Drilldown: Medicines
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generic: (Click arrow to add another value)
brand:
classes:
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) ·
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) ·
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)
mechanism:
None (4) ·
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)
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)
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) ·
34 mg PO once daily (1) ·
42 mg PO once daily with food (no titration) (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:
fda max:
routes:
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) ·
Rapid (within 1 week in trials) (1) ·
Typical antidepressant 4-6 week onset (1) ·
Weeks for psychosis/depression; AD agitation benefit emerges over weeks (1)
duration: (Click arrow to add another value)
halflife:
bioavailability:
pregnancy:
Showing below up to 7 results in range #1 to #7.