Tolterodine Tartrate is used for the treatment of overactive bladder with symptoms such as urge urinary incontinence, urgency, and frequent urination.

Tolterodine is a competitive and specific muscarinic receptor antagonist that shows greater selectivity for the urinary bladder than the salivary glands. This effect has been demonstrated in non-clinical pharmacological in vivo studies. Tolterodine has a high specificity for muscarinic receptors. A major active metabolite of tolterodine, known as the 5-hydroxymethyl derivative, has a pharmacological profile similar to the parent drug. In extensive metabolisers, this metabolite contributes significantly to the therapeutic effect of tolterodine. The therapeutic effect of the treatment can usually be expected within 4 weeks.

Extended-release capsule: The recommended dose is Tolterodine Tartrate 4 mg once daily. The dose may be lowered to 2 mg once daily based on individual response and tolerability. For patients with significantly reduced hepatic or renal function or who are currently taking drugs that are potent inhibitors of CYP3A4, the recommended dose is Tolterodine Tartrate 2 mg once daily.

Film-coated tablet: The recommended dose is Tolterodine Tartrate 2 mg twice daily except in patients with impaired liver function or severely impaired renal function (GFR<30 ml/min) for whom the recommended dose is one Tolterodine Tartrate 1 mg tablet twice daily. In case of troublesome side effects, the dose may be reduced from 2 mg to 1 mg twice daily. The effect of treatment should be re-evaluated after 2-3 months.

Pediatric use: The safety and effectiveness of tolterodine in children have not been established.

Geriatric use: No overall differences in safety were observed between the older and younger patients treated with Tolterodine.

Ketoconazole, a CYP3A4 drug-metabolizing enzyme inhibitor, significantly increases plasma concentrations of Tolterodine when co-administered in poor metabolizer patients. For patients receiving Ketoconazole or other strong CYP3A4 inhibitors such as azole antifungals (e.g., Itraconazole, Miconazole), macrolide antibiotics (e.g., Erythromycin, Clarithromycin), Cyclosporine, or Vinblastine, the recommended dose of Tolterodine Tartrate is 2 mg daily.

Tolterodine Tartrate is contraindicated in patients with urinary retention, gastric retention, uncontrolled narrow-angle glaucoma, or in those with known hypersensitivity to Tolterodine Tartrate.

The most common adverse effects reported with Tolterodine Tartrate include dry mouth, headache, constipation, and abdominal pain.
Dry mouth is the most frequently reported adverse event, occurring in 23.4% of patients treated with Tolterodine Tartrate tablets compared to 7.7% in placebo-treated patients. Expected antimuscarinic side effects include dry mouth, constipation, abnormal vision (accommodation disturbances), urinary retention, and dry eyes. Adverse events were reported regardless of causality.

There are no adequate studies in pregnant women; therefore, Tolterodine Tartrate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether Tolterodine is excreted in human milk; therefore, it should not be used during breastfeeding.
A decision should be made whether to discontinue nursing or discontinue Tolterodine Tartrate therapy.

Tolterodine Tartrate should be used with caution in patients with clinically significant bladder outflow obstruction due to risk of urinary retention.
Caution is also required in gastrointestinal obstructive conditions such as pyloric stenosis due to risk of gastric retention, and in patients treated for narrow-angle glaucoma. For patients with significantly reduced hepatic or renal function, the recommended dose is 2 mg daily. QT interval studies have shown a greater effect at 8 mg/day (double the therapeutic dose) compared to 4 mg/day, with a more pronounced effect in CYP2D6 poor metabolizers. Although the QT effect at 8 mg/day was smaller than that observed with moxifloxacin in a 4-day therapeutic study, confidence intervals overlapped. These findings should be considered when prescribing Tolterodine Tartrate to patients with a history of QT prolongation or those taking Class I A antiarrhythmics (e.g., quinidine, procainamide) or Class III antiarrhythmics (e.g., amiodarone, sotalol). Patients should be informed that antimuscarinic agents may cause blurred vision, dizziness, or drowsiness.

Overdose of Tolterodine Tartrate capsules may lead to severe central anticholinergic effects and should be managed accordingly.
ECG monitoring is recommended in cases of overdose.

BPH / Urinary retention / Urinary incontinence

Store in a cool, dry place. Protect from light. Keep out of reach of children.