Maintenance script: Terminology sweep: drug/medication → medicine

2026-05-16T02:27:26Z

Terminology sweep: drug/medication → medicine

← Older revision		Revision as of 02:27, 16 May 2026
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	\| halflife = ~9 hours (terminal)		\| halflife = ~9 hours (terminal)
	\| bioavailability = 100% (IV)		\| bioavailability = 100% (IV)
	\| pregnancy = ~~Drug~~ is structurally identical to endogenous allopregnanolone; pregnancy considerations relate to breastfeeding during/after infusion. Limited data; brief interruption of breastfeeding considered		\| pregnancy = Medicine is structurally identical to endogenous allopregnanolone; pregnancy considerations relate to breastfeeding during/after infusion. Limited data; brief interruption of breastfeeding considered
	\| legal = Rx; REMS program required (excessive sedation/loss of consciousness during infusion)		\| legal = Rx; REMS program required (excessive sedation/loss of consciousness during infusion)
	\| intro = '''Brexanolone''' (brand name Zulresso) is a cyclodextrin-based IV formulation of '''allopregnanolone''', the body's own neuroactive steroid produced as a metabolite of progesterone. FDA-approved in March 2019 as the first ~~medication~~ specifically for postpartum depression (PPD). Administered as a single 60-hour continuous infusion in a REMS-certified inpatient setting due to risk of excessive sedation. The ~~drug~~'s rationale rests on the observation that allopregnanolone levels fall precipitously after delivery; rapidly restoring those levels via infusion produces a rapid antidepressant response that persists for 30+ days in trials.		\| intro = '''Brexanolone''' (brand name Zulresso) is a cyclodextrin-based IV formulation of '''allopregnanolone''', the body's own neuroactive steroid produced as a metabolite of progesterone. FDA-approved in March 2019 as the first medicine specifically for postpartum depression (PPD). Administered as a single 60-hour continuous infusion in a REMS-certified inpatient setting due to risk of excessive sedation. The medicine's rationale rests on the observation that allopregnanolone levels fall precipitously after delivery; rapidly restoring those levels via infusion produces a rapid antidepressant response that persists for 30+ days in trials.
	\| pharmacodynamics= Positive allosteric modulator at GABA-A receptors at a distinct '''neuroactive steroid binding site''' (separate from benzodiazepine and barbiturate sites). Modulates both '''synaptic''' (phasic, mostly benzo-sensitive α1/α2/α3/α5-containing) and '''extrasynaptic''' (tonic, mostly benzo-insensitive δ-containing) GABA-A receptors. The benzodiazepine-insensitive δ-containing extrasynaptic receptors are hypothesized to be the key target for antidepressant effect, since benzodiazepines themselves do not have antidepressant efficacy.		\| pharmacodynamics= Positive allosteric modulator at GABA-A receptors at a distinct '''neuroactive steroid binding site''' (separate from benzodiazepine and barbiturate sites). Modulates both '''synaptic''' (phasic, mostly benzo-sensitive α1/α2/α3/α5-containing) and '''extrasynaptic''' (tonic, mostly benzo-insensitive δ-containing) GABA-A receptors. The benzodiazepine-insensitive δ-containing extrasynaptic receptors are hypothesized to be the key target for antidepressant effect, since benzodiazepines themselves do not have antidepressant efficacy.
	\| effects = Sedation (very common), loss of consciousness (REMS warning), syncope, dry mouth, flushing. Suicidal thoughts have been observed.		\| effects = Sedation (very common), loss of consciousness (REMS warning), syncope, dry mouth, flushing. Suicidal thoughts have been observed.

Maintenance script: Create Brexanolone page (Stahl-sourced detail with skepticism)

2026-05-16T01:55:59Z

Create Brexanolone page (Stahl-sourced detail with skepticism)

New page

{{MedTemplate
| brand = Zulresso
| classes = Neuroactive steroid, GABA-A positive allosteric modulator
| mechanism = Allopregnanolone (the body's own neurosteroid metabolite of progesterone) delivered IV. Positive allosteric modulator at both benzodiazepine-sensitive and benzodiazepine-insensitive GABA-A receptors. Hypothesized to act primarily at the benzodiazepine-insensitive site, which differentiates it from benzodiazepines (which lack antidepressant efficacy)
| uses = Postpartum depression (PPD) in adults
| starting_dose = Single 60-hour continuous IV infusion: 30 mcg/kg/h × 4h → 60 mcg/kg/h × 20h → 90 mcg/kg/h × 28h → 60 mcg/kg/h × 4h → 30 mcg/kg/h × 4h
| preparations = 100 mg/20 mL vial, single-use
| fda_max = Single 60-hour course
| routes = Intravenous (continuous infusion in a REMS-certified facility)
| onset = Antidepressant effect within hours of infusion start; sustained at 30 days
| duration = Single infusion course
| halflife = ~9 hours (terminal)
| bioavailability = 100% (IV)
| pregnancy = Drug is structurally identical to endogenous allopregnanolone; pregnancy considerations relate to breastfeeding during/after infusion. Limited data; brief interruption of breastfeeding considered
| legal = Rx; REMS program required (excessive sedation/loss of consciousness during infusion)
| intro = '''Brexanolone''' (brand name Zulresso) is a cyclodextrin-based IV formulation of '''allopregnanolone''', the body's own neuroactive steroid produced as a metabolite of progesterone. FDA-approved in March 2019 as the first medication specifically for postpartum depression (PPD). Administered as a single 60-hour continuous infusion in a REMS-certified inpatient setting due to risk of excessive sedation. The drug's rationale rests on the observation that allopregnanolone levels fall precipitously after delivery; rapidly restoring those levels via infusion produces a rapid antidepressant response that persists for 30+ days in trials.
| pharmacodynamics= Positive allosteric modulator at GABA-A receptors at a distinct '''neuroactive steroid binding site''' (separate from benzodiazepine and barbiturate sites). Modulates both '''synaptic''' (phasic, mostly benzo-sensitive α1/α2/α3/α5-containing) and '''extrasynaptic''' (tonic, mostly benzo-insensitive δ-containing) GABA-A receptors. The benzodiazepine-insensitive δ-containing extrasynaptic receptors are hypothesized to be the key target for antidepressant effect, since benzodiazepines themselves do not have antidepressant efficacy.
| effects = Sedation (very common), loss of consciousness (REMS warning), syncope, dry mouth, flushing. Suicidal thoughts have been observed.
| interactions = <pharmaInteractions/>
}}

[[Category:Neuroactive Steroids]]
[[Category:GABAA Positive Allosteric Modulators (General)]]
[[Category:GABAergics]]
[[Category:Antidepressants]]

Brexanolone - Revision history

Maintenance script: Terminology sweep: drug/medication → medicine

Maintenance script: Create Brexanolone page (Stahl-sourced detail with skepticism)