摘要
九十年代各国首次应用的抗细菌抗生素共２４种，其中有头孢菌素１４种，碳青霉烯２种，青霉烯１种，β－内酰胺酶抑制剂与其制剂１种，氨基糖苷、大环内酯与安莎类抗生素各２种。新上市的合成抗菌药共１０种，包括喹诺酮类化合物９种和二氢叶酸还原酶抑制剂１种。还有一批颇具特色的新抗菌药正在研究开发中。１．第四代头孢菌素与第三代口服头孢菌素：概述了头孢匹罗、头孢吡肟、头孢唑兰、头孢瑟利等４种第四代头孢菌素与头孢地尼、头孢布烯、头孢帕肟酯、头孢托仑酯、头孢卡品酯等６种第三代口服头孢菌素的性能。２．碳青霉烯类抗生素：评介了新上市的培尼培南、美洛培南与正在开发中的比阿培南等的特性。３．青霉烯类抗生素：报道了新上市的呋洛培南与正在研究中的利替培南酯与ＴＭＡ－２３０等。４．β－内酰胺酶抑制剂与其制剂，在介绍新β－内酰胺酶抑制剂他唑巴坦与其制剂他唑西林的性状之后，评述了新β－内酰胺酶抑制剂研究的进展。５，其他抗生素：概述了一些对大环内酯耐药菌有作用的新大环内酯和若干对革兰阳性与阴性菌，特别是对四环素耐药菌有作用的广谱新甘氨酰四环素。６．喹诺酮类抗菌药：评述了九十年代面市的替马沙星、芦氟沙星、氟罗沙星、司帕沙星、那氟沙星、左氧氟沙皇、格帕沙?
24 kinds of antibacterial antibiotics including cehpalosporins(14), carbapenems(2), penem(1), aminoglycosides(2), macrolides(2), ansamycin-antibiotics(2) and new β -lactamase inhibitor and its preparation(1) have been developed since 1990 in the World. 10 kinds of synthetically antibacterial agents including 9 quinolone compounds and 1 dihydrofolate reductase inhibitor have been marketed. There are a number of specifical antibacterials under investigation. 1. The 4th-Generation Cephalosporins and 3rd-Generation Oral Cephalosporins. Properties of 4th-generation cephalosporins including cefopirome, cefepime, cefozopran, cefoselis and properties of 3rd-generation oral cephalosporins including cefdinir, ccftibutin, cefpodoxim proxetil, ceftamet pivoxil, cefditoren pivoxil, cefcapene pivoxil were summarized. 2. Carbapenems. Characteristics of new marketing penipenem, meropenem and developing biapenam were recounted. 3. Penems. Characteristics of new marketing fropenem and investigational ritipenem acexil, TMA-230 were reported. 4. β -Lactamase inhibitors and their Preparations. Tazobactam and its preparation Tazocillin were introduced. New advance in search for new β -lactamase inhibitors also were outlined. 5. Other Antibiotics. Some new macrolides activing against macrolid-resistant bacteria and several glycylcylines with a broad antibacterial spectrum,including both gram-positive and gram-negative bacteria, especially tetracyclineresistant strains were expounded. 6. Quinolones, Properties of 9 marketed quinolones (temafloxacin, rufloxacin,fleroxacin, spafloxacin, nadifloxacin, levofloxacin, grepafloxacin, trovafloxacin and alatrafloxacin) and & clinically evaluating quinolones(balofloxacin, clinafloxacin) gatifloxacin, pazufloxacin, prulifloxacin, moxifloxacin and sitafloxacin) were summarized. 7. Search for Anti-MRSA, Anti-VRE and Anti-PRSP Agents. Some new advance in research of glycopeptides, streptogramines, oxazolidinones, 0 - lactam potentiators etc. were reviewed. A huge number of antibacterial agents exhibiting very good activity against Gram-negative bacilli, including Pseudomonas aeruginosa, such as imipenrm - a carbapenem, some third generation cephalosporins and quinolones have been available for clinical use since the 1980s, and excellent efficacy has obtained. More and more resistant bacterialstrains have developed and spread. Bacteria resistant to multiple antibiotics, such as methicillin resistant Staphylococcus aureus (MRSA),penicillin-resistant Pneumococcus(PRSP), vancomycin / teicoplanine-resistant Entero coccus spp.(VRE) have been isolated with increasing frequency. The annihilation of these strains presents a serious problem and continuously requires new, more efficient antibiotics and antimicrobial agents. In the 1990s, a number of newer cephalosporins and quinolones possessing increased activity against many Gram-positive pathogens and anaerobes have been developed. Application of novel 6 -lactamase inhibitors, discovery of 6 -lactam potentiators, appearance of new aminoglycosides exhibiting activity against MRSA, development of streptogramines and other investigational agents will considerably contribute to the improvement of the antibacterial chemotherapy.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2000年第2期139-145,共7页
The Chinese Journal of Clinical Pharmacology
