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逆转耐药性:下一代抗菌药物。

Reversing resistance: The next generation antibacterials.

作者信息

Shah Neel Jayesh

机构信息

Department of Pharmacology, Jawaharlal Institute of Postgraduate Medical Education and Research, Puducherry, India.

出版信息

Indian J Pharmacol. 2015 May-Jun;47(3):248-55. doi: 10.4103/0253-7613.157109.

DOI:10.4103/0253-7613.157109
PMID:26069360
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4450548/
Abstract

Irrational antibiotic usage has led to vast spread resistance to available antibiotics, but we refuse to slide back to "preantibiotic era." The threat is serious with the "Enterococcus, Staphylococcous, Klebsiella, Acinetobacter, Pseudomonas and Enterobacter" organisms causing nosocomial infections that are difficult to treat because of the production of extended spectrum β-lactamases, carbapenamases and metallo-β-lactamases. Facing us is a situation where soon multidrug resistance would have spread across the globe with no antibiotics to withstand it. The infectious disease society of America and Food and Drug Administration have taken initiatives like the 10 × '20 where they plan to develop 10 new antibiotics by the year 2020. Existing classes of antibiotics against resistant bacteria include the carbapenems, oxazolidinones, glycopeptides, monobactams, streptogramins and daptomycin. Newer drugs in existing classes of antibiotics such as cephalosporins, aminoglycosides, tetracyclines, glycopeptides and β-lactamase inhibitors continue to get synthesized. The situation demands newer targets against bacterial machinery. Some of them include the peptidoglycantransferase, outer membrane protein of Pseudomonas, tRNA synthase, fatty acid synthase and mycobacterial ATP synthase. To curb the irrational and excessive usage of presently available antibiotics should be a priority if they are still to be kept in usage for the future.

摘要

不合理使用抗生素已导致对现有抗生素的广泛耐药,但我们拒绝倒退到“抗生素前时代”。“肠球菌、葡萄球菌、克雷伯菌、不动杆菌、假单胞菌和肠杆菌”等微生物引起的医院感染威胁严重,由于它们产生超广谱β-内酰胺酶、碳青霉烯酶和金属β-内酰胺酶,这些感染难以治疗。摆在我们面前的情况是,很快多重耐药性将在全球蔓延,而没有抗生素能够抵御。美国传染病协会和食品药品监督管理局已经采取了一些举措,比如“10×20计划”,他们计划到2020年研发出10种新抗生素。现有的针对耐药菌的抗生素类别包括碳青霉烯类、恶唑烷酮类、糖肽类、单环β-内酰胺类、链阳霉素类和达托霉素。现有抗生素类别中的新型药物,如头孢菌素类、氨基糖苷类、四环素类、糖肽类和β-内酰胺酶抑制剂仍在不断合成。这种情况需要针对细菌机制的新靶点。其中一些靶点包括肽聚糖转移酶、假单胞菌外膜蛋白、tRNA合成酶、脂肪酸合成酶和分枝杆菌ATP合成酶。如果现有的抗生素仍要在未来继续使用,那么遏制其不合理和过度使用应成为首要任务。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf12/4450548/969a86be25b2/IJPharm-47-248-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf12/4450548/6d5f57b2d5a2/IJPharm-47-248-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf12/4450548/517ba5f79bf2/IJPharm-47-248-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf12/4450548/cfafd226d5bb/IJPharm-47-248-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf12/4450548/969a86be25b2/IJPharm-47-248-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf12/4450548/6d5f57b2d5a2/IJPharm-47-248-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf12/4450548/517ba5f79bf2/IJPharm-47-248-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf12/4450548/cfafd226d5bb/IJPharm-47-248-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf12/4450548/969a86be25b2/IJPharm-47-248-g004.jpg

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