Macrocyclic lactone ring is the basischemical structure of all macrolide antibiotics. The classification implies a division into 14, 15 and 16-term. These antibiotics are considered the least toxic.
Macrolides. Classification by type of origin
Natural macrolides:
Macrolide "Erythromycin" is the firstbacteriostatic antibiotic, which marked the beginning of a large group. It was obtained in 1952 from Streptomyces erythreus, a soil actinomycete. Due to the fact that the macrolide "Erythromycin" has the property of reversibly binding to the ribosomal 50S-subunit, it disrupts the formation of peptide bonds between amino acid molecules and blocks the synthesis of proteins of various microorganisms. In this case, the antibiotic "Erythromycin" does not affect the synthesis (compound) of nucleic acids. In large doses in relation to certain types of bacteria can have a bactericidal effect.
Macrolide "Spiramycin" is an antibiotic thatderived from Streptomyces ambofaciens actinomycete, he is the first representative of a group of 16-membered macrolides. Lactone ring - is the structural basis of the drug "Spiramycin". It consists of 16 carbon atoms (C), to which 3 carbohydrate residues are attached: mycarose, forosamine, and mycaminosis. Drugs that have in its composition the active substance spiramycin, distributed in Canada, Latin America and Europe.
Macrolide "Josamycin" is an antibiotic,representative of a group of 16-membered macrolides. Produced by Streptomyces narbonensis. Has a bactericidal effect. Suppresses the synthesis of protein compounds, prevents the fixation of RNA (transport) and connects to the 50S subunit of the ribosomal membrane, thereby blocking the exchange of peptides from center A. It is permitted in the treatment of diseases during pregnancy.
Semi-synthetic macrolides:
Macrolide "Roxithromycin" is the firstsemisynthetic 14-membered atibiotic. Was obtained from the macrolide "Erythromycin". Features of the structure give it a higher resistance to acids, improved microbiological and pharmacokinetic parameters.
Macrolide Clarithromycin is a 14-memberedantibiotic, macrolide derivative "Erythromycin". It has increased resistance to acids and improved pharmacokinetic and antibacterial properties.
Natural macrolide antibiotics are highly active inagainst gram-positive, some gram-negative and intracellular microorganisms. And such modern macrolides, as semi-synthetic, are more active against pseudomonads, enterobacteria, anaerobic microflora and influenza bacilli.
And, finally, the azalides are the macrolides of the last generation:
The antibiotic "Azithromycin" refers to the subclassazalides, which are somewhat different in structure from ordinary macrolides. The ring in the macrolide "Azithromycin" is not lactone, but it is 15-membered. Acid resistance increases by 300 times compared with the antibiotic Erythromycin.
Macrolides. Classification by generation:
1st - drugs "oleandomycin", "Erythromycin";
2nd - macrolides "Roksitromitsin", "Spiramycin", "Dzhozamitsin", "Midekamitsin", "Clarithromycin";
3rd - macrolide "Azithromycin".
Indications for use of macrolide antibiotics. Disease classification
Those that affect the respiratory system: acute sinusitis, streptococcal tonsillopharyngitis, community-acquired pneumonia, exacerbation of bronchitis, whooping cough, diphtheria.
Skin and soft tissues: syphilis, chlamydia, venereal lymphogranuloma, chancroid, acne.
Oral cavity: periostitis and periodontitis.
The digestive system: Campylobacter gastroenteritis, gastric ulcer.
Macrolides are also used to prevent the following diseases: whooping cough, meningitis, rheumatism, endocarditis.
