临床药代动力学性质的大环内酯物抗生素。年龄和各种病理生理状态的影响(第一部分)。

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Periti P, Mazzei T, Mini E, Novelli A

临床药代动力学性质的大环内酯物抗生素。年龄和各种病理生理状态的影响(第一部分)。

Pharmacokinet。1989年4月,16 (4):193 - 214。doi: 10.2165 / 00003088-198916040-00001。

PubMed ID

2656049 (在PubMed

]

文摘

大环内酯物抗生素的人体药代动力学方面,目前正在或即将在市场上(如红霉素、竹桃霉素、螺旋霉素、交沙霉素、麦迪霉素、miocamycin, rosaramycin,罗和阿奇霉素)进行了综述。大环内酯物抗生素基本化合物,不溶于水,大多是在碱性吸收肠道环境。他们是酸不稳定,但更新的半合成衍生物(即罗和阿奇霉素)的特点是在酸性条件下稳定增加。大环内酯类是高度脂溶的,因此渗透到组织,尤其是支气管分泌物,前列腺组织,中耳渗出液和骨骼组织,通过组织/血清浓度比率大于1。他们不渗透到脑脊液。大环内酯类进行广泛的肝脏的生物转化。除了少数例外(如miocamycin),这些药物的代谢物的特点是很少或没有抗菌活性。血浆蛋白质绑定变量从一种化合物转移到另一个。在治疗浓度,蛋白结合的红霉素占总数的80 - 90%药物出现在血液中,和罗的比例是95%。蛋白结合的分数的最低价值观察麦迪霉素和交沙霉素(约15%)和螺旋霉素和miocamycin中间值。beplayapp However, the clinical relevance of this parameter is not clearly established. Plasma half-life (t1/2) values vary for the macrolides described: erythromycin, oleandomycin, josamycin and miocamycin have a t1/2 ranging from 1 to 2 hours; spiramycin, erythromycin stearate, the mercaptosuccinate salt of propionyl erythromycin and rosaramicin have an intermediate t1/2 (about 7, 6.5, 5 and 4.5 hours, respectively); the newer semisynthetic compounds roxithromycin and azithromycin are characterised by high t1/2 values (i.e. 11 and 41 hours, respectively). Under normal conditions, the major route of elimination is the liver. Renal elimination also takes place but it contributes to total clearance only to a small degree, as evidenced by low renal clearance values. The degree of modification of macrolide pharmacokinetics by renal insufficiency or hepatic disease is usually not considered clinically relevant, and no recommendation for dose modification is necessary in these patients. The pharmacokinetics of macrolides are modified in elderly patients. Accordingly, their use must be accompanied by a closer than usual clinical monitoring of the older patient.(ABSTRACT TRUNCATED AT 400 WORDS)

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药物

红霉素

麦迪霉素