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Clinical data | |
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Trade names | Detrol, Detrusitol, others |
Other names | PNU-200583E |
AHFS/Drugs.com | Monograph |
MedlinePlus | a699026 |
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Routes of administration | By mouth |
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Pharmacokinetic data | |
Bioavailability | 77% |
Protein binding | Approximately 96.3% |
Eliminationhalf-life | 1.9–3.7 hours |
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ECHA InfoCard | 100.232.068![]() |
Chemical and physical data | |
Formula | C22H31NO |
Molar mass | 325.496 g·mol−1 |
3D model (JSmol) | |
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Tolterodine, sold under the brand nameDetrol among others, is amedication used to treatfrequent urination,urinary incontinence, orurinary urgency.[5] Effects are seen within an hour.[6] It is taken by mouth.[6][7]
Common side effects include headache, dry mouth, constipation, and dizziness.[6] Serious side effects may includeangioedema,urinary retention, andQT prolongation.[6] Use inpregnancy andbreastfeeding are of unclear safety.[5][8] It works byblocking muscarinic receptors in thebladder thus decreasing bladder contractions.[6]
Tolterodine was approved for medical use in 1998.[6] It is available as ageneric medication.[5] In 2020, it was the 271st most commonly prescribed medication in the United States, with more than 1 million prescriptions.[9][10]
Detrusor overactivity (DO, contraction of the muscular bladder wall) is the most common form of urinary incontinence (UI) in older adults.[medical citation needed] It is characterized by uninhibited bladder contractions causing an uncontrollable urge to void.[medical citation needed] Urinary frequency, urge incontinence and nocturnal incontinence occur.[medical citation needed] Abnormal bladder contractions that coincide with the urge to void can be measured byurodynamic studies.[medical citation needed] Treatment is bladder retraining,[11][unreliable medical source?]pelvic floor therapy or with drugs that inhibit bladder contractions such asoxybutynin and tolterodine.[medical citation needed]
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Known side effects:
The following reactions have been reported in people who have taken tolterodine since it has become available:
Tolterodine is not recommended for use in people withmyasthenia gravis andangle closure glaucoma.
Tolterodine acts on M2 and M3[12] subtypes ofmuscarinic receptors whereas olderantimuscarinic treatments for overactive bladder act more specifically on M3 receptors.[medical citation needed]
Tolterodine, although it acts on all types of receptors, has fewer side effects thanoxybutynin (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.[medical citation needed]
It is marketed byPfizer in Canada and the United States under the brand name Detrol. In Egypt it is also found under the trade names Tolterodine by Sabaa and Incont L.A. by Adwia.
In the US, Detrol is marketed byViatris after Upjohn was spun off from Pfizer.[13][14][15]