Comparative Pharmacology
Head-to-head clinical analysis: VALBENAZINE versus VALBENAZINE TOSYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: VALBENAZINE versus VALBENAZINE TOSYLATE.
VALBENAZINE vs VALBENAZINE TOSYLATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Vesicular monoamine transporter 2 (VMAT2) inhibitor, reducing dopamine release in the striatum.
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.
50 mg orally once daily; can be increased to 75 mg orally once daily based on tolerability and response.
Initial dose: 6 mg orally twice daily; may increase to 12 mg twice daily based on response.
None Documented
None Documented
Terminal elimination half-life is approximately 17-23 hours, allowing for once-daily dosing.
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
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.
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.
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
"The metabolism of Cyclosporine can be decreased when combined with Valbenazine."