Tolterodine

Brand Names: DETROL LA, Detrusitol

Drug Class: Antimuscarinic agent / Urinary antispasmodic

Overview

Tolterodine is an antimuscarinic agent used to treat overactive bladder symptoms including urge urinary incontinence, urgency, and frequency. It works by relaxing bladder smooth muscle through competitive muscarinic receptor antagonism. The extended-release formulation (DETROL LA) provides once-daily dosing for improved convenience.

Mechanism of Action

Tolterodine is a competitive muscarinic receptor antagonist that exerts direct antispasmodic effects on bladder smooth muscle. It selectively targets muscarinic receptors in the urinary bladder, reducing involuntary detrusor contractions and increasing bladder capacity without significantly affecting salivary flow at therapeutic doses.

Indications

  • Treatment of overactive bladder with symptoms of urge urinary incontinence
  • Management of urinary urgency
  • Reduction of urinary frequency

Common Doses

  • 2 mg extended-release capsules
  • 4 mg extended-release capsules

Dosage

The recommended dose for DETROL LA is 4 mg once daily. The dose may be lowered to 2 mg once daily based on individual response and tolerability. Should be taken with water and swallowed whole; do not crush, chew, or divide capsules.

Contraindications

  • Urinary retention
  • Gastric retention
  • Uncontrolled narrow-angle glaucoma
  • Known hypersensitivity to tolterodine or its ingredients
  • Hypersensitivity to fesoterodine fumarate extended-release tablets

Side Effects

  • Dry mouth
  • Constipation
  • Headache
  • Dyspepsia
  • Abdominal pain
  • Blurred vision
  • Dizziness
  • Urinary tract infection
  • Dry eyes
  • Somnolence

Interactions

  • Strong CYP3A4 inhibitors (ketoconazole, clarithromycin) increase tolterodine exposure; maximum dose should be 2 mg daily when co-administered
  • Other anticholinergic drugs may increase frequency and severity of side effects
  • Drugs that prolong QT interval may have additive effects

Counseling Points

  • Take once daily with water; swallow capsule whole
  • May cause dry mouth; maintain good oral hygiene and consider sugar-free gum/candy
  • Avoid driving or operating machinery if experiencing dizziness or blurred vision
  • Report symptoms of urinary retention or severe constipation
  • Stay hydrated in hot weather as medication may decrease sweating
  • Inform healthcare provider of all medications being taken