Drilldown: Medicines

None (1) · Duloxetine (1) · Propranolol (1)

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

Antidepressant (1) · Anxiolytic (1) · Beta Blocker (1) · Dual orexin receptor antagonist (DORA) (1) · Non-selective (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) · Non-selective competitive antagonist at β1 and β2 adrenergic receptors. Lipophilic; significant blood–brain barrier penetration, accounting for its CNS effects. (1) · Serotonin–norepinephrine reuptake inhibition (balanced) (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) · '"`UNIQ--vote-000005E7-QINU`"', '"`UNIQ--vote-000005E8-QINU`"', '"`UNIQ--vote-000005E9-QINU`"', '"`UNIQ--vote-000005EA-QINU`"', '"`UNIQ--vote-000005EB-QINU`"' (1)

None (1) · 10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10–40 mg (situational anxiety); 40 mg BID (HTN) (1)

None (1) · 10, 20, 40, 60, 80 mg tabs; 60/80/120/160 mg ER caps; 1 mg/mL IV (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1)

None (1) · 20 mg/d (1) · 640 mg/d (HTN); 240 mg/d (migraine) (1)

IV (1) · Oral (3)

1–2 h (PO), immediate (IV) (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · ~30 min (1)

6–12 h (IR); 24 h (ER) (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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~25% (extensive hepatic first-pass) (1) · ~50% (highly variable) (1) · ~82% (1)

Category C (2) · Limited data; avoid (1)

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