Therapeutic Classification: urinary tract antispasmodics
Pharmacologic Classification: anticholinergics
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.
(effects on bladder function)
| ROUTE | ONSET | PEAK | DURATION |
|---|
| PO | unknown | unknown | 12 hr |
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.
