[Durgical](https://durgical.com/en/) › [DurgiPedia](https://durgical.com/en/durgipedia/) › [Pharmacology](https://durgical.com/en/pharmacology/) › [Neurosteroid antidepressants](https://durgical.com/en/pharmacology/classes/neurosteroid-antidepressants/) › Brexanolone # Brexanolone ## Neurosteroid antidepressants? Neurosteroid antidepressants Allopregnanolone given as a 60-hour IV infusion for postpartum depression. It boosts GABA-A receptors and can cause sudden loss of consciousness. Updated Nov 1, 2026 Also called: Allopregnanolone ## Quick facts **Group** [Neurosteroid antidepressants](https://durgical.com/en/pharmacology/classes/neurosteroid-antidepressants/) **Target** GABA-A receptor (positive allosteric modulator) **Used for** Postpartum depression in adults **Key effects** Sleepiness and fatigue · Dry mouth **Monitor** Mood and suicidal thoughts · Kidney function **ATC** N06AX29 No doses: the clinician sets them by the current guideline. On this page - The basics Mechanism of action - Indications - Adverse effects - Pharmacokinetics - Memory aid - Safety Contraindications - Key interactions - What is monitored - Administration and safety - Pregnancy and breastfeeding - Nursing care - Study Test yourself - Connections Connections ## Mechanism of action ◎**GABA-A receptor (positive allosteric modulator)**Brexanolone ⓘ The figure shows allopregnanolone (the same molecule as brexanolone) bound to the human alpha1-beta2-gamma2 GABA-A receptor together with GABA. **Target in 3D:** GABA-A receptor (positive allosteric modulator). PDB structure 8SI9 (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/8SI9) · Drag to rotate · pinch to zoom Brexanolone is a formulation of allopregnanolone, a natural neurosteroid. It binds GABA-A receptors at a site distinct from GABA and benzodiazepines and increases the chloride current that GABA opens, so neurons become harder to excite. Restoring this neurosteroid signal may relieve postpartum depression; the same action produces sedation. - Brexanolone binds a neurosteroid site on GABA-A receptors - GABA opens more chloride current: neurons are calmer - May restore a reduced neurosteroid signal - Same action causes sedation and possible loss of consciousness ## Indications - Postpartum depression in adults [Perinatal depression and postpartum psychosis →](https://durgical.com/en/conditions/perinatal-depression-and-postpartum-psychosis/) ## Adverse effects ### Common - Sleepiness and fatigue - Dizziness or a spinning sensation - Dry mouth, mouth or throat pain, heartburn - Flushing and hot flushes ### Serious (rare, important) - Excessive sedation and sudden loss of consciousness (boxed warning) - Suicidal thoughts and behaviour - Racing heartbeat ## Contraindications - End-stage renal disease (the solubilising agent can accumulate) ## Key interactions **Opioids, benzodiazepines, other sedatives, antidepressants and alcohol** Added sedation and risk of loss of consciousness ## What is monitored - Level of sedation at regular intervals while awake during the infusion - Mood and suicidal thoughts - Kidney function ## Administration and safety - Given only in a certified health facility under a restricted distribution programme - The infusion is paused or stopped if excessive sedation occurs - No driving or operating machinery until the sleepiness has passed ## Pregnancy and breastfeeding It is used after childbirth; data on breastfeeding are limited, so the decision is made with the treating team. ## Nursing care - Checks for sleepiness every few hours while the patient is awake and reports excessive sedation at once - Makes sure another adult cares for the baby during and after the infusion - Asks about suicidal thoughts and changes in mood - Reviews other sedating medicines and alcohol use ## Pharmacokinetics **Absorption** Continuous intravenous infusion over about 60 hours (2.5 days) **Metabolism** Keto-reduction, glucuronidation and sulfation, not by CYP enzymes as the main route **Half-life** About 9 hours after the infusion ends ## Memory aid «BREXANolone = BREAKS the postpartum low with Allopregnanolone, but watch the eyes close»: GABA-A boost, IV in hospital, sedation watch. ## Test yourself Think of the answer, then tap the question to see it. ## What natural molecule is brexanolone, and where does it act? Allopregnanolone; it is a positive allosteric modulator of GABA-A receptors. ## Why is brexanolone given only in a monitored facility? It can cause excessive sedation and sudden loss of consciousness. ## Why is it avoided in end-stage renal disease? The solubilising agent in the infusion can accumulate. [Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/brexanolone/) [More Pharmacology questions →](https://durgical.com/en/practice/?f=pharmacology) ## Connections ## Related drugs 1 - [Zuranolone](https://durgical.com/en/pharmacology/zuranolone/) ## Related conditions 1 - [Perinatal depression and postpartum psychosis](https://durgical.com/en/conditions/perinatal-depression-and-postpartum-psychosis/) [← Back to the class: Neurosteroid antidepressants](https://durgical.com/en/pharmacology/classes/neurosteroid-antidepressants/) Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given. Sources: [Brexanolone Injection: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a619037.html) (MedlinePlus (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N06AX29) (WHO Collaborating Centre for Drug Statistics Methodology, 2026). ## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake Representative model, for educational purposes only. --- Source: https://durgical.com/en/pharmacology/brexanolone/ License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/brexanolone/