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Medicines > fda max : 20 mg/d or Indication-specific & routes: Oral

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mechanism:
None (4) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (1) · Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · Selective inhibitor of PDE5. Slightly higher PDE5/PDE6 selectivity vs sildenafil (less visual side effect) but more PDE1 cross-activity (occasional QT effects at high doses). (1) · '"`UNIQ--vote-00000860-QINU`"' Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. Unlike prednisone, it does not require hepatic activation, making it the preferred oral choice in severe hepatic dysfunction'"`UNIQ--ref-00000861-QINU`"'. (1) · '"`UNIQ--vote-000008BE-QINU`"' Preferred over prednisone in advanced hepatic dysfunction where hepatic 11β-HSD1 activation is impaired. Liquid formulations are the workhorse pediatric oral corticosteroid for asthma and croup'"`UNIQ--ref-000008BF-QINU`"'. (1) · '"`UNIQ--vote-00001014-QINU`"' Activates the glucocorticoid receptor to broadly remodel inflammatory, immune, and metabolic transcription. The dipropionate, valerate, and augmented dipropionate ester forms determine topical potency (high to super-high)'"`UNIQ--ref-00001015-QINU`"'. (1) · '"`UNIQ--vote-0000111B-QINU`"' Intraoperative floppy iris syndrome is a recognized class effect. Recently emerging evidence (observational) suggests possible Parkinson's disease risk reduction via PGK1 binding — investigational and not a clinical indication'"`UNIQ--ref-0000111C-QINU`"'. (1) · '"`UNIQ--vote-000013EE-QINU`"' Higher-dose Aygestin (5 mg) achieves more reliable ovulation suppression and is used for endometriosis and DUB. POP requires strict daily timing because the 24-hour cervical-mucus effect window is narrower than COC'"`UNIQ--ref-000013EF-QINU`"'. (1)
uses:
Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · Major depressive disorder in adults (FDA-approved 2013). Notable for evidence of cognitive benefit (processing speed) that distinguishes it from other antidepressants. (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) · '"`UNIQ--vote-00000669-QINU`"' (1) · '"`UNIQ--vote-00000862-QINU`"', '"`UNIQ--vote-00000863-QINU`"', '"`UNIQ--vote-00000864-QINU`"', '"`UNIQ--vote-00000865-QINU`"', '"`UNIQ--vote-00000866-QINU`"' (1) · '"`UNIQ--vote-000008C0-QINU`"', '"`UNIQ--vote-000008C1-QINU`"', '"`UNIQ--vote-000008C2-QINU`"', '"`UNIQ--vote-000008C3-QINU`"' (1) · '"`UNIQ--vote-00000ACD-QINU`"', '"`UNIQ--vote-00000ACE-QINU`"', '"`UNIQ--vote-00000ACF-QINU`"', '"`UNIQ--vote-00000AD0-QINU`"' (1) · '"`UNIQ--vote-00000E23-QINU`"', '"`UNIQ--vote-00000E24-QINU`"', '"`UNIQ--vote-00000E25-QINU`"', '"`UNIQ--vote-00000E26-QINU`"', '"`UNIQ--vote-00000E27-QINU`"', '"`UNIQ--vote-00000E28-QINU`"', '"`UNIQ--vote-00000E29-QINU`"', '"`UNIQ--vote-00000E2A-QINU`"' (1) · '"`UNIQ--vote-00000F1B-QINU`"', '"`UNIQ--vote-00000F1C-QINU`"', '"`UNIQ--vote-00000F1D-QINU`"', '"`UNIQ--vote-00000F1E-QINU`"', '"`UNIQ--vote-00000F1F-QINU`"' (1) · '"`UNIQ--vote-00001016-QINU`"', '"`UNIQ--vote-00001017-QINU`"', '"`UNIQ--vote-00001018-QINU`"', '"`UNIQ--vote-00001019-QINU`"' (1) · '"`UNIQ--vote-0000111D-QINU`"', '"`UNIQ--vote-0000111E-QINU`"' (1) · '"`UNIQ--vote-000013F0-QINU`"', '"`UNIQ--vote-000013F1-QINU`"', '"`UNIQ--vote-000013F2-QINU`"', '"`UNIQ--vote-000013F3-QINU`"', '"`UNIQ--vote-000013F4-QINU`"' (1)
starting dose:
1 mg PO at bedtime to limit first-dose syncope; titrate weekly to 5-10 mg (1) · 10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10 mg PO once daily; may increase to 20 mg as tolerated, or decrease to 5 mg if needed (1) · 10 mg ~1 h before sexual activity (1) · 2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · Antenatal: Celestone Soluspan 12 mg IM q24h × 2 doses; topical: pea-sized amount BID; intra-articular varies by joint (1) · Contraception: Depo-Provera 150 mg IM every 13 weeks; Depo-SubQ 104 mg SC every 12-13 weeks; oral cycling: 5-10 mg PO daily ×5-10 days for amenorrhea (1) · Indication-specific: 0.5-9 mg PO/IV daily for inflammation; 4 mg IV q6h for cerebral edema; 40 mg PO once weekly in MM; 6 mg PO/IV daily ×10 days for severe COVID-19; 0.6 mg/kg PO single dose for croup (max 16 mg) (1) · Pediatric 1-2 mg/kg/d (max 60 mg) PO for asthma exacerbation; adult dosing similar to prednisone milligram-for-milligram (~1:1 potency) (1) · Physiologic replacement 15-25 mg/d divided (e.g., 10 mg AM, 5 mg noon, 5 mg afternoon); stress dose 50-100 mg IV q6-8h; adrenal crisis 100 mg IV then 50-100 mg q6h; topical 0.5-2.5% applied 2-4×/d (1) · PO Medrol Dosepak (5-day taper from 24 mg to 4 mg) is the prototypic short-course outpatient regimen; IV pulse 1 g daily for 3-5 days for MS relapse; intra-articular 4-80 mg per joint q1-5 weeks (1) · POP: 0.35 mg PO daily continuously (no placebo week); high-dose 5 mg Aygestin for amenorrhea/endometriosis 5-10 mg/d (1)
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pregnancy:
None (1) · Category B (1) · Category C (1) · Contraindicated in known pregnancy (Aygestin); the 0.35 mg POP is not teratogenic and does not need to be discontinued before conception planning.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Contraindicated in known pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; avoid (1) · Limited data; weigh benefits/risks (1) · Use when benefits outweigh; small association with oral clefts debated.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Use when benefits outweigh; small association with oral clefts in first trimester debated.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Use when benefits outweigh; widely used at physiologic doses for adrenal insufficiency.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Used in antenatal lung maturation (24-34 weeks gestation; 6 mg IM q12h × 4 doses); broader use weighs benefits against fetal HPA suppression.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

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