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)
Drugs in this class
- TetrabenazineA VMAT2 inhibitor that depletes dopamine to control Huntington chorea. It can cause depression, suicidality and…Vesicular monoamine transporter 2 (VMAT2)
- DeutetrabenazineA deuterated form of tetrabenazine whose active metabolites last longer. Treats Huntington chorea and tardive…Vesicular monoamine transporter 2 (VMAT2)
- ValbenazineA selective VMAT2 inhibitor for tardive dyskinesia and Huntington chorea. Watch for sleepiness, QT prolongation and…Vesicular monoamine transporter 2 (VMAT2)
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.
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 (DailyMed (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).
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Representative model, for educational purposes only.