Drilldown: Medicines
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generic: (Click arrow to add another value)
brand:
Auvelity (dextromethorphan/bupropion ER) (1) ·
Belsomra (1) ·
Caplyta (1) ·
Dayvigo (1) ·
Nuplazid (1) ·
Qelbree (1) ·
Quviviq (1) ·
REL-1017 / esmethadone (investigational; not yet FDA-approved as of mid-2024) (1) ·
Rexulti (1) ·
Sunosi (1) ·
Trintellix (US), Brintellix (formerly) (1) ·
Viibryd (1) ·
Vraylar (1) ·
Wakix (1) ·
Zurzuvae (1)
classes:
5HT1A activity than aripiprazole (1) ·
5HT2A (1) ·
5HT2A/D2 antagonist with proposed differential pre/post-synaptic D2 activity (1) ·
Atypical antipsychotic (3) ·
D2/5HT1A partial agonist with stronger α1A (1) ·
D2/D3/5HT1A partial agonist (1) ·
Dual orexin receptor antagonist (DORA) (3) ·
GABA-A positive allosteric modulator (oral) (1) ·
Histamine H3 receptor inverse agonist / antagonist (1) ·
low-trapping) (1) ·
Multimodal antidepressant: SERT inhibitor + 5HT1A agonist + 5HT1B partial agonist + 5HT3/5HT7 antagonist (1) ·
Neuroactive steroid (1) ·
NMDA receptor antagonist (uncompetitive (1) ·
NMDA receptor antagonist + sigma-1 agonist + NDRI (combination) (1) ·
non-stimulant ADHD agent (1) ·
Norepinephrine-dopamine reuptake inhibitor (NDRI) (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) ·
wake-promoting agent (2)
mechanism:
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 dopamine and norepinephrine reuptake inhibitor (DAT and NET inhibition). Unlike amphetamine, does not significantly release monoamines, pure reuptake inhibition. (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) ·
Synthetic neuroactive steroid (an analog of allopregnanolone), bioavailable orally unlike brexanolone. Positive allosteric modulator at GABA-A receptors including extrasynaptic δ-containing subtypes. (1)
uses:
ADHD in children (6+), adolescents, and adults (FDA-approved 2021 for pediatric, 2022 for adult) (1) ·
Excessive daytime sleepiness in adults with narcolepsy or obstructive sleep apnea (OSA) (1) ·
Excessive daytime sleepiness or cataplexy in adults with narcolepsy (FDA-approved August 2019) (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) ·
Major depressive disorder in adults (FDA-approved August 2022) (1) ·
Postpartum depression (PPD) in adults (FDA-approved 2023) (1) ·
Schizophrenia (FDA-approved 2015). Acute manic or mixed episodes of bipolar I disorder. Bipolar I depression (FDA-approved 2019). Adjunctive treatment of major depressive disorder (FDA-approved Dec 2022). (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)
starting dose:
1 tablet (dextromethorphan 45 mg / bupropion 105 mg) PO daily × 3 days, then increase to 1 tablet BID (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) ·
25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) ·
34 mg PO once daily (1) ·
42 mg PO once daily with food (no titration) (1) ·
5 mg PO at bedtime; may increase to 10 mg if inadequate (1) ·
50 mg PO once daily with fatty food in the evening × 14 days (1) ·
Narcolepsy: 75 mg PO once daily upon awakening, titrate every 3 days. OSA: 37.5 mg PO once daily, titrate. (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) ·
Schizophrenia: 1.5 mg PO daily, increase to 1.5-6 mg as tolerated. Bipolar mania: 1.5 mg, may increase to 3-6 mg. Bipolar depression: 1.5 mg daily for 14 days, then 3 mg. MDD adjunct: 1.5 mg, may increase to 3 mg. (1) ·
Trials use 25 mg or 50 mg PO daily (1) ·
Week 1: 8.9 mg PO once daily in the morning. Week 2: 17.8 mg. Week 3+: 35.6 mg (max). Titrate as needed. (1)
preparations:
0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1) ·
1.5 mg, 3 mg, 4.5 mg, 6 mg capsules (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) ·
20 mg, 25 mg, 30 mg capsules (1) ·
25 mg, 50 mg tablets (1) ·
4.45 mg, 17.8 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) ·
75 mg, 150 mg tablets (1) ·
Dextromethorphan 45 mg + bupropion 105 mg ER tablets (1) ·
Investigational oral capsule (1)
fda max:
10 mg/d (1) ·
150 mg/d (1) ·
2 tablets/day (dextromethorphan 90 mg / bupropion 210 mg) (1) ·
20 mg/d (2) ·
34 mg/d (1) ·
35.6 mg/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) ·
50 mg/d (1) ·
50 mg/d × 14 d (1) ·
6 mg/d (psychosis/mania); 3 mg/d (depression adjunct) (1) ·
Not yet approved (1)
routes: (Click arrow to add another value)
onset:
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) ·
Day 3 of dosing in trials; sustained through day 45 (1) ·
Rapid (within 1 week in trials) (1) ·
Significant antidepressant response by week 1 in trials (faster than monoaminergic antidepressants which take 4-6 weeks) (1) ·
Typical antidepressant 4-6 week onset (1) ·
Wake-promoting effect over weeks of titration (1) ·
Weeks for psychosis/depression; AD agitation benefit emerges over weeks (1) ·
Weeks for psychosis/mood efficacy (1) ·
~30 min (3) ·
~30-60 min (1)
duration:
halflife:
Cariprazine ~2-4 d; major active metabolites desmethyl-cariprazine (DCAR) ~1-3 weeks → 'oral depot' effect with delayed steady-state and reduced effect of missed doses (1) ·
Dextromethorphan ~22 h (when CYP2D6 inhibited); bupropion ~21 h (1) ·
Not formally established (1) ·
~12 hours (1) ·
~16-23 hours (1) ·
~17-19 hours (longer than daridorexant) (1) ·
~18 hours (terminal) (1) ·
~20 hours (1) ·
~25 hours (1) ·
~57 hours (parent), ~200 h (active metabolite) (1) ·
~66 hours (1) ·
~7 hours (1) ·
~7.1 hours (1) ·
~8 hours (shorter than suvorexant and lemborexant) (1) ·
~91 hours (1)
bioavailability:
Adequate (food-dependent, must take with fatty meal) (1) ·
Adequate oral bioavailability (1) ·
Adequate oral bioavailability with extended-release formulation (1) ·
Limited but adequate; take with food (1) ·
Not characterized; oral dosing once daily (1) ·
Not formally characterized for the combination (1) ·
Not formally established; oral once-daily adequate (1) ·
Oral bioavailability suitable for daily dosing (1) ·
~44% (1) ·
~62% (1) ·
~72% (with food); much lower fasting (~36%) (1) ·
~75% (1) ·
~82% (1) ·
~95% (2)
pregnancy:
Investigational (1) ·
Limited data (2) ·
Limited data; avoid (5) ·
Limited data; avoid in pregnancy. Lactation: present in milk; consider risks (1) ·
Limited data; National Pregnancy Registry available (1) ·
Limited data; National Pregnancy Registry for Atypical Antipsychotics (1) ·
Limited data; pitolisant may reduce hormonal contraceptive efficacy (1) ·
Limited data; pregnancy exposure registry available (1) ·
Limited data; weigh benefits/risks (2)
legal:
Investigational (1) ·
Rx (6) ·
Rx, '''not a controlled substance''' (no DEA scheduling) (1) ·
Rx, '''not a controlled substance''' (unique among wake-promoting agents) (1) ·
Rx, Schedule IV (US) (5) ·
Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1)
Showing below up to 15 results in range #1 to #15.