Tolterodine
DETROL
What it isMuscarinic antagonist; overactive bladder.
Why this oneIts extended-release capsule causes less dry mouth than the immediate-release tablet, making formulation choice its practical edge.
What limits itAnticholinergic burden persists, so caution in the elderly. CYP2D6 substrate with CYP3A4 backup; QT prolongation.
FDA-approved for
- overactive bladder (1998)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Overactive bladder | Adult | 4 mg QD | 4 mg QD | 4 mg QD |
| Overactive bladder | Hepatic (Child-Pugh A/B), severe renal (CrCl 10-30), or potent CYP3A4 inhibitors | 2 mg QD | 2 mg QD | 2 mg QD |
Renal 2 mg QD if CrCl 10-30 mL/min; not recommended if CrCl <10
Hepatic 2 mg QD in Child-Pugh A/B; not recommended in Child-Pugh C
Instructions
- Swallow whole with water.
- Reduce to 2 mg QD with potent CYP3A4 inhibitors.
Contraindications
- Urinary retention
- Gastric retention
- Uncontrolled narrow-angle glaucoma
Cautions
- Angioedema/anaphylaxis
- Urinary retention (bladder outflow obstruction)
- Gastric retention (GI obstructive disorders/decreased motility)
- Controlled narrow-angle glaucoma
- CNS effects/somnolence
- Myasthenia gravis
- QT prolongation
Adverse reactions
- Dry mouth
- Headache
- Constipation
- Abdominal pain
Pregnancy No human data; animal developmental toxicity at high exposures
Lactation No human data; excreted in mouse milk in low amounts
NO BOXED WARNINGS
Principal riskAnticholinergic burden
Cost, est. cash$5–$150/month
Generic entry2012
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Tolterodine ballicule
Open Tolterodine in the interactive console ↗
Memory aids: mascots and interaction avatars
treatment for overactive bladder (OAB)
“red as a beet” → anticholinergic
