Drilldown: Medicines

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None (26) · (none, never marketed) (1) · Dalmane (1) · Doral (1) · Doriden (1) · DXM (1) · DXO (1) · Halcion (1) · Hetlioz (1) · Imovane (1) · Lunesta (1) · Mogadon (1) · Nembutal (1) · Placidyl (1) · ProSom (1) · Quaalude (1) · Restoril (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) · Rohypnol (1) · Rozerem (1) · Seconal (1) · Sonata (1) · Spravato (1) · THIP (1) · Versed (1) · Xyrem (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 (4) · Active metabolite of DXM; NMDA antagonist (1) · Contains salvinorin A (1) · Extremely potent GABAA positive allosteric modulator (1) · GABAA positive allosteric modulator (15) · GABAA positive allosteric modulator (non-benzodiazepine) (3) · GABAA positive allosteric modulator; very long half-life (1) · GABAA potentiator (1) · GABAA potentiator and direct activator (2) · GABAB agonist; GHB receptor agonist (1) · Kappa-opioid agonist; NMDA antagonist; SERT/DAT/NET inhibitor (1) · Kappa-opioid receptor agonist (1) · Melatonin receptor agonist (2) · NMDA antagonist (3) · NMDA antagonist; endogenous opioid releaser (1) · NMDA antagonist; fluorinated ketamine analogue (1) · NMDA antagonist; kappa-opioid agonist (1) · NMDA antagonist; ketamine analogue (1) · NMDA antagonist; more stimulating than PCP (1) · NMDA antagonist; opioid agonist (1) · NMDA antagonist; potent opioid agonist (1) · NMDA antagonist; SERT inhibitor; sigma-1 agonist (1) · NMDA antagonist; sigma receptor agonist (2) · NMDA antagonist; sigma receptor agonist; dopaminergic (1) · NMDA antagonist; sigma-1 agonist; serotonin reuptake inhibitor (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) · Selective GABAA agonist (extrasynaptic delta subunit) (1)

None (49) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1) · Treatment-resistant depression (TRD) in adults, as adjunct to oral antidepressant (FDA-approved March 2019). Depressive symptoms in adults with MDD with acute suicidal ideation or behavior (FDA-approved Aug 2020). (1)

None (49) · Induction (TRD): 56 mg intranasal twice weekly × 4 weeks. Maintenance: 56-84 mg once weekly × 4 weeks, then 56-84 mg every 1-2 weeks. For acute suicidality: 84 mg twice weekly × 4 weeks. Administered under medical supervision in REMS-certified site. (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

None (48) · 28 mg/device (each dose uses 2 devices) (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)

None (48) · 50 mg/day oral; 380 mg/4 weeks IM (Vivitrol); 32 mg + 360 mg naltrexone/bupropion daily (Contrave maximum after titration) (1) · 84 mg per session (1) · N/A (never approved) (1)

None (48) · intramuscular (depot) (1) · Intranasal (under direct medical supervision) (1) · intranasal; rectal and IV reported. (1) · Oral (2) · sublingual (1)

None (48) · 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) · Within hours of first administration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)

None (48) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · Oral mu-blockade clinically meaningful for 24-72 hours; IM Vivitrol blockade through 4 weeks. (1)

None (48) · 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) · ~7-12 hours (1)

None (48) · Not formally characterized in humans. (1) · ~48% intranasal (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 (49) · 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) · Avoid; may cause fetal harm (1)

None (50) · Rx, Schedule III (US). REMS program required. (1)