| Schizophrenia in adults View labelExact | Standard titration: 50/20 mg BID (Days 1-2) → 100/20 mg BID (Days 3-7) → 125/30 mg BID (Day 8 onward). Maximum dose 125/30 mg twice daily. | First-in-class muscarinic M1/M4 receptor agonist (xanomeline) combined with peripheral muscarinic antagonist (trospium chloride) for schizophrenia; does not block dopamine D2 receptors. | CYP2D6, CYP2B6, CYP1A2, FMO1, FMO3 | Single-dose mean 5 h; Steady-state mean 5 h | No | — | - Metabolic: weight/BMI, fasting glucose/HbA1c, and lipids (baseline and periodic).
| No | 2026-03-13 |
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| Schizophrenia; acute manic or mixed episodes of bipolar I disorder (monotherapy or adjunct to lithium/valproate); maintenance therapy via LAI formulations; adjunctive treatment of major depressive disorder; irritability in autistic disorder; Tourette disorder. View labelExact | Schizophrenia (adults): start 10–15 mg once daily; therapeutic range 10–30 mg/day. Doses above 30 mg rarely add benefit. | Dopamine D2/D3 partial agonist with 5-HT1A partial agonism and 5-HT2A antagonism, stabilizing dopaminergic tone with comparatively low metabolic and EPS burden.
| CYP2D6, CYP3A4 | Steady-state mean 75 h; Steady-state range 75–146 h | 120–270 ng/mL | | - Metabolic: weight/BMI, fasting glucose/HbA1c, and lipids (baseline and periodic).
- EPS: monitor akathisia/parkinsonism; periodic AIMS for tardive dyskinesia.
| Monthly (q4wk); q4–8wk (varies by strength); Every 2 months (q8wk) | 2025-12-28 |
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| Schizophrenia; acute treatment of manic or mixed episodes (bipolar I) and maintenance; in combination with fluoxetine for bipolar depression. View labelExact | Schizophrenia (adults): initiate 5–10 mg once daily; titrate by 5 mg increments at ≥24-hour intervals to 10–20 mg/day (max 20 mg). | Antagonist at serotonin 5‑HT2A and dopamine D2 receptors; strong H1 and muscarinic activity. | CYP1A2, CYP2D6 (minor) | Steady-state mean 30 h | No | | - Metabolic monitoring (weight/BMI, waist circumference, blood pressure, fasting glucose/A1c, lipids) at baseline and periodically (early and then ongoing) because weight and glycemic changes can occur quickly.
- Appetite changes, sedation, and falls risk—reassess driving and occupational safety after dose changes and when other CNS depressants are added.
- Smoking status and CYP1A2 modulators; reduce dose when smoking stops and reassess if smoking restarts or if CYP1A2 inhibitors are introduced.
- AIMS/EPS monitoring at routine intervals, especially in older adults and at higher doses (EPS risk is lower than FGAs but not zero).
- For depot olanzapine pamoate, adhere to REMS observation and PDSS counseling requirements, including post-injection monitoring and “no driving” instructions on injection day.
| q2–4wk | 2025-12-28 |
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| Schizophrenia; acute mania or mixed episodes (bipolar I) as monotherapy or adjunct; irritability associated with autistic disorder. View labelExact | Schizophrenia (adults): start 1–2 mg/day; increase by 1–2 mg/day to 4–6 mg/day (doses >6 mg/day increase EPS). | Dopamine D2 and serotonin 5‑HT2A receptor antagonism; also alpha‑1 and H1 activity. | CYP2D6 | Single-dose mean 3 h; Steady-state mean 21 h | No | - Weight
- Sedation
- EPS
- Prolactin
| - Metabolic: weight/BMI, fasting glucose/HbA1c, and lipids (baseline and periodic).
- EPS: monitor akathisia/parkinsonism; periodic AIMS for tardive dyskinesia.
- Prolactin: monitor for symptoms (amenorrhea, galactorrhea, sexual dysfunction).
- Sedation: assess next-day impairment and fall risk, especially with other sedatives.
| q2wk; Monthly (q4wk); q4wk or q8wk (by dose) | 2025-12-28 |
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