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吲哚布芬(K 3920)的临床药理学研究:血小板聚集抑制剂

Clinical pharmacology studies with indobufen (K 3920): inhibitor of platelet aggregation.

作者信息

Vinazzer H, Fuccella L M

出版信息

J Clin Pharmacol. 1980 May-Jun;20(5-6 Pt 1):316-25. doi: 10.1177/009127008002000502.

Abstract

When given to 12 subjects at single oral doses of 100 and 300 mg, indobufen caused clear-cut, dose-dependent, reversible inhibition of epinephrine- and collagen-induced platelet aggregation. Platelet factor 3 availability and platelet factor 4 release were not affected by the lower dose but were markedly reduced by the 300-mg dose. Bleeding time was slightly influenced by 100 mg, and 300 mg had a more pronounced effect. Indobufen 300 mg was also intravenously injected to five subjects. When washed platelets obtained before indobufen were resuspended in plasma obtained after indobufen, aggregation was inhibited. This was not the case when washed platelets obtained after indobufen were resuspended in plasma obtained before indobufen. These experiments indicate tha indobufen causes reversible inhibition of platelet functions unlike the effect of acetylsalicylic acid.

摘要

给12名受试者单次口服100毫克和300毫克剂量的吲哚布芬后,吲哚布芬对肾上腺素和胶原诱导的血小板聚集产生了明确的、剂量依赖性的、可逆性抑制作用。较低剂量对血小板因子3的可用性和血小板因子4的释放没有影响,但300毫克剂量可使其显著降低。100毫克剂量对出血时间有轻微影响,300毫克剂量的影响更为显著。还对5名受试者静脉注射了300毫克吲哚布芬。将吲哚布芬给药前获取的洗涤血小板重悬于吲哚布芬给药后获取的血浆中时,聚集受到抑制。而将吲哚布芬给药后获取的洗涤血小板重悬于吲哚布芬给药前获取的血浆中时,情况并非如此。这些实验表明,与阿司匹林的作用不同,吲哚布芬可引起血小板功能的可逆性抑制。

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