dirithromycin的药物动力学。

文章的细节

引用
复制到剪贴板

GD, Cerimele BJ,黑色的人力资源,布施U, DeSante KA

dirithromycin的药物动力学。

J Antimicrob Chemother。1993年3月31日5 C: 65 - 75。

PubMed ID
8478313 (在PubMed
]
文摘

Dirithromycin是一个新成员的大环内酯物类抗生素和了口服药。Dirithromycin是一个拥有14个内酯环大环内酯物erythromycylamine的C9-oxazine导数。dirithromycin人类药物动力学和临床药理学的研究了。区别于红霉素Dirithromycin具有独特的药物动力学。在男人,口服500毫克剂量的dirithromycin后,平均血浆浓度峰值(Cmax) 0.48 mg / L(范围0.1 - -1.97)下观察到4 h。平均面积的血浆浓度与时间曲线(AUC0-24h)测量3.37毫克。h / L(范围0.39 - -17.16)。没有观察到等离子体积累与multiple-dose政府。Dirithromycin可能采取不顾吃饭,虽然食品和H2-receptor拮抗剂在某些病人可能会增加系统生物利用度。基于药物相互作用研究执行安替比林和茶碱,dirithromycin显示更少可能与其他药物代谢的细胞色素P450系统红霉素。等离子体浓度和auc低是由于血管的药物快速运动的空间没有血管的隔间,反映在组织浓度,超过了等离子体浓度给药后4 h。Dirithromycin达到组织浓度相对较高(约0.8 - -5.0毫克/公斤)4-24剂量后h。 The extensive tissue penetration is reflected in a large mean apparent volume of distribution of 800 L (range 504-1041). Dirithromycin is rapidly converted by non-enzymatic hydrolysis during absorption to erythromycylamine, which is microbiologically active. In a 14C-radiolabelled study, 60-90% of the administered dose was hydrolysed to erythromycylamine within 35 min of infusion. After 1.5 h, conversion to erythromycylamine in serum was virtually complete. Plasma protein binding was determined to be 15-30% by ultracentrifugation. Dirithromycin is characterized by a plasma elimination half-life of 44 h (range 16-65 h) that permits once-daily administration. Total body clearance was 226-1040 mL/min in the 14C-radiolabelled study. The primary route of elimination of dirithromycin/erythromycylamine was faecal/hepatic. Following intravenous administration, approximately 17-25% of the radioactivity appeared in the urine and 62-81% appeared in the stool, indicating predominantly hepatic excretion. With oral administration 1.2-2.9% of the radioactivity appeared in the urine and 81-97% in the stool. The major part of urinary excretion occurs within the first 48 h post-administration; however, urinary excretion of radioactivity lasted longer than 240 h. The absolute bioavailability calculated from dose-corrected urinary excretion data was 10% (6-14%).

DrugBank数据引用了这篇文章

药物