Dosing and uses of Detrol, Detrol LA (tolterodine)
Adult dosage forms and strengths
tablet, immediate release
- 1mg
- 2mg
capsule, extended release
- 2mg
- 4mg
Overactive Bladder, Urge Incontinence
Immediate release: 2 mg PO q12hr
Extended release: 2-4 mg PO once daily
Dosing Modifications
Renal impairment
- CrCl 10-30 mL/min: Not to exceed 1 mg PO q12hr (immediate release) or 2 mg PO once daily (extended release)
- CrCl <10 mL/min: Not recommended
Hepatic impairment
- Mild to moderate (Child-Pugh class A or B): Not to exceed 1 mg PO q12hr (immediate release) or 2 mg PO once daily (extended release)
- Severe (Child-Pugh class C): Not recommended
Strong CYP3A4 inhibitors
- Not to exceed 1 mg PO q12hr (immediate release) or 2 mg PO once daily (extended release)
Pediatric dosage forms and strengths
Not recommended
Detrol, Detrol LA (tolterodine) adverse (side) effects
>10%
Dry mouth (40%)
1-10%
Blurred vision
Constipation
Dizziness
Drowsiness
Dyspepsia
Headache
Xerophthalmia
Warnings
Contraindications
Urinary or gastric retention
Uncontrolled narrow-angle glaucoma
Hypersensitivity to drug or ingredients or to fesoterodine fumarate, which is metabolized to 5-hydroxymethyl tolterodine
Cautions
Controlled narrow-angle glaucoma, bladder outflow obstruction, gastrointestinal obstruction, hepatic or renal impairment
Anaphylaxis and angioedema necessitating hospitalization and emergency treatment reported with first or subsequent doses
Anticholinergic central nervous system effects (eg, dizziness, somnolence) reported; patients should not drive or operate heavy machinery until they adjust to therapy
Use with caution in patients with myasthenia gravis, which is characterized by decreased cholinergic activity at neuromuscular junction
When coadministered with strong CYP3A4 inhibitors, tolterodine should be given at reduced dosage
Pregnancy and lactation
Pregnancy category: C
Lactation: Unknown whether drug is distributed in breast milk; do not nurse
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Detrol, Detrol LA (tolterodine)
Mechanism of action
Competitive muscarinic receptor antagonist; decreases bladder contractions; is more specific for bladder than oxybutynin
Absorption
Bioavailability: 77%
Onset: Overactive bladder, 1 wk; urge incontinence, 1 hr
Time to peak effect: 2-4 wk
Peak plasma time: Immediate release, 1-2 hr; extended release, 2-6 hr
Distribution
Vd: 113 L
Metabolism
Metabolized in liver by CYP2D6 and (to minor extent) CYP3A4
Metabolites: 5-Hydroxymethyl, dealkylated tolterodine
Elimination
Half-life: Parent drug, 1.9-3.7 hr; active metabolite (5-hydroxymethyl), 3 hr (8.7 hr in cirrhosis)
Total body clearance: 5.7 L/kg/hr
Excretion: Urine (77%), feces (17%)
