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Brand Name :
Caplyta
Synonyms :
lumateperone
Class :
Serotonin-Dopamine Activity Modulators
Brand Name :
Caplyta
Synonyms :
lumateperone
Class :
Serotonin-Dopamine Activity Modulators
Dosage Forms & StrengthsÂ
CapsuleÂ
42mgÂ
21mgÂ
10.5mgÂ
Indicated for Schizophrenia
42 mg orally every day
The titration of the dose is typically not required
Bipolar Disorder
42 mg orally every day
The titration of the dose is typically not required
It is used for depressive episodes with bipolar I or bipolar II disorders in elderly patients, as adjunctive therapy with valproate or lithium, or as monotherapy
Note:
Coadministration with the CYP3A4 inhibitors
Strong: Diminish the dose to 10.5 mg every day
Moderate: Diminish the dose to 21 mg every day
Hepatic impairment
Moderate-severe: 21mg orally every day
Safety and efficacy not establishedÂ
Refer to adult dosingÂ
may diminish the therapeutic effect of anti-parkinson agents
may diminish the therapeutic effect of anti-parkinson agents
may diminish the therapeutic effect of anti-parkinson agents
may diminish the therapeutic effect of anti-parkinson agents
may diminish the therapeutic effect of anti-parkinson agents
may reduce the therapeutic effect of antiparkinson drugs
may reduce the therapeutic effect of antiparkinson drugs
may reduce the therapeutic effect of antiparkinson drugs
may reduce the therapeutic effect of antiparkinson drugs
It may enhance the toxicity effect when combined with lumateperone
lumateperone: they may enhance the serum concentration of CYP3A Inhibitors
lumateperone: they may enhance the serum concentration of CYP3A Inhibitors
lumateperone: they may enhance the serum concentration of CYP3A Inhibitors
lumateperone: they may enhance the serum concentration of CYP3A Inhibitors
lumateperone: they may enhance the serum concentration of CYP3A Inhibitors
may decrease the therapeutic effect when combined with anti-parkinson agents
may decrease the therapeutic effect when combined with anti-parkinson agents
may decrease the therapeutic effect when combined with anti-parkinson agents
may decrease the therapeutic effect when combined with anti-parkinson agents
may decrease the therapeutic effect when combined with anti-parkinson agents
anti-Parkinson Agents may diminish the therapeutic effect of anti-psychotic Agents
anti-Parkinson Agents may diminish the therapeutic effect of anti-psychotic Agents
anti-Parkinson Agents may diminish the therapeutic effect of anti-psychotic Agents
anti-Parkinson Agents may diminish the therapeutic effect of anti-psychotic Agents
anti-Parkinson Agents may diminish the therapeutic effect of anti-psychotic Agents
anti-Parkinson Agents may diminish the therapeutic effect of anti-psychotic Agents
anti-Parkinson Agents may diminish the therapeutic effect of anti-psychotic Agents
anti-Parkinson Agents may diminish the therapeutic effect of anti-psychotic Agents
anti-Parkinson Agents may diminish the therapeutic effect of anti-psychotic Agents
anti-Parkinson Agents may diminish the therapeutic effect of anti-psychotic Agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may have an increased arrhythmogenic effect when combined with mequitazine
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with antipsychotic agents
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
the effect of lumateperone is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of lumateperone
may have an increased adverse effect when combined with antipsychotic agents
it decreases the effects of antipsychotic agents
may have an increasingly adverse effect when combined with sulpiride
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
antihypertensive drugs may enhance the hypotensive effect of antipsychotic Agents
antihypertensive drugs may enhance the hypotensive effect of antipsychotic Agents
antihypertensive drugs may enhance the hypotensive effect of antipsychotic Agents
antihypertensive drugs may enhance the hypotensive effect of antipsychotic Agents
antihypertensive drugs may enhance the hypotensive effect of antipsychotic Agents
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the adverse/toxic effect of amphetamines
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may enhance the hypotensive effect of beta-blockers
may reduce the therapeutic effect of anti-Parkinson drugs
may reduce the therapeutic effect of anti-Parkinson drugs
may reduce the therapeutic effect of anti-Parkinson drugs
may reduce the therapeutic effect of anti-Parkinson drugs
may reduce the therapeutic effect of anti-Parkinson drugs
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may increase the effect of beta-blockers
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
blood pressure lowering agents increase the effect of hypotension of antipsychotic agents
blood pressure lowering agents increase the effect of hypotension of antipsychotic agents
blood pressure lowering agents increase the effect of hypotension of antipsychotic agents
blood pressure lowering agents increase the effect of hypotension of antipsychotic agents
blood pressure lowering agents increase the effect of hypotension of antipsychotic agents
may increase the hypotensive effect when combined with Antipsychotic Agents
may increase the hypotensive effect when combined with Antipsychotic Agents
may increase the hypotensive effect when combined with Antipsychotic Agents
may increase the hypotensive effect when combined with Antipsychotic Agents
may increase the hypotensive effect when combined with Antipsychotic Agents
may have an increasingly adverse effect when combined with amphetamines
may have an increasingly adverse effect when combined with amphetamines
may have an increasingly adverse effect when combined with amphetamines
may have an increasingly adverse effect when combined with amphetamines
may have an increasingly adverse effect when combined with amphetamines
may diminish the therapeutic effect of the drug
may diminish the therapeutic effect of the drug
may diminish the therapeutic effect of the drug
may diminish the therapeutic effect of the drug
may diminish the therapeutic effect of the drug
may increase the hypotensive effect of antipsychotic agents
may have an increased hypotensive effect when combined with beta-blockers
may have an increased hypotensive effect when combined with beta-blockers
may have an increased hypotensive effect when combined with beta-blockers
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
it may increase the neurotoxic effect of antipsychotic agents
It may increase the neurotoxic effect of Antipsychotic Agents
seizure lowering agents increase the toxic or adverse effects of other antipsychotic agents
It may increase the neurotoxic effect of Antipsychotic Agents
It may increase the neurotoxic effect of Antipsychotic Agents
it may increase the risk of adverse effects of antipsychotic agents
May enhance the hypotensive effect of beta-Blockers
May enhance the hypotensive effect of beta-Blockers
May enhance the hypotensive effect of beta-Blockers
May enhance the hypotensive effect of beta-Blockers
May enhance the hypotensive effect of beta-Blockers
May enhance the hypotensive effect of beta-Blockers
May enhance the hypotensive effect of beta-Blockers
May enhance the hypotensive effect of beta-Blockers
May enhance the hypotensive effect of beta-Blockers
May enhance the hypotensive effect of beta-Blockers
Serotonergic Agents may enhance the adverse/toxic effect of antipsychotic Agents
serotonergic Agents may enhance the adverse/toxic effect of antipsychotic Agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may enhance the neurotoxic (central) effect of antipsychotic agents
may increase the adverse or toxic effect of anti-psychotic agents
may increase the adverse or toxic effect of anti-psychotic agents
may increase the adverse or toxic effect of anti-psychotic agents
may increase the adverse or toxic effect of anti-psychotic agents
may increase the adverse or toxic effect of anti-psychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
antacids may reduce the absorption of antipsychotic agents
may increase the risk of adverse effects of antipsychotic agents
may increase the risk of adverse effects of antipsychotic agents
may increase the risk of adverse effects of antipsychotic agents
may increase the risk of adverse effects of antipsychotic agents
may increase the risk of adverse effects of antipsychotic agents
may increase the hypotensive effect of beta-blockersÂ
may increase the hypotensive effect of beta-blockersÂ
may increase the hypotensive effect of beta-blockersÂ
may increase the hypotensive effect of beta-blockersÂ
may increase the hypotensive effect of beta-blockersÂ
may decrease the absorption of antipsychotic agents
may decrease the absorption of antipsychotic agents
may increase the hypotensive effect of anti-hypertensives
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the adverse effect of antipsychotic agents
may enhance the neurotoxic effect of antipsychotic agents
may enhance the neurotoxic effect of antipsychotic agents
may enhance the neurotoxic effect of antipsychotic agents
may enhance the neurotoxic effect of antipsychotic agents
may enhance the neurotoxic effect of antipsychotic agents
may enhance the neurotoxic effect of antipsychotic agents
may enhance the neurotoxic effect of antipsychotic agents
may enhance the neurotoxic effect of antipsychotic agents
may enhance the neurotoxic effect of antipsychotic agents
may enhance the neurotoxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the adverse/toxic effect of antipsychotic agents
may enhance the hypotensive effect of antipsychotic agents
may enhance the hypotensive effect of antipsychotic agents
may enhance the hypotensive effect of antipsychotic agents
may enhance the hypotensive effect of antipsychotic agents
may enhance the hypotensive effect of antipsychotic agents
moexipril/hydrochlorothiazideÂ
may increase the hypotensive effect of blood pressure-lowering agents
may have an increased neurotoxic effect when combined with antipsychotic agents
may have an increased neurotoxic effect when combined with antipsychotic agents
may enhance the bradycardic effect of beta blockers
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the effect of antipsychotic agents
may increase the hypotensive effect of blood pressure-lowering agents
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may increase the neurotoxic effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may enhance the hypotensive effect
may increase the neurotoxic (central) effect
may increase the neurotoxic (central) effect
may increase the neurotoxic (central) effect
may increase the neurotoxic (central) effect
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased hypotensive effect when combined with antipsychotic agents
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effects
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may increase the risk of adverse effect
may have an increasingly adverse effect when combined with antipsychotic agents
may decrease the therapeutic effect when combined with guanethidine
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may enhance the sedation effect when combined with lumateperone
It may enhance the sedation effect when combined with lumateperone
It may enhance the sedation effect when combined with lumateperone
It may enhance the sedation effect when combined with lumateperone
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It may diminish the effect when combined with lumateperone by affecting CYP3A4 metabolism
It could potentially amplify the QTc-prolonging effect of antipsychotic medications known for their QT-prolongation effects
It may enhance the serum concentration when combined with CYP3A4 Substrates
It may enhance the serum concentration when combined with CYP3A4 Substrates
It may enhance the serum concentration when combined with CYP3A4 Substrates
It may enhance the serum concentration when combined with CYP3A4 Substrates
It may enhance the serum concentration when combined with CYP3A4 Substrates
may have an increased hypotensive effect when combined with antipsychotic agents
may increase the hypotensive effect when combined with Antipsychotic Agents
may increase the hypotensive effect when combined with Antipsychotic Agents
may increase the hypotensive effect when combined with Antipsychotic Agents
may increase the hypotensive effect when combined with Antipsychotic Agents
may increase the hypotensive effect when combined with Antipsychotic Agents
may have an increased hypotensive effect when combined with antipsychotic agents
may have an increased neurotoxic effect when combined with antipsychotic agents
may have an increased neurotoxic effect when combined with antipsychotic agents
itopride: they may decrease the therapeutic effect of antipsychotics
nicorandil: they may decrease the therapeutic effect of antipsychotics
quinagolide: they may decrease the therapeutic effect of antipsychotics
ramosetron: they may decrease the therapeutic effect of antipsychotics
may have an increased neurotoxic effect when combined with antipsychotic agents
When lumateperone is used together in combination with profenamine, this leads to reduction in therapeutic effectiveness of profenamine
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
may increase the hypotensive effect of antipsychotic agents
antipsychotic agents increase the arrhythmogenic effect of mequitazine in the serum
Actions and Spectrum:Â
lumateperone is an antipsychotic medication that acts on several receptors in the brain. It was developed for treating schizophrenia and has been shown to have dopaminergic and serotonergic activity. Here’s a breakdown of the action and spectrum of lumateperone:Â
The combination of its dopaminergic and serotonergic actions gives lumateperone a unique pharmacological profile compared to other antipsychotic medications. It is classified as an “atypical” antipsychotic due to its lower risk of causing extrapyramidal side effects, such as movement disorders.Â
Regarding its spectrum, lumateperone is primarily used for the treatment of schizophrenia. It is indicated for treating adults with schizophrenia experiencing acute episodes or exacerbations. It is not approved for other psychiatric conditions like bipolar disorder or major depressive disorder.Â
Frequency definedÂ
>10%Â
Dizziness (11%)Â
Somnolence/sedation (24%)Â
Headache (14%)Â
1-10%Â
Bipolar disorder as monotherapyÂ
Abdominal pain (2%)Â
Diarrhea (4%)Â
Dizziness (8%)Â
Nausea (8%)Â
URT infection (2%)Â
Vomiting (4%)Â
Dry mouth (5%)Â
Bipolar disorder as adjunctive therapyÂ
Blurred vision (3%)Â
Diarrhea (3%)Â
Vomiting (4%)Â
Dry mouth (5%)Â
Enhanced blood prolactin (2%)Â
Nausea (9%)Â
Extrapyramidal symptoms (1.3%)Â
URT infection (3%)Â
SchizophreniaÂ
Fatigue (3%)Â
Vomiting (3%)Â
Nausea (9%)Â
Diminished appetite (2%)Â
Dizziness (5%)Â
Dry mouth (6%)Â
Hepatic transaminases enhanced (2%)Â
Creatine phosphokinase enhanced (4%)Â
Extrapyramidal symptoms (6.7%)Â
Frequency not definedÂ
DystoniaÂ
Black Box Warning:Â
Contraindication/Caution:Â
ContraindicationÂ
lumateperone has specific contraindications, conditions, or factors that make the medication inadvisable due to the potential risks. The following are known contraindications for lumateperone:Â
CautionÂ
There are specific cautions and precautions to be aware of before using the medication. These cautions include:Â
Pregnancy consideration:Â Â
US FDA pregnancy category: Not assignedÂ
Lactation:  Â
Excreted into human milk: Not known.Â
Pregnancy category:Â
Pharmacology:Â
lumateperone exerts its pharmacological effects through its interactions with several receptors in the brain. As a selective antagonist at dopamine D2 receptors, lumateperone helps regulate dopamine activity, reducing positive symptoms of schizophrenia. It also acts as an antagonist at serotonin 5-HT2A receptors and a partial agonist at serotonin 5-HT1A receptors, modulating serotonin neurotransmission to potentially improve negative symptoms and cognitive impairments.
Additionally, lumateperone enhances glutamatergic neurotransmission by increasing glutamate release, and it acts as an antagonist at histamine H1 receptors, contributing to sedative effects. With its unique pharmacological profile, lumateperone provides a multimodal approach to addressing the complex symptoms of schizophrenia.Â
Pharmacodynamics:Â
Mechanism of action: The action of lumateperone involves its interactions with multiple receptors in the brain. While the exact mechanism is not understood, here are the critical aspects of lumateperone’s mechanism of action:Â
Pharmacokinetics:Â
AbsorptionÂ
lumateperone is well-absorbed after oral administration. Following ingestion, it is readily absorbed from the gastrointestinal tract into the bloodstream. Peak plasma concentrations are reached within 4 to 6 hours after dosing.Â
DistributionÂ
lumateperone has a moderate volume of distribution, indicating that it distributes widely throughout the body. It is extensively bound to plasma proteins, primarily albumin, which may affect its distribution and pharmacokinetics.Â
MetabolismÂ
lumateperone undergoes metabolism primarily in the liver through various enzymatic pathways. The main metabolic pathways involve cytochrome P450 (CYP) enzymes, including CYP3A4. The significant metabolites of lumateperone include hydroxylated and dehydrogenated forms.Â
Elimination and ExcretionÂ
lumateperone and its metabolites are eliminated primarily through feces, with a smaller portion being eliminated in urine. The exact mechanisms of lumateperone excretion, including the involvement of renal and biliary pathways, still need to be fully elucidated.Â
Administration:Â
Oral administrationÂ
lumateperone is available in tablet form and should be taken orally. Here are some guidelines for the administration of lumateperone:Â
Patient information leafletÂ
Generic Name: lumateperoneÂ
Pronounced: [ LOO-ma-TE-per-one ]Â
Why do we use lumateperone?Â
lumateperone is primarily used for the treatment of schizophrenia in adults. Schizophrenia is a chronic mental disorder, which is characterized by symptoms, including hallucinations, delusions, disorganized thinking, and impaired social functioning. lumateperone is indicated for treating adults with schizophrenia and is used to manage acute episodes or exacerbations.Â
lumateperone is an atypical antipsychotic medication that modulates dopamine and serotonin activity in the brain. It acts as a selective antagonist at dopamine D2 receptors, which helps regulate the activity of dopamine, a neurotransmitter associated with psychosis. It also acts as a serotonin 5-HT2A receptor antagonist and a partial agonist at serotonin 5-HT1A receptors, modulating serotonin’s activity, a neurotransmitter involved in mood regulation.Â
In addition to its antipsychotic effects, lumateperone has been shown to have potential benefits for negative symptoms and cognitive impairments associated with schizophrenia. Negative symptoms include a lack of motivation, social withdrawal, and diminished emotional expression, while cognitive impairments may involve difficulties with memory, attention, and problem-solving. It’s important to note that lumateperone is specifically approved for treating schizophrenia and has not been indicated for other psychiatric conditions such as bipolar disorder or major depressive disorder.Â
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