Drilldown: Medicines

None (3) · Amitriptyline (hydrochloride) (1) · Bisoprolol (1) · Doxepin (hydrochloride) (1) · Memantine ER / Donepezil (1) · Mirtazapine (1) · Nebivolol (1) · Nortriptyline (hydrochloride) (1)

Belsomra (1) · Bystolic (1) · Dayvigo (1) · Elavil (US brand discontinued; generic widely available), Endep, Tryptizol (1) · Namzaric (1) · Pamelor (US brand discontinued; generic widely available), Aventyl (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) · Zebeta (1)

Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · Combined cholinesterase inhibitor + NMDA antagonist (1) · Dual orexin receptor antagonist (DORA) (3) · secondary amine)]] (1) · the first approved (1) · [[:Category:Antidepressants|Antidepressant]] (4) · [[:Category:Antihistamines|Antihistamine (potent H1)]] (1) · [[:Category:Migraine prophylactics|Migraine prophylactic]] (2) · [[:Category:Neuropathic pain medicines|Neuropathic pain medicine]] (2) · [[: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:Tricyclic antidepressants|Tricyclic antidepressant (TCA)]] (2)

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) · Donepezil: reversible AChE inhibitor, increases synaptic acetylcholine. Memantine: uncompetitive low-affinity NMDA receptor antagonist, dampens pathological glutamate overactivation while preserving normal synaptic signaling. Targets two distinct mechanisms in Alzheimer's. (1) · Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. (1) · '"`UNIQ--vote-00000019-QINU`"' Therapeutic plasma-level monitoring is standard practice for TCAs given the narrow therapeutic index and the established plasma-level-efficacy correlation. CYP2D6 substrate; CPIC PGx guidance applies for dose individualization'"`UNIQ--ref-0000001A-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`"' (2) · '"`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-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (1) · '"`UNIQ--vote-00000468-QINU`"' (1) · '"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1)

10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (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) · 2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 5 mg daily (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · Depression (rarely used now): 25-75 mg PO at bedtime, titrate to 150 mg/day. Neuropathic pain / migraine prophylaxis: 10-25 mg at bedtime, titrate by 10-25 mg weekly to 50-100 mg/day. Elderly: 10 mg at bedtime (Beers-list cautions apply) (1) · Depression: 25 mg PO TID-QID or 75 mg at bedtime, titrate to 75-150 mg/day. Neuropathic pain: 10-25 mg at bedtime, titrate to 50-100 mg/day. Elderly: 10 mg at bedtime (Beers-list cautions, though less than amitriptyline) (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) · For patients already stable on memantine 28 mg/d + donepezil 10 mg/d, switch to one capsule daily of equivalent strength (1)

2.5, 5, 10, 20 mg tabs (1) · 25 mg, 50 mg tablets (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · 5, 10 mg tabs (1) · 7/10, 14/10, 21/10, 28/10 mg ER capsules (memantine ER / donepezil) (1) · Capsules 10, 25, 50, 75 mg; oral solution 10 mg/5 mL (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 10, 25, 50, 75, 100, 150 mg (1) · Tablets 7.5, 15, 30, 45 mg; orally disintegrating tablets (SolTab) 15, 30, 45 mg (1)

10 mg/d (1) · 150 mg/day; therapeutic plasma-level monitoring recommended (target 50-150 ng/mL window) (1) · 20 mg/d (2) · 28/10 mg/d (1) · 300 mg/day (depression, hospitalized); 150 mg/day outpatient; 6 mg/day for insomnia (1) · 300 mg/day (historical hospitalized inpatient depression); 150 mg/day outpatient typical ceiling (1) · 40 mg/d (1) · 45 mg/day (1) · 50 mg/d (1)

Oral (9) · Oral (capsule whole or opened/sprinkled on applesauce) (1) · topical (1)

1–2 h (2) · Component effects accumulate over weeks (1) · Pain and migraine prophylaxis effect 1-4 weeks; antidepressant effect 4-6 weeks (1) · Sleep effect from first dose; analgesic and migraine-prophylaxis effect 1-4 weeks; antidepressant effect 4-6 weeks (1) · Sleep effect from first dose; antidepressant effect over 1-4 weeks (2) · ~30 min (3)

None · 24 hours · 4-6 hours · 12 hours · 6-8 hours · Daily dosing · 8-12 hours · 12-24 hours · Hours · Hours per application · 24 hours (HS dosing) · 24 hours (once-daily dosing) · 24 h · N/A · N/A (replacement) · Variable · ~7-8 hours · 3-5 hours · 4-6 hours (IR); 24 hours (ER) · 6-12 hours

Other values:

Search

18-44 hours'"`UNIQ--ref-00000020-QINU`"' (1) · 20-40 hours'"`UNIQ--ref-00000023-QINU`"' (1) · 9–12 h (1) · Amitriptyline 10-50 hours (highly variable); nortriptyline active metabolite 18-44 hours'"`UNIQ--ref-00000026-QINU`"' (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1) · ~12 hours (1) · ~15 hours (parent); nordoxepin active metabolite ~30 hours'"`UNIQ--ref-00000020-QINU`"' (1) · ~17-19 hours (longer than daridorexant) (1) · ~60–80 h (memantine); ~70 h (donepezil) (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

~100% both components (1) · ~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~30% (oral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~44% (1) · ~50% (oral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~50% (oral)'"`UNIQ--ref-00000027-QINU`"' (1) · ~50% (oral; substantial first-pass)'"`UNIQ--ref-00000024-QINU`"' (1) · ~62% (1) · ~82% (1) · ~90% (low first-pass) (1)

Category C (2) · 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) · Not relevant (geriatric problem) (1) · Older agent with substantial use experience; observational signals not clearly causal.<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) · TCA class signal; limited human data specific to nortriptyline.<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 (3) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000022-QINU`"' (2) · [[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) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000028-QINU`"' (1)