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Over one\u2010fourth (25\u00b78 per cent) of a 2 mg kg<jats:sup>\u22121<\/jats:sup> intraportal dose of <jats:sup>3<\/jats:sup>H\u2010pentacaine was excreted in bile in urethaneanaesthetized control rats within 3 h. The radioactivity appeared in the form of the parent drug, basic metabolites, and metabolite conjugates, 3\u00b71, 86\u00b75, and 10\u00b74 per cent of the total radioactivity excreted, respectively. Pretreatment of rats with phenobarbital enhanced only slightly the biliary excretion of basic metabolites, and pretreatment with 3\u2010methylcholanthrene had no effect. Phenobarbital also increased the initial rate of excretion of conjugates, but this effect was not sustained. 3\u2010Methylcholanthrene had a tendency to impair excretion of conjugates by bile. Pretreatment of rats with SKF 525\u2010A decreased the biliary excretion of both basic metabolites and conjugates while cimetidine did not alter significantly the biliary excretion of pentacaine metabolites. These results suggest that the canalicular transport of metabolites may be the most important factor in controlling pentacaine metabolite excretion in bile.<\/jats:p>","DOI":"10.1002\/bdd.2510110504","type":"journal-article","created":{"date-parts":[[2006,10,14]],"date-time":"2006-10-14T12:13:19Z","timestamp":1160827999000},"page":"395-401","source":"Crossref","is-referenced-by-count":0,"title":["Effects of inducers and inhibitors of mixed\u2010function oxidases on the biliary excretion of pentacaine metabolites"],"prefix":"10.1002","volume":"11","author":[{"given":"M.","family":"Kukan","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"\u0160.","family":"Bezek","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"V.","family":"\u0160\u010dasn\u00e1r","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"M.","family":"\u010euri\u0161ov\u00e1","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"T.","family":"Trnovec","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2006,1,11]]},"reference":[{"key":"e_1_2_1_2_2","first-page":"1902","volume":"19","author":"Bene\u0161 L.","year":"1969","journal-title":"Arzneim. 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