Comparative Pharmacology
Head-to-head clinical analysis: AUSTEDO XR versus GOCOVRI.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUSTEDO XR versus GOCOVRI.
AUSTEDO XR vs GOCOVRI
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.
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.
Initial: 6 mg orally once daily. Titrate weekly by 6 mg/day increments to a maximum of 48 mg/day. Administer with food.
Initial: 68.5 mg orally once daily at bedtime for 1 week; then increase to 137 mg once daily.
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.
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.
Primarily hepatic metabolism via CYP2D6 and CYP3A4; <5% excreted unchanged in urine; fecal excretion accounts for ~50% of metabolites.
Renal excretion accounts for approximately 80% of elimination, with about 60% as unchanged drug and 20% as metabolites. Fecal excretion is minimal (<5%).
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor