Comparative Pharmacology
Head-to-head clinical analysis: AUSTEDO XR versus VALBENAZINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUSTEDO XR versus VALBENAZINE.
AUSTEDO XR vs VALBENAZINE
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, reducing dopamine release in the striatum.
Initial: 6 mg orally once daily. Titrate weekly by 6 mg/day increments to a maximum of 48 mg/day. Administer with food.
50 mg orally once daily; can be increased to 75 mg orally once daily based on tolerability and response.
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.
Clinical Note
moderateValbenazine + Haloperidol
"The metabolism of Haloperidol can be decreased when combined with Valbenazine."
Clinical Note
moderateValbenazine + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Valbenazine."
Clinical Note
moderateValbenazine + Erythromycin
"The metabolism of Erythromycin can be decreased when combined with Valbenazine."
Clinical Note
moderateValbenazine + Cyclosporine
Terminal elimination half-life is approximately 17-23 hours, allowing for once-daily dosing.
Primarily hepatic metabolism via CYP2D6 and CYP3A4; <5% excreted unchanged in urine; fecal excretion accounts for ~50% of metabolites.
Primarily hepatic metabolism; less than 30% of the dose excreted unchanged in urine and feces combined. Biliary/fecal excretion accounts for approximately 40-60% as metabolites.
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor
"The metabolism of Cyclosporine can be decreased when combined with Valbenazine."