Lumateperone (US brand name Caplyta®) is a second-generation (“atypical”) antipsychotic. Here is basic information about this medication.
Other articles on this website with more advanced information and tips related to this medication are linked to under Related Pages below.
FDA-approved indications
1. Treatment of schizophrenia in adults.
2. Depressive episodes associated with bipolar I or II disorder (bipolar depression) in adults—as monotherapy and as adjunctive therapy with lithium or valproate.
Pharmacodynamics and Mechanism of action
The exact mechanism of action in the treatment of schizophrenia is unknown. But, it is hypothesized that lumateperone’s effects are mediated through antagonism (blocking) of the following two receptors in the brain:
– Postsynaptic dopamine D2 receptors, for which it has moderate binding affinity
– Serotonin 5-HT2A receptors, for which it has a high binding affinity.
Pharmacokinetics
Peak plasma concentration (Cmax)
After it is taken orally, the peak plasma concentration of lumateperone is reached approximately 1 to 2 hours later.
Ingestion of a high-fat meal with lumateperone may lower lumateperone peak plasma concentration by 33%.
Protein binding
About 97% of lumateperone is protein bound.
Half-life and steady-state
The terminal half-life of lumateperone is about 18 hours.
So, it reaches steady-state concentration after about 5 days.
Contraindications
Lumateperone is, obviously, contraindicated in patients who have had an allergic reaction to it.
Potential side effects
The most common side effects of lumateperone are:
– Sedation and
– Dry mouth.
Other potential side effects include:
– Increase in creatine phosphokinase
– Fatigue
– Increase in hepatic transaminases
– Decreased appetite.
Dosage
– No dose titration is required for lumateperone.
– Dose: 42 mg once daily.
– Lumateperone should be taken with food.
Dosage forms and strengths
Capsules: 42 mg
Important! Please refer to the full Prescribing Information (see link below) before prescribing this medication.
Related Pages
Lumateperone (Caplyta™): Basic information
How well does lumateperone (Caplyta) work for schizophrenia?
Potential side effects of lumateperone (Caplyta™) handout
Second-Generation (“Atypical”) Antipsychotics
References
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