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Lurasidone: a profile of the second-generation antipsychotic

Publication at Faculty of Medicine in Hradec Králové |
2019

Abstract

Lurasidone is an antipsychotic of the SDA class, partial agonist of serotonin 5-HT1a receptors, antagonist of 5-HT7 and norepinephrine α2creceptors. Pharmacokinetics of lurasidone dosing 20-160 mg is linear, absorption is enhanced by food intake, it is metabolized via CYP3A4.

In preclinical studies, lurasidone showed antipsychotic, antidepressive, and procognitive effects, with improved neuroplasticity. Clinical trials demonstrated its antipsychotic efficacy in treatment of acute schizophrenia and in the long-term relapse prevention.

Lurasidone in mono-therapy and as an adjunctive treatment to lithium or valproate significantly improved depressive symptoms of bipolar depression. The most frequently reported side effects were somnolence, sedation, nausea, and dose-dependent akathisia and parkinsonism.

It has been associated with low risk of metabolic adverse events, weight gain, QTc prolongation, and sexual dysfunction. In Czechia and EU, lurasidone is approved for acute and maintenance treatment of schizophrenia.

Initial dose is 37 mg (40 mg), therapeutic dosage is 37-148 mg (40-160 mg) once daily, administered with food of minimum 350 calories. Contraindicated is concomitant treatment with CYP3A4 inhibitors or inductors.