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Medicines > classes : Classic Psychedelic or Dissociative or [[:Category:Azapirones|Azapirone]]

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generic:
brand:
None (86) · Buspar (US brand discontinued; generic widely available) (1) · Delysid (historical, Sandoz, withdrawn 1965) (1) · DXM (1) · DXO (1) · Spravato (1)
classes: (Click arrow to add another value)
mechanism:
5-HT2A agonist (26) · Potent 5-HT2A agonist (5) · LSD analogue; 5-HT2A agonist (4) · Prodrug of LSD; 5-HT2A agonist (4) · NMDA antagonist (3) · None (2) · Contains LSA (2) · Contains mescaline (2) · NMDA antagonist; sigma receptor agonist (2)
uses:
None (89) · 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-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"', '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"' (1)
starting dose:
None (89) · 5 mg PO TID or 7.5 mg PO BID; titrate by 5 mg every 2-3 days to clinical effect, commonly 30-60 mg/day divided BID-TID (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 (89) · 28 mg/device (each dose uses 2 devices) (1) · Tablets 5, 7.5, 10, 15, 30 mg (the 15 and 30 mg tablets are scored for halving and quartering) (1)
fda max:
None (89) · 60 mg/day (1) · 84 mg per session (1)
routes:
None (88) · Intranasal (under direct medical supervision) (1) · Oral (2)
onset:
None (88) · '''Anxiolytic effect emerges over 2-4 weeks'''; buspirone does NOT work for acute anxiety, which is the central teaching point and the most common cause of treatment failure (1) · 30–60 minutes (1) · Within hours of first administration (1)
duration:
None (88) · 8–12 hours (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · ~8 hours (TID dosing) (1)
halflife:
None (88) · 3–5 hours (1) · Buspirone 2-3 hours; 1-PP active metabolite 4-6 hours'"`UNIQ--ref-0000001D-QINU`"' (1) · ~7-12 hours (1)
bioavailability:
None (88) · 70–90% (oral) (1) · ~4% (extensive first-pass metabolism)'"`UNIQ--ref-0000001E-QINU`"' (1) · ~48% intranasal (1)
pregnancy:
None (88) · Avoid; may cause fetal harm (1) · Limited human data; older agent with substantial use experience and no clear teratogenic signal.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Not established (1)
legal:
None (88) · Rx, Schedule III (US). REMS program required. (1) · Schedule I (United States) (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, which is a meaningful clinical advantage over benzodiazepine alternatives for chronic anxiety'"`UNIQ--ref-0000001F-QINU`"' (1)

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