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Medicines > classes : Dissociative or Research material or [[:Category:DMARDs|DMARD]]

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generic:
brand:
None (137) · (none, never marketed) (1) · DXM (1) · DXO (1) · Humira; biosimilars Amjevita, Cyltezo, Hadlima, Hulio, Hyrimoz, Idacio, Yusimry, Abrilada (1) · O-DSMT (1) · Plaquenil; mostly prescribed generically (1) · Spravato (1) · Trexall, Otrexup, Rasuvo, Xatmep, Rheumatrex (discontinued) (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) · None (3) · NMDA antagonist (3) · Serotonin/norepinephrine/dopamine releasing agent (3) · Cathinone analogue; monoamine reuptake inhibitor (2) · Dopamine and norepinephrine reuptake inhibitor (2) · NMDA antagonist; sigma receptor agonist (2) · Prodrug of GHB (2)
uses:
None (141) · 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) · '"`UNIQ--vote-000007C1-QINU`"', '"`UNIQ--vote-000007C2-QINU`"', '"`UNIQ--vote-000007C3-QINU`"', '"`UNIQ--vote-000007C4-QINU`"', '"`UNIQ--vote-000007C5-QINU`"', '"`UNIQ--vote-000007C6-QINU`"', '"`UNIQ--vote-000007C7-QINU`"' (1) · '"`UNIQ--vote-000007E7-QINU`"', '"`UNIQ--vote-000007E8-QINU`"', '"`UNIQ--vote-000007E9-QINU`"', '"`UNIQ--vote-000007EA-QINU`"', '"`UNIQ--vote-000007EB-QINU`"' (1)
starting dose:
None (140) · 200-400 mg PO daily; '''dose by actual body weight ≤5 mg/kg/d''' to reduce retinopathy risk (AAO 2016 guideline) (1) · 40 mg SC every other week (most adult indications); IBD induction 160 mg week 0, 80 mg week 2, then 40 mg every other week (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) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) · Rheumatologic: 7.5-15 mg PO or SC '''once weekly''' (not daily — daily dosing is a recognized fatal error); folic acid 1 mg PO daily on non-MTX days; oncology dosing is far higher and indication-specific (1)
preparations:
None (140) · 2.5 mg tablets; 10-50 mg/mL injection; pre-filled subcutaneous autoinjectors (Otrexup, Rasuvo); 2.5 mg/mL oral solution (Xatmep) (1) · 200 mg tablets; 100 mg/5 mL suspension (1) · 28 mg/device (each dose uses 2 devices) (1) · 40 mg/0.4 mL or 40 mg/0.8 mL prefilled syringe and autoinjector pen; 10, 20, 80 mg pediatric/induction strengths (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (140) · 40 mg every week (selected indications); otherwise 40 mg every other week (1) · 400 mg/d typical maintenance; weight-adjusted ceiling per ophthalmology guidance (1) · 84 mg per session (1) · N/A (never approved) (1) · Rheumatologic ~25 mg/week; oncology indication-specific (1)
routes:
None (140) · intramuscular (1) · Intranasal (under direct medical supervision) (1) · intranasal; rectal and IV reported. (1) · intrathecal (1) · IV (1) · Oral (3) · Subcutaneous (2) · sublingual (1)
onset:
None (140) · Rheumatologic effect at 4-8 weeks; ectopic resolution over 2-3 weeks (1) · Rheumatologic effect at 6-12 weeks (1) · Symptomatic effect within weeks; full response by 12-24 weeks (1) · Within hours of first administration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (140) · 2 weeks per dose (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · Once-weekly dosing in rheumatology (1) · Weeks (long half-life) (1)
halflife:
None (140) · 3-10 hours (low dose); 8-15 hours (high dose); much longer in third-space accumulation (pleural effusion, ascites)'"`UNIQ--ref-000007C8-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~14 days'"`UNIQ--ref-00001103-QINU`"' (1) · ~40 days (terminal; reflects extensive tissue distribution)'"`UNIQ--ref-000007EC-QINU`"' (1) · ~7-12 hours (1)
bioavailability:
None (140) · 60-70% PO at low doses; saturable at high doses (parenteral routes preferred above 15-25 mg/week)'"`UNIQ--ref-000007C9-QINU`"' (1) · 70-75% (oral)'"`UNIQ--ref-000007ED-QINU`"' (1) · Not formally characterized in humans. (1) · ~48% intranasal (1) · ~64% from SC depot'"`UNIQ--ref-00001104-QINU`"' (1)
pregnancy:
None (141) · '''Contraindicated in pregnancy''' (Category X); abortifacient and teratogenic. Discontinuation 3-6 months before conception is standard.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (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) · Avoid; may cause fetal harm (1) · Long-considered safe in pregnancy for lupus and other rheumatologic indications; benefits typically outweigh.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (142) · Rx, Schedule III (US). REMS program required. (1) · [[USLegal:Prescription only|Rx-only]] in US (2)

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