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Drilldown: Medicines

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Medicines > generic: None & halflife : ~12 hours or ~16-23 hours

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generic: (Click arrow to add another value)
brand:
Belsomra (1) · Zurzuvae (1)
classes:
Dual orexin receptor antagonist (DORA) (1) · GABA-A positive allosteric modulator (oral) (1) · Neuroactive steroid (1) · the first approved (1)
mechanism:
Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · Synthetic neuroactive steroid (an analog of allopregnanolone), bioavailable orally unlike brexanolone. Positive allosteric modulator at GABA-A receptors including extrasynaptic δ-containing subtypes. (1)
uses:
Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · Postpartum depression (PPD) in adults (FDA-approved 2023) (1)
starting dose:
10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 50 mg PO once daily with fatty food in the evening × 14 days (1)
preparations:
20 mg, 25 mg, 30 mg capsules (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1)
fda max:
20 mg/d (1) · 50 mg/d × 14 d (1)
routes:
Oral (2)
onset:
Day 3 of dosing in trials; sustained through day 45 (1) · ~30 min (1)
duration:
14-day course; effect persists after discontinuation in trials (1) · ~7-8 hours (1)
halflife: (Click arrow to add another value)
bioavailability:
Adequate (food-dependent, must take with fatty meal) (1) · ~82% (1)
pregnancy:
Limited data; avoid (1) · Limited data; avoid in pregnancy. Lactation: present in milk; consider risks (1)
legal:
Rx, Schedule IV (US) (2)

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