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Medicines > classes : Anxiolytic or Dissociative

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generic:
None (1) · 2-FDCK (1) · 3-HO-PCE (1) · 3-HO-PCP (1) · 3-MeO-PCE (1) · 3-MeO-PCP (1) · 4-MeO-PCP (1) · Alprazolam (1) · Bromazepam (1) · Chlordiazepoxide (1) · Clorazepate (1) · Deschloroketamine (1) · Dextromethorphan (1) · Dextrorphan (1) · Diphenidine (1) · Duloxetine (1) · Ephenidine (1) · Eticyclidine (1) · Etizolam (1) · Ibogaine (1) · Kava (1) · Meprobamate (1) · Methoxetamine (1) · Metizolam (1) · Nitrous oxide (1) · O-PCE (1) · Oxazepam (1) · Pyrazolam (1) · Salvia divinorum (1) · Salvinorin A (1) · Sertraline (1) · Xenon (1)
brand:
None (21) · Cymbalta, Drizalma Sprinkle, Irenka, Yentreve (1) · DXM (1) · DXO (1) · Lexotan (1) · Librium (1) · Miltown (1) · Serax (1) · Spravato (1) · Tranxene (1) · Xanax (1) · Zoloft (1)
classes: (Click arrow to add another value)
mechanism:
None (1) · Active metabolite of DXM; NMDA antagonist (1) · Contains salvinorin A (1) · GABA-A positive allosteric modulator'"`UNIQ--ref-00000067-QINU`"' '"`UNIQ--vote-00000068-QINU`"' (1) · GABAA modulator; glycine receptor agonist (1) · GABAA positive allosteric modulator (5) · GABAA positive allosteric modulator; low sedation (1) · GABAA positive allosteric modulator; prodrug of desmethyldiazepam (1) · Kappa-opioid agonist; NMDA antagonist; SERT/DAT/NET inhibitor (1) · Kappa-opioid receptor agonist (1) · Kavalactones; GABAA modulator; sigma receptor activity (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) · Serotonin–norepinephrine reuptake inhibition (balanced) (1) · TrkB/BDNF'"`UNIQ--ref-00000084-QINU`"' '"`UNIQ--vote-00000085-QINU`"' (1)
uses:
None (29) · Depression, anxiety, neuropathic pain, fibromyalgia, chronic musculoskeletal pain (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) · '"`UNIQ--vote-00000069-QINU`"', '"`UNIQ--vote-0000006A-QINU`"', '"`UNIQ--vote-0000006B-QINU`"' (1)
starting dose:
None (29) · 0.25 mg (1) · 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 (29) · 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) · 25 mg, 50 mg, 100 mg tablets; oral concentrate 20 mg/mL (1) · 28 mg/device (each dose uses 2 devices) (1)
fda max:
None (29) · 10 mg/d (1) · 200 mg/d (1) · 84 mg per session (1)
routes:
None (28) · Intranasal (under direct medical supervision) (1) · Oral (3)
onset:
None (28) · 30-60 min (immediate-release); 1-2 h (extended-release) (1) · Anxiolysis classically 3-4 weeks, continuing improvement to 8-12 weeks (1) · Mood: 2–4 weeks. Pain: often within 1–2 weeks. (1) · Within hours of first administration (1)
duration:
None (28) · 6 h (immediate-release); ~11 h (extended-release) (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · Chronic daily dosing (1) · Long (1)
halflife:
None (28) · 11-13 h (immediate-release); 11-16 h (extended-release) (1) · ~12 hours (1) · ~26 h (sertraline; range 13-45 h, longer in females); ~62-104 h (N-desmethylsertraline, weakly active) (1) · ~7-12 hours (1)
bioavailability:
None (28) · 80-90% oral (1) · Absolute bioavailability not precisely characterized; food modestly increases exposure (1) · ~48% intranasal (1) · ~50% (highly variable) (1)
pregnancy:
None (28) · Avoid; may cause fetal harm (1) · Category C (1) · Category C'"`UNIQ--ref-0000008F-QINU`"' (1) · Category D'"`UNIQ--ref-0000006C-QINU`"' (1)
legal:
None (28) · Rx, Schedule III (US). REMS program required. (1) · Rx-only (1) · Rx-only in US (1) · Schedule IV (US) (1)

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