Reversible inhibitors of human vesicular monoamine
transporter type 2
a
Generic name
Trade name
Deutetrabenazine
Austedo
Tetrabenazine
Xenazine
Valbenazine
Ingrezza
Hepatic
impairment
Contraindicated Contraindicated Maximum dose of
40 mg daily with
moderate to severe
impairment (Child-
Pugh score 7–15)
Renal impairment No information
available
No information
available
Use not
recommended
in severe renal
impairment (CrCl
<30 mL/min)
Common adverse
effect
Sedation Sedation,
depression,
extrapyramidal
effects, insomnia,
akathisia, anxiety,
nausea, falls
Sedation
Effect of food on
bioavailability
Food affects
maximal
concentration.
Administer with
food.
Unaffected by
food
Can be taken
with or without
food. High fat
meals decrease
the C
max
and AUC
for valbenazine,
but values for the
active metabolite
(alpha-HTBZ) are
unchanged.
Comments
e
Swallow tablets
whole and do
not chew, crush,
or break. Give in
divided doses;
increase from
initial dose of 12
mg/day by 6 mg/
week to maximum
dose of 48 mg/
day. Retitrate dose
for treatment
interruptions of
more than 1 week.
f
Give in divided
doses; increase
from initial dose
of 25–50 mg/day
by 12.5 mg/ week
to maximum of
150–200 mg/day.
Retitrate dose
for treatment
interruptions
of more than 5
days.
f
Initiate at 40 mg/
day and increase to
80 mg/day after 1
week.
Continuation of
40 mg/day may
be considered for
some patients.
f
e
All VMAT2 inhibitors are contraindicated within 2 weeks of a monoamine oxidase inhibitor,
within 20 days of reserpine, or in patients with active suicidal ideas or untreated depression.
Tetrabenazine and deutetrabenazine carry a boxed warning related to depression and suicidal
ideation in patients with Huntington's disease.
f
Avoid use in patients with congenital long QT syndrome, with arrhythmias associated with a
prolonged QT interval, or with other risks for QTc prolongation, such as interactions via CYP
metabolism.
(cont'd)
