DETROL LA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DETROL LA (DETROL LA).

How it works

Tolterodine is a competitive muscarinic receptor antagonist. It blocks acetylcholine binding at muscarinic receptors (M1–M5), reducing detrusor muscle contraction and bladder pressure, thereby increasing bladder capacity and decreasing urinary frequency.

What the body does with it

Metabolism	Primarily hepatic via CYP2D6 and 3A4. Major metabolite: 5-hydroxymethyl tolterodine (desfesoterodine), which is active and contributes to clinical effect. Metabolites are further conjugated and eliminated renally.
Excretion	Approximately 77% eliminated in urine (primarily as metabolites, <1% unchanged) and 17% in feces.
Half-life	Terminal elimination half-life is approximately 7 hours (range 5-10 hours) for the extended-release formulation, allowing once-daily dosing.
Protein binding	Approximately 96% bound to plasma proteins, primarily alpha-1-acid glycoprotein.
Volume of Distribution	Apparent volume of distribution is about 2.7 L/kg, indicating extensive tissue distribution.
Bioavailability	Absolute bioavailability of the extended-release capsule is approximately 4.1% due to extensive first-pass metabolism; relative bioavailability vs immediate-release is 75%.
Onset of Action	Oral extended-release: Therapeutic effect on urinary frequency and urgency is observed within 2-4 weeks of starting therapy.
Duration of Action	24 hours due to extended-release formulation; clinical effects on urodynamic parameters persist for at least 24 hours post-dose.

Classification & Brands

Dosing & administration

4 mg orally once daily; may be reduced to 2 mg once daily based on tolerability.

Dosage form	CAPSULE, EXTENDED RELEASE
Renal impairment	For CrCl 30-89 mL/min: no adjustment recommended. For CrCl <30 mL/min: not recommended (no data).
Liver impairment	Child-Pugh Class A or B: maximum dose 2 mg once daily. Child-Pugh Class C: not recommended.
Pediatric use	Safety and efficacy in pediatric patients (<18 years) have not been established.
Geriatric use	No specific dose adjustment; monitor anticholinergic effects (e.g., constipation, confusion) more frequently. Initial dose may be 2 mg once daily if frail or at risk of adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DETROL LA (DETROL LA).

Breastfeeding	Excretion into human milk unknown; caution advised. M/P ratio not available. Drug may suppress lactation due to anticholinergic effects. Consider benefits of breastfeeding vs. potential infant exposure.
Teratogenic Risk	Pregnancy Category C. First trimester: no adequate studies; potential risk based on animal data showing fetal toxicity at high doses. Second and third trimesters: no well-controlled human studies; risk cannot be ruled out. Drug should be used only if potential benefit justifies potential risk to fetus.

Warnings & precautions

■ FDA Black Box Warning

No FDA black box warning.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to tolterodine or any component.","Urinary retention.","Gastric retention.","Uncontrolled narrow-angle glaucoma.","Severe hepatic impairment."]

Clinical Precautions

Precautions

["QT prolongation (caution in patients with risk factors, electrolyte abnormalities, or concurrent QT-prolonging drugs).","Urinary retention and gastric retention (use with caution in patients with bladder outflow obstruction or decreased GI motility).","Angioedema (discontinue if occurs).","Hepatic impairment (contraindicated in severe impairment; dose reduction in moderate impairment).","Myasthenia gravis (may exacerbate symptoms)."]

Clinical Tips & Counseling

Drug interactions

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DETROL LA

Clinical safety rating: caution

Comprehensive clinical and safety monograph for DETROL LA (DETROL LA).

How it works

What the body does with it

Metabolism	Primarily hepatic via CYP2D6 and 3A4. Major metabolite: 5-hydroxymethyl tolterodine (desfesoterodine), which is active and contributes to clinical effect. Metabolites are further conjugated and eliminated renally.
Excretion	Approximately 77% eliminated in urine (primarily as metabolites, <1% unchanged) and 17% in feces.
Half-life	Terminal elimination half-life is approximately 7 hours (range 5-10 hours) for the extended-release formulation, allowing once-daily dosing.
Protein binding	Approximately 96% bound to plasma proteins, primarily alpha-1-acid glycoprotein.
Volume of Distribution	Apparent volume of distribution is about 2.7 L/kg, indicating extensive tissue distribution.
Bioavailability	Absolute bioavailability of the extended-release capsule is approximately 4.1% due to extensive first-pass metabolism; relative bioavailability vs immediate-release is 75%.
Onset of Action	Oral extended-release: Therapeutic effect on urinary frequency and urgency is observed within 2-4 weeks of starting therapy.
Duration of Action	24 hours due to extended-release formulation; clinical effects on urodynamic parameters persist for at least 24 hours post-dose.

Classification & Brands

Dosing & administration

4 mg orally once daily; may be reduced to 2 mg once daily based on tolerability.

Dosage form	CAPSULE, EXTENDED RELEASE
Renal impairment	For CrCl 30-89 mL/min: no adjustment recommended. For CrCl <30 mL/min: not recommended (no data).
Liver impairment	Child-Pugh Class A or B: maximum dose 2 mg once daily. Child-Pugh Class C: not recommended.
Pediatric use	Safety and efficacy in pediatric patients (<18 years) have not been established.
Geriatric use	No specific dose adjustment; monitor anticholinergic effects (e.g., constipation, confusion) more frequently. Initial dose may be 2 mg once daily if frail or at risk of adverse effects.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for DETROL LA (DETROL LA).

Breastfeeding	Excretion into human milk unknown; caution advised. M/P ratio not available. Drug may suppress lactation due to anticholinergic effects. Consider benefits of breastfeeding vs. potential infant exposure.
Teratogenic Risk	Pregnancy Category C. First trimester: no adequate studies; potential risk based on animal data showing fetal toxicity at high doses. Second and third trimesters: no well-controlled human studies; risk cannot be ruled out. Drug should be used only if potential benefit justifies potential risk to fetus.

Warnings & precautions

■ FDA Black Box Warning

No FDA black box warning.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to tolterodine or any component.","Urinary retention.","Gastric retention.","Uncontrolled narrow-angle glaucoma.","Severe hepatic impairment."]