Cariprazine (Vraylar)
Atypical antipsychotic with D3-preferring D3/D2 partial agonism and 5-HT1A partial agonism; approved for schizophrenia, bipolar I (manic/mixed and depressive episodes), and adjunctive treatment of major depressive disorder. Typical 1.5-6 mg PO once daily. Cariprazine itself is pharmacologically active; it also yields two active metabolites, desmethyl-cariprazine (DCAR) and didesmethyl-cariprazine (DDCAR). DDCAR has an exceptionally long terminal half-life (~2-3 weeks) that dominates total active-moiety exposure at steady state and delays washout markedly. Parent t1/2 ~2-5 days; total active moiety effective t1/2 ~1 week. Oral bioavailability ~52%. CYP3A4 (+CYP2D6) metabolism. Lower metabolic side-effect burden than olanzapine; akathisia and GI effects common.
Projected serum levels — 3 mg, once daily
Maintenance schedule: 3 mg once daily (oral).
Loading schedule: 9 mg on day 1, then 3 mg once daily — reaching therapeutic levels sooner.
Modeled steady state after ~9 days: peak ≈ 7.1 mg, trough ≈ 5.9 mg body load. Population-based estimate over 24 days for a 3 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Antipsychotic
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 3 days
- Common dose
- 3 mg
- Suggested maximum
- 6 mg/day
- Reference dose range
- 1.5–6 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 1.5 mg oral — Cmax 0.010 mg/L at 5.5 h
Documented interactions
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contraindicated
Clarithromycin (Biaxin) + Cariprazine (Vraylar)
Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Cariprazine (Vraylar) AUC by ~5.14x
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contraindicated
Diltiazem + Cariprazine (Vraylar)
Diltiazem mechanism_based of CYP3A4 predicted to change Cariprazine (Vraylar) AUC by ~5.14x
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contraindicated
Efavirenz (Sustiva) + Cariprazine (Vraylar)
Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Cariprazine (Vraylar) AUC by ~0.14x
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contraindicated
Grapefruit (whole fruit) + Cariprazine (Vraylar)
Grapefruit (whole fruit) mechanism_based of CYP3A4 predicted to change Cariprazine (Vraylar) AUC by ~5.14x
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contraindicated
Grapefruit Juice + Cariprazine (Vraylar)
Grapefruit Juice mechanism_based of CYP3A4 predicted to change Cariprazine (Vraylar) AUC by ~5.14x
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contraindicated
Paxlovid (Nirmatrelvir/Ritonavir) + Cariprazine (Vraylar)
Paxlovid (Nirmatrelvir/Ritonavir) mechanism_based of CYP3A4 predicted to change Cariprazine (Vraylar) AUC by ~5.14x
Serum checks 327 modeled interaction pairings for cariprazine (vraylar) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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Clinical pharmacokinetics and pharmacodynamics of the atypical antipsychotic cariprazine
Comprehensive PK review: parent and DCAR/DDCAR metabolite kinetics, ~3-week DDCAR half-life, and implications for dose adjustment and washout.
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Efficacy and safety of low- and high-dose cariprazine in acute and mixed mania associated with bipolar I disorder
Phase 3 RCT establishing cariprazine 3-6 mg/day and 6-12 mg/day efficacy in acute bipolar I manic/mixed episodes.
2 published studies referenced in the app, each with a plain-language summary.