Comparative Pharmacology
Head-to-head clinical analysis: AUSTEDO XR versus INGREZZA.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUSTEDO XR versus INGREZZA.
AUSTEDO XR vs INGREZZA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Deuterated tetrabenazine; inhibits vesicular monoamine transporter 2 (VMAT2), reducing dopamine and monoamine uptake into synaptic vesicles, thereby depleting presynaptic dopamine and other monoamines.
Vesicular monoamine transporter 2 (VMAT2) inhibitor; reduces presynaptic dopamine release.
Initial: 6 mg orally once daily. Titrate weekly by 6 mg/day increments to a maximum of 48 mg/day. Administer with food.
80 mg orally once daily; may titrate from 40 mg once daily for 7 days to reduce nausea.
None Documented
None Documented
Deutetrabenazine: 9-10 hours; major active metabolites (α-HTBZ and β-HTBZ): 7-15 hours; allows twice-daily dosing for immediate-release, but AUSTEDO XR is once-daily.
Terminal elimination half-life of deutetrabenazine is 9-10 hours; clinical context: supports twice-daily dosing.
Primarily hepatic metabolism via CYP2D6 and CYP3A4; <5% excreted unchanged in urine; fecal excretion accounts for ~50% of metabolites.
Approximately 60% renal (as unchanged drug and metabolites) and 30% fecal.
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor