Comparative Pharmacology
Head-to-head clinical analysis: AUSTEDO XR versus INGREZZA SPRINKLE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AUSTEDO XR versus INGREZZA SPRINKLE.
AUSTEDO XR vs INGREZZA SPRINKLE
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.
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: 6 mg orally once daily. Titrate weekly by 6 mg/day increments to a maximum of 48 mg/day. Administer with food.
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
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.
17-20 hours; steady state reached in approximately 5 days.
Primarily hepatic metabolism via CYP2D6 and CYP3A4; <5% excreted unchanged in urine; fecal excretion accounts for ~50% of metabolites.
60% renal (as unchanged drug and metabolites), 40% fecal (as metabolites).
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor