碳青霉烯类抗生素的研究进展

Research progress in carbapenems antibiotics

目的综述非经典β-内酰胺类抗生素中碳青霉烯类抗生素的药理活性研究进展以及市场前景。方法根据国内外有代表性的19篇文献,对相关内容进行分析、归纳、整理。结果碳青霉烯类抗生素与经典青霉烯的结构相比,除4位硫原子被碳代替外,还存在6位反式羟乙基侧链,此特殊结构,使得这类抗生素成为非典型超广谱的β-内酰胺抗生素,并对β-内酰胺酶有耐受和抑制作用,成为治疗重症感染的一线药物,广泛应用于临床。此类药物存在半衰期短、口服品种少等缺陷,有待进一步开发新品种。结论碳青霉烯类抗生素由于其结构的特殊性,因而相对于其他抗生素具有较强的抗菌性能,已成为目前有关抗生素研究和开发的重要领域,具有广阔的市场前景。

Objective To summarize the progresses of pharmacological research and the potential market share of carbapenems, which is a kind of nonclassical β-lactam antibiotics. Methods The related literatures were analyzed, summarized and rearranged. Results Compared with the classical structure of penems, carbapenems had a 2-hydroxyethyl group With a-stereochemistry attached at C6 position, besides the sulfur atom had been replaced by a methylene moiety. The special structures made carbapenems to be a kind of nonclassical β-lactam antibiotic with ext ended broad-spectrum. Carbapenems was stable and tolerant to many β-lactamases, therefore carbapenems had become the first line drug for severe infection, and had＇a wide clinical application. But there were also many shortages, such as short half-life time, lacking of oral dosage form. Therefore, new drugs, such as oral drugs for releasing the burden of hospitals and patients, needed to be developed. Conclusions In recent years, carbapenems have become the highlight in relative research field and market share for its convincing curative effects and other satisfying clinical features.