Kurata N, Hurst H E, Benz F W, Kemper R A, Waddell W J
Department of Pharmacology and Toxicology, University of Louisville School of Medicine, KY 40292.
Drug Metab Dispos. 1991 Mar-Apr;19(2):388-93.
Ethanol and a variety of other compounds previously have been shown to acutely inhibit the metabolism of ethyl carbamate (EC) when given concurrently in mice. On the other hand, ethanol pretreatment (10% in drinking water for the period 48 to 12 hr prior to EC treatment) is known to have the opposite effect and enhance the clearance of EC from blood of mice. In the present work, acetone has been shown to act similarly. Concurrent acetone treatment inhibits the metabolism of EC (11.1 mg/kg po) in male A/JAX mice in a dose-response manner. Blood clearance (Cl) of this po dose of EC from mice following concurrent acetone treatment (50 mg/kg, 0.86 mmol/kg ip) averaged 185 +/- 5.4 (SE) ml hr-1 kg-1 vs. controls of 804 +/- 24.6 ml hr-1 kg-1. Comparing doses that produce equal effects on the blood clearance values of EC, acetone is approximately 50-fold more potent as an inhibitor than ethanol. Pretreatment of mice with acetone (2 g/kg ip) 48 hr and 24 hr before EC administration po increased the clearance of EC approximately 3-fold (CI = 2623 +/- 123 ml hr-1 kg-1). 2-Propanol was found to be at least as potent as inhibitor as acetone, but with a longer duration of inhibition; this longer duration was explained by the longer persistence of acetone in blood from conversion of 2-propanol to acetone.(ABSTRACT TRUNCATED AT 250 WORDS)
乙醇和其他多种化合物先前已被证明,在小鼠中同时给予时可急性抑制氨基甲酸乙酯(EC)的代谢。另一方面,已知乙醇预处理(在给予EC前48至12小时,饮用水中含10%乙醇)具有相反的效果,可增强小鼠血液中EC的清除率。在本研究中,已证明丙酮也有类似作用。同时给予丙酮可抑制雄性A/JAX小鼠中EC(11.1毫克/千克,口服)的代谢,呈剂量反应关系。同时给予丙酮(50毫克/千克,0.86毫摩尔/千克,腹腔注射)后,该口服剂量的EC从小鼠体内的血液清除率(Cl)平均为185±5.4(标准误)毫升·小时⁻¹·千克⁻¹,而对照组为804±24.6毫升·小时⁻¹·千克⁻¹。比较对EC血液清除率产生同等效应的剂量时,丙酮作为抑制剂的效力约为乙醇的50倍。在口服给予EC前48小时和24小时,用丙酮(2克/千克,腹腔注射)预处理小鼠,可使EC的清除率提高约3倍(Cl = 2623±123毫升·小时⁻¹·千克⁻¹)。发现2-丙醇作为抑制剂的效力至少与丙酮相同,但抑制持续时间更长;这种较长的持续时间可由2-丙醇转化为丙酮后在血液中持续时间更长来解释。(摘要截短于250字)