Lurasidone
Second-generation antipsychotics
Second-generation antipsychotics
A second-generation antipsychotic for schizophrenia and bipolar depression. It must be taken with a meal and cannot be combined with strong CYP3A4 drugs.
Quick facts
- Group
- Second-generation antipsychotics
- Target
- Dopamine D2 and serotonin 5-HT2A and 5-HT7 receptors
- Used for
- Schizophrenia in adults and adolescents
- Key effects
- Akathisia · Sleepiness · Nausea
- Monitor
- Weight · Akathisia and other movement disorders
- ATC
- N05AE05
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows risperidone in the human D2 receptor; lurasidone blocks the same receptor site (no lurasidone-bound structure is available).
Lurasidone blocks dopamine D2 and serotonin 5-HT2A receptors, the shared action of second-generation antipsychotics, and also blocks 5-HT7 receptors. 5-HT7 antagonism is one proposed explanation for its antidepressant effect in bipolar depression. Akathisia is a common adverse effect.
- Blocks D2 and 5-HT2A receptors
- Also blocks 5-HT7 receptors
- Treats psychosis and bipolar depression
- Common motor effect: akathisia
Indications
- Schizophrenia in adults and adolescents Schizophrenia →
- Depressive episodes of bipolar I disorder (alone, or with lithium or valproate in adults) Bipolar disorder →
Adverse effects
Common
- Akathisia (restlessness) and other extrapyramidal symptoms
- Sleepiness
- Nausea
- Raised prolactin: breast changes, missed periods
Contraindications
- Strong CYP3A4 inhibitors (ketoconazole, clarithromycin, ritonavir)
- Strong CYP3A4 inducers (rifampicin, St John's wort, phenytoin, carbamazepine)
- Hypersensitivity to lurasidone
Key interactions
- Strong CYP3A4 inhibitors
- Large rise in lurasidone levels and toxicity; contraindicated.
- Strong CYP3A4 inducers
- Levels fall so much that it stops working; contraindicated.
- Grapefruit juice
- Large amounts can raise levels; avoided.
What is monitored
- Weight, glucose and lipids
- Akathisia and other movement disorders
- Mood and suicidal thoughts in bipolar depression
- Liver and kidney function (doses are lower in impairment)
Administration and safety
- Oral tablet once a day with a meal (a real meal, not a snack).
- Every new prescription is checked for strong CYP3A4 inhibitors or inducers before starting.
- The dose is lowered in moderate or severe liver or kidney impairment.
Pregnancy and breastfeeding
Newborns exposed in the third trimester may have extrapyramidal or withdrawal symptoms; use weighs benefit and risk.
Nursing care
- Before: record weight, glucose and lipids; review all medicines and herbal products.
- During: ask about restlessness and inability to sit still; report it.
- Watch mood and suicidal thoughts.
- Teach to take it with food and to avoid grapefruit and alcohol.
Pharmacokinetics
- Absorption
- Oral; food greatly increases absorption, so it is taken with a meal.
- Metabolism
- Liver, by CYP3A4.
Test yourself
Think of the answer, then tap the question to see it.
Why must lurasidone be taken with food?
Food greatly increases its absorption; on an empty stomach levels are too low.
Why are rifampicin and ketoconazole contraindicated with lurasidone?
Lurasidone depends on CYP3A4: the inducer makes it ineffective and the inhibitor makes it toxic.
Which movement side effect is especially common with lurasidone?
Akathisia (inner restlessness).
Connections
← Back to the class: Second-generation antipsychotics
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Lurasidone: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); LURASIDONE HYDROCHLORIDE tablet, film coated (DailyMed (U.S. National Library of Medicine), 2026); Structure of the D2 Dopamine Receptor Bound to the Atypical Antipsychotic Drug Risperidone (RCSB Protein Data Bank, 2018); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.