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Medicines > classes : Empathogen or Neuroactive steroid or Phenethylamine

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generic:
None (2)
brand:
None (41) · Nexus, Eroxan (historical, late-1980s through mid-1990s) (1) · Zulresso (1) · Zurzuvae (1)
classes: (Click arrow to add another value)
mechanism:
None (1) · 5-HT2A agonist (12) · 5-HT2A agonist; long duration (1) · 5-HT2A agonist; MAO inhibitor (1) · 5-HT2A agonist; milder than other 2C-x (1) · 5-HT2A partial agonist (1) · Extremely potent 5-HT2A agonist; vasoconstrictor (1) · Extremely potent 5-HT2A agonist; very long duration (1) · MAO inhibitor; monoamine releasing agent (1) · MAO inhibitor; serotonin releasing agent (1) · Monoamine releasing agent (3) · Monoamine releasing agent; 5-HT2A agonist (1) · Monoamine releasing agent; serotonergic at higher doses (1) · Potent 5-HT2A agonist (5) · Potent 5-HT2A agonist; no oral activity (1) · Potent 5-HT2A agonist; very long duration (1) · Serotonin releasing agent (2) · Serotonin releasing agent; 5-HT2A agonist (3) · Serotonin/dopamine/norepinephrine releasing agent; 5-HT2A agonist (1) · Serotonin/norepinephrine/dopamine releasing agent (3) · Synthetic neuroactive steroid (an analog of allopregnanolone), bioavailable orally unlike brexanolone. Positive allosteric modulator at GABA-A receptors including extrasynaptic δ-containing subtypes. (1) · Very potent 5-HT2A agonist; long duration (1)
uses:
None (42) · Postpartum depression (PPD) in adults (1) · Postpartum depression (PPD) in adults (FDA-approved 2023) (1)
starting dose:
None (42) · 50 mg PO once daily with fatty food in the evening × 14 days (1) · 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 (1)
preparations:
None (42) · 100 mg/20 mL vial, single-use (1) · 20 mg, 25 mg, 30 mg capsules (1)
fda max:
None (42) · 50 mg/d × 14 d (1) · Single 60-hour course (1)
routes:
None (41) · insufflated (1) · Intravenous (continuous infusion in a REMS-certified facility) (1) · Oral (2) · PR (1)
onset:
None (41) · 45-75 min (oral) (1) · Antidepressant effect within hours of infusion start; sustained at 30 days (1) · Day 3 of dosing in trials; sustained through day 45 (1)
duration:
None (41) · 14-day course; effect persists after discontinuation in trials (1) · 4-8 h (1) · Single infusion course (1)
halflife:
None (41) · Not well characterized (1) · ~16-23 hours (1) · ~9 hours (terminal) (1)
bioavailability:
None (41) · 100% (IV) (1) · Adequate (food-dependent, must take with fatty meal) (1) · Not well characterized (1)
pregnancy:
None (41) · Limited data; avoid in pregnancy. Lactation: present in milk; consider risks (1) · Medicine is structurally identical to endogenous allopregnanolone; pregnancy considerations relate to breastfeeding during/after infusion. Limited data; brief interruption of breastfeeding considered (1) · Not established (1)
legal:
None (41) · Rx, Schedule IV (US) (1) · Rx; REMS program required (excessive sedation/loss of consciousness during infusion) (1) · [[USLegal:DEA Schedule I|Schedule I]] (United States) (1)

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