Tolterodine Tartrate

What it is and how it works

Mechanism of Action Tolterodine acts as a competitive antagonist of acetylcholine at postganglionic muscarinic receptors. Both urinary bladder contraction and salivation are mediated via cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver, resulting in the formation of 5-hydroxymethyl tolterodine (5-HMT), the major pharmacologically active metabolite. 5-HMT, which exhibits an antimuscarinic activity similar to that of tolterodine, contributes significantly to the therapeutic effect.

Indications

1. INDICATIONS AND USAGE Tolterodine tartrate extended-release capsules, USP are indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency . Tolterodine tartrate extended-release capsules, USP are an antimuscarinic indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency.

Dosage and administration (summary)

2. DOSAGE AND ADMINISTRATION 4 mg capsules taken orally once daily with water and swallowed whole 2 mg capsules taken orally once daily with water and swallowed whole in the presence of: mild to moderate hepatic impairment (Child-Pugh class A or B severe renal impairment [Creatinine Clearance (CCr) 10-30 mL/min] drugs that are potent CYP3A4 inhibitors. Tolterodine tartrate extended-release capsules are not recommended for use in patients with CCr <10 mL/min. Tolterodine tartrate extended-release capsules are not recommended for use in patients with severe hepatic impairment (Child-Pugh Class C).

Contraindications

4. CONTRAINDICATIONS Tolterodine tartrate extended-release capsules are contraindicated in patients with urinary retention, gastric retention, or uncontrolled narrow-angle glaucoma. Tolterodine tartrate extended-release capsules are also contraindicated in patients with known hypersensitivity to the drug or its ingredients, or to fesoterodine fumarate extended-release tablets which, like tolterodine tartrate extended-release capsules, are metabolized to 5-hydroxymethyl tolterodine .

Warnings and precautions

5. WARNINGS AND PRECAUTIONS Anaphylaxis and angioedema requiring hospitalization and emergency medical treatment have occurred with the first or subsequent doses of tolterodine tartrate extended-release capsules. Urinary Retention: use caution in patients with clinically significant bladder outflow obstruction because of the risk of urinary retention. Gastrointestinal Disorders: use caution in patients with gastrointestinal obstructive disorders or decreased gastrointestinal motility because of the risk of gastric retention.

Pregnancy

Pregnancy Risk Summary There are no available data with tolterodine tartrate extended-release capsules use in pregnant women to inform drug-associated risks. In animal reproduction studies, oral administration of tolterodine and its 5-HMT metabolite to pregnant mice during organogenesis did not produce adverse developmental outcomes at doses approx…

Storage and supply

16. HOW SUPPLIED/STORAGE AND HANDLING Tolterodine Tartrate Extended-release Capsules, USP are available containing 2 mg or 4 mg of tolterodine tartrate. The 2 mg capsule is white to off white spherical to oval pellets filled in hard gelatin capsule shells of size “4” with "┐ L " imprinted in grey color ink on opaque green colored cap and “013” impr…

Source: Tolterodine Tartrate (Tolterodine Tartrate) — US FDA prescribing information, 2026-01-06, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.