No

Anticholinergic Agent

Treatment of patients with an overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence

C

Urinary retention or gastric retention; uncontrolled narrow-angle glaucoma; demonstrated hypersensitivity to tolterodine or ingredients

Caution in patients with bladder flow obstruction, pyloric stenosis or other GI obstruction, narrow-angle glaucoma (controlled), reduced hepatic/renal function

>10%: Central nervous system: Headache

1% to 10%:

Cardiovascular: Chest pain, hypertension (1.5%)

Central nervous system: Vertigo (8.6%), nervousness (1.1%), somnolence (3.0%)

Dermatologic: Pruritus (1.3%), rash (1.9%), dry skin (1.7%)

Gastrointestinal: Abdominal pain (7.6%), constipation (6.5%), diarrhea (4.0%), dyspepsia (5.9%), flatulence (1.3%), nausea (4.2%), vomiting (1.7%), weight gain (1.5%)

Genitourinary: Dysuria (2.5%), polyuria (1.1%), urinary retention (1.7%), urinary tract infection (5.5%)

Neuromuscular & skeletal: Back pain, falling (1.3%), paresthesia (1.1%)

Ocular: Vision abnormalities (4.7%), dry eyes (3.8%)

Respiratory: Bronchitis (2.1%), cough (2.1%), pharyngitis (1.5%), rhinitis (1.1%), sinusitis (1.1%), upper respiratory infection (5.9%)

Miscellaneous: Flu-like symptoms (4.4%), infection (2.1%)

Overdosage with tolterodine can potentially result in severe central anticholinergic effects and should be treated accordingly. EKG monitoring is recommended in the event of overdosage.

CYP3A3/4 substrate; CYP2D6 substrate

Fluoxetine, which inhibits cytochrome P-450 2D6, increases concentration 4.8 times. Other drugs which inhibit this isoenzyme may also interact. Studies with inhibitors of cytochrome isoenzyme 3A4 have not been performed.

Tolterodine is a competitive antagonist of muscarinic receptors. In animal models, tolterodine demonstrates selectivity for urinary bladder receptors over salivary receptors. Urinary bladder contraction is mediated by muscarinic receptors. Tolterodine increases residual urine volume and decreases detrusor muscle pressure.

Distribution: V_d: 113 ±27 L; highly bound to alpha₁-acid glycoprotein

Metabolism: Extensive hepatic metabolism primarily by hepatic cytochrome P-450 isoenzyme 2D6 (some metabolites share activity). Metabolism via isoenzyme 3A4 is a minor pathway in most patients. In patients with a genetic deficiency of isoenzyme 2D6, metabolism via isoenzyme 3A4 predominates.

Bioavailability: 77%; C_max: 1-2 hours after dose; food increases bioavailability

Elimination: Primarily urinary excretion of parent drug and metabolites; <1% excreted unchanged

Adults: Oral: Initial: 2 mg twice daily; the dose may be lowered to 1 mg twice daily based on individual response and tolerability

Dosing adjustment in renal impairment: Use with caution

Dosing adjustment in hepatic impairment: Administer 1 mg twice daily

Food increases bioavailability (~53% increase)

May cause drowsiness, dizziness, or nervousness

Fluoxetine and likely paroxetine increase the serum concentration of tolterodine

No information available to require special precautions

The anticholinergic effects of tolterodine are selective for the urinary bladder rather than salivary glands; xerostomia should not be significant

Take as directed, preferably with food. You may experience headache (a mild analgesic may help); dizziness, nervousness, or sleepiness (use caution when driving, climbing stairs, or engaging in tasks requiring alertness until response to drug is known); abdominal discomfort, diarrhea, constipation, nausea or vomiting (small frequent meals, increased exercise, adequate fluid intake may help). Report back pain, muscle spasms, alteration in gait, or numbness of extremities; unresolved or persistent constipation, diarrhea, or vomiting; or symptoms of upper respiratory infection or flu. Report immediately any chest pain or palpitations; difficulty urinating or pain on urination. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to be pregnant. Do not breast-feed.

Tablet, as tartrate: 1 mg, 2 mg