Comparative Pharmacology
Head-to-head clinical analysis: GOCOVRI versus INGREZZA SPRINKLE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: GOCOVRI versus INGREZZA SPRINKLE.
GOCOVRI vs INGREZZA SPRINKLE
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.
INGREZZA SPRINKLE contains valbenazine, a selective VMAT2 inhibitor that reduces the release of dopamine into the synaptic cleft, thereby decreasing dopaminergic neurotransmission in the striatum. The exact mechanism for the treatment of tardive dyskinesia is unknown but is thought to involve modulation of dopamine signaling.
Initial: 68.5 mg orally once daily at bedtime for 1 week; then increase to 137 mg once daily.
Initial dose: 40 mg orally once daily (as 1 capsule of INGREZZA SPRINKLE 40 mg or 4 capsules of 10 mg). After 1 week, increase to target dose of 80 mg orally once daily (as 2 capsules of 40 mg or 8 capsules of 10 mg). Capsules may be swallowed whole or opened and sprinkled onto soft food.
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.
17-20 hours; steady state reached in approximately 5 days.
Renal excretion accounts for approximately 80% of elimination, with about 60% as unchanged drug and 20% as metabolites. Fecal excretion is minimal (<5%).
60% renal (as unchanged drug and metabolites), 40% fecal (as metabolites).
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor