Introduction
Ramoplanin is a new kind of glycopeptide antibiotics, which can inhibit the biosynthesis of the cell walls of gram-positive bacteria specifically and quickly. While the inhibition mechanism of ramoplanin is different from vancomycin and teicoplanin, its inhibitory rate against aureus is four to eight times as much as vancomycin and teicoplanin, and it shows very good inhibition effects against many pathogens with drug resistance. Meanwhile, the cytotoxicity of ramoplanin is relative less, and there is no cross resistance problem. Pure ramoplanin is the mixture of Group A1, A2, A3, and the main components are A2 which accounts for 80%.
Pharmacologic action
Ramoplanin can inhibit the biosynthesis of peptidoglycan on the cell wall, effectively inhibit the synthesis of cell wall of gram positive bacteria, and have strong antibacterial activity to Staphylococcus, Streptococcus, actinomycetes, corynebacterium, clostridium, and lactobacillus and so on. Ramoplanin can rapidly and effectively inhibit the activity of N-acetyltransferase and greatly reduce the absorption of N-acetylglucosamine by growth cells. When the concentration of N-acetylglucosaminyltransferase is insufficient and the activity of N-acetylglucosaminyltransferase is lost, N-acetylglucosaminyltransferase cannot be connected to Undeciphenyl muramyl pentapeptide, so that the cell wall precursor (Udp-n-acetyl muramyl pentapeptide) in the growth cells is accumulated in large quantities. It is difficult for bacteria to build up a complete cell wall structure, resulting in bacteria being unable to survive.
Function
Ramoplanin is a peptide antibiotic containing lipoprotein and phenolic acid. It contains 3 natural components (A1, A2 and A3), of which A2 is the main component, accounting for about 80% of the total. Ramoplanin has the broad-spectrum anti gram positive bacteria activity, and can inhibit staphylococcus, actinomycetes, corynebacterium, clostridium and lactobacillus. Ramoplanin has a good antibacterial effect on some resistant pathogens such as methicillin resistant staphylococcus aureus (MRSA), zoxicillin resistant bacteria, penicillin G resistant bacteria and gentamicin.
Pharmacokinetics and metabolism
Ramoplanin's cytotoxicity was relatively small with no obvious side effects. Because ramoplanin is a macromolecular glycopeptide substance with a large molecular weight, it is difficult to enter the blood circulation when taking oral medicine. After oral administration of ramoplanin (200,400mg, 2 times a day), the gastrointestinal tract was almost not absorbed by ramoplanin. Gram positive bacteria were detected in excreted feces, and Gram-negative bacteria were not affected.
References:
Yue-Iing Guo, Zi-di Zhao,Hui-min Ni, Xue-li Zheng. Study Progress on a New Glycopeptide Antibiotics -Remoplanin. HEBEI HUAGONG. 2011, 34(8), 28-31.
