Valbenazine !

A selective VMAT2 inhibitor for tardive dyskinesia and Huntington chorea. Watch for sleepiness, QT prolongation and MAO inhibitor interactions.

Updated 2026-11-01

Class: VMAT2 inhibitors
Transporter: Vesicular monoamine transporter 2 (VMAT2)
ATC code: N07XX13

Vesicular monoamine transporter 2 (VMAT2)Valbenazine

The figure shows valbenazine bound to human VMAT2 (cryo-EM structure).

Target in 3D: Vesicular monoamine transporter 2 (VMAT2). PDB structure 9KQ8 (RCSB PDB, public domain). View the structure at RCSB PDB

Mechanism of action

Valbenazine is converted to an active metabolite that selectively and reversibly inhibits VMAT2. Less dopamine is loaded into vesicles and released onto supersensitive striatal receptors, so the involuntary movements of tardive dyskinesia decrease.

Valbenazine becomes an active VMAT2-blocking metabolite
Less dopamine is stored in vesicles
Supersensitive striatal receptors get less stimulation
Tardive movements of mouth, face and limbs decrease

Pharmacokinetics

Metabolism: Converted to an active metabolite; CYP3A4 and CYP2D6 are involved

Indications

Tardive dyskinesia in adults Antipsychotic-induced movement disorders (dystonia, akathisia, parkinsonism, tardive dyskinesia) →
Chorea of Huntington disease Huntington disease →

Adverse effects

Common

Sleepiness and tiredness
Restlessness (akathisia)
Anticholinergic-type effects: dry mouth, constipation, blurred vision, difficulty urinating
Balance problems and falls, headache, nausea

Contraindications

Hypersensitivity to valbenazine
MAO inhibitors (avoided, including within two weeks)
Caution: long QT syndrome, recent heart attack, heart failure, liver disease

Key interactions

MAO inhibitors (including rasagiline, safinamide, selegiline): Excess monoamines; avoided
Strong CYP2D6 inhibitors (paroxetine, fluoxetine) or CYP3A4 inhibitors: Higher exposure; dose is reduced
St John's wort: May interact; checked before use
Alcohol and sedatives: More drowsiness

What is monitored

Involuntary movement scale over time
Mood and suicidal thoughts
ECG when QT risk factors are present
Sleepiness, gait and falls

Administration and safety

Capsules are given once a day; sprinkle capsules can be mixed with a spoonful of soft food
Breastfeeding is avoided during treatment and for some days after the last dose
Look-alike names with other «-benazine» drugs

Nursing care

Teach not to drive until sleepiness is known; avoid alcohol
Ask about low mood and suicidal thoughts
Report palpitations, fainting or swelling of the face
Ask about grapefruit and new medicines that may interact

Pregnancy and breastfeeding

Human data are limited; pregnancy during treatment is discussed with the specialist.

Test yourself

Think of the answer, then tap the question to see it.

What is the main indication of valbenazine?

Tardive dyskinesia in adults; it is also used for Huntington chorea.

Which cardiac risk is monitored with valbenazine?

QT prolongation, especially with CYP2D6 or CYP3A4 inhibitors or long QT syndrome.

Which drug group must not be combined with valbenazine?

MAO inhibitors, including the MAO-B inhibitors used in Parkinson disease.

Add to my cards (3)

← Back to the class: VMAT2 inhibitors

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Valbenazine: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2025); Farmacología básica y clínica (Katzung), 16.ª ed., cap. 28 (McGraw Hill, 2025); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

Spotted a mistake?We are always improving for the community. Tell us what is wrong and our team will review it.Report a mistake

Representative model, for educational purposes only.