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维拉帕米抑制乙醇消除并延长醉酒感。

Verapamil inhibits ethanol elimination and prolongs the perception of intoxication.

作者信息

Bauer L A, Schumock G, Horn J, Opheim K

机构信息

Department of Pharmacy Practice, University of Washington, Seattle 98195.

出版信息

Clin Pharmacol Ther. 1992 Jul;52(1):6-10. doi: 10.1038/clpt.1992.96.

Abstract

Ten young healthy men received verapamil (80 mg every 8 hours for 6 days) or placebo in a blinded, randomized, crossover design. On the sixth day, ethanol was administered as a single oral dose (0.8 gm/kg), and blood samples were collected over the following 12 hours for determination of verapamil, norverapamil, and ethanol concentrations. Compared with placebo, verapamil increased the peak blood ethanol concentration (106.45 +/- 21.40 to 124.24 +/- 24.74 mg/dl, p less than 0.05) and area under the ethanol concentration versus time curve (365.67 +/- 93.52 to 475.07 +/- 97.24 mg.hr/dl, p less than 0.005). Verapamil areas under the concentration versus time curves (AUC) were positively correlated (r = 0.71, p less than 0.05) to increased ethanol blood AUC values. Each subject's perception of ethanol intoxication was measured by use of a simple visual analog scale. Compared with placebo, verapamil significantly increased area under the effect versus time curve (10.19 +/- 7.6 to 13.83 +/- 7.81 cm.hr, p less than 0.002) but did not change the peak effect or time to peak effect. Ethanol effect versus concentration plots were not significantly different between verapamil and placebo treatment phases when increased ethanol concentrations during verapamil therapy were taken into account. The findings of our study suggest that verapamil significantly inhibits ethanol elimination, resulting in elevated blood ethanol concentrations that prolong the intoxicating effects of alcohol.

摘要

十名年轻健康男性参与了一项采用盲法、随机、交叉设计的实验,他们被给予维拉帕米(每8小时80毫克,持续6天)或安慰剂。在第六天,给予单剂量口服乙醇(0.8克/千克),并在随后的12小时内采集血样,以测定维拉帕米、去甲维拉帕米和乙醇的浓度。与安慰剂相比,维拉帕米使血液乙醇峰值浓度升高(从106.45±21.40毫克/分升升至124.24±24.74毫克/分升,p<0.05),并且使乙醇浓度-时间曲线下面积增加(从365.67±93.52毫克·小时/分升升至475.07±97.24毫克·小时/分升,p<0.005)。维拉帕米的浓度-时间曲线下面积(AUC)与乙醇血液AUC值的增加呈正相关(r = 0.71,p<0.05)。使用简单的视觉模拟量表测量每个受试者对乙醇中毒的感知。与安慰剂相比,维拉帕米显著增加了效应-时间曲线下面积(从10.19±7.6厘米·小时增至13.83±7.81厘米·小时,p<0.002),但未改变峰值效应或达到峰值效应的时间。当考虑到维拉帕米治疗期间乙醇浓度增加的情况时,维拉帕米和安慰剂治疗阶段的乙醇效应-浓度图无显著差异。我们的研究结果表明,维拉帕米显著抑制乙醇消除,导致血液乙醇浓度升高,从而延长了酒精的中毒效应。

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