Ludden T M
Clin Pharmacokinet. 1985 Jan-Feb;10(1):63-79. doi: 10.2165/00003088-198510010-00003.
The macrolide antibiotics erythromycin and triacetyloleandomycin (troleandomycin) are prescribed for many types of infections. As such they are often added to other preexisting drug therapy. Thus, there are frequent opportunities for the interaction of these antibiotics with other drugs. Both erythromycin and triacetyloleandomycin appear to have the potential to inhibit drug metabolism in the liver and also drug metabolism by micro-organisms in the gut, either through their antibiotic effect or through complex formation and inactivation of microsomal drug oxidising enzymes. Of the two agents, triacetyloleandomycin appears to be the more potent inhibitor of microsomal drug metabolism. Published studies indicate that triacetyloleandomycin can significantly decrease the metabolism of methylprednisolone, theophylline and carbamazepine. Its ability to cause ergotism in patients receiving ergot alkaloids and cholestatic jaundice in patients on oral contraceptives may also be related to its inhibitory effect on drug metabolism. Erythromycin appears to be a much weaker inhibitor of drug metabolism. There are numerous reports describing apparent interactions of erythromycin with theophylline and a lesser number of reports dealing with carbamazepine, warfarin methylprednisolone and digoxin. There are sufficient data to suggest that erythromycin can, in some individuals, inhibit the elimination of methylprednisolone, theophylline, carbamazepine and warfarin. The mean change in drug clearance is about 20 to 25% in most cases, with some patients having a much larger change than others. Like tetracycline, erythromycin also appears to have the potential for increasing the bioavailability of digoxin in patients who excrete high amounts of reduced digoxin metabolites, apparently through destruction of the gut flora that form these compounds. Concurrent administration of triacetyloleandomycin with drugs whose metabolism is known to be affected or that could potentially be affected should be avoided unless appropriate adjustments in dosage are made. Coadministration of erythromycin with drugs believed to interact should be undertaken with caution and with appropriate patient monitoring. Among the other macrolide antibiotics, josamycin has seldom been involved in causing drug interactions, while midecamycin and the older derivative spiramycin have not so far been incriminated.
大环内酯类抗生素红霉素和三乙酰竹桃霉素（醋竹桃霉素）可用于治疗多种感染。因此，它们常被添加到已有的其他药物治疗方案中。这样一来，这些抗生素与其他药物之间频繁存在相互作用的机会。红霉素和三乙酰竹桃霉素似乎都有可能抑制肝脏中的药物代谢以及肠道中微生物的药物代谢，这要么是通过它们的抗菌作用，要么是通过形成复合物并使微粒体药物氧化酶失活来实现。在这两种药物中，三乙酰竹桃霉素似乎是更有效的微粒体药物代谢抑制剂。已发表的研究表明，三乙酰竹桃霉素可显著降低甲泼尼龙、茶碱和卡马西平的代谢。它在接受麦角生物碱的患者中导致麦角中毒以及在口服避孕药的患者中引起胆汁淤积性黄疸的能力，可能也与其对药物代谢的抑制作用有关。红霉素似乎是一种较弱的药物代谢抑制剂。有大量报告描述了红霉素与茶碱之间明显的相互作用，而涉及卡马西平、华法林、甲泼尼龙和地高辛的报告较少。有足够的数据表明，红霉素在某些个体中可抑制甲泼尼龙、茶碱、卡马西平和华法林的消除。在大多数情况下，药物清除率的平均变化约为20%至25%，有些患者的变化比其他患者大得多。与四环素一样，红霉素似乎也有可能增加那些排泄大量还原型地高辛代谢物的患者体内地高辛的生物利用度，显然是通过破坏形成这些化合物的肠道菌群来实现的。除非进行适当的剂量调整，否则应避免将三乙酰竹桃霉素与已知代谢会受影响或可能受影响的药物同时使用。红霉素与被认为会相互作用的药物合用时应谨慎，并对患者进行适当监测。在其他大环内酯类抗生素中，交沙霉素很少引起药物相互作用，而麦迪霉素和较老的衍生物螺旋霉素目前尚未被认定有此问题。
