Macrolides. Classification (semisynthetic, natural and azalides)


Lactone ring macrocyclic - this is the basischemical structure of all macrolide antibiotics. Classification implies a division into 14, 15 and 16-tichlennye. These antibiotics are considered the least toxic.

Macrolides. Classification by type of origin

Natural macrolides:

Macrolide "Erythromycin" is the firstbacteriostatic antibiotic, which initiated 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 performs blocking of the synthesis of proteins of various microorganisms. In this case, the antibiotic "Erythromycin" does not affect the synthesis of nucleic acids. In large doses, bactericidal effects may occur with respect to certain bacterial species.

Macrolide "Spiramycin" is an antibiotic thatare obtained from Streptomyces ambofaciens actinomycetes, he is the first representative of a group of 16-member macrolides. The lactone ring is the structural basis of the drug "Spiramycin". It consists of 16 carbon atoms (C), to which are attached 3 carbohydrate residues: mikaroza, forosamine and mycaminosis. Drugs that have active ingredient spiramycin in their composition are common in Canada, Latin America and Europe.

Macrolide "Josamycin" is an antibiotic,representative of a group of 16-member macrolides. Streptomyces narbonensis is produced. Has a bactericidal effect. It suppresses the synthesis of protein compounds, prevents the fixation of RNA (transport) and binds to the 50S subunit of the ribosomal membrane, thereby blocking the exchange of peptides from the center of A. It is allowed to treat diseases during pregnancy.

Semisynthetic macrolides:

Macrolide "Roxithromycin" is the firstsemisynthetic 14-membered antibiotic. Was obtained from macrolide "Erythromycin". The structure features give it a higher resistance to acids, improved microbiological and pharmacokinetic parameters.

Macrolide "Clarithromycin" is a 14-memberantibiotic, macrolide derivative "Erythromycin". Has increased resistance to acids and improved pharmacokinetic and antibacterial properties.

Natural macrolides-antibiotics are highly active ingram-positive, some gram-negative and intracellular microorganisms. And such modern macrolides, as semisynthetic ones, are more active in regard to pseudomonads, enterobacteria, anaerobic microflora and influenza sticks.

And, finally, the azalids - macrolides of the last generation:

Antibiotic "Azithromycin" belongs to the subclassAzalides, which differ somewhat in their structure from ordinary macrolides. The ring in macrolide "Azithromycin" is not lactone, but 15-membered. Acid resistance at the same time increases 300 times compared with the antibiotic "Erythromycin".

Macrolides. Classification by generation:

1-e - preparations "Oleandomycin", "Erythromycin";
2-macrolides "Roxithromycin", "Spiramycin", "Josamycin", "Midekamycin", "Clarithromycin";
3rd - macrolide "Azithromycin".

Indications for the use of antibiotics of macrolides. Classification of diseases

Those that affect the respiratory system: acute sinusitis, streptococcal tonsillopharyngitis, community-acquired pneumonia, exacerbation of bronchitis, whooping cough, diphtheria.

Skin and soft tissue: syphilis, chlamydia, venereal lymphogranuloma, soft chancroid, acne.

The oral cavity: periostitis and periodontitis.

Digestive system: Campylobacter gastroenteritis, stomach ulcer.

Also macrolides are used to prevent the following diseases: whooping cough, meningitis, rheumatism, endocarditis.