Generic Name

Tolterodine Tartrate

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Classification

FDA Approved Indications

• Overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency

Mechanism of Action

Tolterodine selectively antagonizes muscarinic receptors in the bladder detrusor muscle, reducing involuntary contractions and increasing bladder capacity.

Dosage and Administration

Adult: Typically, 4 mg once daily (2 mg twice daily for Detrol), may be adjusted based on response and tolerability.

Pediatric: Not approved for pediatric use.

Geriatric: Use with caution; start at lower doses due to increased susceptibility to side effects.

Renal Impairment: Adjust dose in patients with severe impairment.

Hepatic Impairment: Caution advised; consider dose reduction.

Pharmacokinetics

Absorption: Well absorbed orally, with approximately 65% bioavailability.

Distribution: Widely distributed; crosses the blood-brain barrier.

Metabolism: Primarily metabolized in the liver via CYP3A4 and CYP2D6 enzymes.

Excretion: Excreted mainly in urine and feces.

Half Life: Approximately 2-4 hours for immediate-release; extended-release (Detrol La) has a half-life of about 4-6 hours.

Contraindications

• Urinary retention
• Narrow-angle glaucoma
• Bladder obstruction
• Pregnancy and lactation

Precautions

• Use cautiously in hepatic impairment, elderly, with intestinal obstruction, or with history of urinary retention.

Adverse Reactions - Common

• Dry mouth (Very common)
• Headache (Common)
• Dizziness (Common)
• Constipation (Common)
• Urinary retention (Uncommon)

Adverse Reactions - Serious

• Angioedema (Rare)
• Severe allergic reactions (Rare)
• Visual disturbances (Uncommon)

Drug-Drug Interactions

• Other anticholinergic drugs, CYP3A4 inhibitors (e.g., ketoconazole, ritonavir)

Drug-Food Interactions

• Alcohol may enhance CNS side effects.

Drug-Herb Interactions

N/A

Nursing Implications

Patient/Family Teaching

• Take medication exactly as prescribed.
• Report difficulty urinating, eye pain, or worsening symptoms.
• Avoid alcohol and operating heavy machinery if dizziness occurs.
• Maintain adequate fluid intake to prevent dry mouth.

Special Considerations

Black Box Warnings:

• Use with caution in patients with urinary retention or uncontrolled narrow-angle glaucoma.

Genetic Factors: Metabolism affected by CYP2D6 and CYP3A4 polymorphisms, which may influence drug levels.

Lab Test Interference: None significant.

Overdose Management

Signs/Symptoms: Severe anticholinergic effects such as hallucinations, seizures, tachycardia, or urinary retention.

Treatment: Supportive care, activated charcoal if ingestion was recent, and management of symptoms; no specific antidote.

Storage and Handling

Storage: Store at room temperature, 20-25°C (68-77°F).

Stability: Stable under recommended storage conditions.