Drug information of Brexpiprazole

Brexpiprazole

Drug group:

Second Generation (Atypical) Antipsychotic

Mechanism of effect

Brexpiprazole exhibits partial agonist activity for 5-HT1A and D2 receptors and antagonist activity for 5-HT2A receptors.

Pharmacodynamic

Brexpiprazole exhibits partial agonist activity for 5-HT1A and D2 receptors and antagonist activity for 5-HT2A receptors.

Pharmacokinetics

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

Drug indications

Major depressive disorder: Adjunctive treatment of major depressive disorder (MDD)

Schizophrenia: Treatment of schizophrenia

Dosage

Usual Adult Dose for Schizophrenia

Initial dose: 1 mg orally once a day on Days 1 through 4
Titration regimen: Based on clinical response and tolerability, titrate to 2 mg once a day on Days 5 to 7, then to 4 mg once a day on Day 8.
Maintenance dose: 2 to 4 mg orally once a day
Maximum dose: 4 mg/day

Use: Treatment of schizophrenia

Usual Adult Dose for Depression

Initial dose: 0.5 mg to 1 mg orally once a day
Titration regimen: Based on clinical response and tolerability, dose increases should be done at weekly intervals; titrate to 1 mg once a day, then up 2 mg once a day.
Maintenance dose: 2 mg orally once a day
Maximum dose: 3 mg/day

Comment: Healthcare providers should periodically reassess the need for maintenance treatment.

Use: Adjunctive treatment of major depressive disorder (MDD)

Points of recommendation

Monitoring Parameters

Mental status; vital signs (as clinically indicated); blood pressure (baseline; repeat 3 months after antipsychotic initiation, then yearly); weight, height, BMI, waist circumference (baseline; repeat at 4, 8, and 12 weeks after initiating or changing therapy, then quarterly; consider switching to a different antipsychotic for a weight gain ≥5% of initial weight); CBC (as clinically indicated; monitor frequently during the first few months of therapy in patients with preexisting low WBC or history of drug-induced leukopenia/neutropenia); electrolytes and liver function (annually and as clinically indicated); personal and family history of obesity, diabetes, dyslipidemia, hypertension, or cardiovascular disease (baseline; repeat annually); fasting plasma glucose level/HbA1c (baseline; repeat 3 months after starting antipsychotic, then yearly); fasting lipid panel (baseline; repeat 3 months after initiation of antipsychotic; if LDL level is normal repeat at 2- to 5-year intervals or more frequently if clinical indicated); changes in menstruation, libido, development of galactorrhea, erectile and ejaculatory function (yearly); abnormal involuntary movements or parkinsonian signs (baseline; repeat weekly until dose stabilized for at least 2 weeks after introduction and for 2 weeks after any significant dose increase); tardive dyskinesia (every 12 months; high-risk patients every 6 months); ocular examination (yearly in patients >40 years; every 2 years in younger patients) (ADA 2004; Lehman 2004; Marder 2004); fall risk (baseline and periodically during treatment in patients with diseases or on medications that may also increase fall risk).

Pregnancy level

C

This drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

AU TGA pregnancy category: C
US FDA pregnancy category: Not assigned.

Risk Summary: There are no adequate and well-controlled study data available on use of this drug in pregnant women to inform a drug-related risk.
Pregnancy Considerations
Antipsychotic use during the third trimester of pregnancy has a risk for abnormal muscle movements (extrapyramidal symptoms [EPS]) and/or withdrawal symptoms in newborns following delivery. Symptoms in the newborn may include agitation, feeding disorder, hypertonia, hypotonia, respiratory distress, somnolence, and tremor; these effects may be self-limiting or require hospitalization.

Related drugs

Asenapine , Paliperidone


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