Tolterodine

Tolterodine
Clinical data
Trade namesDetrol, Detrusitol, others
Other namesPNU-200583E
AHFS/Drugs.comMonograph
MedlinePlusa699026
License data
Pregnancy
category
  • AU: B3
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • CA: ℞-only
  • UK: POM (Prescription only)[1]
  • US: ℞-only[2][3]
  • EU: Rx-only[4]
Pharmacokinetic data
Bioavailability77%
Protein bindingApproximately 96.3%
Elimination half-life1.9–3.7 hours
Identifiers
IUPAC name
  • (S)-2-[3-(Diisopropylamino)-1-phenylpropyl]-4-methylphenol
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.232.068
Chemical and physical data
FormulaC22H31NO
Molar mass325.496 g·mol−1
3D model (JSmol)
SMILES
  • Cc1ccc(c(c1)[C@H](CCN(C(C)C)C(C)C)c2ccccc2)O
InChI
  • 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 name Detrol among others, is a medication used to treat frequent urination, urinary incontinence, or urinary 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 include angioedema, urinary retention, and QT prolongation.[6] Use in pregnancy and breastfeeding are of unclear safety.[5][8] It works by blocking muscarinic receptors in the bladder thus decreasing bladder contractions.[6]

Tolterodine was approved for medical use in 1998.[6] It is available as a generic 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

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,[11] pelvic floor therapy or with drugs that inhibit bladder contractions such as oxybutynin and tolterodine.

Side effects

Known side effects:

  • Dry mouth[12]
  • Decreased gastric motility (upset stomach)[12]
  • Headache[12]
  • Constipation[12]
  • Dry eyes[12]
  • Sleepiness[12]
  • Urinary retention[12]

The following reactions have been reported in people who have taken tolterodine since it has become available:

  • Allergic reactions including swelling[12]
  • Rapid heartbeat or abnormal heartbeat[12]
  • Accumulation of fluid in the arms and legs[12]

Tolterodine is not recommended for use in people with myasthenia gravis and angle closure glaucoma.

Pharmacology

Tolterodine acts on M2 and M3[13] subtypes of muscarinic receptors whereas older antimuscarinic treatments for overactive bladder act more specifically on M3 receptors.

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.

Society and culture

Brand names

It is marketed by Pfizer 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 by Viatris after Upjohn was spun off from Pfizer.[14][15][16]

References

  1. ^ "Detrusitol 1mg film-coated tablets - Summary of Product Characteristics (SmPC)". (emc). 9 March 2021. Retrieved 12 May 2022.
  2. ^ "Detrol- tolterodine tartrate tablet, film coated". DailyMed. 29 September 2021. Retrieved 12 May 2022.
  3. ^ "Detrol LA- tolterodine tartrate capsule, extended release". DailyMed. 12 October 2020. Retrieved 12 May 2022.
  4. ^ "List of nationally authorised medicinal products" (PDF). ema.europa.eu. 5 May 2022. Retrieved 9 November 2023.
  5. ^ a b c British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 762. ISBN 9780857113382.
  6. ^ a b c d e f "Tolterodine Tartrate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 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. Retrieved 3 March 2019.
  9. ^ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
  10. ^ "Tolterodine - Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
  11. ^ "Bladder retraining". Interstitial Cystitis Association. Archived from the original on 28 July 2018. Retrieved 6 June 2018.
  12. ^ a b c d e f g h i j "Tolterodine (oral route) - Side effects & dosage". Mayo Clinic. Archived from the original on 29 September 2025. Retrieved 29 September 2025.
  13. ^ "Tolterodine". DrugBank.
  14. ^ "Pfizer Completes Transaction to Combine Its Upjohn Business with Mylan". Pfizer. 16 November 2020. Retrieved 17 June 2024 – via Business Wire.
  15. ^ "Detrol". Pfizer. Retrieved 17 June 2024.
  16. ^ "Brands". Viatris. 16 November 2020. Retrieved 17 June 2024.
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