lurasidone (Rx)

Brand and Other Names:Latuda
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 20mg
  • 40mg
  • 80mg
  • 120mg
more...

Schizophrenia

Indicated for schizophrenia

40 mg PO qDay initially; not to exceed 160 mg/day

Initial dose titration is not required; shown to be effective in a dose range of 40-160 mg/day

Bipolar Depression

Monotherapy

  • Indicated as monotherapy for adults with major depressive episode associated with bipolar I disorder (bipolar depression)
  • 20 mg PO qDay initially; may increase dose if needed, not to exceed 120 mg/day
  • In monotherapy study, higher dose range (80-120 mg/day) did not provide additional efficacy compared to the lower dose range (20-60 mg/day)

Adjunctive therapy

  • Indicated as adjunctive therapy for major depressive episodes associated with bipolar I disorder with lithium or valproate
  • 20 mg PO qDay initially; may increase dose if needed, not to exceed 120 mg/day

Dosage Modifications

CYP3A4 inhibitors or inducers

  • Coadministration with CYP3A4 inhibitors
    • Strong CYP3A4 inhibitor: Contraindicated; do not coadminister (see Contraindications)
    • Moderate CYP3A4 inhibitor (eg, diltiazem, atazanavir, erythromycin, fluconazole, verapamil): Reduce dose to 50% of original dose, not to exceed 80 mg/day; starting dose is 20 mg/day
    • Grapefruit and grapefruit juice: Avoid coadministration
  • Coadministration with CYP3A4 inducers
    • Strong CYP3A4 inducer: Contraindicated; do not coadminister (see Contraindications)
    • Moderate CYP3A4 inducer (eg, bosentan, efavirenz, etravirine, modafinil, nafcillin): It may be necessary to increase lurasidone dose after chronic treatment (ie, ≥7 days) with the inducer

Renal impairment

  • Mild (CrCl ≥50 mL/min): No dosage adjustment required
  • Moderate-to-severe (CrCl <50 mL/min): 20 mg/day initially; not to exceed 80 mg/day

Hepatic impairment

  • Mild (Child-Pugh class A): Use with caution
  • Moderate (Child-Pugh class B [Score 7-9]): 20 mg/day initially; not to exceed 80 mg/day
  • Severe (Child-Pugh class C [Score 10-15]): 20 mg/day initially; not to exceed 40 mg/day

Dosing Considerations

Effectiveness for longer-term use (ie, >6 weeks) has not been established in controlled studies; therefore, the physician who elects to use lurasidone for extended periods should periodically re-evaluate the long-term usefulness of the drug for the individual patient

Dosage Forms & Strengths

tablet

  • 20mg
  • 40mg
  • 80mg

Schizophrenia

Indicated for treatment of schizophrenia in adolescents aged 13-17 years

<13 years: Safety and efficacy not established

13-17 years

  • Starting dose: 40 mg PO qDay; initial dose titration is not required
  • Effective dosage range: 40-80 mg/day; not to exceed 80 mg/day

Bipolar Depression

Indicated as monotherapy for major depressive episode associated with bipolar I disorder (bipolar depression) in adolescents aged 10-17 yr

20 mg PO qDay; initial dose titration is not required

May increase dose after 1 week based on clinical response; not to exceed 80 mg qDay Effective dose range is 20-80 mg/day

Clinical studies found most patients (67%) received 20-40 mg/day

Dosage Modifications

CYP3A4 inhibitors or inducers

  • Coadministration with CYP3A4 inhibitors
    • Strong CYP3A4 inhibitor: Contraindicated; do not coadminister (see Contraindications)
    • Moderate CYP3A4 inhibitor (eg, diltiazem, atazanavir, erythromycin, fluconazole, verapamil): Reduce dose to 50% of original dose, not to exceed 80 mg/day; starting dose is 20 mg/day
    • Grapefruit and grapefruit juice: Avoid coadministration
  • Coadministration with CYP3A4 inducers
    • Strong CYP3A4 inducer: Contraindicated; do not coadminister (see Contraindications)
    • Moderate CYP3A4 inducer (eg, bosentan, efavirenz, etravirine, modafinil, nafcillin): It may be necessary to increase lurasidone dose after chronic treatment (ie, ≥7 days) with the inducer

Renal impairment

  • Mild (CrCl ≥50 mL/min): No dosage adjustment required
  • Moderate-to-severe (CrCl <50 mL/min): 20 mg/day initially; not to exceed 80 mg/day

Hepatic impairment

  • Mild (Child-Pugh class A): Use with caution
  • Moderate (Child-Pugh class B [Score 7-9]): 20 mg/day initially; not to exceed 80 mg/day
  • Severe (Child-Pugh class C [Score 10-15]): 20 mg/day initially; not to exceed 40 mg/day

Dosing Considerations

Effectiveness for longer-term use (ie, >6 weeks) has not been established in controlled studies; therefore, the physician who elects to use lurasidone for extended periods should periodically re-evaluate the long-term usefulness of the drug for the individual patient

Next:

Interactions

Interaction Checker

and lurasidone

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 
            Previous
            Next:

            Adverse Effects

            >10%

            Somnolence, dose related (15-26%)

            Akathisia, dose related (6-22%)

            Extrapyramidal disorder, dose related (6-22%)

            Parkinsonism, dose related (6-17%)

            Fasting glucose increased, dose related (10-14%)

            Nausea, dose related (9-13%)

            Insomnia, dose-related (7-11%)

            1-10%

            Agitation, dose related (3-10%)

            Vomiting, dose related (6-8%)

            Dyspepsia, dose related (5-8%)

            Anxiety, dose related (3-8%)

            Elevated serum creatinine, dose related (1-7.2%)

            Dystonia (5%)

            Dizziness, dose related (4-6%)

            Fatigue (4%)

            Back pain, dose related (2-4%)

            Restlessness (3%)

            Salivary hypersecretion, dose related (1-4%)

            Hypertension

            Rash

            Pruritus

            CPK increased

            Abdominal pain

            Diarrhea

            Blurred vision

            Tachycardia

            <1%

            Anemia

            AV block 1st degree

            Angina pectoris

            Bradycardia

            Vertigo

            Gastritis

            Rhabdomyolysis

            Cerebrovascular accident

            Dysarthria

            Abnormal dreams

            Panic attack

            Sleep disorder

            Dysuria

            Renal failure

            Amenorrhea

            Dysmenorrhea

            Breast enlargement

            Breast pain

            Galactorrhea

            Erectile dysfunction

            Angioedema

            Postmarketing Reports

            Hypersensitivity (urticaria, throat swelling, tongue swelling, and dyspnea)

            Hyponatremia

            Previous
            Next:

            Warnings

            Black Box Warnings

            Increased mortality in elderly patients with dementia-related psychosis

            • Not indicated for dementia-related psychosis
            • Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death; lurasidone is not approved for the treatment of patients with dementia-related psychosis; placebo-controlled trials with other atypical antipsychotics showed higher incidence of cerebrovascular adverse reactions (eg, CVA, TIA), including fatalities, compared with placebo

            Suicidal thoughts and behaviors

            • Antidepressants increased the risk of suicidal thoughts and behavior in children and young adults in short-term studies; closely monitor all antidepressant-treated patients for clinical worsening, and for emergence of suicidal thoughts and behaviors

            Contraindications

            Hypersensitivity

            Coadministration with strong CYP3A4 inhibitors (eg, ketoconazole, clarithromycin, ritonavir, voriconazole, mibefradil)

            Coadministration with strong CYP3A4 inducers (eg, rifampin, St. John’s wort, phenytoin, carbamazepine)

            Cautions

            Possibility of suicide attempt inherent to psychotic illness; close supervision required when therapy is initiated, dosage is changed, or drug is discontinued; the risk of suicidal thoughts and behaviors in pediatric and young adult patients extends to longer-term use (eg, >4 months) is unknown; there is substantial evidence from placebo-controlled maintenance studies in adults with MDD that antidepressants delay the recurrence of depression

            Antidepressant treatment can increase the risk of developing a manic or hypomanic episode, particularly in patients with bipolar disorder

            Patients with Parkinson’s disease or dementia with Lewy bodies are reported to have an increased sensitivity to antipsychotic medication

            Orthostatic hypotension and syncope reported, possibly due to its alpha-1receptor antagonism

            Risk of neuroleptic malignant syndrome (NMS) reported in association with administration of antipsychotic drugs, including lurasidone; clinical manifestations of NMS (eg, hyperpyrexia, muscle rigidity, altered mental status, evidence of autonomic instability); additional symptoms (eg, elevated creatine phosphokinase, myoglobinuria [rhabdomyolysis], acute renal failure); the syndrome can develop, although much less commonly, after relatively brief treatment periods at low doses or may even arise after discontinuation of treatment; if NMS is suspected, immediately discontinue therapy and provide intensive symptomatic treatment and monitoring

            Hyperprolactinemia reported; galactorrhea, amenorrhea, gynecomastia, and impotence reported with prolactin-elevating compounds; long-standing hyperprolactinemia, when associated with hypogonadism, may lead to decreased bone density in both female and male patients

            Exercise caution in patients with a history of seizures or with conditions that lower the seizure threshold (eg, Alzheimer’s dementia); conditions that lower the seizure threshold may be more prevalent in patients ≥65 years

            May cause leukopenia, neutropenia, and agranulocytosis; monitor patients with neutropenia should for fever or other signs of infection and treat promptly if symptoms occur; discontinue treatment in patients with severe neutropenia (ANC <1,000/mm³) and follow WBC until recovery

            May disrupt body temperature regulation

            May lead to cognitive and motor impairment; caution patients about operating hazardous machinery

            Incidence of cerebrovascular effects (eg, transient ischemic attacks, stroke) may increase

            Esophageal dysmotility or aspiration may occur

            May increase QT interval: In trials, increase in baseline adjusted QTc intervals did not exceed mean based on individual correction method (QTcI) was 7.5 ms (120-mg dose) and 4.6 ms (600-mg dose) observed at 2-4 hours after dosing; additionally, in separate trial, QTc did not increase by >60 msec from baseline or exceed 500 msec with supratherapeutic doses (ie, 120 mg/day, 600 mg/day)

            Acute overdose: If antiarrhythmic therapy is administered, disopyramide, procainamide, and quinidine carry theoretical hazard of additive QT-prolonging effects when given to patient with acute lurasidone overdose

            Motor instability, somnolence, and orthostatic hypotension reported, which may lead to falls and, consequently, fractures or other fall-related injuries; assess risk of falls when initiating treatment and recurrently for patients receiving repeated doses, particularly the elderly, with diseases, conditions, or medications that could exacerbate these effects

            Metabolic changes with atypical antipsychotic use

            • Hyperglycemia, some cases extreme and associated with ketoacidosis or hyperosmolar coma or death, reported; monitor glucose control in patients with an established diagnosis of diabetes mellitus who are started on atypical antipsychotics
            • Monitor symptoms of hyperglycemia (eg, polydipsia, polyuria, polyphagia, weakness)
            • In the 6-week, placebo-controlled study of pediatric patients with bipolar depression, mean change in fasting glucose was +1.6 mg/dL for lurasidone 20-80 mg/day
            • Undesirable alterations in lipids observed
            • Weight gain observed; clinically monitor weight

            Tardive dyskinesia

            • Extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia may occur; risk of tardive dyskinesia may increase in the elderly; risk of dystonia may increase with high doses
            • Risk of developing tardive dyskinesia and likelihood of it becoming irreversible may increase as the duration of treatment and total cumulative dose of antipsychotic drugs administered to the patient increase

            Drug interactions overview

            • Coadministration with strong (eg, ketoconazole, clarithromycin, ritonavir, voriconazole, mibefradil) and moderate CYP3A4 inhibitors increased exposure of lurasidone (see Dosage Modifications, Contraindications)
            • Coadministration with strong (eg, rifampin, avasimibe, St. John’s wort, phenytoin, carbamazepine) and moderate CYP3A4 inducers decreased exposure of lurasidone (see Dosage Modifications, Contraindications)
            Previous
            Next:

            Pregnancy & Lactation

            Pregnancy

            Neonates exposed to antipsychotic drugs during 3rd trimester of pregnancy are at risk for extrapyramidal symptoms (EPS) and/or withdrawal symptoms after delivery; these complications vary in severity, with some being self-limited and others requiring ICU support and prolonged hospitalization

            There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to lurasidone during pregnancy

            National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-andresearchprograms/pregnancyregistry

            Lactation

            Unknown whether drug is distributed in breast milk

            Lurasidone is present in rat milk

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
            Previous
            Next:

            Pharmacology

            Mechanism of Action

            Atypical antipsychotic; precise mechanism is unknown; efficacy suggested to involve mediation of central dopamine type 2 and serotonin type 2 (5HT-2A) receptor antagonism

            Absorption

            Bioavailability: 9-19%

            Peak plasma time: 1-3 hr

            Mean peak plasma concentrations and AUC were ~3x and 2x when administered with food compared to levels observed under fasting conditions  

            Distribution

            Protein bound: 99%

            Vd: 6173 L  

            Metabolism

            Metabolized by CYP3A4; biotransformation pathways are oxidative N-dealkylation, hydroxylation of norbornane ring, and S-oxidation

            Metabolites: 2 active (ID-14283, ID-14326) and 2 inactive (ID-20219, ID-20220)

            Elimination

            Half-life: 18 hr

            Clearance: 3902 mL/min

            Excretion: Feces (80%), urine (9%)  

            Previous
            Next:

            Administration

            Oral Administration

            Take with food (at least 350 calories)

            Food substantially increases absorption; increases AUC ~2-fold and Cmax ~3-fold

            Initial dose titration not required

            Storage

            Tablets: Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F)

            Previous
            Next:

            Images

            Previous
            Next:

            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous
            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.