Summary of Use during Lactation

No information is available on the excretion of brexpiprazole in breastmilk. A single case report implicated brexpiprazole as a cause of decreased lactation. A review of case reports found lactation disorders and breast secretion reported as side effects, but details are lacking. Until more data are available, an alternate drug may be preferred.

Drug Levels

Maternal Levels. A woman with schizophrenia received brexpiprazole 2 mg once daily, risperidone 2 mg twice daily and quetiapine 12.5 mg twice daily during pregnancy and postpartum. Concentrations of brexpiprazole in breastmilk were 1 mcg/L on day 4 approximately 2 hours after the last dose, 2.3 mcg/L on day 5 at 6.5 hours after the last dose, and 6 mcg/L on day 6 at 22 hours after the last dose. The authors estimated the relative infant dose to be about 0.7%, although an insufficient amount of sampling was performed to verify this value.[1]

Infant Levels. A breastfed newborn infant whose mother was taking brexpiprazole 2 mg once daily, risperidone 2 mg twice daily and quetiapine 12.5 mg twice daily during pregnancy and postpartum had serum levels measured. At birth, the cord blood level was 3.9 mcg/L from maternal use during pregnancy. The neonate ingested small volumes of colostrum and milk 12 times from 46 to 86.5 hours after birth. Serum levels declined with a half-life of 45.9 hours between 16.5 and 41 hours after birth. By about 115 hours postpartum, brexpiprazole was undetectable (<0.5 mcg/L) in the infant’s serum.[1]

Effects in Breastfed Infants

Relevant published information was not found as of the revision date.

Effects on Lactation and Breastmilk

A woman was taking brexpiprazole 2 mg daily during the third trimester of pregnancy for bipolar disorder. Her newborn infant was hospitalized in the NICU for hypoxic ischemic encephalopathy for 18 days. While her infant was in the NICU, she reduced her brexpiprazole dose to 2 mg every 2 days because of a shortage of medication. The mother, who had successfully breastfed 2 previous infants, pumped milk 10 times daily and was able to pump 120 mL daily by one week postpartum. After her infant was discharged, she increased the dose back to 2 mg daily. At a follow-up clinic visit, she could only pump 30 mL daily. She then stopped brexpiprazole and began a short course of metoclopramide. Within 10 days of stopping brexpiprazole, her milk supply increased, and she could almost exclusively breastfeed her infant who gained weight normally. Her serum prolactin level also increased to normal.[2]

A review of case reports of adverse reactions reported in the US Food and Drug Administration’s Adverse Event Reporting System from 2015 to 2023 found 6 reports of “lactation disorder” and 10 cases of “breast discharge” reported with brexpiprazole. Other details were lacking.[3]

Alternate Drugs to Consider

Haloperidol, Olanzapine, Quetiapine, Risperidone

References

1.

Konishi T, Kitahiro Y, Fujiwara N, et al. Pharmacokinetics of brexpiprazole, quetiapine, risperidone, and its active metabolite paliperidone in a postpartum woman and her baby. Ther Drug Monit 2024. [PubMed: 38648649]

2.

Berlin S, Bodnar K. Low breast milk production associated with brexipiprazole (Rexulti). Breastfeed Med 2020;15:A-3. doi:10.1089/bfm.2020.29162.abstracts [CrossRef]

3.

Jiang Y, Zhou L, Shen Y, et al. Safety assessment of brexpiprazole: Real-world adverse event analysis from the FAERS database. J Affect Disord 2024;346:223-9. [PubMed: 37956832]

Substance Name

Brexpiprazole

CAS Registry Number

913611-97-9

Drug Class

Breast Feeding

Lactation

Milk, Human

Antipsychotic Agents

Serotonin Agents

Dopamine Agonists