大环内酯类抗生素的临床药代动力学性质。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

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

临床药典杂志1989 april;16(4):193-214。doi: 10.2165 / 00003088-198916040-00001。

PubMed ID

2656049 (PubMed视图

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摘要

综述了目前或即将上市的大环内酯类抗生素(即红霉素、奥兰多霉素、螺旋霉素、若沙霉素、中卡霉素、米奥卡霉素、罗沙霉素、罗红霉素和阿奇霉素)在人体内的药代动力学方面。大环内酯类抗生素为碱性化合物，难溶于水，主要在碱性肠道环境中被吸收。它们是酸性不稳定的，但较新的半合成衍生物(如罗红霉素和阿奇霉素)的特点是在酸性条件下稳定性增强。大环内酯具有高脂溶性，因此可以很好地渗透到组织中，特别是支气管分泌物、前列腺组织、中耳渗出液和骨组织，组织/血清浓度比大于1就是明证。它们不能很好地渗透到脑脊液中。大环内酯在肝脏中进行广泛的生物转化。除了少数例外(如缪卡霉素)，这些药物的代谢产物的特点是抗菌活性很少或没有抗菌活性。血浆蛋白结合因化合物的不同而不同。在治疗浓度下，蛋白结合红霉素占血液中总药物的80 - 90%，而罗红霉素的比例为95%。中卡霉素和约沙霉素的蛋白结合分数最低(约15%)，螺旋霉素和米卡霉素的蛋白质结合分数为中间值。 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)

引用本文的药物库数据

药物

红霉素

麦迪霉素