Background: Bethanechol chloride, a cholinergic agonist, is often prescribed in suspected underactive bladders to improve detrusor contractility, despite its limited clinical efficacy. We investigated the usage patter...Background: Bethanechol chloride, a cholinergic agonist, is often prescribed in suspected underactive bladders to improve detrusor contractility, despite its limited clinical efficacy. We investigated the usage pattern of bethanechol in actual practice with the understanding that it would enable the physicians to make an informed decision on the coherent use of bethanechol. Methods: A nation-wide survey was carried out to obtain the responses of the urologists. Out of the 755 urologists approached, 630 survey responses were considered for analysis. Results: Usage of bethanechol was advocated as very common [318 (50.48%)], common [200 (31.75%)], not so common [107 (16.98%)], and rare [5 (0.79%)] in postoperative urinary retention, where it was preferred either exclusively [255 (40.48%)] or along with alpha blockers [247 (39.21%)]. Predilection to use alpha-blocker [247 (39.21%)], alpha-blocker plus naloxone [4 (0.64%)], naloxone [1 (0.16%)], alpha-blocker plus bethanechol plus naloxone [1 (0.16%)] was also observed. It was also preferred individually in pathologies causing urinary retention such as benign prostatic hyperplasia [125 (19.84%)], diabetic neuropathy [82 (13.02%)], neurological diseases [69 (10.95%)], senile bladder [14 (2.22%)], drugs [13 (2.06%)], and infective/inflammatory conditions [6 (0.95%)]. Other [321 (50.95%)] physicians opted to prescribe bethanechol in two or more of the enumerated indications. Bethanechol was prescribed orally as 25 mg thrice daily [441 (70.00%)], 50 mg thrice daily [86 (13.65%)], 25 mg four times daily [59 (9.37%)], and many “strongly agree” and “agree” that its sustained release formulation may offer better treatment compliance [565 (89.68%)], safety [548 (86.99%)], and efficacy [544 (86.35%)]. Conclusion: Bethanechol was the most prescribed drug for the management of postoperative urinary retention and other pathologies suspected to cause underactive bladder.展开更多
AIM:To investigate the pathway(s)mediating rat antral circular smooth muscle contractile responses to the cholinomimetic agent,bethanechol and the subtypes of muscarinic receptors mediating the cholinergic contraction...AIM:To investigate the pathway(s)mediating rat antral circular smooth muscle contractile responses to the cholinomimetic agent,bethanechol and the subtypes of muscarinic receptors mediating the cholinergic contraction. METHODS:Circular smooth muscle strips from the antrum of Sprague-Dawley rats were mounted in muscle baths in Krebs buffer.Isometric tension was recorded.Cumulative concentration-response curves were obtained for(+)-cis- dioxolane(cD),a nonspecific muscarinic agonist,at 10^(-8)- 10^(-4)mol/L,in the presence of tetrodotoxin(TTX,10^(-7)mol/L). Results were normalized to cross sectional area.A repeat concentration-response curve was obtained after incubation of the muscle for 90 min with antagonists for M1(pirenzepine), M2(methoctramine)and M3(darifenadn)muscarinic receptor subtypes.The sensitivity to PTX was tested by the ip injection of 100 mg/kg of PTX 5 d before the experiment.The antral circular smooth muscles were removed from PTX-treated and non-treated rats as strips and dispersed smooth muscle cells to identify whether PTX-linked pathway mediated the contractility to bethanechol. RESULTS:A dose-dependent contractile response observed with bethanechol,was not affected by TTx.The pretreatment of rats with pertussis toxin decreased the contraction induced by bethanechol.Lack of calcium as well as the presence of the L-type calcium channel blocker,nifedipine,also inhibited the cholinergic contraction,with a reduction in response from 2.5±0.4 g/mm^2 to 1.2±0.4 g/mm^2(P<0.05).The dose- response curves were shifted to the right by muscarinic antagonists in the following order of affinity:darifenacin (M_3)>methocramine(M_2)>pirenzepine(M_1). CONCLUSION:The muscarinic receptors-dependent contraction of rat antral circular smooth muscles was linked to the signal transduction pathway(s)involving pertussis-toxin sensitive GTP-binding proteins and to extracellular calcium via L-type voltage gated calcium channels.The presence of the residual contractile response after the treatment with nifedipine,suggests that an additional pathway could mediate the cholinergic contraction.The involvement of more than one muscarinic receptor(functionally predominant type 3 over type 2)also suggests more than one pathway mediating the cholinergic contraction in rat antrum.展开更多
为了探讨红枣水提剂对小鼠肠运动功能的影响,试验采用中华墨汁推进试验,将24只昆明小鼠随机分成6组,每组4只(雌雄各半),分别为Ⅰ组生理盐水组,Ⅱ组红枣水提剂组,Ⅲ组硫酸阿托品注射液组,Ⅳ组氯化氨甲酰甲胆碱注射液组,Ⅴ组红枣加硫酸阿...为了探讨红枣水提剂对小鼠肠运动功能的影响,试验采用中华墨汁推进试验,将24只昆明小鼠随机分成6组,每组4只(雌雄各半),分别为Ⅰ组生理盐水组,Ⅱ组红枣水提剂组,Ⅲ组硫酸阿托品注射液组,Ⅳ组氯化氨甲酰甲胆碱注射液组,Ⅴ组红枣加硫酸阿托品组,Ⅵ组红枣加氯化氨甲酰甲胆碱组,各组小鼠在试验前禁食8 h,给药5 min后,所有小鼠灌胃10%的中华墨汁0.2 m L/只,观察分析红枣水提剂对小鼠肠运动情况的影响。结果表明:红枣水提剂能够显著提高正常小鼠小肠墨汁推进率(P<0.05),并且能协同氯化氨甲酰甲胆碱提高小鼠小肠墨汁推进率,推进率为(93.43±2.15)%。说明红枣水提剂能够明显促进小鼠小肠运动,且对氯化氨甲酰甲胆碱促进小肠推进有协同作用。展开更多
文摘Background: Bethanechol chloride, a cholinergic agonist, is often prescribed in suspected underactive bladders to improve detrusor contractility, despite its limited clinical efficacy. We investigated the usage pattern of bethanechol in actual practice with the understanding that it would enable the physicians to make an informed decision on the coherent use of bethanechol. Methods: A nation-wide survey was carried out to obtain the responses of the urologists. Out of the 755 urologists approached, 630 survey responses were considered for analysis. Results: Usage of bethanechol was advocated as very common [318 (50.48%)], common [200 (31.75%)], not so common [107 (16.98%)], and rare [5 (0.79%)] in postoperative urinary retention, where it was preferred either exclusively [255 (40.48%)] or along with alpha blockers [247 (39.21%)]. Predilection to use alpha-blocker [247 (39.21%)], alpha-blocker plus naloxone [4 (0.64%)], naloxone [1 (0.16%)], alpha-blocker plus bethanechol plus naloxone [1 (0.16%)] was also observed. It was also preferred individually in pathologies causing urinary retention such as benign prostatic hyperplasia [125 (19.84%)], diabetic neuropathy [82 (13.02%)], neurological diseases [69 (10.95%)], senile bladder [14 (2.22%)], drugs [13 (2.06%)], and infective/inflammatory conditions [6 (0.95%)]. Other [321 (50.95%)] physicians opted to prescribe bethanechol in two or more of the enumerated indications. Bethanechol was prescribed orally as 25 mg thrice daily [441 (70.00%)], 50 mg thrice daily [86 (13.65%)], 25 mg four times daily [59 (9.37%)], and many “strongly agree” and “agree” that its sustained release formulation may offer better treatment compliance [565 (89.68%)], safety [548 (86.99%)], and efficacy [544 (86.35%)]. Conclusion: Bethanechol was the most prescribed drug for the management of postoperative urinary retention and other pathologies suspected to cause underactive bladder.
文摘AIM:To investigate the pathway(s)mediating rat antral circular smooth muscle contractile responses to the cholinomimetic agent,bethanechol and the subtypes of muscarinic receptors mediating the cholinergic contraction. METHODS:Circular smooth muscle strips from the antrum of Sprague-Dawley rats were mounted in muscle baths in Krebs buffer.Isometric tension was recorded.Cumulative concentration-response curves were obtained for(+)-cis- dioxolane(cD),a nonspecific muscarinic agonist,at 10^(-8)- 10^(-4)mol/L,in the presence of tetrodotoxin(TTX,10^(-7)mol/L). Results were normalized to cross sectional area.A repeat concentration-response curve was obtained after incubation of the muscle for 90 min with antagonists for M1(pirenzepine), M2(methoctramine)and M3(darifenadn)muscarinic receptor subtypes.The sensitivity to PTX was tested by the ip injection of 100 mg/kg of PTX 5 d before the experiment.The antral circular smooth muscles were removed from PTX-treated and non-treated rats as strips and dispersed smooth muscle cells to identify whether PTX-linked pathway mediated the contractility to bethanechol. RESULTS:A dose-dependent contractile response observed with bethanechol,was not affected by TTx.The pretreatment of rats with pertussis toxin decreased the contraction induced by bethanechol.Lack of calcium as well as the presence of the L-type calcium channel blocker,nifedipine,also inhibited the cholinergic contraction,with a reduction in response from 2.5±0.4 g/mm^2 to 1.2±0.4 g/mm^2(P<0.05).The dose- response curves were shifted to the right by muscarinic antagonists in the following order of affinity:darifenacin (M_3)>methocramine(M_2)>pirenzepine(M_1). CONCLUSION:The muscarinic receptors-dependent contraction of rat antral circular smooth muscles was linked to the signal transduction pathway(s)involving pertussis-toxin sensitive GTP-binding proteins and to extracellular calcium via L-type voltage gated calcium channels.The presence of the residual contractile response after the treatment with nifedipine,suggests that an additional pathway could mediate the cholinergic contraction.The involvement of more than one muscarinic receptor(functionally predominant type 3 over type 2)also suggests more than one pathway mediating the cholinergic contraction in rat antrum.
文摘为了探讨红枣水提剂对小鼠肠运动功能的影响,试验采用中华墨汁推进试验,将24只昆明小鼠随机分成6组,每组4只(雌雄各半),分别为Ⅰ组生理盐水组,Ⅱ组红枣水提剂组,Ⅲ组硫酸阿托品注射液组,Ⅳ组氯化氨甲酰甲胆碱注射液组,Ⅴ组红枣加硫酸阿托品组,Ⅵ组红枣加氯化氨甲酰甲胆碱组,各组小鼠在试验前禁食8 h,给药5 min后,所有小鼠灌胃10%的中华墨汁0.2 m L/只,观察分析红枣水提剂对小鼠肠运动情况的影响。结果表明:红枣水提剂能够显著提高正常小鼠小肠墨汁推进率(P<0.05),并且能协同氯化氨甲酰甲胆碱提高小鼠小肠墨汁推进率,推进率为(93.43±2.15)%。说明红枣水提剂能够明显促进小鼠小肠运动,且对氯化氨甲酰甲胆碱促进小肠推进有协同作用。
