Drilldown: Medicines
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generic:
brand:
Alphagan P (ophthalmic glaucoma), Mirvaso (topical rosacea) (1) ·
Caplyta (1) ·
Ceftin (oral), Zinacef (IV) (1) ·
Cipro, Cipro XR, Ciloxan (ophthalmic) (1) ·
Elavil (US brand discontinued; generic widely available), Endep, Tryptizol (1) ·
Flagyl, Metrocream, Metrogel, Metrogel-Vaginal, Noritate (1) ·
Imodium, Imodium A-D (1) ·
Lovaza, Omtryg (1) ·
Nuplazid (1) ·
Pamelor (US brand discontinued; generic widely available), Aventyl (1) ·
Qelbree (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) ·
Zaditor, Alaway (ophthalmic, OTC); Zaditen (systemic, outside US) (1)
classes:
mechanism:
None (12) ·
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) ·
'"`UNIQ--vote-00001284-QINU`"' Systemic oral ketotifen (available outside US) has historical use for asthma adjunct therapy via the same dual mechanism, but oral use produces sedation and weight gain — the topical ophthalmic application largely avoids both'"`UNIQ--ref-00001285-QINU`"'. (1)
uses:
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) ·
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) ·
'"`UNIQ--vote-00000932-QINU`"', '"`UNIQ--vote-00000933-QINU`"', '"`UNIQ--vote-00000934-QINU`"', '"`UNIQ--vote-00000935-QINU`"', '"`UNIQ--vote-00000936-QINU`"', '"`UNIQ--vote-00000937-QINU`"' (1) ·
'"`UNIQ--vote-00000BE3-QINU`"', '"`UNIQ--vote-00000BE4-QINU`"', '"`UNIQ--vote-00000BE5-QINU`"', '"`UNIQ--vote-00000BE6-QINU`"', '"`UNIQ--vote-00000BE7-QINU`"', '"`UNIQ--vote-00000BE8-QINU`"', '"`UNIQ--vote-00000BE9-QINU`"', '"`UNIQ--vote-00000BEA-QINU`"' (1) ·
'"`UNIQ--vote-00000FCF-QINU`"', '"`UNIQ--vote-00000FD0-QINU`"', '"`UNIQ--vote-00000FD1-QINU`"' (1) ·
'"`UNIQ--vote-00000FF3-QINU`"', '"`UNIQ--vote-00000FF4-QINU`"', '"`UNIQ--vote-00000FF5-QINU`"', '"`UNIQ--vote-00000FF6-QINU`"', '"`UNIQ--vote-00000FF7-QINU`"', '"`UNIQ--vote-00000FF8-QINU`"' (1) ·
'"`UNIQ--vote-000010CE-QINU`"', '"`UNIQ--vote-000010CF-QINU`"', '"`UNIQ--vote-000010D0-QINU`"' (1) ·
'"`UNIQ--vote-00001286-QINU`"' (1)
starting dose:
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) ·
250-500 mg PO BID × 7-14 days; IV 1.5 g q8h for serious infections (1) ·
34 mg PO once daily (1) ·
4 g PO daily (as 4 x 1 g capsules once daily, or 2 capsules BID) (1) ·
4 mg PO initially, then 2 mg after each loose stool, '''not to exceed 16 mg/d''' (8 mg OTC); chronic-use lower (1) ·
42 mg PO once daily with food (no titration) (1) ·
500 mg PO TID × 7-10 days (most indications); 2 g single dose for trichomoniasis; 500 mg IV q8h for severe anaerobic infection; rectal 1 g BID (1) ·
500-750 mg PO BID; 400 mg IV q8-12h (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) ·
Ophthalmic 1 drop in affected eye(s) TID; topical Mirvaso 0.33% gel applied to face daily (1) ·
Ophthalmic 1 drop in each eye every 8-12 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)
preparations:
0.025%, 0.035% ophthalmic solutions (1) ·
0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza) (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) ·
125, 250, 500 mg tablets; 125 mg/5 mL, 250 mg/5 mL suspension; 750 mg, 1.5 g IV vials (1) ·
2 mg capsules and tablets; 1 mg/5 mL oral solution; combined with simethicone (Imodium Multi-Symptom) (1) ·
250, 500 mg tablets; 750 mg ER; 500 mg/100 mL IV; 0.75-1% topical gel/cream; 0.75% vaginal gel; suppository (1) ·
250, 500, 750 mg IR tablets; 500, 1000 mg ER tablets (XR); 250, 500 mg/5 mL oral suspension; 200, 400 mg IV; 0.3% ophthalmic solution and ointment; 0.2% otic (1) ·
42 mg capsules (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)
fda max:
1 drop per eye q8-12h (1) ·
1 g/d (oral); 6 g/d (IV) (1) ·
150 mg/day; therapeutic plasma-level monitoring recommended (target 50-150 ng/mL window) (1) ·
16 mg/d (8 mg/d OTC) (1) ·
20 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) ·
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) ·
Not yet approved (1) ·
TID per eye (1) ·
~1500 mg/d (oral); 1200 mg/d (IV) (1) ·
~4 g/d (severe systemic infection) (1)
routes:
onset:
30-60 minutes (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) ·
Hours (3) ·
IOP lowering at 1 hour; max at 2-3 hours (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) ·
Within minutes (1)
duration: (Click arrow to add another value)
halflife:
18-44 hours'"`UNIQ--ref-00000020-QINU`"' (1) ·
20-40 hours'"`UNIQ--ref-00000023-QINU`"' (1) ·
4 hours'"`UNIQ--ref-00000938-QINU`"' (1) ·
6-8 hours'"`UNIQ--ref-00000BEB-QINU`"' (1) ·
Amitriptyline 10-50 hours (highly variable); nortriptyline active metabolite 18-44 hours'"`UNIQ--ref-00000026-QINU`"' (1) ·
Not formally established (1) ·
Not meaningfully described for ophthalmic use'"`UNIQ--ref-00001287-QINU`"' (1) ·
Not well characterized; tissue incorporation over weeks'"`UNIQ--ref-00000051-QINU`"' (1) ·
~1.5 hours'"`UNIQ--ref-00000FF9-QINU`"' (1) ·
~15 hours (parent); nordoxepin active metabolite ~30 hours'"`UNIQ--ref-00000020-QINU`"' (1) ·
~18 hours (terminal) (1) ·
~25 hours (1) ·
~3 hours'"`UNIQ--ref-000010D1-QINU`"' (1) ·
~57 hours (parent), ~200 h (active metabolite) (1) ·
~66 hours (1) ·
~7 hours (1) ·
~9-14 hours'"`UNIQ--ref-00000FD2-QINU`"' (1) ·
~91 hours (1)
bioavailability:
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) ·
Topical with minimal systemic absorption'"`UNIQ--ref-00001288-QINU`"' (1) ·
Topical; clinically meaningful systemic absorption can produce systemic α2 effects (somnolence, hypotension), especially in children'"`UNIQ--ref-000010D2-QINU`"' (1) ·
~0.3% (oral; extensive first-pass via CYP3A4 and P-glycoprotein-mediated efflux at the intestinal and blood-brain barriers limit systemic and CNS exposure at therapeutic doses)'"`UNIQ--ref-00000FD3-QINU`"' (1) ·
~30% (oral)'"`UNIQ--ref-00000021-QINU`"' (1) ·
~37% (oral, as axetil prodrug; food modestly improves absorption)'"`UNIQ--ref-00000FFA-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) ·
~70% (oral; reduced by divalent cations — antacids, iron, calcium, dairy)'"`UNIQ--ref-00000939-QINU`"' (1) ·
~72% (with food); much lower fasting (~36%) (1) ·
~75% (1) ·
~80% (oral)'"`UNIQ--ref-00000BEC-QINU`"' (1) ·
~95% (1)
pregnancy:
'''Avoid in pregnancy where alternatives exist''' (animal cartilage toxicity; class-wide concern); use only when benefit clearly outweighs.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Generally considered acceptable when needed.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Generally considered safe (minimal systemic exposure).<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Generally considered safe after the first trimester; first-trimester use weighed against indication.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Generally considered safe in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Investigational (1) ·
Limited data (1) ·
Limited data.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited data; avoid (1) ·
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.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited human data<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Older agent with substantial use experience; observational signals not clearly causal.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
TCA class signal; limited human data specific to doxepin.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
TCA class signal; limited human data specific to nortriptyline.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
legal:
None (1) ·
Investigational (1) ·
OTC in US (2) ·
Rx (4) ·
Rx, '''not a controlled substance''' (no DEA scheduling) (1) ·
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 (4) ·
[[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)
Showing below up to 18 results in range #1 to #18.