What Is Tolterodine Tartrate? Uses and Side Effects

Tolterodine tartrate is a widely prescribed oral medication used to manage symptoms associated with bladder dysfunction, helping patients gain better control over urinary function. It is available in two distinct formulations: an immediate-release tablet, typically taken multiple times daily, and an extended-release capsule, designed for once-daily dosing. Both formulations provide relief for chronic bladder issues.

Understanding How Tolterodine Tartrate Works

Tolterodine tartrate is an antimuscarinic agent. It acts as a competitive antagonist, blocking the activity of the chemical messenger acetylcholine at specific muscarinic receptors. Although these receptors are found throughout the body, the drug primarily targets those located in the wall of the urinary bladder.

The detrusor muscle, the primary muscle of the bladder, is controlled by these receptors. When acetylcholine binds, it triggers involuntary contractions leading to bladder spasm and the sudden urge to urinate. By inhibiting acetylcholine, tolterodine relaxes the detrusor muscle. This relaxation reduces the frequency and intensity of involuntary bladder contractions, increasing the bladder’s functional capacity.

After consumption, the drug is metabolized in the liver into 5-hydroxymethyl tolterodine. This metabolite is also active and contributes to the therapeutic effect. Both the parent drug and its metabolite show specificity for the bladder’s muscarinic receptors, providing targeted relief from bladder overactivity.

Conditions Treated with Tolterodine Tartrate

The main application for tolterodine tartrate is the treatment of Overactive Bladder (OAB). OAB is characterized by urinary symptoms resulting from the involuntary contraction of the bladder muscle. The drug alleviates the distress caused by these uncontrolled muscle spasms.

The medication manages urinary urgency, defined as the sudden, compelling need to pass urine that is difficult to postpone. It also addresses urinary frequency, the need to urinate more often than typical. If urgency causes involuntary leakage, known as urge incontinence, tolterodine helps reduce the incidence of these episodes.

By improving bladder control, the drug allows the bladder to hold a greater volume of urine before signaling the need to void. This reduces the disruptive nature of OAB symptoms on daily life.

Common and Serious Adverse Effects

As an antimuscarinic agent, tolterodine tartrate can cause side effects by blocking muscarinic receptors outside the bladder. The most frequently reported adverse effect is dry mouth, which occurs because the drug reduces saliva production. Other common effects include:

  • Headache
  • Constipation due to slowed gastrointestinal movement
  • Dry eyes, which may cause blurred vision

Some effects, though less common, are serious. Because the drug suppresses bladder muscle contraction, it carries a risk of urinary retention, where the bladder cannot empty completely. Signs such as severe difficulty urinating or a significant decrease in urine output require immediate medical consultation.

Rarely, severe allergic reactions may occur, manifesting as angioedema (swelling of the face, lips, tongue, or throat) and difficulty breathing. These symptoms are a medical emergency. The drug is contraindicated in patients with existing conditions like urinary retention, gastric retention, and uncontrolled narrow-angle glaucoma, as its action can worsen these issues. Patients with severe hepatic or renal impairment may require a lower dose or be advised against using the medication due to how it is metabolized and cleared.