Drilldown: Medicines

None (10) · Amitriptyline (hydrochloride) (1) · Doxepin (hydrochloride) (1) · Mirtazapine (1) · Nortriptyline (hydrochloride) (1) · Omega-3-acid ethyl esters (1)

Belsomra (1) · Caplyta (1) · Dayvigo (1) · Elavil (US brand discontinued; generic widely available), Endep, Tryptizol (1) · Lovaza, Omtryg (1) · Nuplazid (1) · Pamelor (US brand discontinued; generic widely available), Aventyl (1) · Qelbree (1) · Quviviq (1) · REL-1017 / esmethadone (investigational; not yet FDA-approved as of mid-2024) (1) · Remeron (US brand discontinued; generic widely available), Remeron SolTab (ODT) (1) · Rexulti (1) · Sinequan (oral antidepressant, US brand discontinued), Silenor (low-dose for insomnia), Prudoxin / Zonalon (topical cream) (1) · Trintellix (US), Brintellix (formerly) (1) · Viibryd (1)

5HT1A activity than aripiprazole (1) · 5HT2A (1) · 5HT2A/D2 antagonist with proposed differential pre/post-synaptic D2 activity (1) · Atypical antipsychotic (2) · D2/5HT1A partial agonist with stronger α1A (1) · Dual orexin receptor antagonist (DORA) (3) · low-trapping) (1) · Multimodal antidepressant: SERT inhibitor + 5HT1A agonist + 5HT1B partial agonist + 5HT3/5HT7 antagonist (1) · NMDA receptor antagonist (uncompetitive (1) · non-stimulant ADHD agent (1) · secondary amine)]] (1) · Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) (1) · Selective norepinephrine reuptake inhibitor (NRI) with 5HT1A partial agonism (1) · Serotonin partial agonist reuptake inhibitor (SPARI) (1) · the first approved (1) · [[:Category:Antidepressants|Antidepressant]] (4) · [[:Category:Antihistamines|Antihistamine (potent H1)]] (1) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (1) · [[:Category:Migraine prophylactics|Migraine prophylactic]] (2) · [[:Category:Neuropathic pain medicines|Neuropathic pain medicine]] (2) · [[:Category:Omega-3_fatty_acids|Omega-3 fatty acid]] (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:Tricyclic antidepressants|Tricyclic antidepressant (TCA)]] (2)

None (8) · 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) · Partial agonist at D2 and 5HT1A. Antagonist at 5HT2A, α1A, α1B, α2C. More potent 5HT2A antagonism, 5HT1A partial agonism, and α1 antagonism (relative to D2 partial agonism) than aripiprazole, proposed to reduce akathisia and enhance affective/cognitive effects. (1) · Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (1) · Selective NET inhibitor (no significant DAT activity, distinguishes from amphetamine/methylphenidate). Also: 5HT1A receptor partial agonism, 5HT2B and 5HT7 receptor antagonism. The serotonergic actions may underlie better tolerability and possibly different efficacy spectrum than atomoxetine. (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) · '"`UNIQ--vote-0000004E-QINU`"' The EPA+DHA mix is biochemically and clinically distinct from icosapent ethyl'"`UNIQ--ref-0000004F-QINU`"'. (1)

ADHD in children (6+), adolescents, and adults (FDA-approved 2021 for pediatric, 2022 for adult) (1) · Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (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) · Investigational for major depressive disorder; trials underway (phase 3 mixed results) (1) · Major depressive disorder in adults (FDA-approved 2011) (1) · Major depressive disorder in adults (FDA-approved 2013). Notable for evidence of cognitive benefit (processing speed) that distinguishes it from other antidepressants. (1) · Schizophrenia (FDA-approved 2015). Adjunctive treatment of major depressive disorder (2015). '''Agitation associated with dementia due to Alzheimer disease''' (FDA-approved May 2023, first agent specifically approved for this problem). Investigational for PTSD (combined with sertraline). (1) · Schizophrenia (FDA-approved Dec 2019). Bipolar depression as monotherapy or adjunct to lithium/valproate (FDA-approved Dec 2021). (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-00000050-QINU`"' (1)

10 mg PO 30 min before bedtime (with ≥7 hours of sleep planned) (1) · 10 mg PO once daily × 7 days, then 20 mg × 7 days, then 40 mg as target dose (take with food) (1) · 10 mg PO once daily; may increase to 20 mg as tolerated, or decrease to 5 mg if needed (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) · 34 mg PO once daily (1) · 4 g PO daily (as 4 x 1 g capsules once daily, or 2 capsules BID) (1) · 42 mg PO once daily with food (no titration) (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) · Pediatric 6-11: 100 mg PO daily, titrate weekly to max 400 mg. Adolescent 12-17: 200 mg, max 400 mg. Adult: 200 mg, max 600 mg. (1) · Schizophrenia: 1 mg PO daily × 4 days, then 2 mg daily × 3 days, then 4 mg daily. MDD adjunct: 0.5-1 mg daily, increase to 2 mg max. AD agitation: 0.5 mg daily, titrate to 2-3 mg daily. (1) · Trials use 25 mg or 50 mg PO daily (1)

0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1) · 1 g soft gelatin capsules containing ~465 mg EPA + ~375 mg DHA as ethyl esters (1) · 10 mg, 20 mg, 40 mg tablets (1) · 10 mg, 34 mg capsules/tablets (1) · 100 mg, 150 mg, 200 mg extended-release capsules (can be sprinkled on food) (1) · 25 mg, 50 mg tablets (1) · 42 mg capsules (1) · 5 mg, 10 mg tablets (1) · 5 mg, 10 mg, 15 mg, 20 mg tablets (1) · 5 mg, 10 mg, 20 mg tablets (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) · Investigational oral capsule (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) · 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) · 34 mg/d (1) · 4 g/d (1) · 4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct) (1) · 40 mg/d (1) · 400 mg/d (pediatric); 600 mg/d (adult) (1) · 42 mg/d (1) · 45 mg/day (1) · 50 mg/d (1) · Not yet approved (1)

Oral (15) · topical (1)

4-6 weeks for full antidepressant effect (claimed earlier onset for some patients due to 5HT1A partial agonism) (1) · ADHD symptom improvement reported within 1-2 weeks (faster than atomoxetine which takes 4-6 weeks) (1) · Antipsychotic effect over weeks (1) · Benefit over weeks of dosing (1) · Pain and migraine prophylaxis effect 1-4 weeks; antidepressant effect 4-6 weeks (1) · Rapid (within 1 week in trials) (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) · Triglyceride lowering at 2-4 weeks; max at 8 weeks (1) · Typical antidepressant 4-6 week onset (1) · Weeks for psychosis/depression; AD agitation benefit emerges over weeks (1) · ~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) · Amitriptyline 10-50 hours (highly variable); nortriptyline active metabolite 18-44 hours'"`UNIQ--ref-00000026-QINU`"' (1) · Not formally established (1) · Not well characterized; tissue incorporation over weeks'"`UNIQ--ref-00000051-QINU`"' (1) · ~12 hours (1) · ~15 hours (parent); nordoxepin active metabolite ~30 hours'"`UNIQ--ref-00000020-QINU`"' (1) · ~17-19 hours (longer than daridorexant) (1) · ~18 hours (terminal) (1) · ~25 hours (1) · ~57 hours (parent), ~200 h (active metabolite) (1) · ~66 hours (1) · ~7 hours (1) · ~8 hours (shorter than suvorexant and lemborexant) (1) · ~91 hours (1)

Adequate oral bioavailability with extended-release formulation (1) · Improved with food'"`UNIQ--ref-00000052-QINU`"' (1) · Limited but adequate; take with food (1) · Not characterized; oral dosing once daily (1) · Oral bioavailability suitable for daily dosing (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) · ~72% (with food); much lower fasting (~36%) (1) · ~75% (1) · ~82% (1) · ~95% (1)

Investigational (1) · Limited data (1) · Limited data; avoid (4) · Limited data; National Pregnancy Registry available (1) · Limited data; National Pregnancy Registry for Atypical Antipsychotics (1) · Limited data; weigh benefits/risks (2) · 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) · Limited human data<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)

Investigational (1) · Rx (4) · Rx, '''not a controlled substance''' (no DEA scheduling) (1) · Rx, Schedule IV (US) (3) · Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (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`"' (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)