24
Treatment
Reversible inhibitors of human vesicular monoamine
transporter type 2
a
Genric 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,
minor substrate
of CYP1A2 and
CYP3A4
Major substrate
of CYP2D6
Major substrate
of CYP3A4,
minor substrate
of CYP2D6
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%
