Antimuscarinic (overactive bladder) Pregnancy: Not recommended during pregnancy — there are no adequate data in pregnant women and animal studies have shown reproductive toxicity. Tolterodine should be avoided during lactation (SPC §4.6).

Tolterodine tartrate

Brand names: Detrusitol, Detrusitol XL

Tolterodine tartrate is an oral antimuscarinic, available as immediate- and modified-release forms, used to treat overactive bladder with urinary frequency, urgency and urge incontinence.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 2 mg twice daily (immediate-release tablets)

Route: Oral

Frequency: Twice daily

UK SPC (Detrusitol 1 mg film-coated tablets) §4.2: adults, including elderly — the recommended dose is 2 mg twice daily, except in patients with impaired liver function or severely impaired renal function (GFR ≤30 ml/min), for whom the recommended dose is 1 mg twice daily. In case of troublesome side effects the dose may be reduced from 2 mg to 1 mg twice daily. The effect of treatment should be re-evaluated after 2–3 months. No maximum dose is stated in the retrieved §4.2. Paediatric: efficacy has not been demonstrated in children, therefore Detrusitol is not recommended for children. Cross-check — US labelling in this bundle describes a DIFFERENT formulation: tolterodine tartrate extended-release capsules 4 mg once daily with water, swallowed whole, lowered to 2 mg once daily in mild to moderate hepatic impairment (Child-Pugh A or B), severe renal impairment (CrCl 10–30 mL/min) or with potent CYP3A4 inhibitors; not recommended if CrCl <10 mL/min or in severe hepatic impairment (Child-Pugh C). Do not apply the modified-release regimen to immediate-release tablets.

Dose adjustments

Renal

Severely impaired renal function (GFR ≤30 ml/min): 1 mg twice daily (SPC §4.2). US labelling for the extended-release capsules: 2 mg once daily if CrCl 10–30 mL/min; not recommended if CrCl <10 mL/min.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Urinary retention
Uncontrolled narrow-angle glaucoma
Myasthenia gravis
Known hypersensitivity to tolterodine or to any of the excipients
Severe ulcerative colitis
Toxic megacolon

Side effects

Dry mouth (very common — 35% of treated patients vs 10% placebo)
Headache (very common — 10.1% vs 7.4% placebo)
Dyspepsia, constipation, abdominal pain, flatulence, vomiting, diarrhoea (common)
Dry eyes and abnormal vision including abnormal accommodation (common)
Dizziness, somnolence, paraesthesia; nervousness; vertigo; palpitations (common)
Dysuria and urinary retention (uncommon); confusion, hallucinations, disorientation (uncommon)

Interactions

Potent CYP3A4 inhibitors (macrolides such as erythromycin and clarithromycin, azole antifungals such as ketoconazole and itraconazole, antiproteases) — concomitant systemic use is not recommended, due to increased serum tolterodine concentrations in poor CYP2D6 metabolisers and risk of overdosage
Other medicines with antimuscarinic properties — more pronounced therapeutic effect and side effects
Muscarinic cholinergic receptor agonists — may reduce the therapeutic effect of tolterodine
Prokinetics such as metoclopramide and cisapride — their effect may be decreased by tolterodine
Fluoxetine (potent CYP2D6 inhibitor) — no clinically significant interaction; no interactions shown with warfarin or combined oral contraceptives (ethinylestradiol/levonorgestrel)
Medicines known to prolong the QT interval, including Class IA (quinidine, procainamide) and Class III (amiodarone, sotalol) antiarrhythmics — use tolterodine with caution (SPC §4.4)

Clinical monograph

How it works

It is a competitive muscarinic receptor antagonist that reduces detrusor overactivity, with relative functional selectivity for the bladder over the salivary glands.

Prescribing in practice

Contraindicated in urinary retention, uncontrolled narrow-angle glaucoma, significant gastric outflow obstruction and myasthenia gravis.
Antimuscarinic effects add to those of other anticholinergic drugs and may impair cognition and precipitate falls in the elderly.
Reduce dose in significant renal or hepatic impairment and with potent CYP3A4 inhibitors; it can prolong the QT interval.

Monitoring

Assess symptom benefit, anticholinergic side effects and cumulative anticholinergic burden after several weeks of treatment.

Counselling the patient

Dry mouth, constipation and blurred vision are common; report difficulty passing urine.
Tell your prescriber about all other medicines, as anticholinergic effects can add up.

Evidence & guidelines

NICE recognises antimuscarinics including tolterodine as established pharmacological treatment for overactive bladder after conservative measures.

Reference: NICE NG123; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

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