Fesoterodine

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Fesoterodine
Fesoterodine.svg
Space-filling model of the fesoterodine molecule
Names
Trade namesToviaz, others
  • [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)
  • O=C(Oc1ccc(cc1[C@@H](c2ccccc2)CCN(C(C)C)C(C)C)CO)C(C)C
  • 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
 ☒NcheckY (what is this?)  (verify)

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. 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 "Fesoterodine Monograph for Professionals". Drugs.com. Retrieved 23 July 2021.
  2. "Fesoterodine (Toviaz) Use During Pregnancy". Drugs.com. 7 November 2019. Retrieved 12 August 2020.
  3. 3.0 3.1 3.2 "Toviaz". Retrieved 4 August 2021.
  4. 4.0 4.1 4.2 BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 821. ISBN 978-0-85711-369-6.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. 7.0 7.1 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.

External links

External sites:
Identifiers: