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valbenazine

Adjunctive therapy

Brand: INGREZZA

Published 2025-12-22 · Last reviewed 2025-12-29 · 5 references

Content sourced from FDA labeling (DailyMed) and peer-reviewed literature.

Print sheet Review evidence

At a glance

Class: Adjunctive therapy·Typical dose: Initiate 40 mg once daily for 7 days, then increase to 80 mg once daily if tolerated.·Half-life: Mean half-life ≈15–22 hours (parent) and ≈18–20 hours (active metabolite); ~60% of the dose is recovered in urine and ~30% in feces, primarily as metabolites (<2% unchanged).·LAI available: No

Class: Adjunctive therapy
Typical dose: Initiate 40 mg once daily for 7 days, then increase to 80 mg once daily if tolerated.
Half-life: Mean half-life ≈15–22 hours (parent) and ≈18–20 hours (active metabolite); ~60% of the dose is recovered in urine and ~30% in feces, primarily as metabolites (<2% unchanged).
LAI available: No

Quick answers

What is valbenazine?: Valbenazine (Ingrezza) is an oral vesicular monoamine transporter 2 (VMAT2) inhibitor indicated for adults with tardive dyskinesia who remain on dopamine receptor–blocking agents.
What is INGREZZA?: INGREZZA is a brand name for valbenazine.
What is INGREZZA (valbenazine) used for?: Label indications include: Tardive dyskinesia.
What drug class is INGREZZA (valbenazine)?: VMAT2 Inhibitor.
What is the mechanism of action of INGREZZA (valbenazine)?: Vesicular monoamine transporter 2 (VMAT2) inhibitor.
What strengths does INGREZZA (valbenazine) come in?: Hard gelatin capsules: 40 mg, 60 mg, 80 mg (administer once daily with or without food).

General information

Valbenazine (Ingrezza) is an oral vesicular monoamine transporter 2 (VMAT2) inhibitor indicated for adults with tardive dyskinesia who remain on dopamine receptor–blocking agents.

Randomized trials demonstrate clinically meaningful Abnormal Involuntary Movement Scale (AIMS) reductions within two weeks that persist through 48-week extensions, supporting guideline placement as first-line VMAT2 therapy despite access hurdles such as prior authorization and copay costs.

The compare view can help compare dosing cadence, QT risk, and sedation across VMAT2 options and align AIMS-driven monitoring with site tardive dyskinesia protocols.

U.S. approvals

Tardive dyskinesia (adults) (2017)

Formulations & strengths

Hard gelatin capsules: 40 mg, 60 mg, 80 mg (administer once daily with or without food).

Generic availability

No generic formulation available as of 2025.

Frequently preferred over deutetrabenazine because of once-daily dosing and a modest monitoring burden; financial assistance is often required to initiate or continue therapy.

View labelExact

Mechanism of action

Refer to the Glossary entry on Neurotransmitters for background on receptor systems involved in serious mental illness.

Reversibly inhibits VMAT2, reducing vesicular packaging and synaptic release of dopamine within the nigrostriatal pathway.

Minimal affinity for serotonin, adrenergic, muscarinic, or histamine receptors preserves antipsychotic efficacy while dampening dyskinetic movements.

High-affinity VMAT2 inhibitor (parent and active metabolite).
Negligible binding to dopamine D2, serotonin 5-HT2, adrenergic, or muscarinic receptors.

Metabolism & pharmacokinetics

Median Tmax 4–8 hours; >99% protein bound with an apparent volume of distribution ≈92 L.
Extensively metabolized by CYP3A4/5 and CYP2D6 to the active metabolite NBI-98782; exposure increases in CYP2D6 poor metabolizers and with strong inhibitors.
Mean half-life ≈15–22 hours (parent) and ≈18–20 hours (active metabolite); ~60% of the dose is recovered in urine and ~30% in feces, primarily as metabolites (<2% unchanged).

Dosing & administration

Initiate 40 mg once daily for 7 days, then increase to 80 mg once daily if tolerated.
Limit to 40 mg once daily with strong CYP3A4 inhibitors or in moderate/severe hepatic impairment (Child-Pugh B/C); avoid use in Child-Pugh C when risk outweighs benefit.
Avoid strong CYP3A4 inducers (rifampin, carbamazepine, St. John’s wort) and consider 40 mg maintenance in CYP2D6 poor metabolizers or with strong CYP2D6 inhibitors.
Not recommended in severe renal impairment (eGFR <30 mL/min/1.73 m^2).

Monitoring & labs

Baseline and follow-up AIMS scoring (and functional impact) to document benefit and support payer renewals.
Sedation and falls risk, especially in older adults and when other CNS depressants are co-prescribed.
QTc monitoring when cardiac risk exists or when other QT-prolonging drugs are used.
Medication reconciliation for CYP3A4/2D6 inhibitors/inducers that can shift exposure and tolerability.

Valbenazine treats TD symptoms while the dopamine-blocking agent often continues; monitoring focuses on AIMS response and on sedation/QT-related safety.

Adverse effects

FDA boxed warnings

Common side effects (≥10%)

Somnolence: Warn patients about driving or operating machinery until they know their response.
Dry mouth: Usually mild; encourage hydration and oral care.
Fatigue and gait instability: Monitor older adults for falls—consider dose reduction if problematic.

Other notable effects

Dose-dependent QTc prolongation (mean ~6 msec at 80 mg); obtain baseline and follow-up ECGs when other QT-prolonging risks are present.
Rare parkinsonism or akathisia; reduce dose or discontinue if new movement symptoms emerge.
Potential for hypersensitivity reactions and angioedema reported in post-marketing surveillance.

Interactions

Contraindicated with strong CYP3A4 inducers (rifampin, carbamazepine, phenytoin, St. John’s wort) due to markedly reduced exposure.
Strong CYP3A4 inhibitors (ketoconazole, clarithromycin) and strong CYP2D6 inhibitors (paroxetine, fluoxetine, quinidine) increase exposure—limit to 40 mg/day and monitor for somnolence and QTc effects.
Additive QT prolongation with other QT-active agents (e.g., ziprasidone, methadone, class Ia/III antiarrhythmics); avoid or monitor closely.
Avoid concomitant reserpine or other VMAT2 inhibitors because of theoretical additive monoamine depletion.

Other useful information

Document baseline AIMS score and reassess every 4–12 weeks to gauge benefit and guide payer renewals.
Maintain the underlying antipsychotic when clinically feasible; valbenazine treats TD symptoms rather than the primary psychiatric disorder.
If two or more consecutive doses are missed, instruct patients to restart at 40 mg for one week before re-escalating.
Discuss pregnancy registry participation and lactation data limitations when applicable.
Review other QT-active medications and CYP3A4/2D6 modulators before dose increases; this helps prevent avoidable sedation or QTc effects.

References

Related hubs:SMI toolkit·Support resources