In a group such as macrolides, the list of drugs is large, which indicates a sufficient breadth of therapeutic use. These medicinal substances are safe and used for many diseases of an infectious nature, including those caused by intracellular parasitic bacteria. They are suitable for the treatment of diseases of the skin, joints, respiratory system, including bronchitis and pneumonia of various severity.
In severe pneumonia, macrolides are also used, the list of drugs of which is indicated in standard treatment protocols. However, they do contain information on the need for combination with other antimicrobials. Most often they are used together with cephalosporins. This combination allows you to mutually increase the effectiveness of both drugs without increasing their toxicity.
Macrolide classification
The most competent and convenient classification of this group of drugs is chemical. It reflects differences in the structure and origin of antibiotics of the group called "Macrolides". The list of drugs will be given below, and the substances themselves are distinguished by:
- 14 membered macrolides:
- natural origin - erythromycin and oleandomycin;
- semi-synthetic - clarithromycin and roxithromycin, dirithromycin and flurithromycin, telithromycin.
2. Azalide (15 membered) macrolides: azithromycin.
3.16-membered macrolides:
- natural origin - midecamycin, spiramycin and josamycin;
- semi-synthetic - midecamycin acetate.
This classification reflects only the structural features of class drugs. The list of trade names is presented below.
List of drugs
Macrolides are drugs, the list of which is very wide. In total, as of 2015, there are 12 drugs of this class. And the number of drugs containing these active substances is much higher. Many of them can be found in the pharmacy network and taken to treat a number of diseases. Moreover, part of the drugs is not available in the CIS, as it is not registered in the pharmacopeia. Examples of trade names for preparations containing macrolides are as follows:
- Erythromycin is often available in drugs with the same name, and is also included in the complex medicines Zinerit and Isotrexin.
- Oleandomycin is a medicinal substance of the drug Oletetrin.
- Clarithromycin: Clubax and Claricar, Clerimed and Clacid, Claire and Lekoklar, Pilobact and Fromilide, Ecositrin and Erasid, Zimbactar and Arvitsin, Kispar and Klarbakt, Klaritrosin and Klaritsin, Klasin and Coater, Clerimed and Romiklar, Seidon and SR-Klaren.
- Roxithromycin is often found in the form of a generic brand name, and is also part of the following drugs: Xitrocin and Romik, Elrox and Rulitsin, Esparoxy.
- Azithromycin: Azivok and Azidrop, Azimycin and Azitral, Azitroks and Azitrus, Zetamax and Zi-Factor, Zitnob and Zitrolid, Zitracin and Sumaklid "," Sumamed "and" Sumamox "," Sumatrolide "and" Tremax-Sanovel "," Hemomycin "and" Ekomed "," Safotsid ".
- Midecamycin is available in the form of the drug Macropen.
- Spiramycin is available in both Rovamycin and Spiramycin Vero.
- Dirithromycin, flurithromycin, as well as telithromycin and josamycin are not available in the CIS.
The mechanism of action of macrolides
This specific pharmacological group - macrolides - has a bacteriostatic effect on the susceptible cell of the causative agent of infectious diseases. Only in high concentrations can a bactericidal effect be possible, although this has been proven only in laboratory studies. The only mechanism of action of macrolides is the inhibition of protein synthesis of microbial cells. This disrupts all the vital processes of the virulent microorganism, as a result of which it dies after some time.
The mechanism of inhibition of protein synthesis is associated with the attachment of bacterial ribosomes to the 50S subunit. They are responsible for building the polypeptide chain in DNA synthesis. Thus, the synthesis of structural proteins and bacterial virulence factors is disrupted. Moreover, high specificity specifically for the bacterial ribosome determines the relative safety of macrolides for the human body.
Comparison of macrolides and antibiotics of other classes
Macrolides are similar in properties to tetracyclines, but are safer. They do not violate the development of the skeleton in childhood. Like tetracyclines with fluoroquinolones, macrolides (the list of drugs are presented above) can penetrate into the cell and create therapeutic concentrations in the three compartments of the body. This is important in the treatment of mycoplasma pneumonia, legionellosis, campylobacteriosis and chlamydial infection. At the same time, macrolides are safer than fluoroquinolones, although they are less effective.
All macrolides are more toxic than penicillins, but the safest in terms of the likelihood of allergies. At the same time, penicillin antibiotics are record holders in safety, but tend to cause allergies. Thus, having a similar spectrum of antimicrobial activity, macrolides can replace aminopenicillins in infections of the respiratory system. Moreover, laboratory studies show that macrolides reduce the effectiveness of penicillins when taken together, although modern treatment protocols allow their combination.
Macrolides during pregnancy and pediatric therapy
Macrolides are safe drugs along with cephalosporins and penicillins. This allows them to be used during pregnancy and in the treatment of children. They do not disrupt the development of the bone and cartilage skeleton, do not have teratogenic properties. Azithromycin alone should be limited in use in the third trimester of pregnancy. In pediatric therapy, penicillins, and cephalosporins, and macrolides, the list of which is indicated in the standard protocols for treating diseases, can be used without the risk of toxic damage to the body.
Description of some macrolides
Macrolides (drugs, the list we gave above) are widely used in clinical practice, including in the CIS. Most often, 4 of their representatives are used: clarithromycin and azithromycin, midecamycin and erythromycin. Spiramycin is much less commonly used. The effectiveness of macrolides is approximately the same, although it is achieved in different ways. In particular, clarithromycin and midecamycin must be taken twice a day to achieve the clinical effect, while azithromycin acts 24 hours. One dose per day is enough to treat infectious diseases.
Erythromycin is the shortest of all macrolides. It must be taken 4-6 times a day. Therefore, it is most often used in the form of local forms for the treatment of acne and skin infections. It is noteworthy that macrolides for children are safe, although they can cause diarrhea.