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Chemical Compound Review

SureCN580446     2-[3-(dipropan-2-ylamino)-1- phenyl-propyl]...

Synonyms: SureCN820421, ACMC-1BZ12, AG-D-52853, BSPBio_002725, KBioGR_001641, ...
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Disease relevance of tolterodine


Psychiatry related information on tolterodine


High impact information on tolterodine

  • The enzyme 25-hydroxylated vitamin D(3), 1 alpha-hydroxyvitamin D(3) and vitamin D(2) and also converted tolterodine, a substrate for human CYP2D6, into its 5-hydroxymethyl metabolite [8].
  • The pharmacokinetics of tolterodine and 5-hydroxymethyl metabolite were determined, and the pharmacodynamic were measured [9].
  • Tolterodine caused a similar decrease in salivation in both panels [9].
  • CONCLUSIONS: Changes in pH affected the release of tolterodine from ER-tolterodine, while they had no effect on the release of oxybutynin from the proprietary ER technology used in ER-oxybutynin [10].
  • Tolterodine is metabolised via CYP2D6 to the active metabolite 5-hydroxymethyl-tolterodine and via CYP3A to N-dealkylated metabolites [11].

Chemical compound and disease context of tolterodine


Biological context of tolterodine


Anatomical context of tolterodine

  • Tolterodine shows functional selectivity for the bladder over the salivary glands in vivo, which is not attributable to muscarinic receptor subtype selectivity [20].
  • Also, muscarinic receptor binding affinity of oxybutynin and its metabolite N-desethyl-oxybutynin in the cerebral cortex compared with that in the bladder was 2 to 3 times higher, whereas that of tolterodine and 5-hydroxymethyl metabolite was approximately 2 times lower [13].
  • CONCLUSIONS: Compared with oxybutynin, tolterodine, 5-HM and DPr-P-4(N-->O) may bind more selectively to muscarinic receptors in the human bladder than in the parotid gland [21].
  • CONCLUSIONS: These results suggest that at low doses tolterodine exerts an inhibitory effect on C-fiber bladder afferent nerves, thereby, improving BC during the storage phase [22].
  • Tolterodine and 5-HM were 2-fold more potent for inhibiting specific [(3)H]NMS binding at cell membranes expressing the M(2) vs the M(3) subtype [21].

Associations of tolterodine with other chemical compounds

  • Based upon the nonselective tolterodine, the highly M(2)-selective (R)-4-[2-[3-(4-methoxy-benzoylamino)-benzyl]-piperidin-1-ylmethyl]piperidine-1-carboxylic acid amide (Ro-320-6206), and the highly M(3)-selective darifenacin and 3-(1-carbamoyl-1,1-diphenylmethyl)-1-(4-methoxyphenylethyl)pyrrolidine (APP), contraction occurs via M(3) receptors [23].
  • CONCLUSION: The study demonstrates comparable efficacy, tolerability, and improvement in the quality of life of 15 mg propiverine twice-daily and 2mg tolterodine twice-daily in the treatment of the symptoms of idiopathic detrusor overactivity [15].
  • METHODS: Twelve healthy male volunteers (eight extensive metabolisers [EMs] and four poor metabolisers [PMs] with respect to CYP2D6) received 4 mg tolterodine L-tartrate orally twice daily for 6 days [24].
  • RESULTS: Several anticholinergic drugs are available for the treatment of OAB, including oxybutymn, tolterodine, trospium chloride, and propiverine (not available in the United States) [25].
  • Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of oxybutynin and tolterodine [26].

Gene context of tolterodine


Analytical, diagnostic and therapeutic context of tolterodine


  1. Therapeutic opportunities from muscarinic receptor research. Eglen, R.M., Choppin, A., Watson, N. Trends Pharmacol. Sci. (2001) [Pubmed]
  2. Combination treatment with an alpha-blocker plus an anticholinergic for bladder outlet obstruction: a prospective, randomized, controlled study. Athanasopoulos, A., Gyftopoulos, K., Giannitsas, K., Fisfis, J., Perimenis, P., Barbalias, G. J. Urol. (2003) [Pubmed]
  3. Tolterodine extended release attenuates lower urinary tract symptoms in men with benign prostatic hyperplasia. Kaplan, S.A., Walmsley, K., Te, A.E. J. Urol. (2005) [Pubmed]
  4. Tolterodine treatment for children with symptoms of urinary urge incontinence suggestive of detrusor overactivity: results from 2 randomized, placebo controlled trials. Nijman, R.J., Borgstein, N.G., Ellsworth, P., Djurhuus, J.C. J. Urol. (2005) [Pubmed]
  5. Tolterodine and memory: dry but forgetful. Womack, K.B., Heilman, K.M. Arch. Neurol. (2003) [Pubmed]
  6. Safety profile of tolterodine as used in general practice in England: results of prescription-event monitoring. Layton, D., Pearce, G.L., Shakir, S.A. Drug safety : an international journal of medical toxicology and drug experience. (2001) [Pubmed]
  7. Failure of tolterodine to treat clozapine-induced nocturnal enuresis. English, B.A., Still, D.J., Harper, J., Saklad, S.R. The Annals of pharmacotherapy. (2001) [Pubmed]
  8. Porcine microsomal vitamin D(3) 25-hydroxylase (CYP2D25). Catalytic properties, tissue distribution, and comparison with human CYP2D6. Hosseinpour, F., Wikvall, K. J. Biol. Chem. (2000) [Pubmed]
  9. Influence of CYP2D6 polymorphism on the pharmacokinetics and pharmacodynamic of tolterodine. Brynne, N., Dalén, P., Alván, G., Bertilsson, L., Gabrielsson, J. Clin. Pharmacol. Ther. (1998) [Pubmed]
  10. Effect of antacid on the pharmacokinetics of extended-release formulations of tolterodine and oxybutynin. Sathyan, G., Dmochowski, R.R., Appell, R.A., Guo, C., Gupta, S.K. Clinical pharmacokinetics. (2004) [Pubmed]
  11. Clinical pharmacokinetics of drugs used to treat urge incontinence. Guay, D.R. Clinical pharmacokinetics. (2003) [Pubmed]
  12. Oxybutynin extended-release: a review of its use in the management of overactive bladder. Siddiqui, M.A., Perry, C.M., Scott, L.J. Drugs (2004) [Pubmed]
  13. Comparative evaluation of central muscarinic receptor binding activity by oxybutynin, tolterodine and darifenacin used to treat overactive bladder. Oki, T., Kageyama, A., Takagi, Y., Uchida, S., Yamada, S. J. Urol. (2007) [Pubmed]
  14. Therapeutic efficacy of extended release oxybutynin chloride, and immediate release and long acting tolterodine tartrate in children with diurnal urinary incontinence. Reinberg, Y., Crocker, J., Wolpert, J., Vandersteen, D. J. Urol. (2003) [Pubmed]
  15. Propiverine versus tolterodine: efficacy and tolerability in patients with overactive bladder. Jünemann, K.P., Halaska, M., Rittstein, T., Mürtz, G., Schnabel, F., Brünjes, R., Nurkiewicz, W. Eur. Urol. (2005) [Pubmed]
  16. A comparison of the effects on saliva output of oxybutynin chloride and tolterodine tartrate. Chancellor, M.B., Appell, R.A., Sathyan, G., Gupta, S.K. Clinical therapeutics. (2001) [Pubmed]
  17. Food does not influence the pharmacokinetics of a new extended release formulation of tolterodine for once daily treatment of patients with overactive bladder. Olsson, B., Szamosi, J. Clinical pharmacokinetics. (2001) [Pubmed]
  18. Multiple dose pharmacokinetics of a new once daily extended release tolterodine formulation versus immediate release tolterodine. Olsson, B., Szamosi, J. Clinical pharmacokinetics. (2001) [Pubmed]
  19. Safety and tolerability of tolterodine for the treatment of overactive bladder in men with bladder outlet obstruction. Abrams, P., Kaplan, S., De Koning Gans, H.J., Millard, R. J. Urol. (2006) [Pubmed]
  20. Tolterodine. Hills, C.J., Winter, S.A., Balfour, J.A. Drugs (1998) [Pubmed]
  21. Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder. Maruyama, S., Oki, T., Otsuka, A., Shinbo, H., Ozono, S., Kageyama, S., Mikami, Y., Araki, I., Takeda, M., Masuyama, K., Yamada, S. J. Urol. (2006) [Pubmed]
  22. Effects of tolterodine on an overactive bladder depend on suppression of C-fiber bladder afferent activity in rats. Yokoyama, O., Yusup, A., Miwa, Y., Oyama, N., Aoki, Y., Akino, H. J. Urol. (2005) [Pubmed]
  23. Signal transduction underlying carbachol-induced contraction of human urinary bladder. Schneider, T., Fetscher, C., Krege, S., Michel, M.C. J. Pharmacol. Exp. Ther. (2004) [Pubmed]
  24. Tolterodine does not affect the human in vivo metabolism of the probe drugs caffeine, debrisoquine and omeprazole. Brynne, N., Böttiger, Y., Hallén, B., Bertilsson, L. British journal of clinical pharmacology. (1999) [Pubmed]
  25. Central nervous system safety of anticholinergic drugs for the treatment of overactive bladder in the elderly. Scheife, R., Takeda, M. Clinical therapeutics. (2005) [Pubmed]
  26. Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of oxybutynin and tolterodine. Dmochowski, R., Chen, A., Sathyan, G., MacDiarmid, S., Gidwani, S., Gupta, S. Journal of clinical pharmacology. (2005) [Pubmed]
  27. Tolterodine, a new muscarinic receptor antagonist, is metabolized by cytochromes P450 2D6 and 3A in human liver microsomes. Postlind, H., DanielsonA, n.u.l.l., Lindgren, A., Andersson, S.H. Drug Metab. Dispos. (1998) [Pubmed]
  28. The importance of residues in substrate recognition site 3 for the catalytic function of CYP2D25 (vitamin D 25-hydroxylase). Hosseinpour, F., Hidestrand, M., Ingelman-Sundberg, M., Wikvall, K. Biochem. Biophys. Res. Commun. (2001) [Pubmed]
  29. Overactive bladder in the elderly: a guide to pharmacological management. Staskin, D.R. Drugs & aging. (2005) [Pubmed]
  30. Benefit-risk assessment of tolterodine in the treatment of overactive bladder in adults. Garely, A.D., Burrows, L. Drug safety : an international journal of medical toxicology and drug experience. (2004) [Pubmed]
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