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Rexulti
brexpiprazole
Black Box Warnings .
Dementia-Related Psychosis
not approved for dementia-related psychosis without agitation associated with dementia due to Alzheimer disease; incr. mortality risk in elderly patients on antipsychotic tx for dementia-related psychosis; most deaths due to cardiovascular or infectious events
Suicidality
incr. suicidality risk in peds and young adult patients in short-term studies; observe all antidepressant-treated patients for clinical worsening, suicidality, or unusual behavior changes; advise families and caregivers of need for close observation and communication with prescriber; not approved for depression in peds patients
Adult Dosing .
Dosage forms: TAB: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg
major depressive disorder, adjunct tx
- [2 mg PO qd]
- Start: 0.5-1 mg PO qd, may incr. dose qwk; Max: 3 mg/day; Info: decr. dose 50% in CYP2D6 poor metabolizers; periodically reassess need for tx
schizophrenia
- [2-4 mg PO qd]
- Start: 1 mg PO qd x4 days, then 2 mg PO qd x3 days, then may incr. to 4 mg PO qd; Max: 4 mg/day; Info: decr. dose 50% in CYP2D6 poor metabolizers; periodically reassess need for tx
dementia-associated agitation, patients with Alzheimer disease
- [2 mg PO qd]
- Start: 0.5 mg PO qd x7 days, then 1 mg PO qd x7 days, then 2 mg PO qd, then may incr. to 3 mg PO qd after at least 14 days; Max: 3 mg/day; Info: decr. dose 50% in CYP2D6 poor metabolizers; periodically reassess need for tx
renal dosing
- [schizophrenia]
- CrCl <60: max 3 mg/day
- HD/PD: not defined
- [all other indications]
- CrCl <60: max 2 mg/day
- HD/PD: not defined
hepatic dosing
- [schizophrenia]
- Child-Pugh Class B or C: max 3 mg/day
- [all other indications]
- Child-Pugh Class B or C: max 2 mg/day
Peds Dosing .
- Dosage forms: TAB: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg
schizophrenia
- [13-17 yo]
- Dose: 2-4 mg PO qd; Start: 0.5 mg PO qd x4 days, then 1 mg PO qd x3 days, then may incr. to 2 mg PO qd, then may incr. by 1 mg/day qwk; Max: 4 mg/day; Info: decr. dose 50% in CYP2D6 poor metabolizers; periodically reassess need for tx
renal dosing
- [adjust dose amount]
- CrCl <60: max 3 mg/day
- HD/PD: not defined
hepatic dosing
- [adjust dose amount]
- Child-Pugh Class B or C: max 3 mg/day
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- caution: cardiovascular disease
- caution: MI history
- caution: ischemic heart disease
- caution: heart failure
- caution: hypovolemia
- caution: dehydration
- caution: hypotension, orthostatic
- caution: hepatic impairment, moderate-severe
- caution: CrCl <60
- caution: aspiration pneumonia risk
- caution: elderly patients
- caution: cerebrovascular disease
- caution: psychosis, dementia-associated
- caution: seizure history
- caution: seizure threshold, lowered
- caution: CYP2D6 poor metabolizers
- caution: diabetes mellitus
- caution: diabetes mellitus risk
- caution: environmental temperature, high
- caution: patients <25 yo (depression use)
- caution: leukopenia history, drug-induced
- caution: neutropenia history, drug-induced
- caution: leukopenia
- caution: neutropenia
Drug Interactions .
Overview
brexpiprazole
atypical antipsychotic
- CYP2D6 substrate
- CYP3A4 substrate
- CNS depression
- decreases central histamine effects
- extrapyramidal effects
- hyperglycemic effects
- hyperthermia
- hypotensive effects
- lowers seizure threshold
Avoid/Use Alternative
- aldesleukin
- amifampridine
- aripiprazole bimonthly injection
- aripiprazole lauroxil
- aripiprazole monthly injection
- aripiprazole oral
- asenapine
- benztropine
- butalbital
- clonidine
- codeine
- doxylamine
- ethanol (alcoholic beverage)
- ethanol injection
- grapefruit
- haloperidol
- hydrocodone
- iloperidone
- isocarboxazid
- kava
- kratom
- lofexidine
- lumateperone
- lurasidone
- metaxalone
- metoclopramide
- midazolam
- milsaperidone
- netupitant
- olanzapine
- oxybate
- phenelzine
- pitolisant
- promethazine
- ropeginterferon alfa-2b
- scopolamine
- thalidomide
- tradipitant
- tranylcypromine
- trimethobenzamide
- ziprasidone
- zuranolone
Monitor/Modify Tx
- abiraterone acetate
- acarbose
- acebutolol
- adagrasib
- alfentanil
- alfuzosin
- aliskiren
- alogliptin
- alprazolam
- alprostadil intracavernous
- amantadine
- amifostine
- amiloride
- amitriptyline
- amlodipine
- amoxapine
- apalutamide
- apomorphine
- apraclonidine ophthalmic
- aprepitant
- aprocitentan
- articaine
- atazanavir
- atenolol
- avacopan
- avanafil
- azilsartan medoxomil
- baclofen intrathecal
- benazepril
- berberine
- berotralstat
- betaxolol
- betaxolol ophthalmic
- bethanechol
- bexagliflozin
- bisoprolol
- bortezomib
- bosentan
- brimonidine ophthalmic
- brimonidine topical
- bromocriptine
- bumetanide
- bupivacaine
- bupivacaine liposomal
- buprenorphine
- bupropion
- butorphanol
- cabergoline
- canagliflozin
- candesartan cilexetil
- cannabis
- capivasertib
- captopril
- carbamazepine
- cariprazine
- carteolol ophthalmic
- carvedilol
- cenobamate
- ceritinib
- chloramphenicol
- chlordiazepoxide
- chloroprocaine
- chlorothiazide
- chlorpromazine
- chlorthalidone
- cilostazol
- cinacalcet
- ciprofloxacin
- clarithromycin
- clevidipine
- clobazam
- clofarabine
- clofazimine
- clomipramine
- clonazepam
- clorazepate
- clozapine
- cobicistat
- coenzyme Q-10
- colesevelam
- conivaptan
- crizotinib
- cyclosporine
- dabrafenib
- dacomitinib
- danazol
- dapagliflozin
- daridorexant
- darunavir
- denileukin diftitox
- desflurane
- desipramine
- dexmedetomidine
- dexmedetomidine injection
- diazepam
- dihydrocodeine
- diltiazem
- dinutuximab
- dipyridamole
- doxazosin
- doxepin
- dronabinol
- dronedarone
- droperidol
- dulaglutide
- duloxetine
- duvelisib
- efavirenz
- eliglustat
- empagliflozin
- enalapril
- enalaprilat
- encorafenib
- entacapone
- entrectinib
- enzalutamide
- eplerenone
- epoprostenol
- ertugliflozin
- erythromycin
- esketamine
- esmolol
- estazolam
- eszopiclone
- ethacrynic acid
- ethanol (in some formulations)
- etomidate
- etravirine
- etripamil nasal
- exenatide
- fedratinib
- felodipine
- fenoldopam
- fentanyl
- ferumoxytol
- fexinidazole
- flaxseed
- flibanserin
- fluconazole
- fluoxetine
- fluphenazine
- flurazepam
- fosamprenavir
- fosinopril
- foslevodopa
- fosphenytoin
- furosemide
- gabapentin
- gabapentin enacarbil
- garlic
- gilteritinib
- givosiran
- glimepiride
- glipizide
- glyburide
- guanfacine
- hydralazine
- hydrochlorothiazide
- hydromorphone
- hydroxyzine
- idelalisib
- ifosfamide
- iloprost
- imatinib
- imipramine
- indapamide
- insulin
- iohexol
- iopamidol
- irbesartan
- iron sucrose
- isavuconazonium
- isoflurane
- isosorbide dinitrate
- isosorbide mononitrate
- isradipine
- itraconazole
- ivosidenib
- ketamine
- ketoconazole
- labetalol
- landiolol
- lefamulin
- lemborexant
- lenacapavir
- letermovir
- levobunolol ophthalmic
- levodopa
- levoketoconazole
- levorphanol
- lidocaine
- linagliptin
- liraglutide
- lisinopril
- lithium
- lixisenatide
- lonafarnib
- lopinavir/ritonavir
- lorazepam
- lorlatinib
- losartan
- loxapine
- lubiprostone
- lumacaftor/ivacaftor
- magnesium sulfate
- maraviroc
- mavacamten
- mavorixafor
- meperidine
- mepivacaine
- metformin
- methadone
- methohexital
- methyldopa
- methylene blue injection
- metolazone
- metoprolol
- mifepristone
- miglitol
- milrinone
- minoxidil
- mirabegron
- mirtazapine
- mitapivat
- mitotane
- modafinil
- moexipril
- molindone
- morphine
- nadolol
- nafcillin
- nalbuphine
- nateglinide
- nattokinase
- naxitamab
- nebivolol
- nefazodone
- nelarabine
- nelfinavir
- niacin (vitamin B3)
- nicardipine
- nifedipine
- nilotinib
- nimodipine
- nirogacestat
- nisoldipine
- nitric oxide
- nitrite
- nitroglycerin
- nitroprusside
- nortriptyline
- obinutuzumab
- oliceridine
- olmesartan medoxomil
- opicapone
- opium
- oxazepam
- oxybutynin
- oxycodone
- oxymorphone
- pacritinib
- paliperidone
- palopegteriparatide
- paroxetine
- pentamidine
- pentazocine
- pentobarbital
- perindopril
- perphenazine
- pexidartinib
- phenobarbital
- phenoxybenzamine
- phentolamine
- phenytoin
- pindolol
- pioglitazone
- posaconazole
- pramipexole
- pramlintide
- prazosin
- pregabalin
- primidone
- procarbazine
- prochlorperazine
- propafenone
- propofol
- propranolol
- protriptyline
- quazepam
- quetiapine
- quinapril
- quinidine (antiarrhythmic)
- quinidine (CYP2D6 inhibitor)
- ramipril
- rasagiline
- remifentanil
- remimazolam
- repaglinide
- repotrectinib
- ribociclib
- rifabutin
- rifampin
- rifapentine
- rilzabrutinib
- riociguat
- risperidone
- ritonavir
- rolapitant
- ropinirole
- ropivacaine
- rosiglitazone
- rotigotine transdermal
- sacubitril
- safinamide
- saxagliptin
- selegiline
- selegiline transdermal
- semaglutide
- sevoflurane
- sildenafil
- silodosin
- sitagliptin
- sodium ferric gluconate complex
- sotagliflozin
- sotalol
- sotorasib
- sparsentan
- spironolactone
- St. John's wort
- sufentanil
- suvorexant
- tadalafil
- tagraxofusp
- tamsulosin
- tapentadol
- taurine
- telmisartan
- temazepam
- terazosin
- terbinafine
- thioridazine
- thiothixene
- timolol
- timolol ophthalmic
- tipranavir
- tirzepatide
- tizanidine
- tolcapone
- torsemide
- tramadol
- trandolapril
- trazodone
- treprostinil
- triamterene
- triazolam
- trifluoperazine
- trimipramine
- tucatinib
- valsartan
- vardenafil
- verapamil
- voriconazole
- vosoritide
- yohimbe
- zaleplon
- ziconotide
- zolpidem
Caution Advised
- 5-HTP
- acetazolamide
- aclidinium inhaled
- allopurinol
- almotriptan
- atropine
- baclofen
- belladonna alkaloids
- botulinum toxin
- brivaracetam
- brompheniramine
- buspirone
- busulfan
- cannabidiol
- carbinoxamine
- carisoprodol
- cetirizine
- chamomile, German
- chlophedianol
- chlorambucil
- chlorcyclizine
- chloroquine
- chlorpheniramine
- chlorzoxazone
- citalopram
- clemastine
- clidinium
- cyclobenzaprine
- cyproheptadine
- dantrolene
- darifenacin
- desvenlafaxine
- deutetrabenazine
- dexbrompheniramine
- dexchlorpheniramine
- dichlorphenamide
- dicyclomine
- difelikefalin
- difenoxin
- dimenhydrinate
- diphenhydramine
- diphenoxylate
- disopyramide
- domperidone
- doxepin topical
- eletriptan
- elinzanetant
- escitalopram
- eslicarbazepine acetate
- ethosuximide
- felbamate
- fenfluramine
- fesoterodine
- flavoxate
- fluvoxamine
- frovatriptan
- galantamine
- ganaxolone
- glofitamab
- glycopyrrolate
- glycopyrrolate inhaled
- glycopyrronium topical
- homatropine
- hydroxychloroquine
- hyoscyamine
- ipratropium inhaled
- lacosamide
- lamotrigine
- levetiracetam
- levocetirizine
- levomilnacipran
- linvoseltamab
- magnesium citrate
- meclizine
- melatonin
- meprobamate
- methazolamide
- methocarbamol
- methscopolamine
- methsuximide
- metyrapone
- metyrosine
- milnacipran
- mosunetuzumab
- mycophenolate mofetil
- naltrexone
- naratriptan
- orphenadrine
- oxcarbazepine
- passion flower
- perampanel
- pheniramine
- pimozide
- polyethylene glycol
- polyethylene glycol/electrolytes
- pyrilamine
- ramelteon
- revefenacin inhaled
- rivastigmine
- rizatriptan
- rufinamide
- selinexor
- sertraline
- sodium picosulfate
- sofpironium topical
- solifenacin
- stiripentol
- sulfate bowel prep
- sumatriptan
- tasimelteon
- tetrabenazine
- thiotepa
- tiagabine
- tiotropium inhaled
- tolterodine
- topiramate
- treosulfan
- trihexyphenidyl
- triprolidine
- trospium
- umeclidinium inhaled
- valbenazine
- valerian
- valproic acid
- venlafaxine
- vigabatrin
- vilazodone
- viloxazine
- zolmitriptan
- zonisamide
Adverse Reactions .
Serious Reactions
- neuroleptic malignant syndrome
- extrapyramidal symptoms, severe
- tardive dyskinesia
- dystonia
- stroke
- TIA
- syncope
- hypotension, orthostatic
- seizures
- hyperglycemia
- diabetes mellitus
- dysphagia, severe
- aspiration
- hyperthermia
- leukopenia
- neutropenia
- agranulocytosis
- suicidality
- depression exacerbation
Common Reactions
- weight gain
- hyperglycemia
- dyslipidemia
- akathisia
- extrapyramidal symptoms
- somnolence
- weight loss
- restlessness
- tremor
- nasopharyngitis
- nausea
- dizziness
- insomnia
- anxiety
- headache
- appetite incr.
- impaired body temperature regulation
- fatigue
- dyspepsia
- diarrhea
- constipation
- cortisol decr.
- CPK incr.
- sedation
- compulsive behaviors
- hyperprolactinemia
Safety/Monitoring .
Monitoring Parameters
fasting glucose, lipid profile at baseline, then periodically; CBC with diff frequently during initial tx if pre-existing or history of leukopenia/neutropenia; weight; BP, HR in patients with orthostatic hypotension risk; symptoms of suicidality, clinical worsening, and/or unusual behavior changes, especially during initial tx or after dose changes
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy, especially in 3rd trimester; no human data available, though risk of neonatal extrapyramidal and withdrawal symptoms based on human data with other antipsychotics; no known risk of fetal harm based on animal data at up to 73x and 146x MRHD
Pregnancy Registry
encourage patients 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: for brexpiprazole: liver; CYP450: 2D6, 3A4 substrate; Info: CYP2D6 poor metabolizers have 4.8 fold increased active drug exposure
Excretion: for brexpiprazole: feces 46% (14% unchanged), urine 25% (<1% unchanged); Half-life: 91h
Subclass: Antipsychotics, 2nd generation
Mechanism of Action
for brexpiprazole: exact mechanism of action unknown; partially agonizes dopamine D2 and serotonin 5-HT1A receptors, antagonizes serotonin 5-HT2A receptors
Formulary .
No Formulary Selected
Manufacturer/Pricing .
Manufacturer: Otsuka America Pharmaceuticals, Inc.
DEA/FDA: Rx
Retail Price
Estimated prices only. For current pricing, visit GoodRx.
oral tablet:
- 0.25 mg (30 ea): $1,281.00
- 0.5 mg (30 ea): $1,281.00
- 1 mg (30 ea): $1,281.00
- 2 mg (30 ea): $1,281.00
- 3 mg (30 ea): $1,281.00
- 4 mg (30 ea): $1,281.00
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