Toltrex is indicated for the management of an overactive bladder associated with symptoms such as:
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Tolterodine is a competitive and selective muscarinic receptor antagonist that primarily targets the urinary bladder, with minimal effect on the salivary glands.
Its action reduces involuntary bladder contractions, increasing bladder capacity and decreasing urgency episodes.
The drug has a high affinity for muscarinic receptors, and its active metabolite (5-hydroxymethyl derivative) contributes significantly to its therapeutic activity—especially in extensive metabolizers.
Clinical improvement is usually noticeable within 4 weeks of treatment.
Extended-Release Capsule:
Recommended dose: 4 mg once daily.
Adjustments: May be reduced to 2 mg once daily based on tolerance and clinical response.
For patients with hepatic or renal impairment or those taking potent CYP3A4 inhibitors (e.g., ketoconazole), the dose should be 2 mg once daily.
Film-Coated Tablet:
Standard dose: 2 mg twice daily.
For patients with severe renal impairment (GFR <30 ml/min) or impaired liver function, use 1 mg twice daily.
If side effects occur, the dose may be lowered to 1 mg twice daily.
The therapeutic response should be reassessed after 2–3 months.
Pediatric Use: Safety and efficacy in children have not been established.
Geriatric Use: No significant difference in safety between older and younger adults.
Co-administration with CYP3A4 inhibitors such as ketoconazole, itraconazole, miconazole, erythromycin, clarithromycin, cyclosporine, or vinblastine may significantly increase Toltrex levels.
In such cases, the dose should be reduced to 2 mg daily.
No adequate studies exist in pregnant women; use only if the potential benefit outweighs the risk.
It is unknown whether Tolterodine is excreted in breast milk; therefore, avoid use during lactation or discontinue breastfeeding during treatment.
Store in a cool, dry place, protected from light and moisture.
Keep out of reach of children.
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