Fesoterodine

Fesoterodine
Space-filling model of the fesoterodine molecule
Names
Trade namesToviaz, others
IUPAC name
  • [2-[(1R)-3-(Di(propan-2-yl)amino)-1-phenylpropyl]-4-(hydroxymethyl)phenyl] 2-methylpropanoate
Clinical data
Drug classAntimuscarinic[1]
Main usesOveractive bladder syndrome (OAB)[1]
Side effectsDry mouth, constipation[1]
Pregnancy
category
  • US: N (Not classified yet)[2]
    Routes of
    use    		By mouth
    Typical dose4 to 8 mg/day[1]
    External links
    AHFS/Drugs.comMonograph
    US NLMFesoterodine
    MedlinePlusa609021
    Legal
    License data
    Legal status
    Pharmacokinetics
    Bioavailability52% (active metabolite)
    Protein binding50% (active metabolite)
    MetabolismLiver (CYP2D6- and 3A4-mediated)
    Elimination half-life7–8 hours (active metabolite)
    ExcretionKidney (70%) and fecal (7%)
    Chemical and physical data
    FormulaC26H37NO3
    Molar mass411.586 g·mol−1
    3D model (JSmol)
    SMILES
    • O=C(Oc1ccc(cc1[C@@H](c2ccccc2)CCN(C(C)C)C(C)C)CO)C(C)C
    InChI
    • InChI=1S/C26H37NO3/c1-18(2)26(29)30-25-13-12-21(17-28)16-24(25)23(22-10-8-7-9-11-22)14-15-27(19(3)4)20(5)6/h7-13,16,18-20,23,28H,14-15,17H2,1-6H3/t23-/m1/s1 checkY
    • Key:DCCSDBARQIPTGU-HSZRJFAPSA-N checkY

    Fesoterodine, sold under the brand name Toviaz among others, is a medication used to treat the symptoms of overactive bladder syndrome (OAB).[1][3] It is a second line medication for this use.[4] It is taken by mouth.[1]

    Common side effects include dry mouth and constipation.[1] Other side effects may include urinary retention, trouble sleeping, and dizziness.[1][4] It is not recommended in people with severe liver problems or myasthenia gravis.[3] It is an antimuscarinic and works via the same chemical as tolterodine.[1]

    Fesoterodine was approved for medical use in Europe in 2007,[3] the United States in 2008,[1] and Canada in 2012.[5] In the United States it costs about 310 USD per month as of 2021.[6] This amount in the United Kingdom costs the NHS about £26.[4]

    Medical uses

    Fesoterodine has the advantage of allowing more flexible dosage than other muscarinic antagonists.[7] Its tolerability and side effects are similar to other muscarinic antagonists and as a new drug seems unlikely to make great changes in practices of treatment for overactive bladder.[7]

    A Japanese study from 2017, showed that urgency and urge incontinence are improved after 3 days administration of the drug, with full efficacy able to be judged after 7 days administration. Overactive bladder was found to be resolved in 88% of patients after seven days usage. [8]

    Dosage

    It is usually used at 4 to 8 mg once per day.[1]

    Mechanism of action

    Fesoterodine is a prodrug. It is broken down into its active metabolite, desfesoterodine, by plasma esterases.

    References

    1. 1 2 3 4 5 6 7 8 9 10 11 "Fesoterodine Monograph for Professionals". Drugs.com. Archived from the original on 26 January 2021. Retrieved 23 July 2021.
    2. ↑ "Fesoterodine (Toviaz) Use During Pregnancy". Drugs.com. 7 November 2019. Archived from the original on 29 November 2020. Retrieved 12 August 2020.
    3. 1 2 3 "Toviaz". Archived from the original on 12 November 2020. Retrieved 4 August 2021.
    4. 1 2 3 BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 821. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
    5. ↑ "Notice of Decision for TOVIAZ". Archived from the original on 2012-04-23. Retrieved 2012-04-20.
    6. ↑ "Toviaz Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 4 August 2021.
    7. 1 2 Vella M, Cardozo L (September 2011). "Review of fesoterodine". Expert Opinion on Drug Safety. 10 (5): 805–8. doi:10.1517/14740338.2011.591377. PMID 21639817. S2CID 9653506.
    8. ↑ "Sato N, Fuji K, Ogawa Y (2017). "Transactions of The Showa University Society: The 335th Meeting". The Showa University Journal of Medical Sciences. 29 (2): 201–217. doi:10.15369/sujms.29.201. ISSN 2185-0968.
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