Drilldown: Medicines

None (3) · Naltrexone (1)

Belsomra (1) · Dayvigo (1) · Quviviq (1) · ReVia (oral, 50 mg tablets), Depade (oral, generic), Vivitrol (extended-release IM injection 380 mg monthly); Contrave (naltrexone + bupropion ER tablets for weight management) (1)

Dual orexin receptor antagonist (DORA) (3) · the first approved (1) · [[:Category:AUD medicines|Alcohol use disorder medicine]] (1) · [[:Category:Opioid antagonists|Opioid antagonist (mu and kappa)]] (1) · [[:Category:OUD medicines|Opioid use disorder medicine]] (1)

None (2) · 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)

None (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)

None (1) · 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)

25 mg, 50 mg tablets (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · Oral tablets 50 mg (ReVia, Depade, generics); Vivitrol extended-release IM suspension 380 mg single-dose vial; Contrave (naltrexone 8 mg + bupropion 90 mg ER tablets); compounded 1, 2, 3, 4.5 mg tablets/capsules for LDN (1)

10 mg/d (1) · 20 mg/d (1) · 50 mg/d (1) · 50 mg/day oral; 380 mg/4 weeks IM (Vivitrol); 32 mg + 360 mg naltrexone/bupropion daily (Contrave maximum after titration) (1)

intramuscular (depot) (1) · Oral (4)

Oral peak plasma 1 hour; therapeutic opioid blockade within hours of first dose. IM Vivitrol: peak plasma 2-3 days; therapeutic blockade through the dosing interval. (1) · ~30 min (3)

None · 24 hours · 4-6 hours · 12 hours · 6-8 hours · Daily dosing · 8-12 hours · 12-24 hours · Hours · Hours per application · 24 hours (HS dosing) · 24 hours (once-daily dosing) · 24 h · N/A · N/A (replacement) · Variable · ~7-8 hours · 3-5 hours · 4-6 hours (IR); 24 hours (ER) · 6-12 hours

Other values:

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Naltrexone parent ~4 hours (oral); 6-beta-naltrexol (active metabolite) ~13 hours. Vivitrol depot terminal half-life 5-10 days with sustained release from microspheres maintaining blockade for the 4-week dosing interval.'"`UNIQ--ref-0000004F-QINU`"' (1) · ~12 hours (1) · ~17-19 hours (longer than daridorexant) (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

~44% (1) · ~5-40% (oral, highly variable due to extensive first-pass metabolism; mean ~5-10% for parent naltrexone with the majority of pharmacologic effect coming from 6-beta-naltrexol). IM Vivitrol bypasses first-pass entirely.'"`UNIQ--ref-00000050-QINU`"' (1) · ~62% (1) · ~82% (1)

None (1) · Limited data; avoid (3)

None (1) · Rx, Schedule IV (US) (3)