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Medicines > classes : Benzodiazepine or Dissociative or [[:Category:Schedule III controlled substances|Schedule III controlled substance]]

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generic:
brand:
None (27) · Dalmane (1) · Doral (1) · DXM (1) · DXO (1) · Halcion (1) · Lexotan (1) · Librium (1) · Mogadon (1) · Onfi (1) · ProSom (1) · Restoril (1) · Rohypnol (1) · Serax (1) · Spravato (1) · Tranxene (1) · Versed (1) · Xanax (1)
classes: (Click arrow to add another value)
mechanism:
None (2) · Active metabolite of DXM; NMDA antagonist (1) · Contains salvinorin A (1) · Extremely potent GABAA positive allosteric modulator (1) · GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"' (1) · GABAA positive allosteric modulator (18) · GABAA positive allosteric modulator; low sedation (1) · GABAA positive allosteric modulator; prodrug of desmethyldiazepam (1) · GABAA positive allosteric modulator; very long half-life (1) · Kappa-opioid agonist; NMDA antagonist; SERT/DAT/NET inhibitor (1) · Kappa-opioid receptor agonist (1) · 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)
uses:
None (41) · 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) · '"`UNIQ--vote-0000004B-QINU`"', '"`UNIQ--vote-0000004C-QINU`"', '"`UNIQ--vote-0000004D-QINU`"', '"`UNIQ--vote-0000004E-QINU`"' (1) · '"`UNIQ--vote-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1)
starting dose:
None (42) · 0.25 mg (1) · 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)
preparations:
None (42) · 0.25 mg, 0.5 mg, 1 mg, 2 mg tablets (immediate-release and orally disintegrating); 0.5 mg, 1 mg, 2 mg, 3 mg extended-release tablets; 1 mg/mL oral concentrate (1) · 28 mg/device (each dose uses 2 devices) (1)
fda max:
None (41) · 10 mg/d (1) · 84 mg per session (1) · MOUD: typical effective max 24 mg/day sublingual (doses above offer limited additional mu-occupancy due to ceiling). Pain (Belbuca): 900 mcg every 12 hours. (1)
routes:
None (41) · buccal (Belbuca for pain) (1) · Intranasal (under direct medical supervision) (1) · IV/IM (Buprenex). Oral swallowed: very low bioavailability due to first-pass; not therapeutic. (1) · Oral (1) · SC depot (Sublocade) (1) · Sublingual (primary for MOUD) (1) · transdermal (Butrans) (1)
onset:
None (41) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · Sublingual analgesic effect 30-60 minutes; MOUD craving suppression within hours; Butrans patch steady-state in 3 days. (1) · Within hours of first administration (1)
duration:
None (41) · 6 h (immediate-release); ~11 h (extended-release) (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · MOUD: 24-72 hours per sublingual dose (long; permits every-other-day or three-times-weekly dosing in stable patients); Butrans patch: 7 days; Sublocade depot: 28+ days; Buprenex IV/IM: 6-8 hours. (1)
halflife:
None (41) · 11-13 h (immediate-release); 11-16 h (extended-release) (1) · Buprenorphine sublingual: 24-42 hours (long, contributes to extended dosing intervals). Norbuprenorphine (active metabolite, weaker mu-agonist): 24-48 hours.'"`UNIQ--ref-0000004F-QINU`"' (1) · ~7-12 hours (1)
bioavailability:
None (41) · 80-90% oral (1) · ~30% (sublingual; the primary therapeutic route); ~10-20% (oral swallowed, low due to first-pass); ~50% (buccal Belbuca); transdermal Butrans bypasses first-pass.'"`UNIQ--ref-00000050-QINU`"' (1) · ~48% intranasal (1)
pregnancy:
None (42) · Avoid; may cause fetal harm (1) · Category D'"`UNIQ--ref-0000006C-QINU`"' (1)
legal:
None (42) · Rx, Schedule III (US). REMS program required. (1) · Schedule IV (US) (1)

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