
>99%, primarily to serum albumin and alpha1-acid glycoprotein
Metabolism:
Hepatic, primarily by CYP3A4 and CYP2D6; major metabolite, DM-3411 (inactive)
Excretion:
Feces (46%, ~14% of the total dose as unchanged drug); urine (25%, <1% of the total dose as unchanged drug)

Hypersensitivity (eg, anaphylaxis, facial swelling, rash, urticaria) to brexpiprazole or any component of the formulation

1. Safety data related to atypical antipsychotics during pregnancy is limited and routine use is not recommended. However, if a woman is inadvertently exposed to an atypical antipsychotic while pregnant, continuing therapy may be preferable to switching to a typical antipsychotic.
2. Antipsychotic use during the third trimester of pregnancy has a risk for abnormal muscle movements (EPS) and/or withdrawal symptoms in newborns following delivery (agitation, feeding disorder, hypertonia, hypotonia, respiratory distress, somnolence, and tremor)

It is not known if brexpiprazole is present in breast milk. According to the manufacturer, the decision to continue or discontinue breastfeeding during therapy should take into account the risk and the benefits.

Common:
Increased serum triglycerides, weight gain, akathesia
Postmardeting:
Diabetes mellitus, dyslipidemia, impulse control disorder (including pathological gambling, increased libido, shopping, eating), neuroleptic malignant syndrome

Schizophrenia, Treatment:
1. Initial 1 mg once daily for 4 days
2. Titrate based on response and tolerability to 2 mg once daily for 3 days, followed by 4 mg on day 8
3. Target dose: 2 to 4 mg/day; maximum daily dose: 4 mg

Dosage adjustment for CYP2D6 poor metabolizers:
Administer 1/2 of the usual dose; in patients also taking moderate/strong CYP3A4 inhibitors, administer 1/4 of the usual dose.
Discontinuation of therapy:
1. In the treatment of chronic psychiatric disease, switching therapy rather than discontinuation is generally advised if side effects are intolerable or treatment is not effective.
2. If patient insists on stopping treatment, gradual dose reduction (ie, over several weeks to months) is advised to detect a re-emergence of symptoms and to avoid withdrawal reactions (eg, agitation, alternating feelings of warmth and chill, anxiety, diaphoresis, dyskinesias, GI symptoms, insomnia, irritability, myalgia, paresthesia, psychosis, restlessness, rhinorrhea, tremor, vertigo) unless discontinuation is due to significant adverse effects.

1. CrCl >60 mL/minute: No dosage adjustment necessary
2. CrCl <60 mL/minute: Maximum dose 3mg once daily (Schizophrenia)
3. Hemodialysis: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied); however, removal by dialysis unlikely since brexpiprazole is highly protein bound.

1. Mild impairment (Child-Pugh class A): There are no dosage adjustments provided in the manufacturer's labeling
2. Moderate to severe impairment (Child-Pugh class B or C): Maximum dose 3 mg once daily