Comparative Pharmacology
Head-to-head clinical analysis: INGREZZA SPRINKLE versus VALBENAZINE TOSYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: INGREZZA SPRINKLE versus VALBENAZINE TOSYLATE.
INGREZZA SPRINKLE vs VALBENAZINE TOSYLATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Valbenazine is a selective vesicular monoamine transporter 2 (VMAT2) inhibitor. By inhibiting VMAT2, it reduces the uptake of monoamines into synaptic vesicles, thereby decreasing presynaptic dopamine concentrations and mitigating dopaminergic hyperactivity associated with tardive dyskinesia.
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.
Initial dose: 6 mg orally twice daily; may increase to 12 mg twice daily based on response.
None Documented
None Documented
17-20 hours; steady state reached in approximately 5 days.
The terminal elimination half-life of valbenazine is approximately 15–22 hours for the parent drug and 20–25 hours for its active metabolite, (+)-α-dihydrotetrabenazine (dihydrotetrabenazine). The long half-life supports once-daily dosing.
60% renal (as unchanged drug and metabolites), 40% fecal (as metabolites).
Approximately 73% of the dose is excreted in feces (primarily as parent drug and metabolites) and 20% in urine. The major metabolites are valbenazine glucuronide and its acid metabolite.
Category C
Category C
VMAT2 Inhibitor
VMAT2 Inhibitor