Comparative Pharmacology
Head-to-head clinical analysis: GOCOVRI versus VALBENAZINE TOSYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GOCOVRI versus VALBENAZINE TOSYLATE.
GOCOVRI vs VALBENAZINE TOSYLATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
GOCOVRI (amantadine) is an NMDA receptor antagonist that modulates glutamate-mediated excitotoxicity and increases dopamine release by inhibiting the vesicular monoamine transporter 2 (VMAT2) and potentiating dopaminergic function. It also has anticholinergic properties.
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: 68.5 mg orally once daily at bedtime for 1 week; then increase to 137 mg once daily.
Initial dose: 6 mg orally twice daily; may increase to 12 mg twice daily based on response.
None Documented
None Documented
The terminal elimination half-life is approximately 60–70 hours in healthy subjects, which supports once-daily dosing. Half-life may be prolonged in renal impairment.
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.
Renal excretion accounts for approximately 80% of elimination, with about 60% as unchanged drug and 20% as metabolites. Fecal excretion is minimal (<5%).
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