Drug reference

Lurasidone

Atypical Antipsychotic · Antipsychotic

Atypical AntipsychoticAntipsychotic

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

FDA category + note

Top interactionssee all 12 →

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Mechanism

Lurasidone is a dopamine D2, 5-HT2A, 5-HT7, alpha2A- and alpha2C- adrenoceptor antagonist, and is a partial agonist at 5-HT1a receptors. This activity contributes to its antipsychotic effects.

Indications

SchizophreniaSchizophrenia when given with concomitant moderate CYP3A4 inhibitors (e.g. diltiazem, erythromycin, fluconazole, and verapamil)bipolar depressionbipolar depression (monotherapy and adjunct)

Dosing

Adult: For Schizophrenia: Initially 37 mg once daily by mouth, increased if necessary up to 148 mg once daily. For Schizophrenia with concomitant moderate CYP3A4 inhibitors: Initially 18.5 mg once daily by mouth.
Pediatric: Bipolar I depression (ages 10–17): approved.
Geriatric: High doses in elderly may lead to susceptibility to QT-interval prolongation. Postural hypotension and interference with temperature regulation are dose-related side-effects liable to cause dangerous falls and hypothermia or hyperthermia.
Max dose: 148 mg once daily (or 74 mg once daily when given with concomitant moderate CYP3A4 inhibitors)

Pharmacokinetics

Peak effect

1–3 h

Half-life

18–36 h

Bioavailability

9%–19%. Mean Cmax and AUC increased 3-fold and 2-fold, respectively, when administered with food.

Metabolism

CYP3A4

Contraindications

DO NOT USE with strong inducers of CYP3A4
cannot be used with strong CYP3A4 inhibitors
use in elderly dementia patients (increased mortality risk)

Side effects

Common

Anxietydroolingfatiguegastrointestinal discomfortmuscle complaintsmusculoskeletal stiffnessnauseaoculogyric crisisoral disorderspainpsychiatric disorderssleep disordersAppetite decreaseddysarthriadysuriagait abnormalgastrointestinal disordershot flushPostural hypotension (especially during initial dose titration)SyncopeReflex tachycardiaLow risk for anticholinergic side effectslow risk for sedationlow risk for weight gainlow risk for hypotensionlow risk of metabolic adverse effects

Serious

Neuroleptic malignant syndrome (rare, potentially fatal)
QT-interval prolongation (especially with high doses in elderly)
Sudden death (cases have occurred with antipsychotic drugs)
Hypothermia or hyperthermia (in the elderly due to interference with temperature regulation)
Blood dyscrasias (perform blood counts if unexplained infection or fever develops)
Neuroleptic malignant syndrome
increased mortality in elderly dementia patients