title: Tolterodine.
abstract: Tolterodine is a competitive muscarinic receptor antagonist which has recently been launched for the treatment of overactive bladder. Tolterodine shows functional selectivity for the bladder over the salivary glands in vivo, which is not attributable to muscarinic receptor subtype selectivity. It is as potent as oxybutynin in inhibiting bladder contraction, but is much less potent in inhibiting salivation, suggesting that it may have less propensity to cause dry mouth in clinical use. In patients with overactive bladder, toleterodine significantly reduces the frequency of micturition and number of incontinence episodes, while increasing the average volume voided. The onset of pharmacological action of tolterodine is < 1 hour and therapeutic efficacy is maintained during long term treatment. In comparative trials, tolterodine and oxybutynin are equivalent in terms of efficacy. However, tolterodine is significantly better tolerated than oxybutynin, particularly with respect to the incidence and severity of dry mouth. No clinically relevant ECG changes have been noted with tolterodine.
authors.affiliation: Adis International Limited, Chester, England and Auckland, New Zealand.
authors.forename: C J
authors.initials: CJ
authors.lastname: Hills
authors.forename: S A
authors.initials: SA
authors.lastname: Winter
authors.forename: J A
authors.initials: JA
authors.lastname: Balfour
mesh_terms: D000818:Animals; D001559:Benzhydryl Compounds / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D018680:Cholinergic Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use; D018849:Controlled Clinical Trials as Topic; D003408:Cresols / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006207:Half-Life; D006801:Humans; D066298:In Vitro Techniques; D008333:Mandelic Acids / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use; D018727:Muscarinic Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000627:therapeutic use*; D010665:Phenylpropanolamine; D000068737:Tolterodine Tartrate; D001743:Urinary Bladder / Q000187:drug effects* / Q000378:metabolism; D014549:Urinary Incontinence / Q000188:drug therapy*
chemical_list: D001559:Benzhydryl Compounds; D018680:Cholinergic Antagonists; D003408:Cresols; D008333:Mandelic Acids; D018727:Muscarinic Antagonists; D010665:Phenylpropanolamine; D000068737:Tolterodine Tartrate; C005419:oxybutynin