水杨酸酯类药物的临床药代动力学。

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水杨酸酯类药物的临床药代动力学。

临床药典杂志1985 Mar-Apr;10(2):164-77。doi: 10.2165 / 00003088-198510020-00004。

PubMed ID

3888490 (PubMed视图

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摘要

水杨酸酯类药物用于治疗风湿病已有100多年的历史。最近对其对血小板和内皮细胞功能的修饰的认识已导致其在其他医学领域的使用。阿司匹林(乙酰水杨酸)仍然是最常用的水杨酸。阿司匹林以水溶液形式口服后，在胃的pH值较低时被迅速吸收。其他配方的吸收速度较慢，这是由于片剂崩解的速率限制步骤——后者在碱性ph下最大。阿司匹林的吸收率不仅取决于配方，还取决于胃排空率。阿司匹林的吸收遵循一级动力学，吸收半衰期为5 - 16分钟。阿司匹林被非特异性酯酶水解为水杨酸发生在肝脏中，在较小程度上发生在胃中，因此只有68%的剂量作为阿司匹林进入体循环。阿司匹林和水杨酸都与血清白蛋白结合(阿司匹林能不可逆地使许多蛋白质乙酰化)，两者都分布在滑膜腔、中枢神经系统和唾液中。阿司匹林的血清半衰期大约为20分钟。阿司匹林浓度的下降与水杨酸浓度的迅速上升有关。 Salicylic acid is renally excreted in part unchanged and the rate of elimination is influenced by urinary pH, the presence of organic acids, and the urinary flow rate. Metabolism of salicylic acid occurs through glucuronide formation (to produce salicyluric acid), and salicyl phenolic glucoronide), conjugation with glycine (to produce salicyluric acid), and oxidation to gentisic acid. The rate of formation of salicyl phenolic glucuronide and salicyluric acid are easily saturated at low salicylic acid concentrations and their formation is described by Michaelis-Menten kinetics. The other metabolic products follow first-order kinetics. The serum half-life of salicylic acid is dose-dependent; thus, the larger the dose employed, the longer it will take to reach steady-state. There is also evidence that enzyme induction of salicyluric acid formation occurs. No significant differences exist between the pharmacokinetics of the salicylates in the elderly or in children when compared with young adults. Apart from differences in free versus albumin-bound salicylate in various disease states and physiological conditions associated with low serum albumin, pharmacokinetic parameters in patients with rheumatoid arthritis, osteoarthritis, chronic renal failure or liver disease are essentially the same.(ABSTRACT TRUNCATED AT 400 WORDS)

引用本文的药物库数据

药物

水杨酸苯酯

胆碱水杨酸