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Tolterodine

From Wikipedia, the free encyclopedia
Benzhydryl compound

Pharmaceutical compound
Tolterodine
Clinical data
Trade namesDetrol, Detrusitol, others
Other namesPNU-200583E
AHFS/Drugs.comMonograph
MedlinePlusa699026
License data
Pregnancy
category
Routes of
administration
By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability77%
Protein bindingApproximately 96.3%
Eliminationhalf-life1.9–3.7 hours
Identifiers
  • (S)-2-[3-(Diisopropylamino)-1-phenylpropyl]-4-methylphenol
CAS Number
PubChemCID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard(EPA)
ECHA InfoCard100.232.068Edit this at Wikidata
Chemical and physical data
FormulaC22H31NO
Molar mass325.496 g·mol−1
3D model (JSmol)
  • Cc1ccc(c(c1)[C@H](CCN(C(C)C)C(C)C)c2ccccc2)O
  • InChI=1S/C22H31NO/c1-16(2)23(17(3)4)14-13-20(19-9-7-6-8-10-19)21-15-18(5)11-12-22(21)24/h6-12,15-17,20,24H,13-14H2,1-5H3/t20-/m1/s1 checkY
  • Key:OOGJQPCLVADCPB-HXUWFJFHSA-N checkY
  (verify)

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]

Medical uses

[edit]

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]

Side effects

[edit]

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.

Pharmacology

[edit]

Tolterodine acts on M2 and M3[13] 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]

Society and culture

[edit]

Brand names

[edit]

It is marketed byPfizer in Canada and the United States under the brand name Detrol, while in Indonesia it is marketed under the brand name Detrusitol. 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.[14][15][16]

References

[edit]
  1. ^"Detrusitol 1mg film-coated tablets - Summary of Product Characteristics (SmPC)".(emc). 9 March 2021. Retrieved12 May 2022.
  2. ^"Detrol- tolterodine tartrate tablet, film coated".DailyMed. 29 September 2021. Retrieved12 May 2022.
  3. ^"Detrol LA- tolterodine tartrate capsule, extended release".DailyMed. 12 October 2020. Retrieved12 May 2022.
  4. ^"List of nationally authorised medicinal products"(PDF).ema.europa.eu. 5 May 2022. Retrieved9 November 2023.
  5. ^abcBritish national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 762.ISBN 9780857113382.
  6. ^abcdef"Tolterodine Tartrate Monograph for Professionals".Drugs.com. American Society of Health-System Pharmacists. Retrieved3 March 2019.
  7. ^Narain S, Parmar M (January 2021)."Tolterodine".StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing.PMID 32491781.
  8. ^"Tolterodine Pregnancy and Breastfeeding Warnings".Drugs.com. Retrieved3 March 2019.
  9. ^"The Top 300 of 2020".ClinCalc. Retrieved7 October 2022.
  10. ^"Tolterodine - Drug Usage Statistics".ClinCalc. Retrieved7 October 2022.
  11. ^"Bladder retraining". Interstitial Cystitis Association. Archived fromthe original on 28 July 2018. Retrieved6 June 2018.
  12. ^abcdefghij"Tolterodine (oral route) - Side effects & dosage".Mayo Clinic. Archived fromthe original on 29 September 2025. Retrieved29 September 2025.
  13. ^"Tolterodine".DrugBank.
  14. ^"Pfizer Completes Transaction to Combine Its Upjohn Business with Mylan". Pfizer. 16 November 2020. Retrieved17 June 2024 – via Business Wire.
  15. ^"Detrol".Pfizer. Retrieved17 June 2024.
  16. ^"Brands".Viatris. 16 November 2020. Retrieved17 June 2024.
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