Comparative Pharmacology
Head-to-head clinical analysis: AUSTEDO versus AUSTEDO XR.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUSTEDO versus AUSTEDO XR.
AUSTEDO vs AUSTEDO XR
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Deuterated tetrabenazine; inhibits vesicular monoamine transporter 2 (VMAT2), reducing dopamine uptake into synaptic vesicles and leading to decreased presynaptic dopamine release, similar to tetrabenazine but with altered pharmacokinetics due to deuterium substitution.
Deuterated tetrabenazine; inhibits vesicular monoamine transporter 2 (VMAT2), reducing dopamine and monoamine uptake into synaptic vesicles, thereby depleting presynaptic dopamine and other monoamines.
Initial 6 mg orally once daily; titrate by 6 mg increments at weekly intervals to a maximum of 48 mg/day. For tolerability, may divide into twice daily dosing (e.g., 12 mg twice daily).
Initial: 6 mg orally once daily. Titrate weekly by 6 mg/day increments to a maximum of 48 mg/day. Administer with food.
None Documented
None Documented
5-9 hours (parent); 7-10 hours (active metabolite). Steady state within 2-3 days.
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.
Urine (75-85% as metabolites, <5% unchanged); feces (10-15%)
Primarily hepatic metabolism via CYP2D6 and CYP3A4; <5% excreted unchanged in urine; fecal excretion accounts for ~50% of metabolites.
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor