Drilldown: Medicines

None (3) · Doxepin (hydrochloride) (1) · Mirtazapine (1) · Nitrofurantoin (1) · Vardenafil (1)

Belsomra (1) · Dayvigo (1) · Levitra, Staxyn (1) · Macrobid (monohydrate/macrocrystals), Macrodantin (macrocrystals), Furadantin (suspension) (1) · Quviviq (1) · Remeron (US brand discontinued; generic widely available), Remeron SolTab (ODT) (1) · Sinequan (oral antidepressant, US brand discontinued), Silenor (low-dose for insomnia), Prudoxin / Zonalon (topical cream) (1)

Dual orexin receptor antagonist (DORA) (3) · PDE5 Inhibitor (1) · the first approved (1) · [[:Category:Antibacterials|Antibacterial]] (1) · [[:Category:Antidepressants|Antidepressant]] (2) · [[:Category:Antihistamines|Antihistamine (potent H1)]] (1) · [[:Category:Nitrofurans|Nitrofuran]] (1) · [[:Category:Sleep aids|Sleep aid (off-label)]] (1) · [[:Category:Sleep aids|Sleep aid (Silenor low-dose)]] (1) · [[:Category:Tetracyclic antidepressants|Tetracyclic antidepressant]] (1) · [[:Category:Tricyclic antidepressants|Tricyclic antidepressant (TCA)]] (1) · [[:Category:Urinary_anti-infectives|Urinary anti-infective]] (1)

None (4) · 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)

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`"' (1) · '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"' (1) · '"`UNIQ--vote-00000669-QINU`"' (1) · '"`UNIQ--vote-000008A1-QINU`"', '"`UNIQ--vote-000008A2-QINU`"' (1)

10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10 mg ~1 h before sexual activity (1) · 100 mg PO BID × 5 days (Macrobid) for cystitis; 50-100 mg HS for chronic prophylaxis (1) · 15 mg PO at bedtime, titrate to 30-45 mg/day after 1-2 weeks. '''Counterintuitive dose paradox''': lower doses (7.5-15 mg) are more sedating than higher doses because H1 antihistamine effect dominates at low dose (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) · Depression: 25-75 mg/day to start, titrate to 75-150 mg/day at bedtime. Insomnia (Silenor): 3 mg PO 30 minutes before bedtime, max 6 mg. Topical (Prudoxin): apply to affected area every 3-4 hours (1)

2.5, 5, 10, 20 mg tabs (Levitra); 10 mg ODT (Staxyn) (1) · 25 mg, 50 mg tablets (1) · 25 mg/5 mL suspension; 25, 50, 100 mg capsules (Macrodantin); 100 mg Macrobid capsule (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · Capsules 10, 25, 50, 75, 100, 150 mg; oral concentrate 10 mg/mL; Silenor tablets 3, 6 mg; topical cream 5% (Prudoxin, Zonalon) (1) · Tablets 7.5, 15, 30, 45 mg; orally disintegrating tablets (SolTab) 15, 30, 45 mg (1)

10 mg/d (1) · 20 mg/d (2) · 300 mg/day (depression, hospitalized); 150 mg/day outpatient; 6 mg/day for insomnia (1) · 400 mg/d (rarely used) (1) · 45 mg/day (1) · 50 mg/d (1)

Oral (7) · topical (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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12 hours (Macrobid) (1) · 24 hours (HS dosing) (2) · 4–5 h (1) · ~7-8 hours (3)

20-40 hours'"`UNIQ--ref-00000023-QINU`"' (1) · 4–5 h (1) · ~12 hours (1) · ~15 hours (parent); nordoxepin active metabolite ~30 hours'"`UNIQ--ref-00000020-QINU`"' (1) · ~17-19 hours (longer than daridorexant) (1) · ~20-60 minutes (plasma; not the relevant kinetic since urinary concentration matters)'"`UNIQ--ref-000008A3-QINU`"' (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

~15% (extensive hepatic first-pass) (1) · ~30% (oral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~44% (1) · ~50% (oral; substantial first-pass)'"`UNIQ--ref-00000024-QINU`"' (1) · ~62% (1) · ~82% (1) · ~90% (oral; food increases absorption)'"`UNIQ--ref-000008A4-QINU`"' (1)

'''Avoid at term (38-42 weeks) and during labor''' (risk of neonatal hemolytic anemia, especially with G6PD deficiency); generally safe in earlier pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Category B (1) · Limited data; avoid (3) · Limited human data; some observational signals reassuring relative to other antidepressants.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · TCA class signal; limited human data specific to doxepin.<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:Prescription only|Rx-only]] in US (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000022-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000025-QINU`"' (1)