Tolterodine Tartrate

Trade Names:
Detrol
- Tablets 1 mg
- Tablets 2 mg

Trade Names:
Detrol LA
- Capsule, extended-release 2 mg
- Capsule, extended-release 4 mg

Pharmacology

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Antagonizes muscarinic receptor, which mediates urinary bladder contraction and salivation.

Pharmacokinetics

Absorption

Tolterodine is rapidly absorbed. After dosing, T _max is within 1 to 2 h (immediate-release) and 2 to 6 h (extended-release). Food increases bioavailability (about 53%) of immediate-release, but has no effect on extended-release formulation.

Distribution

Tolterodine is highly protein bound. Vd is about 113 L.

Metabolism

Tolterodine is extensively metabolized by the liver following oral dosing. The primary metabolic route involves oxidation of the 5-methyl group and is mediated by the cytochrome P-450 2D6 isoenzyme and leads to a pharmacologically active 5-hydroxymethyl metabolite.

Elimination

77% is recovered in urine and 17% is recovered in feces within 7 days. Tolterodine's t _½ is approximately 2 to 4 h.

Special Populations

Patients with reduced renal function should receive no more than 2 mg tolterodine/day. Use caution.

Patients with significantly reduced hepatic function should not receive doses more than 1 mg twice daily.

Indications and Usage

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

Contraindications

Urinary retention; gastric retention; uncontrolled narrow-angle glaucoma.

Dosage and Administration

PO 1 to 2 mg daily.

PO 2 to 4 mg daily.

Storage/Stability

Store at room temperature in tightly closed container.

Drug Interactions

May increase tolterodine plasma levels, which may increase activity and side effects.

Plasma levels of tolterodine may be decreased while the AUC of the active 5-hydroxymethyl metabolite may be increased; requires no dosage adjustment.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension.

CNS

Headache; somnolence; paresthesia, nervousness (immediate-release); dizziness, anxiety (extended-release).

Dermatologic

Pruritus; dry skin.

EENT

Abnormal vision (accommodation abnormalities); xerophthalmia; sinusitis (extended-release).

GI

Dry mouth; constipation; abdominal pain; dyspepsia; flatulence, vomiting, nausea (immediate-release).

Genitourinary

Dysuria (extended-release).

Metabolic

Weight gain.

Respiratory

Bronchitis; coughing.

Miscellaneous

Chest pain; infection; fungal infection; falling (immediate-release); fatigue (extended-release).

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Renal Function

Use with caution.

Hepatic Function

Use with caution.

Controlled narrow-angle glaucoma

Use with caution.

Urinary/Gastric retention

Use with caution.

Overdosage

Symptoms

Dry mouth, thirst, cardiac slowing followed by acceleration, palpitations, hypertension, hypotension, inhibition of sweating, flushing, hot skin, photophobia, dilated pupils, blurred vision, speech disturbances, CNS stimulation, delirium, restlessness, drowsiness, stupor, headache, decreased intestinal peristalsis, abdominal distension, ataxia, hallucinations, seizures, coma.

Patient Information

• Instruct patient to take the medication as prescribed at the same time each day.
• Advise patient that antimuscarinic agents such as tolterodine may produce side effects including blurred vision and to notify primary health care giver if side effects occur or if there are any other concerns.
• Caution female patients to notify the health care provider immediately should they become or plan to become pregnant.

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Overactive Bladder, Urinary Incontinence

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