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Medicines > classes : Dissociative or Research material or [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]]

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generic:
brand:
None (137) · (none, never marketed) (1) · Avapro (1) · Benicar (1) · Cozaar (1) · Diovan; Entresto (in fixed-dose combination with sacubitril) (1) · DXM (1) · DXO (1) · Micardis (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) · NMDA antagonist (3) · Serotonin/norepinephrine/dopamine releasing agent (3) · None (2) · 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-000000B8-QINU`"', '"`UNIQ--vote-000000B9-QINU`"', '"`UNIQ--vote-000000BA-QINU`"', '"`UNIQ--vote-000000BB-QINU`"' (1) · '"`UNIQ--vote-000004CA-QINU`"', '"`UNIQ--vote-000004CB-QINU`"', '"`UNIQ--vote-000004CC-QINU`"' (1) · '"`UNIQ--vote-0000056B-QINU`"' (1) · '"`UNIQ--vote-00000840-QINU`"', '"`UNIQ--vote-00000841-QINU`"' (1) · '"`UNIQ--vote-00000AEC-QINU`"', '"`UNIQ--vote-00000AED-QINU`"' (1)
starting dose:
None (140) · 150 mg PO once daily; titrate to 300 mg if needed (1) · 20 mg PO once daily; titrate to 40 mg/d after 2 weeks if needed (1) · 40 mg PO once daily; titrate to 80 mg (1) · 50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1) · 80-160 mg PO once daily (40 mg BID in HFrEF, titrating up to 160 mg BID) (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) · 20, 40, 80 mg tablets (1) · 25 mg, 50 mg, 100 mg tablets (1) · 28 mg/device (each dose uses 2 devices) (1) · 40, 80, 160, 320 mg tablets; oral suspension (1) · 5, 20, 40 mg tablets (1) · 75, 150, 300 mg tablets (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (140) · 100 mg/d (1) · 300 mg/d (1) · 320 mg/d (hypertension); 320 mg/d (HF) (1) · 40 mg/d (1) · 80 mg/d (1) · 84 mg per session (1) · N/A (never approved) (1)
routes:
None (140) · Intranasal (under direct medical supervision) (1) · intranasal; rectal and IV reported. (1) · Oral (6) · sublingual (1)
onset:
None (140) · BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) · BP effect 1-2 weeks; max at 2-3 weeks (1) · BP effect 2 hours; max at 4-6 weeks (1) · BP effect within 1-2 weeks (2) · Within hours of first administration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (140) · 24 hours (5) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1)
halflife:
None (140) · 11-15 hours'"`UNIQ--ref-00000842-QINU`"' (1) · 2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~13 hours'"`UNIQ--ref-0000056C-QINU`"' (1) · ~24 hours (longest of the ARB class; suits patients with morning BP surge)'"`UNIQ--ref-00000AEE-QINU`"' (1) · ~6 hours'"`UNIQ--ref-000004CD-QINU`"' (1) · ~7-12 hours (1)
bioavailability:
None (140) · 42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"' (1) · 60-80% (oral; not significantly affected by food)'"`UNIQ--ref-00000843-QINU`"' (1) · Not formally characterized in humans. (1) · ~25% (oral; food reduces absorption ~40%)'"`UNIQ--ref-000004CE-QINU`"' (1) · ~26% (oral; prodrug hydrolyzed by intestinal esterases to active olmesartan; not affected by food)'"`UNIQ--ref-0000056D-QINU`"' (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) · ~48% intranasal (1)
pregnancy:
None (140) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000004CF-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-0000056E-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000844-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000AF0-QINU`"' (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)
legal:
None (141) · Rx, Schedule III (US). REMS program required. (1) · [[USLegal:Prescription only|Rx-only]] in US (5)

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