Lumateperone

Lumateperone is a prescription medication used to:

• treat the symptoms of schizophrenia and bipolar disorder in adults
• treatment of schizophrenia in adults
• treatment of depressive episodes associated with bipolar I or II disorder (bipolar depression) in adults, as monotherapy and as adjunctive therapy with lithium or valproate
• adjunctive therapy with antidepressants for the treatment of major depressive disorder (MDD) in adults

Lumateperone is available under the following different brand names: Caplyta

Common side effects of Lumateperone include:

• somnolence (excessive sleepiness)
• headache
• dry mouth
• nausea
• dizziness
• fatigue
• diarrhea

Serious side effects of Lumateperone include:

• increased mortality in elderly patients with dementia-related psychosis  
• suicidal thoughts and behaviors  
• cerebrovascular adverse reactions, including stroke, in elderly patients with dementia-related psychosis 
• neuroleptic malignant syndrome 
• tardive dyskinesia 
• metabolic changes 
• leukopenia, neutropenia, and agranulocytosis
• orthostatic hypotension and syncope 
• falls 
• seizures 
• potential for cognitive and motor impairment 
• body temperature dysregulation 
• dysphagia 

Rare side effects of Lumateperone include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Capsule

• 10.5mg
• 21mg
• 42mg

Schizophrenia

Adult dosage

• 42 mg orally once a day
• Dose titration not required

Bipolar Disorder

Adult dosage

• 42 mg orally once a day
• Dose titration not required

Major Depressive Disorder

Adult dosage

• 42 mg orally once a day
• Dose titration not required

Dosage Considerations – Should be Given as Follows: 

• See “Dosages"

If your doctor has directed you to use this medication, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

Drug interaction overview

• CYP3A4 inhibitors
  • Strong inhibitors: Reduce Lumateperone dose to 10.5 mg/day
  • Moderate inhibitors: Reduce Lumateperone dose to 21 mg/day
  • Moderate or strong CYP3A4 inhibitors increase systemic exposure of lumateperone
• CYP3A4 inducers
  • Avoid coadministration
  • CYP3A4 inducers decrease systemic exposure of Lumateperone

Contraindications

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

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Lumateperone?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Lumateperone?”

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
• Monitor all antidepressant-treated patients for any indication of clinical worsening and emergence of suicidal thoughts and behaviors, especially during the initial few months of drug therapy, and at times of dosage changes; counsel family members or caregivers of patients to monitor for changes in behavior and to alert the healthcare provider; consider changing the therapeutic regimen, including possibly discontinuing therapy, in patients whose depression is persistently worse, or who are experiencing suicidal thoughts or behaviors
• Neuroleptic malignant syndrome (NMS), a potentially fatal symptom complex, is reported with the administration of antipsychotic drugs; if NMS is 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 were reported with antipsychotic agents, including lumateperone; agranulocytosis was 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 a history of seizures or with conditions that lower seizure threshold
• It 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
    • Strong inhibitors: Reduce lumateperone dose to 10.5 mg/day
    • Moderate inhibitors: Reduce lumateperone dose to 21 mg/day
    • Moderate or strong CYP3A4 inhibitors increase the systemic exposure of lumateperone
  • CYP3A4 inducers
    • Avoid coadministration
    • CYP3A4 inducers decrease the systemic exposure of lumateperone

Pregnancy and Lactation

• 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 athttps://womensmentalhealth.org/clinical-and-research-programs/pregnancyregistry/
• Clinical considerations
  • There is a risk to the mother from untreated schizophrenia, including an 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
  • Lumateperone and its metabolites are present in human breast milk in low amounts; in a clinical lactation study, lumateperone was detected in human milk at an estimated daily infant dose of 0.0004 mg/kg, with a relative infant dose (RID) of 0.06% the maternal weight-adjusted dosage
  • Several major circulating metabolites were similarly detected in breast milk in low amounts; however, aniline metabolites were not present in milk or maternal plasma at quantifiable levels; there is no data on the effects of therapy on the breastfed infant or effects on milk production
  • Consider the developmental and health benefits of breastfeeding, along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed child from therapy or from the underlying maternal condition