Tolterodine
- Atc Codes:G04BD07
- CAS Codes:124937-51-5#124937-52-6
- PHARMGKB ID:124937-51-5#124937-52-6
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Detrusitol, Tolterodin; Belgium: Detrusitol; Bulgaria: Detrusitol; Cyprus: Detrusitol; Czech Republic: Detrusitol, Tolterodine, Uroflow; Denmark: Detrusitol; Estonia: Detrusitol, Tolterodine, Uroflow; Finland: Detrusitol; France: Detrusitol; Germany: Detrusitol, Tolterodin; Greece: Detrusitol; Hungary: Detrusitol, Incontev, Tolterodin; Ireland: Detrusitol; Italy: Detrusitol; Latvia: Detrusitol, Uroflow; Lithuania: Detrusitol, Tolterodine, Uroflow; Malta: Detrusitol, Tolterodine; Netherlands: Detrusitol, Tolterodinetartraat; Poland: Detrusitol, Tolterodine, Uroflow; Portugal: Detrusitol, Tolterrodina; Romania: Detrusitol, Tolterodina, Uroflow; Slovakia: Detrusitol, Uroflow; Slovenia: Detrusitol; Spain: Detrusitol, Urotrol; Sweden: Detrusitol, Detsel, Protol, Tolterodin, Tolterodine; UK: Detrusitol.
North America
Canada: Detrol; USA: Detrol.
Latin America
Argentina: Breminal, Coli-Q, Detrusitol, Toltem, Urginol; Brazil: Detrusitol; Mexico: Detrusitol.
Asia
Japan: Detrusitol.
Drug combinations
Chemistry
Tolterodine: C~22~H~31~NO. Mw: 325.49. (+)-(R)-2-[α-[2-(Diisopropylamino)ethyl]benzyl]-p-cresol. CAS-124937-51-5 (1997).
Tolterodine Tartrate: C~22~H~31~NO C~4~H~6~O~6~. Mw: 475.57. (1)(R)-2-[3-[Bis(1-methylethyl)amino]-1-phenylpropyl]-4-methylphenol [R-(R*,R*)]-2,3-dihydroxybutanedioate (1:1); (2)(+)-(R)-2-[I-[2-(Diisopropylamino)ethyl]benzyl]-p-cresol L-tartrate (1:1). CAS-124937-52-6 (1997).
Pharmacologic Category
Genitourinary Smooth Muscle Relaxants. Anticholinergic Agent. (ATC-Code: G04BD07).
Mechanism of action
A competitive antagonist of muscarinic receptors. In animal models, tolterodine demonstrates selectivity for urinary bladder receptors over salivary receptors. Urinary bladder contraction mediated by muscarinic receptors. Tolterodine increases residual urine volume and decreases detrusor muscle pressure.
Therapeutic use
Treatment of overactive bladder with symptoms of urinary frequency, urgency, or urge incontinence.
Pregnancy and lactiation implications
Teratogenic effects observed in some animal studies. There are no adequate, well-controlled studies in pregnant women. Use during pregnancy only if potential benefit to mother outweighs possible risk to fetus. Excretion in breast milk unknown (not recommended in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to tolterodine or any component of the formulation. Urinary retention. Gastric retention. Uncontrolled narrow-angle glaucoma.
Warnings and precautions
Use with caution in bladder flow obstruction (may increase risk of urinary retention), and in renal impairment. May cause drowsiness and/or blurred vision. Use with caution in decreased GI motility or GI obstructive disorders (may increase risk of gastric retention). Associated with QTc prolongation at high (supratherapeutic) doses. Use caution in congenital prolonged QT or in patients receiving concurrent therapy with QTc-prolonging drugs (class Ia or III antiarrhythmics). Individuals who are CYP2D6 poor metabolizers or in presence of inhibitors of CYP2D6 and CYP3A4 may be more likely to exhibit prolongation. Use with caution in controlled (treated) narrow-angle glaucoma, in hepatic impairment, and in myasthenia gravis.