Fesoterodine

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Fesoterodine.jpg

[edit] MECHANISM OF ACTION

Fesoterodine is a competitive muscarinic receptor antagonist. After oral administration, fesoterodine is rapidly and extensively hydrolyzed by nonspecific esterases to its active metabolite, 5-hydroxymethyl tolterodine, which is responsible for the antimuscarinic activity of fesoterodine.

Muscarinic receptors play a role in contractions of urinary bladder smooth muscle and stimulation of salivary secretion. By preventing the binding of acetylcholine to these receptors, Fesoterodine's active metabolite reduces smooth muscle tone in the bladder, allowing the bladder to retain larger volumes of urine and reducing the number of micturition, urgency and incontinence episodes.

[edit] INDICATIONS

  • Treatment of overactive bladder with symptoms of urge urinary incontinence, urgency, and frequency

[edit] DOSAGE

4 mg taken once daily with or without food. Based upon individual response and tolerability, the dose may be increased to 8 mg once daily.

Do not exceed 4 mg once daily in patients with:

[edit] CONTRAINDICATIONS

  • Urinary retention
  • Gastric retention
  • Uncontrolled narrow-angle glaucoma
  • Hypersensitivity to Fesoterodine

[edit] WARNINGS AND PRECAUTIONS

  • Angioedema: Angioedema of the face, lips, tongue, and/or larynx has been reported with fesoterodine. In some cases angioedema occurred after the first dose.
  • Anaphylactic reactions have been reported rarely
  • Urinary Retention: Administer with caution to patients with clinically significant bladder outflow obstruction because of the risk of urinary retention.
  • Gastrointestinal Disorders: Fesoterodine like other antimuscarinic drugs, should be used with caution in patients with decreased gastrointestinal motility, such as those with severe constipation.
  • Central Nervous System Effects: Somnolence has been reported with Fesoterodine. Advise patients not to drive or operate heavy machinery until they know how Fesoterodine affects them.
  • Controlled Narrow-Angle Glaucoma: Use with caution in patients being treated for narrow-angle glaucoma and only where the potential benefits outweigh the risks
  • Myasthenia gravis: Fesoterodine should be used with caution in patients with myasthenia gravis, a disease characterized by decreased cholinergic activity at the neuromuscular junction.

[edit] INTERACTIONS

  • Coadministration of Fesoterodine with other antimuscarinic agents that produce dry mouth, constipation, urinary retention, and other anticholinergic pharmacological effects may increase the frequency and/or severity of such effects.
  • CYP3A4 Inhibitors: Doses of Fesoterodine greater than 4 mg are not recommended in patients taking potent CYP3A4 inhibitors, such as ketoconazole, itraconazole, and clarithromycin
  • CYP3A4 Inducers: No dosing adjustments are recommended in the presence of CYP3A4 inducers, such as rifampin and carbamazepine.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Fesoterodine should be used during pregnancy only if the potential benefit for the mother justifies the potential risk to the fetus.
  • Fesoterodine should not be administered during nursing unless the potential benefit outweighs the potential risk to the neonate.

[edit] SIDE EFFECTS

The most frequently reported adverse events (≥4%) for Fesoterodine were: dry mouth (placebo, 7%; Fesoterodine 4 mg, 19%; Fesoterodine 8 mg, 35%) and constipation (placebo, 2%; Toviaz 4 mg, 4%; Toviaz 8 mg, 6%)

Heat prostration (due to decreased sweating) can occur when anticholinergic drugs, such as Fesoterodine, are used in a hot environment.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Urinary incontinence/Overactive bladder syndrome
Urinary antispasmodics (primarily antimuscarinics) Fesoterodine   Flavoxate   Oxybutynin (Oral)   Oxybutynin (Transdermal)   Propiverine   Solifenacin   Tolterodine   Trospium chloride