Importance of pharmacological and physicochemical properties for tolerance of antimuscarinic drugs in the treatment of detrusor instability and detrusor hyperreflexia - Chances for improvement of therapy

International Journal of Clinical Pharmacology and Therapeutics

Volumn 37, Issue 5, 1999, Pages 209-218

  Schwantes, U ^a,b   Topfmeier, P ^a  

^a Dr R Pfleger GmbH   (Germany)

^b Dr R Pfleger GmbH   (Germany)

Author keywords

Antimuscarinic drugs; Dermal delivery system; Detrusor hyperreflexia; Detrusor instability; Intravesical instillation; Oral administration; Tolerance

Indexed keywords

FLAVOXATE; MUSCARINIC RECEPTOR; MUSCARINIC RECEPTOR BLOCKING AGENT; OXYBUTYNIN; PROPIVERINE; TOLTERODINE; TROSPIUM CHLORIDE; VAMICAMIDE;

CLINICAL TRIAL; DATA ANALYSIS; DETRUSOR DYSSYNERGIA; DETRUSOR MUSCLE; DROWSINESS; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG TOLERANCE; HUMAN; HYPERACTIVITY; HYPERREFLEXIA; INSOMNIA; INTRAVENOUS DRUG ADMINISTRATION; INTRAVESICAL DRUG ADMINISTRATION; NERVOUSNESS; NEUROGENIC BLADDER; ORAL DRUG ADMINISTRATION; PHOTOPHOBIA; PHYSICAL CHEMISTRY; REVIEW; SIDE EFFECT; TRANSDERMAL DRUG ADMINISTRATION; URINE RETENTION; VERTIGO; XEROSTOMIA;

ADMINISTRATION, CUTANEOUS; ADMINISTRATION, INTRAVESICAL; ADMINISTRATION, ORAL; BIOLOGICAL AVAILABILITY; HUMANS; MUSCARINIC ANTAGONISTS; RECEPTORS, MUSCARINIC; REFLEX, ABNORMAL; UROLOGIC DISEASES;

EID: 0032910264     PISSN: 09461965     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (79)

1. Aaltonen L, Allonen H, Iisalo E, Juhakoski A, Kleimola T, Sellman R 1984 Antimuscarinic activity of oxybutynin in the human plasma quantitated by a radioreceptor assay. Acta Pharmacol Toxicol 55: 100-103
2. Abrams P, Freeman RN, Anderström C, Mattiasson A 1997 Efficacy and tolerability of tolterodine vs. oxybutynin and placebo in patients with detrusor instability. J Urol 157 (Suppl 4): Abstract 402
3. Amarenco G, Adba M-A, Kerdraon J 1992 Intérêt de l'oxybutinine en instillation intra-vésicale dans les hyperactivités vésicales rebelles. Etude de 15 patients. Prog Urol 2: 660-663
4. Arzneistoff-Profile - Basisinformation über arzneiliche Wirkstoffe 1996 Frankfurt, 11. Erg-Lief
5. Baigrie RJ, Kelleher JP, Fawcett DP, Pengelly AW 1988 Oxybutynin: Is it safe? Br J Urol 62: 319-322
6. Brendler CB, Radebaugh LC, Mohler JL 1989 Topical oxybutynin chloride for relaxation of dysfunctional bladders. J Urol 141: 1350-1352
7. Breuel H-P, Mürtz G, Bondy S, Horkulak J, Gianetti BM 1993 Safety and tolerance of trospium chloride in the high dose range. Arzneimittelforschung/Drug Res 43: 461-464
8. Brown JH, Taylor P 1996 Muscarinic receptor agonists and antagonists. In: Hardmann JG et al (eds) Goodman and Gilman's the pharmacological basis of therapeutics. McGraw-Hill, New York, pp 141-160
9. Brynne N, Stahl MMS, Hallen B, Edlund PO, Palmer L, Höglund 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
10. Buyse G, Verpoorten C, Vereecken R, Casaer P 1995 Treatment of neurogenic bladder dysfunction in infants and children with neurospinal dysraphism with clean intermittent (self)catheterisation and otpimized intravesical oxybutynin hydrochloride therapy. Eur J Pediatr Surg 5 (Suppl 1): 31-34
11. Cornella JL, Ostergarf DR, Bent AE, Horbach NS 1990 Prospective study utilising transdermal scopolamine in detrusor instability. Urology 25: 96-97
12. Donnellan CA, Fook L, McDonald P, Player JR 1997 Oxybutynin and cognitive dysfunction. Br Med J 315: 1363-1364
13. Dorofeeva NA, Shelkovnikov SA, Starshinova LA, Danilov AF, Nedoma J, Tueck S 1992 Quest for agonist and antagonist selectivity at muscarinic receptors in guinea-pig smooth muscles and cardiac atria. Naunyn Schmiedebergs Arch Pharmacol 346: 383-390
14. Douchamps J, Derenne F, Stockis A, Gangji D, Juvent M, Herchuelz A 1988 The pharmacokinetics of oxybutynin in man. Eur J Clin Pharmacol 35: 515-520
15. Drutz H, Appell RA 1997 Clinical efficacy and safety of tolterodine vs. oxybutynin and placebo in patients with unstable bladder (abstract). XV FIGO World Congress of Gynecology and Obstetrics, Aug. 3-8, Copenhagen
16. Eckert RE, Kurz M, Alloussi S, Ziegler M 1998 Zelluläre Ebene der muskulotropen und neurotropen Potenz von Propiverin. Urologe A (Suppl 1): F3.5
17. Eckert RE, Wilhelm A, Schwantes U, Utz J, Alloussi S, Trautwein W, Ziegler M 1995 Modulation der zytoplasmatischen Ca2+-Konzentration isolierter Myozyten des Detrusor vesicae durch Anticholinergika. Akt Urol 26:4-6
18. Eglen RM, Michel AD, Montgomery WW, Kunysz EA, Machado CA, Whiting RL 1990 The interaction of parafluorohexahydrosiladifenidol at muscarinic receptors in vitro. Br J Pharmacol 99: 637-642
19. Eglen RM, Hedge SS, Watson N 1996a Muscarinic receptor subtypes and smooth muscle function. Pharmacol Rev 48: 531-565
20. Eglen RM, Pelle B, Pulido-Rios MT, Leung E 1996b Muscarinic M2 receptors modulate relaxant responses to 5-HT receptor and β3-adrenoceptor agonism in isolated oesophageal muscularis mucosae of rat. Br J Pharmacol 117 (Suppl): 108
21. Enzelsberger H, Helmer H, Kurz C 1995 Intravesical instillation of oxybutynin in women with idiopathic detrusor instability: A randomized trial. Br J Obstetr Gynaecol 102: 929-930
22. Friebe TP, Mutschler E, Lambrecht G 1993 Muskarinrezeptor-Subtypen: Pharmakologische Charakterisierung, molekulare Struktur, Lokalisation, Funktion und Rezeptor-Effektor-Kopplung. Pharm Z Wiss 1: 3-11
23. Fröhlich G, Burmeister S, Wiedemann A, Bulitta M 1998 Intravesikale Instillation von Trospiumchlorid, Oxyutynin und Verapamil zur Relaxation des Hamblasen-Detrusors - Eine Plazebo-kontrollierte, randomisierte klinische Prüfung. Arzneimittelforschung/Drug Res 48: 486-491
24. Gyermek L 1997 Pharmacology of antimuscarinic agents. CRC Press, Boca Raton, pp 65-66
25. Haustein K-O, Hüller G 1988 On the pharmacokinetics and metabolism of propiverine in man. Eur J Drug Metabol Pharmacokinet 13: 81-90
26. 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
27. Hüller G, Barthel W, Klatt H, Haustein K-O 1993 Determination of N-butyl-scopolamine bromide in human plasma and urine by HPLC method. Evidence of negligible absorption after oral administration. Pharmazie 48: 548-549
28. Iwatsubo E, Okada E, Tamada K, Takehara T 1994 Clinical effects of high dose vamicamide (FK176) for the treatment of neurogenic bladder dysfunction. Nishinihon J Urol 56: 378-384
29. Jaquetin B, Wyndaele JJ 1997 Tolterodine reduces the number of incontinence episodes in patients with detrusor overactivity. 22nd Annual Meeting of the International Urogynecological Association (Abstract), Jul 30-Aug 2, Amsterdam
30. Jonas U, Höfner K, Madersbacker H, Holmdahl TH 1997 Efficacy and safety of two doses of tolterodine versus placebo in patients with detrusor overactivity and symptoms of frequency, urge incontinence, and urgency: Urodynamic evaluation. World J Urol 15: 144-151
31. Kainuma H, Fujiwara S, Terakawa M, Oyasu H 1993a Phase I study of vamicamide (1) - single- and multiple-dose studies. Jpn Pharmacol Ther 21: 185-219
32. Kainuma H, Kageyama H, Terakawa M, Oyasu H 1993b Phase I study of vamicamide (2) - single- and multiple-dose studies. Jpn Pharmacol Ther 21: 221-246
33. Kaplinsky R, Greenfield S, Wan J, Fera M 1996 Expanded followup of intravesical oxybutynin chloride use in children with neurogenic bladder. J Urol 156: 753-756
34. Katz IR, Sands LP, Bilker W, DiFilippo S, Boyce A, D'Angelo K 1998 Identification of medications that cause cognitive impairment in older people: The case of oxybutynin chloride. J Am Geriatr Soc 48: 8-13
35. Keshary P, Jones D, Milchell J, Pool J, Hwang K, Yong C 1991 Development of transdermal delivery systems for oxybutynin: in-vivo bioavailability. Pharm Res 8 (Suppl 10): 205
36. Kondo S, Morita T 1993 A study of muscarinic cholinergic receptor subtypes in human detrusor muscle using radioligand binding techniques. Jpn J Urol 84: 1255-1261
37. Kondo S, Monta T, Tashima Y 1995 Muscarinic cholinergic receptor subtypes in human detrusor muscle studied by labeled and nonlabeled pirenzepine, AFDX-116 and 4DAMP. Urol Int 54: 150-153
38. Krishnan KR, Fowler C, Powell J, Soni BM, Lukkari E, Vaidyanathan S 1996 A double-blind, randomized, placebo-controlled, parallel-group, multicenter study of intravesical oxybutynin in the symptomatic relief of urge incontinence with detrusor instability/hyperreflexia. Neurourol Urodynamics 15: 674-676
39. Kumazawa J, Yamashita H, Takei M, Koyanagi T, Morita H, Shinno Y, Tsuchida S, Harada T. Noto H, Shiraiwa Y, Yamaguchi O, Fukada Y, Yokota T, Akimoto M, Horuchi K, Sato M, Shimazaki J, Yasuda K, Miyake K, Kondo A, Kato K, Osada Y, Kitada S, Ogawa N 1994a Clinical evaluation of vamicamide (FK176) for the treatment of neurogenic bladder and unstable bladder - Multi-center double-blind controlled study with placebo. Nishinihon J Urol 56: 345-362
40. Kumazawa J, Yamashita H, Takei M, Koyanagi T, Morita H, Shinno Y, Tsuchida S, Harada Y, Akimoto M, Yajima I 1994b Clinical evaluation of vamicamide (FK176) for the treatment of neurogenic bladder and unstable bladder - Early phase II clinical study. Nishinihon J Urol 56: 320-330
41. Kumazawa J, Yamashita H, Takei M, Koyanagi T, Morita H, Shinno Y, Tsuchida S, Harada Y, Noto H, Akimoto M, Yajima I, Sato M, Shimazaki J, Yasuda K, Miyake K, Kondo A, Kato K, Ogawa N 1994c Clinical evaluation of vamicamide (FK176) for the treatment of neurogenic bladder and unstable bladder - Late phase clinical study. Nishinihon J Urol 56: 331-344
42. Lace R, Cavallini A, Ridolfi L, Veronese V, Marras E 1994 Trattamento della vescica neurologica con ossibutinina cloridrato endovesicale. Acta Urol Ital 5: 249-253
43. Langguth P, Kubis A, Krumbiegel G, Lang W, Merkle HP, Wächter W, Spahn-Langguth H, Weyhenmeyer R 1997 Intestinal absorption of the quaternary trospium chloride: Permeability-lowering factors and bioavailability for oral dosage forms. Eur J Pharm Biopharm 43: 265-272
44. Leyson JF, Seebode J 1988 Comparative study between oral and transdermal suppression of bladder reflex activity in spinal cord injury patients. J Urol 139: 349A
45. Madersbacher H, Jilg G 1991 Control of detrusor hyperreflexia by the intravesical instillation of oxybutynine hydrochloride. Paraplegia 29: 84-90
46. Madersbacher H, Knoll M 1995 Intravesical application of oxybutynine: Mode of action in controlling detrusor hyperreflexia - Preliminary results. Eur Urol 28: 340-344
47. Madersbacher H, Stöhrer M, Richter R, Burgdörfer H, Hacken HJ, Mürtz G 1995 Trospium chloride versus oxybutynin: A randomized, double-blind, multicentre trial in the treatment of detrusor hyperreflexia. Br J Urol 75: 452-456
48. Massad CA, Kogan BA, Trigo-Rocha FE 1992 The pharmacokinetics of intravesical and oral oxybutynin chloride. J Urol 148: 595-597
49. Mazur D, Göcking K, Wehnert J, Dorschner W, Herfurth G, Alken R-G, Anger G, Höfner K, Krücke S 1994 Verträglichkeit und Wirksamkeit einer Langzeittherapie mit Propiverinhydrochlorid bei neurogener Harninkontinenz. Eine multizentrische Studie. Kontinenz 3: 74-78
50. Mazur D, Wehnert J, Dorschner W, Schubert G, Herfurth G, Alken R-G 1995 Clinical and urodynamic effects of propiverine in patients suffering from urgency and urge incontinence. Scand J Urol Nephrol 29: 289-294
51. McGrother C, Resnick M, Yalla SV, Kirschner-Hermanns R, Broseta E, Müller C, Welz-Barth A, Fischer GC, Mattelaer J, McGuire EJ 1998 Epidemiology and etiology of urinary incontinence in the elderly. World J Urol 16 (Suppl 1): 3-9
52. Milani R, Scalambrino S, Milia R, Sambruni I, Riva D, Pulici L, Avaldi F, Vigano R 1993 Double-blind crossover comparison of flavoxale and oxybutynin in woman affected by urinary urge syndrome. Int Urogynecol J 4: 3-8
53. Moore KH, Hay DM, Imrie AE 1990 Oxybutynin hydrochloride (3 mg) in the treatment of women with idiopathic detrusor instability. Br J Urol 66: 479-485
54. Newgreen DT, Naylor AM 1996 Comparison of the functional muscarinic receptor selectivity of darifenacin with tolterodine and oxybutynin. Br J Pharmacol 117 (Suppl): 107
55. Newgreen DT, Anderson CWP, Carter TJ, Naylor AM 1996 Darifenacin - A novel bladder-selective muscarinic antagonist for the treatment of urge incontinence. Proc Am Urol Assoc 155 (Suppl): 600A
56. Nilvebrant L, Sundquist S, Gillberg P-G 1996 Tolterodine is not subtype (m1-m5) selective but exhibits functional selectivity in vivo. Neurourol Urodynamics 15: 310-311
57. Nilvebrant L, Gillberg P-G, Sparf B 1997a Antimuscarinic potency and bladder selectivity of PNU-200577, a major metabolite of tolterodine. Pharmacol Toxicol 81: 169-172
58. Nilvebrant L, Andersson K-E, Gillberg P-G, Stahl M, Sparf B 1997b Tolterodine - A novel bladder selective antimuscarinic agent. Eur J Pharmacol 327: 195-207
59. Ogiso T, Iwaki M, Hirota T, Tanino T, Muraoka O 1995 Comparison of the in vitro skin penetration of propiverine with that of terodiline. Biol Pharm Bull 18: 968-975
60. Osca-Garcia JM, Martinez Agullo E, Conejero Sugranes J, Jiminez Cruz JF 1997 Tropiumchlorid versus Oxybutynin in der Behandlung der hyperaktiven Blase -eine randomisierte doppelblinde Studie. Jatros Urol 13: 35-39
61. Ouslander JG, Schnelle JF, Uman G, Fingold S, Nigam JG, Tuico E, Jensen BB 1995 Does oxybutynin add to the effectiveness of prompted voiding for urinary incontinence among nursing home residents? A placebo-controlled trial. J Am Geriatr Soc 43: 610-617
62. Oyasu H, Yamamoto T, Sato N, Sawada T, Ozaki R, Mukai T, Ozaki T, Nishii M, Sato H, Tozuka Z, Koibuchi Y, Honbo T, Esumi K, Ohtsuka M, Shimimura K 1994 Urinary bladder-selective action of the new antimuscarinic compound vamicamide. Arzneimittelforschung/Drug Res 44: 1242-1249
63. Palmer LS, Zebold K, Firlit CF, Kaplan WE 1997 Complications of intravesical oxybutynin chloride therapy in the pediatric myelomeningocele population. J Urol 157: 638-640
64. Pietzko A, Dimpfel W, Schwantes U, Topfmeier P 1994 Influences of trospium chloride and oxybutynin on quantitative EEG in healthy volunteers. Eur J Clin Pharmacol 47: 337-343
65. Pilz U, Pilz A 1985 Nebenwirkungen von Mictonorm am Auge. Z Klin Med 40: 1211-1215
66. Poli E, Monica M, Zappia L, Pozzoti C, Bertaccini G 1992 Antimuscarinic activity of telenzepine on isolated human urinary bladder: No role for M1-muscarinic receptors. Gen Pharmacol 108: 132-138
67. Sone A, Tanaka H 1994 Clinical effects of vamicamide (FK176) for the treatment of neurogenic bladder and unstable bladder. Nishinihon J Urol 56: 371-377
68. Stahl MMS, Ekström B, Sparf B, Mattiasson A, Andersson K-E 1995 Urodynamic and other effects of tolterodine: A novel antimuscarinic drug for the treatment of detrusor overactivity. Neurourol Urodynamics 14: 647-655
69. Stöhrer M, Bauer P, Giannetti BM, Richter R, Burgdörfer H, Mürtz G. 1991 Effect of trospium chloride on urodynamic parameters in patients with detrusor hyperreflexia due to spinal cord injuries. A multicentre placebo-controlled double-blind trial. Urol Int 47: 138-145
70. Sugiyama Y 1997 Parkinsonism induced by propiverine hydrochloride - Report of 3 cases. Clin Neurol 37: 873-875
71. Tokuno H, Chowdhury JU, Tomita T 1993 Inhibitory effects of propiverine on rat and guinea-pig urinary bladder muscle. Naunyn-Schmiedebergs Arch Pharmacol 348: 659-662
72. Urae A, Yamashita H, Irie S, Kageyama H, Terakawa M, Oyasu H, Kwnazawa J 1993 Phase I study of vamicamide (3) - Single- and multiple-dose studies. Jpn Pharmacol Ther 21: 247-269
73. Waldeck K, Larsson B, Andersson K-E 1997 Comparison of oxybutynin and its active metabolite N-desethyloxybutynin, in the human detrusor and parotid gland. J Urol 157: 1093-1097
74. Wallis RM, Alker D, Burges RA, Cross PE, Newgreen DT, Quinn P 1993 Zamifenacin: A novel gut selective muscarinic receptor antagonist. Br J Pharmacol 109: 36
75. Walter P, Kramer G, Grosse J, Schwantes U, Schulz H-U, Stöhrer M 1998 Plasmaspiegel von Trospiumchlorid (TC) nach einmaliger intravesikaler Instillation. Forum Urodynamicum (Abstract), April 02-04, Mainz
76. Wang P, Luthin GR, Ruggieri MR 1995 Muscarinic receptor subtypes mediating urinary bladder contractility and coupling to GTP binding proteins. J Pharmacol Exp Ther 273: 959-966
77. Weese DL, Roskamp DA, Leach GE, Zimmern PE 1993 Intravesical oxybutynin chloride: Experience with 42 patients. Urology 41: 527-530
78. Wehnert J, Sage S 1992 Therapie der Blaseninstabilität und Urge-Inkontinenz mit Propiverinhydrochlorid (Mictonorm) und Oxybutyninchlorid (Dridase) -eine randomisierte Cross-over-Vergleichsstudie. Akt Urol 23: 7-11
79. Yarker YE, Goa KL, Fitton A 1995 Oxybutynin, a review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in detrusor instability. Drugs Aging 6: 243-262