Drug reference

Tolterodine

Antimuscarinic · Urinary antispasmodic

Also known as tolterodine tartrate

AntimuscarinicUrinary antispasmodic

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

4 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

Potassium ChlorideSevereDatabaseDDInter
Potassium CitrateSevereDatabaseDDInter
TopiramateSevereDatabaseDDInter
ZonisamideSevereDatabaseDDInter

Mechanism

Tolterodine is an anticholinergic drug, exerting antimuscarinic effects. Its use contributes to the overall anticholinergic burden, which can lead to cognitive impairment.

Indications

Urgency incontinence (considered after bladder training has been trialled, especially when frequency is a problem and symptoms persist)Overactive bladderOveractive bladder with urinary frequency and urgency

Dosing

Adult: Lower initial doses recommended for patients with low CYP2D6 activity
Hepatic adjustment: Dose should be halved in patients receiving CYP3A4 inhibitors (erythromycin, ketoconazole, etc.)
Geriatric: Treatment should be reviewed every 6 months for women over 75 years of age. Clinicians should consider total anticholinergic load, coexisting conditions (such as cognitive impairment or poor bladder emptying), and the risk of side-effects when prescribing anticholinergic medicine. Refer to 'Dementia p. 315' when prescribing in patients with dementia.

Pharmacokinetics

Bioavailability

EM: 26 ± 18%; PM: 91 ± 40%

Protein binding

T: 96.3%; 5-HM: 64%

Metabolism

Metabolized by CYP2D6 to 5-hydroxymethyltolterodine (an active metabolite)

Excretion

EM: Negligible; PM: <2.5%

Contraindications

Cognitive impairment
Poor bladder emptying
When anticholinergic treatment is contra-indicated (mirabegron may be considered as an alternative in such cases)

Side effects

Common

Cognitive impairmentXerostomiaBlurred visionConstipationGastrointestinal discomfortDrowsinessDizzinessConfusionLess likely to cause dryness of mouth and other anticholinergic side effects compared to non-selective agents