Drilldown: Medicines

None (2) · Duloxetine (1)

Belsomra (1) · Cymbalta, Drizalma Sprinkle, Irenka, Yentreve (1) · Zurzuvae (1)

Antidepressant (1) · Anxiolytic (1) · Dual orexin receptor antagonist (DORA) (1) · GABA-A positive allosteric modulator (oral) (1) · Neuroactive steroid (1) · SNRI (1) · the first approved (1)

Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · Serotonin–norepinephrine reuptake inhibition (balanced) (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)

Depression, anxiety, neuropathic pain, fibromyalgia, chronic musculoskeletal pain (1) · 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)

None (1) · 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)

None (1) · 20 mg, 25 mg, 30 mg capsules (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1)

None (1) · 20 mg/d (1) · 50 mg/d × 14 d (1)

Oral (3)

Day 3 of dosing in trials; sustained through day 45 (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · ~30 min (1)

14-day course; effect persists after discontinuation in trials (1) · Chronic daily dosing (1) · ~7-8 hours (1)

None · ~12 hours · ~27 days · ~5 h (caffeine) · '''Autoinduction''': 25-65 hours initially, falling to 12-17 hours after 2-3 weeks of dosing as carbamazepine induces its own CYP3A4 metabolism. Major clinical implication: doses require re-titration after the autoinduction period'"`UNIQ--ref-0000001D-QINU`"' · 0.5-1.5 hours (plasma); pharmacodynamic effect persists 24+ hours'"`UNIQ--ref-000000DE-QINU`"' · 1-1.3 hours'"`UNIQ--ref-000001A1-QINU`"' · 1-1.5 hours'"`UNIQ--ref-00000DE3-QINU`"' · 1-2 hours (parent compound)'"`UNIQ--ref-00000029-QINU`"' · 1-2 hours (parent); 18-30 hours for active metabolite oxypurinol'"`UNIQ--ref-0000030F-QINU`"' · 1-2 hours'"`UNIQ--ref-00000017-QINU`"' · 1-3 hours (normal liver); markedly prolonged in overdose with glutathione depletion'"`UNIQ--ref-000006A5-QINU`"' · 1-3 minutes (very short)'"`UNIQ--ref-00000C0F-QINU`"' · 1.4 hours (parent); 13-24 hours for active metabolite canrenone'"`UNIQ--ref-00000354-QINU`"' · 1.5-2 hours (longer in renal failure)'"`UNIQ--ref-00000222-QINU`"' · 1.5-2 hours'"`UNIQ--ref-00000020-QINU`"' · 10-11 hours (benazeprilat, the active metabolite)'"`UNIQ--ref-00000A22-QINU`"' · 11-13 h (immediate-release); 11-16 h (extended-release) · 11-15 hours'"`UNIQ--ref-00000842-QINU`"' · 12-15 hours (intermediate); '''no active metabolites''' (key clinical feature)'"`UNIQ--ref-00000023-QINU`"'

Other values:

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Adequate (food-dependent, must take with fatty meal) (1) · ~50% (highly variable) (1) · ~82% (1)

Category C (1) · Limited data; avoid (1) · Limited data; avoid in pregnancy. Lactation: present in milk; consider risks (1)

Rx, Schedule IV (US) (2) · Rx-only (1)