Treatment of patients with an overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence

Tolterodine is a competitive antagonist of muscarinic receptors. In animal models, tolterodine demonstrates selectivity for urinary bladder receptors over salivary receptors. Urinary bladder contraction is mediated by muscarinic receptors. Tolterodine increases residual urine volume and decreases detrusor muscle pressure.

Protein binding: >96% (primarily to alpha1-acid glycoprotein); Metabolism: Extensively hepatic, primarily via CYP2D6 (some metabolites share activity) and 3A4 usually (minor pathway); Elimination half-life: in Extensive metabolizers: ~7 hours; Poor metabolizers: ~18 hours; Excretion: Urine (77%); feces (17%); primarily as metabolites (<1% unchanged drug)

Hypersensitivity to tolterodine or any component of the formulation; urinary retention; gastric retention; uncontrolled narrow-angle glaucoma

C

Avoided.

Dry mouth, dyspepsia, abnormal vision, dry eyes, headache

The recommended dose is 4 mg once daily except in patients with impaired liver function and severely impaired renal function (GFR ≦ 30 ml/min) for whom the recommended dose is 2 mg once daily. The prolonged-released capsules can be taken with or without food and must be swallowed whole. Do not crush, chew, or open it. Children: Safety and effectiveness in children have not yet been established.

severely impaired renal function (GFR ≦ 30 ml/min): the recommended dose is 2 mg once daily.

with impaired liver function: the recommended dose is 2 mg once daily.