Elsevier

Life Sciences

Volume 68, Issues 22–23, 27 April 2001, Pages 2549-2556
Life Sciences

Novel theapeutic approache
Clinical experiences with tolterodine

https://doi.org/10.1016/S0024-3205(01)01051-7Get rights and content

Abstract

Tolterodine is the first muscarinic receptor antagonist that has been specifically developed for the treatment of overactive bladder. The objectives in the discovery program were to design a potent muscarinic receptor antagonist that is equipotent to oxybutynin in the bladder, but less potent in salivary glands, with the aim of improving tolerability (less dry mouth) in patients with overactive bladder. Tolterodine is non-selective with respect to the muscarinic M1–M5 receptor subtypes, but has a greater effect on the bladder than on salivary glands in vivo, in both animals and humans. Clinical results show that the efficacy and safety of tolterodine in overactive bladder is equal to that of oxybutynin, but that tolterodine is significantly better tolerated by the patients.

References (0)

Cited by (32)

  • Pharmacokinetic drug interaction study between overactive bladder drugs mirabegron and tolterodine in Japanese healthy postmenopausal females

    2016, Drug Metabolism and Pharmacokinetics
    Citation Excerpt :

    While tolterodine itself has no detectable effect on CYP2D6, CYP3A4, CYP2C19 and CYP1A2 [7], it is known to be a sensitive substrate of CYP2D6. Tolterodine is eliminated primarily by metabolism involving CYP2D6 and CYP3A4 [8,9] and undergoes metabolism to form the 5-hydroxymethyl tolterodine (5-HMT) derivative [10,11], a major metabolite which is pharmacologically active and has equivalent antimuscarinic potency to tolterodine in vitro [12]. Serum concentrations of tolterodine were higher in CYP2D6 poor metabolizers (PMs) than in extensive metabolizers (EMs), and the AUC of tolterodine was increased by 4.8-fold in CYP2D6 EM with fluoxetine 20 mg, which is known as a potent CYP2D6 inhibitor [13].

  • Tolterodine

    2007, xPharm: The Comprehensive Pharmacology Reference
  • High performance liquid chromatography-electrospray ionization mass spectrometric determination of tolterodine tartrate in human plasma

    2005, Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences
View all citing articles on Scopus
View full text