Macrolids are antibiotics of natural and semi-synthetic origin, having a macrocyclic lactone ring at the core. Depending on the amount of carbon atoms in the structure of the ring, the antibiotic is divided:

• 14-ticked (erythromycin, roxitromycin, oleandomycin, clarithromycin);
• 15-ticked (azithromycin preparations);
• 16-ticked (drugs of Midekamycin, Sp Ramicin and Josamamicina).

Natural macrolides include Erythromycin, Spiramycin, Josamamicina and Midekamycin preparations. The remaining macrolides belong to semi-synthetic antibiotics.

Preparations of the macrolide row have a bacteriostatic action. Inhibition of the growth of pathogenic microorganisms is due to the braking of protein synthesis in ribosomes.

An increase in dosage helps to achieve a bactericidal action.
Macrolid preparations refer to the least toxic antibacterial agents. With the reception of macrolides, there are no cases of severe nephrotoxic reactions, secondary dystrophic lesions of the joints, photosensibilization, manifesting the hypersensitivity of the skin to the effects of ultraviolet. Anaphylaxis and the emergence of antibiotic-associated states are found in a small percentage of patients.

The main direction in the use of this group of antibiotics is the treatment of nosocomial infections of the respiratory tract caused by gram-positive flora and atypical causative agents of 9 chladdi, mycoplasma, legionella, etc.).

Modern macrolides are similar in structure with their own source-erythromycin, the differences are manifested only in the nature of the side chains and in the amount of carbon atoms (14, 15 and 16). Side chains determine the activity with respect to the blue rod. The basis of the chemical structure of macrolides is a macrocyclic lactone ring.

Macrolids are classified according to the method of obtaining and on a chemical structural basis.

Method of receipt

In the first case, they are divided into synthetic, natural and prodrugs (erythromycin esters, oleandomycin salts, etc.). The prodrugs have a modified structure compared with the drug, but in the body under the influence of enzymes, they turn into the same active medicine having a characteristic pharmacological effect.

Prodrugs have improved taste qualities, high rates bioavailability. They are resistant to acidity drops.

Chemical structural basis

The classification implies the division of macrolides into 3 groups:

* Pr.- Natural.
** floor - semi-synthetic.

It is worth noting that azithromycin ® is azalid, since its ring contains a nitrogen atom.

Features of the structure of each MACR. affect activity indicators, medicinal interaction with other drugs, for pharmacokinetic properties, tolerability, etc. Mechanisms of influence on microbiocenosis in the presented pharmacological means Identical.

Macrolid Antibiotics Group: List of Preparations

Characteristics of each macrolide

Consider the main representatives of the group separately.

Erythromy ®.

The drug inhibits the growth of chlamydia, legionell, staphylococcus, mycoplasm and legionelle, a blue chopstick, Klebsiellas etc.

Bioavailability can reach sixty percent, it depends on food receptions. It is absorbed in the digestive tract partially.

Among the side effects are: dyspepsia, nausea, narrowing of one of the stomach departments (diagnosed in newborns), allergies, "shortness of shortness of breath".

Used in the treatment of tonsillitis, otites, sinusites, skin infections, lesteriosis, gonorrhea, diphtheria, legogella, etc.

Treatment with erythromycin during pregnancy and during lactation is contraindicated.

Roxitromycin ®.

Inhibits the growth of microorganisms that produce an enzyme that cleaves beta-lactam antibiotics. The drug is resistant to acids and alkalis. Bactericidal action is achieved due to the increase in dosage. The half-life is about ten o'clock. Bioavailability is equal to fifty percent.

Roxitromycin ® is well tolerated and excreted from the body unchanged.

We are prescribed with inflammation of the mucous membrane of the bronchi, larynx, the incomplete sinuses, the middle ear, the sky, the gallbladder, the urethra, the vaginal segment of the cervix, the infections of the skin, the musculoskeletal system, brucellose, etc.
Pregnancy (can be applied according to life indications), lactation period and age up to two months are contraindications.

Clarithromycin ®.

Inhibits the growth of aerobes and anaerobes. There is a low activity in relation to the koche wand. Excellence erythromycin on microbiological indicators. The preparation has acid resistance. Alkaline medium affects the achievement of antimicrobial action.

Clarithromycin ® is the most active macrolide with respect to the Helicobacter Pilori infecting various areas Stomach, and 12 pans. The half-life is about five hours. The bioavailability of the drug does not depend on food.

The drug is prescribed in infection of wounds, infectious diseases of the ENT organs, purulent rashes, pneumonia, bronchitis, furuncoolose, mycoplasmosis, mycobacteriosis against the background of the immunodeficiency virus. The tool also applies as part of comprehensive treatment schemes of the stomach and 12-two-seaman ulcers.

Infant age up to six months is contraindicated.

Oleandomycin ®.

Oleandomycin ® inhibits proteins synthesis in pathogen cells. Bacteriostatic action is enhanced in alkaline environment.

To date, cases of oleandomycin are single, as it is outdated.
The remedy is prescribed during brucellosis, abscessive pneumonia, bronchiectatic disease, trypper, inflammation brain shells, inner heart sheath, upper infections respiratory tract, purulent pleurisy, furunculese.

Azithromycin ®.

This is an antibiotic azalid, which in its structure differs from classic macrolides. K - H inhibits grams +, gramphors, aerobes, anaerobes and acts intracellularly.

The antibiotic has a wide range of action.

Josamamicin ® (Vilprafen Soluteab ®)

Natural antibiotic, obtained from a rainy fungus Streptomyces Narbonensis. Bactericidal action is achieved at high concentrations in the infection focus. Antibiotic ingbirket Synthesis protein and suppresses the growth of pathogens.

Josamicin therapy ® often leads to a decrease arterial pressure. The drug is actively used in otorinolaryngology (angina, pharyngitis, otitis), pulmonology (bronchitis, ornithosis, pneumonia), dermatology (furuncoolosis, corrosive inflammation, acne), urology (urethritis, prostatitis).

It is allowed to use during lactation, it is prescribed for the treatment of pregnant women. Newborn and children under fourteen years have shown a suspension form.

MIDEKAMICIN ® (MACROPEN ®)

Differs high indicators of microbial activity and good pharmacokinetic properties. Bactericidal action is achieved due to a significant increase in the dose. Bacteriostatic effect is associated with inhibiting protein synthesis.

Pharmacological effect depends on the type of malicious microorganism, the concentration of the drug, the size of the inoculum, etc. Midcamicine ® is used in infectious lesions of the skin, subcutaneous tissue, respiratory tract.

Midcamicine ® is a reserve antibiotic, and it is prescribed to patients with hypersensitivity to beta lactams. Actively applied in pediatrics.

Lactation period (penetrates breast milk) and pregnancy are contraindications. Sometimes the drug is prescribed by vital testimony and in the event that the benefit for the mother exceeds the potential risk to the fetus.

Spiramycin ®.

The bioavailability of the drug reaches forty percent.

The activity of the drug is reduced in an acidic medium and increases in alkaline. Alcohol contributes to an increase in penetrating ability: the antibiotic gets better in the cells of pathogens.

It has been scientifically proven that Spiramcine ® does not affect embryonic development, so it is permissible to take it to carry a child.

Breastfeeding antibacterial therapy stop.

Macrolid Group Antibiotics: Titles for children

Macrolides are well transferred and rarely cause heavy adverse reactions. Unwanted effects in children can manifest themselves with pain in the abdomen, a sense of discomfort in epigatstray, vomiting, nausea, allergic reactions.

Preparations, invented relatively recently, practically do not stimulate the motility of the gastrointestinal tract. Dyspeptic manifestations As a result of the use of MIDEKAMYCIN ®, MIDEKAMICINE acetate ® are not observed at all.

Clarithromycin ®, superior to other macrolides in many indicators deserves separate attention. Children up to 12 years old this drug is recommended to assign in the form of a suspension.

Macrolids are used at:

• therapies of atypical mycobacterial infections,
• hypersensitivity to β-lactams,
• diseases of bacterial genesis (sinusitis, otitis, tonsillites, bronchitis, skin infections and soft tissues, acne, helicobacter infection, etc.).

However, macrolide antibiotics should be appointed only by the pediatrician. Self-treatment is unacceptable.

Unwanted medicinal reactions

Macrolid therapy extremely rarely becomes the cause of anato-functional changes, but the occurrence of side effects is not excluded.

Allergy

In the course of scientific studied, in which about 2 thousand people took part, it was revealed that the likelihood of anaphylactoid reactions at the reception of macrolides is minimal. Cases of cross-allergies have not been recorded at all. Allergic reactions are manifested in the form of a nettle fever and rash. In isolated cases, anaphylactic shock is possible.

Zhkt.

Dyspecical phenomena arise due to a prokinetic effect characteristic of macrolides. Most patients celebrate rapid defecation, painfulness In the abdomen, violation of taste sensations, vomiting. Newborn may have a violation of food evacuation from the stomach into the small intestine.

The cardiovascular system

Pyruette ventricular tachycardia, cardiac arrhythmia, the syndrome of the elongated Qt interval is the main manifestations of the cardiotoxicity of this group of antibiotics. Exacerbate the position of old age, heart disease, dosage, water and electrolyte disorders.

Structural and functional liver disorders

CNS.

A long course of treatment, the dosage excess is the main causes of heputoxicity. Macrolids act differently on cytochrome - an enzyme involved in the metabolism of alien to the body of chemicals: erythromycin inhibits it, Josamamicin ® affects the enzyme of a little less, and the azithromycin ® does not have any effect.

History and development

Macrolids are a promising class of antibiotics. They were invented more than half a century ago, but still actively used in medical practice. The uniqueness of the macrolide rendered therapeutic effect It is due to the favorable pharmacokinetic and pharmacodynamic properties and the ability to penetrate the cell wall of pathogens.

High concentrations of macrolides contribute to the eradication of pathogens such as Chlamydia Trachomatis, Mycoplasma, Legionella, Campylobacter. These properties are beneficial to macrolides on the background of β-lactam.

Erythromycin ® laid the beginning of the macrolide class.

The first acquaintance with erythromycin occurred in 1952. Portfolio of the newest pharmaceutical preparations An international American innovative company Ilay Lilly & Company ® (ELI LILLY & COMPANY ®) has replenished. Her scientists brought erythromycin from radiant fungus living in the soil. Erythromycin has become an excellent alternative for patients who have hypersensitivity to penicillin-row antibiotics.

Expanding the scope of application, development and implementation of macrolides, modernized on microbiological indicators, dates from the seventies-eighties.

The erythromycine row is different:

• high activity against Streptococcus and Staphylococcus and intracellular microorganisms;
• low toxicity indicators;
• lack of cross allergies with beta-lactam antibiotics;
• creation of high and stable concentrations in tissues.

On our site you can get acquainted with the majority of antibiotics groups, full lists These drugs, classifications, history and other important information. To do this, the "" section is created in the upper menu of the site.

Content

Group medicinesThe basis of the structure of which is a macrocyclic lactone ring of 14 or 16 members, is called antibiotics by macrolides. They belong to polyceticids of natural origin. Their use helps to stop the growth and development of harmful bacteria.

The group of macrolides includes azalids (15-membered substances) and ketolides (14-membered drugs), nominally applies to an immunosuppressant tacrolimus (23-membered). The antimicrobial effect of funds is associated with a disruption of protein synthesis on the ribosomes of the microbial cell. Therapeutic doses of drugs have a bacteriostatic action, in high concentrations there are bactericidal on the causative agents of the cough, diphtheria, pneumococci.

Macrolids are effective against gram-positive coils, have immunomodulatory and anti-inflammatory activity.

With their admission, hematotoxicity, nephrotoxicity, the development of chondro- and arthropathic, photosensitization is not observed. The use of drugs does not lead to anaphylactic reactions, severe allergies, diarrhea.

Macrolids are distinguished high concentrations In the tissues (higher than in the blood plasma), the absence of cross allergies with beta lactams. They act on streptococcus, mycoplasmas, staphylococcus, chlamydia, legionelle, capampacteria. To means of resistant enterobacteria, pseudomonads, asinobacteria. Indications for the use of antibiotics are:

• tonsillopharygitis, acute sinusitis;
• exacerbation chronic bronchitis, non-hospital atypical pneumonia;
• whooping cough;
• chlamydia, syphilis;
• periodontitis, periostitis.

Macrolids are careful with severe liver diseases. Contraindications to their use are the intolerance to the components of the composition, pregnancy, lactation. Possible side effects Specified in the instructions:

• hepatitis, jaundice;
• fever, general malaise;
• hearing impairment;
• thrombophlebitis, phlebit;
• allergy, rash, urticaria.

Classification

Antibiotics of a number of macrolides are divided by the method of obtaining on natural and synthetic, according to a chemical structure for 14-, 15- and 16-membered, for generations on the first, second and third, on the duration of action on fast and long. Main classification:

Macrolred antibiotics

Antimicrobial drugs of a group of macrolides are represented by tablets, capsules, oral suspensions, parenteral solutions. Oral shapes are used in the easy course of the disease, intravenous and intramuscular - with severe or if it is impossible to receive tablets.

First generation

The first generation macrolides are limited in monotherapy, because microbial stability is rapidly developing. Acid resistance preparations are accepted inside, combined with tetracycles wide spectrum Applications. The means quickly reach the maximum concentration in the blood, act up to 6 hours, penetrate well in the tissue, are removed with feces and bile. Group representatives:

Second

The second-generation macrolides are higher than active in relation to the enterobacterium, a stick of influenz, pseudomonadam, anaerobam. They are resistant to acid hydrolysis, better absorbed in the stomach, act for a long time. Their prolonged half-life allows the use of drugs 1-2 times a day. Group representatives:

Third

Macrolids last generation It is well tolerated, resistance to them develops very slowly, they are better absorbed. The angry synthesis of the microbial cell protein, they lead to bacteriography. Preparations penetrate the tissue well, especially bone, are removed by the kidneys, with bile, act up to 12 hours. Group representatives:

Macrolids for children

The antibiotics of the macrolide group are used in children for starting therapy of atypical infections of respiratory organs (bronchitis, pneumonia caused by mycoplasmas, chlamydias) in the intolerance to beta-lactam. In the kids under five years old, drugs are used to treat bronchitis, angina, pharyngitis. Children can give oral or parenteral forms of drugs for otitis, tonsillopharygitis, diphtheria, cough. Popular Group Tools for Pediatric Use:

• Clarithromycin;
• Roxymitrocyne;
• Azithromycin;
• Spiramycin;
• Josamamicin.

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- These are bacteriostatically effective antibiotics, but in large concentrations there can be a bactericidal effect. This group of antibiotics has a wide range of action. The prototype of macrolide antibiotics is erythromycin derived from mushrooms.

In order to improve the pharmacokinetic properties of the macrolides, semi-synthetic derivatives were obtained, which have better acid stability, a wider range of action in a gram-negative range and a longer half-life. That is why macrolide antibiotics are divided into generations:

• 1 generation -, oleandomycin;
• 2 generation -;
• 3 generation - (Summen).

Macrolids inhibit the biosynthesis of protein of bacteria by attaching to the 50s subunit ribosoma. Further migration and growth of the resulting polypeptide chain, due to the blockade of the translochase enzyme, stops. therefore macrolides have a bacteriostatic action On bacteria that have an active metabolism. Macrolids are not very effective against the "rest bacteria."

Interaction and methods of application

Macrolred antibiotics can not be littered with grapefruit juice!

Macrolids are metabolized in the liverBy biotransformation of cytochrome P450 - CYP3A4 isoenzyme. When taking macrolides with medicines or products, which are also metabolized by CYP3A4 (for example, cimetidine, statins, cyclosporine, grapefruit) can occur. Macrolids inhibit the metabolism of other medicines through CYP3A4 and thereby increase their effect on efficiency.

Macrolids are used intravenously, intramuscularly and inside. They penetrate well into the pulmonary fabric, pleural, synovial and peritoneal cavities, in the liquid of the average and inner ear, in adenoids, almonds. Accumulate in macrophages and amplify phagocytosis. Easily penetrate into milk. Bad - through the GEB (hemato-encephalotic barrier), placenta.

Use during pregnancy should be carried out only by strict indications.

Development of stability and spectrum of action

Antibiotic resistance to macrolides is widespread among bacteria. Resistance is relatively simply manifested by bacteria, as they modify ribosomal enzyme systems. It is believed that if bacterium is resistant to a macrolid, it is also resistant to all other antibiotics (cross-resistance).

However, Ketolides, according to the latest studies, were effective when applied to the bacteria having resistance to azithromycin.

Macrolides have a bactericidal effect in a relationship:

• chlamydia
• mycoplasmas
• gram of positive coccobs,
• corinbacteria.

Bacteriostatic effect:

• neasery
• legionella
• hemophilic stick
• treplema
• klostridia,
• rickettsia.

The second generation of macrolides is more efficient in relation to grams of negative bacteria. Third generation + toxoplasm, hemophilic stick.

Side effects

Macrolred antibiotics are among the safe antibiotics. Ordinary side effects harmless, serious side effects are very rare. Common side effects include gastrointestinal disorders: dyspepsia - nausea, vomiting, diarrhea, rarely pseudomembranous colitis. Very rarely found allergic reactions and liver damage. The least complications, according to statistics, gives 3 generation macrolides.

If there is a violation of the liver function and is known to be allergic to macrolides, other antibiotics should be used.

An increase in dosage helps to achieve a bactericidal action.

Macrolids belong to the class of polyketides. Polyceticids are polycarbonyl compounds that are intermediate metabolic products in animal, plants and mushrooms.

With the reception of macrolides, there were no cases of selective violation of blood cell functions, its cellular composition, nephrotoxic reactions, secondary dystrophic lesions of joints, photosensitization, manifesting the hypersensitivity of the skin to the effects of ultraviolet. Anaphylaxis and the emergence of antibiotic-associated states are found in a small percentage of patients.

The antibiotics of the macrolide row occupy a leading position among the safest antimicrobial drugs.

The main direction in the use of this group of antibiotics is the treatment of nosocomial infections of the respiratory tract caused by gram-positive flora and atypical pathogens. A small lettering certificate will help us to systematize information and determine which antibiotics refer to macrolides.

Macrolids are classified according to the method of obtaining and on a chemical structural basis.

In the first case, they are divided into synthetic, natural and prodrugs (erythromycin esters, oleandomycin salts, etc.). The prodrugs have a modified structure compared with the drug, but in the body under the influence of enzymes, they turn into the same active medicine having a characteristic pharmacological effect.

Prodrugs have improved taste qualities, high bioavailability. They are resistant to acidity drops.

The classification implies the division of macrolides into 3 groups:

* Pr.- Natural.
* floor - semi-synthetic.

It is worth noting that azithromycin is azalid, since its ring contains a nitrogen atom.

Features of the structure of each MACR. affect the indicators of activity, drug interaction with other drugs, on pharmacokinetic properties, tolerability, etc. The mechanisms of influence on microbiocenosis in the presented pharmacological funds are identical.

Consider the main representatives of the group separately.

ER. Inhibits the growth of chlamydia, Legionell, staphylococci, mycoplasm and legionell, a blue chopstick, Klebsiella.
Bioavailability can reach sixty percent, it depends on food receptions. It is absorbed in the digestive tract partially.

Among the side effects are: Dislepsy, dyspepsia, narrowing of one of the stomach departments (diagnosed in newborns), allergies, "shortness of shortness of breath".

Prescribed in diphtheria, vibriosis, infectious lesions of skin, chlamydia, Pittsburgh pneumonia, etc.
Treatment with erythromycin during pregnancy and in the lactation period is excluded.

Inhibits the growth of microorganisms that produce an enzyme that splitting beta-lactam has an anti-inflammatory effect. R. resistient to acids and alkalis. Bactericidal action is achieved due to the increase in dosage. The half-life is about ten o'clock. Bioavailability is equal to fifty percent.

Roxitromycin is well tolerated and excreted from the body unchanged.

We are prescribed with inflammation of the mucous membrane of the bronchi, larynx, the incomplete sinuses, the middle ear, the sky, the gallbladder, the urethra, the vaginal segment of the cervix, the infections of the skin, the musculoskeletal system, brucellose, etc.
Pregnancy, lactation period and age up to two months are contraindications.

Inhibits the growth of aerobes and anaerobes. There is a low activity in relation to the koche wand. Clarithromycin is superior to erythromycin on microbiological indicators. The preparation has acid resistance. Alkaline medium affects the achievement of antimicrobial action.

Clarithromycin is the most active macrolide with respect to the helicobacter pylori infecting various areas of the stomach, and the 12th intestine. The half-life is about five hours. The bioavailability of the drug does not depend on food.

K. We are prescribed when infection of wounds, infectious diseases of the ENT organs, purulent rashes, furunculese, mycoplasmosis, mycobacteriosis against the background of the immunodeficiency virus.
The reception of clarithromycin in the early periods of pregnancy is prohibited. Infant age up to six months is also contraindicated.

Ol. Inhibits proteins synthesis in pathogen cells. Bacteriostatic action is enhanced in an alkaline environment.
To date, cases of oleandomycin are single, as it is outdated.
Ol. Prescribed in brucellosis, abscessive pneumonia, bronchiectatic disease, tripper, inflammation of the brain shells, the inner shell of the heart, the infections of the upper respiratory tract, purulent pleurite, furunculese, the hit of pathogenic microorganisms in the bloodstream.

The antibiotic demonstrates high indicators of activity in relation to helicobacter pylori, hemophilic chopstick, gonococcus. Azithromycin in three hundred times acid resistant erythromycin. Indicators of digestibility reach forty percent. Like all erythromycinic row antibiotics, azithromycin is well tolerated. The long-lasting period of half-life (more than 2 days) allows you to prescribe a medicine once a day. The maximum course of treatment does not exceed five days.

Effective in the eradication of streptococcus, the treatment of equity pneumonia, infectious lesions of the organs of the small pelvis, the urogenital system, tick-boring borreliosisVenusal diseases. During the length of the child is appointed by life indications.
Acceptors of HIV azithromycin - infected patients prevents the development of mycobacteriosis.

Natural antibiotic, obtained from a rainy fungus Streptomyces Narbonensis. Bactericidal action is achieved at high concentrations in the infection focus. J - H will slow down the synthesis of protein and suppresses the growth of pathogens.

Josamicin therapy often leads to a decrease in blood pressure. The drug is actively used in otorinolaryngology (angina, pharyngitis, otitis), pulmonology (bronchitis, ornithosis, pneumonia), dermatology (furuncoolosis, corrosive inflammation, acne), urology (urethritis, prostatitis).

It is allowed to use during lactation, it is prescribed for the treatment of pregnant women. Newborn and children under fourteen years have shown a suspension form.

Differs high indicators of microbial activity and good pharmacokinetic properties. Bactericidal action is achieved due to a significant increase in the dose. Bacteriostatic effect is associated with inhibiting protein synthesis.

Pharmacological effect depends on the type of malicious microorganism, the concentration of the drug, the size of the inoculum, etc. Midcamicine is used in infectious lesions of the skin, subcutaneous tissue, respiratory tract.

Midcamicine is a reserve antibiotic, and it is prescribed to patients with hypersensitivity to beta lactams. Actively applied in pediatrics.

Lactation period (penetrates breast milk) and pregnancy are contraindications. Sometimes Mn appointed vital testimony and in case the benefit for the mother exceeds the potential risk to the fetus.

Different from other macrollows by regulates immune system. The bioavailability of the drug reaches forty percent.

The activity of the drug is reduced in an acidic medium and increases in alkaline. Alcohol contributes to an increase in penetrating ability: the antibiotic gets better in the cells of pathogens.

It has been scientifically proven that spiramycin does not affect embryonic development, therefore it is permissible to take it upon the time to enter the child. The antibiotic affects breastfeeding, so in the lactation period it is worth finding an alternative drug.

Macrolid antibiotics for children should not be administered by intravenous infusion.

In the treatment of macrolides, the occurrence of life-degrading drug reactions is excluded. NLR in children are manifested by pain in the abdomen, a sense of discomfort in epigatstria, vomiting. Generally, children's organism Well tolerate macrolide antibiotics.

Preparations, invented relatively recently, practically do not stimulate the motility of the gastrointestinal tract. Dyspeptic manifestations as a result of the use of midecamicin, midecamicine acetate are not observed at all.

Separate attention deserves Clerythromycin, superior to other macrolides in many indicators. As part of a randomized controlled test, it was revealed that the antibiotic acts as an immunomodulator, providing a stimulating effect on the protective functions of the body.

Macrolids are used at:

• therapies of atypical mycobacterial infections,
• hypersensitivity to β-lactams,
• diseases of bacterial genesis.

They became popular in pediatrics due to the possibility of injecting administration in which the drug minus the gastrointestinal tract. This becomes necessary in emergency cases. The macrolide antibiotic is that most often prescribes a pediatrician in the treatment of infections in small patients.

Macrolid therapy extremely rarely becomes the cause of anato-functional changes, but the occurrence of side effects is not excluded.

In the course of scientific studied, in which about 2 thousand people took part, it was revealed that the likelihood of anaphylactoid reactions at the reception of macrolides is minimal. Cases of cross-allergies have not been recorded at all. Allergic reactions are manifested in the form of a networpiece and examine. In isolated cases, anaphylactic shock is possible.

Dyspecical phenomena arise due to a prokinetic effect characteristic of macrolides. Most patients celebrate rapid defecation, pain in the abdomen, violation of taste sensations, vomiting. The newborn develops pylorostenosis, the disease in which the evacuation of food from the stomach is difficult to the small intestine.

Pyruette ventricular tachycardia, cardiac arrhythmia, the syndrome of the elongated Qt interval is the main manifestations of the cardiotoxicity of this group of antibiotics. Exacerbate the position of old age, heart disease, dosage, water and electrolyte disorders.

A long course of treatment, the dosage excess is the main causes of heputoxicity. Macrolids act differently on cytochrome - an enzyme involved in the metabolism of alien to the body of chemicals: erythromycin inhibits it, Josamamicin affects the enzyme a little less, and the azithromycin does not at all have any influence.

Few doctors know by appointing a macrolide antibiotic that this is a direct threat to mental health. Neriva-mental disorders are most often occurring at the reception of Clarithromycin.

Video about the considered group:

Macrolids are a promising class of antibiotics. They were invented more than half a century ago, but still actively used in medical practice. The uniqueness of the macrolides of the therapeutic effect is due to the favorable pharmacokinetic and pharmacodynamic properties and the ability to penetrate through the cell wall of pathogens.

High concentrations of macrolides contribute to the eradication of pathogens such as Chlamydia Trachomatis, Mycoplasma, Legionella, Campylobacter. These properties are beneficial to macrolides on the background of β-lactam.

Erythromycin laid the beginning of the Class of Macrolides.

The first acquaintance with erythromycin occurred in 1952. The portfolio of the latest pharmaceutical preparations has replenished the international American innovative company Ilay Lilly & Company (Eli Lilly & Company) (ELI LILLY & COMPANY). Her scientists brought erythromycin from radiant fungus living in the soil. Erythromycin has become an excellent alternative for patients who have hypersensitivity to penicillin-row antibiotics.

Expanding the scope of application, development and implementation of macrolides, modernized on microbiological indicators, dates from the seventies-eighties.

The erythromycine row is different:

• high activity against Streptococcus and Staphylococcus and intracellular microorganisms;
• low toxicity indicators;
• lack of cross allergies with beta lactima antibiotics;
• creation of high and stable concentrations in tissues.

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Macrolids are antibiotics whose chemical structure is based on the presence of a macrocyclic lactone ring. The 14-membered ring has antibiotics such as erythromycin, clarithromycin, roxitromycin, fluritromycin; 15-mea - azithromycin; 16-membered Midcamicine, Spiramycin, Josamamicin, Leukiucin, Miocamicin. According to the method of obtaining macrolides, they are divided into natural (erythromycin, midekamycin, spiramsycin, josamycin) and semi-synthetic (clarithromycin, roxitromycin, azithromycin, midcamicine acetate). The division of macrolides on natural and semi-synthetic conditionally, since a row of natural antibiotics is obtained by synthesis.

In 1949, the Philippine scientist Alberto Aguilar found a new radiant fungus in the soil, which had the ability to suppress the growth of bacteria. In 1950, the American MAK MAIR from this fungus allocated the first antibiotic macrolide called - erythromycin.

Macrolids in therapeutic doses have a bacteriostatic effect, but, in high concentrations (increasing the dosage 2-4 times), a bactericidal on beta-hemolytic streptococci, pneumococcus, coat agents of the cough and diphtheria are capable of acting.
The antibacterial effect of antibiotics-macrolides are carried out by braking protein synthesis in ribosomes of growing microbial cells, and spiramycin, unlike other macrolides, is able to associate three 50s subunits of ribosomes at once, due to which there has a longer antimicrobial effect. On the microbial cells in the rest phase, these antibiotics do not have any impact. The spectrum of the action of macrolides is close to penicillins; They also suppress the reproduction of microbes resistant to penicillins, tetracycline and leftomycetins.
Macrolids have very high activity against gram-positive Catkops (Streptococcus Pneumoniae, Streptococcus aureus), intracellular pathogens (mycoplasma, Legionella SPP. Chlamydia SPP. Mycoplasma Pneumoniae) and many gram-negative microorganisms ( Haemophilus influenzae., Mrachlla, etc.). The most powerful antibacterial effect on gram-negative bacteria has azithromycin. Meanwhile, such families like - Enterobacteriaceae, Pseudomonas SPP. and Acinetobacter SPP. - Naturally resistant to all antibiotics macrolides. Many macrolides are manifesting in relation to gram-positive Cockkops an additional libeotic effect, i.e., can inhibit the vital activity of bacteria after their short-term contact with the antibiotic macrolide. At the same time, irreversible changes in the ribosomes of microbial cells occur, which allows to increase and prolong the overall antibacterial effect of the drug. Spiramycin has the highest post-libeotic effect among macrolides.

Antibiotics - macrolides have the ability to accumulate in the parenchyma of the lung, mucous membrane of the bronchi, tracheobronchial secrete, while creating high antibiotic concentrations in these tissues, which provides high bioavailability of these antibiotics. Macrolids are resistant and to -B-lactamase enzymes that produce Haemophilus Influenzae. In this connection, the main use of macrolides are found in treatment: the infections of the upper and lower respiratory tract (streptococcal tonsillopharygitis, sharp sinusitis), bronchitis, off-hospital pneumonia, cough. It is also used in skin and soft tissue infections, as well as for the treatment of chlamydia, syphilis, oral infections. Macrolides having a 15 and 16 membrane lactone ring (spiramycin, azithromycin, roxitromycin, clarithromycin) are preparations of the first selection when complete-friendly pneumonia.
Unlike other groups of antibiotics, macrolides have an immunomodulatory and moderate anti-inflammatory effect. The immunomodulatory effect occurs due to the ability of the antibiotic to inhibit the formation of inter-leukin-2, which takes part in the autoimmune tissue damage. This is due to the suppressive effect of the macrolide on T-lymphocytes. The anti-inflammatory effect of the macrolide is provided by their antioxidant properties. Macrolids affect the production of cytokines, contribute to the endogenous increase in glucocorticoids by activating the hypothalamic-pituitary-adrenal system.

Macrolids are low toxic and well tolerated patients. Many is acid resistant, which allows you to use both parenteral and oral forms of preparations. Sometimes they cause undesirable effects from the gastrointestinal tract in the form of nausea, dyspepsia, reducing appetite, vomiting, diarrhea. Rarely there are allergic reactions in the form of skin rashes. All this allows the use of macrolides as an alternative to beta-lactam antibiotics in the treatment of patients with infections of the upper and lower respiratory tract, for the prevention of rheumatism, cough (erythromycin), for the prevention of meningitis (spiramizin).

Contraindications when receiving macrolides: an allergic reaction, pregnancy and lactation. Carefully apply with liver diseases.

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c) erythromycin antibiotics

The antibiotics group includes erythromycin and oleandomycin. Those produced by some fungi Streptomyces.

According to the spectrum of action erythromycin and oleandomycin close to benzylpenicillin. They act on the same microorganisms as benzylpenicillin, and, moreover, active in relation to Bruzell, Rickettsius and Chlamydia (Fig. 29).

Fig. 29. Action spectra of antibiotics

Accordingly, the spectrum of action erythromycin and oleandomycin is effective for purulent-septic infections (sepsis, abscesses, osteomyelitis, sophisticated inflammation, angina, purulent inflammation of the middle ear, putty sinuses nasal, urine and biliary tract, etc.), pneumonia, epidemic meningitis, gonor, diphtheria, brucellosis and certain diseases caused by chlamydia (trachoma, psyttecosis).

In the process of treating erythromycin and oleandomycin infections, drug stability of microorganisms is very rapidly developing. Erythromycin and oleandomycin for therapy infectious diseases Used as backup antibiotics (see Table 15).

The side effect of drugs of this group is manifested mainly by allergic reactions and dyspeptic disorders. Erythromycin sometimes causes impaired liver functions.

Erythromycin. Erythromycinum - white powder, bitter taste, a little soluble in water.

Assign inside For 1-1 1/2 hours before the meal of 0.2-0.25 g every 4-6 hours.

Higher doses (for adults): inside - one-time 0.5 g, daily 2 g.

For the treatment of infectious lesions of the skin and mucous membranes (metal skin diseases, infected wounds, burns, trachoms) prescribe the drug a place In the form of official ointhromycini (Unguentum Erythromycini) containing 0.01 g of erythromycin in 1 g

Forms of release. Tablets at 0.1 and 0.25 g; capsules of 0.1 and 0.2 g; ointment in tubes 3; 7; 10; 15 and 30 g

Storage. List b; In the light-protected place.

In addition, erythromycin is produced in the form of soluble salt - phosphate erythromycin (Phosphas Erythromycini), which is designed for intravenous administration and produced in hermetically visited bottles of 0.05; 0.1 and 0.2 g

Oleandomycin phosphate. Olegomycini Phosphas is a white bitter taste powder, easily soluble in water.

Assign inside After eating 0.25 g every 4-6 hours.

Higher doses (for adults); inside - one-time 0.5 g, daily 2 g

Form release. Shell-covered tablets, 0.125

Storage. List B.

Description and instruction of erythromycin

Erythromycin is a fairly famous antibiotic. Macrolidal. This drug is striking the ability of bacteria to reproduction. Mostly gram-positive microorganisms are sensitive to its action, such as: staphylococci, streptococci. Clostridium, Corinbacteria. For the most part, gram-negative microorganisms do not show sensitivity to erythromycin. However, there are some infections caused by bacteria of this group that can be treated with this antibiotic. This medicinal product is prescribed for the treatment of diseases such as: diphtheria, brucellosis, cough, meningitis, otitis, syphilis and so on.

Eritromycin is produced in tablet form. Dosing features for patients of different age groups and reception schemes describes the instructions of the drug. The treatment of patients with individual intolerance to the drug or antibiotics of the group, people with severe liver disorders with him, is not shown. In periods of pregnancy or infant feeding, the use of erythromycin is not recommended. Those few studies that were conducted in relation to this drug, I revealed, albeit minor, but present teratogenic activity. That is, the ability to cause the fetus malformations of development. As side effects that are possible when taking this antibiotic, various disorders from the gastrointestinal tract and allergies are described, up to the development of anaphylactic shock.

Patients leaving their feedback on erythromycin, most often, express about this medicinal agent positively. However, there are reports of his by-step. For example, one girl drinking the tablet of this antibiotic in connection with the inflammation of the throat, felt strong spasmic pain in the stomach area. Similar messages left some other patients. Moreover, most of them have evolved such phenomena after the first dose of erythromycin.

Very often, this drug is used to treat urogenital infections, for example, chlamydia. It is worth only, remember that such therapy should appoint a doctor. One of the blatant examples of unacceptable self-treatment can be the story of one lady, which, desperate to cure from chlamydia on the recommendations of specialists, decided to appoint drugs on their own. She acted according to the principle: try all antibiotics, consistently. She described his experience in a bulk article. Dosages, drug reception schemes and their combinations in this "opus" completely contradict and pharmacological standards, and common sense. The author of "Methods" is confident that she "won" chlamydia, it is, with the help of erythromycin. However, acquaintance with its experience leaves doubts not only in her physical, but also psycho-emotional health.

Not many of us are decided to describe their own, copyright, ways to treat, but, put your hand on the heart, you have to admit that we often neglect the warnings and act on your own fear and risk, reading reviews about the drug or, sometimes, even just instructions. For some states and drugs, this is not critical. But with antibiotics, in general, and erythromycin, in particular, it is impossible to experiment. After all, these medicines have a strong, systemic effect on our body.

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Most antibiotics, overwhelming infectious agents, in parallel, have a negative impact on the internal microbiocenosis human organismBut, unfortunately, a number of diseases without using antibacterial agents are simply impossible.

The optimal exit from the situation is the drugs of the group of macrolides that occupy the leading positions in the list of the safest antimicrobial drugs.

The first representative of the class of antibiotics was erythromycin, obtained from soil bacteria in the middle of the last century. As a result of research, it was found that the basis of the chemical structure of the medication is the lactone macrocyclic ring to which carbon atoms are attached; This feature determined the name of the whole group.

The new tool was almost immediately widely popular; It was involved in the fight against diseases provoked by gram-positive bacteria. Three years later, the list of macrolides was replenished with oleandomycin and spyramsycin.

The development of the following generations of antibiotics of this series was due to the detection of the activity of early drugs in relation to Campylobacteria, chlamydia and mycoplasmas.

Today, after almost 70 years from the moment of discovery, erythromycin and spyramcin are still present in therapeutic schemes. In modern medicine, the first of these drugs is often used as a drug selection if patients have individual intolerance to penicillins, the second - as a highly efficient means characterized by a long antibacterial effect and the absence of a thermogenic effect.

Oleandomycin use an order less frequently: many specialists belong to this antibiotic to the number of obsolete.

Currently there are three generations of macrolides; The study of the properties of drugs continues.

The classification of drugs included in the described group of antibiotics is a chemical structure, a method of obtaining, the duration of exposure and a generation of medication.

Details about the distribution of drugs - in the table below.

Complete the specified classification follows three moments:

The list of drugs includes a tacrolimus - a medication, having a structure 23 atom and at the same time related to immunosuppressants and to the series under consideration.

The azithomycin structure includes a nitrogen atom, so the medicine is azalid.
Macrolid antibiotics have both natural and semi-synthetic origin.

Natural, in addition to the medicines already mentioned in the historical certificate, are Midekamycin and Josamicin; To synthesized artificially - azithromycin, clarithromycin, roxitromycin, etc. From the total group, prodrugs have a somewhat modified structure:

• erythromycin ethers and oleandomycin, their salts (propionyl, toleandomycin, phosphate, hydrochloride);
• esters of the first representative of a number of macrolides (Estolat, actentrant);
• midcamicin salts (myocamicin).

All the preparations under consideration have a bacteriostatic type of action: they oppress the growth of the colonies of infectious agents by disrupting the protein synthesis in pathogens. In some cases, the clinics specialists prescribe to patients an increased dosage of medicines: drugs involved in this way acquire a bactericidal effect.

Antibiotics groups of macrolides are characterized by:

• a wide range of exposure to pathogens (among microorganisms sensitive to drugs - pneumococci and streptococci, listera and spirochetes, ureaplasma and a number of other pathogens of diseases);
• minimal toxicity;
• high activity.

As a rule, the drugs under consideration are used in genitalia therapy (syphilis, chlamydia), oral diseases having bacterial etiology (periodontitis, periostitis), diseases of the respiratory system (cough, bronchitis, sinusitis).

The effectiveness of medicines relating to macrolides and in combating folliculites and furunculosis has been proven. In addition, antibiotics are prescribed at:

• gastroenterite;
• cryptosporidize;
• atypical pneumonia;
• acne (severe disease flow).

In order to prevent the macrolide, a group of macrolides is used to rehabilitate Meningococcus carriers, with surgical manipulations in the lower intestinal department.

Modern medicine actively uses in the patterns of erythromycin therapy, clarithromycin, illosone, spiramizin and a number of other representatives of the considered group of antibiotics. The main forms of their release are listed in the table below.

Pharmacy networks also offer consumers Summen in the form of aerosol, lyophilisate for infusion, chemomycin - in the form of a powder for cooking injection solutions. Erythromycin-liniment is faced into aluminum tubes. Illosone is produced in the form of rectal suppositories.

Brief description of popular funds - in the material below.

Resistant to the effects of alkalis, acids. It is prescribed mainly for diseases of the ENT organs, a genitourinary system, skin.

It is contraindicated in women in position and lactating, as well as small patients under the age of 2 months. Half-life - 10 hours.

Under the strict control of the doctor, the use of medication in the treatment of pregnant women (in difficult cases) is allowed. The bioavailability of the antibiotic directly depends on the meal, so drinking the drug before eating. Among the side effects are allergic reactions, violation of the functioning of the gastrointestinal system (including diarrhea).

Another name is Midcamicine.

It is used if the patient has individual intolerance to beta-lactam. It is assigned to curb the symptoms of the ailments, affecting the skin, respiratory organs.

Contraindications - pregnancy, period of natural feeding. Enabled in pediatrics.

Used in the treatment of pregnant women lactating ladies. Pediatrics are used in the form of a suspension. Can reduce patient hell. It is accepted regardless of the time of food eating.

He stops symptoms of diseases such as angina, bronchitis, furunculese, urethritis, etc.

Characterized by increased activity in relation to pathogens causing inflammatory processes in gastrointestinal (among them and Helicobacter pylori).

Bioavailability does not depend on the eating time. Among the contraindications - the first trimester of pregnancy, infant age. The half-life is short, does not exceed five hours.

The effect of the use of the medication increases when it enters an alkaline environment.

Provided with:

• bronchiectatic disease;
• purulent pleurisy;
• brucellosis;
• diseases of the upper respiratory tract.

The drug is a new generation. Acid-resistant.

The structure of the antibiotic differs from most medicines belonging to the described group. When involved in the treatment of HIV-infected people prevents mycobacteriosis.

Half-life - more than 48 hours; This feature reduces the use of the drug to 1 r. / day.

Incompatible with clindamycin, lincomycin, chloramphenicol; Reduces the effectiveness of beta-lactams and hormonal contraceptives. For severe course Disease is introduced intravenously. It does not apply during pregnancy, hypersensitivity to the drug component, during lactation.

It is characterized by the ability to adjust the immune system. Does not affect the fetus during the period of tooling, is involved in the treatment of pregnant women.

Safe for children (the dosage is determined by the doctor, taking into account weight, the age of the patient and the severity of his disease). Not subjected to cell metabolism, does not split in the liver.

Low-toxic macrolides of the last generation. Actively used in the therapy of adults and small (from 6 months) patients, since they do not have a significant negative impact on the body. Characterized by the presence of a long half-life, as a result of which are used no more than 1 time for 24 hours.

The new generation macrolides practically do not have contraindications, are well tolerated by patients when involved in therapeutic schemes. The duration of treatment with these drugs should not exceed 5 days.

It is impossible to use macrolids in the treatment of diseases.

It should be remembered: to use antibiotics without prior consultation with the doctor - it means that it is irresponsible to refer to the state of your health.

Most of the drug preparations are characterized by minor toxicity, but no attention to the information contained in the instructions for the use of macrolide medicines should not be discussed. According to annotation, when using medicines may occur:

• violations in the work of the gastrointestinal system (nausea, vomiting, dysbacteriosis), kidneys, liver and CNS;
• allergic reactions;
• vision disorders, hearing;
• arrhythmia, tachycardia.

If the patient's history is present the individual intolerance to the macrolides, it is impossible to use medical products in treatment.

Prohibited:

• drink alcohol by treatment;
• increase or decrease the prescribed dosage;
• skip the reception of tablets (capsules, suspension);
• stop accepting without re-passing analyzes;
• use medicines with an expired expiration date.

In the absence of improvements, the appearance of new symptoms should immediately apply to the attending physician.

Medical terms are often incomprehensible to the wide sections of the population, unfamiliar with narrow concepts. A non-specialist is difficult to figure out that the doctor discharges, since the name of the drug or group of medicines does not say anything to the patient. What is hidden behind the word "macrolides", which drugs are included in this group and for which they are needed - all this in the article.

Macrolids are a group of antibiotics. They are the preparations of the last generation.

Chemical structure of macrolides:

• The basis is a macrocyclic 14- or 16-membered lactone ring. Lactones are the complex cyclic esters of hydroxy acids, containing a certain group of elements in their ring (-C (O) O-).
• The structure is attached several (maybe one) of carbohydrate residues.

A group of medicines, the basis of the structure of which is a macrocyclic lactone ring from 14 or 16 members, is called antibiotics by macrolides. They belong to polyceticids of natural origin. Their use helps to stop the growth and development of harmful bacteria.

Mechanism of action macrolides

The group of macrolides includes azalids (15-membered substances) and ketolides (14-membered drugs), nominally applies to an immunosuppressant tacrolimus (23-membered). The antimicrobial effect of funds is associated with a disruption of protein synthesis on the ribosomes of the microbial cell. Therapeutic doses of drugs have a bacteriostatic action, in high concentrations there are bactericidal on the causative agents of the cough, diphtheria, pneumococci.

Macrolids are effective against gram-positive coils, have immunomodulatory and anti-inflammatory activity.

This is the least toxic antibiotics, safe and well tolerated patients. With their admission, hematotoxicity, nephrotoxicity, the development of chondro- and arthropathic, photosensitization is not observed. The use of drugs does not lead to anaphylactic reactions, severe allergies, diarrhea.

Macrolids are characterized by high concentrations in tissues (higher than in blood plasma), lack of cross allergies with beta lactams. They act on streptococcus, mycoplasmas, staphylococcus, chlamydia, legionelle, capampacteria. To means of resistant enterobacteria, pseudomonads, asinobacteria. Indications for the use of antibiotics are:

• tonsillopharygitis, acute sinusitis;
• exacerbation of chronic bronchitis, community-acquired atypical pneumonia;
• whooping cough;
• chlamydia, syphilis;
• periodontitis, periostitis.

Macrolids are careful with severe liver diseases. Contraindications to their use are the intolerance to the components of the composition, pregnancy, lactation. Possible side effects are indicated in the instructions:

• hepatitis, jaundice;
• fever, general malaise;
• hearing impairment;
• thrombophlebitis, phlebit;
• allergy, rash, urticaria.

Classification

Antibiotics of a number of macrolides are divided by the method of obtaining on natural and synthetic, according to a chemical structure for 14-, 15- and 16-membered, for generations on the first, second and third, on the duration of action on fast and long. Main classification:

Macrolred antibiotics

Antimicrobial drugs of a group of macrolides are represented by tablets, capsules, oral suspensions, parenteral solutions. Oral shapes are used in the easy course of the disease, intravenous and intramuscular - with severe or if it is impossible to receive tablets.

First generation

The first generation macrolides are limited in monotherapy, because microbial stability is rapidly developing. Acid resistance preparations are accepted inside, combined with a broad spectrum tetracycles. The means quickly reach the maximum concentration in the blood, act up to 6 hours, penetrate well in the tissue, are removed with feces and bile. Group representatives:

Second

The second-generation macrolides are higher than active in relation to the enterobacterium, a stick of influenz, pseudomonadam, anaerobam. They are resistant to acid hydrolysis, better absorbed in the stomach, act for a long time. Their prolonged half-life allows the use of drugs 1-2 times a day. Group representatives:

Third

The latter generation macrolides are well transferred, resistance to them develops very slowly, they are better absorbed. The angry synthesis of the microbial cell protein, they lead to bacteriography. Preparations penetrate the tissue well, especially bone, are removed by the kidneys, with bile, act up to 12 hours. Group representatives:

Macrolids for children

The antibiotics of the macrolide group are used in children for starting therapy of atypical infections of respiratory organs (bronchitis, pneumonia caused by mycoplasmas, chlamydias) in the intolerance to beta-lactam. In the kids under five years old, drugs are used to treat bronchitis, angina, pharyngitis. Children can give oral or parenteral forms of drugs for otitis, tonsillopharygitis, diphtheria, cough. Popular Group Tools for Pediatric Use:

• Clarithromycin;
• Roxymitrocyne;
• Azithromycin;
• Spiramycin;
• Josamamicin.

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