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Fesoterodine: Mechanism of Action, Adverse Effects, Contraindications, and Dosage

• Anticholinergics: general pharmacology
• Trospium chloride
• Oxybutynin
• Propiverine
• Tolterodine
• Fesoterodine
• Darifenacin
• Solifenacin
• Butylscopolamine

Mechanism of Action

Fesoterodine is a lipophilic tertiary amine with anticholinergic effects on muscarinic receptors. After oral absorption, fesoterodine is hydrolyzed into an active metabolite (5-hydroxymethyl tolterodine, as with tolterodine). In direct comparison with tolterodine, fesoterodine has advantages in terms of efficacy and tolerability.

The inhibition of M₃ receptors with Fesoterodine reduces smooth muscle detrusor contraction, increases functional bladder capacity, and alleviates symptoms of urgency. Fesoterodine is used to treat overactive bladder, urge incontinence, neurogenic lower urinary tract dysfunction and catheter-related bladder discomfort (CRBD).

Pharmacokinetics of Fesoterodine:

After oral adsorption, there is a reliable metabolism to 5-hydroxymethyl tolterodine. Mainly renal excretion of the metabolites, with a half-life of seven hours.

Adverse Effects of Fesoterodine

Muscarinic receptors are present in numerous organs. M₃ receptors are mainly found in smooth muscle and glands. Fesoterodine exhibits some organ selectivity and may result in fewer side effects compared to other anticholinergics.

Eye:

• Mydriases
• Disturbed accommodation
• Dry eyes due to an inhibited lacrimal gland
• Risk of increased intraocular pressure in patients with glaucoma

Gastrointestinal tract:

• Dry mouth due to inhibited salivary glands
• Inhibition of intestinal motility (constipation)

Heart:

• Tachycardia

CNS:

• Dizziness, loss of concentration, drowsiness
• Aggravation of dementia
• Headache
• Fear, anxiety, and confusion are possible psychiatric side effects.

Skin:

• Dry skin due to inhibited sweat glands.
• Impaired temperature regulation in fever.

Drug Interactions

Increased anticholinergic effect with antiparkinson drugs, antihistamines, antipsychotics, and tricyclic antidepressants. Amplification of the tachycardic effect of sympathomimetic medications. Fesoterodine mitigates the effects of gastrointestinal prokinetics. Ketakonazole and macrolid antibiotics may increase the plasma concentration of Fesoterodine.

Contraindications of Fesoterodine

• Risk of urinary retention
• Narrow-angle glaucoma
• Ileus, gastrointestinal stenosis
• Myasthenia gravis
• Tachyarrhythmias
• Pregnancy
• Children
• Severe liver failure
• Be cautious in patients with severe renal insufficiency, QT prolongation, electrolyte disturbances, and manifest heart disease.

Dosage of Fesoterodine:

The starting dose is 4 mg once daily. Depending on effectiveness, the dose may be increased to 8 mg once daily. Full effect is achieved after 2–8 weeks of therapy. Do not increase the dosage in patients with severe hepatic or renal insufficiency or concomitant administration of inhibitors of cytochrome CYP3A4 such as ketoconazole or macrolide antibiotics.

References

Ouslander 2004 OUSLANDER, J. G.: Management of overactive bladder.
In: N Engl J Med
350 (2004), Nr. 8, S. 786–99

Yoshimura und Chancellor 2002 YOSHIMURA, N. ; CHANCELLOR, M. B.: Current and future pharmacological treatment for overactive bladder.
In: J Urol
168 (2002), Nr. 5, S. 1897–913

  Deutsche Version: Nebenwirkungen und Dosierung von Fesoterodin

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