Drilldown: Medicines

Bromazolam (1) · Naltrexone (1)

(none, never marketed) (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)

Research material · Classic Psychedelic · Stimulant · Opioid · Sedative-hypnotic · Phenethylamine · Tryptamine · Benzodiazepine · Botanical · [[:Category:Antihypertensives|Antihypertensive]] · Dissociative · Anticonvulsant · Antidepressant · Plant Medicine · Analgesic · Antiparkinsonian · Antipsychotic · Empathogen · Neuroleptic · Cathinone

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None (1) · Positive allosteric modulator of the GABA_A receptor at the benzodiazepine binding site; increases frequency of Cl⁻ channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1)

None (1) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1)

None (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

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)

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)

None · Oral · IV · topical · IM · intranasal · rectal · Subcutaneous · topical ophthalmic · ophthalmic · intramuscular · intravenous · transdermal · vaginal · Subcutaneous (abdomen · sublingual · thigh · inhaled · SC · intra-articular

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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)

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)

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)

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)

None (1) · 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)

None (2)