Trade name Latuda
Oral drug that is an atypical antipsychotic agent.
Approved for the treatment of depressive episodes associated with bipolar I disorder in adults alone or in combination with lithium or valproate.
Approved for the treatment of schizophrenia.
In a comparison of 15 antipsychotic drugs in effectiveness in treating schizophrenic symptoms, it demonstrates mild effectiveness.
Is not approved for the treatment of behavior disorders in older adults with dementia.
Its use is contraindicated in patients taking strong inhibitors of the liver enzyme CYP3A4 (ketoconazole, clarithromycin, ritonavir, levodropropizine, etc.) or inducers (carbamazepine, St. John’s wort, phenytoin, rifampicin).
It has received approval for bipolar I depression.
Few available atypical antipsychotics are known to possess antidepressant efficacy in bipolar disorder: quetiapine, olanzapine and possibly asenapine.
It may be used together with a mood stabilizer such as lithium or valproate.
It is taken by mouth.
Pregnancy category US: B (No risk in non-human studies).
Its use in pregnant women is not recommended.
It is not indicated for use in children.
Approved for bipolar I depression.
Drug class-Atypical antipsychotic.
Bioavailability 9–19%.
It has an estimated absorption rate of 9 to 19%, and when taken with food, absorption increases about twofold.
Peak blood plasma concentrations are reached after one to three hours.
99% of the circulating substance are bound to plasma proteins.
It is mainly metabolized in the liver via the enzyme CYP3A4.
The native drug makes up 11% of circulating metabolite, the main active metabolite 4%, and the inactive carboxylic acids 24% and 11%, respectively.
Biological half-life is 20 to 40 hours.
Protein binding about 99%.
Excretion Fecal (67–80%).
Renal excretion (9–19%)
Available as 40mg and 80mg tablets.
Metabolism by hepatic enzyme CYP3A4-mediated.
Half-life of 18 hours with fecal excretion and renal excretion of about 9%.
May be useful for the management of cognitive and memory deficits seen in schizophrenia.
Has activity serotonin receptors involved in learning and memory.
It acts as an antagonist of the dopamine D2 and D3 receptors, the serotonin 5-HT2A and 5-HT7 receptors, and the α2C-adrenergic receptor.
It is a partial agonist of the serotonin 5-HT1A receptor.
The drug has no antihistamine or anticholinergic effects.
Lacks anticholinergic effects that impair cognitive processes and memory.
Not presently approved for the treatment of behavior disorders in older adults with dementia.
Side effects similar to other antipsychotic agents.
Side effects include: sleepiness, movement disorders, nausea, and diarrhea, tardive dyskinesia, as well as neuroleptic malignant syndrome, an increased risk of suicide, angioedema, and high blood sugar levels.
Has a relatively well-tolerated side effect profile.
Use associated with low propensity for QTc interval changes, weight gain and lipid-related adverse effects.
In the elderly it is associated with increased risk for a stroke or transient ischemic attack.
Has a low propensity for QTc interval changes, and associated with the least QT interval prolongation.
Favorable weight gain profile compared to other antipsychotic agents.
Weight gain is reported in up to 15 percent of users.
It should not be used to treat dementia-related psychosis, as evidence has shown increased mortality with antipsychotic use.
Low rate of extrapyramidal and sedation side effects.
Should not be used to treat dementia-related psychosis, as it is associated evidence with an increased mortality.
It may increase risk of death in elderly dementia associated psychosis patients.
Its use in pregnancy is of questionable safety.
Rarely tardive dyskinesia can occur when the drug is discontinued.
Blood levels may be increased when combined with CYP3A4 inhibitors, possibly leading to more side effects.
Ketoconazole increases lurasidone exposure by a factor of 9, and is also expected for other 3A4 inhibitors such as grapefruit juice.
CYP3A4 inducers like rifampicin or St. John’s wort can reduce plasma levels and consequently decrease the effects of the drug.
For rifampicin, the reduction was sixfold in a study.
Mechanism of action is believed to involve effects on dopamine and serotonin in the brain.
Plasma concentrations may be increased when combined with CYP3A4 inhibitors like ketoconazole or grapefruit juice.
Co-administration of CYP3A4 inducers like rifampicin or St. John’s wort can reduce plasma levels and consequently decrease the effects of the drug.
In a meta-analysis of the efficacy and tolerability of 15 antipsychotic drugs: it produced the second least weight gain, the least QT interval prolongation, the fourth most extrapyramidal side effects and the sixth least sedation.
Puts elderly at an increased risk for a stroke or transient ischemic attacks.
A gradual withdrawal is recommended when discontinuing the drug to avoid acute withdrawal syndrome or rapid relapse.
Symptoms of withdrawal include: nausea, vomiting, loss of appetite, restlessness, increased sweating, trouble sleeping, spinning, numbness, or muscle pains.
Withdrawal symptoms generally resolve after a short period of time.
Once-daily oral agent.
Available as 40mg and 80mg tablets.
May be useful for treating the cognitive and memory deficits seen in schizophrenia.
Has activity at several serotonin receptors that are involved in learning and memory.
Unlike most other antipsychotics, lacks any anticholinergic effects, which are known to impair cognitive processes and memory.
These properties may underlie its improved effectiveness in treating these symptoms relative to older agents.
Adverse effects of lurasidone: similar to other antipsychotics, low propensity for QTc interval changes, weight, lipid-related adverse effects, extrapyramidal side effects, and sedation.