Muscarinic receptor antagonist for overactive bladder
ATC code: G04BD07 (Tolterodine)
Brand names
Detrol LA, Detrol
Competitive antagonist of muscarinic M2 and M3 receptors without significant subtype selectivity. CYP2D6 metabolises tolterodine to 5-hydroxymethyl-tolterodine, an active metabolite of equal pharmacological activity. In CYP2D6 poor metabolisers (5–10% of Europeans) the parent compound dominates, increasing adverse effect risk. Half-life 2–3 hours in extensive metabolisers, up to 10 hours in poor metabolisers.
Second line
Tolterodine is a second-line muscarinic blocker for overactive bladder. NG123 (2024) and EAU 2024 recommend behavioural therapy first: bladder training, caffeine restriction, a 3-day voiding diary. If symptoms persist, AEMPS approves tolterodine 2 mg twice daily (or 4 mg once daily SR). The STAR trial (Chapple 2007, Eur Urol) showed solifenacin 5–10 mg achieves better urgency control than tolterodine 4 mg SR.
Second line
AEMPS approves tolterodine for urge urinary incontinence in adults after behavioural therapy fails. Cochrane 2012 (CD003781) pooled antimuscarinic data: they reduce incontinence episodes by 1–3 per day vs placebo, NNT around 8. Dry mouth 20–30%, and around 35–40% of patients stop therapy at 6 months due to side effects.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Tolterodine is sometimes prescribed to children with nocturnal enuresis against international guidelines. ICCS 2020 and 2023 place desmopressin and alarm therapy (moisture-triggered alarm) as first line. In children under 12 years, tolterodine is not approved by AEMPS or . Cochrane Review (Sureshkumar 2003, updated 2011) rated the evidence for antimuscarinics in children as low quality: 4 small RCTs with varied methodology and wide effect estimates. In a child, the drug increases the risk of urinary retention and cognitive side effects. If tolterodine was prescribed to a child without a trial of alarm therapy and desmopressin, consider seeking a second opinion.
Not recommended
Tolterodine is for overactive bladder, not a symptomatic drug for frequent toilet visits. Increased urinary frequency can mean UTI, diabetes mellitus, BPH, neurological disease, or excess caffeine and fluid intake. In older patients with UTI, a muscarinic blocker masks the infection and delays antibacterial therapy. Per Beers Criteria 2023 (AGS) all muscarinic blockers fall into the «avoid in older adults» category, especially with cognitive impairment. If tolterodine was prescribed without a bladder ultrasound, urinalysis, or discussion of behavioural therapy, consider seeking a second opinion.
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FDA Category C. No controlled human pregnancy studies. AEMPS does not recommend use in pregnancy; animal models showed increased embryonic mortality at supra-therapeutic doses.
Limited data. The active metabolite appears in animal milk. AEMPS advises choosing between therapy and breastfeeding. When an antimuscarinic is required during lactation, trospium is preferable (quaternary amine with minimal milk transfer).
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Tolterodine is evaluated for the following indications with varying evidence strength: Overactive bladder (evidence tier B), Urge urinary incontinence (evidence tier B), Nocturnal enuresis in children (evidence tier D). See the full indication matrix with dosing and citations above on this page.
Common side effects of Tolterodine (≥ 1 in 100): Dry mouth (20–30%), Constipation (5–7%), Dry eyes, Headache, Somnolence, Dry skin. See the Safety section for uncommon and serious reactions.
FDA category C. FDA Category C. No controlled human pregnancy studies. AEMPS does not recommend use in pregnancy; animal models showed increased embryonic mortality at supra-therapeutic doses.
Limited data. The active metabolite appears in animal milk. AEMPS advises choosing between therapy and breastfeeding. When an antimuscarinic is required during lactation, trospium is preferable (quaternary amine with minimal milk transfer).
Tolterodine is contraindicated in: Hypersensitivity to tolterodine; Urinary retention; Gastric retention; Uncontrolled narrow-angle glaucoma; Myasthenia gravis. Full list in the Safety section.