What is the optimal time of day to administer Detrol (tolterodine)?

Optimal Timing for Detrol (Tolterodine) Administration

Detrol should be administered at bedtime for patients with overactive bladder and nocturnal enuresis, as anticholinergic medications like tolterodine are specifically dosed at bedtime to suppress nighttime detrusor overactivity. 1

Evidence-Based Timing Recommendations

Bedtime Administration for Enuresis and Overactive Bladder

• The International Children's Continence Society guidelines explicitly state that anticholinergics including tolterodine should be given "at bedtime" when used for enuresis treatment. 1
• The usual dose is 2 mg tolterodine at bedtime, though this may need to be doubled depending on response. 1
• The anti-enuretic effect should appear within a maximum of 2 months, and sometimes much earlier. 1

Twice-Daily Dosing for Standard Overactive Bladder Treatment

• For the immediate-release formulation, tolterodine is administered as 2 mg twice daily (morning and evening), which is the standard FDA-approved dosing regimen. 2, 3
• Despite short terminal half-lives of 2-3 hours for tolterodine and 3-4 hours for its active metabolite, twice-daily dosing is effective due to prolonged pharmacodynamic effects. 3
• The majority of patients (85%) prefer and tolerate the 2 mg twice-daily dose over the lower 1 mg twice-daily dose. 4

Once-Daily Extended-Release Formulation

• Tolterodine ER 4 mg can be administered once daily at any consistent time, offering improved convenience and 23% lower rates of dry mouth compared to the immediate-release formulation. 5
• The extended-release formulation demonstrated 18% greater effectiveness in reducing urge incontinence episodes compared to immediate-release tolterodine. 5

Clinical Considerations for Timing

Onset of Action

• Treatment effects begin within 1 week of initiating therapy, with maximum effects occurring after 5-8 weeks of continuous treatment. 2, 4
• Improvements are maintained during long-term treatment for up to 24 months. 2

Important Caveats

• Tolterodine should only be used after nonpharmacological methods have been tried first, including establishing regular voiding habits. 1
• Constipation must be excluded or treated before starting anticholinergic therapy, as it is the most bothersome side effect and may herald decreasing anti-enuretic effect. 1
• Post-void residual urine must be measured via uroflowmetry with ultrasound before initiating treatment, as residual urine may cause urinary tract infections. 1
• Patients must maintain sound voiding habits and report dysuria or unexplained fever immediately. 1

Dosage Adjustments

• Dosage reduction is recommended in hepatic impairment and during concurrent therapy with CYP450 2D6 and 3A4 inhibitors (such as ketoconazole). 3, 6
• No dosage adjustment is needed for elderly patients, as the safety profile is similar across age groups. 6