What is Valbenazine
Valbenazine is an oral pre-synaptic human vesicular monoamine transporter type 2 (VMAT2) inhibitor. The drug causes an inhibition of dopamine release via this mechanism. It is used to treat tardive dyskinesia (TD).
The efficacy of valbenazine in treating TD was shown in a randomized, double-blind, placebo controlled clinical trial (the KINECT 3 trial). After 6 weeks, adult participants who received valbenazine had improvement in the severity of abnormal involuntary movements, as measured by the Abnormal Involuntary Movement Scale (AIMS), compared to those who received placebo.
Somnolence is a common adverse effect of valbenazine and QT prolongation may occur during coadministration of a strong CYP2D6 or CYP3A4 inhibitor, or in those who are poor metabolizers of CYP2D6. Valbenazine received FDA approval for tardive dyskinesia in adults under fast-track, priority review and breakthrough drug designations in April 2017, as it was the first drug to receive approval for this condition.
Valbenazine was granted orphan drug designation by the FDA in October 2017 for the treatment of pediatric patients with Tourette’s syndrome; the drug is still investigational for this use.
Brand Name
INGREZZA
Indications
- tardive dyskinesia
Side Effects
- akathisia
- angioedema
- anxiety
- arthralgia
- blurred vision
- cholestasis
- constipation
- dizziness
- drowsiness
- dyskinesia
- fatigue
- headache
- hyperglycemia
- hyperprolactinemia
- hypersalivation
- infection
- insomnia
- nausea
- pruritus
- QT prolongation
- rash
- restlessness
- urinary retention
- urticaria
- vomiting
- weight gain
- xerostomia
Monitoring Parameters
- AIMS assessment
- neurologic function
Contraindications
- alcoholism
- bradycardia
- breast-feeding
- cardiac arrhythmias
- children
- coronary artery disease
- diabetes mellitus
- driving or operating machinery
- ethanol ingestion
- females
- geriatric
- heart failure
- hepatic disease
- hypertension
- hypocalcemia
- hypokalemia
- hypomagnesemia
- infants
- long QT syndrome
- malnutrition
- MAOI therapy
- myocardial infarction
- poor metabolizers
- pregnancy
- QT prolongation
- renal failure
- renal impairment
- thyroid disease
Interactions
- Acetaminophen; Butalbital
- Acetaminophen; Butalbital; Caffeine
- Acetaminophen; Butalbital; Caffeine; Codeine
- Amobarbital
- Amoxicillin; Clarithromycin; Lansoprazole
- Amoxicillin; Clarithromycin; Omeprazole
- Apalutamide
- Artemether; Lumefantrine
- Aspirin, ASA; Butalbital; Caffeine
- Aspirin, ASA; Butalbital; Caffeine; Codeine
- Atazanavir; Cobicistat
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Barbiturates
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Benzhydrocodone; Acetaminophen
- Boceprevir
- Butabarbital
- Cabergoline
- Carbamazepine
- Ceritinib
- Chloramphenicol
- Cinacalcet
- Clarithromycin
- Cobicistat
- Conivaptan
- Dacomitinib
- Darunavir
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Delavirdine
- Deutetrabenazine
- Dextromethorphan; Quinidine
- Digoxin
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Enzalutamide
- Fluoxetine
- Fluoxetine; Olanzapine
- Fosphenytoin
- Goserelin
- Idelalisib
- Indinavir
- Isocarboxazid
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Itraconazole
- Ketoconazole
- Letermovir
- Lofexidine
- Lopinavir; Ritonavir
- Mephobarbital
- Methohexital
- Mitotane
- Monoamine oxidase inhibitors
- Nefazodone
- Nelfinavir
- Ombitasvir; Paritaprevir; Ritonavir
- Paroxetine
- Pentobarbital
- Phenelzine
- Phenobarbital
- Phenytoin
- Posaconazole
- Primidone
- Quinidine
- Rasagiline
- Ribociclib
- Ribociclib; Letrozole
- Rifampin
- Ritonavir
- Safinamide
- Secobarbital
- Selegiline
- St. John’s Wort, Hypericum perforatum
- Telaprevir
- Telithromycin
- Tetrabenazine
- Thiopental
- Tipranavir
- Tranylcypromine
- Tucatinib
- Voriconazole
