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[Pharmacology](https://durgical.com/en/pharmacology/) · [Overactive bladder agents](https://durgical.com/en/pharmacology/classes/overactive-bladder-agents/)

# Tolterodine

An antimuscarinic for overactive bladder whose active metabolite is made by CYP2D6, so genetics and interacting drugs change its levels.

Updated 2026-11-01

- Class: [Overactive bladder agents](https://durgical.com/en/pharmacology/classes/overactive-bladder-agents/)
- Receptor: Muscarinic receptors of the bladder (M3)
- ATC code: G04BD07

◎**Muscarinic receptors of the bladder (M3)**Tolterodine

ⓘ No structure of tolterodine bound to its receptor exists. The figure shows tiotropium, another muscarinic antagonist, in the acetylcholine pocket of the rat M3 receptor, the subtype that contracts the bladder; the pocket is nearly identical in the human receptor.

**Target in 3D:** Muscarinic receptors of the bladder (M3). PDB structure 4DAJ (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/4DAJ) · Drag to rotate · pinch to zoom

## Mechanism of action

Tolterodine is a competitive antagonist of acetylcholine at muscarinic receptors. In the liver, CYP2D6 turns it into 5-hydroxymethyl tolterodine (5-HMT), which is just as active. Bladder contraction and salivation are both muscarinic, but in studies it showed some selectivity for the bladder over the salivary glands.

- CYP2D6 converts it to an equally active metabolite
- Both block muscarinic receptors of the detrusor
- Urgent contractions decrease

## Pharmacokinetics

**Metabolism**
Liver CYP2D6 forms the active 5-HMT; in poor metabolizers CYP3A4 takes over and tolterodine itself rises

**Elimination**
Clearance is much lower in cirrhosis and altered in severe kidney disease, so lower doses are used

## Indications

- Overactive bladder with urge incontinence, urgency and frequency [Overactive bladder and urge incontinence →](https://durgical.com/en/conditions/overactive-bladder-and-urge-incontinence/)

## Adverse effects

### Common

- Dry mouth (the most common reason to stop)
- Headache
- Constipation
- Abdominal pain
- Dizziness and drowsiness

### Serious (rare, important)

- Anaphylaxis and angioedema
- Urinary retention with outlet obstruction
- QT prolongation, more in CYP2D6 poor metabolizers

## Contraindications

- Urinary retention
- Gastric retention
- Uncontrolled narrow-angle glaucoma
- Hypersensitivity to tolterodine or fesoterodine

## Key interactions

**Fluoxetine and other strong CYP2D6 inhibitors**
Tolterodine levels rose about fivefold with fluoxetine

**Strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin, ritonavir)**
Higher levels; a lower dose is used

**Other anticholinergic drugs**
More dry mouth, constipation, blurred vision and drowsiness

## What is monitored

- Liver and kidney function before choosing the dose
- Mental status and drowsiness
- ECG if there is QT risk

## Administration and safety

- Extended-release capsules are swallowed whole

## Nursing care

- Review other medicines for CYP2D6 and CYP3A4 inhibitors
- Warn about driving if dizzy or drowsy
- Use caution in myasthenia gravis

## Pregnancy and breastfeeding

No human data in pregnancy; animal studies at usual exposures did not show harm.

## Memory aid

TOLTERodine is «TOLD» by CYP2D6 what to become: its active metabolite.

## Test yourself

Think of the answer, then tap the question to see it.

## Which enzyme forms tolterodine's active metabolite?

CYP2D6, which makes 5-hydroxymethyl tolterodine.

## Why do CYP2D6 poor metabolizers need attention with tolterodine?

Tolterodine itself accumulates and the QT effect is more pronounced.

## Hypersensitivity to which related drug is also a contraindication?

Fesoterodine, which is converted to the same active metabolite.

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## Related drugs

- [Oxybutynin](https://durgical.com/en/pharmacology/oxybutynin/)
- [Solifenacin](https://durgical.com/en/pharmacology/solifenacin/)
- [Mirabegron](https://durgical.com/en/pharmacology/mirabegron/)

## Related conditions

- [Overactive bladder and urge incontinence](https://durgical.com/en/conditions/overactive-bladder-and-urge-incontinence/)

[← Back to the class: Overactive bladder agents](https://durgical.com/en/pharmacology/classes/overactive-bladder-agents/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [DailyMed - TOLTERODINE TARTRATE- tolterodine capsule, extended release](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=db6e0b6d-0ce5-41d7-881f-881c11f530a4) (DailyMed (U.S. National Library of Medicine), 2026); [Tolterodine: MedlinePlus Drug Information](https://medlineplus.gov/druginfo/meds/a699026.html) (MedlinePlus (U.S. National Library of Medicine), 2026); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 11 (McGraw Hill, 2023).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/tolterodine/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/tolterodine/