Zuranolone: Difference between revisions
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| duration = 14-day course; effect persists after discontinuation in trials | | duration = 14-day course; effect persists after discontinuation in trials | ||
| halflife = ~16-23 hours | | halflife = ~16-23 hours | ||
| bioavailability = Adequate (food-dependent | | bioavailability = Adequate (food-dependent, must take with fatty meal) | ||
| pregnancy = Limited data; avoid in pregnancy. Lactation: present in milk; consider risks | | pregnancy = Limited data; avoid in pregnancy. Lactation: present in milk; consider risks | ||
| legal = Rx, Schedule IV (US) | | legal = Rx, Schedule IV (US) | ||
| intro = '''Zuranolone''' (brand name Zurzuvae) is the first '''oral''' neuroactive steroid approved for postpartum depression, FDA-approved in August 2023. Like brexanolone, it acts as a positive allosteric modulator at GABA-A receptors, including extrasynaptic δ-containing subtypes thought to mediate antidepressant effect. Administered as a 14-day fixed-duration course rather than chronic daily dosing | | intro = '''Zuranolone''' (brand name Zurzuvae) is the first '''oral''' neuroactive steroid approved for postpartum depression, FDA-approved in August 2023. Like brexanolone, it acts as a positive allosteric modulator at GABA-A receptors, including extrasynaptic δ-containing subtypes thought to mediate antidepressant effect. Administered as a 14-day fixed-duration course rather than chronic daily dosing, an unusual paradigm in psychiatry. Initially studied for major depressive disorder (MDD) as well but the MDD application was rejected by FDA; only PPD problem approved. | ||
| pharmacodynamics= Positive allosteric modulator at synaptic and extrasynaptic GABA-A receptors at the neuroactive steroid binding site, with affinity for δ-containing extrasynaptic receptors. Oral bioavailability with food enables outpatient dosing, unlike brexanolone's IV infusion. | | pharmacodynamics= Positive allosteric modulator at synaptic and extrasynaptic GABA-A receptors at the neuroactive steroid binding site, with affinity for δ-containing extrasynaptic receptors. Oral bioavailability with food enables outpatient dosing, unlike brexanolone's IV infusion. | ||
| effects = Somnolence (most common, can affect driving | | effects = Somnolence (most common, can affect driving, black-box warning about CNS depressant activities for ≥12 hours after dose), dizziness, sedation, headache, diarrhea, fatigue. Suicidal thoughts reported. | ||
| interactions = <pharmaInteractions/> | | interactions = <pharmaInteractions/> | ||
}} | }} | ||