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    / Megapharm


    Active Ingredient
    Iloperidone 1, 2, 4, 6, 8, 10, 12 mg

    Status in Israel
    RX

    Presentation and Status in Health Basket

    Presentation Basket Yarpa Pharmasoft

    Tablets

    60 X 1 mg

    partial basket chart 43871 6505

    Tablets

    60 X 2 mg

    partial basket chart 43873 6506

    Tablets

    60 X 4 mg

    partial basket chart 43874 6508

    Tablets

    60 X 6 mg

    partial basket chart 43875 6507

    Tablets

    60 X 8 mg

    partial basket chart 43876 6509

    Tablets

    60 X10 mg

    partial basket chart 58457 6548

    Tablets

    60 X 12 mg

    partial basket chart 58459 6549

    Related information


    Dosage

    Adults-Titration phase: Iloperidone must be titrated slowly from a low starting dose to avoid orthostatic hypotension due to its alpha-adrenergic blocking properties.  The recommended starting dose for Iloperidone tablets is 1 mg twice daily. Increases to reach the target dose range of 6-12 mg twice daily may be made with daily dosage adjustments to 2 mg twice daily, 4 mg twice daily, 6 mg twice daily, 8 mg twice daily, 10 mg twice daily, and 12 mg twice daily on days 2, 3, 4, 5, 6, and 7, respectively. Efficacy was demonstrated with Iloperidone in a dose range of 6 to 12 mg twice daily. Prescribers should be mindful of the fact that patients need to be titrated to an effective dose of Iloperidone. Thus, control of symptoms may be delayed during the first 1 to 2 weeks of treatment compared to some other antipsychotic medicinal products that do not require similar titration. Prescribers should also be aware that some adverse reactions associated with Iloperidone use are dose-related. To minimize initial tolerability issues, patients may want to take the medication with food.
    Maintenance Treatment: The recommended maintenance dose for Iloperidone is 12 mg/day, administered as either 6 mg twice daily or 12 mg once daily. Patients should be periodically reassessed to determine the need for maintenance treatment.
    Maximum dose: The maximum recommended dose is 12 mg twice daily (24 mg/day); Iloperidone doses above 24 mg/day have not been systematically evaluated in the clinical trials.
    Reinitiation of treatment in patients previously discontinued: Although there are no data to specifically address re-initiation of treatment, it is recommended that the initiation titration schedule be followed whenever patients have had an interval off Iloperidone of more than 3 days.
    Switching from other antipsychotics: There are no specific data to address how patients with schizophrenia can be switched from other antipsychotics toIloperidone or how Iloperidone can be used concomitantly with other antipsychotics. Although immediate discontinuation of the previous antipsychotic treatment may be acceptable for some patients with schizophrenia, more gradual discontinuation may be most appropriate for others. In all cases, the period of overlapping antipsychotic administration should be minimized. This drug is not approved for the treatment of patients with Dementia-Related Psychosis.
    Paediatric population: Safety and efficacy of Iloperidone in patients <18 years of age have not been established. No data are available.
    Renal impairment: Because Iloperidone is highly metabolized, with less than 1% of the medicinal product excreted unchanged, renal impairment alone is unlikely to have a significant impact on the pharmacokinetics of Iloperidone. See prescribing information for full details.
    Hepatic impairment: A study in mild and moderate liver impairment has not been conducted. Iloperidone is not recommended for patients with hepatic impairment. See prescribing information for full details.
    Elderly: Clinical studies of Iloperidone in the treatment of schizophrenia did not include sufficient numbers of patients aged 65 years and over to determine whether or not they respond differently than younger adult patients.
    See prescribing information for full details. 


    Indications

    An atypical antipsychotic agent indicated for the treatment of schizophrenia in adult.


    Contra-Indications

    Hypersensitivity to the active substance, or to any of the excipients.


    Special Precautions

    During antipsychotic treatment, improvement in the patient’s clinical condition may takebvseveral days to some weeks. Patients should be closely monitored during this period.
    QT interval: Use of this product should be avoided in patients with known cardiovascular disease or family history of QT prolongation, and in concomitant use with other medicines thought to prolong the QT interval including Class 1A (e.g., quinidine, procainamide) or Class III (e.g., amiodarone, sotalol) antiarrhythmic medicinal products, antipsychotic medicinal products (e.g., chlorpromazine, thioridazine), antibiotics (e.g., gatifloxacin, moxifloxacin), or any other class of medicinal products known to prolong the QTc inteval (e.g., pentamidine, levomethadyl acetate, methadone).
    Neuroleptic malignant syndrome: Neuroleptic Malignant Syndrome (NMS), characterised by hyperthermia, muscle rigidity, autonomic instability, altered consciousness, and elevated serum creatine phosphokinase levels has been reported to occur with Iloperidone. Additional clinical signs may include myoglobinuria (rhabdomyolysis) and acute renal failure. If a patient develops signs or symptoms indicative of NMS, all antipsychotics, includingIloperidone, should be discontinued.
    Tardive dyskinesia: Medicinal products with dopamine receptor antagonistic properties have been associated with the induction of tardive dyskinesia characterized by rhythmical, involuntary movements, predominantly of the tongue and/or face. If signs and symptoms of tardive dyskinesia appear, the discontinuation of all antipsychotics, includingIloperidone, should be considered.
    Hyperglycaemia and diabetes mellitus: Hyperglycemia, in some cases extreme and associated with ketoacidosis or hyperosmolar coma or death, has been reported in patients treated with atypical antipsychotics including Iloperidone. Assessment of the relationship between atypical antipsychotic use and glucose abnormalities is complicated by the possibility of an increased background risk of diabetes mellitus in patients with schizophrenia and the increasing incidence of diabetes mellitus in the general population. Given these confounders, the relationship between atypical antipsychotic use and hyperglycemia-related adverse reactions is not completely understood. However, epidemiological studies suggest an increased risk of treatment-emergent hyperglycemia related adverse reactions in patients treated with the atypical antipsychotics included in these studies. Because Iloperidone was not marketed at the time these studies were performed, it is not known if Iloperidone is associated with this increased risk. Precise risk estimates for hyperglycemia-related adverse reactions in patients treated with atypical antipsychotics are not available. Patients with an established diagnosis of diabetes mellitus who are started on atypical antipsychotics should be monitored regularly for worsening of glucose control. Patients with risk factors for diabetes mellitus (e.g., obesity, family history of diabetes) who are starting treatment with atypical antipsychotics should undergo fasting blood glucose testing at the beginning of treatment and periodically during treatment. Any patient treated with atypical antipsychotics should be monitored for symptoms of hyperglycemia including polydipsia, polyuria, polyphagia, and weakness. Patients who develop symptoms of hyperglycemia during treatment with atypical antipsychotics should undergo fasting blood glucose testing. In some cases, hyperglycemia has resolved when the atypical antipsychotic was discontinued; however, some patients required continuation of antidiabetic treatment despite discontinuation of the suspect drug.
    Orthostatic hypotension: Iloperidone may induce orthostatic hypotension in some patients based on its alpha-blocking activity. Based on pooled data from four, placebo-controlled, 4- or 6-week, fixed- and flexible-dose trials with Iloperidone, orthostatic hypotension was reported in 3% of patients treated with 10-16 mg/day Iloperidone, 5% of patients treated with 20-24 mg/day Iloperidone, compared with 1% of patients treated with placebo.
    See prescribing information for full details.


    Side Effects

    Dizziness, dry mouth, fatigue, nasal congestion, orthostatic hypotension, somnolence (including sedation), tachycardia, and weight gain.
    See prescribing information for full details.


    Drug interactions

    The Iloperidone dose should be reduced by one-half when administered concomitantly with strong CYP2D6 inhibitors, such as fluoxetine or paroxetine, and/or strong CYP3A4 inhibitors, such as ketoconazole or clarithromycin. When the CYP2D6 and/or CYP3A4 inhibitor(s) is withdrawn from the combination therapy, theIloperidone dose should then be increased to where it was before. Iloperidone should be reduced by one-half for poor metabolizers of CYP2D6.


    Pregnancy and Lactation

    Pregnancy: There are no adequate data for the use of Iloperidone in pregnant women. Iloperidone was not teratogenic in animal studies. See prescribing information for full details.
    Lactation:  It is unknown whether Iloperidone is excreted in human breast milk. Animal studies have shown excretion of Iloperidone in breast milk. This drug should not be used while breast feeding. 


    Overdose

    There is no specific antidote for Iloperidone. Therefore, appropriate supportive measures should be instituted. In case of acute overdose, the physician should establish and maintain an airway and ensure adequate oxygenation and ventilation. Gastric lavage (after intubation, if patient is unconscious) and administration of activated charcoal together with a laxative should be considered. The possibility of obtundation, seizures or dystonic reaction of the head and neck following overdose may create a risk of aspiration with induced emesis. Cardiovascular monitoring should commence immediately and should include continuous ECG monitoring to detect possible arrhythmias. If antiarrhythmic therapy is administered, disopyramide, procainamide and quinidine should not be used, as they have the potential for QT prolonging effects that might be additive to those of Iloperidone. Similarly, it is reasonable to expect that the alpha-blocking properties of bretylium might be additive to those of Iloperidone, resulting in problematic hypotension. Hypotension and circulatory collapse should be treated with appropriate measures such as intravenous fluids or sympathomimetic agents (epinephrine and dopamine should not be used, since beta stimulation may worsen hypotension in the setting of Iloperidone-induced alpha blockade). In cases of severe extrapyramidal symptoms, anticholinergic medication should be administered. Close medical supervision should continue until the patient recovers.
    See prescribing information for full details.  


    Manufacturer
    Patheon Inc. Canada
    Licence holder
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