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Fanapt
iloperidone
Black Box Warnings .
Dementia-Related Psychosis
not approved for dementia-related psychosis; incr. mortality risk in elderly pts on antipsychotic tx for dementia-related psychosis; most deaths due to cardiovascular or infectious events
Adult Dosing .
Dosage forms: TAB: 1 mg, 2 mg, 4 mg, 6 mg, 8 mg, 10 mg, 12 mg; convenience pack
Special Note
- [convenience pack components]
- Info: titration pack contains 1 mg tab x2 and 2 mg tab x2 and 4 mg tab x2 and 6 mg tab x2
schizophrenia
- [6-12 mg PO bid]
- Start: 1 mg PO bid on day 1, then 2 mg PO bid on day 2, then incr. by 4 mg/day to target dose; Max: 24 mg/day; Info: may use convenience pack for titration; decr. maint. dose by 50% in CYP2D6 poor metabolizers, see pkg insert for titration; periodically reassess need for tx; D/C if ANC <1000; consider D/C if unexplained decr. in WBC
bipolar I disorder, acute manic/mixed
- [12 mg PO bid]
- Start: 1 mg PO bid on day 1, then 3 mg PO bid on day 2, then incr. by 6 mg/day x3 days to target 12 mg PO bid; Max: 24 mg/day; Info: decr. maint. dose by 50% in CYP2D6 poor metabolizers, see pkg insert for titration; periodically reassess need for tx; D/C if ANC <1000; consider D/C if unexplained decr. in WBC
renal dosing
- [see below]
- renal impairment: no adjustment
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B: consider decr. usual dose; Child-Pugh Class C: not defined
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- glaucoma surgery
- cataract surgery
- long QT syndrome, congenital
- arrhythmia hx
- MI, recent
- heart failure, decompensated
- QT prolongation
- caution: QT prolongation family hx
- caution: bradycardia
- caution: electrolyte abnormalities
- caution: hypokalemia
- caution: hypomagnesemia
- caution: cardiovascular dz
- caution: cerebrovascular dz
- caution: CYP2D6 poor metabolizers
- caution: hepatic impairment, Child-Pugh Class B-C
- caution: elderly pts
- caution: psychosis, dementia-associated
- caution: aspiration pneumonia risk
- caution: diabetes mellitus
- caution: diabetes mellitus risk
- caution: neuroleptic malignant syndrome hx
- caution: seizure hx
- caution: seizure risk
- caution: hypovolemia
- caution: dehydration
- caution: environmental temperature, high
- caution: leukopenia
- caution: leukopenia hx, drug-induced
- caution: neutropenia
- caution: neutropenia hx, drug-induced
Drug Interactions .
Overview
iloperidone
atypical antipsychotic
- CYP2D6 substrate
- CYP3A4 substrate
- CNS depression
- decreases central histamine effects
- dopamine antagonist
- extrapyramidal effects
- hyperglycemic effects
- hyperprolactinemic effects
- hyperthermia
- hypotensive effects
- lowers seizure threshold
- myelosuppressive effects
- prolongs QT interval (conditional)
Contraindicated
- pimozide
- quinidine (CYP2D6 inhibitor)
- thioridazine
Avoid/Use Alternative
- adagrasib
- aldesleukin
- alfuzosin
- amifampridine
- amiodarone
- anagrelide
- apalutamide
- apomorphine
- aripiprazole bimonthly injection
- aripiprazole lauroxil
- aripiprazole monthly injection
- aripiprazole oral
- arsenic trioxide
- artemether/lumefantrine
- asenapine
- azithromycin
- bedaquiline
- benztropine
- bromocriptine
- butalbital
- cabergoline
- cabozantinib
- ceritinib
- chloroquine
- cisapride
- citalopram
- cladribine oral
- clarithromycin
- clofazimine
- clonidine
- codeine
- crizotinib
- deferiprone
- degarelix
- desflurane
- desipramine
- dexmedetomidine
- dexmedetomidine injection
- disopyramide
- dofetilide
- domperidone
- donepezil
- doxazosin
- doxylamine
- dronedarone
- droperidol
- encorafenib
- ephedra
- epirubicin
- eribulin
- erythromycin
- ethanol
- fexinidazole
- flecainide
- fluorouracil
- ganciclovir
- gilteritinib
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- histrelin
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- hydroxychloroquine
- hydroxyzine
- ibutilide
- inotuzumab ozogamicin
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- ivosidenib
- kava
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- levofloxacin
- levoketoconazole
- lofexidine
- lonafarnib
- macimorelin
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- midazolam
- mobocertinib
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- netupitant
- nilotinib
- oliceridine
- ondansetron
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- panobinostat
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- phenoxybenzamine
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- pitolisant
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- primaquine
- procainamide
- promethazine
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- quinine
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- revumenib
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- romidepsin
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- selegiline transdermal
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- sotalol
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- telavancin
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- tetrabenazine
- thalidomide
- toremifene
- tramadol
- tranylcypromine
- triclabendazole
- trifluridine
- trimethobenzamide
- triptorelin
- valganciclovir
- vandetanib
- vemurafenib
- yohimbe
- ziprasidone
- zuranolone
Monitor/Modify Tx
- abemaciclib
- abiraterone acetate
- acalabrutinib
- acarbose
- acebutolol
- ado-trastuzumab emtansine
- afamitresgene autoleucel
- albendazole
- alemtuzumab
- alfentanil
- aliskiren
- allopurinol
- alogliptin
- alprazolam
- amantadine
- amifostine
- amiloride
- amitriptyline
- amlodipine
- amoxapine
- anti-thymocyte globulin
- apraclonidine ophthalmic
- aprepitant
- aprocitentan
- articaine
- asciminib
- atazanavir
- atenolol
- atidarsagene autotemcel
- auranofin
- avacopan
- avanafil
- axicabtagene ciloleucel
- azacitidine
- azathioprine
- azilsartan medoxomil
- baclofen intrathecal
- balsalazide
- baricitinib
- belantamab mafodotin
- belinostat
- benazepril
- bendamustine
- benznidazole
- berberine
- berotralstat
- betaxolol
- betaxolol ophthalmic
- bethanechol
- betibeglogene autotemcel
- bevacizumab
- bexagliflozin
- bexarotene
- bisoprolol
- blinatumomab
- bortezomib
- bosutinib
- brentuximab vedotin
- brexpiprazole
- brexucabtagene autoleucel
- brimonidine ophthalmic
- brimonidine topical
- bumetanide
- bupivacaine
- bupivacaine liposomal
- buprenorphine
- bupropion
- busulfan
- butorphanol
- cabazitaxel
- canagliflozin
- candesartan cilexetil
- cannabis
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- capivasertib
- captopril
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- carboplatin
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- carmustine
- carteolol ophthalmic
- carvedilol
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- chlordiazepoxide
- chloroprocaine
- chlorothiazide
- chlorpromazine
- chlorthalidone
- cidofovir
- cilostazol
- ciltacabtagene autoleucel
- cinacalcet
- ciprofloxacin
- cisplatin
- cladribine injection
- clevidipine
- clobazam
- clofarabine
- clomipramine
- clonazepam
- clorazepate
- clozapine
- cobicistat
- coenzyme Q-10
- colchicine
- colesevelam
- conivaptan
- copanlisib
- cyclophosphamide
- cyclosporine
- cytarabine
- dacarbazine
- dacomitinib
- dactinomycin
- danazol
- dapagliflozin
- dapsone
- daratumumab
- daridorexant
- darunavir
- dasatinib
- daunorubicin
- decitabine
- deferasirox
- denileukin diftitox
- deuruxolitinib
- dexrazoxane
- diazepam
- dihydrocodeine
- diltiazem
- dinutuximab
- dipyridamole
- docetaxel
- dostarlimab
- doxepin
- doxorubicin
- dronabinol
- dulaglutide
- duloxetine
- duvelisib
- eflornithine
- eliglustat
- elivaldogene autotemcel
- elranatamab
- empagliflozin
- enalapril
- enalaprilat
- enfortumab vedotin
- entacapone
- entrectinib
- epcoritamab
- eplerenone
- epoprostenol
- ertugliflozin
- esketamine
- esmolol
- estazolam
- eszopiclone
- ethacrynic acid
- ethanol (in some formulations)
- etomidate
- etoposide
- everolimus
- exagamglogene autotemcel
- exenatide
- fam-trastuzumab deruxtecan
- fedratinib
- felodipine
- fenoldopam
- fentanyl
- ferumoxytol
- flaxseed
- flibanserin
- floxuridine
- fluconazole
- flucytosine
- fludarabine
- fluoxetine
- fluphenazine
- flurazepam
- fosamprenavir
- foscarnet
- fosinopril
- foslevodopa
- fostamatinib
- furosemide
- gabapentin
- gabapentin enacarbil
- garlic
- gemcitabine
- gemtuzumab ozogamicin
- givinostat
- givosiran
- glimepiride
- glipizide
- glofitamab
- glyburide
- grapefruit
- guanfacine
- hydralazine
- hydrochlorothiazide
- hydromorphone
- hydroxyurea
- ibritumomab tiuxetan
- ibrutinib
- idarubicin
- idecabtagene vicleucel
- idelalisib
- ifosfamide
- iloprost
- iloprost inhaled
- imatinib
- imetelstat
- imipramine
- indapamide
- insulin
- interferon beta 1a
- interferon beta 1b
- interferon gamma 1b
- iohexol
- iopamidol
- irbesartan
- irinotecan
- iron sucrose
- isatuximab
- isavuconazonium
- isosorbide dinitrate
- isosorbide mononitrate
- isradipine
- itraconazole
- ixabepilone
- ketamine
- ketoconazole
- labetalol
- landiolol
- leflunomide
- lemborexant
- lenacapavir
- lenalidomide
- letermovir
- levobunolol ophthalmic
- levodopa
- levorphanol
- lidocaine
- lifileucel
- linagliptin
- linezolid
- liraglutide
- lisinopril
- lisocabtagene maraleucel
- lithium
- lomustine
- loncastuximab tesirine
- lopinavir/ritonavir
- lorazepam
- losartan
- lovotibeglogene autotemcel
- loxapine
- lubiprostone
- lumateperone
- lurasidone
- lurbinectedin
- lutetium Lu 177 dotatate
- lutetium Lu 177 vipivotide tetraxetan
- lymphocyte immune globulin, anti-thymocyte globulin
- magnesium sulfate
- maraviroc
- mavorixafor
- melphalan
- meperidine
- mepivacaine
- mercaptopurine
- mesalamine
- mesalamine rectal
- metformin
- methohexital
- methotrexate
- methyldopa
- methylene blue injection
- metolazone
- metoprolol
- midostaurin
- mifepristone
- miglitol
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- minoxidil
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- mirtazapine
- mitomycin
- mitotane
- mitoxantrone
- moexipril
- mogamulizumab
- molindone
- momelotinib
- morphine
- mosunetuzumab
- mycophenolate mofetil
- mycophenolic acid
- nadolol
- nalbuphine
- nateglinide
- nattokinase
- naxitamab
- nebivolol
- nefazodone
- nelarabine
- nelfinavir
- niacin (vitamin B3)
- nicardipine
- nifedipine
- nimodipine
- niraparib
- nirogacestat
- nisoldipine
- nitric oxide
- nitrite
- nitroglycerin
- nitroprusside
- nortriptyline
- obecabtagene autoleucel
- obinutuzumab
- ofatumumab
- olanzapine
- olaparib
- olmesartan medoxomil
- olsalazine
- omacetaxine mepesuccinate
- opicapone
- opium
- oxaliplatin
- oxazepam
- oxybutynin
- oxycodone
- oxymorphone
- paclitaxel
- palbociclib
- palopegteriparatide
- paroxetine
- peginterferon alfa 2a
- peginterferon beta 1a
- pemetrexed
- penicillamine
- pentazocine
- pentobarbital
- pentostatin
- perindopril
- perphenazine
- phenobarbital
- pindolol
- pioglitazone
- pirtobrutinib
- polatuzumab vedotin
- pomalidomide
- ponatinib
- posaconazole
- pralatrexate
- pramipexole
- pramlintide
- pregabalin
- primidone
- procarbazine
- prochlorperazine
- proguanil
- propofol
- propranolol
- protriptyline
- pyrimethamine
- quazepam
- quetiapine
- quinapril
- ramipril
- rasagiline
- remifentanil
- remimazolam
- repaglinide
- rifabutin
- riociguat
- risperidone
- ritonavir
- rituximab
- rolapitant
- ropinirole
- ropivacaine
- rosiglitazone
- rotigotine transdermal
- ruxolitinib
- ruxolitinib topical
- sacituzumab govitecan
- sacubitril
- safinamide
- sarilumab
- satralizumab
- saxagliptin
- selegiline
- selinexor
- semaglutide
- sildenafil
- sirolimus
- sirolimus albumin-bound
- sitagliptin
- sodium ferric gluconate complex
- sotagliflozin
- sparsentan
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- teclistamab
- telmisartan
- temazepam
- temozolomide
- temsirolimus
- teplizumab
- terbinafine
- teriflunomide
- thioguanine
- thiotepa
- thiothixene
- timolol
- timolol ophthalmic
- tipranavir
- tirzepatide
- tisagenlecleucel
- tizanidine
- tocilizumab
- tofacitinib
- tolcapone
- topotecan
- torsemide
- trabectedin
- trandolapril
- trastuzumab
- trazodone
- treosulfan
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- triazolam
- trifluoperazine
- trimethoprim
- trimipramine
- tucatinib
- upadacitinib
- valproic acid
- valsartan
- vardenafil
- venetoclax
- verapamil
- vinblastine
- vincristine
- vinorelbine
- voriconazole
- vosoritide
- zaleplon
- zanubrutinib
- ziconotide
- zidovudine
- ziv-aflibercept
- zolpidem
Caution Advised
- 5-HTP
- acetazolamide
- aclidinium inhaled
- almotriptan
- atropine
- baclofen
- belladonna alkaloids
- botulinum toxin
- brivaracetam
- brompheniramine
- buspirone
- cannabidiol
- carbinoxamine
- carisoprodol
- cenobamate
- cetirizine
- chamomile, German
- chasteberry
- chlophedianol
- chlorpheniramine
- chlorzoxazone
- clemastine
- clidinium
- cyclobenzaprine
- cyproheptadine
- dantrolene
- darifenacin
- desvenlafaxine
- deutetrabenazine
- dexbrompheniramine
- dexchlorpheniramine
- dichlorphenamide
- dicyclomine
- difelikefalin
- difenoxin
- dimenhydrinate
- diphenhydramine
- diphenoxylate
- doxepin topical
- efavirenz
- eletriptan
- escitalopram
- eslicarbazepine acetate
- ethosuximide
- felbamate
- fenfluramine
- fesoterodine
- flavoxate
- fluvoxamine
- fosphenytoin
- frovatriptan
- galantamine
- ganaxolone
- glycopyrrolate
- glycopyrrolate inhaled
- glycopyrronium topical
- homatropine
- hyoscyamine
- ipratropium inhaled
- lacosamide
- lamotrigine
- lasmiditan
- levetiracetam
- levocetirizine
- levomilnacipran
- lindane topical
- magnesium citrate
- meclizine
- melatonin
- meprobamate
- methocarbamol
- methscopolamine
- methsuximide
- metyrapone
- metyrosine
- milnacipran
- naltrexone
- naratriptan
- orphenadrine
- oxcarbazepine
- passion flower
- perampanel
- pheniramine
- phenytoin
- polyethylene glycol
- polyethylene glycol/electrolytes
- pyrilamine
- ramelteon
- repotrectinib
- revefenacin inhaled
- rivastigmine
- rizatriptan
- rufinamide
- scopolamine
- sertraline
- sodium picosulfate
- sofpironium topical
- solifenacin
- solriamfetol
- sulfate bowel prep
- sumatriptan
- tasimelteon
- tiagabine
- tiotropium inhaled
- tolterodine
- topiramate
- trihexyphenidyl
- triprolidine
- trospium
- umeclidinium inhaled
- valbenazine
- valerian
- venlafaxine
- vigabatrin
- vilazodone
- viloxazine
- zolmitriptan
- zonisamide
Adverse Reactions .
Serious Reactions
- QT prolongation
- arrhythmia
- AV block
- cardiac failure
- hypotension, orthostatic
- syncope
- stroke
- neuroleptic malignant syndrome
- hyperthermia
- priapism
- extrapyramidal sx
- tardive dyskinesia
- dystonia
- hyperglycemia
- diabetes mellitus
- seizures
- leukopenia
- neutropenia
- agranulocytosis
- anemia
- dysphagia, severe
- hypersensitivity rxn
- anaphylaxis
- angioedema
- intraoperative floppy iris syndrome
Common Reactions
- dizziness
- somnolence
- tachycardia
- nausea
- xerostomia
- ALT or AST incr.
- weight gain
- dyslipidemia
- hyperglycemia
- nasal congestion
- diarrhea
- fatigue
- headache
- hypotension, orthostatic
- extrapyramidal sx
- arthralgia
- musculoskeletal stiffness
- abdominal discomfort
- abdominal pain
- nasopharyngitis
- URI
- hypotension
- tremor
- akathisia
- ejaculatory dysfxn
- dyspnea
- rash
- blurred vision
- lethargy
- hyperprolactinemia
- impaired body temperature regulation
Safety/Monitoring .
Monitoring Parameters
fasting glucose and lipid panel at baseline, then periodically; K, Mg at baseline if electrolyte disturbance risk, then periodically; CBC w/ diff frequently during initial tx if pre-existing or hx of leukopenia/neutropenia; consider orthostatic vital signs if hypotension risk; weight
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy, esp. in 3rd trimester; inadequate human data available, though risk of neonatal extrapyramidal and withdrawal sx based on human data w/ other antipsychotics; no known risk of teratogenicity, though possible risk of decr. fetal growth and fetal death based on animal data at 20x and 26x MRHD
Pregnancy Registry
encourage pts to enroll in National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or www.womensmentalhealth.org
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; no human data available to assess risk of infant harm or effects on milk production
Pharmacology .
Metabolism: liver extensively; CYP450: 2D6, 3A4 substrate; Info: active metabolites
Excretion: urine 45-58% (<1% unchanged), feces 20-22%; Half-life: 18h (CYP2D6 extensive metabolizers), 33h (CYP2D6 poor metabolizers)
Subclass: Antipsychotics, 2nd generation ; Bipolar Disorder
Mechanism of Action
exact mechanism of action unknown; antagonizes dopamine D2 receptors, serotonin 5-HT2 receptors, others
Formulary .
No Formulary Selected
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