Comparative Pharmacology
Head-to-head clinical analysis: AUSTEDO versus VALBENAZINE TOSYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUSTEDO versus VALBENAZINE TOSYLATE.
AUSTEDO vs VALBENAZINE TOSYLATE
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.
Valbenazine is a selective vesicular monoamine transporter 2 (VMAT2) inhibitor. By inhibiting VMAT2, it reduces the uptake of monoamines into synaptic vesicles, thereby decreasing presynaptic dopamine concentrations and mitigating dopaminergic hyperactivity associated with tardive dyskinesia.
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 dose: 6 mg orally twice daily; may increase to 12 mg twice daily based on response.
None Documented
None Documented
5-9 hours (parent); 7-10 hours (active metabolite). Steady state within 2-3 days.
The terminal elimination half-life of valbenazine is approximately 15–22 hours for the parent drug and 20–25 hours for its active metabolite, (+)-α-dihydrotetrabenazine (dihydrotetrabenazine). The long half-life supports once-daily dosing.
Urine (75-85% as metabolites, <5% unchanged); feces (10-15%)
Approximately 73% of the dose is excreted in feces (primarily as parent drug and metabolites) and 20% in urine. The major metabolites are valbenazine glucuronide and its acid metabolite.
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor