Drilldown: Medicines

Naltrexone (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)

[[: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 (1)

None (1)

None (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)

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 (1)

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)

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

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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)

~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)

None (1)

None (1)