Medications and Drugs
GENERIC NAME: tolterodine
BRAND NAME: Detrol, Detrol LA
DRUG CLASS AND MECHANISM: Tolterodine belongs to a class of
drugs called cholinergic (acetyl-choline) 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 acetyl-
choline, 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 (e.g., 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 acetyl-choline 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.
GENERIC AVAILABLE: no
PRESCRIPTION: yes
PREPARATIONS: Tolterodine tablets: 1mg and 2mg. Long acting tolterodine capsules: 2mg and 4 mg.
STORAGE: Tablets and capsules should be stored at room temperature, 15-
30°C (59-86°F).
PRESCRIBED FOR: Tolterodine is used to treat
uncontrollable urination due to what is often referred to as
an "overactive" bladder. Symptoms include the need to urinate
frequently, an urge to urinate immediately, and an inability to
control urine release (urinary incontinence).
DOSING: Tolterodine usually is taken twice daily. The
starting dose is 2mg twice daily. With the long-acting tolterodine, the starting dose is 4mg daily, and may be reduced to 2mg if the larger dose is not tolerated. The dose may need to be reduced for patients who have impaired function of the liver or kidneys. Caution is
recommended for patients with narrow-angle glaucoma, obstruction to
the flow of urine, or poor emptying of the stomach since these
medical conditions may worsen with tolterodine administration.
DRUG INTERACTIONS: Tolterodine follows a specific path
through the liver in order to be eliminated from the body. Drugs
that block this path may slow the elimination of tolterodine, raise
tolterodine blood levels, and lead to side effects. No formal
studies have been conducted showing such interactions, however. The
list of drugs that might possibly interfere with the elimination of
tolterodine includes is erythromycin, clarithromycin (Biaxin),
ketoconazole (Nizoral), itraconazole (Sporanox), and miconazole
(Monistat, Micatin). The dose of tolterodine should be reduced to 1mg
twice daily if taken with any of these drugs.
PREGNANCY: At doses much greater than those used in humans, tolterodine causes fetal abnormalities in animals. 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.
NURSING MOTHERS: Tolterodine is secreted into breast milk in animals; however, it is not
known if tolterodine is secreted into the breast milk of women. Therefore, its use is not recommended
in nursing mothers.
SIDE EFFECTS: The most common side effects seen while
taking tolterodine are dry mouth, dry eyes, headache, upset stomach
and constipation. Tolterodine also may cause blurred vision.
Reference: FDA Prescribing Information
Last Editorial Review: 11/15/2001
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
- Drug Interactions - Learn about potential drug interactions you may be exposed to. Drug interactions can occur with prescription drugs, OTC medication, vitamins, herbs, and supplements.
- Urinary Incontinence - Learn about urinary incontinence (UI) in men. Find out the signs and symptoms of UI, what causes it, and what the treatment options are. Male urinary incontinence can occur because of prostate cancer along with other bladder control problems.
- Drugs: What You Should Know About Your Drugs - Find out what you should know about your drugs such as side effects, warnings and precautions, storage information, and if a generic version is as good as the brand name.
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