普萘洛尔对人体茶碱代谢抑制作用的选择性和剂量依赖性。
Selectivity and dose-dependency of the inhibitory effect of propranolol on theophylline metabolism in man.
作者信息
Miners J O, Wing L M, Lillywhite K J, Robson R A
出版信息
Br J Clin Pharmacol. 1985 Sep;20(3):219-23. doi: 10.1111/j.1365-2125.1985.tb05064.x.
Abstract
The effects of separate 5 day pretreatments of propranolol 120 mg day-1 and 720 mg day-1 on theophylline clearance and metabolism at steady-state were determined in seven healthy males. Propranolol 120 mg day-1 decreased theophylline plasma clearance (CL) by 30%. Clearance of theophylline to each metabolite was reduced by this treatment, clearances to the two demethylated products by 42-43% and clearance to the 8-hydroxylation product by 27%. Propranolol 720 mg day-1 decreased theophylline CL by 52%. Again, clearance of theophylline to each metabolite was reduced by this treatment, clearances to the two demethylation products by 73-77% and clearance to the 8-hydroxylation product by 44%. These data are consistent with a dose-dependent and selective inhibitory effect of propranolol on the separate forms of cytochrome P-450 involved in theophylline demethylation and 8-hydroxylation.
摘要
在7名健康男性中，测定了每天120毫克和每天720毫克的普萘洛尔分别进行5天预处理对稳态时茶碱清除率和代谢的影响。每天120毫克的普萘洛尔使茶碱的血浆清除率（CL）降低了30%。该处理降低了茶碱向每种代谢物的清除率，向两种去甲基化产物的清除率降低了42 - 43%，向8 - 羟基化产物的清除率降低了27%。每天720毫克的普萘洛尔使茶碱CL降低了52%。同样，该处理降低了茶碱向每种代谢物的清除率，向两种去甲基化产物的清除率降低了73 - 77%，向8 - 羟基化产物的清除率降低了44%。这些数据与普萘洛尔对参与茶碱去甲基化和8 - 羟基化的细胞色素P - 450不同形式具有剂量依赖性和选择性抑制作用一致。
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