Renton K W, Gray J D, Hung O R
Clin Pharmacol Ther. 1981 Sep;30(3):422-6. doi: 10.1038/clpt.1981.182.
The elimination of a single oral dose of theophylline was studied in 12 healthy subjects before and after 250 mg erythromycin every 8 hr for 10 days. Serum theophylline elimination half-life rose from 4.79 +/- 0.43 hr before to 7.53 +/- 0.71 hr after erythromycin. Theophylline clearance decreased from a mean of 91.6 +/- 27.0 to 54.8 +/- 10.0 ml/kg/hr after erythromycin and the mean apparent volumes of distribution were much the same before and after the antibiotic. The excretion of theophylline and its metabolites was studied in the urine of three of the subjects. In each case the amount of 3-methylxanthine and 1,3-dimethyluric acid decreased after antibiotic. Adjustments of the theophylline dosage may be necessary for patients who take theophylline and erythromycin concurrently to minimize the risk of theophylline toxicity.
在12名健康受试者中,研究了每8小时服用250毫克红霉素,持续10天前后单次口服茶碱的消除情况。血清茶碱消除半衰期从服用红霉素前的4.79±0.43小时升至服用后的7.53±0.71小时。服用红霉素后,茶碱清除率从平均91.6±27.0降至54.8±10.0毫升/千克/小时,且抗生素服用前后平均表观分布容积大致相同。对其中三名受试者的尿液进行了茶碱及其代谢物排泄研究。在每种情况下,服用抗生素后3-甲基黄嘌呤和1,3-二甲基尿酸的量均减少。同时服用茶碱和红霉素的患者可能需要调整茶碱剂量,以尽量降低茶碱中毒风险。