|Trade names||Detrol, Detrusitol, others|
|Protein binding||Approximately 96.3%|
|Elimination half-life||1.9–3.7 hours|
|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||325.496 g·mol−1|
|3D model (JSmol)|
Tolterodine, sold under the brand names Detrol among others, is medication used to treat frequent urination, urinary incontinence, or urinary urgency. Effects are seen within an hour. It is taken by mouth.
Common side effects include headache, dry mouth, constipation, and dizziness. Serious side effects may include angioedema, urinary retention, and QT prolongation. Use in pregnancy and breastfeeding are of unclear safety. It works by blocking muscarinic receptors in the bladder thus decreasing bladder contractions.
Tolterodine was approved for medical use in 1998. It is available as a generic medication. A month supply costs the NHS about GB£2.09 per month as of 2019. In the United States the wholesale cost of this amount is about US$37.16. In 2017, it was the 229th most commonly prescribed medication in the United States, with more than two million prescriptions.
Detrusor overactivity (DO, contraction of the muscular bladder wall) is the most common form of urinary incontinence (UI) in older adults. It is characterized by uninhibited bladder contractions causing an uncontrollable urge to void. Urinary frequency, urge incontinence and nocturnal incontinence occur. Abnormal bladder contractions that coincide with the urge to void can be measured by urodynamic studies. Treatment is bladder retraining, pelvic floor therapy or with drugs that inhibit bladder contractions such as oxybutynin and tolterodine.
Known side effects:
- Dry mouth
- Decreased gastric motility (upset stomach)
- Dry eyes
- Urinary retention
The following reactions have been reported in patients who have taken tolterodine since it has become available:
- Allergic reactions including swelling
- Rapid heartbeat or abnormal heartbeat
- Accumulation of fluid in the arms and legs
Tolterodine, although it acts on all types of receptors, has fewer side effects than oxybutynin (M3 and M1 selective, but more so in the parotid than in the bladder) as tolterodine targets the bladder more than other areas of the body. This means that less drug needs to be given daily (due to efficient targeting of the bladder) and so there are fewer side effects.
It is marketed by Pfizer in Canada and the United States by its brand name Detrol. In Egypt it is also found under the trade names Tolterodine by Sabaa and Incont L.A. by Adwia.
- British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 762. ISBN 9780857113382.
- "Tolterodine Tartrate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
- "tolterodine Use During Pregnancy". Drugs.com. Retrieved 3 March 2019.
- "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
- "The Top 300 of 2020". ClinCalc. Retrieved 11 April 2020.
- "Tolterodine Tartrate - Drug Usage Statistics". ClinCalc. Retrieved 11 April 2020.
- "Bladder retraining". Interstitial Cystitis Association. Retrieved 6 June 2018.
-  Archived November 26, 2012, at the Wayback Machine
- "Tolterodine". Drug Information Portal. U.S. National Library of Medicine.