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Ingrezza Sprinkle
valbenazine
Black Box Warnings .
Depression and Suicidality
incr. risk of depression and suicidality in pts w/ Huntington dz, esp. if depression hx or prior suicide attempts or ideation; weigh risk vs. benefit; observe all pts for new or worsening depression, suicidality, or unusual behavior changes; inform pts and caregivers of depression and suicidality risk and instruct to report any concerning behaviors
Adult Dosing .
Dosage forms: CAP: 40 mg, 60 mg, 80 mg
Restricted Distribution in US
- [1-844-647-3992 or www.ingrezzahcp.com for more info]
tardive dyskinesia
- [80 mg PO qd]
- Start: 40 mg PO qd x1wk, then incr. to 80 mg PO qd; Info: may consider 40-60 mg PO qd based on response and tolerability; give 40 mg PO qd in CYP2D6 poor metabolizers; may open cap, but do not crush/chew contents; do not sprinkle contents in milk or water
chorea, Huntington dz-associated
- [80 mg PO qd]
- Start: 40 mg PO qd, then incr. by 20 mg/day q2wk; Info: may consider 40-60 mg PO qd based on response and tolerability; give 40 mg PO qd in CYP2D6 poor metabolizers; may open cap, but do not crush/chew contents; do not sprinkle contents in milk or water
renal dosing
- [see below]
- renal impairment: no adjustment
- HD/PD: not defined
hepatic dosing
- [adjust dose amount]
- Child-Pugh Class B or C: 40 mg qd
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- MAO inhibitor use w/in 14 days
- long QT syndrome, congenital
- arrhythmia hx
- avoid: breastfeeding during tx and x5 days after D/C
- caution: CYP2D6 poor metabolizers
- caution: depression hx
- caution: suicidality hx
- caution: neuroleptic malignant syndrome hx
- caution: hepatic impairment, Child-Pugh Class B-C
- caution: electrolyte abnormalities
- caution: QT prolongation
- caution: QT prolongation family hx
- caution: bradycardia
- caution: MI, recent
- caution: CHF
Drug Interactions .
Overview
valbenazine
VMAT2 inhibitor
- CYP2D6 substrate
- CYP3A4 substrate
- P-gp inhibitor, weak
- CNS depression
- increases synaptic monoamines
- prolongs QT interval (conditional)
- add MAO inhibitor to Interaction Check if recent (14 days) use
Contraindicated
- colchicine
- deutetrabenazine
- pimozide
- quinidine (CYP2D6 inhibitor)
- tetrabenazine
- thioridazine
Avoid/Use Alternative
- apalutamide
- apixaban
- arsenic trioxide
- bedaquiline
- bosentan
- butalbital
- carbamazepine
- cenobamate
- ceritinib
- cisapride
- clonidine
- codeine
- crizotinib
- dabigatran
- dabrafenib
- domperidone
- doxylamine
- dronedarone
- efavirenz
- encorafenib
- ensartinib
- enzalutamide
- ephedra
- ethanol
- etravirine
- fexinidazole
- fosphenytoin
- futibatinib
- hydrocodone
- hydroxychloroquine
- isocarboxazid
- isoniazid
- ivosidenib
- kava
- kratom
- lefamulin
- linezolid
- lonafarnib
- lopinavir/ritonavir
- lorlatinib
- lumacaftor/ivacaftor
- mavacamten
- metaxalone
- methylene blue injection
- methylene blue oral
- metoclopramide
- midazolam
- mitapivat
- mitotane
- mobocertinib
- modafinil
- nafcillin
- neratinib
- oxybate
- pacritinib
- pentobarbital
- pexidartinib
- phenelzine
- phenobarbital
- phenytoin
- pralsetinib
- primidone
- procarbazine
- promethazine
- quizartinib
- rasagiline
- relugolix
- repotrectinib
- rifabutin
- rifampin
- rifapentine
- rivaroxaban
- safinamide
- selegiline
- selegiline transdermal
- sirolimus albumin-bound
- sotalol
- sotorasib
- St. John's wort
- thalidomide
- topotecan
- toremifene
- tranylcypromine
- trimethobenzamide
- vandetanib
- venetoclax
- yohimbe
- ziprasidone
- zuranolone
Monitor/Modify Tx
- adagrasib
- afatinib
- aldesleukin
- alfentanil
- alprazolam
- amiodarone
- anagrelide
- apomorphine
- artemether/lumefantrine
- asenapine
- atazanavir
- atorvastatin
- azithromycin
- baclofen intrathecal
- buprenorphine
- bupropion
- butorphanol
- cabozantinib
- chloramphenicol
- chlordiazepoxide
- chloroquine
- chlorpromazine
- citalopram
- clarithromycin
- clobazam
- clofazimine
- clonazepam
- clorazepate
- cobicistat
- cyclosporine
- dacomitinib
- daridorexant
- degarelix
- desflurane
- desipramine
- dexmedetomidine
- dexmedetomidine injection
- diazepam
- digoxin
- dihydrocodeine
- disopyramide
- dofetilide
- donepezil
- droperidol
- edoxaban
- enfortumab vedotin
- epirubicin
- eribulin
- erythromycin
- esketamine
- estazolam
- eszopiclone
- ethanol (in some formulations)
- etomidate
- everolimus
- fentanyl
- flecainide
- fluorouracil
- fluoxetine
- fluphenazine
- flurazepam
- gabapentin
- gabapentin enacarbil
- gilteritinib
- glasdegib
- goserelin
- haloperidol
- histrelin
- hydromorphone
- hydroxyzine
- ibutilide
- idelalisib
- ifosfamide
- inotuzumab ozogamicin
- isoflurane
- itraconazole
- ketamine
- ketoconazole
- landiolol
- lemborexant
- leuprolide
- levofloxacin
- levoketoconazole
- levorphanol
- lofexidine
- lorazepam
- macimorelin
- mavorixafor
- meperidine
- methadone
- methohexital
- mifepristone
- mirtazapine
- morphine
- moxifloxacin
- nalbuphine
- nefazodone
- nelarabine
- nelfinavir
- nilotinib
- olanzapine
- oliceridine
- ondansetron
- opicapone
- opium
- osimertinib
- oxazepam
- oxybutynin
- oxycodone
- oxymorphone
- paliperidone
- palonosetron
- panobinostat
- paroxetine
- pasireotide
- pentamidine
- pentazocine
- perphenazine
- posaconazole
- pregabalin
- procainamide
- propafenone
- propofol
- quazepam
- quinidine (antiarrhythmic)
- quinine
- ranolazine
- remifentanil
- remimazolam
- revumenib
- ribociclib
- ritonavir
- romidepsin
- rucaparib
- selpercatinib
- sevoflurane
- sirolimus
- sufentanil
- suvorexant
- tacrolimus
- talazoparib
- tapentadol
- telavancin
- temazepam
- tenofovir alafenamide
- tenofovir disoproxil
- terbinafine
- thiothixene
- tipranavir
- tramadol
- triazolam
- triclabendazole
- trifluridine
- triptorelin
- tucatinib
- ubrogepant
- vemurafenib
- voriconazole
- zaleplon
- ziconotide
- zolpidem
Caution Advised
- 5-HTP
- allopurinol
- almotriptan
- amantadine
- amitriptyline
- amoxapine
- apraclonidine ophthalmic
- aripiprazole bimonthly injection
- aripiprazole lauroxil
- aripiprazole monthly injection
- aripiprazole oral
- baclofen
- brexpiprazole
- brimonidine ophthalmic
- brimonidine topical
- brivaracetam
- bromocriptine
- brompheniramine
- buspirone
- cannabidiol
- cannabis
- carbinoxamine
- cariprazine
- carisoprodol
- cetirizine
- chamomile, German
- chlophedianol
- chlorpheniramine
- chlorzoxazone
- clemastine
- clomipramine
- clozapine
- cyclobenzaprine
- cyproheptadine
- dantrolene
- darifenacin
- darolutamide
- desvenlafaxine
- dexbrompheniramine
- dexchlorpheniramine
- dichlorphenamide
- difelikefalin
- difenoxin
- dimenhydrinate
- diphenhydramine
- diphenoxylate
- doxepin
- doxepin topical
- dronabinol
- duloxetine
- eletriptan
- entacapone
- entrectinib
- escitalopram
- eslicarbazepine acetate
- ethosuximide
- felbamate
- fenfluramine
- fesoterodine
- flibanserin
- fluvoxamine
- foslevodopa
- frovatriptan
- ganaxolone
- glecaprevir
- glofitamab
- glycopyrrolate
- guanfacine
- hyoscyamine
- iloperidone
- imipramine
- lacosamide
- lamotrigine
- lasmiditan
- levetiracetam
- levocetirizine
- levodopa
- levomilnacipran
- loxapine
- lumateperone
- lurasidone
- meclizine
- melatonin
- meprobamate
- methocarbamol
- methsuximide
- methyldopa
- metyrapone
- metyrosine
- milnacipran
- molindone
- mosunetuzumab
- mycophenolate mofetil
- naldemedine
- naltrexone
- naratriptan
- nortriptyline
- oxcarbazepine
- passion flower
- perampanel
- pheniramine
- pibrentasvir
- pramipexole
- prochlorperazine
- protriptyline
- pyrilamine
- quetiapine
- ramelteon
- risperidone
- rizatriptan
- ropeginterferon alfa-2b
- ropinirole
- rotigotine transdermal
- rufinamide
- scopolamine
- selinexor
- sertraline
- solifenacin
- stiripentol
- sumatriptan
- tasimelteon
- thiotepa
- tiagabine
- tizanidine
- tolcapone
- tolterodine
- topiramate
- trazodone
- trifluoperazine
- trihexyphenidyl
- trimipramine
- triprolidine
- trospium
- valerian
- valproic acid
- venlafaxine
- vigabatrin
- vilazodone
- viloxazine
- zolmitriptan
- zonisamide
Adverse Reactions .
Serious Reactions
- suicidality
- depression
- QT prolongation
- hypersensitivity rxn
- angioedema
- neuroleptic malignant syndrome
- parkinsonism
Common Reactions
- somnolence
- fatigue
- urticaria
- rash
- akathisia
- insomnia
- anticholinergic effects
- parkinsonism
- diarrhea
- nausea
- depression (pts w/ Huntington dz)
- back pain
- balance disorder
- headache
- vomiting
- arthralgia
Safety/Monitoring .
Monitoring Parameters
ECG before dose incr. if QT prolongation risk; s/sx depression, behavior changes, suicidality
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; inadequate human data available; no known risk of teratogenicity, though risk of decr. fetal wt and delayed ossification based on animal data at 24x MRHD
Lactation
Clinical Summary
avoid breastfeeding during tx and x5 days after D/C; no human data available to assess risk of infant harm, though possible drug excretion into milk based on drug properties; no human data available to assess effects on milk production
Pharmacology .
Metabolism: hydrolysis, oxidation; CYP450: 2D6, 3A4/5 (primary) substrate; Info: active metabolites
Excretion: urine 60% (<2% unchanged), feces 30% (<2% unchanged); Half-life: 15-22h
Subclass: VMAT2 Inhibitors
Mechanism of Action
exact mechanism of action unknown; selectively and reversibly inhibits human vesicular monoamine transporter type 2 (VMAT2), decreasing monoamine uptake into synaptic vesicles and depleting monoamine stores
Formulary .
No Formulary Selected
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