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Related Experiment Videos

alpha1-adrenoceptor selectivity: the North American experience.

M G Wyllie1

  • 1Urodoc, Herne Bay, Kent, UK. urodoc@dial.pipex.com

European Urology
|July 7, 1999
PubMed
Summary

The 0.4 mg dose of tamsulosin is suboptimal for blocking alpha-adrenergic receptors, offering less efficacy than 0.8 mg. This dose is equivalent to 1 mg of doxazosin, with no evidence of prostate selectivity observed for tamsulosin.

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Area of Science:

  • Pharmacology
  • Urology

Background:

  • Recent studies suggest tamsulosin's response may be dose-dependent and suboptimal at 0.4 mg.
  • Investigating the dose-response relationship of alpha-blockers is crucial for optimizing treatment.

Purpose of the Study:

  • To determine pharmacologically equivalent alpha-blocking doses of doxazosin and tamsulosin.
  • To further evaluate the concepts of 'uroselectivity' and 'prostate selectivity' in a clinical context.

Main Methods:

  • Controlled, crossover studies in healthy male volunteers.
  • Measurement of phenylephrine (PE)-induced urethral and vascular responses.
  • Correlation of drug effects with plasma concentrations and in vitro receptor binding data.

Main Results:

  • Doxazosin demonstrated effective blockade of PE-induced responses from 1-16 mg without organ selectivity.
  • Tamsulosin's blockade efficacy was time-dependent.
  • 0.4 mg tamsulosin showed significantly less blockade than 0.8 mg tamsulosin or 1 mg doxazosin.

Conclusions:

  • No evidence of prostate selectivity for tamsulosin was found.
  • 0.4 mg tamsulosin is an under-dosed regimen, equivalent to 1 mg of doxazosin.
  • Future studies should assess a range of doses including the ED50 for benefit-risk analysis.

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