生物活性

• 描述Propiverine HCl is a bladder spasmolytic with calcium antagonistic and anticholinergic properties. Propiverine (0.5 mg/day; p.o. once daily for 2 weeks) significantly increases UBP and LPP during passive intravesical pressure elevation, and also increases plasma norepinephrine and epinephrine levelsin rats. Propiverine (0.01-1 mg/kg; i.v.) decreases the UBP and totally suppresses the sneeze reflex at the dose of 1 mg/kg in vivo^[2]. Propiverine (10-3000 nM) inhibits the specific binding of [3H]NMS, with Kis of 339, 193 and 497 nM in the bladder, submaxillary gland and heart of mice respectively. After the oral administration of propiverine, dose- and time-dependent increases in the dissociation constant for specific [(3) H]NMS binding were observed in the bladder and other tissues of mice, indicating that orally administered propiverine and/or its metabolite undergo significant binding to muscarinic receptors in mouse tissues. A longer-lasting binding of muscarinic receptor was seen in the bladder than in the submaxillary gland at relatively low doses of propiverine. Furthermore, the decrease in maximal number of binding sites values for [(3) H]NMS binding was more remarkable in the bladder than submaxillary gland of propiverine treated mice. There was a dose-dependent rise in the plasma concentrations of propiverine and 1-methy-4-piperidyl benzilate N-oxide in mice after the oral administration of propiverine^[3]. PH (Propiverine hydrochloride) reduced the frequency of FI (fecal incontinence) in patients with both FI and UI (urinary incontinence)^[4]. Propiverine not only improved bladder dysfunction through its previously reported actions (anti-muscarinic effect, Ca antagonist effect, and inhibition of noradrenaline re-uptake), but also by reducing inflammation^[5]. Propiverine add a1-adrenoceptor antagonist was more effective in terms of decreasing difficulty in voiding^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03662893	Overactive Bladder	Not Applicable	Completed	-	Turkey ... more >> Ankara Training and Research Hospital Ankara, Turkey, 06340 Collapse <<
  NCT02294396	Overactive Bladder (OAB)	Phase 4	Completed	-	Japan ... more >> Chubu, Japan Chugoku, Japan Hokkaido, Japan Kansai, Japan Kantou, Japan Kyushu, Japan Tohoku, Japan Collapse <<
  NCT00646880	Urinary Bladder, Overactive	Phase 3	Completed	-	Korea, Republic of ... more >> Pfizer Investigational Site Seoul, Korea, Republic of, 110-744 Collapse <<

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• 参考文献

• [2] Kitta T, Tyagi V, Nanri M, Kiniwa M, Nonomura K, Yoshimura N. Effects of propiverine hydrochloride, an anticholinergic agent, on urethral continence mechanisms and plasma catecholamine concentration in rats. Int Urogynecol J. 2013 Apr;24(4):683-8

  [3] Ito Y, Kato A, Fujino Oki T, Okura T, Yoshida K, Nanri M, Yamada S. Muscarinic Receptor Binding and Plasma Drug Concentration after the Oral Administration of Propiverine in Mice. Low Urin Tract Symptoms. 2010 Apr;2(1):43-9

  [4] Irei Y, Takano S, Yamada K. Propiverine Hydrochloride as a Treatment for Fecal Incontinence. Ann Coloproctol. 2020 Apr;36(2):88-93

  [5] Nishijima S, Sugaya K, Kadekawa K, Ashitomi K, Ueda T, Yamamoto H. Mechanisms underlying the effects of propiverine on bladder activity in rats with pelvic venous congestion and urinary frequency. Biomed Res. 2019;40(4):145-152

  [6] Huang W, Zong H, Zhou X, Wang T, Zhang Y. Efficacy and Safety of Propiverine Hydrochloride for Overactive Bladder in Adult: a Systematic Review and Meta-analysis. Indian J Surg. 2015 Dec;77(Suppl 3):1369-77

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