Cyp2d6 Inhibitors And Cyp3a4 Inhibitors
Severe
Textbook
Increased AUC 4.8- to 5.1-fold.
Reduce brexpiprazole dose by 75%.
Source: G&G 14e · p366
Drug reference
brexpiprazole
D2 Partial Agonist, 5HT1A Partial Agonist, Atypical Antipsychotic · Antipsychotic, Antidepressant
D2 Partial Agonist, 5HT1A Partial Agonist, Atypical AntipsychoticAntipsychotic, Antidepressant
CDSCO approved
EXCRETION
—
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
C
FDA category + note
Top interactionssee all 12 →
- Cyp2d6 Inhibitors And Cyp3a4 InhibitorsSevereTextbookG&G 14e · p366
- AbirateroneSevereDatabaseDDInter
- AlfentanilSevereDatabaseDDInter
- AmprenavirSevereDatabaseDDInter
Mechanism
Partial agonist at D2 receptors with lower D2 receptor agonist efficacy and high partial agonist effects at the 5HT1A receptor.
Indications
SchizophreniaDepression (adjunctive treatment)major depressive disorder (adjunct)unipolar depression (adjunct)agitation in patients with AD dementia
Dosing
- Adult
- 2–4 mg/day (oral)
Pharmacokinetics
Peak effect
4 h
Half-life
91 h
Bioavailability
95%
Metabolism
CYPs 2D6 and 3A4 convert to inactive metabolite (DM-3411).
Contraindications
- Use in elderly dementia patients (increased mortality risk)
Side effects
Common
weight gainmetabolic syndromeLow risk of metabolic adverse effectslowers serum prolactin
Serious
- Neuroleptic malignant syndrome
- increased mortality in elderly dementia patients
Pregnancy & lactation
Pregnancy
C
Lactation
Not specified
Drug interactions
Abiraterone
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Alfentanil
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Amprenavir
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Aprepitant
Severe
Database
Increased AUC by 2-fold.
Reduce brexpiprazole dose by 50%.
Source: DDInter
Atazanavir
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Benzhydrocodone
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Berotralstat
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Boceprevir
Severe
Database
Drug interaction classified as: metabolism
Source: DDInter
Buprenorphine
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Bupropion
Severe
Database
Increased AUC by 2-fold.
Reduce brexpiprazole dose by 50%.
Source: DDInter
Butorphanol
Severe
Database
Drug interaction classified as: synergy
Source: DDInter
Related guidelines
Ask House about brexpiprazole
Continue into a citation-backed clinical answer with the drug context already attached.
Sources: Goodman & Gilman 14e, Harrison 22e·Verified: 2026-05-10 · House clinical team