Antimuscarinics for the treatment of overactive bladder: Current options and emerging therapies

Current Opinion in Investigational Drugs

Volumn 5, Issue 1, 2004, Pages 40-49

  Hegde, Sharath S ^a   Mammen, Mathai ^a   Jasper, Jeffrey R ^a  

^a THERAVANCE INC   (United States)

Author keywords

Antimuscarinic; Darifenacin; Micturition; Muscarinic receptor; Overactive bladder; Oxybutynin; Solifenacin; Tolterodine; Tropsium; Urge incontinence

Indexed keywords

ALVAMELINE; CHOLINERGIC RECEPTOR BLOCKING AGENT; CYTOCHROME P450 2D6; DARIFENACIN; FESOTERODINE; IMIDAZOLE DERIVATIVE; KRP 197; MUSCARINIC M1 RECEPTOR; MUSCARINIC M2 RECEPTOR; MUSCARINIC M2 RECEPTOR ANTAGONIST; MUSCARINIC M3 RECEPTOR; MUSCARINIC M3 RECEPTOR ANTAGONIST; MUSCARINIC M4 RECEPTOR; MUSCARINIC M5 RECEPTOR; MUSCARINIC RECEPTOR BLOCKING AGENT; NC 2200; OXYBUTYNIN; PIPERIDINE DERIVATIVE; PLACEBO; RECEPTOR SUBTYPE; RO 320 2904; RO 320 3206; SOLIFENACIN; SPM 007; SPM 7605; SVT 40776; TOLTERODINE; TROSPIUM CHLORIDE; UNCLASSIFIED DRUG;

ACCURACY; ARTICLE; BLADDER FUNCTION; CENTRAL NERVOUS SYSTEM DISEASE; CHOLINERGIC SYSTEM; CLINICAL PHARMACOLOGY; CLINICAL TRIAL; CONFUSION; CONSTIPATION; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG ELIMINATION; DRUG FORMULATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG RELEASE; DRUG SAFETY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TARGETING; DRUG TOLERABILITY; EYE DISEASE; FATIGUE; GASTROINTESTINAL DISEASE; HEART DISEASE; HUMAN; IC 50; MEDICAL DECISION MAKING; NONHUMAN; OVERACTIVE BLADDER; PRURITUS; RECEPTOR OCCUPANCY; REGULATORY MECHANISM; RESTLESSNESS; SALIVARY GLAND DISEASE; VISUAL IMPAIRMENT; XEROSTOMIA;

ANIMALS; DRUG DESIGN; HUMANS; MUSCARINIC ANTAGONISTS; RECEPTORS, MUSCARINIC; STRUCTURE-ACTIVITY RELATIONSHIP; URINARY BLADDER; URINARY BLADDER DISEASES; URINARY BLADDER, NEUROGENIC; URINARY INCONTINENCE; URINATION DISORDERS;

EID: 2342444247     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (81)

1. Wein AJ, Rovner ES: Definition and epidemiology of overactive bladder. Urology (2002) 60(5 Suppl 1):7-12.
2. de Groat WC: A neurologic basis for the overactive bladder. Urology (1997) 50(6A):36-52.
3. Andersson KE, Yoshida M: Antimuscarinics and the overactive detrusor - which is the main mechanism of action? Eur Urol (2003) 43(1):1-5.
4. Andersson KE, Appell R, Cardozo LD, Chapple C, Drutz HP, Finkbeiner AE, Haab F, Vela Navarrete R: The pharmacological treatment of urinary incontinence. Br J Urol Int (1999) 84(9):923-947.
5. Chapple CR: Muscarinic receptor antagonists in the treatment of overactive bladder. Urology (2000) 55(5A Suppl):33-46.
6. Chapple CR, Yamanishi T, Chess-Williams R: Muscarinic receptor subtypes and management of the overactive bladder. Urology (2002) 60(5 Suppl 1):82-88.
7. Chess-Williams R: Muscarinic receptors of the urinary bladder: Detrusor, urothelial and prejunctional. Auton Autacoid Pharmacol (2002) 22(3):133-145.
8. Wang P, Luthin GR, Ruggieri MR: Muscarinic acetylcholine receptor subtypes mediating urinary bladder contractility and coupling to GTP binding proteins. J Pharmacol Exp Ther (1995) 273(2):959-966.
9. Hegde SS, Eglen RM: Muscarinic receptor subtypes modulating smooth muscle contractility in the urinary bladder. Life Sci (1999) 64(6-7):419-428.
10. 3-receptors mediate contraction of human detrusor muscle in vitro. J Auton Pharmacol (2001) 21(5-6 ):243-248.
11. 3 muscarinic receptors mediate contraction of human urinary bladder. Br J Pharmacol (2002) 136(5):641-643.
12. 2+ sources. J Pharmacol Exp Ther (2003 ):10,1124/jpet.103.058248.
13. 3 subtype. Proc Natl Acad Sci USA (2000) 97(17 ):9579-9584.
14. 4 receptor subtypes using receptor knockout mice. Life Sci (2001) 68(22-23):2473-2479.
15. + channels in rat bladder smooth muscle. Int J Urol (2002) 9(12):689-696.
16. 2. Am J Physiol Regulat Integrat Comparat Physiol (2003) 285(3):R701-R708.
17. 2 muscarinic receptor contributes to contraction of the denervated rat urinary bladder. Am J Physiol (1998) 275(5 Pt 2):R1654-R1660.
18. 3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo. Br J Pharmacol (1997) 120(8):1409-1418.
19. 2-muscarinic receptors in mediating contraction of the pig urinary bladder in vitro. Br J Pharmacol (2000) 131(7):1482-1488.
20. 2 receptor knockout mice. J Pharmacol Exp Ther (2003) 305(1 ):106-113.
21. Fovaeus M, Fujiwara M, Hogestatt ED, Persson K, Andersson KE: A non-nitrergic smooth muscle relaxant factor released from rat urinary bladder by muscarinic receptor stimulation. J Urol (1999) 161(2):649-653.
22. Hawthorn MH, Chapple CR, Cock M, Chess-Williams R: Urothelium-derived inhibitory factor(s) influences on detrusor muscle contractility in vitro. Br J Pharmacol (2000) 129(3):416-419.
23. 1 muscarinic receptor-mediated facilitation of acetylcholine release in the rat urinary bladder. J Physiol (1994) 480(1):81-89.
24. 4 receptor subtype. Br J Pharmacol (2000) 129(3):493-500.
25. 4-receptor-deficient mice. Naunyn Schmiedebergs Arch Pharmacol (2002) 365(2):112-122.
26. Caulfield MP: Muscarinic receptors - characterization, coupling and function. Pharmacol Ther (1993) 58(3):319-379.
27. Eglen RM, Hegde SS, Watson N: Muscarinic receptor subtypes and smooth muscle function. Pharmacol Rev (1996) 48(4):531-565.
28. 5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic system. Neurochem Res (2003) 28(3-4):437-442.
29. Wess J: Novel insights into muscarinic acetylcholine receptor function using gene targeting technology. Trends Pharmacol Sci (2003) 24(8):414-420.
30. 3 muscarinic acetylcholine receptors in the regulation of second messenger and extracellular signal-regulated kinase signalling pathways in Chinese hamster ovary cells. Br J Pharmacol (2003) 138(7):1340-1350.
31. Yarker YE, Goa KL, Fitton A: Oxybutynin. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in detrusor instability. Drugs Aging (1995) 6(3):243-262.
32. Comer AM, Goa KL: Extended-release oxybutynin. Drugs Aging (2000) 16(2):149-155; discussion 156-157.
33. Anderson RU, Mobley D, Blank B, Saltzstein D, Susset J, Brown JS: Once daily controlled versus immediate release oxybutynin chloride for urge urinary incontinence. OROS Oxybutynin Study Group. J Urol (1999) 161(6):1809-1812.
34. Rovner ES, Wein AJ: Once-daily, extended-release formulations of antimuscarinic agents in the treatment of overactive bladder: A review. Eur Urol (2002) 41(1):6-14.
35. Bang LM, Easthope SE, Perry CM: Transdermal oxybutynin: For overactive bladder. Drugs Aging (2003) 20(11):857-864.
36. Dmochowski RR, Sand PK, Zinner NR, Gittelman MC, Davila GW, Sanders SW, Transdermal Oxybutynin Study Group: Comparative efficacy and safety of transdermal oxybutynin and oral tolterodine versus placebo in previously treated patients with urge and mixed urinary incontinence. Urology (2003) 62(2):237-242.
37. Dmochowski RR, Staskin DR: Advances in drug delivery: Improved bioavailability and drug effect. Curr Urol Rep (2002) 3(6):439-444.
38. Nilvebrant L, Hallen B, Larsson G: Tolterodine - a new bladder selective muscarinic receptor antagonist: Preclinical pharmacological and clinical data. Life Sci (1997) 60(13-14):1129-1136.
39. Abrams P: Evidence for the efficacy and safety of tolterodine in the treatment of overactive bladder. Exp Opin Pharmacother (2001) 2(10):1685-1701.
40. Van Kerrebroeck P, Kreder K, Jonas U, Zinner N, Wein A, Tolterodine Study Group: Tolterodine once-daily: Superior efficacy and tolerability in the treatment of the overactive bladder. Urology (2001) 57(3):414-421.
41. Chapple CR: Tolterodine once daily. Selectivity for bladder over effects on salivation compared to ditropan XL. J Urol (2001) 165(Suppl):253.
42. Diokno AC, Appell RA, Sand PK, Dmochowski RR, Gburek BM, Klimberg IW, Kell SH, OPERA Study Group: Prospective, randomized, double-blind study of the efficacy and tolerability of the extended-release formulations of oxybutynin and tolterodine for overactive bladder: Results of the OPERA trial. Mayo Clin Proc (2003) 78(6):687-695.
43. Sussman D, Garely A: Treatment of overactive bladder with once-daily extended-release tolterodine or oxybutynin: The antimuscarinic clinical effectiveness trial (ACET). Curr Med Res Opin (2002) 18(4):177-184.
44. Dmochowski RR: (S)-oxybutynin (Sepracor). Curr Opin Investig Drugs (2002) 3(10):1508-1511.
45. Kachur JF, Peterson JS, Carter JP, Rzeszotarski WJ, Hanson RC, Noronha-Blob L: R and S enantiomers of oxybutynin: Pharmacological effects in guinea pig bladder and intestine. J Pharmacol Exp Ther (1988) 247(3):867-872.
46. Wallis RM, Napier CM: Muscarinic antagonists in development for disorders of smooth muscle function. Life Sci (1999) 64(6-7):395-401.
47. 3 receptor subtype. Annual Meeting of the International Continence Society, Hiedelberg, Germany (2002):Abs 445.
48. 3 receptor is competitive and reversible. Br J Pharmacol (2003) 138(Suppl):125P.
49. 3 antimuscarinic agent, in the anesthetised dog. Eur Urol Suppl (2002) 1(1):131.
50. Gillberg P-G, Sundquist S, Nilvebrant L: Comparison of the in vitro and in vivo profiles of tolterodine with those of subtype-selective muscarinic receptor antagonists. Eur J Pharmacol (1998) 349(2-3):285-292.
51. Williamson IJ, Newgreen DT, Naylor AM: The effects of darifenacin and oxybutynin on bladder function and salivation in the conscious rat. Br J Pharmacol (1997) 120(Suppl):205P.
52. Beaumont KC, Cussans NJ, Nichols DJ, Smith DA: Pharmacokinetics and metabolism of darifenacin in the mouse, rat, dog and man. Xenobiotica (1998) 28(1):63-75.
53. 3 muscarinic antagonist. Pharmacol Toxicol (2001) Suppl 12-15:318.
54. Nichols D, Colli E, Goka J, Wesnes K: Darifenacin demonstrated no adverse effect on cognitive and cardiac function: Results from a double-blind, randomised, placebo-controlled study. Annual Meeting of the International Continence Society, Seoul, South Korea (2001):Abs 354.
55. 3 antagonist for overactive bladder: comparison with oxybutynin on ambulatory urodynamic monitoring and salivary flow. Annual Meeting of the International Continence Society, Seoul, South Korea (2001):Abs 221.
56. Cardozo L, Prescott K, Serdarevic D, Skillern L: Can medication prolong warning time? Neurourol Urodyn (2003) 22(5):468-469.
57. 3 receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland. Naunyn Schmiedebergs Arch Pharmacol (2002) 366(2):97-103.
58. Kuipers M, Smulders R, Krauwinkel W: The safety, tolerability, and pharmacokinetics of solifenacin succinate in patients with hepatic impairment. Annual Meeting of the International Continence Society, Florence, Italy (2003):Abs 308.
59. Smulders R, Smith N, Krauwinkel W, Balan G: The safety, tolerability, and pharmacokinetics of solifenacin succinate in patients mild, moderate, and severe renal disease. Annual Meeting of the International Continence Society, Florence, Italy (2003):Abs 303.
60. Cardozo L, Kuzmin I, Lisec ML, Millard RJ, van Vierssen Trip, OB, Ridder AM, Drogengijk TE, for the European YM905 Study group: YM905 (solifenacin succinate, Vesicare™) in symptomatic overactive bladder: Results of phase 3A, randomized placebo-controlled trial. J Urol (2003) 169(4):350.
61. Gittelman M, Chu F, Klimberg I, Fincher R, Smith N, Tempel D, Ridge S: Two randomized, double-blind, placebo controlled, parallel-group, fized-dose, multicenter studies assess the efficacy and safety of daily oral administration of 10 mg YM905 (solifenacin succinate, Vesicare®) versus placebo in male and female subjects with overactive bladder. J Urol (2003) 169(4):349.
62. Kaufman J, Knapp P, Siami P, Harris R, Smith N, Ridge S, Tempel D, on behalf of the YM-905 study group: YM 905 (solifenacin succinate, Vesicare™) 10 mg increases the proportion of male and female patients with overactive bladder who become continent. J Urol (2003) 169(4):351.
63. Chapple C, Rechberger T, AI-Shukri S, Meffan P, Everaert K, Ridder A: Results of a randomized phase 3 study comparing solifenacin succinate with tolterodine and placebo in patients with symptomatic overactive bladder. Neurourol Urodyn (2003) 22(5):534-535.
64. Frohlich G, Bulitta M, Strosser W: Trospium chloride in patients with detrusor overactivity: Meta-analysis of placebo-controlled, randomized, double-blind, multi-center clinical trials on the efficacy and safety of 20 mg trospium chloride twice daily. Int J Clin Pharmacol Ther (2002) 40(7):295-303.
65. Halaska M, Ralph G, Wiedemann A, Primus G, Ballering-Bruhl B, Hofner K, Jonas U: Controlled, double-blind, multicentre clinical trial to investigate long-term tolerability and efficacy of trospium chloride in patients with detrusor instability. World J Urol (2003) 20(6):392-399.
66. Norman Z, Gittelman, M; Harris R, Susset J, Kanellos A, Auerbach S: Trospium chloride improves overactive bladder symptoms: A multicenter phase III trial. Annual Meeting of the American Urological Association, Chicago, USA (2003):Abs DP51.
67. 3 muscarinic antagonist: Human receptor binding profile and bladder effects in the guinea pig. Neurourol Urodyn (2003) 22(5):382-384.
68. Waldeck K, Larsson B, Sandberg B, Andersson K-E: Actions of the new antimuscarinic compound Lu 25-109 on isolated human and pig detrusor. Neurourol Urodyn (2002) 21(1):92-98.
69. Gomes CM, Chacko S, Gupta S: LU 25-109: A novel anti-muscarinic agent for treatment of overactive bladder without potential for causing dry mouth. J Urol (2000) 163(4 Suppl):225-226.
70. Sramek JJ, Forrest M, Mengel H, Jhee SS, Hourani J, Cutler NR: A bridging study of LU 25-109 in patients with probable Alzheimer's disease. Life Sci (1998) 62(3):195-202.
71. Miyachi H, Kiyota H, Uchiki H, Segawa M: Synthesis and antimuscarinic activity of a series of 4-(1-imidazolyl)-2,2-diphenylbutyramides: Discovery of potent and subtype-selective antimuscarinic agents. Bioorg Med Chem (1999) 7(6):1151-1161.
72. Yoshida M, Murakami S, Yono M, Seshita H, Miyamoto Y, Inadome A, Miyamae K, Iwashita H, Ueda S: Pharmacological effects of a new muscarinic receptors antagonist: KRP-197 on human isolated urinary bladder. Neurourol Urodyn (2000) 19(4):435-436.
73. Brynne N, Dalen P, Alvan G, Bertilsson L, Gabrielsson J: Influence of CYP2D6 polymorphism on the pharmacokinetics and pharmacodynamic of tolterodine. Clin Pharmacol Ther (1998) 63(5):529-539.
74. Breidenbach A, Pandita R, Selve N, Andersson K: Pharmacodynamic profiling of the novel antimuscarinic drug fesoterodine on rat bladder. Annual Meeting of the International Continence Society, Heidelberg, Germany (2002):Abs 449.
75. Sachse R, Cawello W, Haag MC, Horstmann R: Dose-proportional pharmacokinetics of the new antimuscarinic fesoterodine. Naunyn-Schmiedebergs Archives of Pharmacol (2003) 367(1):R115.
76. Sasche R, Cawello W, Hammes W, Horstmann R: Safety and pharmacokinetics of the novel antimuscarinic drug fesoterodine in populations of different age or gender. Annual Meeting of the International Continence Society, Heidelberg, Germany (2002):Abs 441.
77. Sachse R, Cawello W, Hammes W, Horstmann R: Safety and pharmacokinetics of the novel bladder-selective antimuscarinic fesoterodine in populations of different ethnic origin. Annual Meeting of the International Continence Society, Florence, Italy (2003):Abs 377.
78. Shetty SG, Cefalu JS, Hegde SS, Loeb MD, Moy TM, Watson N, Nunn PA: RO320-2904, A novel bladder selective anti-muscarinic. Pharmacologist (2002) 44(2 Suppl 1):25.7.
79. Greene B, Scott DS, Hegde SS, Blue D: The effect of the muscarinic antagonists, RO320-2904 (RO), tolterodine (TOL) and oxybutynin (OXY) on pilocarpine (PIL)-induced bladder contraction and salivation in conscious dogs. Pharmacologist (2000) 44(2 Suppl 1):25.12.
80. 2 muscarinic receptor antagonists. Am Chem Soc Proc (2001) 221:ORGN-597.
81. Herbison P, Hay-Smith J, Ellis G, Moore K: Effectiveness of anticholinergic drugs compared with placebo in the treatment of overactive bladder. Systematic review. Br Med J (2003) 326(7394):841-844.