Tolterodine is a competitive muscarinic receptor antagonist that was developed for the management of OAB. There are currently two oral formulations: an immediate-release (Detrol) available in 1- and 2-mg tablets given twice per day, and an extended-release pill available as 4mg given once per day (Detrol LA; Pfizer, Inc., New York, NY).
Tolterodine immediate-release has consistently demonstrated a 20% reduction in micturition episodes, and a 40% to 60% reduction in weekly urge incontinence episodes versus placebo in randomized, double-blind, placebo-controlled studies.810
The mechanism of action is similar to oxybutynin, but the adverse side-effect profile is improved. The better tol-erability profile of tolterodine compared with immediate-release oxybutynin has been confirmed in two randomized studies of detrusor overactivity. In a meta-analysis including 1120 patients, Appell11 reported severe xerostomia in 6% of placebo, 4% of the 2-mg tolterodine arm, 17% of the 4-mg tolterodine arm, and 60% of the 15-mg immediate-release oxybutynin arm.
Extended-release tolterodine (Detrol LA) is a once-daily dosage that utilizes a microsphere system to deliver a more uniform serum concentration. Van Kerrebroeck et al.12 demonstrated in a phase III study that Detrol LA was statistically superior to Detrol in terms of tolerability, namely, xerostomia (P < .02), whereas maintaining similar efficacy in significantly reducing mean urge incontinence episodes per week and mean micturition frequency.
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