Treatment of the overactive bladder syndrome with muscarinic receptor antagonists - A matter of metabolites?

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 374, Issue 2, 2006, Pages 79-85

  Michel, Martin C ^a   Hegde, Sharath S ^b  

^a UNIVERSITY OF AMSTERDAM   (Netherlands)

^b THERAVANCE INC   (United States)

Author keywords

Darifenacin; Drug metabolite; Fesoterodine; Oxybutynin; Propiverine; Solifenacin; Tolterodine; Trospium

Indexed keywords

5 HYDROXYMETHYL TOLTERODINE; DARIFENACIN; DRUG METABOLITE; FESOTERODINE; GLYCOLIC ACID DERIVATIVE; HYDROXYSOLIFENACIN; ITRACONAZOLE; MUSCARINIC RECEPTOR BLOCKING AGENT; N DESALKYL TOLTERODINE; N DESETHYL OXYBUTYNIN; OMEPRAZOLE; OXYBUTYNIN; PHENYLCYCLOHEXYLGLYCOLIC ACID; PNU 200577; PROPIVERINE; SOLIFENACIN; SOLIFENACIN N OXIDE; SPM 7605; TOLTERODINE; TROSPIUM CHLORIDE; UK 148 993; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG EFFICACY; DRUG EXCRETION; DRUG FORMULATION; DRUG MECHANISM; DRUG METABOLISM; DRUG TOLERABILITY; HUMAN; NONHUMAN; OVERACTIVE BLADDER; REVIEW; XEROSTOMIA;

BENZHYDRYL COMPOUNDS; BENZILATES; BENZOFURANS; CRESOLS; HUMANS; MANDELIC ACIDS; MUSCARINIC ANTAGONISTS; NORTROPANES; PARASYMPATHOLYTICS; PHENYLPROPANOLAMINE; PYRROLIDINES; QUINUCLIDINES; TETRAHYDROISOQUINOLINES; URINARY BLADDER, OVERACTIVE;

EID: 33750432148     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00210-006-0105-y     Document Type: Review

References (56)

1. Abrams P, Cardozo L, Fall M, Griffiths D, Rosier P, Ulmsten U, van Kerrebroeck P, Victor A, Wein A (2002) The standardisation of terminology of lower urinary tract function: report from the standardisation sub-committee of the International Continence Society. Neurourol Urodyn 21:167-178
2. Beaumont KC, Cussans NJ, Nichols DJ, Smith DA (1998) Pharmacokinetics and metabolism of darifenacin in the mouse, rat, dog and man. Xenobiotica 28:63-75
3. Borchert VE, Czyborra P, Fetscher C, Goepel M, Michel MC (2004) Extracts from Rhois aromatica and Solidaginis vigaurea inhibit rat and human bladder contraction. Naunyn-Schmiedeberg's Arch Pharmacol 369:281-286
4. Brynne N, Stahl MM, Hallen B, Edlund PO, Palmer L, Hoglund P, Gabrielsson J (1997) Pharmacokinetics and pharmacodynamics of tolterodine in man: a new drug for the treatment of urinary bladder overactivity. Int J Clin Pharmacol Ther 35:287-295
5. Brynne N, Dalen P, Alvan G, Bertilsson L, Gabrielsson J (1998) Influence of CYP2D6 polymorphism on the pharmacokinetics and pharmacodynamics of tolterodine. Clin Pharmacol Ther 63:529-539
6. Burk O, Wojnowski L (2004) Cytochrome P450 3A4 and their regulation. Naunyn-Schmiedeberg's Arch Pharmacol 369:105-124
7. Buyse G, Waldeck K, Verpoorten C, Björk H, Casaer P, Andersson K-E (1998) Intravesical oxybutynin for neurogenic bladder dysfunction: less systemic side effects due to reduced first pass metabolism. J Urol 160:892-896
8. Chapple C, Khullar V, Gabriel Z, Dooley JA (2005) The effects of antimuscarinic treatments in overactive bladder: a systematic review and meta-analysis. Eur Urol 48:5-26
9. Cole P (2004) Fesoterodine, an advanced antimuscarinic for the treatment of overactive bladder: a safety update. Drugs Fut 29:715-720
10. Davila GW, Daugherty CA, Sanders SW (2001) A short-term, multicenter, randomized double-blind dose titration study of the efficacy and anticholingeric side effects of transdermal compared to immediate release oral oxybutynin treatment of patients with urge urinary incontinence. J Urol 166:140-145
11. Dmochowski R, Chen A, Sathyan G, MacDiarmid S, Gidwani S, Gupta S (2005a) Effect of the proton pump inhibitor omeprazole on the pharmacokinetics of extended-release formulations of oxybutynin and tolterodine. J Clin Pharmacol 45:961-968
12. Dmochowski RR, Nitti V, Staskin D, Luber K, Appell R, Davila GW (2005b) Transdermal oxybutynin in the treatment of adults with overactive bladder: combined results of two randomized clinical trials. World J Urol 23:263-270
13. Doroshyenko O, Jetter A, Odenthal KP, Fuhr U (2005) Clinical pharmacokinetics of trospium chloride. Clin Pharmacokin 44:701-720
14. Douchamps J, Derenne F, Stockis A, Gangji D, Juvent M, Herchhuelz A (1988) The pharmacokinetics of oxybutynin in man. Eur J Clin Pharmacol 35:515-520
15. Gerloff T (2004) Impact of genetic polymorphisms in transmembrane carrier-systems on drug and xenobiotic distribution. Naunyn-Schmiedeberg's Arch Pharmacol 369:69-77
16. Guay DRP (2003) Clinical pharmacokinetics of drugs used to treat urge incontinence. Clin Pharmacokin 42:1243-1285
17. Gupta SK, Sathyan G (1999) Pharmacokinetics of an oral once-a-day controlled-release oxybutynin formulation compared with immediate-release oxybutynin. J Clin Pharmacol 39:289-296
18. Haustein KO, Huller G (1988) On the pharmacokinetics and metabolism of propiverine in man. Eur J Drug Metab Pharmacokinet 13:81-90
19. Hegde SS (2006) Muscarinic receptors in the bladder: from basic research to therapeutics. Br J Pharmacol 147:S80-S87
20. Hughes KM, Lang JCT, Lazare R, Gordon D, Stanton SL, Malone-Lee J, Geraint M (1992) Measurement of oxybutynin and its N-desethyl metabolite in plasma, and its application to pharmacokinetic studies in young, elderly and frail elderly volunteers. Xenobiotica 22:859-869
21. Kerbusch T, Milligan PA, Karlsson MO (2003) Assessment of the relative in vivo potency of the hydroxylated metabolite of darifenacin in its ability to decrease salivary flow using pooled population pharmacokinetic-pharmacodynamic data. Br J Clin Pharmacol 57:170-180
22. Krauwinkel WJ, Smulders RA, Mulder H, Swart PJ, Taekema-Roelvink ME (2005) Effect of age on the pharmacokinetics of solifenacin in men and women. Int J Clin Pharmacol Ther 43:227-238
23. Lukkari E, Juhakoski A, Aranko K, Neuvonen PJ (1997) Itraconazole moderately increases serum concentrations of oxybutynin but does not affect those of the active metabolite. Eur J Clin Pharmacol 52:403-406
24. Lukkari E, Taavitsainen P, Juhakoski A, Pelkonen O (1998) Cytochrome P450 specificity of metabolism and interactions of oxybutynin in human liver microsomes. Pharmacol Toxicol 82:161-166
25. Madersbacher H, Mürtz G (2001) Efficacy, tolerability and safety profile of propiverine in the treatment of the overactive bladder (non-neurogenic and neurogenic). World J Urol 19:324-335
26. Michel MC (2002) A benefit-risk assessment of extended-release oxybutynin. Drug Safety 25:867-876
27. Michel MC, Yanagihara T, Minematsu T, Swart PJ, Smulders RA (2005) Disposition and metabolism of solifenacin in humans. Br J Clin Pharmacol 59:647
28. Milsom I, Abrams P, Cardozo L, Roberts RG, Thüroff JW, Wein AJ (2001) How widespread are the symptoms of an overactive bladder and how are they managed? A population-based prevalence study. BJU Int 87:760-766
29. Müller C, Siegmund W, Huupponen R, Kaila T, Franke G, Iisalo E, Zschiesche M (1993) Kinetics of propiverine as assessed by radioreceptor assay in poor and extensive metabolizers of debrisoquine. Eur J Drug Metab Pharmacokinet 18:265-272
30. Nilvebrant L (2002) Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists. Pharmacol Toxicol 90:260-267
31. Nilvebrant L, Hallen B, Larsson G (1997) Tolterodine - a new bladder selective muscarinic receptor antagonist: preclinical pharmacological and clinical data. Life Sci 60:1129-1136
32. Oki T, Kimura R, Saito M, Miyagawa I, Yamada S (2004) Demonstration of bladder selective muscarinic receptor binding by intravesical oxybutynin to treat overactive bladder. J Urol 172:2059-2064
33. Oki T, Kawashima A, Uchida M, Yamada S (2005a) In vivo demonstration of muscarinic receptor binding activity of N-desethyl-oxybutynin, active metabolite of oxybutynin. Life Sci 76:2445-2456
34. Oki T, Sato S, Miyata K, Yamada S (2005b) Muscarinic receptor binding, plasma concentration and inhibition of salivation after oral administration of a novel antimuscarinic agent, solifenacin succinate in mice. Br J Pharmacol 145:219-227
35. Oki T, Maruyama S, Takagi Y, Yamamura HI, Yamada S (2006a) Characterization of muscarinic receptor binding and inhibition of salivation after oral administration of tolterodine in mice. Eur J Pharmacol 529:157-163
36. Oki T, Toma-Okura A, Yamada S (2006b) Advantages for transdermal over oral oxybutynin to treat overactive bladder: muscarinic receptor binding, plasma drug concentration, and salivary secretion. J Pharmacol Exp Ther 316:1137-1145
37. Olsson B, Szamosi J (2001) Multiple dose pharmacokinetics of a new once daily extended release tolterodine formulation versus immediate release formulation. Clin Pharmacokin 40: 227-235
38. Postlind H, Dnielson A, Lindgren A, Andersson SHG (1998) Tolterodine, a new muscarinic receptor antagonist, is metabolized by cytochromes P450 2D6 and 3A in human liver microsomes. Drug Metab Dispos 26:289-293
39. Sathyan G, Chancellor MB, Gupta SK (2001a) Effects of OROS controlled-release delivery on the pharmacokinetics and pharmacodynamics of oxybutynin chloride. Br J Clin Pharmacol 52:409-418
40. Sathyan G, Hu W, Gupta SK (2001b) Lack of effect of food on the pharmacokinetics of an extended-release oxybutynin formulation. J Clin Pharmacol 41:187-192
41. Schneider T, Hein P, Michel-Reher M, Michel MC (2005) Effects of ageing on muscarinic receptor subtypes and function in rat urinary bladder. Naunyn-Schmiedeberg's Arch Pharmacol 372:71-78
42. Shibukawa A, Yoshikawa Y, Kimura T, Kuroda Y, Nakagawa T, Wainer IW (2002) Binding study of desethyloxybutynin using high-performance frontal analysis method. J Chromatography 768:189-197
43. Siepmann M, Nokhodian A, Thümmler D, Kirch W (1998) Pharmacokinetics and safety of propiverine in patients with fatty liver disease. Eur J Clin Pharmacol 54:767-771
44. Skerjanec A (2006) The clinical pharmacokinetics of darifenacin. Clin Pharmacokin 45:325-350
45. Uchida M, Koganei M, Murata N, Yamaji T (2004) Effects of 4-ethylamino-2-butynyl(2-cyclohexyl-2-phenyl)glycolate hydrochloride, a metabolite of oxybutynin, on bladder specimens and rhythmic contraction in rats in comparison with oxybutynin. J Pharmacol Sci 94:122-128
46. van Kerrebroeck P, Kreder K, Jonas U, Zinner N, Wein A (2001) Tolterodine once-daily: superior efficacy and tolerability in the treatment of overactive bladder. Urology 57:414-421
47. Waldeck K, Larsson B, Andersson K-E (1997) Comparison of oxybutynin and its active metabolite, N-desethyl-oxybutynin, in the human detrusor and parotid gland. J Urol 157:1093-1097
48. Wuest M, Braeter M, Schoeberl C, Ravens U (2005a) Juvenile pig detrusor: effects of propiverine and three of its metabolites. Eur J Pharmacol 524:145-148
49. Wuest M, Hecht J, Christ T, Braeter M, Schoeberl C, Hakenberg OW, Wirth MP, Ravens U (2005b) Pharmacodynamics of propiverine and three of its metabolites on detrusor contraction. Br J Pharmacol 145:608-619
50. Wuest M, Morgenstern K, Graf E-M, Braeter M, Hakenberg OW, Wirth MP, Ravens U (2005c) Cholinergic and purinergic responses in isolated human detrusor in relation to age. J Urol 173:2182-2189
51. Wuest M, Weiss A, Waelbrock M, Braeter M, Kelly L-U, Hakenberg OW, Ravens U (2006) Propiverine and metabolites: differences in binding tomuscarinic receptors and in functionalmodels of detrusor contraction. Naunyn-Schmiedeberg's Arch Pharmacol (in press). DOI 10.1007/s00210-006-103-0
52. Yaich M, Popon M, Medard Y, Aigrain EJ (1998) In-vitro cytochrome P450 dependent metabolism of oxybutynin to N-deethyloxybutynin in humans. Pharmacogenetics 8:449-451
53. Yono M, Yoshida M, Wada Y, Kikukawa H, Takahashi W, Inadome A, Seshita H, Ueda S (1999) Pharmacological effects of tolterodine on human isolated urinary bladder. Eur J Pharmacol 368:223-230
54. Zanger UM, Raimundo S, Eichelbaum M (2004) Cytochrome P450 2D6: overview and update on pharmacology, genetics, biochemistry. Naunyn-Schmiedeberg's Arch Pharmacol 369:23-37
55. Zobrist RH, Schmid B, Feick A, Quan D, Sanders SW (2001) Pharmacokinetics of the R- and S-enantiomers of oxybutynin and N-desethyloxybutynin following oral and transdermal administration of the racemate in healthy volunteers. Pharm Res 18:1029-1034
56. Zobrist RH, Quan D, Thomas HM, Stanworth S, Sanders SW (2003) Pharmacokinetics and metabolism of transdermal oxybutynin: in vitro and in vivo performance of a novel delivery system. Pharm Res 20:103-109