Propiverine hydrochloride
(Synonyms: 盐酸丙哌维林) 目录号 : GC61933
A muscarinic acetylcholine receptor antagonist
Cas No.:54556-98-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Propiverine is an antagonist of muscarinic acetylcholine receptors (mAChRs).1 It binds to M1 and M2 mAChRs in rat bladder and submaxillary gland, respectively (Kis = 0.3 and 0.19 ?M, respectively), and inhibits carbachol-induced contraction of bladder strips isolated from patients with normal bladder activity and detrusor overactivity associated with benign prostatic hyperplasia (pA2s = 7.7 and 7.6, respectively).2 Formulations containing propiverine have been used in the treatment of overactive bladder.
1.Yamada, S., Ito, Y., Taki, Y., et al.The N-oxide metabolite contributes to bladder selectivity resulting from oral propiverine: Muscarinic receptor binding and pharmacokineticsDrug Metab. Dispos.38(8)1314-1321(2010) 2.Yamanishi, T., Kaga, K., Fuse, M., et al.The role of muscarinic receptor subtypes on carbachol-induced contraction of normal human detrusor and overactive detrusor associated with benign prostatic hyperplasiaJ. Pharmacol. Sci.128(2)65-70(2015)
| Cas No. | 54556-98-8 | SDF | |
| 别名 | 盐酸丙哌维林 | ||
| Canonical SMILES | O=C(C(C1=CC=CC=C1)(C2=CC=CC=C2)OCCC)OC3CCN(CC3)C.[H]Cl | ||
| 分子式 | C23H30ClNO3 | 分子量 | 403.94 |
| 溶解度 | DMSO : 50 mg/mL (123.78 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4756 mL | 12.3781 mL | 24.7562 mL |
| 5 mM | 0.4951 mL | 2.4756 mL | 4.9512 mL |
| 10 mM | 0.2476 mL | 1.2378 mL | 2.4756 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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.PMID:27011567DOI:10.1007/s12262-015-1264-1.
We carried out a systematic review and meta-analysis to assess the efficacy and safety of propiverine for treating overactive bladder (OAB) in adult. A literature review was performed to identify all published randomized placebo-controlled trials (RCT) of propiverine for the treatment of OAB. The search included the following databases: PUBMED and EMBASE. The reference lists of retrieved studies were also investigated. A systematic review and meta-analysis were conducted. Ten publications involving nine different RCTs were used in the analysis. We found that propiverine was effective in treating OAB in our meta-analysis. The decrease in number of micturitions/24 h (P < 0.00001, the mean decrease was from 1.80 to 2.57) indicated that propiverine was more effective than the placebo. Propiverine also decrease the number of urgency, urgency incontinence, and nocturia and increase urine volume. However, the incidence of difficulty in voiding was higher with propiverine therapy compared with the placebo (P = 0.05, the mean percentage range from 0.34 to 4.93 %). The decrease of total international prostate symptom score (IPSS) (P < 0.0001, the mean decrease was from 12.5 to 16.1) indicated that propiverine add a1-adrenoceptor antagonist was more effective in decreasing the lower urinary tract symptom (LUTS). The combination therapy also decreases the voiding symptom and storage symptom scores and increases maximum flow rate. This meta-analysis shows that propiverine is a safe and effective treatment for OAB. The major adverse event associated with propiverine treatment was difficulty in voiding. Propiverine add a1-adrenoceptor antagonist was more effective in terms of decreasing difficulty in voiding.
Propiverine hydrochloride as a Treatment for Fecal Incontinence
Ann Coloproctol 2020 Apr;36(2):88-93.PMID:32178499DOI:10.3393/ac.2019.09.30.2.
Purpose: Propiverine hydrochloride (PH) is widely used for the treatment of urinary incontinence (UI) due to bladder overactivity. Moreover, the comorbidity of UI with fecal incontinence (FI) is known to be due to the relationship of both to nervous system disorders and dysfunction or weakening of the pelvic floor muscles. The aim of this single-arm prospective study was to evaluate the therapeutic value of PH for FI. Methods: Patients (n = 24) who were diagnosed as having both FI and UI from April 2015 to November 2016 were included in the study and administered a dosage of 10-20 mg PH every day for 1 month. The primary endpoint was to create a reduction in the frequency of FI per week. An evaluation criterion of ≥50% reduction in frequency was determined as effective. The percentage of the patients who achieved the ≥50% endpoint (responders) was also calculated. Results: The frequency of FI per week was 6.0 ± 8.2 (0.25-30) at baseline and reduced to 1.6 ± 2.1 (0-7) at the posttherapeutic state (P = 0.005). A reduction of ≥50% was seen in 14 of the patients (58.3%). Conclusion: PH reduced the frequency of FI in patients with both FI and UI. This study introduces a possible therapeutic option for the pharmacological treatment of FI.
Efficacy of Propiverine hydrochloride for urinary incontinence after robot-assisted or laparoscopic radical prostatectomy
Can J Urol 2021 Jun;28(3):10706-10712.PMID:34129467doi
Introduction: To clarify the efficacy and safety of Propiverine hydrochloride for incontinence after robot-assisted laparoscopic prostatectomy (RALP)/laparoscopic radical prostatectomy (LRP), along with changes in the urethral pressure profile (UPP) and quality of life in patients treated with Propiverine hydrochloride. Materials and methods: In this randomized, comparative study, 104 patients who were aware of urinary incontinence after RALP or LRP were assigned to receive Propiverine hydrochloride (treatment group) or not (controls). Pad test results, International Consultation on Incontinence Questionnaire-Short Form (ICIQ-SF) scores, and UPP results [including maximum urethral closure pressure (MUCP) and functional urethral length (FUL)], were recorded immediately and at 6 months postoperatively. Results: No serious intraoperative complications or adverse events were caused by Propiverine hydrochloride. The pad-test negative rate was significantly greater in the treatment group than in controls (89.1% vs. 73.2%, p = 0.044). Changes in ICIQ-SF scores and MUCP were significantly greater in the treatment group than in controls [-6.5 vs. -4.5 points (p = 0.021), and +49.5 vs. +28.7 mmHg (p = 0.038), respectively]. FUL change did not significantly differ between groups [+4.5 vs. +3.8 mm (p = 0.091)]. In univariate logistic regression analyses, body mass index (BMI), MUCP, and treatment with Propiverine hydrochloride were significantly associated with continence status. In multivariate analyses, BMI and MUCP were independently associated with continence status [odds ratio (OR), 1.266; 95% confidence interval (CI), 1.047-1.530 (p = 0.015), and OR, 0.986; 95% CI, 0.973-0.999 (p = 0.042), respectively]. Conclusions: Treatment with Propiverine hydrochloride alleviated urinary incontinence while improving patient symptoms and quality of life after RALP or LRP.
Evaluation of Usefulness of Propiverine hydrochloride in Poor Responders to Previous Anticholinergics
Low Urin Tract Symptoms 2018 May;10(2):116-121.PMID:29664239DOI:10.1111/luts.12145.
Objectives: In recent years, some patients have been unresponsive to anticholinergics used in the treatment of pollakisuria/urinary incontinence. It has been suggested that Propiverine hydrochloride, which has not only anticholinergic activity, but also calcium antagonistic activity, may be useful in poor responders to other anticholinergics. In this study, a specific drug use-results survey was conducted in poor responders to other anticholinergics to evaluate the usefulness of Propiverine hydrochloride. Methods: In this survey, Propiverine hydrochloride was administered for 12 weeks to poor responders to previous anticholinergics, and its usefulness was evaluated by the overactive bladder symptom score (OABSS). Results: A total of 3851 subjects at 680 institutions were enrolled in the survey. Of the 3624 subjects included in the safety evaluation (male 1899, female 1725, mean age 73.4 years), 2932 were included in the efficacy evaluation (male 1610, female 1322, mean age 73.8 years). Propiverine hydrochloride significantly improved the OABSS without any safety concerns in poor responders to previous anticholinergics (OABSS, 8.22 at baseline, 6.50 at Week 4, 5.87 at Week 8, and 5.57 at Week 12, P < 0.001). Conclusions: The present findings indicate that Propiverine hydrochloride may be a useful therapeutic option for poor responders to previous anticholinergics.
Excitatory effect of Propiverine hydrochloride on urethral activity in rats
Int J Urol 2012 Jun;19(6):575-82.PMID:22376304DOI:10.1111/j.1442-2042.2012.02977.x.
Objectives: To investigate the effects of the antimuscarinic agent, propiverine, on the bladder and urethra in rats. Methods: A total of 54 female rats were given propiverine, imidafenacin (an antimuscarinic agent), or distilled water by gavage once or twice daily. After 2 weeks, bladder and urethral activity were recorded under urethane anesthesia. In the propiverine group, the changes of bladder and urethral activity before and after intravenous injection of α(1) -adrenergic antagonists (prazosin, silodosin and naftopidil) were also recorded. Furthermore, the leak point pressure after electrical stimulation of abdominal wall muscles was measured in rats with vaginal distension from the control and propiverine groups. Results: Intravesical baseline pressure was significantly lower in the propiverine and imidafenacin groups compared with the control group, whereas the urethral baseline pressure was significantly higher in the propiverine group compared with the control or imidafenacin groups. Intravenous injection of prazosin (an α(1) -receptor antagonist) significantly decreased the urethral baseline pressure in both of the propiverine and control groups. Intravenous injection of silodosin and naftopidil (α(1A) - and α(1D) -receptor antagonists, respectively) significantly decreased the maximum contraction pressure and the urethral baseline pressure in the propiverine group. The leak point pressure of the propiverine group was significantly higher than that of the control group. Conclusions: An increase of catecholamines after propiverine administration might activate smooth muscle of the proximal urethra via α(1A) - and α(1D) -adrenergic receptors, as well as activating urethral and pelvic floor striated muscle via the spinal motoneurons.