Comparative Pharmacology
Head-to-head clinical analysis: LUSEDRA versus TOLTERODINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: LUSEDRA versus TOLTERODINE.
LUSEDRA vs TOLTERODINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
LUSEDRA (valbenazine) is a selective vesicular monoamine transporter 2 (VMAT2) inhibitor. It reduces presynaptic dopamine release by inhibiting VMAT2, thereby reducing dopamine neurotransmission in the striatum.
Competitive antagonist of muscarinic acetylcholine receptors (M1, M2, M3, M4, M5), with selectivity for the M3 receptor subtype involved in detrusor muscle contraction, reducing bladder smooth muscle contractility and increasing bladder capacity.
5 mg orally once daily.
2 mg PO twice daily; may reduce to 1 mg twice daily if tolerated.
None Documented
None Documented
8-12 hours (terminal, prolonged in renal impairment; dose adjustment needed if CrCl <30 mL/min).
Clinical Note
moderateTolterodine + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Tolterodine."
Clinical Note
moderateTolterodine + Cyclosporine
"The metabolism of Cyclosporine can be decreased when combined with Tolterodine."
Clinical Note
moderateTolterodine + Fluconazole
"The metabolism of Fluconazole can be decreased when combined with Tolterodine."
Clinical Note
moderateTolterodine + Clotrimazole
Terminal elimination half-life is 2-4 hours in extensive CYP2D6 metabolizers; increased to 4-10 hours in poor metabolizers or with CYP3A4 inhibitors.
Primarily renal (70-80% as unchanged drug); 20-30% via biliary/fecal.
Primarily hepatic metabolism via CYP2D6 and CYP3A4; renal excretion accounts for <5% of unchanged drug; ~80% excreted in urine as metabolites, ~20% in feces.
Category C
Category A/B
Anticholinergic
Anticholinergic
"The metabolism of Clotrimazole can be decreased when combined with Tolterodine."