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tolterodine (tol-ter-oh-deen)

Detrol, Detrol LA


Therapeutic: urinary tract antispasmodics

Pharmacologic: anticholinergics


Treatment of overactive bladder function that results in urinary frequency, urgency, or urge incontinence.


Acts as a competitive muscarinic receptor antagonist resulting in inhibition of cholinergically mediated bladder contraction. Therapeutic Effects: ↓ urinary frequency, urgency, and urge incontinence.

Adverse Reactions/Side Effects

CNS: headache, dizziness. EENT: blurred vision, dry eyes. GI: dry mouth, constipation, dyspepsia.


Examination and Evaluation

  • Assess dizziness that might affect gait, balance, and other functional activities (See Appendix C). Report balance problems and functional limitations to the physician, and caution the patient and family/caregivers to guard against falls and trauma.

  • Monitor signs of urine retention (difficult urination, painful or distended abdomen). Excessive urinary retention may require dose adjustment by physician.


  • When appropriate, implement pelvic floor muscle strengthening activities and other therapeutic exercises to help maintain bladder control.

Patient/Client-Related Instruction

  • Advise patient to increase fluid intake and dietary fiber to avoid constipation. Laxatives may also be helpful in patients susceptible to fecal impaction.

  • Instruct patient and family/caregivers to report other troublesome side effects such as severe or prolonged headache, blurred vision, dry eyes, or GI problems (dry mouth, indigestion).


Absorption: Well absorbed (77%) following oral administration.

Distribution: Unknown.

Protein Binding: 96.3%.

Metabolism and Excretion: Extensively metabolized by the liver; 1 metabolite (5-hydroxymethyltolterodine) is active; other metabolites are excreted in urine.

Half-life: Tolterodine—1.9–3.7 hr;

5-hydroxymethyltolterodine—2.9–3.1 hr.

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TIME/ACTION PROFILE (effects on bladder function)

PO unknown unknown 12 hr


Contraindicated in: Urinary retention; Gastric retention; Uncontrolled angle-closure glaucoma; Lactation.

Use Cautiously in: GI obstructive disorders, including pyloric stenosis (increased risk of gastric retention); Significant bladder outflow obstruction (↑ risk of urinary retention); Controlled angle-closure glaucoma; Significant hepatic impairment (lower doses recommended); Impaired renal function; Pregnancy (safe use not established; use only if potential maternal benefit justifies potential risk to fetus); Children (safety not established).


Drug-Drug: Erythromycin, clarithromycin, ketoconazole, itraconazole, and miconazole may inhibit metabolism and ↑ effects of tolterodine.


PO (Adults): 2 mg bid as tablets; may be lowered depending on response or 2–4 mg once daily as extended-release capsules.

PO (Adults with Impaired Hepatic Function or Concurrent Enzyme Inhibitors):...

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