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Medicines > routes : IV infusion (60 min) every 2 weeks; outpatient or infusion-center setting or Oral & pregnancy: Limited data

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generic:
None (3)
brand:
Leqembi (1) · Qelbree (1) · Vraylar (1)
classes:
Anti-amyloid beta (Aβ) monoclonal antibody (1) · Atypical antipsychotic (1) · D2/D3/5HT1A partial agonist (1) · non-stimulant ADHD agent (1) · Selective norepinephrine reuptake inhibitor (NRI) with 5HT1A partial agonism (1) · targets protofibrils (1)
mechanism:
None (2) · 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) · Alzheimer disease (MCI or mild dementia stage); FDA accelerated approval Jan 2023 → traditional approval July 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)
starting dose:
10 mg/kg IV every 2 weeks (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: 1.5 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)
preparations:
1.5 mg, 3 mg, 4.5 mg, 6 mg capsules (1) · 100 mg, 150 mg, 200 mg extended-release capsules (can be sprinkled on food) (1) · 200 mg/2 mL, 500 mg/5 mL vials for IV infusion (1)
fda max:
10 mg/kg q2w (1) · 400 mg/d (pediatric); 600 mg/d (adult) (1) · 6 mg/d (psychosis/mania); 3 mg/d (depression adjunct) (1)
routes: (Click arrow to add another value)
onset:
ADHD symptom improvement reported within 1-2 weeks (faster than atomoxetine which takes 4-6 weeks) (1) · Slowing of cognitive decline over 18 months (modest effect, ~27% relative slowing) (1) · Weeks for psychosis/mood efficacy (1)
duration:
Daily dosing (1) · Daily dosing; active metabolites with very long half-lives (up to 1-3 weeks) (1) · Ongoing dosing (1)
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) · ~5-7 days (1) · ~7 hours (1)
bioavailability:
100% (IV) (1) · Adequate oral bioavailability (1) · Adequate oral bioavailability with extended-release formulation (1)
pregnancy: (Click arrow to add another value)
legal:
Rx (1) · Rx, '''not a controlled substance''' (no DEA scheduling) (1) · Rx; REMS-like program for ARIA monitoring (1)

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