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肾盂和逼尿肌平滑肌对替芬那明、奥昔布宁和维拉帕米的体外药理反应分析。

Analysis of the in vitro pharmacologic response of renal pelvis and detrusor smooth muscle to thiphenamil, oxybutynin and verapamil.

作者信息

Levounis P, Constantinou C E

机构信息

Stanford University Medical School, Calif.

出版信息

Urol Int. 1988;43(4):211-8. doi: 10.1159/000281340.

DOI:10.1159/000281340
PMID:3188289
Abstract

A new computerized methodology was used to acquire and analyze the relative pharmacologic sensitivity of the renal pelvis and urinary bladder of the rabbit to pharmacologic stimulation. Comparison was made of the effects of thiphenamil, verapamil and oxybutynin on the spontaneous contractions of isolated detrusor and renal pelvis. Data collected by computer were evaluated in terms of amplitude, frequency, and tension change to varying concentration of pharmacologic stimulation. Data were analyzed using a frequency/time domain algorithm developed specifically to evaluate the contribution of the oscillatory components of tension associated with smooth muscle tissues. For the renal pelvis the results show 6 X 10(-5) M thiphenamil, 10(-3) M oxybutynin, and 5 X 10(-6) M verapamil resulted in a 50% inhibition of the phasic contractions. Thiphenamil significantly increased the contractile frequency of the renal pelvis. For the bladder 10(-3) M thiphenamil resulted in a 50% inhibition of the phasic contractions, while 3 X 10(-4) M oxybutynin and 3 X 10(-6) M verapamil were needed to achieve the same level of inhibition. Thiphenamil at lower doses (10(-4) M to 5 X 10(-4) M) showed a biphasic effect--an increase of the bladder tissue activity followed by a relaxation phase--that oxybutynin and verapamil failed to produce. The results show that the calcium blocker suppresses the spontaneous activity of the upper and lower urinary tract at lower concentrations than the anticholinergic or thiphenamil.

摘要

采用一种新的计算机化方法来获取和分析兔肾盂和膀胱对药物刺激的相对药理敏感性。比较了替哌米明、维拉帕米和奥昔布宁对离体逼尿肌和肾盂自发收缩的影响。通过计算机收集的数据根据药物刺激不同浓度下的振幅、频率和张力变化进行评估。使用专门开发的频域/时域算法分析数据,以评估与平滑肌组织相关的张力振荡成分的贡献。对于肾盂,结果显示6×10⁻⁵M替哌米明、10⁻³M奥昔布宁和5×10⁻⁶M维拉帕米可使相性收缩抑制50%。替哌米明显著增加肾盂的收缩频率。对于膀胱,10⁻³M替哌米明可使相性收缩抑制50%,而需要3×10⁻⁴M奥昔布宁和3×10⁻⁶M维拉帕米才能达到相同的抑制水平。较低剂量(10⁻⁴M至5×10⁻⁴M)的替哌米明显示出双相效应——膀胱组织活性先增加随后进入松弛期——这是奥昔布宁和维拉帕米所没有的。结果表明,钙通道阻滞剂在比抗胆碱能药物或替哌米明更低的浓度下就能抑制上尿路和下尿路的自发活动。

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1
Analysis of the in vitro pharmacologic response of renal pelvis and detrusor smooth muscle to thiphenamil, oxybutynin and verapamil.肾盂和逼尿肌平滑肌对替芬那明、奥昔布宁和维拉帕米的体外药理反应分析。
Urol Int. 1988;43(4):211-8. doi: 10.1159/000281340.
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引用本文的文献

1
Oxybutynin extended-release: a review of its use in the management of overactive bladder.奥昔布宁缓释制剂:用于治疗膀胱过度活动症的综述
Drugs. 2004;64(8):885-912. doi: 10.2165/00003495-200464080-00011.
2
Oxybutynin. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in detrusor instability.
Drugs Aging. 1995 Mar;6(3):243-62. doi: 10.2165/00002512-199506030-00007.