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原发性高血压患者中普萘洛尔与阿替洛尔的药代动力学比较

[Pharmacokinetic comparison of propranolol and atenolol in people with primary hypertension].

作者信息

Telatyńska-Smieszek Bogumiła

机构信息

Kliniki Nefrologii, Transplantologii i Chorób Wewnetrznych Instytutu Chorób Wewnetrznych Pomorskiej Akademii Medycznej w Szczecinie, al. Powstańców Wlkp. 72, 70-111 Szczecin.

出版信息

Ann Acad Med Stetin. 2002;48:367-80.

Abstract

The influence of primary hyperlipidemia on the pharmacokinetics of lipophilic propranolol and hydrophilic atenolol was studied. Thirty patients with hypercholesterolemia, hypertriglyceridemia and mixed hyperlipidemia and healthy subjects were enrolled. A single dose of 80 mg propranolol or 100 mg atenolol was administered orally using a cross-over study design. Pharmacokinetic parameters were calculated according to the noncompartmental open model. The results reflect the general tendency to altered pharmacokinetics of lipophilic and hydrophilic drugs in patients with disorders of lipid metabolism. In the case of lipophilic propranolol, the most pronounced changes were observed in mixed hyperlipidemia, with a tendency to reduced steady state distribution volume, decrease in the elimination rate constant and total body clearance. In conclusion, the present study revealed an influence of lipid disorders on the pharmacokinetics of beta-blockers, with the most significant alterations seen in mixed hyperlipidemia. The dosage of beta-blockers should be modified in patients with an abnormal lipid profile in serum.

摘要

研究了原发性高脂血症对亲脂性普萘洛尔和亲水性阿替洛尔药代动力学的影响。纳入了30例高胆固醇血症、高甘油三酯血症和混合性高脂血症患者以及健康受试者。采用交叉研究设计口服单剂量80mg普萘洛尔或100mg阿替洛尔。根据非房室开放模型计算药代动力学参数。结果反映了脂质代谢紊乱患者亲脂性和亲水性药物药代动力学改变的总体趋势。对于亲脂性普萘洛尔,在混合性高脂血症中观察到最明显的变化,稳态分布容积有降低趋势,消除速率常数和全身清除率降低。总之,本研究揭示了脂质紊乱对β受体阻滞剂药代动力学的影响,在混合性高脂血症中观察到最显著的改变。血清脂质谱异常的患者应调整β受体阻滞剂的剂量。

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