lumateperone (Rx)

Brand and Other Names:Caplyta
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

capsule

  • 42mg

Schizophrenia

Indicated for treatment of schizophrenia

42 mg PO qDay

Dose titration not required

Dosage Modifications

Renal impairment: No dose adjustment required

Hepatic impairment

  • Mild (Child-Pugh A): No dose adjustment required
  • Moderate or severe (Child-Pugh B or C): Avoid use; increased systemic exposure to lumateperone associated

Safety and efficacy not established

Not indicated for dementia-related psychosis

Geriatric patients with dementia-related psychosis treated with antipsychotic drugs are at increased risk of death

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Interactions

Interaction Checker

and lumateperone

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Somnolence/sedation (24%)

            1-10%

            Nausea (9%)

            Extrapyramidal symptoms (6.7%)

            Dry mouth (6%)

            Dizziness (5%)

            Creatine phosphokinase increased (4%)

            Fatigue (3%)

            Vomiting (3%)

            Hepatic transaminases increased (2%)

            Decreased appetite (2%)

            Frequency Not Defined

            Dystonia

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            Warnings

            Black Box Warnings

            Increased mortality in elderly patients with dementia-related psychosis observed when treated with antipsychotic drugs

            Not approved for treatment of patients with dementia-related psychosis

            Contraindications

            History of hypersensitivity; reactions have included pruritus, rash (eg, allergic dermatitis, papular rash, and generalized rash), and urticaria

            Cautions

            Geriatric patients with dementia-related psychosis who are treated with antipsychotic drugs are at increased risk of death

            Geriatric patients with dementia who were treated with antipsychotics had a higher incidence of stroke and transient ischemic attacks, including fatal stroke

            Neuroleptic malignant syndrome (NMS), a potentially fatal symptom complex, reported with administration of antipsychotic drugs; if NMS suspected, immediately discontinue lumateperone and provide intensive symptomatic treatment and monitoring

            Tardive dyskinesia, a syndrome consisting of potentially irreversible, involuntary, dyskinetic movements, may develop in patients treated with antipsychotic drugs; risk appears to be highest among elderly individuals, especially women, but it is not possible to predict which patients are likely to develop the syndrome

            May cause metabolic changes, including hyperglycemia, diabetes mellitus, dyslipidemia, and weight gain

            Leukopenia and neutropenia reported with antipsychotic agents, including lumateperone; agranulocytosis reported with other agents in the class

            May cause orthostatic hypotension and syncope; risk is greatest during initial dose administration

            Antipsychotics, including lumateperone, may cause somnolence, postural hypotension, and motor and sensory instability, which may lead to falls and, consequently, fractures and other injuries

            May cause seizures; risk is greatest with history of seizures or with conditions that lower seizure threshold

            May cause somnolence and has the potential to impair judgment, thinking, and motor skills

            May disrupt the body’s ability to reduce core body temperature; strenuous exercise, exposure to extreme heat, dehydration, and anticholinergic medications may contribute to an elevated core body temperature

            Esophageal dysmotility and aspiration reported with antipsychotic drug use

            Drug interaction overview

            • CYP3A4 inhibitors or inducers
              • Moderate or strong inhibitors: Avoid coadministration
              • Inducers: Avoid coadministration
            • UGT inhibitors
              • Coadministration may increase lumateperone and/or its metabolites
              • Avoid coadministration
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            Pregnancy & Lactation

            Pregnancy

            Neonates exposed to antipsychotic drugs during the third trimester are at risk for extrapyramidal and/or withdrawal symptoms following delivery

            Available data from case reports on use in pregnant women are insufficient to establish any drug-associated risks for birth defects, miscarriage, or adverse maternal or fetal outcomes

            Register patients by contacting the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or online at http://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/

            Animal studies

            • No malformations were observed with oral administration of lumateperone to pregnant rats and rabbits during organogenesis at doses up to 2.4 and 9.7 times, respectively, the maximum recommended human dose (MRHD) of 42 mg/day on a mg/m2 basis
            • When pregnant rats were administered lumateperone during organogenesis through lactation, the number of perinatal deaths of pups was increased at 4.9 times the MRHD, with no adverse effects on pups at 2.4 times the MRHD

            Clinical considerations

            • There is risk to the mother from untreated schizophrenia, including increased risk of relapse, hospitalization, and suicide
            • Schizophrenia is associated with increased adverse perinatal outcomes, including preterm birth; unknown if this is a direct result of the illness or other comorbid factors

            Infertility

            • Based on findings from animal studies, lumateperone may impair male and female fertility

            Lactation

            Data are not available regarding presence of lumateperone or its metabolites in human milk, effect on breastfed infants, or effect on milk production

            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.

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            Pharmacology

            Mechanism of Action

            The mechanism of action of lumateperone in the treatment of schizophrenia is unknown; however, efficacy could be mediated through a combination of antagonist activity at central serotonin 5-HT2A receptors and postsynaptic antagonist activity at central dopamine D2 receptors

            Absorption

            Bioavailability: 4.4%

            Peak plasma time: 1-2 hr

            Ingestion with high-fat meal

            • Lowers lumateperone mean peak plasma concentration by 33% and increases mean AUC by 9%
            • Median peak plasma time delayed ~1 hr (from 1 hr at fasted state to 2 hr in the presence of food)

            Distribution

            Protein bound: 97.4%

            Vd: 4.1 L/kg

            Metabolism

            Extensively metabolized with >20 metabolites identified in vivo

            Multiple enzymes, including but not limited to uridine 5’-diphospho- glucuronosyltransferases (UDP-glucuronosyltransferase, UGT) 1A1, 1A4, and 2B15, aldoketoreductase (AKR)1C1, 1B10, and 1C4, and cytochrome P450 (CYP) 3A4, 2C8, and 1A2, are involved in the metabolism of lumateperone

            Elimination

            Half-life: ~18 hr (IV administration)

            Clearance: 27.9 L/hr

            Excretion: Feces: 29%; urine 58%

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            Administration

            Oral Administration

            Administer with food

            Storage

            Store at controlled room temperature 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)

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            Formulary

            FormularyPatient Discounts

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