26.Tigecycline is also known as the 9- tert butyl glycyl amino minocycline or Ding Gan minocycline, and is a new broad-spectrum activity of intravenous injection with antibiotics, belonging to 9- tert butyl glycyl amino minocycline derivatives, is the first glycocholic acid antibiotics, in order to solve the resistance of early achromycin. In June, 1995, it is approved by the United States FDA. Although its structure is similar to minocycline, but after the molecular structure changes, not only its antibacterial activity is greatly improved, and compared with other tetracycline drugs, bacteria is not easy to produce drug resistance, Staphylococcus aureus, which is resistance to methicillin resistant , also has activity the resistance.
The prime mechanism of tigecycline are similar to tetracycline antibiotics, both combine with bacterial 30S ribosomal, stop entering the transfer RNA, make the amino acid uncombined into peptide chains, eventually blocking protein synthesis of bacteria, limiting bacterial growth. But the binding capacity of tigecycline with ribosome is 5 times of other tetracyclines drugs. That showed that the resistance to bacterial was stonger than other tetracyclines drugs. Antibacterial spectrum of tetracyclines including gram positive bacteria, gram negative bacteria and anaerobic bacteria. The vitro experiments and clinical trials show that tetracyclines are sensitive to the part of the aerobic gram negative bacteria (such as Citrobacter freundii, Enterobacter cloacae, Escherichia coli, Klebsiella oxytoca and Klebsiella pneumoniae, Bowman Acinetobacter, Aeromonas water vapor, G freundii, Enterobacter aerogenes, Pasteurella multocida, Serratia marcescens and stenotrophomonas maltophilia,etc.). Pseudomonas aeruginosa bacteria is resistance to tigecycline.
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