Clenbuterol gehört zu den langwirksamen Spasmolytika, wobei es neben Bambuterol eines der wenigen Beta-2-Sympathomimetikum darstellt, die oral eingenommen werden können. Die Elimination erfolgt sowohl über den Urin als auch über den Stuhl. Die Plasmahalbwertszeit beträgt ungefähr 37 Stunden.
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