Reversible inhibitors of human vesicular monoamine
transporter type 2
a
Generic name
Trade name
Deutetrabenazine
Austedo
Tetrabenazine
Xenazine
Valbenazine
Ingrezza
Available
formulations
(mg)
Tablet: 6, 9, 12 Tablet: 12.5, 25 Capsule: 40, 80
Typical dose
range (mg/day)
12–48 25–75 40–80
Bioavailability 80% 75% 49%
Time to peak
level (hours)
3–4 1–2 0.5–1
Protein binding 60% to 68%
(alpha-HTBZ)
59% to 63%
(beta-HTBZ)
82% to 85%
60% to 68%
(alpha-HTBZ)
59% to 63%
(beta-HTBZ)
>99%
64% alpha-HTBZ
Metabolism Hepatic Hepatic Hepatic
Metabolic
enzymes/
transporters
Major substrate
of CYP2D6
b
,
minor substrate
of CYP1A2 and
CYP3A4
Major substrate
of CYP2D6
c
Major substrate
of CYP3A4, minor
substrate of
CYP2D6
d
Metabolites Deuterated alpha-
and beta-HTBZ:
Active
Alpha-, beta-, and
O-dealkylated
HTBZ: Active
alpha-HTBZ: Active
Elimination half-
life (hours)
Deuterated alpha-
and beta-HTBZ:
9–10
Alpha-HTBZ: 4–8
Beta-HTBZ: 2–4
15–22
Excretion Urine (~75%-85%
changed);
feces (~8%–11%)
Urine (~75%
changed);
feces (~7%–16%)
Urine: 60%; feces:
30%
a
This table includes information compiled from multiple sources. Detailed information on issues
such as dose regimen, dose adjustments, medication administration procedures, handling
precautions, and storage can be found in product labeling. It is recommended that readers
consult product labeling information for authoritative information on these medications.
b
Do not exceed total daily dosage of 36 mg/day (18 mg/dose) in poor CYP2D6 metabolizers or
patients taking a strong CYP2D6 inhibitor. Assess ECG before and after increasing the daily dose
above 24 mg in patients at risk for QTc prolongation.
c
Test for CYP2D6 metabolizer status before giving doses >50 mg/day. Do not exceed 50 mg/day
in poor metabolizers or in patients treated with a strong inhibitor of CYP2D6.
d
Use is not recommended with strong CYP3A4 inducer. A reduced dose is recommended with
concomitant use of strong CYP3A4 or CYP2D6 inhibitors or in poor CYP2D6 metabolizers.
Treatment
