Bipolar major depression、Major depressive disorder with mixed features、Schizophrenia

Second Generation (Atypical) Antipsychotic

Absorption
1. Increased in fed state.
2. Bioavailability:9%-19%
3. Time to peak:1 to 3 hours; steady state concentrations achieved within 7 days.
Distribution
1. Vd:6173 L
2. Protein binding:~99%
Metabolism
Primarily via CYP3A4; two active metabolites (ID-14283 and ID-14326) and two major nonactive metabolites (ID-20219 and ID-20220) produced. Excretion
Urine (~9%); feces (~80%).
Pharmakodynamics
Half-life Elimination:18 to 40 hours; Main active metabolite, ID-14283 (exo-hydroxy metabolite), exhibits a half-life of 7.5 to 10 hours (Citrome 2011).

Hypersensitivity to lurasidone or any component of the formulation (including angioedema); concomitant use with strong CYP3A4 inhibitors (eg, ketoconazole, clarithromycin, ritonavir, voriconazole, mibefradil) and inducers (eg, rifampin, avasimibe, St. John's wort, phenytoin, carbamazepine).

1. Antipsychotic use during the third trimester of pregnancy has a risk for abnormal muscle movements (extrapyramidal symptoms [EPS]) and/or withdrawal symptoms in newborns following delivery.
2. Safety data related to atypical antipsychotics during pregnancy is limited and routine use is not recommended.

It is not known if lurasidone is excreted in breast milk. According to the manufacturer, the decision to continue or discontinue breast-feeding during therapy should take into account the risk of infant exposure, the benefits of breast-feeding to the infant, and benefits of treatment to the mother.

>10%:
Endocrine & metabolic:
Increase in fasting plasma glucose (2% to 13%), increased serum cholesterol (6% to 14%), increased serum triglycerides (6% to 14%)
Gastrointestinal: Nausea (7% to 17%)
Infection: Viral infection (adolescents: 10% to 11%)
Nervous system:
Akathisia (adolescents: 9%; adults: 6% to 22%), drowsiness (children and adolescents: 11% to 15%; adults: 7% to 26%), extrapyramidal reaction (children and adolescents: 6% to 14%; adults: 5% to 39%), insomnia (5% to 11%), parkinsonism (adolescents: 4%; adults: 5% to 17%)

Bipolar major depression
1. Bipolar major depression, acute, with mixed features (off label) or without (labeled use) (monotherapy or in combination with antimanic therapy): Oral: Initial: 20 mg once daily in the evening within 30 minutes of food (≥350 calories); may increase daily dose based on response and tolerability in increments of 20 mg every ≥2 days to a maximum dose of 120 mg/day
2. Maintenance treatment for depressive episodes (off-label use): Oral: Continue dose and combination regimen that was used to achieve control of the acute episode. Maximum dose: 120 mg/day.

Major depressive disorder with mixed features (monotherapy) (off-label use): Oral: Initial: 20 mg once daily in the evening within 30 minutes of food (≥350 calories) for 7 days; may subsequently increase daily dose based on response and tolerability by 20 mg every 2 to 7 days up to 60 mg/day.

Schizophrenia Oral: Initial: 40 mg once daily in the evening within 30 minutes of food ≥ 350 calories); may increase daily dose based on response and tolerability in increments of 40 mg every ≥ 3 days to a maximum dose of 160 mg/day; usual dose: 40 to 80 mg/day

Bipolar depression:
Children ≥10 years and Adolescents <18 years:
Monotherapy: Oral: Initial: 20 mg once daily; may increase dose after 1 week based on response and tolerability; reported range: 20 to 80 mg/day.
Adolescents 18 years:
Monotherapy or as adjunct to lithium or divalproex: Oral: Initial: 20 mg once daily in the evening; may increase dose further based on response and tolerability in 20 mg increments every 2 to 7 days up to 120 mg/day.

Schizophrenia: Adolescents ≥13 years: Oral: Initial: 40 mg once daily; may increase dose further based on response and tolerability; age-dependent maximum recommended daily dose: for ages <18 years: 80 mg/day; for ages≥18 years: 160 mg/day.

CrCl <50 mL/minute:
Oral: Initial: 20 mg daily; maximum daily dose: 80 mg/day.

Moderate impairment:
Oral: Initial: 20 mg daily; maximum daily dose: 80 mg/day.
Severe impairment::
Oral: Initial: 20 mg daily; maximum daily dose: 40 mg/day.

should be stored below 25°C; short-term transport allows storage at 15°C - 30°C.