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许多细菌产生的β-内酰胺酶(简称β-lase)水解β-内酰胺类抗生素的β-内酰胺环,使其丧失活性,是耐药性产生的机制之一.在克服β-lase所致耐药性的方法中,最有效的是应用β-内酰胺类抗生素与β-lase抑制剂的复合制剂.不可逆的竞争性β-lase抑制剂tazobactam(TAZ,YTR830)是继克拉维酸、舒巴坦后发现的作用谱更广和抑酶活性更强的β-lase抑制剂.哌拉西林(PIPC)与TAZ复合制剂tazocin(tazocillin,Zosyn,以下简称P/T),于1992年由日本大鹏药品开发,其后转让给美国Cyanamid、Lederle公司生产,目前已在欧美等许多国家应用.俄罗斯Yakovlev根据俄罗斯临床应用经验、美国Lederle公司提供的资料和最近大量文献报道,对其抗菌活性、药动学和临床应用等作了扼要的介绍.
Many bacteria produce β-lactamase (β-lase) hydrolysis β-lactam antibiotics β-lactam ring, so that loss of activity is one of the mechanisms of drug resistance in the overcoming β-lase by The most effective way to induce drug resistance is to use a combination of a β-lactam antibiotic and a β-lase inhibitor, tazobactam (TAZ, YTR830), an irreversible and competitive β-lase inhibitor, Sulbactam and a more potent inhibitor of beta-lase, an inhibitor of tazocin (tazocillin, Zosyn, hereinafter referred to as P / T), a combination of piperacillin (PIPC) and TAZ, Japan Dapeng drug development, then transferred to the United States Cyanamid, Lederle company, has been in many countries such as Europe and the United States. Russia Yakovlev based on clinical experience in Russia, the United States provided information Lederle company and a large number of recent reports on its antibacterial activity , Pharmacokinetics and clinical applications made a brief introduction.