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[Pharmacology](https://durgical.com/en/pharmacology/) · Class

# VMAT2 inhibitors

Drugs that empty dopamine stores in nerve endings. Used for Huntington chorea and tardive dyskinesia; they can cause depression and parkinsonism.

Updated 2026-11-01

## What they are

Tetrabenazine, deutetrabenazine and valbenazine block the vesicular monoamine transporter 2. They treat hyperkinetic movement disorders: chorea of Huntington disease and tardive dyskinesia caused by long-term antipsychotics.

## Mechanism of action

VMAT2 loads dopamine, serotonin, noradrenaline and histamine into synaptic vesicles. Blocking it reversibly leaves the transmitters in the cytoplasm, where they are broken down, so less dopamine is released onto striatal neurons.

Target: Vesicular monoamine transporter 2 (VMAT2)

## Key points

- Depression and suicidality: boxed warning in Huntington disease; contraindicated in untreated depression or active suicidality.
- Not combined with MAO inhibitors or reserpine, nor with each other.
- CYP2D6 metabolism: strong CYP2D6 inhibitors (fluoxetine, paroxetine) raise exposure; QT prolongation is a risk.
- Adverse effects from monoamine depletion: somnolence, parkinsonism, akathisia and, rarely, neuroleptic malignant syndrome.

## Drugs in this class

- [**Tetrabenazine** A VMAT2 inhibitor that depletes dopamine to control Huntington chorea. It can cause depression, suicidality and… Vesicular monoamine transporter 2 (VMAT2)](https://durgical.com/en/pharmacology/tetrabenazine/)
- [**Deutetrabenazine** A deuterated form of tetrabenazine whose active metabolites last longer. Treats Huntington chorea and tardive… Vesicular monoamine transporter 2 (VMAT2)](https://durgical.com/en/pharmacology/deutetrabenazine/)
- [**Valbenazine** A selective VMAT2 inhibitor for tardive dyskinesia and Huntington chorea. Watch for sleepiness, QT prolongation and… Vesicular monoamine transporter 2 (VMAT2)](https://durgical.com/en/pharmacology/valbenazine/)

## Test yourself

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

## Which two hyperkinetic disorders are treated with VMAT2 inhibitors?

Chorea of Huntington disease and tardive dyskinesia.

## Which psychiatric warning applies to VMAT2 inhibitors in Huntington disease?

Increased risk of depression and suicidal thoughts.

## Why do VMAT2 inhibitors cause parkinsonism?

They deplete dopamine stores in nerve terminals, so less dopamine reaches striatal receptors.

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

Sources: Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 21 (McGraw Hill, 2023); Farmacología básica y clínica (Katzung), 16.ª ed., cap. 28 (McGraw Hill, 2025); [DailyMed - TETRABENAZINE tablet](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=471ac1d8-e3ad-7729-87c5-c26ae92c32eb) (DailyMed (U.S. National Library of Medicine), 2026); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N07XX) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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