What is Detrol LA (Tolterodine Tartrate)? What Is It Used For?

Detrol LA is a prescription medication used to treat the symptoms of Overactive Bladder and Urge Incontinence. It can be used alone or in combination with other drugs. Detrol LA belongs to a class of drugs called Anticholinergics, Genitourinary. It is not known if it is safe and effective in children.

What Are the Possible Side Effects of Detrol LA?

Detrol LA can cause serious side effects including:

  • chest pain, fast or irregular heart rate
  • confusion, hallucinations
  • urinating less than usual or not urinating at all
  • painful or difficult urination
  • dry mouth, headache
  • blurred vision, dizziness, drowsiness
  • constipation, diarrhea, stomach pain

Tell your doctor if you have any side effects that bother you or do not go away.

What are the indications?

Detrol LA Capsules are indicated for the treatment of overactive bladder with symptoms of urinary incontinence, urgency and frequency.

What are the dosage and usage recommendations?

The recommended dose of Detrol LA Capsules is 4 mg once a day, swallowed whole with water. The dose may be reduced to 2 mg per day depending on individual response and tolerability; however, limited efficacy data are available for Detrol LA 2 mg.

The recommended dose of Detrol LA for patients with mild to moderate hepatic impairment or severe renal impairment is 2 mg once daily. Detrol LA is not recommended for use in patients with severe hepatic impairment.

What are the Storage Conditions?

Detrol LA should be stored at 20°–25°C (68°–77°F) and out of reach of children; can be found outside up to 15–30°C (59–86°F). It should be protected from light and stored in a dry place.

Warnings and Precautions

Angioedema: Anaphylaxis and angioedema requiring hospitalization and emergency medical treatment may occur with the first or subsequent doses of Detrol LA. In case of difficulty in breathing, upper airway obstruction or drop in blood pressure, Detrol LA should be discontinued and appropriate treatment instituted immediately.

Urinary Retention: Detrol LA Capsules should be administered with caution to patients with clinically significant bladder outlet obstruction due to the risk of urinary retention.

gastrointestinalspousetinal Disorders: Due to the risk of gastric retention, Detrol LA should be administered with caution in patients with gastrointestinal obstructive disorders. Detrol LA, like other antimuscarinic drugs, may reduce gastrointestinal motility and should be used with caution in conditions associated with decreased gastrointestinal motility.

Narrow Angle Glaucoma: Detrol LA should be administered with caution in patients treated for narrow-angle glaucoma.

Central Nervous System Effects: Detrol LA is associated with anticholinergic, central nervous system (CNS) effects. Patients should be monitored for signs of anticholinergic CNS effects, especially after initiating therapy or increasing the dose. Patients should be advised not to operate heavy machinery until the effects of the drug have been determined. If a patient experiences anticholinergic CNS effects, dose reduction or discontinuation of the drug should be considered.

Liver failure: The clearance of orally administered tolterodine immediate release is significantly lower in cirrhotic patients than in healthy subjects. The recommended dose of Detrol LA for patients with mild to moderate hepatic impairment is 2 mg once daily. Detrol LA is not recommended for use in patients with severe hepatic impairment.

Kidney failure: Renal failure can significantly alter the regulation of tolterodine and its metabolites. In patients with severe renal impairment, the dose of Detrol LA should be reduced to 2 mg once daily. Patients with CCr<10 mL/min have not been studied and the use of Detrol LA is not recommended in this population.

Myasthenia Gravis: Detrol LA should be administered with caution in patients with myasthenia gravis, a disease characterized by decreased cholinergic activity at the neuromuscular junction.

Use in Patients with Congenital or Acquired QT Prolongation: Caution should be exercised in clinical decisions to prescribe Detrol LA to patients with a known history of QT prolongation or to patients taking Class IA or Class III antiarrhythmic drugs.

Pregnancy: There are no studies of tolterodine in pregnant women.

Breastfeeding Period: It is not known whether tolterodine is excreted in human milk. In nursing mothers, a decision should be made whether to continue breastfeeding or to continue Detrol LA.

Pediatric Use: Efficacy in the pediatric population has not been demonstrated.

Geriatric Use: No overall differences in safety were observed between elderly and younger patients treated with tolterodine. However, no overall differences in safety were observed between elderly and younger patients using tolterodine in controlled clinical studies; therefore, no dose adjustment of tolterodine is recommended for elderly patients.

What should be done in case of overdose?

Overdose of Detrol LA Capsules can cause potentially serious central anticholinergic effects and should be treated accordingly. In case of overdose, ECG monitoring is recommended.

What are the contraindications?

Detrol LA is contraindicated in patients with urinary retention, gastric retention or uncontrolled narrow-angle glaucoma.

Detrol LA is contraindicated in patients with known hypersensitivity to the drug or its components, or to fesoterodine fumarate extended-release tablets that are metabolized to 5-hydroxymethyl tolterodine, such as Detrol LA.

Movement Mechanism

Tolterodine acts as a competitive antagonist of acetylcholine at postganglionic muscarinic receptors. Both bladder contraction and salivation are mediated by cholinergic muscarinic receptors. After oral administration, tolterodine is metabolized in the liver to form the main pharmacologically active metabolite, 5-hydroxymethyl tolterodine (5-HMT). Exhibiting an antimuscarinic activity similar to that of tolterodine, 5-HMT contributes significantly to the therapeutic effect. Both tolterodine and 5-HMT exhibit high specificity for muscarinic receptors, as they both show negligible activity or affinity for other potential cellular targets such as other neurotransmitter receptors and calcium channels. Food has no effect on the pharmacokinetics of tolterodine extended release.

Tolterodine is extensively metabolized by the liver following oral dosing. The primary metabolic pathway involves the oxidation of the 5-methyl group and is mediated by cytochrome P450 2D6 (CYP2D6) leading to the formation of 5-HMT, a pharmacologically active metabolite. Following administration of tolterodine solution, 77% of the radioactivity is recovered in the urine and 17% in the faeces within 7 days.

What are the Required Information for Safe and Effective Use?

Medications are sometimes prescribed for conditions not covered in the patient information leaflet. Detrol LA should only be used as directed by the doctor and should not be shared with others, even if they have the same symptoms.

Source: Detrol LA (Tolterodine Tartrate) Drug, 2020

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