Comparative Pharmacology
Head-to-head clinical analysis: AUSTEDO versus INGREZZA SPRINKLE.
Head-to-head clinical analysis: AUSTEDO versus INGREZZA SPRINKLE.
AUSTEDO 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 uptake into synaptic vesicles and leading to decreased presynaptic dopamine release, similar to tetrabenazine but with altered pharmacokinetics due to deuterium substitution.
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 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 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
5-9 hours (parent); 7-10 hours (active metabolite). Steady state within 2-3 days.
17-20 hours; steady state reached in approximately 5 days.
Urine (75-85% as metabolites, <5% unchanged); feces (10-15%)
60% renal (as unchanged drug and metabolites), 40% fecal (as metabolites).
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor