What is tolterodine, and how does it work (mechanism of action)?
Tolterodine belongs to a class of drugs
called cholinergic (acetylcholine) receptor blockers. It is used to treat
disorders of the urinary bladder that affect urination. The urinary bladder is a
muscular "bag." Urine coming from the kidneys fills the bladder and causes it to
stretch like a balloon. As it stretches, pressure in the bladder increases and,
when the bladder reaches a certain level of stretch, a desire to urinate is
felt. Nerves in the muscular wall of the bladder release acetylcholine, a
chemical that attaches to receptors on the muscle cells and causes the cells to
contract (tighten). This contributes further to the increase in pressure within
the bladder and the desire to urinate. At the appropriate time (for example, when a
toilet is available), there is conscious relaxation of the muscle at the outlet
of the bladder, and the high bladder pressure forces urine out of the bladder.
Normally, urination is under conscious control; however, in some individuals
normal control as well as normal sensation are lost. The desire to urinate may
be felt when there is little urine in the bladder, and urination may occur
without warning or control. By blocking the effect of acetylcholine on the
muscle cells, tolterodine slows the build-up of pressure in the bladder, reduces
the sensation to urinate, and prevents uncontrolled urination. The FDA approved
tolterodine in 1998. An extended release form of tolterodine, (Detrol LA) was
approved by the FDA in 2001.
What brand names are available for tolterodine?
Detrol, Detrol LA
Is tolterodine available as a generic drug?
Do I need a prescription for tolterodine?
What are the side effects of tolterodine?
The most common side effects of tolterodine are:
Tolterodine also may cause blurred vision. Caution is recommended for patients with
narrow-angle glaucoma, obstruction to the flow of
urine, or poor emptying of the stomach since tolterodine may worsen these
What is urinary incontinence?
What is the dosage for tolterodine?
Tolterodine usually is taken twice daily. The starting dose is
1 or 2 mg twice daily. The starting dose when using long-acting tolterodine is 2
or 4 mg daily. The dose may need to be reduced for patients who have impaired
liver or kidney function.
Which drugs or supplements interact with tolterodine?
Tolterodine is broken down by liver enzymes before
elimination from the body. Drugs that block these liver enzymes may slow the
elimination of tolterodine, raise tolterodine blood levels, and lead to side
effects. The list of drugs that may interfere with the elimination of
tolterodine includes erythromycin, clarithromycin (Biaxin), ketoconazole (Nizoral),
itraconazole (Sporanox), cyclosporine, vinblastine, and miconazole (Monistat,
Micatin). The dose of tolterodine should be reduced to 1 mg twice daily if taken
with any of these drugs.
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Is tolterodine safe to take if I’m pregnant or breastfeeding?
At doses much greater than those used in humans,
tolterodine causes fetal abnormalities in animals, but there are no studies with
tolterodine in pregnant women. Therefore, tolterodine should only be given to
pregnant women if the benefits are felt to outweigh the potential risks.
Tolterodine is secreted into
breast milk in animals;
however, it is not known if tolterodine is secreted into the breast milk of
women. Therefore, nursing mothers should either not breast feed or discontinue
What else should I know about tolterodine?
What preparations of tolterodine are available?
Tablets: 1 and 2mg. Long acting capsules: 2 and 4 mg.
How should I keep tolterodine stored?
Tablets and capsules should be stored at room temperature, 15 C – 30 C (59 F – 86 F).