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Medicines > classes : Dissociative or Research material or [[:Category:Hormone_replacement_therapy|Hormone replacement therapy]]

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generic:
brand:
None (137) · (none, never marketed) (1) · DXM (1) · DXO (1) · Estrace, Vivelle-Dot, Climara, Divigel, Evamist, Estring, Estraderm, Premarin (CEE, not strictly estradiol) (1) · O-DSMT (1) · Prometrium (oral), Endometrin (vaginal), Crinone (vaginal gel), Prochieve (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-000003B5-QINU`"', '"`UNIQ--vote-000003B6-QINU`"', '"`UNIQ--vote-000003B7-QINU`"', '"`UNIQ--vote-000003B8-QINU`"', '"`UNIQ--vote-000003B9-QINU`"' (1) · '"`UNIQ--vote-00000722-QINU`"', '"`UNIQ--vote-00000723-QINU`"', '"`UNIQ--vote-00000724-QINU`"', '"`UNIQ--vote-00000725-QINU`"' (1)
starting dose:
None (140) · HRT cyclic: 200 mg PO HS days 1-12 of each month; continuous: 100 mg PO daily; ART luteal support 100 mg vaginal TID or 90 mg gel daily (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) · 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 (140) · 28 mg/device (each dose uses 2 devices) (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (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) · Oral 100, 200 mg capsules (peanut oil; check allergy); 100 mg vaginal insert (Endometrin); 4%, 8% vaginal gel (Crinone); IM 50 mg/mL (1)
fda max:
None (140) · 84 mg per session (1) · Indication-dependent; 200-400 mg/d oral typical (1) · Indication-specific; lowest effective dose for shortest duration is the WHI-era standard (1) · N/A (never approved) (1)
routes:
None (140) · cypionate) (1) · IM (estradiol valerate (1) · intramuscular (1) · Intranasal (under direct medical supervision) (1) · intranasal; rectal and IV reported. (1) · Oral (3) · sublingual (1) · transdermal (1) · vaginal (2)
onset:
None (140) · Sedation/dizziness within hours of oral dose; endometrial effects over days (1) · Vasomotor relief 2-4 weeks; bone density gains over months (1) · Within hours of first administration (1) · ~20–40 min PO; faster sublingual/intranasal. (1)
duration:
None (140) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Acute effect ~24 hours; cumulative effect builds with repeated dosing (1) · Oral: 8-12 hours; vaginal: 24+ hours; IM: days (1) · Route- and formulation-dependent (1)
halflife:
None (140) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~13-20 hours (oral); transdermal pharmacokinetics buffer the peaks/troughs of oral dosing'"`UNIQ--ref-000003BA-QINU`"' (1) · ~5-20 hours (oral micronized; highly variable)'"`UNIQ--ref-00000726-QINU`"' (1) · ~7-12 hours (1)
bioavailability:
None (140) · Not formally characterized in humans. (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) · Oral: very low (extensive first-pass); micronization improves uptake somewhat. Vaginal: high local effect with lower systemic levels (first-uterine-pass concentration)'"`UNIQ--ref-00000727-QINU`"' (1) · ~48% intranasal (1)
pregnancy:
None (141) · 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) · 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)
legal:
None (141) · Rx, Schedule III (US). REMS program required. (1) · [[USLegal:Prescription only|Rx-only]] in US (2)

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