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Medicines > legal : Currently legal in most jurisdictions with thujone limits or Rx, Schedule IV (US) or [[USLegal:DEA Schedule I|Schedule I]] (United States)

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generic:
None (5) · 2C-B (1) · Artemisia absinthium (1) · DMT (1)
brand:
None (1) · Belsomra (1) · Dayvigo (1) · Nexus, Eroxan (historical, late-1980s through mid-1990s) (1) · Quviviq (1) · Sunosi (1) · Wormwood, absinthe, la Fée Verte, the Green Muse (1) · Zurzuvae (1)
classes:
2C-x series (1) · Dual orexin receptor antagonist (DORA) (3) · GABA-A positive allosteric modulator (oral) (1) · Neuroactive steroid (1) · Norepinephrine-dopamine reuptake inhibitor (NDRI) (1) · Phenethylamine (1) · Plant Medicine (1) · Psychedelic (1) · Rhapsodica (1) · the first approved (1) · wake-promoting agent (1) · [[:Category:Classical Psychedelics (Serotonergic)|Classic Psychedelic]] (1) · [[:Category:Tryptamines|Tryptamine]] (1)
mechanism:
None (1) · 5-HT2A partial agonist (1) · 5-HT2A partial agonist; sigma-1 agonist (1) · Active principle is thujone, a GABA-A antagonist (the opposite of most CNS depressants). Also present in cooking sage (''Salvia officinalis''), tansy, and ''Thuja'' cedars. (1) · Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance. (1) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · Selective dopamine and norepinephrine reuptake inhibitor (DAT and NET inhibition). Unlike amphetamine, does not significantly release monoamines, pure reuptake inhibition. (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:
None (2) · Excessive daytime sleepiness in adults with narcolepsy or obstructive sleep apnea (OSA) (1) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) (1) · Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (1) · Postpartum depression (PPD) in adults (FDA-approved 2023) (1) · '"`UNIQ--vote-00000008-QINU`"', '"`UNIQ--vote-00000009-QINU`"' (1)
starting dose:
None (2) · 10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · 50 mg PO once daily with fatty food in the evening × 14 days (1) · A measured pour of absinthe diluted 5:1 with cold water over sugar (the louche ritual) (1) · Narcolepsy: 75 mg PO once daily upon awakening, titrate every 3 days. OSA: 37.5 mg PO once daily, titrate. (1)
preparations:
None (2) · 20 mg, 25 mg, 30 mg capsules (1) · 25 mg, 50 mg tablets (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · 75 mg, 150 mg tablets (1) · Dried leaves; absinthe liqueur (120–160 proof, with hyssop, lemon balm, fennel, anise, sometimes Acorus calamus) (1)
fda max:
None (3) · 10 mg/d (1) · 150 mg/d (1) · 20 mg/d (1) · 50 mg/d (1) · 50 mg/d × 14 d (1)
routes:
None (1) · insufflated (1) · Oral (7) · PR (1)
onset:
None (2) · 45-75 min (oral) (1) · Day 3 of dosing in trials; sustained through day 45 (1) · ~30 min (3) · ~30-60 min (1)
duration:
None (1) · 14-day course; effect persists after discontinuation in trials (1) · 4-8 h (1) · About 20 minutes (1) · ~7-8 hours (3) · ~9 hours (1)
halflife:
None (1) · 9–12 minutes (intravenous) (1) · Not well characterized (1) · ~12 hours (1) · ~16-23 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~7.1 hours (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)
bioavailability:
None (2) · Adequate (food-dependent, must take with fatty meal) (1) · Not well characterized (1) · ~44% (1) · ~62% (1) · ~82% (1) · ~95% (1)
pregnancy:
None (2) · Limited data; avoid (3) · Limited data; avoid in pregnancy. Lactation: present in milk; consider risks (1) · Limited data; pregnancy exposure registry available (1) · Not established (1)
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