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[口服抗凝剂的药理学]

[Pharmacology of oral anticoagulants].

作者信息

Richter M, Markwardt F

出版信息

Z Gesamte Inn Med. 1979 Jan 1;34(1):8-17.

PMID:433362
Abstract

The present view on the mechanism of vitamin K-dependent synthesis of the clotting factors II, VII, IX and X in the liver and its inhibition by 4-hydroxycoumarine and 1,3-indandione-type anticoagulants is given. The discovery of gamma-carboxyglutamyl residues in intact clotting factors and the role of this amino acid as the calcium-binding principle is pointed out. After general considerations on the pharmacokinetics of coumarine-type anticoagulants detailed information on the pharmacokinetics of phenprocoumon, almost exclusively used in the GDR, is presented. The importance of pharmacokinetic aspects for control of oral anticoagulation is emphasized. As a possible tool for evaluation of individual pharmacokinetic parameters during already ongoing medication the additional administration of a single dose of radioactively labelled anticoagulant is proposed. Toxic effects in case of overdosage, untoward reactions and interference with oral anticoagulants by comedication are described.

摘要

本文阐述了目前关于肝脏中维生素K依赖的凝血因子II、VII、IX和X合成机制以及4-羟基香豆素和1,3-茚二酮类抗凝剂对其抑制作用的观点。指出了完整凝血因子中γ-羧基谷氨酸残基的发现以及该氨基酸作为钙结合原理的作用。在对香豆素类抗凝剂的药代动力学进行一般性考虑之后,介绍了几乎仅在民主德国使用的苯丙香豆素的药代动力学详细信息。强调了药代动力学方面对口服抗凝控制的重要性。作为评估正在进行的药物治疗期间个体药代动力学参数的一种可能工具,建议额外给予单剂量放射性标记的抗凝剂。描述了过量用药时的毒性作用、不良反应以及合并用药对口服抗凝剂的干扰。

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