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Medicines > classes : Research material or [[:Category:AUD medicines|Alcohol use disorder medicine]]

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generic:
brand:
None (130) · (none, never marketed) (1) · O-DSMT (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)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · Monoamine releasing agent (9) · GABAA positive allosteric modulator (8) · CB1/CB2 agonist (7) · Dopamine/norepinephrine reuptake inhibitor (5) · Potent 5-HT2A agonist (5) · LSD analogue; 5-HT2A agonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · Serotonin/norepinephrine/dopamine releasing agent (3) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist (2) · Prodrug of GHB (2)
uses:
None (132) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1)
starting dose:
None (132) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (131) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (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)
fda max:
None (131) · 50 mg/day oral; 380 mg/4 weeks IM (Vivitrol); 32 mg + 360 mg naltrexone/bupropion daily (Contrave maximum after titration) (1) · N/A (never approved) (1)
routes:
None (131) · intramuscular (depot) (1) · intranasal; rectal and IV reported. (1) · Oral (2) · sublingual (1)
onset:
None (131) · 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) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (131) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Oral mu-blockade clinically meaningful for 24-72 hours; IM Vivitrol blockade through 4 weeks. (1)
halflife:
None (131) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · 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)
bioavailability:
None (131) · Not formally characterized in humans. (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)
pregnancy:
None (132) · Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1)
legal:
None (133)

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