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Medicines > classes : Dissociative or Research material or [[:Category:Loop_diuretics|Loop diuretic]]

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generic:
brand:
None (137) · (none, never marketed) (1) · Bumex (1) · Demadex, Soaanz (1) · DXM (1) · DXO (1) · Lasix (1) · O-DSMT (1) · Spravato (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 (140) · 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-0000021C-QINU`"', '"`UNIQ--vote-0000021D-QINU`"', '"`UNIQ--vote-0000021E-QINU`"', '"`UNIQ--vote-0000021F-QINU`"', '"`UNIQ--vote-00000220-QINU`"', '"`UNIQ--vote-00000221-QINU`"' (1) · '"`UNIQ--vote-00000B42-QINU`"', '"`UNIQ--vote-00000B43-QINU`"', '"`UNIQ--vote-00000B44-QINU`"', '"`UNIQ--vote-00000B45-QINU`"' (1) · '"`UNIQ--vote-00000DDF-QINU`"', '"`UNIQ--vote-00000DE0-QINU`"', '"`UNIQ--vote-00000DE1-QINU`"', '"`UNIQ--vote-00000DE2-QINU`"' (1)
starting dose:
None (140) · 0.5-1 mg PO/IV once or twice daily; titrate to clinical response. Approximate equipotency: bumetanide 1 mg ≈ furosemide 40 mg ≈ torsemide 20 mg (1) · 10-20 mg PO/IV once daily; titrate by clinical response. 1:1 IV to PO conversion (unlike furosemide's 1:2) (1) · 20-40 mg PO/IV; titrate by clinical response. In diuretic-resistant heart failure or CKD, doses to 200 mg or higher may be needed (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)
preparations:
None (140) · 0.5, 1, 2 mg tablets; 0.25 mg/mL IV (1) · 20, 40, 80 mg tablets; 10 mg/mL oral solution; 10 mg/mL IV (1) · 28 mg/device (each dose uses 2 devices) (1) · 5, 10, 20, 100 mg tablets; 10 mg/mL IV (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (140) · 200 mg/d typical practical ceiling (1) · 600 mg/d typical practical ceiling in heart failure (1) · 84 mg per session (1) · N/A (never approved) (1) · ~10 mg/d typical (1)
routes:
None (140) · IM (2) · Intranasal (under direct medical supervision) (1) · intranasal; rectal and IV reported. (1) · IV (3) · Oral (4) · sublingual (1)
onset:
None (140) · IV: 5 minutes; PO: 30-60 minutes (1) · PO 1 hour; IV 10 minutes (1) · PO 30-60 minutes; IV minutes (1) · Within hours of first administration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (140) · 4-6 hours (1) · 6-8 hours (1) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · IV: ~2 hours; PO: 6-8 hours (1)
halflife:
None (140) · 1-1.5 hours'"`UNIQ--ref-00000DE3-QINU`"' (1) · 1.5-2 hours (longer in renal failure)'"`UNIQ--ref-00000222-QINU`"' (1) · 3-4 hours (similar between PO and IV due to high oral bioavailability)'"`UNIQ--ref-00000B46-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~7-12 hours (1)
bioavailability:
None (140) · Not formally characterized in humans. (1) · ~48% intranasal (1) · ~50% (oral; highly variable, 10-100%, hence the standard 1:2 IV-to-PO conversion)'"`UNIQ--ref-00000223-QINU`"' (1) · ~80% (oral; predictable absorption — a substantive practical advantage over furosemide whose oral absorption is 10-100% variable)'"`UNIQ--ref-00000B47-QINU`"' (1) · ~80-95% (oral; more reliable than furosemide, comparable to torsemide)'"`UNIQ--ref-00000DE4-QINU`"' (1)
pregnancy:
None (140) · Avoid where possible; can reduce uteroplacental perfusion and produce neonatal electrolyte disturbance. Reserved for compelling indications.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Avoid where possible; class concerns as for other loop diuretics.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · 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)
legal:
None (141) · Rx, Schedule III (US). REMS program required. (1) · [[USLegal:Prescription only|Rx-only]] in US (3)

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