쐽 Iloperidone ꔴ SPECIAL CONCERNS 
 쐽 SPECIAL CONCERNS 
 ( EYE - loh - PER - i - done ) 
 Classification ( s ) : Antipsychotic . 
 RX : Fanapt . 
 Acute treatment of schizophrenia in adults . 
 NOTE : When deciding whether to prescribe iloperidone , consider the drug is associated with prolongation of the QTc interval . 
 ACTION / KINETICS 
 and , low affinity for serotonin 5 - HT 1 A , dopamine 
 D 1 , and histamine H 1 receptors . Manifests moderate incidence of sedation and orthostatic hypotension and a low incidence of extrapyramidal symptoms , anticholinergic effects , and weight gain . 
 plasma levels : 2 – 4 hr . Can be given without regard to meals . Metabolized primarily by three 
 poor metabolizers . One of the metabolites ( P 88 ) 
 is active . Excreted in both the urine ( about 50 %) 
 and feces ( about 20 %). t 1 / 2 , elimination : 18 , 26 , 
 and 23 hr , respectively , for iloperidone , P 88 , and 
 P 95 ( another metabolite ) in extensive metabolizers and 33 , 37 , and 31 hr , respectively , for poor 
 metabolizers . Plasma protein binding : About 
 Hypersensitivity to iloperidone or any component 
 of the product . Use with other drugs known to 
 prolong QTc . Use in those with hepatic impairment , in those with dementia - related psychosis , in 
 those with congenital long QT syndrome , in 
 those with a history of cardiac arrhythmias , in 
 those with a history of significant CV illness ( e . g . , 
 QT prolongation , recent acute MI , uncompensated heart failure ) . Lactation . 
 ꔴ ( 1 ) Increased mortality in elderly clients 
 with dementia - related psychosis . Elderly 
 clients with dementia - related psychosis treated with antipsychotic drugs are at an increased risk of death . Analysis of 17 placebocontrolled trials ( modal duration , 10 weeks ) , 
 largely in clients taking atypical antipsychotic 
 drugs , revealed a risk of death in the drugtreated clients of between 1 . 6 and 1 . 7 times 
 the risk of death in placebo - treated clients . 
 Over the course of a typical 10 - week controlled trial , the rate of death in drug - treated 
 clients was about 4 . 5 %, compared with a rate 
 of about 2 . 6 % in the placebo group . Although 
 the causes of death were varied , most of the 
 deaths appeared to be either CV ( e . g . , heart 
 failure , sudden death ) or infectious ( e . g . , 
 pneumonia ) in nature . ( 2 ) Observational 
 studies suggest that , similar to atypical antipsychotic drugs , treatment with conventional 
 antipsychotic drugs may increase mortality . 
 The extent to which the findings of increased 
 mortality in observational studies may be attributed to antipsychotic drug as opposed to 
 some characteristic ( s ) of the clients is not 
 clear . ( 3 ) Iloperidone is not approved for the 
 treatment of clients with dementia - related 
 psychosis . ꔴ 
 ● Use with caution with known CV disease ( e . g . , 
 heart failure , history of MI ischemia , conduction 
 abnormalities ) , CV disease , or conditions that 
 predispose to hypotension ( e . g . , dehydration , hypovolemia , antihypertensive drugs ) . 
 ● Use with caution in those at risk for aspiration 
 pneumonia ( e . g . , elderly especially those with 
 advanced Alzheimer ’ s dementia ) . 
 ● Those with Parkinson ’ s disease or dementia have 
 an increased sensitivity to antipsychotic drugs . 
 ● Use with caution when used with other CNS 
 ● Safety and efficacy not known in children and 
 Dizziness , dry mouth , fatigue , nasal congestion , 
 somnolence , tachycardia , orthostatic hypotension , 
 CNS : Dizziness , somnolence , extrapyramidal disorder , tremor , lethargy , tardive dyskinesia , extra - 
 pyramidal symptoms ( akathisia , bradykinesia , dyskinesia , Parkinsonism , tremor ) , dystonia , pseudoparkinsonism , vertigo , depression ( may be significant ) , seizures , suicide attempt , paresthesia , 
 psychomotor hyperactivity , restlessness , amnesia , 
 aggression , delusion , hostility , paranoia , confusional state , mania , catatonia , mood swings , panic 
 attack , OCD , bulimia nervosa , delirium , psychogenic polydipsia , impulse - control disorder . Impaired judgment , thinking , or motor skills . GI : 
 Nausea , dry mouth , diarrhea , abdominal discomfort , dysphagia , gastritis , salivary hypersecretion , 
 fecal incontinence , mouth ulceration , aphthous 
 stomatitis , duodenal ulcer , esophageal ulcer , esophagitis , hiatal hernia , hyperchlorhydria , lip ulceration , GERD , reflux esophagitis , stomatitis , cholelithiasis . CV : Tachycardia , bradycardia , orthostatic hypotension , hypotension , syncope , palpitations , arrhythmia , first - degree AV block , CHF , 
 acute cardiac failure . Prolongation of QT interval leading to arrhythmia ( including torsades de 
 pointes and sudden death ) . NOTE : Elderly 
 clients with dementia - related psychosis are at an 
 increased risk of death and CV - related side effects , 
 including stroke . Respiratory : Nasopharyngitis , 
 URTI , bronchopneumonia , nasal congestion , 
 dyspnea , epistaxis , asthma , rhinorrhea , sinus congestion , nasal dryness , dry throat , sleep apnea syndrome , exertional dyspnea . Musculoskeletal : Arthralgia , joint pain , musculoskeletal stiffness , difficulty walking , myalgia , muscle spasms , torticollis , 
 restless legs syndrome . Dermatologic : Rash , skin 
 pigmentation ( especially in women on long - term 
 therapy ) . GU : Ejaculation failure , priapism , decreased / loss of libido , anorgasmia , urinary incontinence , dysuria , pollakiuria , enuresis , nephrolithiasis , urinary retention , acute renal failure , erectile dysfunction , testicular pain , amenorrhea , 
 breast pain , irregular menses , gynecomastia , menorrhagia , metrorrhagia , menstrual irregularities , 
 urinary retention , postmenopausal hemorrhage , 
 prostatitis . Metabolic / Endocrine : Hyperglycemia , diabetes mellitus , hypothyroidism . Hematologic : Leukopenia , neutropenia , anemia , iron deficiency anemia , thrombocytopenia , agranulocytosis . Ophthalmic : Blurred vision , conjunctivitis 
 ( including allergic ) , dry eyes , blepharitis , eyelid 
 edema , eye swelling , lenticular / corneal opacities , 
 cataract , hyperemia , nystagmus . Otic : Tinnitus . 
 Body as a whole : Fatigue , weight gain / loss , edema , thirst , hyperthermia , dehydration , fluid reten - 
 tion . Miscellaneous : Neuromalignant syndrome 
 ( including symptoms of hyperpyrexia , muscle rigidity , altered mental status , catatonic signs , irregular pulse or BP , tachycardia , diaphoresis , cardiac 
 dysrhythmia , rhabdomyolysis , acute renal failure ) . 
 Disruption of control of body temperature , increased appetite . 
 LABORATORY TEST CONSIDERATIONS 
 e Neutrophils . a H & H . Hyperprolactinemia , hypokalemia . 
 use together contraindicated 
 Chlorpromazine / Prolongation of QTc interval c 
 cardiac arrhythmias , including torsades de 
 Fluoxetine / e Iloperidone blood levels R / T inhibition of CYP 2 D 6 
 Ketoconazole / e Iloperidone blood levels R / T inhibition of CYP 3 A 4 
 Moxifloxacin / Prolongation of QTc interval c 
 Paroxetine / e Iloperidone blood levels R / T inhibition of CYP 2 D 6 
 Pentamidine / Prolongation of QTc interval c 
 Procainamide / Prolongation of QTc interval c 
 together contraindicated 
 Sotalol / Prolongation of QTc interval c cardiac 
 Thioridazine / Prolongation of QTc interval c 
 Tablets : 1 mg , 2 mg , 4 mg , 6 mg , 8 mg , 10 mg , 
 Adults , initial : 1 mg twice a day on 
 twice a day on days , 2 , 3 , 4 , 5 , 6 , and 7 
 respectively . Maintenance : 6 – 12 mg 
 twice a day . Maximum dose : 12 mg 
 twice a day ( i . e . , 24 mg / day ) . No data 
 are available to determine the length of 
 should be continued beyond the acute 
 response . Periodically reassess to determine the need for continued treatment . 
 IMPLEMENTATION / ADMINISTRATION / STORAGE 
 1 . Dosage adjustment is not routinely indicated 
 on the basis of age , gender , race , or renal impairment . 
 2 . Can be given without regard to meals . 
 3 . Titrate slowly from a starting dose to avoid orthostatic hypotension ( iloperidone is an alpha - adrenergic blocker ) . 
 4 . Clients must be titrated to an effective dose . 
 Thus , control of symptoms may be delayed 
 during the first 1 – 2 weeks of therapy compared with some other antipsychotic drugs 
 that do not require similar titration . 
 5 . Reduce the dose of iloperidone by one - half if 
 coadministered with strong CYP 2 D 6 inhibitors 
 ( e . g . , fluoxetine , paroxetine ) . When the 
 CYP 2 D 6 inhibitor is withdrawn , increase the iloperidone dose to where it was before . 
 6 . Reduce the dose of iloperidone by one - half if 
 coadministered with strong CYP 3 A 4 inhibitors 
 ( e . g . , clarithromycin , ketoconazole ) . When the 
 CYP 3 A 4 inhibitor is withdrawn , increase the iloperidone dose to where it was before . 
 7 . Poor metabolizers of CYP 2 D 6 have a higher 
 exposure to iloperidone compared with extensive metabolizers . Laboratory tests can determine CYP 2 D 6 poor metabolizers . 
 8 . Whenever a client has had an interval of more 
 than 3 days off iloperidone , reinitiate using a 
 titration schedule . 
 9 . When switching from other antipsychotics , 
 immediate discontinuation may be appropri - 
 ate for some clients but not others . In all 
 cases , the period of overlapping medications 
 10 . Store from 15 – 30 ° C ( 59 – 86 ° F ) . Protect from 
 1 . Note reasons for therapy , clinical , and behavioral manifestations , other agents trialed and 
 2 . Assess for any history of CVD , QT prolongation , arrhythmias , or dementia related psychosis . 
 3 . Monitor VS , ECG , weight , CBC , K +, Mg ++, BS , 
 renal and LFTs . 
 1 . Review dosing guidelines and take as prescribed with or without food . Drug is started at 
 a low dose and titrated up slowly to prevent 
 sudden drop in BP . 
 2 . Avoid activities that require mental alertness 
 3 . Change positions slowly to prevent a sudden 
 drop in BP . Hot tubs , hot showers , or baths 
 may aggravate dizziness . 
 4 . Practice reliable contraception , report if pregnancy suspected . 
 5 . May alter temperature regulation . Avoid alcohol , CNS depressants , OTC agents , strenuous 
 exercise , overheating , or dehydration . 
 6 . Report any suicide ideations , change in ability 
 to interact or increased psychosis . 
 7 . Any S & S of NMS ( neuroleptic malignant syndrome ) : increased temperature , muscle rigidity , irregular heart rate / BP , arrhythmias , or severe diaphoresis require immediate attention . 
 9 . Keep all F / U to assess response and for adverse SE . 
 OUTCOMES / EVALUATE 
 ● Improvement in PANSS and DSM III / IV - TR 
 ● Improved behavioral and emotional presentation 
 ● a Delusions / suspiciousness and hostility 
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