水杨酸盐的临床药物动力学。
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下午需要CJ,布鲁克斯
水杨酸盐的临床药物动力学。
Pharmacokinet。1985; 3 - 4月10 (2):164 - 77。doi: 10.2165 / 00003088-198510020-00004。
- PubMed ID
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3888490 (在PubMed]
- 文摘
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水杨酸盐的使用在风湿性疾病已经建立100多年了。最近承认他们的血小板和内皮细胞功能的修改导致药物的使用在其他领域。阿司匹林(乙酰水杨酸)仍然是最常用的水杨酸。作为水溶液中阿司匹林口服后迅速吸收低pH值的胃millieu。少快速吸收观察与其他配方是由于平板衰变的速率限制步骤——后者因素最大的碱性博士阿司匹林吸收的速度不仅依赖制定还在胃排空的速度。阿司匹林吸收遵循一阶动力学与吸收半衰期从5到16分钟。由非特异性酯酶水解的阿司匹林,水杨酸发生在肝脏,并在较小程度上,胃,因此只有68%的剂量阿司匹林到达体循环。阿司匹林和水杨酸都绑定到血清白蛋白(阿司匹林能够不可逆的乙酰化许多蛋白质),都分布在滑膜腔,中枢神经系统和唾液。阿司匹林的血清半衰期约为20分钟。阿司匹林浓度的下降与水杨酸浓度快速上升。 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)
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物