Luurila H, Olkkola K T, Neuvonen P J
Department of Clinical Pharmacology, University of Helsinki, Finland.
Ther Drug Monit. 1994 Dec;16(6):548-51. doi: 10.1097/00007691-199412000-00003.
Erythromycin is a strong inhibitor of cytochrome P450 [CYP3A4] and has a potentially dangerous interaction with midazolam and triazolam. The possible interaction between erythromycin and a short-acting benzodiazepine, temazepam, was investigated in a double-blind, randomized crossover study. Ten healthy volunteers received 500 mg erythromycin or placebo orally three times a day for 6 days followed by a challenge dose of 20 mg temazepam. Plasma samples were collected for the determination of temazepam, oxazepam, and erythromycin, and psychomotor effects were measured during the 24 h after intake of temazepam. Erythromycin did not change the pharmacokinetics or pharmacodynamics of temazepam to a statistically significant degree. The metabolic fate of temazepam and its almost complete bioavailability explain the lack of interaction. Temazepam, unlike midazolam or triazolam, can thus be prescribed in the usual doses for patients receiving erythromycin.
红霉素是细胞色素P450[CYP3A4]的强效抑制剂,与咪达唑仑和三唑仑存在潜在的危险相互作用。在一项双盲、随机交叉研究中,对红霉素与短效苯二氮䓬类药物替马西泮之间可能的相互作用进行了研究。10名健康志愿者每天口服3次500mg红霉素或安慰剂,持续6天,随后给予20mg替马西泮的挑战剂量。采集血浆样本以测定替马西泮、奥沙西泮和红霉素,并在服用替马西泮后的24小时内测量精神运动效应。红霉素对替马西泮的药代动力学或药效动力学没有产生具有统计学意义的改变。替马西泮的代谢命运及其几乎完全的生物利用度解释了缺乏相互作用的原因。因此,与咪达唑仑或三唑仑不同,替马西泮可以以常规剂量开给接受红霉素治疗的患者。