Szefler S J, Ellis E F, Brenner M, Rose J Q, Spector S L, Yurchak A M, Andrews F, Jusko W J
J Allergy Clin Immunol. 1982 May;69(5):455-60. doi: 10.1016/0091-6749(82)90121-x.
Troleandomycin (TAO) is a macrolide antibiotic that has an apparent "steroid-sparing" effect when used in the treatment of severe steroid-dependent asthmatic patients. Recent observations demonstrated the effect of TAO on inhibiting methylprednisolone elimination, possibly contributing to its beneficial effects. Prednisolone and methylprednisolone disposition were studied before and 1 wk after initiation of TAO therapy in three patients. Methylprednisolone elimination was characteristically impaired in the presence of TAO therapy; however, there was no apparent effect on prednisolone elimination. Methylprednisolone elimination was also evaluated before and after initiation of TAO therapy in three patients receiving concomitant anticonvulsant therapy with phenobarbital-1, phenytoin-2. Methylprednisolone clearance before TAO was at least 4 times faster than normal and was probably related to enzyme induction by the anticonvulsant medication. Methylprednisolone clearance was subsequently reduced by approximately 70% in the presence of TAO therapy. The effect of TAO on corticosteroid disposition is steroid-specific and TAO can diminish the effect of certain drugs on the induction of corticosteroid metabolism.
醋竹桃霉素（TAO）是一种大环内酯类抗生素，在治疗严重依赖类固醇的哮喘患者时具有明显的“类固醇节省”效应。最近的观察结果表明TAO对抑制甲基强的松龙消除有作用，这可能是其产生有益效果的原因。对3例患者在开始TAO治疗前及治疗1周后进行了泼尼松龙和甲基强的松龙处置的研究。在TAO治疗期间，甲基强的松龙的消除明显受损；然而，对泼尼松龙的消除没有明显影响。对3例同时接受苯巴比妥-1、苯妥英-2抗惊厥治疗的患者在开始TAO治疗前及治疗后也进行了甲基强的松龙消除的评估。TAO治疗前甲基强的松龙的清除速度至少比正常情况快4倍，这可能与抗惊厥药物的酶诱导作用有关。在TAO治疗期间，甲基强的松龙的清除率随后降低了约70%。TAO对皮质类固醇处置的影响具有类固醇特异性，TAO可以减弱某些药物对皮质类固醇代谢诱导的影响。
