DETRUSITOL 2/MG TAB 28/TAB

Indications

Approved Uses

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

Dosage & Administration

Dosing by Condition

Overactive bladder (adults, immediate‑release tablets): 2 mg twice daily; may reduce to 1 mg twice daily based on tolerability/impairment. (Extended‑release capsule: 4 mg once daily; may reduce to 2 mg once daily.)

Initial Dose

2 mg twice daily

Maintenance Dose

1mg to 2mg twice daily.

Maximum Dose

4mg per day (as 2mg twice daily).

Children's Dosage

Not approved for children.

Dose Adjustment Notes

Reduce to 1 mg twice daily in severe renal impairment (CrCl 10-30 mL/min) or hepatic impairment; also use 1 mg twice daily when co‑administered with potent CYP3A4 inhibitors (especially in poor CYP2D6 metabolizers).

How to Take

Swallow the 2 mg film‑coated tablet whole with water; may be taken with or without food; take twice daily at consistent times as prescribed.

Side Effects

Common Side Effects

Dry mouth, constipation, headache, dizziness, dry eyes, blurred vision, dyspepsia, abdominal pain, fatigue, somnolence

Side Effect Frequency

Very common (>10%): dry mouth. Common (1-10%): constipation, headache, dizziness, somnolence/drowsiness, blurred vision, dry eyes, dyspepsia/abdominal pain. Uncommon/rare: urinary retention, palpitations/tachycardia, peripheral edema, cognitive/psychiatric effects (confusion, hallucinations), hypersensitivity including angioedema.

Safety & Warnings

Contraindications

Contraindications: urinary retention; gastric retention; uncontrolled narrow-angle glaucoma; hypersensitivity to tolterodine (or excipients).

Warnings & Precautions

Use caution in bladder outlet obstruction (risk urinary retention); GI obstructive disorders/constipation risk; controlled narrow‑angle glaucoma; renal impairment; hepatic impairment; patients at risk for QT prolongation (congenital/acquired QT prolongation, electrolyte abnormalities, or concomitant QT‑prolonging drugs); and in older adults due to cognitive/CNS anticholinergic effects.

Age Restriction

Pediatric use: safety and efficacy have not been established; not recommended in patients <18 years.

Driving Warning

May Cause Drowsiness

Drug Interactions

Drug Interactions

Major: strong CYP3A4 inhibitors (e.g., ketoconazole/itraconazole, clarithromycin, ritonavir) increase tolterodine exposure-dose reduction/avoidance may be needed; Moderate: other anticholinergics (additive effects), QT‑prolonging drugs (additive QT risk); CYP2D6 inhibitors (e.g., fluoxetine/paroxetine) can increase tolterodine exposure mainly in CYP2D6 poor metabolizers; may reduce effect of prokinetics (e.g., metoclopramide).

Interaction Severity

MAJOR: Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin/erythromycin, ritonavir) ↑ tolterodine exposure-dose reduction/avoid; additive QT‑prolongation risk with QT‑prolonging drugs in susceptible patients. MODERATE: Other anticholinergics (additive anticholinergic toxicity); CYP2D6 inhibitors may alter metabolite/parent exposure. MINOR: May reduce effect of prokinetics/cholinesterase inhibitors.

Food Interaction

May be taken with or without food; avoid/limit grapefruit or grapefruit juice if possible due to potential CYP3A4 inhibition increasing exposure.

Special Populations

Children

Not approved for children.

Elderly

No specific dose adjustment required based on age alone; however, start at 1 mg twice daily in frail elderly patients due to increased sensitivity to anticholinergic effects; monitor for cognitive impairment and urinary retention

Kidney Impairment

Severe renal impairment (CrCl 10-30 mL/min): reduce to 1 mg twice daily; CrCl <10 mL/min: not recommended/avoid; CrCl >30 mL/min: no adjustment.

Liver Impairment

Mild-moderate hepatic impairment: reduce to 1 mg twice daily; severe hepatic impairment: not recommended/avoid.

Storage & Patient Advice

Missed Dose

Take as soon as remembered; skip if it is almost time for the next dose; do not double the dose

Stopping the Medicine

May be stopped without tapering; advise patient to consult prescriber and expect OAB symptoms may recur after stopping.

Overdose

Overdose: anticholinergic toxicity (e.g., mydriasis/blurred vision, dry mouth, tachycardia, agitation/confusion/hallucinations, urinary retention) and possible QT prolongation; management is supportive (airway/ventilation, IV fluids, benzodiazepines for agitation/seizures), consider activated charcoal if early, ECG monitoring, and physostigmine may be considered in severe central anticholinergic syndrome under expert supervision.

Patient Counseling

Take exactly as prescribed (usually 2 mg twice daily); swallow whole; may take with or without food. Common effects: dry mouth/constipation-use sugar‑free gum/sips of water and maintain fiber/fluids. Use caution driving if blurred vision/dizziness occurs; avoid alcohol if it worsens drowsiness. Seek care for difficulty urinating/urinary retention, severe constipation, palpitations, or allergic reaction. Tell your clinician about other medicines (especially strong CYP3A4 inhibitors/QT‑prolongers). Store below 25°C (SFDA).

Monitoring Requirements

Monitor for urinary retention and worsening constipation; monitor anticholinergic CNS effects (confusion) especially in older adults; consider ECG/QT risk assessment in patients with risk factors or on QT‑prolonging drugs; monitor renal/hepatic function when impairment is present for dosing.

Pharmacology

Mechanism of Action

Competitive muscarinic receptor antagonist in the bladder (functional M3 blockade; nonselective), reducing detrusor overactivity, increasing bladder capacity, and decreasing urgency/frequency.

Onset of Action

Symptom improvement typically begins within days to 1-2 weeks; maximal benefit often requires ~4-8 weeks.

Duration of Effect

Immediate‑release tablets provide roughly 12‑hour symptom control per dose (supports twice‑daily dosing).

Half-Life

Tolterodine immediate-release: ~2-3 hours in extensive (CYP2D6) metabolizers and ~10 hours in poor metabolizers; active 5-hydroxymethyl metabolite (5-HMT): ~3 hours.

Bioavailability

Oral bioavailability is CYP2D6‑dependent: ~17% in extensive metabolizers and ~65% in poor metabolizers; food may increase Cmax but does not require dose adjustment.

Metabolism

Extensively hepatic: primarily CYP2D6 to the active 5-hydroxymethyl metabolite (5-HMT); in CYP2D6 poor metabolizers, CYP3A4 becomes the main pathway (forming inactive metabolites).

Excretion

Approximately 77% excreted in urine and ~17% in feces, predominantly as metabolites; <1% excreted unchanged in urine.

Product Information

Available Dosage Forms

Film‑coated tablet (immediate‑release); extended‑release capsule (tolterodine LA) exists as a separate dosage form in clinical use.

Composition per Dose

Each film-coated tablet: 2 mg tolterodine as tolterodine tartrate

Generic Availability

Yes

OTC Alternatives

No OTC alternative

Urological Condition

Overactive Bladder

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