Last update June 26, 2022

7-{4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one

Likely Compatibility

Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.

It is an atypical or second generation antipsychotic indicated in the treatment of schizophrenia and major depressive disorder. Oral administration once daily.

Since the last update we have not found published data on its excretion in breastmilk.

Its pharmacokinetic data (very high percentage of protein binding, moderately high molecular weight and very wide volume of distribution) make it highly unlikely that significant quantities will pass into breast milk.

Brexpiprazole produces a minimal increase in prolactin levels. (Clayton 2020, Ivkovic 2019, Ishigooka 2018)

A doubtful cause of lactation suppression attributed to brexpiprazole has been published. (Berlin 2020)

Until there is further published data on this drug in relation to breastfeeding, known safer alternatives are preferable (Wichniak 2021), especially during the neonatal period and in cases of prematurity.


See below the information of these related products:

Alternatives

  • Olanzapine (Safe product and/or breastfeeding is the best option.)
  • Paliperidone (Safe product and/or breastfeeding is the best option.)
  • Quetiapine Fumarate (Safe product and/or breastfeeding is the best option.)
  • Risperidone (Safe product and/or breastfeeding is the best option.)

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

Jose Maria Paricio, Founder & President of APILAM/e-Lactancia

Your contribution is essential for this service to continue to exist. We need the generosity of people like you who believe in the benefits of breastfeeding.

Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Other names

7-{4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one is Brexpiprazole in Chemical name.

Is written in other languages:

Groups

7-{4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one belongs to these groups or families:

Tradenames

Main tradenames from several countries containing 7-{4-[4-(1-Benzothiophen-4-yl)piperazin-1-yl]butoxy}quinolin-2(1H)-one in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 95 %
Molecular weight 434 daltons
Protein Binding > 99 %
VD 1.56 l/Kg
pKa 13.56 -
Tmax 4 hours
91 - 96 hours

References

  1. Wichniak A, Siwek M, Rymaszewska J, Janas-Kozik M, Wolańczyk T, Bieńkowski P, Dudek D, Heitzman J, Szulc A, Samochowiec J. The position statement of the Working Group of the Polish Psychiatric Association on the use of D2/D3 dopamine receptor partial agonists in special populations. Psychiatr Pol. 2021 Oct 31;55(5):967-987. Abstract Full text (link to original source) Full text (in our servers)
  2. Clayton AH, Ivkovic J, Chen D, George V, Hobart M. Effect of Brexpiprazole on Prolactin and Sexual Functioning: An Analysis of Short- and Long-Term Study Data in Major Depressive Disorder. J Clin Psychopharmacol. 2020 Nov/Dec;40(6):560-567. Abstract Full text (link to original source)
  3. Berlin S, Bodnar K. Low breast milk production associated with brexipiprazole (Rexulti). The Academy of Breastfeeding Medicine 25th Annual International Meeting. Breastfeed Med 2020;15:A-3. Poster-Abstract #4. Abstract Full text (link to original source)
  4. Ivkovic J, Lindsten A, George V, Eriksson H, Hobart M. Effect of Brexpiprazole on Prolactin: An Analysis of Short- and Long-Term Studies in Schizophrenia. J Clin Psychopharmacol. 2019 Jan/Feb;39(1):13-19. Abstract Full text (link to original source)
  5. Ishigooka J, Iwashita S, Higashi K, Liew EL, Tadori Y. Pharmacokinetics and Safety of Brexpiprazole Following Multiple-Dose Administration to Japanese Patients With Schizophrenia. J Clin Pharmacol. 2018 Jan;58(1):74-80. Abstract Full text (link to original source)

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