Tolterodine

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[edit] BRAND NAMES

[edit] STRUCTURE

Tolterodine.jpg

[edit] MECHANISM OF ACTION

Tolterodine is a muscarinic receptor antagonist that shows in vivo selectivity for the urinary bladder over salivary glands, compared with oxybutynin. A major active metabolite, the 5-hydroxymethyl tolterodine (5-HMT), has a similar pharmacological profile.

In patients with overactive bladder, characterised by involuntary bladder contractions and symptoms such as urgency, frequency, and nocturia, with or without urge incontinence, Tolterodine relaxes bladder smooth muscle and increases maximum urinary bladder capacity and thus, reduces the number of urge incontinence episodes.

[edit] INDICATIONS

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

[edit] DOSAGE

  • Extended release capsules (Detrol® LA): 4 mg capsules taken orally once daily with water and swallowed whole.
    In the presence of mild to moderate hepatic impairment, severe renal impairment, drugs that are potent CYP3A4 inhibitors: 2 mg capsules taken orally once daily with water and swallowed whole

[edit] CONTRAINDICATIONS

  • Hypersensitivity to Tolterodine or to fesoterodine.
  • Tolterodine is contraindicated in patients with urinary retention, severe decreased gastrointestinal motility conditions, uncontrolled narrow-angle glaucoma.

[edit] WARNINGS AND PRECAUTIONS

*Anaphylaxis and angioedema requiring hospitalization and emergency medical treatment have occurred with the first or subsequent doses of Tolterodine. In the event of difficulty in breathing, upper airway obstruction, or fall in blood pressure, the drug should be discontinued and appropriate therapy promptly provided.

  • Tolterodine should be administered with caution to patients with gastrointestinal obstructive disorders because of the risk of gastric retention
  • Because Tolterodine may produce drowsiness, somnolence, or blurred vision, patients should be advised to exercise caution when driving or using machinery
  • Urinary Retention: Use caution in patients with clinically significant bladder outflow obstruction because of the risk of urinary retention.
  • Myasthenia gravis: Use with caution in patients with myasthenia gravis, a disease characterized by decreased cholinergic activity at the neuromuscular junction.
  • Controlled Narrow-Angle Glaucoma: use caution in patients being treated for narrow-angle glaucoma.
  • QT Prolongation: Tolterodine should be used with caution in patients with risk factors for QT prolongation or to patients who are taking Class IA (e.g., quinidine, procainamide) or Class III (e.g., amiodarone, sotalol) antiarrhythmic medications

[edit] INTERACTIONS

  • Potent CYP3A4 Inhibitors such as itraconazole, erythromycin and clarithromycin: Coadministration may increase systemic exposure to Tolterodine. Reduce Tolterodine dose to 2 mg once daily.
  • The concomitant use of Tolterodine with other anticholinergic drugs may increase the frequency or severity of dry mouth, constipation and drowsiness.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US): Tolterodine should be used during pregnancy only if the potential benefit for the mother justifies the potential risk to the fetus.
  • Nursing mothers: Tolterodine should not be administered during nursing.

[edit] SIDE EFFECTS

The most common adverse reactions (incidence >4% and >placebo) were dry mouth, headache, constipation, and abdominal pain.

[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