LaForce C F, Szefler S J, Miller M F, Ebling W, Brenner M
J Allergy Clin Immunol. 1983 Jul;72(1):34-9. doi: 10.1016/0091-6749(83)90049-0.
Methylprednisolone elimination is reduced in the presence of treatment with troleandomycin (TAO), a macrolide antibiotic. To assess whether a similar interaction occurs with a more commonly used and less hepatotoxic macrolide antibiotic, erythromycin, we evaluated methylprednisolone pharmacokinetics before and after a 1 wk course of erythromycin base in nine adolescent patients with chronic asthma. These data were compared to results of studies of the troleandomycin methylprednisolone interaction evaluated in 10 adolescent asthmatic patients. Methylprednisolone clearance and apparent volume of distribution were significantly decreased and mean residence time and half-life significantly increased in the presence of both erythromycin and troleandomycin. The latter caused greater inhibition of methylprednisolone elimination. A nonlinear pattern of methylprednisolone disposition was observed in the presence of concomitant macrolide antibiotic administration. Addition of erythromycin base to methylprednisolone therapy results in inhibition of methylprednisolone elimination and may potentially increase the beneficial and adverse effects of this corticosteroid.
在使用大环内酯类抗生素三乙酰竹桃霉素（TAO）治疗时，甲基泼尼松龙的消除会减少。为了评估一种更常用且肝毒性较小的大环内酯类抗生素红霉素是否会产生类似的相互作用，我们对9名患有慢性哮喘的青少年患者在服用1周红霉素碱前后的甲基泼尼松龙药代动力学进行了评估。这些数据与10名青少年哮喘患者中评估的三乙酰竹桃霉素与甲基泼尼松龙相互作用的研究结果进行了比较。在同时使用红霉素和三乙酰竹桃霉素的情况下，甲基泼尼松龙的清除率和表观分布容积显著降低，平均驻留时间和半衰期显著延长。后者对甲基泼尼松龙消除的抑制作用更强。在同时使用大环内酯类抗生素时，观察到甲基泼尼松龙处置的非线性模式。在甲基泼尼松龙治疗中添加红霉素碱会导致甲基泼尼松龙消除受到抑制，并可能潜在地增加这种皮质类固醇的有益和不良反应。
