Comparative Pharmacology
Head-to-head clinical analysis: TOLTERODINE versus VESICARE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: TOLTERODINE versus VESICARE.
TOLTERODINE vs VESICARE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Competitive antagonist at muscarinic acetylcholine receptors (M1-M5), with selectivity for M3 receptors over M2. Inhibits bladder detrusor muscle contraction, increasing bladder capacity and reducing urinary urgency.
2 mg PO twice daily; may reduce to 1 mg twice daily if tolerated.
5 mg orally once daily; may increase to 10 mg once daily if needed.
None Documented
None Documented
Terminal elimination half-life is 2-4 hours in extensive CYP2D6 metabolizers; increased to 4-10 hours in poor metabolizers or with CYP3A4 inhibitors.
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 approximately 45 hours (range 33–57 hours), supporting once-daily dosing.
Primarily hepatic metabolism via CYP2D6 and CYP3A4; renal excretion accounts for <5% of unchanged drug; ~80% excreted in urine as metabolites, ~20% in feces.
Approximately 70% of an oral dose is excreted in urine (mainly as metabolites, <15% unchanged) and 25% in feces.
Category A/B
Category C
Anticholinergic
Anticholinergic
"The metabolism of Clotrimazole can be decreased when combined with Tolterodine."