Drilldown: Medicines

None (2) · Duloxetine (1) · Lidocaine (hydrochloride) (1)

Belsomra (1) · Cymbalta, Drizalma Sprinkle, Irenka, Yentreve (1) · Wakix (1) · Xylocaine (injectable, oral solution, topical), Lidoderm (patch), ZTLido (patch), Glydo (jelly), EMLA (with prilocaine, topical) (1)

Antidepressant (1) · Anxiolytic (1) · Dual orexin receptor antagonist (DORA) (1) · Histamine H3 receptor inverse agonist / antagonist (1) · SNRI (1) · the first approved (1) · wake-promoting agent (1) · [[:Category:Anesthetics|Anesthetic]] (1) · [[:Category:Antiarrhythmics|Antiarrhythmic (Vaughan Williams Class IB)]] (1) · [[:Category:Local anesthetics|Local anesthetic (amide class)]] (1)

None (2) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · Serotonin–norepinephrine reuptake inhibition (balanced) (1)

Depression, anxiety, neuropathic pain, fibromyalgia, chronic musculoskeletal pain (1) · Excessive daytime sleepiness or cataplexy in adults with narcolepsy (FDA-approved August 2019) (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-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (1)

None (1) · 10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · Infiltration: 1-2% solution; '''4.5 mg/kg ceiling without epinephrine, 7 mg/kg with epinephrine'''. IV antiarrhythmic: 1-1.5 mg/kg bolus then infusion 1-4 mg/minute. Lidoderm patch: up to 3 patches per 12 hours (1) · Week 1: 8.9 mg PO once daily in the morning. Week 2: 17.8 mg. Week 3+: 35.6 mg (max). Titrate as needed. (1)

None (1) · 4.45 mg, 17.8 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · Injection 0.5-4% solutions (with and without epinephrine); topical cream 4-5%; transdermal patch 5% (Lidoderm), 1.8% (ZTLido); oral 2% viscous solution; jelly 2%; ophthalmic (1)

None (1) · '''4.5 mg/kg (without epinephrine), 7 mg/kg (with epinephrine)''' for infiltration; serum level monitoring required for prolonged IV antiarrhythmic use (1) · 20 mg/d (1) · 35.6 mg/d (1)

epidural (1) · infiltration (1) · intravenous (1) · nerve block) (1) · Oral (3) · oral mucosal (1) · regional anesthesia (spinal (1) · Topical (1)

<1 minute (IV); 1-2 minutes (infiltration); 30+ minutes (patch on adult skin, faster on thinner pediatric skin) (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · Wake-promoting effect over weeks of titration (1) · ~30 min (1)

30-90 minutes (infiltration without epinephrine); 90-200 minutes (with epinephrine); 12 hours (patch) (1) · Chronic daily dosing (1) · Daily morning 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 days acute, 4-6 days chronic; 4-16 days for norfluoxetine'"`UNIQ--ref-0000004C-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`"'

Other values:

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Not formally established; oral once-daily adequate (1) · ~35% (oral, extensive first-pass; not used orally for systemic effect); ~100% (IV)'"`UNIQ--ref-00000021-QINU`"' (1) · ~50% (highly variable) (1) · ~82% (1)

Category C (1) · Extensive use experience in obstetric anesthesia; broadly considered safe'"`UNIQ--ref-00000022-QINU`"' (1) · Limited data; avoid (1) · Limited data; pitolisant may reduce hormonal contraceptive efficacy (1)

Rx, '''not a controlled substance''' (unique among wake-promoting agents) (1) · Rx, Schedule IV (US) (1) · Rx-only (1) · [[USLegal:Prescription only|Rx-only]] for most formulations; some low-concentration topical formulations are [[USLegal:Over-the-counter|OTC]] (4% cream) (1)