Fesoterodine

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Fesoterodine
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
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

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. 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. ↑ 3.0 3.1 3.2 "Toviaz". Archived from the original on 12 November 2020. 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.{{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. ↑ 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:
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