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Further, limited data on its activity on non\u2010gastrointestinal (GI) smooth muscle spasms after oral dosing are available, causing its effects beyond the GI tract to be questioned. This pharmacokinetic\/pharmacodynamic (PK\/PD) study, conducted using female rats, aimed to cover this gap.<\/jats:p><\/jats:sec><jats:sec><jats:title>Experimental Approach<\/jats:title><jats:p>PK study: HBB and atropine (as a comparator agent) were administered PO and IV to rats, and concentrations in plasma and tissues (colon, uterus and urinary bladder; CUB) were measured. PD study 1: concentration\u2013response curves of HBB and atropine (10<jats:sup>\u22129<\/jats:sup>\u201310<jats:sup>\u22124<\/jats:sup>\u2009M) were obtained for carbachol\u2010induced (10<jats:sup>\u22125<\/jats:sup>\u2009M) pre\u2010contracted tissues; PD study 2: CUB were pre\u2010incubated with HBB and atropine at maximum concentrations (<jats:italic>C<\/jats:italic><jats:sub>max<\/jats:sub>) from PK studies and carbachol concentration\u2013response curves (10<jats:sup>\u22129<\/jats:sup>\u201310<jats:sup>\u22124<\/jats:sup>\u2009M) were obtained; PD study 3: HBB and atropine were administered PO and IV to rats as for PK study, CUB tissues were collected at 0.5\u2009h (IV) and 4\u2009h (PO), and carbachol concentration\u2013response curves (10<jats:sup>\u22129<\/jats:sup>\u201310<jats:sup>\u22124<\/jats:sup>\u2009M) obtained.<\/jats:p><\/jats:sec><jats:sec><jats:title>Key Results<\/jats:title><jats:p>PO HBB showed higher <jats:italic>C<\/jats:italic><jats:sub>max<\/jats:sub> in CUB tissues than in plasma. HBB and atropine reduced, concentration\u2010dependently, carbachol\u2010induced contractions in CUB tissues. PO HBB showed highest spasmolytic activity in colon (40%), followed by uterus (30%) and urinary bladder (10%).<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusion and Implications<\/jats:title><jats:p>This is the first comparison of PO and IV HBB and atropine in GI and non\u2010GI tissues. Despite low bioavailability, PO HBB accumulated and exerted spasmolytic effects in tissues beyond the GI tract.<\/jats:p><\/jats:sec>","DOI":"10.1111\/bph.17474","type":"journal-article","created":{"date-parts":[[2025,2,13]],"date-time":"2025-02-13T23:45:01Z","timestamp":1739490301000},"page":"2487-2502","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":1,"title":["Oral hyoscine butylbromide exerts spasmolytic effects in both gastrointestinal and urogenital tissues in rats"],"prefix":"10.1111","volume":"182","author":[{"given":"Sara","family":"Traserra","sequence":"first","affiliation":[{"name":"Department of Cell Biology, Physiology and Immunology and Neurosciences Institute Universitat Aut\u00f2noma de Barcelona  Barcelona Spain"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Terence","family":"Appelqvist","sequence":"additional","affiliation":[{"name":"Sanofi  Neuilly\u2010sur\u2010Seine 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