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选择性β受体阻滞剂他林洛尔在人体中的胆汁排泄

The biliary elimination of the selective beta-receptor blocking drug talinolol in man.

作者信息

Terhaag B, Gramatté T, Richter K, Voss J, Feller K

机构信息

Institute of Clinical Pharmacology, Medical Academy Carl Gustav Carus, Dresden, GDR.

出版信息

Int J Clin Pharmacol Ther Toxicol. 1989 Apr;27(4):170-2.

PMID:2565889
Abstract

The biliary elimination of the beta-1-receptor blocking agent talinolol was investigated after intravenous administration of 30 mg in 6 patients with a T-tube drain after cholecystectomy. Serum concentration decreased in a biexponential manner with a median terminal half-life time of 4.4 h (range: 3.0-6.2 h). In some patients a second peak of the serum level was found. Concentration-time curves in bile paralleled serum profiles. The bile:serum concentration ratio (b:s-ratio) ranged from 24 to 98. The biliary clearance amounted to 43 ml/h.kg (range: 13-212 ml/h.kg). The median of the amount of talinolol eliminated by bile was 2.8 mg (range: 1.1-7.4 mg). It is concluded that talinolol undergoes an enterohepatic circulation. However, the amount eliminated cannot provide a sufficient explanation for the second peak, observed in some patients.

摘要

在6例胆囊切除术后留置T形管引流的患者静脉注射30 mgβ1受体阻滞剂他林洛尔后,研究了其经胆汁的排泄情况。血清浓度呈双指数下降,中位终末半衰期为4.4小时(范围:3.0 - 6.2小时)。部分患者血清水平出现第二个峰值。胆汁中的浓度 - 时间曲线与血清曲线平行。胆汁与血清浓度比(b:s比)范围为24至98。胆汁清除率为43 ml/h·kg(范围:13 - 212 ml/h·kg)。经胆汁排泄的他林洛尔量的中位数为2.8 mg(范围:1.1 - 7.4 mg)。结论是他林洛尔存在肝肠循环。然而,排泄量不足以充分解释部分患者中观察到的第二个峰值。

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1
The biliary elimination of the selective beta-receptor blocking drug talinolol in man.选择性β受体阻滞剂他林洛尔在人体中的胆汁排泄
Int J Clin Pharmacol Ther Toxicol. 1989 Apr;27(4):170-2.
2
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Multiple peaking phenomena in pharmacokinetic disposition.
药代动力学处置中的多重峰现象。
Clin Pharmacokinet. 2010 Jun;49(6):351-77. doi: 10.2165/11319320-000000000-00000.
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Unexpected effect of concomitantly administered curcumin on the pharmacokinetics of talinolol in healthy Chinese volunteers.姜黄素与他林洛尔同时给药对健康中国志愿者他林洛尔药代动力学的意外影响。
Eur J Clin Pharmacol. 2007 Jul;63(7):663-8. doi: 10.1007/s00228-007-0298-0. Epub 2007 Apr 28.
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In silico modeling of non-linear drug absorption for the P-gp substrate talinolol and of consequences for the resulting pharmacodynamic effect.对P-糖蛋白底物他林洛尔的非线性药物吸收进行计算机模拟及其对药效学效应的影响。
Pharm Res. 2006 Aug;23(8):1712-20. doi: 10.1007/s11095-006-9020-7.
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Simvastatin does not influence the intestinal P-glycoprotein and MPR2, and the disposition of talinolol after chronic medication in healthy subjects genotyped for the ABCB1, ABCC2 and SLCO1B1 polymorphisms.辛伐他汀不影响肠道P-糖蛋白和多特异性有机阴离子转运体2,以及在针对ABCB1、ABCC2和SLCO1B1基因多态性进行基因分型的健康受试者中长期用药后他林洛尔的处置。
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