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Chemical Compound Review

Bladuril     2-(1-piperidyl)ethyl 3-methyl-4-oxo-2...

Synonyms: Flavoxato, Urispas, flavoxate, Flavossato, Flavoxatum, ...
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Disease relevance of flavoxate


High impact information on flavoxate

  • These results suggest that flavoxate caused muscle relaxation through the inhibition of L-type Ca(2+) channels in human detrusor [6].
  • Of the investigated alternative drug regimens, the papaverine-like smooth muscle relaxant flavoxate was reported to be ineffective [7].
  • These findings suggest that signal transduction via Gi-coupled receptors is involved, at least in part, in the inhibition of the micturition reflex by flavoxate in rats [2].
  • REC 15/2053 showed only weak binding to [3H]nitrendipine sites (IC50 = 14 microM) and muscarinic receptors (IC50 = 18 microM), whereas flavoxate was slightly active only at muscarinic receptors (IC50 = 12.2 microM) [8].
  • The effect of Flavoxate on hyperactive detrusor contraction was studied in 37 patients, including 11 patients in whom the drug was administered intravenously during the urodynamic study [9].

Chemical compound and disease context of flavoxate


Biological context of flavoxate


Anatomical context of flavoxate

  • The ability of imipramine, oxybutynin, and flavoxate to antagonize carbamylcholine and barium chloride (BaCl2)-induced contractions of rabbit detrusor, and to block impulse conduction in desheathed frog sciatic nerves has been assessed in vitro [13].
  • Conformational evaluation and detailed (1)H and (13)C NMR assignments of flavoxate, a urinary tract antispasmodic agent [14].
  • In order to clarify the pharmacological activity of flavoxate, its effect on the tone and spontaneous activity of the guinea-pig isolated ureter and of the muscle strip from rat urinary bladder were studied [15].
  • Flavoxate microinjected into the nucleus reticularis pontis oralis (PoO; pontine micturition inhibitory region) of decerebrated cats inhibited the reflex micturition, but had no effect when microinjected into the locus coeruleus alpha (pontine micturition center) or locus subcoeruleus (pontine urine storage center) [16].
  • The paradoxical effect of flavoxate on uterine motility may be caused by its relaxation of vascular smooth muscle, which results in increased blood flow and, consequently, increased oxygen supply to the myometrium [17].

Associations of flavoxate with other chemical compounds


Analytical, diagnostic and therapeutic context of flavoxate


  1. The effect of flavoxate on uninhibited detrusor contractions and urinary incontinence in the elderly. Briggs, R.S., Castleden, C.M., Asher, M.J. J. Urol. (1980) [Pubmed]
  2. Brain pertussis toxin-sensitive G proteins are involved in the flavoxate hydrochloride-induced suppression of the micturition reflex in rats. Oka, M., Kimura, Y., Itoh, Y., Sasaki, Y., Taniguchi, N., Ukai, Y., Yoshikuni, Y., Kimura, K. Brain Res. (1996) [Pubmed]
  3. Rociverine for nocturia in the elderly: medium-term controlled clinical trial. Daccò, L., Barbagallo, M., Carbognati, A., Girasole, G. Clinical therapeutics. (1986) [Pubmed]
  4. Urinary tract disorders. Clinical comparison of flavoxate and phenazopyridine. Gould, S. Urology (1975) [Pubmed]
  5. Flavoxate, a drug with smooth muscle relaxing activity. Ruffmann, R., Sartani, A. Drugs under experimental and clinical research. (1987) [Pubmed]
  6. The effects of flavoxate hydrochloride on voltage-dependent L-type Ca2+ currents in human urinary bladder. Tomoda, T., Aishima, M., Takano, N., Nakano, T., Seki, N., Yonemitsu, Y., Sueishi, K., Naito, S., Ito, Y., Teramoto, N. Br. J. Pharmacol. (2005) [Pubmed]
  7. Drug therapy of urinary urge incontinence: a systematic review. Haeusler, G., Leitich, H., van Trotsenburg, M., Kaider, A., Tempfer, C.B. Obstetrics and gynecology. (2002) [Pubmed]
  8. Receptor binding studies of the flavone, REC 15/2053, and other bladder spasmolytics. Abbiati, G.A., Ceserani, R., Nardi, D., Pietra, C., Testa, R. Pharm. Res. (1988) [Pubmed]
  9. Effect of flavoxate on hyperactive detrusor muscle. Jonas, U., Petri, E., Kissel, J. Eur. Urol. (1979) [Pubmed]
  10. Motor urge incontinence: diagnosis and treatment. Gaudenz, R., Weil, A. Urologia internationalis. (1980) [Pubmed]
  11. Pharmacokinetics of Flavoxate in man. Bertoli, M., Conti, F., Conti, M., Cova, A., Setnikar, I. Pharmacological research communications. (1976) [Pubmed]
  12. Development of a high-performance liquid chromatographic method for bioequivalence study of flavoxate tablets. Sheu, M.T., Yeh, G.C., Ke, W.T., Ho, H.O. J. Chromatogr. B Biomed. Sci. Appl. (2001) [Pubmed]
  13. Comparative in vitro effects of imipramine, oxybutynin, and flavoxate on rabbit detrusor. Fredericks, C.M., Green, R.L., Anderson, G.F. Urology (1978) [Pubmed]
  14. Conformational evaluation and detailed (1)H and (13)C NMR assignments of flavoxate, a urinary tract antispasmodic agent. Pérez-Hernández, N., Morales-Ríos, M.S., Cerda-García-Rojas, C.M., Joseph-Nathan, P. Journal of pharmaceutical and biomedical analysis. (2006) [Pubmed]
  15. Mechanism of flavoxate antispasmodic activity comparative in vitro studies. Cazzulani, P., Panzarasa, R., De Stefani, C., Graziani, G. Archives internationales de pharmacodynamie et de thérapie. (1985) [Pubmed]
  16. Mechanisms of the suppression of the bladder activity by flavoxate. Kimura, Y., Sasaki, Y., Hamada, K., Fukui, H., Ukai, Y., Yoshikuni, Y., Kimura, K., Sugaya, K., Nishizawa, O. International journal of urology : official journal of the Japanese Urological Association. (1996) [Pubmed]
  17. Paradoxical effect of flavoxate on human uterine contractility in vivo. Coutinho, E.M., Darzé, E., Gesteira, S.K. International journal of gynaecology and obstetrics: the official organ of the International Federation of Gynaecology and Obstetrics. (1980) [Pubmed]
  18. Rociverine citrate: a new spasmolytic agent, potentially useful in the treatment of urinary bladder hyperreflexia. Subissi, A., Maggi, C.A., Meli, A. Jpn. J. Pharmacol. (1986) [Pubmed]
  19. Urinary incontinence. Couture, J.A., Valiquette, L. The Annals of pharmacotherapy. (2000) [Pubmed]
  20. Flavoxate, a potent phosphodiesterase inhibitor. Conti, M., Setnikar, I. Archives internationales de pharmacodynamie et de thérapie. (1975) [Pubmed]
  21. Antispasmodic activity of tiropramide. Setnikar, I., Cereda, R., Pacini, M.A., Revel, L., Makovec, F. Arzneimittel-Forschung. (1989) [Pubmed]
  22. Pharmacokinetics of flavoxate in rats. Setnikar, I., Cova, A., Magistretti, M.J. Arzneimittel-Forschung. (1975) [Pubmed]
  23. Double-blind, placebo-controlled, cross-over study of flavoxate in the treatment of idiopathic detrusor instability. Chapple, C.R., Parkhouse, H., Gardener, C., Milroy, E.J. British journal of urology. (1990) [Pubmed]
  24. Pharmacological studies on the mode of action of flavoxate. Cazzulani, P., Panzarasa, R., Luca, C., Oliva, D., Graziani, G. Archives internationales de pharmacodynamie et de thérapie. (1984) [Pubmed]
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