Tolterodine

Tolterodine acts as a competitive antagonist of acetylcholine at postganglionic muscarinic receptors. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors.

• Tolterodine tartrate extended-release capsules are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency [see Clinical Studies (14) ] . Tolterodine tartrate extended-release capsules are an antimuscarinic indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.ICD-10: N32.81

• Tolterodine tartrate extended-release capsules are contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. Tolterodine tartrate extended-release capsules are also contraindicated in patients with known hypersensitivity to the drug or its ingredients, or to fesoterodine fumarate extended-release tablets which, like tolterodine tartrate extended-release capsules, are metabolized to 5-hydroxymethyl tolterodine [see Warnings and Precautions (5.2 , 5.3 , 5.4) ] .contraindicated

• 4 mg capsules taken orally once daily with water and swallowed whole. ( 2.1 ) • 2 mg capsules taken orally once daily with water and swallowed whole in the presence of: o mild to moderate hepatic impairment (Child-Pugh class A or B) ( 2.2 ) o severe renal impairment [Creatinine Clearance (CCr) 10-30 mL/min] ( 2.2 ) o drugs that are potent CYP3A4 inhibitors. ( 2.2 ) • Tolterodine tartrate extended-release capsules are not recommended for use in patients with CCr <10 mL/min. ( 2.2 ) • Tolterodine tartrate extended-release capsules are not recommended for use in patients with severe hepatic impairment (Child-Pugh Class C). ( 2.2 ) 2.1 Dosing Information The recommended dose of tolterodine tartrate extended-release capsules is 4 mg once daily with water and swallowed whole. The dose may be lowered to 2 mg daily based on individual response and tolerability; however, limited efficacy data are available for tolterodine tartrate extended-release capsules 2 mg [see Clinical Studies (14) ] . 2.2 Dosage Adjustment in Specific Populations For patients with mild to moderate hepatic impairment (Child-Pugh Class A or B) or severe renal impairment (CCr 10-30 mL/min), the recommended dose of tolterodine tartrate extended-release capsules is 2 mg once daily. Tolterodine tartrate extended-release capsules are not recommended for use in patients with severe hepatic impairment (Child-Pugh Class C).

• Anaphylaxis and angioedema requiring hospitalization and emergency medical treatment have occurred with the first or subsequent doses of tolterodine tartrate extended-release capsules. ( 5.1 ) • Urinary Retention: use caution in patients with clinically significant bladder outflow obstruction because of the risk of urinary retention. ( 5.2 ) • Gastrointestinal Disorders: use caution in patients with gastrointestinal obstructive disorders or decreased gastrointestinal motility because of the risk of gastric retention. ( 5.3 ) • Controlled Narrow-Angle Glaucoma: use caution in patients being treated for narrow-angle glaucoma. ( 5.4 ) • Central Nervous System Effects: Somnolence has been reported with tolterodine tartrate extended-release capsules. Advise patients not to drive or operate heavy machinery until they know how tolterodine tartrate extended-release capsules affect them ( 5.5 ). • Myasthenia Gravis: use caution in patients with myasthenia gravis. ( 5.8 ) • QT Prolongation: consider observations from the thorough QT study in clinical decisions to prescribe tolterodine tartrate extended-release capsules to patients with a known history of QT prolongation or to patients who are taking Class IA (e.g., quinidine, procainamide) or Class III (e.g., amiodarone, sotalol) antiarrhythmic medications. ( 5.9 ) 5.1 Angioedema Anaphylaxis and angioedema requiring hospitalization and emergency medical treatment have occurred with the first or subsequent doses of tolterodine tartrate extended-release capsules.

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The most common adverse reactions (incidence ≥4% and >placebo) were dry mouth, headache, constipation, and abdominal pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Viatris at 1-877-446-3679 (1-877-4-INFO-RX) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience The efficacy and safety of tolterodine tartrate extended-release capsules was evaluated in 1073 patients (537 assigned to tolterodine tartrate extended-release capsules; 536 assigned to placebo) who were treated with 2, 4, 6, or 8 mg/day for up to 15 months. These included a total of 1012 patients (505 randomized to tolterodine tartrate extended-release capsules 4 mg once daily and 507 randomized to placebo) enrolled in a randomized, placebo-controlled, double-blind, 12-week clinical efficacy and safety study. Adverse events were reported in 52% (n=263) of patients receiving tolterodine tartrate extended-release capsules and in 49% (n=247) of patients receiving placebo. The most common adverse events reported by patients receiving tolterodine tartrate extended-release capsules were dry mouth, headache, constipation, and abdominal pain.

• Renal Impairment: Tolterodine tartrate extended-release capsules are not recommended for use in patients with CCr <10 mL/min. Dose adjustment in severe renal impairment (CCr: 10-30 mL/min). ( 8.6 ) • Hepatic Impairment: Not recommended for use in severe hepatic impairment (Child Pugh Class C). Dose adjustment in mild to moderate hepatic impairment (Child Pugh Class A, B). ( 8.7 ) 8.1 Pregnancy Risk Summary There are no available data with tolterodine tartrate extended-release capsules use in pregnant women to inform drug-associated risks. In animal reproduction studies, oral administration of tolterodine and its 5-HMT metabolite to pregnant mice during organogenesis did not produce adverse developmental outcomes at doses approximately 9 to 12 times the clinical exposure at a dose of 20 mg/kg/day; however, higher doses produced adverse developmental outcomes (see Data ) . In the U.S. general population, the estimated background rate of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively.

Metabolism

Absorption In a study with 14 C-tolterodine solution in healthy volunteers who received a 5 mg oral dose, at least 77% of the radiolabeled dose was absorbed. C max and area under the concentration-time curve (AUC) determined after dosage of tolterodine immediate release are dose-proportional over the range of 1 to 4 mg.

Overdosage with tolterodine tartrate extended-release capsules can potentially result in severe central anticholinergic effects and should be treated accordingly. ECG monitoring is recommended in the event of overdosage. In dogs, changes in the QT interval (slight prolongation of 10% to 20%) were observed at a suprapharmacologic dose of 4.5 mg/kg, which is about 68 times higher than the recommended human dose. In clinical trials of normal volunteers and patients, QT interval prolongation was observed with tolterodine immediate release at doses up to 8 mg (4 mg bid) and higher doses were not evaluated [see Warnings and Precautions (5.9) and Clinical Pharmacology (12.2) ] . A 27-month-old child who ingested 5 to 7 tolterodine immediate release 2 mg tablets was treated with a suspension of activated charcoal and was hospitalized overnight with symptoms of dry mouth. The child fully recovered.

• Mar 25, 1998NDANDA020771Upjohn
• Dec 22, 2000NDANDA021228Upjohn
• Feb 23, 2015ANDAANDA077006Ivax Sub Teva Pharms
• Aug 11, 2015ANDAANDA203016Torrent
• Aug 31, 2015ANDAANDA203409Macleods Pharms Ltd
• Nov 22, 2016ANDAANDA079141Teva Pharms Usa
• Dec 12, 2017ANDAANDA206419Hetero Labs Ltd Iii
• Aug 19, 2019ANDAANDA204562Inventia Hlthcare

1. 1Drug Ineffective2,16811%
2. 2Fall1,1946.1%
3. 3Fatigue1,1525.9%
4. 4Dizziness9885.1%
5. 5Nausea9865.0%
6. 6Diarrhoea9154.7%
7. 7Headache8884.5%
8. 8Pain8104.1%
9. 9Dry Mouth7453.8%
10. 10Dyspnoea7363.8%
11. 11Asthenia7333.8%
12. 12Constipation7093.6%
13. 13Urinary Tract Infection7083.6%
14. 14Arthralgia6123.1%
15. 15Vomiting5762.9%

Recent PubMed references pinned to Tolterodine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Selective one-pot fluorescent probing technique for determination of tolterodine in dosage forms, content uniformity, and human plasma via coumarin synthesis.
  Talanta · 2026 · Oraby M, Badr El-Din KM, Derayea SM, et al.
  PMID 42102773DOI 10.1016/j.talanta.2026.129927
• Analysis of Major Impurities in Tolterodine Tartrate Tablets by 2D-UPLC-Q-TOF/MS.
  Rapid communications in mass spectrometry : RCM · 2026 · Pan F, Jin Z, Xu D, et al.
  PMID 42011887DOI 10.1002/rcm.70084
• Clinical outcomes and safety of duloxetine and tolterodine combination in the treatment of mixed-type urinary incontinence: A single-arm retrospective study.
  The Journal of international medical research · 2026 · Polat H, Ekşi M, Çatık A, et al.
  PMID 41852229DOI 10.1177/03000605261430142
• GLANCE-aided snapshotting for sustainable integration of synchronous spectrofluorimetry and micellar boosting for nanoscale assay of tolterodine binary mixtures in crucial matrices.
  Scientific reports · 2025 · Yosrey E, Elmansi H, Shalan S, et al.
  PMID 41345187DOI 10.1038/s41598-025-27144-0
• Response to anticholinergic therapy and its predictors in pediatric overactive bladder.
  European journal of pediatrics · 2025 · Canbaz FA
  PMID 41182445DOI 10.1007/s00431-025-06545-3
• Green HPLC-Fluorescence detection method for concurrent analysis of Tamsulosin hydrochloride and Tolterodine tartrate in dosage forms and biological fluids.
  Scientific reports · 2025 · Derayea SM, Badr El-Din KM, Ahmed AS, et al.
  PMID 40148346DOI 10.1038/s41598-025-92183-6
• Monotherapy with tolterodine or mirabegron is insufficient for ameliorating cyclophosphamide-induced bladder overactivity in rats.
  Autonomic neuroscience : basic & clinical · 2025 · Fjelltveit H, Carlsson T, Perez F, et al.
  PMID 39977963DOI 10.1016/j.autneu.2025.103253
• Tolterodine is a novel candidate for assessing CYP3A4 activity through metabolic volatiles to predict drug responses.
  Scientific reports · 2025 · Stock V, Hofer R, Lochmann F, et al.
  PMID 39828876DOI 10.1038/s41598-025-86450-9

The 10 most recently updated of 117 ClinicalTrials.gov registrations naming Tolterodine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Efficacy of Low-Intensity Shockwave Therapy in Treating Radiation Cystitis
  Completed · Early phase 1 · Interventional · 25 enrolled · Thanakrit Visuthikosol
  NCT07016451updated 2026-05-15
• A Multidisciplinary, Multimodal Bundled Care Approach to Chronic Pelvic Pain
  Terminated · Phase 3 · Interventional · 26 enrolled · Jocelyn Fitzgerald
  NCT05658874updated 2026-04-01
• TReating Incontinence for Underlying Mental and Physical Health
  Recruiting · Phase 4 · Interventional · 270 enrolled · University of California, San Francisco
  NCT05362292updated 2026-03-06
• Oxybutynin for Post-surgical Bladder Pain and Urgency
  Recruiting · Phase 3 · Interventional · 100 enrolled · University of California, Davis
  NCT03952299updated 2026-01-29
• Deprescribing dRrugs for Overactive Bladder in General Practice (DROP)
  Active not recruiting · Interventional · 72 enrolled · Anne Estrup Olesen
  NCT06110975updated 2025-12-02
• The Effect of Nighttime Mirabegron, Solifenacin, Tolterodine, or Oxybutynin on Nocturia, Sexual Function, Autonomic Function, and Lower Urinary Tract Blood Flow Perfusion in Women With Overactive Bladder Syndrome: Randomized Controlled Trial
  Not yet recruiting · Phase 3 · Interventional · 220 enrolled · Far Eastern Memorial Hospital
  NCT07114640updated 2025-08-11
• Treatment of Overactive Bladder With Anticholinergic Agents
  Active not recruiting · Observational · 120 enrolled · Sehit Prof. Dr. Ilhan Varank Sancaktepe Training and Research Hospital
  NCT07046156updated 2025-07-01
• Efficacy and Tolerability of DITROPAN XL (Oxybutynin Chloride) Versus DETROL LA (Tolterodine Tartrate) in Treatment of Overactive Bladder
  Completed · Phase 3 · Interventional · 790 enrolled · Alza Corporation, DE, USA
  NCT00293839updated 2025-02-03
• Study to Test the Long Term Safety and Efficacy of the Beta-3 Agonist Mirabegron (YM178) in Patients With Symptoms of Overactive Bladder
  Completed · Phase 3 · Interventional · 2,792 enrolled · Astellas Pharma Inc
  NCT00688688updated 2024-11-20
• Study to Assess the Efficacy and Safety of the Beta-3 Agonist Mirabegron (YM178) in Patients With Symptoms of Overactive Bladder
  Completed · Phase 3 · Interventional · 2,336 enrolled · Astellas Pharma Inc
  NCT00689104updated 2024-11-20

CPIC-curated drug–gene pairs for Tolterodine. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

• CYP2D6CPIC C (provisional)ClinPGx 3FDA label: Informative PGx

Frequently asked questions

How does Tolterodine work?

Tolterodine acts as a competitive antagonist of acetylcholine at postganglionic muscarinic receptors. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors.

What is Tolterodine used for?

According to FDA labeling, Tolterodine carries indications including: Tolterodine tartrate extended-release capsules are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency [see Clinical Studies (14) ] . Tolterodine tartrate extended-release capsules are an antimuscarinic indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tolterodine?

Tolterodine is classified as Drugs for urinary frequency and incontinence, Cholinergic Muscarinic Antagonist, Cholinergic Muscarinic Antagonists, Decreased Bladder Contractility.

What are the brand names for Tolterodine?

Tolterodine is marketed under brand names including Detrol.

What are the contraindications for Tolterodine?

Tolterodine labeling lists contraindications including: Tolterodine tartrate extended-release capsules are contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. Tolterodine tartrate extended-release capsules are also contraindicated in patients with known hypersensitivity to the drug or its ingredients, or to fesoterodine fumarate extended-release tablets which, like tolterodine tartrate extended-release capsules, are metabolized to 5-hydroxymethyl tolterodine [see Warnings and Precautions (5.2 , 5.3 , 5.4) ] .. Always consult the full prescribing information and a clinician.