Dosing & Uses
Dosage Forms & Strengths
capsule
- 40mg
- 80mg
Tardive Dyskinesia
Indicated for treatment of adults with tardive dyskinesia
40 mg PO qDay x1 week, then increase to the recommended dose of 80 mg PO qDay
40-60 mg qDay may be considered depending on response and tolerability
Dosage Modifications
Strong CYP3A4 inducers: Coadministration not recommended
Strong CYP3A4 inhibitors: If coadministered, reduce valbenazine dose to 40 mg/day
Strong CYP2D6 inhibitors or known CYP2D6 poor metabolizers: If coadministered, reduce valbenazine dose to 40 mg/day
Hepatic impairment
- Mild: No dose adjustment required
- Moderate-to-severe (Child-Pugh 7-15): Not to exceed 40 mg/day
Renal impairment
- Mild-to-severe: No dose adjustment required
Chorea (Orphan)
Orphan designation for treatment of chorea associated with Huntington disease
Orphan sponsor
- Neurocrine Biosciences; Inc; 12780 El Camino Real; San Diego, California 92130
Tardive dyskinesia: Safety and efficacy not established
Tourette Syndrome (Orphan)
Orphan designation for treatment of Tourette syndrome
Sponsor
- Neurocrine Biosciences, Inc; 12780 El Camino Real; San Diego, California 92130
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (2)
- deutetrabenazine
deutetrabenazine, valbenazine. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Do not use these drugs concomitantly.
- tetrabenazine
tetrabenazine, valbenazine. Either increases effects of the other by pharmacodynamic synergism. Contraindicated. Do not use these drugs concomitantly.
Serious - Use Alternative (43)
- abametapir
abametapir will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.
- apalutamide
apalutamide will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.
- butalbital
butalbital will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- carbamazepine
carbamazepine will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- ceritinib
ceritinib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- cobicistat
cobicistat will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- dabrafenib
dabrafenib will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- dacomitinib
dacomitinib will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug. Avoid use with CYP2D6 substrates where minimal increases in concentration of the CYP2D6 substrate may lead to serious or life-threatening toxicities.
- dexamethasone
dexamethasone will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- enzalutamide
enzalutamide will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- eslicarbazepine acetate
eslicarbazepine acetate will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- fexinidazole
fexinidazole will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.
- fosphenytoin
fosphenytoin will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- givosiran
givosiran will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP2D6 substrates with givosiran. If unavoidable, decrease the CYP2D6 substrate dosage in accordance with approved product labeling.
- iobenguane I 131
valbenazine will decrease the level or effect of iobenguane I 131 by Other (see comment). Avoid or Use Alternate Drug. Based on the mechanism of action of iobenguane, drugs that reduce catecholamine uptake or that deplete catecholamine stores may interfere with iobenguane uptake into cells, and thus, reduce iobenguane efficacy. Discontinue interfering drugs for at least 5 half-lives before administration of either the dosimetry or an iobenguane dose. Do not administer these drugs until at least 7 days after each iobenguane dose.
- isocarboxazid
isocarboxazid, valbenazine. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of valbenazine with MAOIs may increase monoamine neurotransmitter concentration in synapses, potentially increasing risk of serotonin syndrome or attenuating valbenazine effect.
- ivosidenib
ivosidenib will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of sensitive CYP3A4 substrates with ivosidenib or replace with alternative therapies. If coadministration is unavoidable, monitor patients for loss of therapeutic effect of these drugs.
- linezolid
linezolid, valbenazine. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of valbenazine with MAOIs may increase monoamine neurotransmitter concentration in synapses, potentially increasing risk of serotonin syndrome or attenuating valbenazine effect.
- lonafarnib
lonafarnib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.
- lumacaftor/ivacaftor
lumacaftor/ivacaftor will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- methylene blue
methylene blue, valbenazine. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of valbenazine with MAOIs may increase monoamine neurotransmitter concentration in synapses, potentially increasing risk of serotonin syndrome or attenuating valbenazine effect.
- mifepristone
mifepristone will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- mitotane
mitotane will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- nevirapine
nevirapine will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- oxcarbazepine
oxcarbazepine will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- pentobarbital
pentobarbital will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- phenelzine
phenelzine, valbenazine. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of valbenazine with MAOIs may increase monoamine neurotransmitter concentration in synapses, potentially increasing risk of serotonin syndrome or attenuating valbenazine effect.
- phenobarbital
phenobarbital will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- phenytoin
phenytoin will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- primidone
primidone will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- rasagiline
rasagiline, valbenazine. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of valbenazine with MAOIs may increase monoamine neurotransmitter concentration in synapses, potentially increasing risk of serotonin syndrome or attenuating valbenazine effect.
- ribociclib
ribociclib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- rifabutin
rifabutin will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- rifampin
rifampin will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- rifapentine
rifapentine will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- safinamide
safinamide, valbenazine. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of valbenazine with MAOIs may increase monoamine neurotransmitter concentration in synapses, potentially increasing risk of serotonin syndrome or attenuating valbenazine effect.
- secobarbital
secobarbital will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- selegiline
selegiline, valbenazine. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of valbenazine with MAOIs may increase monoamine neurotransmitter concentration in synapses, potentially increasing risk of serotonin syndrome or attenuating valbenazine effect.
- selegiline transdermal
selegiline transdermal, valbenazine. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of valbenazine with MAOIs may increase monoamine neurotransmitter concentration in synapses, potentially increasing risk of serotonin syndrome or attenuating valbenazine effect.
- St John's Wort
St John's Wort will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Concomitant use not recommended.
- tranylcypromine
tranylcypromine, valbenazine. Other (see comment). Avoid or Use Alternate Drug. Comment: Coadministration of valbenazine with MAOIs may increase monoamine neurotransmitter concentration in synapses, potentially increasing risk of serotonin syndrome or attenuating valbenazine effect.
- tucatinib
tucatinib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.
- voxelotor
voxelotor will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.
Monitor Closely (194)
- albuterol
valbenazine and albuterol both increase QTc interval. Use Caution/Monitor.
- alfuzosin
valbenazine and alfuzosin both increase QTc interval. Use Caution/Monitor.
- amiodarone
valbenazine and amiodarone both increase QTc interval. Use Caution/Monitor.
- amisulpride
valbenazine and amisulpride both increase QTc interval. Use Caution/Monitor.
- amitriptyline
valbenazine and amitriptyline both increase QTc interval. Use Caution/Monitor.
- amobarbital
amobarbital will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely.
- amoxapine
valbenazine and amoxapine both increase QTc interval. Use Caution/Monitor.
- anagrelide
valbenazine and anagrelide both increase QTc interval. Use Caution/Monitor.
- apomorphine
valbenazine and apomorphine both increase QTc interval. Use Caution/Monitor.
- arformoterol
valbenazine and arformoterol both increase QTc interval. Use Caution/Monitor.
- aripiprazole
valbenazine and aripiprazole both increase QTc interval. Use Caution/Monitor.
- arsenic trioxide
valbenazine and arsenic trioxide both increase QTc interval. Use Caution/Monitor.
- artemether
valbenazine and artemether both increase QTc interval. Use Caution/Monitor.
- artemether/lumefantrine
valbenazine and artemether/lumefantrine both increase QTc interval. Use Caution/Monitor.
- asenapine
valbenazine and asenapine both increase QTc interval. Use Caution/Monitor.
- atazanavir
atazanavir will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg daily when coadministered with strong CYP3A4 inhibitors.
- atomoxetine
valbenazine and atomoxetine both increase QTc interval. Use Caution/Monitor.
- azithromycin
valbenazine and azithromycin both increase QTc interval. Use Caution/Monitor.
- bedaquiline
valbenazine and bedaquiline both increase QTc interval. Use Caution/Monitor.
- bosentan
bosentan will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- buprenorphine
valbenazine and buprenorphine both increase QTc interval. Use Caution/Monitor.
- bupropion
bupropion will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
- ceritinib
valbenazine and ceritinib both increase QTc interval. Use Caution/Monitor.
- chloramphenicol
chloramphenicol will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose when coadministered with a strong CYP3A4 inhibitor.
- chloroquine
valbenazine and chloroquine both increase QTc interval. Use Caution/Monitor.
- chlorpromazine
chlorpromazine will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
valbenazine and chlorpromazine both increase QTc interval. Use Caution/Monitor. - cinacalcet
cinacalcet will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
- ciprofloxacin
valbenazine and ciprofloxacin both increase QTc interval. Use Caution/Monitor.
- cisapride
valbenazine and cisapride both increase QTc interval. Use Caution/Monitor.
- citalopram
valbenazine and citalopram both increase QTc interval. Use Caution/Monitor.
- clarithromycin
clarithromycin will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
valbenazine and clarithromycin both increase QTc interval. Use Caution/Monitor. - clomipramine
valbenazine and clomipramine both increase QTc interval. Use Caution/Monitor.
- clozapine
valbenazine and clozapine both increase QTc interval. Use Caution/Monitor.
- cobicistat
cobicistat will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2E1 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- cocaine topical
cocaine topical will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
- conivaptan
conivaptan will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- crizotinib
valbenazine and crizotinib both increase QTc interval. Use Caution/Monitor.
- darunavir
darunavir will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- dasatinib
valbenazine and dasatinib both increase QTc interval. Use Caution/Monitor.
- degarelix
valbenazine and degarelix both increase QTc interval. Use Caution/Monitor.
- desflurane
valbenazine and desflurane both increase QTc interval. Use Caution/Monitor.
- desipramine
valbenazine and desipramine both increase QTc interval. Use Caution/Monitor.
- deutetrabenazine
valbenazine and deutetrabenazine both increase QTc interval. Use Caution/Monitor.
- dexmedetomidine
dexmedetomidine will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
- disopyramide
valbenazine and disopyramide both increase QTc interval. Use Caution/Monitor.
- dofetilide
valbenazine and dofetilide both increase QTc interval. Use Caution/Monitor.
- dolasetron
valbenazine and dolasetron both increase QTc interval. Use Caution/Monitor.
- donepezil
valbenazine and donepezil both increase QTc interval. Use Caution/Monitor.
- doxepin
valbenazine and doxepin both increase QTc interval. Use Caution/Monitor.
- dronedarone
valbenazine and dronedarone both increase QTc interval. Use Caution/Monitor.
- droperidol
valbenazine and droperidol both increase QTc interval. Use Caution/Monitor.
- duvelisib
duvelisib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Coadministration with duvelisib increases AUC of a sensitive CYP3A4 substrate which may increase the risk of toxicities of these drugs. Consider reducing the dose of the sensitive CYP3A4 substrate and monitor for signs of toxicities of the coadministered sensitive CYP3A substrate.
- efavirenz
valbenazine and efavirenz both increase QTc interval. Use Caution/Monitor.
- elagolix
elagolix decreases levels of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.
- eliglustat
valbenazine and eliglustat both increase QTc interval. Use Caution/Monitor.
- elvitegravir/cobicistat/emtricitabine/tenofovir DF
elvitegravir/cobicistat/emtricitabine/tenofovir DF will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- encorafenib
encorafenib, valbenazine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Encorafenib both inhibits and induces CYP3A4 at clinically relevant plasma concentrations. Coadministration of encorafenib with sensitive CYP3A4 substrates may result in increased toxicity or decreased efficacy of these agents.
valbenazine and encorafenib both increase QTc interval. Use Caution/Monitor. - entrectinib
valbenazine and entrectinib both increase QTc interval. Use Caution/Monitor.
- eribulin
valbenazine and eribulin both increase QTc interval. Use Caution/Monitor.
- erythromycin base
valbenazine and erythromycin base both increase QTc interval. Use Caution/Monitor.
- erythromycin ethylsuccinate
valbenazine and erythromycin ethylsuccinate both increase QTc interval. Use Caution/Monitor.
- erythromycin lactobionate
valbenazine and erythromycin lactobionate both increase QTc interval. Use Caution/Monitor.
- erythromycin stearate
valbenazine and erythromycin stearate both increase QTc interval. Use Caution/Monitor.
- escitalopram
valbenazine and escitalopram both increase QTc interval. Use Caution/Monitor.
- etravirine
etravirine will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- fedratinib
fedratinib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.
fedratinib will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP2D6 substrates as necessary. - fexinidazole
valbenazine and fexinidazole both increase QTc interval. Use Caution/Monitor.
- fingolimod
valbenazine and fingolimod both increase QTc interval. Use Caution/Monitor.
- flecainide
valbenazine and flecainide both increase QTc interval. Use Caution/Monitor.
- fluconazole
valbenazine and fluconazole both increase QTc interval. Use Caution/Monitor.
- fluoxetine
fluoxetine will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
valbenazine and fluoxetine both increase QTc interval. Use Caution/Monitor. - fluphenazine
valbenazine and fluphenazine both increase QTc interval. Use Caution/Monitor.
- fluvoxamine
valbenazine and fluvoxamine both increase QTc interval. Use Caution/Monitor.
- fosamprenavir
fosamprenavir will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- foscarnet
valbenazine and foscarnet both increase QTc interval. Use Caution/Monitor.
- fostemsavir
valbenazine and fostemsavir both increase QTc interval. Use Caution/Monitor.
- ganaxolone
valbenazine and ganaxolone both increase sedation. Use Caution/Monitor.
- gemifloxacin
valbenazine and gemifloxacin both increase QTc interval. Use Caution/Monitor.
- gemtuzumab
valbenazine and gemtuzumab both increase QTc interval. Use Caution/Monitor.
- gilteritinib
valbenazine and gilteritinib both increase QTc interval. Use Caution/Monitor.
- glasdegib
valbenazine and glasdegib both increase QTc interval. Use Caution/Monitor.
- goserelin
valbenazine and goserelin both increase QTc interval. Use Caution/Monitor.
- granisetron
valbenazine and granisetron both increase QTc interval. Use Caution/Monitor.
- grapefruit
grapefruit will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- haloperidol
valbenazine and haloperidol both increase QTc interval. Use Caution/Monitor.
- histrelin
valbenazine and histrelin both increase QTc interval. Use Caution/Monitor.
- hydroxychloroquine sulfate
valbenazine and hydroxychloroquine sulfate both increase QTc interval. Use Caution/Monitor.
- hydroxyzine
valbenazine and hydroxyzine both increase QTc interval. Use Caution/Monitor.
- ibutilide
valbenazine and ibutilide both increase QTc interval. Use Caution/Monitor.
- idelalisib
idelalisib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- iloperidone
valbenazine and iloperidone both increase QTc interval. Use Caution/Monitor.
- imatinib
imatinib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- imipramine
valbenazine and imipramine both increase QTc interval. Use Caution/Monitor.
- indacaterol, inhaled
valbenazine and indacaterol, inhaled both increase QTc interval. Use Caution/Monitor.
- indinavir
indinavir will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- inotuzumab
valbenazine and inotuzumab both increase QTc interval. Use Caution/Monitor.
- isoflurane
valbenazine and isoflurane both increase QTc interval. Use Caution/Monitor.
- isoniazid
isoniazid will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- istradefylline
istradefylline will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.
- itraconazole
itraconazole will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
valbenazine and itraconazole both increase QTc interval. Use Caution/Monitor. - ivosidenib
valbenazine and ivosidenib both decrease QTc interval. Use Caution/Monitor.
- ketoconazole
ketoconazole will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- lapatinib
valbenazine and lapatinib both increase QTc interval. Use Caution/Monitor.
- lefamulin
valbenazine and lefamulin both increase QTc interval. Use Caution/Monitor.
- lenvatinib
valbenazine and lenvatinib both increase QTc interval. Use Caution/Monitor.
- leuprolide
valbenazine and leuprolide both increase QTc interval. Use Caution/Monitor.
- levalbuterol
valbenazine and levalbuterol both increase QTc interval. Use Caution/Monitor.
- levofloxacin
valbenazine and levofloxacin both increase QTc interval. Use Caution/Monitor.
- levoketoconazole
levoketoconazole will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- lithium
valbenazine and lithium both increase QTc interval. Use Caution/Monitor.
- lofexidine
valbenazine and lofexidine both increase QTc interval. Use Caution/Monitor. ECG monitoring is recommended.
- loperamide
valbenazine and loperamide both increase QTc interval. Use Caution/Monitor.
- lopinavir
lopinavir will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
lopinavir will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
valbenazine and lopinavir both increase QTc interval. Use Caution/Monitor. - lorcaserin
lorcaserin will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
- lorlatinib
lorlatinib will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- macimorelin
valbenazine and macimorelin both increase QTc interval. Use Caution/Monitor.
- maprotiline
valbenazine and maprotiline both increase QTc interval. Use Caution/Monitor.
- mefloquine
valbenazine and mefloquine both increase QTc interval. Use Caution/Monitor.
- methadone
valbenazine and methadone both increase QTc interval. Use Caution/Monitor.
- midostaurin
valbenazine and midostaurin both increase QTc interval. Use Caution/Monitor.
- mifepristone
valbenazine and mifepristone both increase QTc interval. Use Caution/Monitor.
- mirtazapine
valbenazine and mirtazapine both increase QTc interval. Use Caution/Monitor.
- mobocertinib
valbenazine and mobocertinib both increase QTc interval. Use Caution/Monitor.
- moxifloxacin
valbenazine and moxifloxacin both increase QTc interval. Use Caution/Monitor.
- nafcillin
nafcillin will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- nefazodone
nefazodone will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- nelfinavir
nelfinavir will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- nicardipine
nicardipine will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- nilotinib
valbenazine and nilotinib both increase QTc interval. Use Caution/Monitor.
- nortriptyline
valbenazine and nortriptyline both increase QTc interval. Use Caution/Monitor.
- octreotide
valbenazine and octreotide both increase QTc interval. Use Caution/Monitor.
- ofloxacin
valbenazine and ofloxacin both increase QTc interval. Use Caution/Monitor.
- olanzapine
valbenazine and olanzapine both increase QTc interval. Use Caution/Monitor.
- olodaterol inhaled
valbenazine and olodaterol inhaled both increase QTc interval. Use Caution/Monitor.
- ondansetron
valbenazine and ondansetron both increase QTc interval. Use Caution/Monitor.
- osilodrostat
valbenazine and osilodrostat both increase QTc interval. Use Caution/Monitor.
- osimertinib
valbenazine and osimertinib both increase QTc interval. Use Caution/Monitor.
- oxaliplatin
valbenazine and oxaliplatin both increase QTc interval. Use Caution/Monitor.
- ozanimod
valbenazine and ozanimod both increase QTc interval. Use Caution/Monitor.
- paliperidone
valbenazine and paliperidone both increase QTc interval. Use Caution/Monitor.
- panobinostat
valbenazine and panobinostat both increase QTc interval. Use Caution/Monitor.
- paroxetine
paroxetine will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
valbenazine and paroxetine both increase QTc interval. Use Caution/Monitor. - pasireotide
valbenazine and pasireotide both increase QTc interval. Use Caution/Monitor.
- pazopanib
valbenazine and pazopanib both increase QTc interval. Use Caution/Monitor.
- pentamidine
valbenazine and pentamidine both increase QTc interval. Use Caution/Monitor.
- perphenazine
valbenazine and perphenazine both increase QTc interval. Use Caution/Monitor.
- pimavanserin
valbenazine and pimavanserin both increase QTc interval. Use Caution/Monitor.
- pimozide
valbenazine and pimozide both increase QTc interval. Use Caution/Monitor.
- pitolisant
valbenazine and pitolisant both increase QTc interval. Use Caution/Monitor.
- ponesimod
valbenazine and ponesimod both increase QTc interval. Use Caution/Monitor.
- posaconazole
posaconazole will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
valbenazine and posaconazole both increase QTc interval. Use Caution/Monitor. - primaquine
valbenazine and primaquine both increase QTc interval. Use Caution/Monitor.
- procainamide
valbenazine and procainamide both increase QTc interval. Use Caution/Monitor.
- prochlorperazine
valbenazine and prochlorperazine both decrease QTc interval. Use Caution/Monitor.
- promethazine
valbenazine and promethazine both decrease QTc interval. Use Caution/Monitor.
- propafenone
valbenazine and propafenone both increase QTc interval. Use Caution/Monitor.
- protriptyline
valbenazine and protriptyline both increase QTc interval. Use Caution/Monitor.
- quinidine
quinidine will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
- ranolazine
valbenazine and ranolazine both increase QTc interval. Use Caution/Monitor.
- remimazolam
remimazolam, valbenazine. Either increases toxicity of the other by sedation. Modify Therapy/Monitor Closely. Coadministration may result in profound sedation, respiratory depression, coma, and/or death. Continuously monitor vital signs during sedation and recovery period if coadministered. Carefully titrate remimazolam dose if administered with opioid analgesics and/or sedative/hypnotics.
- rilpivirine
valbenazine and rilpivirine both increase QTc interval. Use Caution/Monitor.
- risperidone
valbenazine and risperidone both increase QTc interval. Use Caution/Monitor.
- ritonavir
ritonavir will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Consider reducing valbenazine dose based on tolerability if coadministered with a strong CYP2D6 inhibitor.
ritonavir will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor. - rolapitant
rolapitant will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Use Caution/Monitor. Rolapitant may increase plasma concentrations of CYP2D6 substrates for at least 28 days following rolapitant administration.
- romidepsin
valbenazine and romidepsin both increase QTc interval. Use Caution/Monitor.
- rucaparib
rucaparib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.
- salmeterol
valbenazine and salmeterol both increase QTc interval. Use Caution/Monitor.
- saquinavir
saquinavir will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
valbenazine and saquinavir both increase QTc interval. Use Caution/Monitor. - selpercatinib
valbenazine and selpercatinib both increase QTc interval. Use Caution/Monitor.
- sertraline
valbenazine and sertraline both increase QTc interval. Use Caution/Monitor.
- sevoflurane
valbenazine and sevoflurane both increase QTc interval. Use Caution/Monitor.
- siponimod
valbenazine and siponimod both increase QTc interval. Use Caution/Monitor.
- solifenacin
valbenazine and solifenacin both increase QTc interval. Use Caution/Monitor.
- sorafenib
valbenazine and sorafenib both increase QTc interval. Use Caution/Monitor.
- stiripentol
stiripentol, valbenazine. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Stiripentol is a CYP3A4 inhibitor and inducer. Monitor CYP3A4 substrates coadministered with stiripentol for increased or decreased effects. CYP3A4 substrates may require dosage adjustment.
- sunitinib
valbenazine and sunitinib both increase QTc interval. Use Caution/Monitor.
- tacrolimus
valbenazine and tacrolimus both increase QTc interval. Use Caution/Monitor.
- tazemetostat
tazemetostat will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tecovirimat
tecovirimat will decrease the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Tecovirimat is a weak CYP3A4 inducer. Monitor sensitive CYP3A4 substrates for effectiveness if coadministered.
- telavancin
valbenazine and telavancin both increase QTc interval. Use Caution/Monitor.
- terbinafine
terbinafine will increase the level or effect of valbenazine by affecting hepatic enzyme CYP2D6 metabolism. Modify Therapy/Monitor Closely. Assess need to reduce dose of CYP2D6-metabolized drug.
- tipranavir
tipranavir will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
- trazodone
valbenazine and trazodone both increase QTc interval. Use Caution/Monitor.
- trifluoperazine
valbenazine and trifluoperazine both decrease QTc interval. Use Caution/Monitor.
- trimipramine
valbenazine and trimipramine both increase QTc interval. Use Caution/Monitor.
- triptorelin
valbenazine and triptorelin both increase QTc interval. Use Caution/Monitor.
- umeclidinium bromide/vilanterol inhaled
valbenazine and umeclidinium bromide/vilanterol inhaled both decrease QTc interval. Use Caution/Monitor.
- vandetanib
valbenazine and vandetanib both increase QTc interval. Use Caution/Monitor.
- vardenafil
valbenazine and vardenafil both increase QTc interval. Use Caution/Monitor.
- vemurafenib
valbenazine and vemurafenib both increase QTc interval. Use Caution/Monitor.
- venlafaxine
valbenazine and venlafaxine both decrease QTc interval. Use Caution/Monitor.
- vilanterol/fluticasone furoate inhaled
valbenazine and vilanterol/fluticasone furoate inhaled both increase QTc interval. Use Caution/Monitor.
- voriconazole
voriconazole will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Reduce valbenazine dose to 40 mg once daily when coadministered with a strong CYP3A4 inhibitor.
valbenazine and voriconazole both increase QTc interval. Use Caution/Monitor. - vorinostat
valbenazine and vorinostat both increase QTc interval. Use Caution/Monitor.
Minor (4)
- acetazolamide
acetazolamide will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- anastrozole
anastrozole will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- cyclophosphamide
cyclophosphamide will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
- larotrectinib
larotrectinib will increase the level or effect of valbenazine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.
Adverse Effects
>10%
Somnolence (10.9%)
1-10%
Anticholinergic effects (5.4%)
Balance disorders/fall (4.1%)
Headache (3.4%)
Akathisia (2.7%)
Vomiting (2.6%)
Nausea (2.3%)
Arthralgia (2.3%)
Postmarketing Reports
Hypersensitivity
QT prolongation
Skin and subcutaneous tissue disorders: rash
Warnings
Contraindications
History of hypersensitivity to drug or components; rash urticaria, and reactions consistent with angioedema (eg, swelling of face, lips, mouth) reported
Cautions
Can cause somnolence; warn patients not to perform activities requiring mental alertness (eg, driving or operating hazardous machinery) until they know how they will be affected
Increased exposure (Cmax and AUC) to active metabolite is anticipated in CYP2D6 poor metabolizers; increased exposure of active metabolite may increase risk of exposure-related adverse reactions; dose reduction recommended
Parkinsonism
- May cause parkinsonism in patients with tardive dyskinesia
- Also reported with other VMAT2 inhibitors
- Postmarketing safety reports have described parkinson-like symptoms that required hospitalization
- In most cases, severe parkinsonism occurred within first two weeks of initiating or increasing dose of drug
- Associated symptoms have included falls, gait disturbances, tremor, drooling and hypokinesia
- In cases in which follow-up clinical information was available, parkinson-like symptoms were reported to resolve following discontinuation of therapy
- Reduce dose or discontinue treatment in patients who develop clinically significant parkinson-like signs or symptoms
QT prolongation
- May prolong the QT interval, although the degree of QT prolongation is not clinically significant at concentrations expected with recommended dosing
- If coadministered with a strong CYP2D6 or CYP3A4 inhibitor, or patients who are CYP2D6 poor metabolizers, valbenazine concentrations may increase and cause clinically significant QT prolongation (see Dosage Modifications)
- Avoid in patients with congenital long QT syndrome or with arrhythmias associated with a prolonged QT interval
- For patients at increased risk of a prolonged QT interval, assess the QT interval before increasing the dosage
Drug interaction overview
-
MAOIs
- Avoid coadministration
- Concomitant use may increase concentration of monoamine neurotransmitters in synapses, potentially leading to increased risk of adverse reactions (eg, serotonin syndrome) or attenuated treatment effect of valbenazine
-
Strong CYP3A4 inhibitors
- Reduce valbenazine dose (see Dosage Modifications)
- Coadministration increases exposure (Cmax and AUC) to valbenazine and its active metabolite compared with the use of valbenazine alone
-
Strong CYP2D6 inhibitors
- Reduce valbenazine dose (see Dosage Modifications)
- Coadministration increases exposure (Cmax and AUC) to valbenazine’s active metabolite compared with the use of valbenazine alone
-
Strong CYP3A4 inducers
- Concomitant use not recommended
- Coadministration decreases systemic exposure of valbenazine and its active metabolite, thereby decreasing efficacy
-
Digoxin
- Coadministration increases digoxin levels owing to P-gp inhibition
- Monitor digoxin levels if coadministered; dosage adjustment of digoxin may be necessary
Pregnancy
Pregnancy
Data are limited on use in pregnant women
Based on animal studies, may cause fetal harm; advise pregnant women of the potential risk
Animal studies
- Administration to pregnant rats during organogenesis through lactation produced an increase in the number of stillborn pups and postnatal pup mortalities at doses <1 times the maximum recommended human dose (MRHD) of 80 mg/day based on mg/m² body surface area
- However, no malformations were observed when administered orally to rats and rabbits during the period of organogenesis at doses up to 1.8 or 24 times, respectively, the MRHD
Lactation
Unknown if distributed in human breast milk
Valbenazine and its metabolites have been detected in rat milk at concentrations higher than in plasma following oral administration at doses 0.1-1.2 times the MRHD based on mg/m²
Based on animal findings of increased perinatal mortality in exposed fetuses and pups, advise a woman not to breastfeed during treatment and for 5 days after the final dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
The mechanism of action of valbenazine in the treatment of tardive dyskinesia is unknown, but is thought to be mediated through the reversible inhibition of vesicular monoamine transporter 2 (VMAT2), a transporter that regulates monoamine uptake from the cytoplasm to the synaptic vesicle for storage and release
Absorption
Bioavailability: ~49%
Peak plasma time: 0.5-1 hr (parent); 4-8 hr (active metabolite)
Steady-state: 1 week
Distribution
Protein bound: >99% (parent); ~64% (active metabolite)
Vd: 92 L
Metabolism
Extensively metabolized after oral administration by hydrolysis of the valine ester to form the active metabolite ([+]-alpha-HTBZ) and by oxidative metabolism, primarily by CYP3A4/5, to form mono-oxidized valbenazine and other minor metabolites
[+]-alpha-HTBZ appears to be further metabolized in part by CYP2D6
Elimination
Half-life: 15-22 hr (parent drug and active metabolite)
Total plasma clearance: 7.2 L/hr
Excretion: 60% urine; 30% feces; <2% excreted as unchanged valbenazine or [+]-alpha-HTBZ
Pharmacogenomics
CYP2D6 poor metabolizers
- Consider reducing valbenazine dose based on tolerability for known CYP2D6 poor metabolizers
- Increased exposure (Cmax and AUC) to the active metabolite is anticipated in CYP2D6 poor metabolizers, which may increase risk for exposure-related adverse effects
Administration
Oral Administration
May take with or without food
Storage
Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F)
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Ingrezza Initiation Pack oral - | 40 mg (7)- 80 mg (21) capsule |  | |
| Ingrezza oral - | 80 mg capsule |  | |
| Ingrezza oral - | 40 mg capsule |  | |
| Ingrezza oral - | 60 mg capsule |  |
Copyright © 2010 First DataBank, Inc.
Formulary
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