Comparative Pharmacology
Head-to-head clinical analysis: AUSTEDO XR versus XENAZINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUSTEDO XR versus XENAZINE.
AUSTEDO XR vs XENAZINE
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.
Deutetrabenazine selectively and reversibly inhibits vesicular monoamine transporter 2 (VMAT2), thereby reducing dopamine and monoamine storage and release in presynaptic neurons.
Initial: 6 mg orally once daily. Titrate weekly by 6 mg/day increments to a maximum of 48 mg/day. Administer with food.
12.5 mg orally twice daily initially; titrate slowly by 12.5 mg every 3-5 days up to 50 mg twice daily (total daily dose 100 mg). Maximum recommended total daily dose: 100 mg.
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.
7-16 hours (mean 9-12 hours); requires twice-daily dosing for steady-state control of chorea.
Primarily hepatic metabolism via CYP2D6 and CYP3A4; <5% excreted unchanged in urine; fecal excretion accounts for ~50% of metabolites.
Primarily renal (75-85% as metabolites, <2% unchanged); minimal biliary/fecal elimination.
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor