Iloperidone (Dosage)

Iloperidone is an atypical antipsychotic used in the treatment of schizophrenia. A relationship has been established between the efficacy of this drug and pharmacogenetics, which can determine the final plasma concentration of the metabolite.

Iloperidone is a second generation or atypical antipsychotic used to treat the symptoms of schizophrenia.


The action mechanism of iloperidone is yet unknown. It is believed that the efficacy of iloperidone is mediated through a combination of the antagonism of dopamine type 2 receptors and serotonin type 2 receptors.


Is not recommended the prescription of iloperidone in patients with hepatic insufficiency

In elderly patients with psychosis related to dementia, there is an increased risk of mortality during treatment with iloperidone.

Iloperidone prolongs the cardiac QT interval, avoid supplying iloperidone with other substances that prolong the QT interval: class IA antiarrhythmics (such as quinidine, procainamide) or antiarrhythmics class III (such as amiodarone, sotalol), antiarrhythmic substances, antipsychotics (such as ziprasidone, chlorpromazine, thioridazine), antibiotics (such as gatifloxacin, moxifloxacin) or any other substance that prolongs the QTc interval (such as pentamidine, levomethadyl acetate, methadone).

Special caution should be taken in patients with a history of cardiac arrhythmias and congenital long QT syndrome. Extreme caution in circumstances that increase the risk of torsade de pointes, such as bradycardia, hypokalemia, hypomagnesemia, congenital prolongation of the QT interval, recent acute myocardial infarction, decompensated heart failure.

In patients with hyperglycemia and diabetes mellitus, regular monitoring should be performed. This regular control should be extended to patients with risk factors for diabetes mellitus such as obesity, family history (fasting glucose control should be performed at the beginning of treatment with iloperidone and periodically during the duration of treatment).

Extreme caution in patients with a history of seizures or in conditions that potentially decrease the seizure threshold (Alzheimer's type dementia).

Iloperidone can affect judgment, thinking and motor skills. In patients at risk of suicide perform close supervision during treatment.


Plasma concentrations of iloperidone may be increased by: potent inhibitors of CYP3A4 (eg ketoconazole, itraconazole), potent inhibitors of CYP2D6 (eg paroxetine, fluoxetine).


Palpitations; prolongation of the cardiac QT interval; conjunctivitis (including allergic); weight loss; myalgia, muscle spasms; restlessness, aggressiveness, delirium; urinary incontinence; erectile dysfunction.


  • Fanapt®

Genes analyzed



Brennan MD. Pharmacogenetics of second-generation antipsychotics. Pharmacogenomics, 2014; 15(6):869–84.

PharmGKB Annotation of FDA Label for iloperidone and CYP2D6.

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