Tolterodine

Tolterodine, sold under the brand names Detrol among others, is medication used to treat frequent urination, urinary incontinence, or urinary urgency.[1] Effects are seen within an hour.[2] It is taken by mouth.[2]

Tolterodine
Clinical data
Trade namesDetrol, Detrusitol, others
AHFS/Drugs.comMonograph
MedlinePlusa699026
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
    Routes of
    administration    		By mouth
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Bioavailability77%
    Protein bindingApproximately 96.3%
    Elimination half-life1.9–3.7 hours
    Identifiers
    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 mass325.488 g/mol g·mol−1
    3D model (JSmol)
      (verify)

    Common side effects include headache, dry mouth, constipation, and dizziness.[2] Serious side effects may include angioedema, urinary retention, and QT prolongation.[2] Use in pregnancy and breastfeeding are of unclear safety.[1][3] It works by blocking muscarinic receptors in the bladder thus decreasing bladder contractions.[2]

    Tolterodine was approved for medical use in 1998.[2] It is available as a generic medication.[1] A month supply costs the NHS about GB£2.09 per month as of 2019.[1] In the United States the wholesale cost of this amount is about US$37.16.[4] In 2016 it was the 300th most prescribed medication in the United States with more than a million prescriptions.[5]

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

    Side effects

    Known side effects:

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

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

    Pharmacology

    Tolterodine acts on M2 and M3[7] 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. This means that less drug needs to be given daily (due to efficient targeting of the bladder) and so there are fewer side effects.

    Brand names

    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.

    References
    1. British national formulary : BNF 76 (76 ed.). Pharmaceutical Press. 2018. p. 762. ISBN 9780857113382.
    2. "Tolterodine Tartrate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
    3. "tolterodine Use During Pregnancy". Drugs.com. Retrieved 3 March 2019.
    4. "NADAC as of 2019-02-27". Centers for Medicare and Medicaid Services. Retrieved 3 March 2019.
    5. "The Top 300 of 2019". clincalc.com. Retrieved 22 December 2018.
    6. "Bladder retraining". Interstitial Cystitis Association. Retrieved 6 June 2018.
    7. Archived November 26, 2012, at the Wayback Machine
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