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Tolterodine: Mechanism of Action, Side Effects, Contraindications, and Dosage

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

Mechanism of Action

Tolterodine is a lipophilic tertiary amine with anticholinergic effects on muscarinic receptors. Tolterodine has a certain organ selectivity, leading to a stronger effect on the bladder than on the salivary glands.

The inhibition of M₃ receptors with Tolterodine reduces smooth muscle detrusor contraction, increases functional bladder capacity, and alleviates urgency symptoms. Tolterodine is used to treat overactive bladder, urge incontinence, and neurogenic lower urinary tract dysfunction.

Pharmacokinetics of Tolterodine:

There is a pronounced hepatic metabolism to active metabolites by cytochrome CYP2D6 after oral absorption. Half-life 3–10 hours (depending on CYP2D6 activity and release formulation), mainly renal excretion of the metabolites.

Side Effects of Tolterodine

Muscarinic receptors are present in numerous organs. M₃ receptors are mainly found in smooth muscle and glands. Tolterodine has a certain organ selectivity and may lead to fewer side effects compared to other anticholinergics.

Eye:

• Mydriases
• Disturbed accommodation
• Dry eyes due to 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. Propiverine mitigates the effects of gastrointestinal prokinetics. Ketakonazole and macrolid antibiotics may increase the plasma concentration of Tolterodine.

Contraindications of Tolterodine

• 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 Tolterodine:

Depending on the effect (and side effects), either 1–2 mg twice daily or a extended-release formulation 2–4 mg once daily.

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 Tolterodin

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