Desfesoterodine

Products

Desfesoterodine was approved in many countries in 2019 in sustained-release tablet form (generic, tovedeso).

Structure and properties

Desfesoterodine (C22H31NO2, Mr = 341.5 g/mol) is the active metabolite of the prodrug fesoterodine as well as tolterodine (detrusitol). It is also referred to as 5-hydroxymethyltolterodine. In the drug, it is present as desfesoterodine succinate.

Effects

Desfesoterodine (ATC G04BD13) has anticholinergic (parasympatholytic) properties. The effects are due to competitive antagonism at muscarinic acetylcholine receptors. Full efficacy is delayed, occurring after 2 to 8 weeks. The half-life is approximately 7 hours.

Indications

In adults, for the symptomatic treatment of increased urinary frequency and/or imperative urination and/or urge incontinence, as may occur in overactive bladder syndrome.

Dosage

According to the SmPC. The sustained-release tablets are taken once daily and independently of meals.

Contraindications

  • Hypersensitivity
  • Urinary retention
  • Stomach retention
  • Inadequately treated or untreated narrow-angle glaucoma.
  • Myasthenia gravis
  • Severe impairment of liver function
  • Concurrent use of strong CYP3A4 inhibitors in patients with moderate to severe hepatic or renal impairment.
  • Severe ulcerative colitis
  • Toxic megacolon

For complete precautions, see the drug label.

Interactions

Desfesoterodine is a substrate of CYP2D6 and of CYP3A4 and corresponding interactions may occur. Pharmacodynamic interactions are possible with anticholinergics and prokinetics.

Adverse effects

The most common possible adverse effects include: