Tolterodine

Muscarinic receptor antagonist for overactive bladder

ATC code: G04BD07

Brand names: Detrol LA, Detrol

Updated 24 Sep 2026 · Methodology

Indications

Overactive bladder

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.

Sources

ICD-10: N32.8 · ICD-11: GC50.0

Urge urinary incontinence

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.

Sources

ICD-10: N39.4 · ICD-11: MF50.21

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

Nocturnal enuresis in children

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.

Sources

ICD-10: F98.0 · ICD-11: 6C00.0

Frequent urination without prior evaluation

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.

Sources

ICD-10: R35 · ICD-11: MF50.0

How to read tiers A–F

AStrong evidence – first or second line in international guidelines
BRecommended in selected cases
CStudy data contradict each other
DBenefit not proven, no documented harm
FDocumented harm, or risk without benefit

Mechanism of action

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.

Safety

Contraindications

Hypersensitivity to tolterodine
Urinary retention
Gastric retention
Uncontrolled narrow-angle glaucoma
Myasthenia gravis
Severe ulcerative colitis and toxic megacolon

Serious adverse effects

QT prolongation (especially in CYP2D6 poor metabolisers)
Acute urinary retention
Angio-oedema
Cognitive impairment in older patients
Acute angle-closure glaucoma

Common adverse effects

Dry mouth (20–30%)
Constipation (5–7%)
Dry eyes
Headache
Somnolence
Dry skin

Pregnancy: can you take Tolterodine?

AEMPS summary of product characteristics (section 4.6): there are insufficient data on tolterodine use in pregnant women, animal studies have shown reproductive toxicity and the potential risk in humans is unknown. Tolterodine is therefore not recommended during pregnancy.

Breastfeeding: can you take Tolterodine?

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).

Calculate RID

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Label mentions35 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

MajorClarithromycin
«No se recomienda la administración sistémica concomitante con inhibidores potentes de CYP3A4, como antibióticos macrólidos (p. ej.: eritromicina y claritromicina), agentes antifúngicos (p. ej…»
AEMPS, section 4.5 · Open on CIMA
MajorClarithromycin
«Potent CYP3A4 Inhibitors: Ketoconazole (200 mg daily), a potent CYP3A4 inhibitor, increased the mean C max and AUC of tolterodine by 2- and 2.5-fold, respectively, in CYP2D6 poor metabolizers. For…»
FDA, section 7 · Open on DailyMed
MajorErythromycin
«No se recomienda la administración sistémica concomitante con inhibidores potentes de CYP3A4, como antibióticos macrólidos (p. ej.: eritromicina y claritromicina), agentes antifúngicos (p. ej…»
AEMPS, section 4.5 · Open on CIMA
MajorItraconazole
«No se recomienda la administración sistémica concomitante con inhibidores potentes de CYP3A4, como antibióticos macrólidos (p. ej.: eritromicina y claritromicina), agentes antifúngicos (p. ej…»
AEMPS, section 4.5 · Open on CIMA
MajorItraconazole
«Potent CYP3A4 Inhibitors: Ketoconazole (200 mg daily), a potent CYP3A4 inhibitor, increased the mean C max and AUC of tolterodine by 2- and 2.5-fold, respectively, in CYP2D6 poor metabolizers. For…»
FDA, section 7 · Open on DailyMed
MajorKetoconazole
«No se recomienda la administración sistémica concomitante con inhibidores potentes de CYP3A4, como antibióticos macrólidos (p. ej.: eritromicina y claritromicina), agentes antifúngicos (p. ej…»
AEMPS, section 4.5 · Open on CIMA
MajorKetoconazole
«Potent CYP3A4 Inhibitors: Ketoconazole (200 mg daily), a potent CYP3A4 inhibitor, increased the mean C max and AUC of tolterodine by 2- and 2.5-fold, respectively, in CYP2D6 poor metabolizers. For…»
FDA, section 7 · Open on DailyMed
Majormacrólidosclass named in the label
«No se recomienda la administración sistémica concomitante con inhibidores potentes de CYP3A4, como antibióticos macrólidos (p. ej.: eritromicina y claritromicina), agentes antifúngicos (p. ej…»
AEMPS, section 4.5 · Open on CIMA
MajorRitonavir
«Potent CYP3A4 Inhibitors: Ketoconazole (200 mg daily), a potent CYP3A4 inhibitor, increased the mean C max and AUC of tolterodine by 2- and 2.5-fold, respectively, in CYP2D6 poor metabolizers. For…»
FDA, section 7 · Open on DailyMed
ModerateCYP3A4 inhibitorsclass named in the label
«Potent CYP3A4 Inhibitors: Ketoconazole (200 mg daily), a potent CYP3A4 inhibitor, increased the mean C max and AUC of tolterodine by 2- and 2.5-fold, respectively, in CYP2D6 poor metabolizers. For…»
FDA, section 7 · Open on DailyMed
Moderateinhibidores del CYP3A4class named in the label
«No se recomienda la administración sistémica concomitante con inhibidores potentes de CYP3A4, como antibióticos macrólidos (p. ej.: eritromicina y claritromicina), agentes antifúngicos (p. ej…»
AEMPS, section 4.5 · Open on CIMA
anticonceptivos hormonalesclass named in the label
«Los estudios de interacción farmacológica no han mostrado interacciones con la warfarina ni con anticonceptivos orales combinados (etinilestradiol/levonorgestrel).»
AEMPS, section 4.5 · Open on CIMA
Caffeine
«Other Drugs Metabolized by Cytochrome P450 Isoenzymes: In vivo drug-interaction data show that tolterodine immediate release does not result in clinically relevant inhibition of CYP1A2, 2D6, 2C9…»
FDA, section 7 · Open on DailyMed
Cisapride
«El efecto de procinéticos como metoclopramida y cisaprida puede verse disminuido por la tolterodina.»
AEMPS, section 4.5 · Open on CIMA
CYP2D6 inhibitorsclass named in the label
«Potent CYP2D6 Inhibitors: Fluoxetine, a potent inhibitor of CYP2D6 activity, significantly inhibited the metabolism of tolterodine immediate release in CYP2D6 extensive metabolizers, resulting in a…»
FDA, section 7 · Open on DailyMed
diureticsclass named in the label
«Other Interactions: No clinically relevant interactions have been observed when tolterodine was co-administered with warfarin, with a combined oral contraceptive drug containing ethinyl estradiol and…»
FDA, section 7 · Open on DailyMed
Estradiol
«Other Interactions: No clinically relevant interactions have been observed when tolterodine was co-administered with warfarin, with a combined oral contraceptive drug containing ethinyl estradiol and…»
FDA, section 7 · Open on DailyMed
Ethinylestradiol
«Los estudios de interacción farmacológica no han mostrado interacciones con la warfarina ni con anticonceptivos orales combinados (etinilestradiol/levonorgestrel).»
AEMPS, section 4.5 · Open on CIMA
Fluoxetine
«El tratamiento concomitante con fluoxetina (un potente inhibidor de CYP2D6) no produce una interacción clínicamente significativa, ya que tolterodina y su metabolito dependiente de CYP2D6…»
AEMPS, section 4.5 · Open on CIMA
Fluoxetine
«Potent CYP2D6 Inhibitors: Fluoxetine, a potent inhibitor of CYP2D6 activity, significantly inhibited the metabolism of tolterodine immediate release in CYP2D6 extensive metabolizers, resulting in a…»
FDA, section 7 · Open on DailyMed
hormonal contraceptivesclass named in the label
«Other Interactions: No clinically relevant interactions have been observed when tolterodine was co-administered with warfarin, with a combined oral contraceptive drug containing ethinyl estradiol and…»
FDA, section 7 · Open on DailyMed
Levonorgestrel
«Los estudios de interacción farmacológica no han mostrado interacciones con la warfarina ni con anticonceptivos orales combinados (etinilestradiol/levonorgestrel).»
AEMPS, section 4.5 · Open on CIMA
Levonorgestrel
«Other Interactions: No clinically relevant interactions have been observed when tolterodine was co-administered with warfarin, with a combined oral contraceptive drug containing ethinyl estradiol and…»
FDA, section 7 · Open on DailyMed
Metoclopramide
«El efecto de procinéticos como metoclopramida y cisaprida puede verse disminuido por la tolterodina.»
AEMPS, section 4.5 · Open on CIMA
Omeprazole
«Other Drugs Metabolized by Cytochrome P450 Isoenzymes: In vivo drug-interaction data show that tolterodine immediate release does not result in clinically relevant inhibition of CYP1A2, 2D6, 2C9…»
FDA, section 7 · Open on DailyMed
Warfarin
«Los estudios de interacción farmacológica no han mostrado interacciones con la warfarina ni con anticonceptivos orales combinados (etinilestradiol/levonorgestrel).»
AEMPS, section 4.5 · Open on CIMA
Warfarin
«Other Interactions: No clinically relevant interactions have been observed when tolterodine was co-administered with warfarin, with a combined oral contraceptive drug containing ethinyl estradiol and…»
FDA, section 7 · Open on DailyMed

From other drugs’ labels

ModerateClarithromycin
«DRUG INTERACTIONS: Tolterodine (patients deficient in CYP2D6 activity) Use With Caution Tolterodine: The primary route of metabolism for tolterodine is via CYP2D6. However, in a subset of the…»
FDA, section 7 · Open on DailyMed
ModerateDuloxetine
«Medicamentos metabolizados por el CYP2D6 : Duloxetina es un inhibidor moderado del CYP2D6. Cuando se administró duloxetina a una dosis de 60 mg dos veces al día con una dosis única de desipramina, un…»
AEMPS, section 4.5 · Open on CIMA
ModerateRivastigmine
«Teniendo en cuenta sus efectos farmacodinámicos y los posibles efectos acumulativos, la rivastigmina no debe administrarse junto con otras sustancias colinomiméticas. Rivastigmina podría interferir…»
AEMPS, section 4.5 · Open on CIMA
Clarithromycin
«Tolterodina: La vía principal para el metabolismo de tolterodina es a través de la isoforma 2D6 del citocromo P450 (CYP2D6). Sin embargo, en un subconjunto de población carente de CYP2D6 la ruta…»
AEMPS, section 4.5 · Open on CIMA
Fesoterodine
«CYP3A4 Inhibitors: In a study in adults, coadministration of the strong CYP3A4 inhibitor ketoconazole with fesoterodine led to approximately a doubling of the maximum concentration (C max ) and area…»
FDA, section 7 · Open on DailyMed
Itraconazole
«Urológicos: hidroximetil-tolterodina.»
AEMPS, section 4.5 · Open on CIMA
Paroxetine
«DRUG INTERACTIONS: Examples propafenone, flecainide, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivolol, perphenazine, tolterodine, venlafaxine, risperidone.»
FDA, section 7 · Open on DailyMed
Sertraline
«Clinically Significant Drug Interactions: Examples: propafenone, flecainide, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivolol, perphenazine, thioridazine, tolterodine, venlafaxine»
FDA, section 7 · Open on DailyMed

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Frequently asked

What is Tolterodine used for?

Tolterodine is evaluated for the following indications with varying evidence strength: Urge urinary incontinence (evidence tier B), Overactive bladder (evidence tier B), Nocturnal enuresis in children (evidence tier D). See the full indication matrix with dosing and citations above on this page.

What are the side effects of Tolterodine?

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.

Is Tolterodine safe during pregnancy?

Is Tolterodine compatible with breastfeeding?

Who should not take Tolterodine?

Tolterodine is contraindicated in: Hypersensitivity to tolterodine; Urinary retention; Gastric retention; Uncontrolled narrow-angle glaucoma; Myasthenia gravis. Full list in the Safety section.

Official sources

Direct links to regulator labels. Open in a new tab.

AEMPS / CIMALabel dated 09/28/2022
FDA / DailyMedLabel dated 02/09/2026

Other drugs in this group

Trospium, Vardenafil, Dutasteride, Dutasteride + Tamsulosin, Finasteride, Pumpkin seed extract, Silodosin, Fesoterodine