Pharmacokinetics and Pharmacodynamics of Lurasidone Hydrochloride, a Second-Generation Antipsychotic: A Systematic Review of the Published Literature

  title={Pharmacokinetics and Pharmacodynamics of Lurasidone Hydrochloride, a Second-Generation Antipsychotic: A Systematic Review of the Published Literature},
  author={William M Greenberg and Leslie Citrome},
  journal={Clinical Pharmacokinetics},
Lurasidone hydrochloride, a benzisothiazol derivative, is a second-generation (atypical) antipsychotic agent that has received regulatory approval for the treatment of schizophrenia in the US, Canada, the EU, Switzerland, and Australia, and also for bipolar depression in the US and Canada. In addition to its principal antagonist activity at dopamine D2 and serotonin 5-HT2A receptors, lurasidone has distinctive 5-HT7 antagonistic activity, and displays partial agonism at 5-HT1A receptors, as… 

Lurasidone – pharmacodynamic and pharmacokinetic properties, clinical potential and interaction risk

Lurasidone is a novel second-generation antipsychotic approved for the treatment of schizophrenia and bipolar depression in adults. It displays high affinity for D2 and 5-HT2A and 5-HT7 receptors,

Lurasidone: efficacy and safety in the treatment of psychotic and mood disorders

Available research findings indicate that LRSD is effective and well-tolerated for short-term treatment of schizophrenia, and for acute bipolar depression, but its risk of akathisia may exceed that of other modern antipsychotics.

Practical Guidance on the Use of Lurasidone for the Treatment of Adults with Schizophrenia

Given the crucial importance of addressing the physical as well as mental healthcare needs of patients, lurasidone is a rational therapeutic choice for adults with schizophrenia, both in the acute setting and over the long term.

Sustained Impairment of Lurasidone Clearance After Discontinuation of Posaconazole: Impact of Obesity, and Implications for Patient Safety

This study evaluated the time-course of recovery from the posaconazole drug interaction, and the effect of obesity on the recovery process, and recommended requiring normal-weight and obese patients to limit the dosage of lurasidone, or undergo a washout period, for two and three weeks, respectively, after discontinuation of posaconzole.

The Effect of Chronic Treatment with Lurasidone on Rat Liver Cytochrome P450 Expression and Activity in the Chronic Mild Stress Model of Depression

It can be suggested that the metabolism of endogenous substrates and drugs, catalyzed by the isoforms CYP 2B, CYP2C11, or CYP3A, may proceed at a different rate in the two groups of animals (nonstressed and stressed) in the rat CMS model.

Identification of clinical phenotypes in schizophrenia: the role of lurasidone

It is established that lurasidone is suggested at any age, with no gender difference, at all stages of the disease, and is among the best-tolerated antipsychotics, and its use is indicated in the presence of different comorbidities.

Lurasidone for Adolescents With Complex Mental Disorders: A Case Series

Preliminary data supporting lurasidone’s potential use in adolescents of complex clinical needs (but without a clinical diagnosis of bipolar disorder) within real-life clinical settings is provided.

Asenapine, iloperidone and lurasidone exposures in young children reported to U.S. poison centers

It is suggested that in children under 6 years of age, lurasidone exposures were least serious and iloperidones exposures were most serious based on clinical effects, management sites and coded outcomes.

Lurasidone in the Treatment of Bipolar Depression: Systematic Review of Systematic Reviews

This overview stipulates the effectiveness of lurasidone in the acute treatment of Type I bipolar depression overall, and recommendations for future research should include further controlled trials of extended duration.



Critical appraisal of lurasidone in the management of schizophrenia

Lurasidone is a new atypical antipsychotic in the benzoisothiazoles class of chemicals. Like most second-generation antipsychotics it is a full antagonist at dopamine D2 and serotonin 5-HT2A

Lurasidone for schizophrenia: a brief review of a new second-generation antipsychotic.

  • L. Citrome
  • Medicine
    Clinical schizophrenia & related psychoses
  • 2011
Lurasidone is a second-generation antipsychotic newly approved by the U.S. Food and Drug Administration for the treatment of schizophrenia associated with minimal weight gain and no clinically meaningful alterations in glucose, lipids, or the ECG QT interval.

Lurasidone drug-drug interaction studies: a comprehensive review

Lurasidone PK is altered by strong cytochrome P450 (CYP) 3A4 inhibitor or inducers, and coadministration is contraindicated; whereas moderate CYP3A4 inhibitors have less effect, and lurasid one dosage restrictions are recommended.

Vilazodone: a brief pharmacological and clinical review of the novel serotonin partial agonist and reuptake inhibitor

Vilazodone will lend itself to the current armamentarium in the treatment of major depressive disorder and may hold promise for patients who cannot tolerate other antidepressants, and its unique SPARI mechanism of action could also be efficacious for Patients who do not respond to SSRI or SNRI antidepressant monotherapies.

Amisulpride is a potent 5-HT7 antagonist: relevance for antidepressant actions in vivo

It is discovered that amisulpride was a potent competitive antagonist at 5-HT7a receptors and that interactions with no other molecular target investigated in this paper could explain its antidepressant actions in vivo.

Lurasidone in Schizophrenia: New Information About Dosage and Place in Therapy

  • L. Citrome
  • Psychology, Medicine
    Advances in Therapy
  • 2012
The totality of the evidence supports the overall tolerability of lurasidone, with minimal weight gain and no clinically-meaningful alterations in glucose, lipids, or the electrocardiogram corrected QT (ECG QTc) interval.

The Role of Serotonin in Antipsychotic Drug Action

  • H. Meltzer
  • Psychology, Medicine
  • 1999

D2 receptor occupancy following lurasidone treatment in patients with schizophrenia or schizoaffective disorder

Positron emission tomography occupancy data suggest that greater than 65% occupancy can be achieved across the dose range of 80–160 mg/day and that some patients require higher doses to achieve antipsychotic efficacy; this finding supports prior randomized clinical trial results.