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This double\u2010blind, placebo\u2010controlled crossover study with six healthy volunteers is the first to date investigating the role of the ADH inhibitor fomepizole (4\u2010methylpyrazole (4MP)) in moderating this conversion in humans. Participants received on two different days either intravenous placebo or 15\u00a0mg\/kg 4MP followed by oral administration of 25\u00a0mg\/kg BDO. Pretreatment with 4MP resulted in significantly higher BDO maximal plasma concentration (<jats:italic><jats:bold>P<\/jats:bold><\/jats:italic>\u00a0=\u00a00.001) and area under the concentration\u2010time curve (AUC; <jats:italic><jats:bold>P<\/jats:bold><\/jats:italic>\u00a0=\u00a00.028), confirming that ADH is the primary pathway for the conversion of BDO to GHB in humans. With 4MP, the mean arterial pressure was significantly lower at 105\u00a0minutes compared to baseline (<jats:italic><jats:bold>P<\/jats:bold><\/jats:italic>\u00a0=\u00a00.003), indicating that blood pressure lowering, observed not with a temporal relationship to 4MP administration\u00a0but after the maximum BDO concentration was reached, may be an intrinsic effect of BDO.<\/jats:p>","DOI":"10.1002\/cpt.1306","type":"journal-article","created":{"date-parts":[[2018,11,19]],"date-time":"2018-11-19T08:34:30Z","timestamp":1542616470000},"page":"1196-1203","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":10,"title":["Butanediol Conversion to Gamma\u2010Hydroxybutyrate Markedly Reduced by the Alcohol Dehydrogenase Blocker Fomepizole"],"prefix":"10.1111","volume":"105","author":[{"given":"Evangelia","family":"Liakoni","sequence":"first","affiliation":[{"name":"Division of Clinical Pharmacology and Experimental Therapeutics Department of Medicine University of California  San Francisco California USA"},{"name":"Clinical Pharmacology and Toxicology Department of General Internal Medicine, Inselspital Bern University Hospital University of Bern  Bern Switzerland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hallam","family":"Gugelmann","sequence":"additional","affiliation":[{"name":"California Poison Control Center University of California  San Francisco California USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Delia A.","family":"Dempsey","sequence":"additional","affiliation":[{"name":"Division of Clinical Pharmacology and Experimental Therapeutics Department of Medicine University of California  San Francisco California USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Timothy J.","family":"Wiegand","sequence":"additional","affiliation":[{"name":"University of Rochester Medical Center  Rochester New York USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Christopher","family":"Havel","sequence":"additional","affiliation":[{"name":"Division of Clinical Pharmacology and Experimental Therapeutics Department of Medicine University of California  San Francisco California USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Peyton","family":"Jacob","sequence":"additional","affiliation":[{"name":"Division of Clinical Pharmacology and Experimental Therapeutics Department of Medicine University of California  San Francisco California USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Neal L.","family":"Benowitz","sequence":"additional","affiliation":[{"name":"Division of Clinical Pharmacology and Experimental Therapeutics Department of Medicine University of California  San Francisco California USA"},{"name":"California Poison Control Center University of California  San Francisco California USA"},{"name":"Department of Bioengineering and Therapeutic Sciences University of California  San Francisco California USA"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2019,1,8]]},"reference":[{"key":"e_1_2_10_1_1","doi-asserted-by":"publisher","DOI":"10.1592\/phco.22.9.798.34063"},{"key":"e_1_2_10_2_1","doi-asserted-by":"publisher","DOI":"10.2165\/00002018-200427050-00002"},{"key":"e_1_2_10_3_1","unstructured":"Product Information: Xyrem\u00aeoral solution sodium oxybate oral solution(Jazz Pharmaceuticals (per FDA) Palo Alto CA 2012). <http:\/\/pp.jazzpharma.com\/pi\/xyrem.en.USPI.pdf>."},{"key":"e_1_2_10_4_1","doi-asserted-by":"publisher","DOI":"10.1186\/s13049-016-0299-z"},{"key":"e_1_2_10_5_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.toxlet.2017.05.030"},{"key":"e_1_2_10_6_1","doi-asserted-by":"publisher","DOI":"10.1093\/jat\/23.3.141"},{"key":"e_1_2_10_7_1","doi-asserted-by":"publisher","DOI":"10.1177\/0269881105049041"},{"key":"e_1_2_10_8_1","first-page":"1","article-title":"NTP summary report on the metabolism, disposition, and toxicity of 1,4\u2010butanediol (CAS No. 110\u201063\u20104)","volume":"54","author":"Irwin R.D.","year":"1996","journal-title":"Toxic. 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