慢性肝病中拉贝洛尔首过代谢降低。
Decreased first-pass metabolism of labetalol in chronic liver disease.
作者信息
Homeida M, Jackson L, Roberts C J
出版信息
Br Med J. 1978 Oct 14;2(6144):1048-50. doi: 10.1136/bmj.2.6144.1048.
The effect of chronic liver disease on the rate of elimination and extent of "first-pass" metabolism of labetalol was studied. Pharmacokinetic measurements were made after both oral and intravenous administration to seven healthy subjects and to 10 patients with chronic liver disease. Plasma half life was similar in the two groups. Plasma concentrations were considerably higher in the patients than in the healthy subjects after oral administration but similar after intravenous injection. Thus the bioavailability of labetalol was increased in liver disease due to reduced first-pass metabolism. Bioavailability in the group of patients correlated negatively with serum albumin concentration. There were falls in supine heart rate and blood pressure which tended to be greater after oral administration in the patients with liver disease, suggesting an exaggerated response related to the increased bioavailability. Oral dosage requirements of labetalol and possibly other drugs susceptible to first-pass metabolism are reduced in the presence of liver disease.
研究了慢性肝病对拉贝洛尔消除速率和“首过”代谢程度的影响。对7名健康受试者和10名慢性肝病患者进行了口服和静脉给药后的药代动力学测量。两组的血浆半衰期相似。口服给药后患者的血浆浓度明显高于健康受试者，但静脉注射后相似。因此，由于首过代谢减少，拉贝洛尔在肝病患者中的生物利用度增加。患者组的生物利用度与血清白蛋白浓度呈负相关。肝病患者仰卧心率和血压下降，口服给药后下降趋势更明显，提示与生物利用度增加相关的反应过度。肝病患者拉贝洛尔以及可能其他易受首过代谢影响的药物的口服剂量需求降低。
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