维拉帕米和硝苯地平对模型物质生物转化和吲哚菁绿消除的影响。

H Sigusch, L Henschel, A Hoffmann
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引用次数: 0

摘要

12名健康受试者在口服维拉帕米(3 × 80 mg)或硝苯地平(3 × 20 mg) 5天治疗的第5天单独接受混合模型物质(含甲胺唑:1000 mg、咖啡因:200 mg、磺胺嘧啶:500 mg和溴异喹:10 mg),以评估维拉帕米和硝苯地平对肝脏生物转化的影响。在口服维拉帕米(80 mg)或硝苯地平(20 mg) 12和1小时后静脉注射吲哚菁绿(0.5 mg/kg)观察肝脏血流。本研究未观察到维拉帕米和硝苯地平治疗对肝脏药物氧化系统的影响。口服硝苯地平(20mg)后,静脉注射吲哚菁绿的消除半衰期仅为1小时。硝苯地平(20mg)或维拉帕米(80mg)治疗后12小时以及维拉帕米(80mg)治疗后1小时,吲哚菁绿消除未见变化。估计口服硝苯地平后肝脏血流量的增加可能导致其他口服药物的吸收增加,并可能加速肝脏对高肝提取率药物的消除。快速乙酰化6例,慢速乙酰化6例。硝苯地平或维拉帕米治疗后,这种分类没有改变。
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[The effects of verapamil and nifedipine on the biotransformation of model substances and on the indocyanine green elimination].

Twelve healthy subjects received a cocktail of model substances (containing metamizol: 1000 mg, caffeine: 200 mg, sulfadimidine: 500 mg, and debrisoquine: 10 mg) alone and on the fifth day of a five day therapy of oral verapamil (3 x 80 mg) or nifedipine (3 x 20 mg) to assess the effect of verapamil and nifedipine on hepatic biotransformation. To investigate liver blood flow intravenous indocyanine green (0,5 mg/kg) was given 12 and 1 hours after oral verapamil (80 mg) or nifedipine (20 mg). In the presented study an influence of verapamil and nifedipine treatment on the hepatic drug oxidizing system was not observed. The elimination half-life of intravenous indocyanine green was only 1 hour after oral nifedipine (20 mg) significantly decreased. 12 hours after nifedipine (20 mg) or verapamil (80 mg) as well as 1 hour after verapamil (80 mg) treatment no change in indocyanine green elimination was observed. The estimated increase of liver blood flow after oral nifedipine may cause increased absorption of other oral administered drugs and may accelerate hepatic elimination of drug with high hepatic extraction rate. 6 fast an 6 slow acetylators were found. This classification did not change after nifedipine or verapamil therapy.

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