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Medicines > classes: D2/5HT1A partial agonist with stronger α1A & duration : Daily dosing or N/A (replacement)

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generic:
None (1)
brand:
Rexulti (1)
classes: (Click arrow to add another value)
mechanism:
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)
uses:
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)
starting dose:
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)
preparations:
0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1)
fda max:
4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct) (1)
routes:
Oral (1)
onset:
Weeks for psychosis/depression; AD agitation benefit emerges over weeks (1)
duration: (Click arrow to add another value)
halflife:
~91 hours (1)
bioavailability:
~95% (1)
pregnancy:
Limited data; National Pregnancy Registry available (1)
legal:
Rx (1)

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