Tolterodine

Pronunciation: tol-TER-oh-deen.

Generic name
tolterodine tartrate
Brand names
Detrol / Detrol LA (United States), Detrusitol / Detrusitol XL (United Kingdom, European Union, Canada, Australia, New Zealand)
Drug class
Muscarinic-receptor antagonist (antimuscarinic/anticholinergic), used for overactive bladder
Form
Immediate-release tablet (1 mg, 2 mg) or extended-release/prolonged-release capsule (2 mg, 4 mg), depending on brand and market
Route
Oral
Legal status
Prescription-only in all markets reviewed.

Availability and supply rules vary by country

Trade names by country: United States · United Kingdom · Canada · Australia · New Zealand

Australia: Detrusitol (5) · Full directory

What tolterodine tartrate is and how it works

Tolterodine is a prescription medicine that blocks muscarinic receptors in the bladder, helping to calm an overactive bladder muscle. (1) (2)

It is used for overactive bladder symptoms -- urgency, frequent urination, and urge incontinence (leaking urine after a sudden strong urge). Tolterodine does not carry a formal FDA boxed warning, but it does require a genuine reduced dose (usually 2 mg daily instead of 4 mg) if you have significant kidney or liver impairment, or if you take certain other medicines (potent CYP3A4 inhibitors) -- always take exactly the dose your prescriber recommends.

Mechanism of action: how tolterodine tartrate works

Tolterodine is a competitive muscarinic-receptor antagonist with functional selectivity for the bladder over salivary glands in vivo, despite similar in vitro receptor affinity; this reduces detrusor muscle overactivity and is metabolised (in extensive metabolisers) to an active 5-hydroxymethyl metabolite with a similar pharmacological profile. (1) (2)

What tolterodine tartrate is used for

Overactive bladder

Treats the symptoms of overactive bladder: urinary urgency, increased urinary frequency, and urge urinary incontinence (leaking urine after a sudden, strong need to urinate). (1) (2)

Before taking tolterodine tartrate

Do not take / not appropriate for

  • Do not take tolterodine if you have urinary retention (difficulty emptying your bladder) or gastric retention (difficulty emptying your stomach). (all countries) (1) (2)
  • Do not take tolterodine if you have uncontrolled narrow-angle glaucoma. (all countries) (1) (2)
  • Do not take tolterodine if you have myasthenia gravis, severe ulcerative colitis, or toxic megacolon. (United Kingdom, European Union) (2)
  • Do not take tolterodine if you have a known allergy to tolterodine or any ingredient in the product. (all countries) (1) (2)

Tell your clinician about

  • Any kidney or liver problems -- your dose is usually lower (2 mg daily) if you have significant kidney or liver impairment.
  • All other medicines you take, especially azole antifungals, certain antibiotics (like clarithromycin), and other potent CYP3A4-inhibiting medicines, since these usually require the same lower 2 mg daily dose.
  • Any bladder outlet obstruction, gastrointestinal obstructive disorder, autonomic neuropathy, or hiatus hernia.
  • Any personal or family history of heart rhythm problems, especially QT prolongation.
  • Pregnancy, plans for pregnancy, or breastfeeding.
(1) (2)

How to take tolterodine tartrate

  • Take tolterodine exactly as your prescriber directs -- do not take more or less, and do not change your dose yourself.
  • Extended-release/prolonged-release capsules are swallowed whole with water, with or without food -- do not chew, divide, or crush them.
  • Your prescriber will usually check your response after 2 to 3 months of treatment.
  • Avoid becoming overheated or dehydrated, since tolterodine can reduce sweating and increase the risk of heat-related illness in hot conditions.
(1) (2)

Procedures and treatment changes

Tell the treating team before surgery, procedures, or any medicine change. Do not alter treatment without the responsible clinician. (1) (2) (3) (4) (5) (6)

Missed dose

If you miss a dose, contact your pharmacist or prescriber for guidance, or take the next dose at your usual time -- do not take a double dose to make up for the one you missed.

Overdose

Seek urgent medical attention or contact a poison control centre if you think you or someone else has taken too much tolterodine, especially with symptoms such as severe dry mouth, blurred vision, confusion, a fast heartbeat, difficulty urinating, or seizures. (1) (2)

Side effects

Side effects and their urgency vary; report severe, persistent, or concerning symptoms.

Dry mouth -- the most common side effect.

What to notice: Dry mouth -- the most common side effect.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)

Headache and dizziness.

What to notice: Headache and dizziness.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)

Constipation, dyspepsia (indigestion), and abdominal discomfort.

What to notice: Constipation, dyspepsia (indigestion), and abdominal discomfort.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)

Dry eyes and blurred or abnormal vision.

What to notice: Dry eyes and blurred or abnormal vision.

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (1) (2)

Drowsiness (somnolence).

What to notice: Drowsiness (somnolence).

What to do: Discuss persistent or troublesome symptoms with the treating clinician or pharmacist. (2)

Serious warnings

Angioedema (swelling of the face, lips, tongue, or throat) — emergency

Symptoms: Swelling of the face, lips, tongue, and/or throat, sometimes with difficulty breathing.

Action: Seek emergency medical help immediately -- this is a rare but genuine reaction that has been reported with tolterodine; your care team will decide whether tolterodine can be continued afterward. (1) (2)

Inability to urinate (urinary retention) — high caution

Symptoms: Increasing difficulty passing urine, or being unable to urinate at all, especially if you have an enlarged prostate or other bladder outlet obstruction.

Action: Contact your prescriber promptly, or seek urgent care if you cannot urinate at all -- this may need immediate assessment and treatment. (1) (2)

Heart rhythm changes (QT prolongation) — high caution

Symptoms: A fast, irregular, or pounding heartbeat, or fainting.

Action: Contact your prescriber promptly, especially if you have a personal or family history of heart rhythm problems or take other medicines that affect heart rhythm. (1) (2)

Heat-related illness — high caution

Symptoms: Feeling excessively hot, confusion, or fainting, particularly in hot weather or with strenuous activity.

Action: Tolterodine can reduce sweating; move to a cool place, rehydrate, and seek medical help if symptoms are severe -- take extra care in hot conditions. (1)

Interactions

  • Potent CYP3A4 inhibitor medicines (such as certain antifungals like ketoconazole, and antibiotics like clarithromycin) increase tolterodine levels; UK labelling advises avoiding this combination altogether, while US labelling requires a reduced 2 mg daily dose if combined. (1) (2)
  • Other antimuscarinic/anticholinergic medicines can increase tolterodine's effects (such as dry mouth, constipation, and blurred vision). (2)
  • Muscarinic agonists and prokinetic medicines (such as metoclopramide) may have reduced effectiveness when combined with tolterodine, or may reduce tolterodine's own effect. (2)
  • Fluoxetine, warfarin, and oral contraceptives showed no clinically significant interaction with tolterodine in the sources reviewed. (2)

Pregnancy, breastfeeding, kidney/liver function, age

Pregnancy

Tolterodine is not recommended during pregnancy, based on animal studies showing reproductive toxicity and a lack of adequate human data; discuss family planning with your prescriber before starting. (1) (2) (3) (4) (5) (6)

Breastfeeding

Tolterodine should be avoided during breastfeeding, since there is not enough data on whether it passes into breast milk. (1) (2) (3) (4) (5) (6)

Children

Safety and effectiveness have not been established in children in the sources reviewed for this dossier; it is not an approved use in children. (1) (2) (3) (4) (5) (6)

Elderly

No dose adjustment is required based on age alone, but older adults may be more sensitive to anticholinergic side effects such as confusion, dry mouth, and constipation. (1) (2) (3) (4) (5) (6)

Hepatic_impairment

Moderate or worse liver impairment requires the lower 2 mg daily dose; severe (Child-Pugh C) hepatic impairment is not recommended for use per the reviewed US label. (1) (2) (3) (4) (5) (6)

Renal_impairment

Significantly reduced kidney function (creatinine clearance/GFR of 30 mL/min or less) requires the lower 2 mg daily dose. (1) (2) (3) (4) (5) (6)

Monitoring

Before starting

  • Kidney and liver function
  • Review of other medicines for CYP3A4 interactions
  • Screening for urinary/gastric retention, glaucoma, and bladder outlet obstruction

During treatment

  • Reassessment of symptom response, typically after 2 to 3 months of treatment.
  • Watch for signs of angioedema, worsening urinary retention, or heart rhythm changes and seek prompt medical attention if they occur.
(1) (2)

Storage

Store at controlled room temperature (around 25degC/77degF, with excursions permitted between 15-30degC/59-86degF in the US label), away from excess heat and moisture, and out of reach of children.

Professional information

Clinician-facing context only, sourced from the current US FDA DETROL LA prescribing information and current UK emc Detrusitol XL SmPC; verify against the current full local label before prescribing.

United States / United Kingdom

Indication: Overactive bladder

Dose summary: Standard: 4 mg once daily (extended-release). Reduced to 2 mg once daily for significantly reduced renal function (CrCl/GFR <=30 mL/min), moderate-or-worse hepatic impairment, concomitant potent CYP3A4 inhibitors, or intolerance of the standard dose. UK labelling recommends avoiding potent CYP3A4 inhibitors altogether rather than dose-reducing.

Renal context: CrCl/GFR <=30 mL/min: reduce to 2 mg once daily. (1) (2)

Mechanism of action

Hepatic guidance

Moderate hepatic impairment requires the reduced 2 mg daily dose; severe (Child-Pugh C) hepatic impairment is not recommended per the reviewed US label.

Overdose note

Overdose can cause severe anticholinergic effects (central and peripheral); manage with gastric lavage/activated charcoal where appropriate, physostigmine for severe central anticholinergic effects, benzodiazepines for convulsions, artificial respiration for respiratory insufficiency, beta-blockers for tachycardia, catheterisation for urinary retention, and pilocarpine eye drops for mydriasis. (1) (2)

Frequently asked questions

Does tolterodine have a boxed warning?

No -- tolterodine's current US DETROL LA label does not carry a formal FDA boxed warning. It still requires care: a reduced 2 mg daily dose is needed for significant kidney or liver impairment or with certain interacting medicines, and it carries warnings for angioedema, urinary retention, and heart rhythm (QT) effects. (1)

Is tolterodine available in the US, UK, Europe, Canada, Australia, and New Zealand?

Yes. It is authorised in all of these regions, sold as Detrol/Detrol LA in the United States and as Detrusitol/Detrusitol XL in the United Kingdom, European Union, Canada, Australia, and New Zealand. (1) (2) (3) (4) (5) (6)

Why might my dose be 2 mg instead of 4 mg?

A lower 2 mg daily dose is used if you have significantly reduced kidney function, moderate or worse liver impairment, if you take certain medicines that increase tolterodine levels (potent CYP3A4 inhibitors), or if the standard dose causes side effects you cannot tolerate. Your prescriber decides the right dose for you. (1) (2)

What is the mechanism of action of tolterodine tartrate?

Tolterodine is a competitive muscarinic-receptor antagonist with functional selectivity for the bladder over salivary glands in vivo, despite similar in vitro receptor affinity; this reduces detrusor muscle overactivity and is metabolised (in extensive metabolisers) to an active 5-hydroxymethyl metabolite with a similar pharmacological profile. (1) (2)

What is the generic name of Tolterodine?

The generic name is tolterodine tartrate. It is sold under brand names including Detrol / Detrol LA (United States), Detrusitol / Detrusitol XL (United Kingdom, European Union, Canada, Australia, New Zealand). (1) (2)

What class of drug is tolterodine tartrate?

Tolterodine is classed as: Muscarinic-receptor antagonist (antimuscarinic/anticholinergic), used for overactive bladder. (1) (2)

References

  1. DETROL LA (tolterodine tartrate extended-release capsules) -- full prescribing informationU.S. Food and Drug Administration / DailyMed (NIH), full prescribing information · United States · accessed 2026-07-30 · source 1
  2. Detrusitol XL 4mg prolonged-release capsules, hard -- Summary of Product Characteristicselectronic medicines compendium (emc), United Kingdom -- Viatris Products Limited · United Kingdom · accessed 2026-07-30 · source 2
  3. Tolterodine -- list of nationally authorised medicinal products (PSUSA/00002993/202109)European Medicines Agency (EMA) -- list of nationally authorised medicinal products (PSUSA procedure) · European Union · accessed 2026-07-30 · source 3
  4. DETROL and DETROL LA (tolterodine L-tartrate) -- Product MonographsHealth Canada product monograph, Viatris / BGP Pharma ULC · Canada · accessed 2026-07-30 · source 4
  5. DETRUSITOL tolterodine tartrate 1 mg / 2 mg tablet blister pack -- ARTG entries 99393 / 99394Therapeutic Goods Administration (TGA), Australia · Australia · accessed 2026-07-30 · source 5
  6. DETRUSITOL 1 mg, 2 mg film-coated tablet -- New Zealand Data SheetMedsafe (New Zealand regulator) · New Zealand · accessed 2026-07-30 · source 6

Brand names by country

Single-ingredient tolterodine tartrate names are shown separately by country. Product availability, strengths, and supply rules can change; combination products are not included here.

Priority countries

United States

  • Detrol1 mg, 2 mg · viatris specialty llc

United Kingdom

  • Detrusitol (2)MHRA licensed emc smpc confirmed · 1 mg, 2 mg · Viatris Products Limited
  • Detrusitol XL (2)MHRA licensed emc smpc confirmed · 4 mg · Viatris Products Limited

Canada

  • DETROL
  • DETROL LA
  • MYLAN-TOLTERODINE ER
  • TEVA-TOLTERODINE LA
  • SANDOZ TOLTERODINE LA

Australia

  • Detrusitol (5)TGA ARTG registered 2004-12-15 · 1 mg, 2 mg · Viatris Pty Ltd

New Zealand

  • Detrusitol (6)Medsafe data sheet located · 1 mg, 2 mg · not independently confirmed beyond data-sheet existence in this pass
View brands in additional countries.

European Union

Detrusitol / Detrusitol XL (3)

This page provides general reference information about tolterodine and is not a substitute for advice from the prescriber managing your treatment. All dosing and treatment decisions should be made with your prescriber.

Related medicines

Related conditions