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Medicines > classes : Dissociative or Research material or [[:Category:Overactive_bladder_medications|Overactive bladder medication]]

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generic:
brand:
None (137) · (none, never marketed) (1) · Ditropan, Ditropan XL, Oxytrol (transdermal), Gelnique (gel) (1) · DXM (1) · DXO (1) · Myrbetriq (1) · O-DSMT (1) · Spravato (1) · Vesicare (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-000006DE-QINU`"', '"`UNIQ--vote-000006DF-QINU`"', '"`UNIQ--vote-000006E0-QINU`"' (1) · '"`UNIQ--vote-00000C4C-QINU`"', '"`UNIQ--vote-00000C4D-QINU`"' (1) · '"`UNIQ--vote-00000DFC-QINU`"', '"`UNIQ--vote-00000DFD-QINU`"' (1)
starting dose:
None (140) · 25 mg PO once daily; titrate to 50 mg after 4-8 weeks if needed (1) · 5 mg PO once daily; titrate to 10 mg after 2 weeks if 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) · IR 5 mg PO BID-TID; ER 5-10 mg PO daily, titrate; transdermal patch 3.9 mg/d twice weekly (OTC) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)
preparations:
None (140) · 25, 50 mg ER tablets; 8 mg/mL granules for oral suspension (Myrbetriq Granules, pediatric) (1) · 28 mg/device (each dose uses 2 devices) (1) · 5 mg IR tablets; 5, 10, 15 mg ER tablets; 5 mg/5 mL syrup; 3.9 mg/24 h transdermal patch (Oxytrol); 10% topical gel (1) · 5, 10 mg tablets (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (1)
fda max:
None (140) · 10 mg/d (5 mg if severe renal or moderate hepatic impairment, or strong CYP3A4 inhibitors) (1) · 30 mg/d (XL) typical (1) · 50 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) · intravesical (1) · Oral (4) · sublingual (1) · topical gel (1) · transdermal (1)
onset:
None (140) · 30-60 minutes (PO) (1) · Symptom improvement within 1-2 weeks (1) · Symptom improvement within weeks (1) · Within hours of first administration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (140) · 24 hours (2) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · IR: 6-10 hours; ER: 24 hours (1)
halflife:
None (140) · 2-3 hours (parent and active N-desethyl metabolite)'"`UNIQ--ref-000006E1-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~45-68 hours'"`UNIQ--ref-00000DFE-QINU`"' (1) · ~50 hours'"`UNIQ--ref-00000C4E-QINU`"' (1) · ~7-12 hours (1)
bioavailability:
None (140) · 25 mg: ~29%; 50 mg: ~35%; food reduces absorption'"`UNIQ--ref-00000C4F-QINU`"' (1) · Not formally characterized in humans. (1) · ~48% intranasal (1) · ~6% IR oral (substantial first-pass to active N-desethyl metabolite, which contributes most of the antimuscarinic adverse effects); transdermal bypasses first-pass and is better tolerated'"`UNIQ--ref-000006E2-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000DFF-QINU`"' (1)
pregnancy:
None (140) · 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) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (3)
legal:
None (141) · OTC (transdermal patch in women) and [[USLegal:Prescription only|Rx-only]] (other forms) in US (1) · Rx, Schedule III (US). REMS program required. (1) · [[USLegal:Prescription only|Rx-only]] in US (2)

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