Tolterodine: Presentation, Mechanism of Action, Indications, Dosage, Side Effects and Interactions

It is a benzhydryl compound that has antimuscarinic and antispasmodic properties. It is a muscarinic receptor antagonist.

Tolterodine is an antispasmodic and anticholinergic.


  • This medicine has a presentation in the form of tablets of immediate release.
  • Another presentation is in the form of long-acting capsules.

Mechanism of action

Tolterodine and its active metabolite, 5-hydroxymethylolterodine, operate as competitive antagonists at muscarinic receptors.

This antagonism produces the inhibition of the bladder contraction, the decrease in the pressure of the detrusor muscle of the bladder and an incomplete emptying of the bladder.

This drug is used for the treatment of an overactive bladder .

By relaxing the muscles of the bladder, tolterodine improves the ability to control urination, helps reduce urine loss and the frequent need to urinate.


It is used to treat patients with overactive bladder problems that have symptoms that include frequent urination, urgency, or involuntary loss of urine.

Tolterodine helps these symptoms by preventing contractions or spasms of the bladder.


  • This medication in the form of an immediate-release tablet is usually prescribed a 2 mg tablet twice a day with or without food.
  • In the form of a long-acting capsule, 4 mg is usually prescribed once a day.

Side effects

Most patients do not have serious side effects, but symptoms such as:

Dry mouth, headache, dry eyes, discomfort, stomach pain, constipation, dizziness, tiredness, blurred vision, drowsiness, signs of kidney infection such as: burning and pain when urinating, back pain, fever, difficulty urinating and changes in heart rate.


Interactions with other medications can change how they work or increase the risk of serious side effects.

The doctor should be informed if he is being treated with the following medications:

  • Anticholinergic drugs such as atropine and scopolamine.
  • Antispasmodics such as dicyclomine, propantheline and certain medications prescribed for Parkinson’s disease, such as benztropine, trihexyphenidyl, belladonna alkaloids, pramlintide and potassium.
  • Other medications such as: amiodarone, dofetilide, pimozide, procainamide, quinidine, sotalol, macrolide antibiotics such as erythromycin, among others.
  • Products that cause drowsiness, such as alcohol, marijuana, antihistamines suchas diphenhydramine, cetirizine, sleeping or anxiety drugs such as alprazolam, zolpidem, diazepam, analgesics, and muscle relaxants.

A lower dose of tolterodine is usually used if you are receiving treatment with:

  • Medicines for fungal or yeast infections.
  • Medications for bacterial infections.
  • Antirheumatic medications such as cyclosporine or vinblastine.


Do not take tolterodine if you have any of these problems:

  • They can not empty their bladder (urinary retention).
  • Slowly delayed or emptying your stomach (gastric retention).
  • You have an eye problem called “uncontrolled narrow-angle glaucoma.”
  • They are allergic to tolterodine or any of its ingredients.
  • They are allergic to Toviaz, which contains fesoterodine.
  • Medications such as tolterodine may cause blurred vision or drowsiness.
  • Be careful driving or doing other dangerous activities until you know how tolterodine affects you.

Precautions and contraindications

The use of tolterodine is not recommended in case of:

  • Allergy to tolterodine or to the components of the drug.
  • Problems to empty your bladder (urinary retention, obstruction of flow), severe obstruction of the digestive tract, ulcerative colitis , slow movement of the stomach or intestines, severe constipation, myasthenia, glaucoma , heart diseases such as heart failure , prolongation of QT in the electrocardiogram, slow heartbeat, family history with sudden cardiac death.
  • Hepatic and renal insufficiencies.
  • Low levels of magnesium or potassium in the blood.
  • If you are in a state of pregnancy.

Caution should be exercised in the use of this medicine with older adults as they may be more sensitive to side effects, especially QT prolongation, drowsiness, constipation, confusion or difficulty urinating.

Confusion and drowsiness may increase the risk of falls.

Caution should also be exercised during breastfeeding, as it is not known whether tolterodine is excreted in breast milk.

The safety and efficacy of the use of this medication have not been established for children.

The relief of the symptoms can begin in 2 weeks approximately after beginning the treatment and the total improvement can not be observed until a little after 8 weeks of treatment.