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Medicines > classes : Classic Psychedelic or Dissociative or [[:Category:Estrogens|Estrogen]]

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generic:
brand:
None (86) · Delysid (historical, Sandoz, withdrawn 1965) (1) · DXM (1) · DXO (1) · Estrace, Vivelle-Dot, Climara, Divigel, Evamist, Estring, Estraderm, Premarin (CEE, not strictly estradiol) (1) · Spravato (1)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-000003B5-QINU`"', '"`UNIQ--vote-000003B6-QINU`"', '"`UNIQ--vote-000003B7-QINU`"', '"`UNIQ--vote-000003B8-QINU`"', '"`UNIQ--vote-000003B9-QINU`"' (1)
starting dose:
None (89) · 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) · Oral 1-2 mg daily; transdermal patch 0.025-0.05 mg/d twice weekly; transdermal gel 0.5-1 g/d; vaginal 10 mcg tablet twice weekly for GSM. Always combine with a progestogen in patients with an intact uterus. (1)
preparations:
None (89) · 28 mg/device (each dose uses 2 devices) (1) · Oral 0.5, 1, 2 mg tablets; transdermal patches (twice-weekly and once-weekly); 0.06% gel; 1.53 mg/spray topical; vaginal ring (Estring); vaginal tablet (Vagifem/Yuvafem); vaginal cream (1)
fda max:
None (89) · 84 mg per session (1) · Indication-specific; lowest effective dose for shortest duration is the WHI-era standard (1)
routes:
None (88) · cypionate) (1) · IM (estradiol valerate (1) · Intranasal (under direct medical supervision) (1) · Oral (2) · transdermal (1) · vaginal (1)
onset:
None (88) · 30–60 minutes (1) · Vasomotor relief 2-4 weeks; bone density gains over months (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) · Route- and formulation-dependent (1)
halflife:
None (88) · 3–5 hours (1) · ~13-20 hours (oral); transdermal pharmacokinetics buffer the peaks/troughs of oral dosing'"`UNIQ--ref-000003BA-QINU`"' (1) · ~7-12 hours (1)
bioavailability:
None (88) · 70–90% (oral) (1) · Oral ~5% (extensive first-pass to estrone and conjugates); transdermal bypasses first-pass, giving more physiologic estradiol:estrone ratio'"`UNIQ--ref-000003BB-QINU`"' (1) · ~48% intranasal (1)
pregnancy:
None (88) · Avoid; may cause fetal harm (1) · Contraindicated in pregnancy (use is not appropriate during gestation; class label X). Lactation considerations vary by indication.<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 (1)

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