替考拉宁药代动力学/药效学研究与给药方案优化  

Pharmacokinetics/pharmacodynamics and administration regimen optimization of teicoplanin

作　　者：江学维[1] 梁蓓蓓[1] 王凯[1] 王瑾[1] 王睿[1] 

机构地区：[1]中国人民解放军总医院转化医学中心药物/器械临床试验中心,北京100853

出　　处：《中国临床药理学杂志》2015年第16期1662-1664,共3页The Chinese Journal of Clinical Pharmacology

基　　金："十二五"国家重大科技专项基金资助项目(2012ZX09303004-002)

摘　　要：细菌耐药已经成为一个世界性的卫生问题,糖肽类药物替考拉宁一直作为治疗耐甲氧西林金黄色葡萄球菌的首选药物之一。替考拉宁口服不吸收,蛋白结合率高,半衰期长,大部分以原型经肾排出,肾功能不全患者半衰期延长。替考拉宁对多种革兰氏阳性菌敏感,杀菌曲线相对平缓,为非浓度依赖性,杀菌作用呈现持续效应,有明显抗生素后效应。当AUC/MIC≥345时可达到最佳治疗效果,为此,应使用负荷剂量使其快速达到有效谷浓度,同时应重视维持剂量,也可根据不同病原菌的最低抑菌浓度而选择不同的治疗方案。Bacterial resistance has become a worldwide health problem,and teicoplanin has been used as one of first- choice drugs of methicillin- resistant Staphylococcus aureus（ MRSA）. Teicoplanin is not absorbed by oral administration,has high protein binding rate and long half- life.Most of the drug excreted in the kidneys with prototype,so that the half- life prolonged in patients with renal insufficiency. Teicoplanin,a non- concentration- dependent antibiotic which has significantly post antibiotic effect,is sensitive against a variety of gram- positive bacteria and has a relatively flat killing curve. When the AUC / MIC≥345,teicoplanin can achieve the best therapeutic effect. Therefore,to quickly reach an effective trough concentration,loading dose is needed and the maintenance dose should be paid attention to. According to the MIC against different bacteria,a different treatment selection were also recommended.

关 键 词：替考拉宁 药代动力学/药效学 方案优化 负荷剂量 有效谷浓度 

分 类 号：R969.3[医药卫生—药理学] R978.1[医药卫生—药学]