Drilldown: Medicines

None (1)

Rexulti (1)

5HT1A activity than aripiprazole (1) · 5HT2A (1) · Atypical antipsychotic (1) · D2/5HT1A partial agonist with stronger α1A (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)

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: 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)

0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets (1)

4 mg/d (schizophrenia); 3 mg/d (AD agitation); 3 mg/d (MDD adjunct) (1)

Oral (1)

Weeks for psychosis/depression; AD agitation benefit emerges over weeks (1)

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

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~91 hours (1)

None · 100% (IV) · ~100% from subcutaneous depot · ~80% (oral)'"`UNIQ--ref-00000027-QINU`"' · 70–90% (oral) · ~100% (oral)'"`UNIQ--ref-0000001C-QINU`"' · ~50% (oral)'"`UNIQ--ref-00000021-QINU`"' · ~95% · '''Saturable''' via the LAT-1 amino-acid transporter, producing nonlinear pharmacokinetics: ~60% at 300 mg single dose, falling to ~35% at 1200 mg single dose'"`UNIQ--ref-0000002A-QINU`"' · 10-20% (oral; reduced by food, calcium, antacids, PPIs, tea/coffee; enhanced by ascorbate) · 100% (IV); essentially complete (oral) · 100% (IV); rapidly neutralized by gastric acid (oral) · 16-21% capsule, 25% suspension (oral; iron and antacids reduce absorption substantially)'"`UNIQ--ref-000009E5-QINU`"' · 25 mg: ~29%; 50 mg: ~35%; food reduces absorption'"`UNIQ--ref-00000C4F-QINU`"' · 30-40% (oral; increases with repeated dosing as gastric pH rises)'"`UNIQ--ref-000000DF-QINU`"' · 40-45% (oral; not significantly affected by food)'"`UNIQ--ref-0000025C-QINU`"' · 40-80% (oral); reduced by food, calcium, iron, PPIs, fiber; take fasting with water'"`UNIQ--ref-00000037-QINU`"' · 42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"' · 50-60% (oral; decreased with food, but food given anyway for GI tolerance)'"`UNIQ--ref-00000019-QINU`"' · 60-70% PO at low doses; saturable at high doses (parenteral routes preferred above 15-25 mg/week)'"`UNIQ--ref-000007C9-QINU`"'

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Limited data; National Pregnancy Registry available (1)

Rx (1)