Lurasidone
- CAS Codes:139563-29-4
- PHARMGKB ID:139563-29-4
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
USA: Latuda.
Drug combinations
Chemistry
Lurasidone Hydrochloride: C~28~H~36~N~4~O~2~S HCl. Mw: 529.14. (1)(3aR,4S,7R,7aS)-2-{(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)piperazin-1-ylmethyl] cyclohexylmethyl}hexahydro-4,7-methano-2H-isoindole-1,3-dione hydrochloride; (2)(1R,2S,3R,4S)-N-(1R,2R)-2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinylmethyl)-1-cyclohexylmethyl)]-2,3-bicyclo[2.2.1]heptanedicarboximide hydrochloride. CAS-139563-29-4 (hydrochloride).
Pharmacologic Category
Atypical Antipsychotics; Benzoisothiazol Derivatives; D~2~, 5HT~1A~, 5HT~2A~, 5HT~7~ Receptor Ligand.
Mechanism of action
The mechanism of action of lurasidone, as with other drugs having efficacy in schizophrenia, is unknown. It has been suggested that the efficacy of lurasidone in schizophrenia is mediated through a combination of central dopamine type 2 (D~2~) and serotonin type 2 (5HT~2A~) receptor antagonism. In vitro receptor binding studies revealed that lurasidone is an antagonist with high affinity at dopamine D~2~ receptors and the 5-hydroxytryptamine (5-HT, serotonin) receptors 5-HT~2A~ and 5-HT~7~, is an antagonist with moderate affinity at human α~2C~-adrenergic receptors, is a partial agonist at serotonin 5-HT~1A~ receptors, and is an antagonist at α~2A~-adrenergic receptors. Lurasidone exhibits little or no affinity for histamine H~1~ and muscarinic M~1~ receptors.
Therapeutic use
Treatment of patients with schizophrenia (efficacy was established in four 6-week controlled studies of adult patients with schizophrenia).
Pregnancy and lactiation implications
Use during pregnancy only if potential benefit justifies potential risk. Breast feeding not recommended during therapy.
Unlabeled use
Contraindications
Any known hypersensitivity to lurasidone or any components in the formulation. Co-administration with a strong CYP3A4 inhibitor (e.g. ketoconazole) or inducer (e.g. rifampin).
Warnings and precautions
An increased incidence of cerebrovascular adverse events (e.g. stroke, transient ischemic attack) has been seen in elderly patients with dementia-related psychoses treated with atypical antipsychotic drugs. A potentially fatal symptom complex sometimes referred to as Neuroleptic Malignant Syndrome (NMS) has been reported in association with administration of antipsychotic drugs (manage with immediate discontinuation and close monitoring). Tardive dyskinesia can develop in patients treated with lurasidone (discontinue if clinically appropriate). Atypical antipsychotic drugs have been associated with metabolic changes (hyperglycemia, dyslipidemia, and weight gain) that may increase cardiovascular/cerebrovascular risk. Prolactin elevations may occur. Leukopenia, neutropenia, and agranulocytosis have been reported with antipsychotics (in patients with a pre-existing low white blood cell count (WBC) or history of leukopenia/neutropenia should have their complete blood count (CBC) monitored frequently during the first few months of therapy and this should be discontinued at the first sign of a decline in WBC in the absence of other causative factors). Dizziness, tachycardia or bradycardia, and syncope may occur, especially early in treatment (caution in patients with known cardiovascular or cerebrovascular disease, and in antipsychotic-naïve patients). Use cautiously in patients with history of seizures or with conditions that lower the seizure threshold. Lurasidone has the potential to impair judgment, thinking or motor skills (use caution when operating machinery). The possibility of a suicide attempt is inherent in schizophrenia (closely supervise high-risk patients). Esophageal dysmotility and aspiration have been associated with antipsychotic drug use (should not be used in patients at risk for aspiration pneumonia).