Drilldown: Medicines

Amitriptyline (hydrochloride) (1) · Doxepin (hydrochloride) (1) · Melatonin (N-acetyl-5-methoxytryptamine) (1) · Mirtazapine (1) · Nortriptyline (hydrochloride) (1)

Elavil (US brand discontinued; generic widely available), Endep, Tryptizol (1) · Multiple OTC dietary supplement formulations (1) · Pamelor (US brand discontinued; generic widely available), Aventyl (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)

secondary amine)]] (1) · [[:Category:Antidepressants|Antidepressant]] (4) · [[:Category:Antihistamines|Antihistamine (potent H1)]] (1) · [[:Category:Chronobiotics|Chronobiotic (circadian phase regulator)]] (1) · [[:Category:Melatonin receptor agonists|Melatonin receptor agonist]] (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:Sleep aids|Sleep aid]] (1) · [[:Category:Tetracyclic antidepressants|Tetracyclic antidepressant]] (1) · [[:Category:Tricyclic antidepressants|Tricyclic antidepressant (TCA (1) · [[:Category:Tricyclic antidepressants|Tricyclic antidepressant (TCA)]] (2)

None (4) · '"`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)

'"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (2) · '"`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-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)

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) · 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) · 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)

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) · OTC tablets, sublingual tablets, gummies, liquid, extended-release tablets and capsules; common strengths 0.5, 1, 3, 5, 10 mg (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)

150 mg/day; therapeutic plasma-level monitoring recommended (target 50-150 ng/mL window) (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) · 45 mg/day (1) · Not formally established (dietary supplement); doses above ~3-5 mg show no additional efficacy but increase next-day sedation risk (1)

Oral (5) · sublingual (1) · topical (1)

30-60 minutes (immediate-release oral) (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)

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) · 30-50 minutes (short)'"`UNIQ--ref-00000021-QINU`"' (1) · Amitriptyline 10-50 hours (highly variable); nortriptyline active metabolite 18-44 hours'"`UNIQ--ref-00000026-QINU`"' (1) · ~15 hours (parent); nordoxepin active metabolite ~30 hours'"`UNIQ--ref-00000020-QINU`"' (1)

~15% (oral; highly variable due to extensive and variable first-pass metabolism)'"`UNIQ--ref-00000022-QINU`"' (1) · ~30% (oral)'"`UNIQ--ref-00000021-QINU`"' (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)

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) · 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) · 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)

[[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. 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)