tolterodine

Therapeutic Classification: urinary tract antispasmodics

Pharmacologic Classification: anticholinergics

Indications ⬆ ⬇

REMS

Overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence.

Action ⬆ ⬇

Acts as a competitive muscarinic receptor antagonist resulting in inhibition of cholinergically mediated bladder contraction.

Therapeutic effects:

Decreased urinary frequency, urgency, and urge incontinence.

Pharmacokinetics ⬆ ⬇

Absorption: Well absorbed (77%) following oral administration.

Distribution: Extensively distributed to tissues.

Protein Binding: 96.3%.

Metabolism/Excretion: Extensively metabolized by the liver, via the CYP2D6 isoenzyme; (the CYP2D6 enzyme system exhibits genetic polymorphism; ∼7% of population may be poor metabolizers and may have significantly ↑ tolterodine concentrations and an ↑ risk of adverse effects); one metabolite (5-hydroxymethyltolterodine) is active; other metabolites are excreted in urine.

Half-Life: Tolterodine: 1.9–3.7 hr; 5-hydroxymethyltolterodine: 2.9–3.1 hr.

Time/Action Profile ⬆ ⬇

(effects on bladder function)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	unknown	12 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to tolterodine or fesoterodine;
Urinary retention;
Gastric retention;
Severe hepatic impairment;
End-stage renal disease (CCr <10 mL/min);
Uncontrolled angle-closure glaucoma;
Lactation: Lactation.

Use Cautiously in:

GI obstructive disorders, including pyloric stenosis (↑ risk of gastric retention);
Significant bladder outflow obstruction (↑ risk of urinary retention);
Controlled angle-closure glaucoma;
Myasthenia gravis;
Mild to moderate hepatic impairment (↓ dose);
Severe renal impairment (CCr 10–30 mL/min) (↓ dose);
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

EENT: blurred vision, dry eyes

GI: dry mouth, constipation, dyspepsia

Neuro: dizziness, headache, sedation

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A4 inhibitors, including erythromycin, clarithromycin, cyclosporine, itraconazole, ketoconazole, and vinblastine, may ↑ levels and the risk of toxicity.

Route/Dosage ⬆ ⬇

Immediate-Release Tablets

PO (Adults ): 2 mg twice daily; may be lowered depending on response; Concurrent use of strong CYP3A4 inhibitors: 1 mg twice daily.
PO (Adults ): Mild to moderate hepatic impairment or severe renal impairment (CCr 10–30 mL/min): 1 mg twice daily.

Extended-Release Capsules

PO (Adults ): 4 mg once daily; may be lowered depending on response; Concurrent use of strong CYP3A4 inhibitors: 2 mg once daily.
PO (Adults ): Mild to moderate hepatic impairment or severe renal impairment (CCr 10–30 mL/min): 2 mg once daily.

Availability ⬆ ⬇

(Generic available)

Extended-release capsules: 2 mg; 4 mg
Tablets: 1 mg; 2 mg

Assessment ⬆ ⬇

Assess patient for urinary urgency, frequency, and urge incontinence periodically during therapy.
Monitor for signs and symptoms of anaphylaxis and angioedema (difficulty breathing, upper airway obstruction, fall in BP, rash, swelling of face or neck). Have emergency equipment readily available.

Implementation ⬆ ⬇

PO: Administer without regard to food.
- DNC: Extended-release capsules should be swallowed whole; do not open, crush, dissolve, or chew.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take tolterodine as directed.
May cause dizziness and blurred vision. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Instruct patient to notify health care professional immediately if rash or signs and symptoms of anaphylaxis or angioedema occur.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Pronunciation ⬇

Classifications ⬆ ⬇