环丙沙星 ADME
中文名称
通路描述
环丙沙星（Cipro）是一种广泛使用的广谱细菌抗生素。由于其与可能导致严重且持久不良反应的关联以及目前高水平的耐药性，其使用现在仅推荐用于没有替代治疗选项的呼吸道和泌尿道感染、皮肤和软组织感染、骨和关节感染、感染性腹泻、伤寒和淋病患者，前提是菌株敏感。不良反应包括腱鞘炎、腱断裂、周围神经病变和 CNS 效应。常用剂量为 250 mg 和 500 mg（FDA，2016；Bayer Inc，2020）。环丙沙星在 pH 5 以下和 pH 10 以上的水溶液中高度溶解。约 60 至 80% 被身体吸收。环丙沙星的主要吸收部位是上消化道，直至空肠（Harder et al, 1990；总结在 Olivera et al, 2011）。在生物药剂学分类系统（BCS）中，环丙沙星“不高度溶解”，且“不高度渗透”。它被分类为 BCS 类 2、3 和 4，摄取和外排转运蛋白对其吸收和排泄有很大影响。BCS 类 4 药物主要通过胆道或肾脏途径以未改变的形式排泄（Wu and Benet, 2005）。血浆浓度下，肾和胆囊中观察到环丙沙星的高浓度；肝脏、前列腺组织和肺中也发现了高浓度。未改变环丙沙星的主要排泄途径是肾脏（约 65% 的血浆量）和肠道（约 10%）（Rohwedder et al, 1990；Viell et al, 1992；综述由 Sörgel, 1989）。肠道数据包括通过上皮胃肠道细胞和通过肝细胞和胆管的排泄。其余血浆环丙沙星（10 至 20%）被代谢，从尿液中回收的主要物种是氧环丙沙星，在粪便中是硫环丙沙星。两者分别占总排泄量的约五分之一（综述由 Campoli-Richards et al, 1988）。
英文描述
Ciprofloxacin ADME Ciprofloxacin (Cipro) is a widely used broad spectrum bacterial antibiotic. Due to its association with disabling and potentially persistent adverse reactions and current high levels of resistance its use is now recommended in patients who have no alternative treatment option for respiratory and urinary tract infections, skin and soft tissue infections, bone and joint infections, infectious diarrhea, typhoid fever and gonorrhea with susceptible strains. Adverse reactions include tendinitis, tendon rupture, peripheral neuropathy, and CNS effects. The usual dosages are 250 mg and 500 mg (FDA, 2016; Bayer Inc, 2020).Cipro is highly soluble in aqeuous media below pH 5 and above pH 10. About 60 to 80 percent are taken up by the body. The main absorption site of ciprofloxacin is the upper GI tract, up to the jejunum (Harder et al, 1990; summarized in Olivera et al, 2011). In the context of the Biopharmaceutics Classification System (BCS) Cipro is "not highly soluble", and "not highly permeable". It is classified as BCS class 2, 3, and 4, and uptake and efflux transporters have a big effect on its absorption and excretion. BCS class 4 drugs are primarily excreted unchanged via the biliary or renal routes (Wu and Benet, 2005). Very high concentrations of Cipro with respect to plasma concentrations are seen in kidney and gall bladder; high concentrations are also found in liver, prostatic tissue, and lung. The main excretion routes for unchanged Cipro are renal (about 65% of plasma amount) and intestinal (about 10%) (Rohwedder et al, 1990; Viell et al, 1992; reviewed by Sörgel, 1989). The intestinal figure includes excretion through epithelial GI cells, and through hepatic cells and the bile duct. The rest of plasma Cipro (10 to 20%) is metabolised, with the major species recovered from urine being oxociprofloxacin and, in faeces, sulfociprofloxacin. Both account for about five per cent each of total excretion (reviewed by Campoli-Richards et al, 1988).
所含基因
5 个基因