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Medicines > halflife : 1.5-2 hours'"`UNIQ--ref-00000020-QINU`"' or ~12 hours or ~4 h

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generic:
None (1) · Duloxetine (1) · Lidocaine (hydrochloride) (1) · Sildenafil (1)
brand:
Belsomra (1) · Cymbalta, Drizalma Sprinkle, Irenka, Yentreve (1) · Viagra, Revatio (1) · Xylocaine (injectable, oral solution, topical), Lidoderm (patch), ZTLido (patch), Glydo (jelly), EMLA (with prilocaine, topical) (1)
classes:
Antidepressant (1) · Anxiolytic (1) · Dual orexin receptor antagonist (DORA) (1) · PDE5 Inhibitor (1) · SNRI (1) · the first approved (1) · [[:Category:Anesthetics|Anesthetic]] (1) · [[:Category:Antiarrhythmics|Antiarrhythmic (Vaughan Williams Class IB)]] (1) · [[:Category:Local anesthetics|Local anesthetic (amide class)]] (1)
mechanism:
None (1) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · Selective inhibitor of phosphodiesterase type 5 (PDE5), preventing cGMP breakdown in vascular smooth muscle. In the corpus cavernosum, potentiates the NO/cGMP cascade triggered by sexual stimulation. (1) · Serotonin–norepinephrine reuptake inhibition (balanced) (1)
uses:
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-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (1) · '"`UNIQ--vote-00000705-QINU`"', '"`UNIQ--vote-00000706-QINU`"' (1)
starting dose:
None (1) · 10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 50 mg ~1 h before sexual activity (ED); 20 mg TID (PAH) (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)
preparations:
None (1) · 25, 50, 100 mg tabs (Viagra); 20 mg tabs and 10 mg/mL oral suspension (Revatio) (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)
fda max:
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) · 100 mg/d (ED); 20 mg TID (PAH) (1) · 20 mg/d (1)
routes:
epidural (1) · infiltration (1) · intravenous (1) · IV (Revatio) (1) · nerve block) (1) · Oral (3) · oral mucosal (1) · regional anesthesia (spinal (1) · Topical (1)
onset:
30–60 min (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) · ~30 min (1)
duration:
30-90 minutes (infiltration without epinephrine); 90-200 minutes (with epinephrine); 12 hours (patch) (1) · Chronic daily dosing (1) · ~4 h (1) · ~7-8 hours (1)
halflife: (Click arrow to add another value)
bioavailability:
~35% (oral, extensive first-pass; not used orally for systemic effect); ~100% (IV)'"`UNIQ--ref-00000021-QINU`"' (1) · ~40% (1) · ~50% (highly variable) (1) · ~82% (1)
pregnancy:
Category B (1) · Category C (1) · Extensive use experience in obstetric anesthesia; broadly considered safe'"`UNIQ--ref-00000022-QINU`"' (1) · Limited data; avoid (1)
legal:
Rx, Schedule IV (US) (1) · Rx-only (1) · Rx-only in US (1) · [[USLegal:Prescription only|Rx-only]] for most formulations; some low-concentration topical formulations are [[USLegal:Over-the-counter|OTC]] (4% cream) (1)
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