Luraprex

Approved Indications:

• Schizophrenia: in adults and adolescents (13–17 years)
• Bipolar I Disorder – Major Depressive Episode (BP‑D): monotherapy or adjunctive with lithium/valproate in adults
• Bipolar I Depression: in adolescents (10–17 years)

Off‑Label Use (clinically accepted):

• Bipolar II depression
• Augmentation in treatment‑resistant major depressive disorder

Route: Oral

• Schizophrenia (≥13 years): Start at 40 mg once daily; range 40–160 mg based on response
• Bipolar Depression (adults): 20–60 mg once daily; adjunctive with lithium/valproate
• Pediatric Bipolar (10–17 years): 20–80 mg once daily
• Elderly: Begin at lowest dose; monitor for hypotension and sedation
• Renal Impairment: No adjustment for mild/moderate; caution for severe
• Hepatic Impairment: Use 20 mg in mild/moderate cases; avoid in severe
• Administration: Take once daily with food (~350 kcal at least)

Lurasidone is an atypical antipsychotic with high-binding affinity at dopamine D₂ and serotonin 5‑HT₂A receptors (antagonist), and partial agonism at 5‑HT₁A receptors, along with antagonism at 5‑HT₇ receptors. This profile contributes to its antipsychotic and antidepressant effects, while negligible histamine H₁ and muscarinic receptor binding reduces sedation and anticholinergic side effects.

• Absorption: 9–19% bioavailability with food; Tmax 1–3 hours
• Protein Binding: >99%
• Metabolism: via CYP3A4 to active metabolite ID-14283
• Half-Life: ~18 hours
• Excretion: Feces (~80%), urine (~9%)

• Pregnancy: No FDA category; animal studies show no teratogenicity. Use only if benefits outweigh risks.
• Lactation: Unknown excretion in breast milk. Use with caution and monitor the infant.

• Primary Class: Atypical antipsychotic
• Subclass: Dopamine D₂/5‑HT₂A receptor antagonist with serotonergic modulation

• Allergy to lurasidone or excipients
• Concomitant strong CYP3A4 inhibitors (e.g., ketoconazole) or inducers (e.g., rifampin)

• Elderly with dementia: Increased mortality and stroke risk (black box)
• Neuroleptic Malignant Syndrome: Discontinue if suspected
• Tardive Dyskinesia: Monitor regularly
• Metabolic changes: Track weight, glucose, lipids
• EPS & Akathisia: Assess and adjust dose as needed
• Orthostatic Hypotension: Monitor blood pressure in susceptible patients
• QT Prolongation: Monitor with doses >120 mg or with additional QT-prolonging meds

Common (≥5%): somnolence, akathisia, nausea, EPS, dizziness
Serious (rare): NMS, severe akathisia, QT prolongation, excessive sedation
Onset: EPS and akathisia may appear within days; labs should be monitored periodically

• CYP3A4 Inhibitors (e.g., ketoconazole): ↑ Lurasidone levels—AVOID
• CYP3A4 Inducers (e.g., rifampin): ↓ Lurasidone levels—AVOID
• CNS depressants/hypotensives: Additive sedation or orthostatic effects
• QT-prolonging drugs: Risk of prolonged QT interval

• APA & CANMAT (2023): Endorse lurasidone for bipolar depression due to lower metabolic risks
• FDA (2022): Strengthened recommendation for ECG monitoring with doses >120 mg
• EMA (2021): Reinforced restrictions with strong CYP3A4 modulators

• Temperature: 20–25 °C (allowed 15–30 °C)
• Humidity: Store in original, dry container
• Light: Keep bottle tightly closed
• Handling: Do not freeze; keep out of reach of children; discard expired medication