Drilldown: Medicines

None (3) · Doxazosin (1) · Melatonin (N-acetyl-5-methoxytryptamine) (1) · Terazosin (1) · Vardenafil (1)

Belsomra (1) · Cardura, Cardura XL (1) · Dayvigo (1) · Hytrin (US brand discontinued); mostly generic (1) · Levitra, Staxyn (1) · Multiple OTC dietary supplement formulations (1) · Quviviq (1)

Dual orexin receptor antagonist (DORA) (3) · PDE5 Inhibitor (1) · the first approved (1) · [[:Category:Alpha-1_blockers|Alpha-1 adrenergic blocker (non-selective)]] (2) · [[:Category:Antihypertensives|Antihypertensive]] (2) · [[:Category:BPH_treatments|Benign prostatic hyperplasia treatment]] (2) · [[:Category:Chronobiotics|Chronobiotic (circadian phase regulator)]] (1) · [[:Category:Melatonin receptor agonists|Melatonin receptor agonist]] (1) · [[:Category:Sleep aids|Sleep aid]] (1)

None (3) · Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance. (1) · Competitive antagonist at OX1R and OX2R. First-in-class DORA. Receptor dissociation slower than lemborexant or daridorexant. (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-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)

Insomnia (sleep onset and/or maintenance) in adults (FDA-approved August 2014). Also studied for insomnia in mild-moderate Alzheimer disease. (1) · Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) (1) · Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"' (1) · '"`UNIQ--vote-00000669-QINU`"' (1) · '"`UNIQ--vote-00000AAD-QINU`"', '"`UNIQ--vote-00000AAE-QINU`"', '"`UNIQ--vote-00000AAF-QINU`"' (1) · '"`UNIQ--vote-0000111D-QINU`"', '"`UNIQ--vote-0000111E-QINU`"' (1)

0.5-3 mg PO 30-60 minutes before bedtime. Some patients respond to micro-doses (0.3 mg) without additional benefit at higher doses. For circadian phase shifting, timing relative to dim-light melatonin onset matters more than absolute dose (1) · 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 ~1 h before sexual activity (1) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · IR 1 mg PO at bedtime, titrate weekly; XL 4-8 mg PO daily (1)

1, 2, 4, 8 mg IR tablets; 4, 8 mg XL tablets (1) · 1, 2, 5, 10 mg capsules and tablets (1) · 2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) · 25 mg, 50 mg tablets (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · OTC tablets, sublingual tablets, gummies, liquid, extended-release tablets and capsules; common strengths 0.5, 1, 3, 5, 10 mg (1)

10 mg/d (1) · 16 mg/d (IR); 8 mg/d (XL) (1) · 20 mg/d (3) · 50 mg/d (1) · Not formally established (dietary supplement); doses above ~3-5 mg show no additional efficacy but increase next-day sedation risk (1)

Oral (7) · sublingual (1)

None · Hours · 30-60 minutes · 1-2 hours · ~30 min · LDL lowering at 2 weeks, max by 4 weeks · ~1 hour · 15-30 minutes · 15–30 min · 1–2 h · 30–60 min · Antidepressant effect emerges over 1-2 weeks · BP and symptomatic LUTS improvement within 1-2 weeks · BP effect within 1-2 weeks · Clinical improvement within 24-72 hours · Days · Motor improvement over days at therapeutic dose · Over weeks · Postprandial glucose effect within days; HbA1c by 12 weeks · Sleep effect from first dose; antidepressant effect over 1-4 weeks

Other values:

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24 hours (2) · 3-4 hours (1) · 4–5 h (1) · ~7-8 hours (3)

30-50 minutes (short)'"`UNIQ--ref-00000021-QINU`"' (1) · 4–5 h (1) · ~12 hours (1) · ~12 hours'"`UNIQ--ref-0000111F-QINU`"' (1) · ~17-19 hours (longer than daridorexant) (1) · ~22 hours'"`UNIQ--ref-00000AB0-QINU`"' (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

>90% (oral; not significantly affected by food)'"`UNIQ--ref-00001120-QINU`"' (1) · ~15% (extensive hepatic first-pass) (1) · ~15% (oral; highly variable due to extensive and variable first-pass metabolism)'"`UNIQ--ref-00000022-QINU`"' (1) · ~44% (1) · ~62% (1) · ~65% (oral)'"`UNIQ--ref-00000AB1-QINU`"' (1) · ~82% (1)

Category B (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 (3) · Limited data; rarely indicated in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; endogenous hormone, but supplemental pharmacological doses are not well characterized in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

Rx, Schedule IV (US) (3) · Rx-only in US (1) · [[USLegal:Over-the-counter|OTC]] dietary supplement in the US ('''not FDA-regulated as a medicine'''; multiple studies show OTC products contain 50-470% of labeled melatonin content); [[USLegal:Prescription only|Rx-only]] in the EU and UK (1) · [[USLegal:Prescription only|Rx-only]] in US (2)