Comparative Pharmacology
Head-to-head clinical analysis: AUSTEDO versus GOCOVRI.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUSTEDO versus GOCOVRI.
AUSTEDO 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 uptake into synaptic vesicles and leading to decreased presynaptic dopamine release, similar to tetrabenazine but with altered pharmacokinetics due to deuterium substitution.
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 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: 68.5 mg orally once daily at bedtime for 1 week; then increase to 137 mg once daily.
None Documented
None Documented
5-9 hours (parent); 7-10 hours (active metabolite). Steady state within 2-3 days.
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.
Urine (75-85% as metabolites, <5% unchanged); feces (10-15%)
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