Section 17 · Monograph
Tolterodine
Reviewed Nov 2026FDA label
DetrolAntimuscarinic
- Forms
- Tab: 1, 2mg | ER cap: 2, 4mg
- Dose
- 2mg BID (or ER 4mg once daily); 1mg BID with hepatic impairment or strong CYP3A4 inhibitors
- MOA
- Muscarinic receptor blockade
Indications
- Overactive bladder with symptoms of urge urinary incontinence, urgency and frequencyFDA-labeled
Mechanism of Action
- Competitive muscarinic receptor antagonist that reduces detrusor contractility
Full Dosing
Adult / usual
- Immediate-release: 2mg twice daily; may reduce to 1mg twice daily
Hepatic
- Extended-release: 4mg once daily (2mg once daily with significant hepatic impairment or strong CYP3A4 inhibitors)
Contraindications
- Urinary retention
- Gastric retention
- Uncontrolled narrow-angle glaucoma
- Known hypersensitivity
Drug Interactions
- CYP2D6 and CYP3A4 inhibitors raise levels
- Other anticholinergics: additive effects
- Cholinesterase inhibitors are antagonized
Adverse Effects
- Dry mouth, constipation, headache
- QT prolongation at higher exposures
- Blurred vision, cognitive effects
Monitoring Parameters
- Post-void residual in neurogenic bladder
- Cognition in older adults
Pregnancy & Lactation
- Limited data; use only if benefit justifies risk
- Unknown whether present in human milk