List of macrolide preparations with a detailed description. Macrolides: a group of antibiotics of the latest generation in the treatment of ENT diseases
is a class of antibiotics. The basis of the chemical structure of macrolides is the macrocyclic lactone ring. Depending on the number of carbon atoms, macrolides are divided into 14-membered (natural - erythromycin, semi-synthetic - clarithromycin, roxithromycin), 15-membered (semi-synthetic - azithromycin), 16-membered (natural - josamycin, spiramycin, midecamycin; semi-synthetic - midecamycin acetate). The activity of macrolides against gram-positive cocci and intracellular pathogens (legionella, campylobacter, chlamydia, mycoplasma) is considered the main clinical significance macrolides. Macrolides are included in the list of antibiotics with the least toxicity.
Mechanism of action
They have an antimicrobial effect due to a violation of protein synthesis on the ribosomes of a microbial cell. Often, macrolides exhibit a bacteriostatic effect, but their high concentrations contribute to the provision of a bactericidal effect against pneumococci, GABHS, diphtheria and whooping cough pathogens. The manifestation of PAE macrolides is characteristic of gram-positive cocci. Macrolides, in addition to antibacterial action, have immunomodulatory and moderately anti-inflammatory activity.
Activity Circle
Macrolide activity manifests itself in relation to gram-positive cocci (S.pyogenes, S.pneumoniae, S.aureus, with the exception of MRSA). Per recent times an increase in resistance was detected, however, in certain cases, 16-membered macrolides may remain active against pyogenic streptococci and pneumococci that are not amenable to the effects of 14- and 15-membered drugs.
Macrolides are active against pathogens of diphtheria and whooping cough, ureaplasma, mycoplasma, chlamydia, spirochetes, listeria, campylobacter, legionella, moraxella, anaerobes (except B.fragilis).
Azithromycin is better than other macrolides for H.influenzae, and clarithromycin for H.pylori and atypical mycobacteria (for example, M.avium, etc.). Roxithromycin, azithromycin and spiramycin are active against some protozoa (Cryptosporidium spp., T. gondii). Clarithromycin acts on H.influenzae and other pathogens with enhanced activity due to its active metabolite, 14-hydroxyclarithromycin.
In microorganisms of the family Acinetobacter spp., Pseudomonas spp. and Enterobacteriaceae revealed natural resistance to the action of all macrolides.
Pharmacokinetics
Type of drug, its lek. the form and intake of food affect the absorption of macrolides in gastrointestinal tract. Due to the presence of food, the bioavailability of erythromycin is significantly reduced, less - midecamycin, azithromycin and roxithromycin. The presence of food has little effect on the bioavailability of josamycin, spiramycin and clarithromycin.
Concentrations of macrolides in blood serum are an order of magnitude lower than those in tissues and vary in different drugs Therefore, antibiotics of the macrolide group are referred to as tissue antibiotics. The lowest concentrations are observed in azithromycin, the highest in roxithromycin.
The connection of macrolides with blood plasma proteins is carried out to varying degrees. Roxithromycin has the highest binding to plasma proteins - 90%, spiramycin - the smallest - less than 20%. Macrolides are well distributed in the body, while high concentrations are created in various organs and tissues (including the prostate gland), especially during inflammation. Macrolides are able to penetrate into cells and create high concentrations there. Possess poor conductivity through the hemato-ophthalmic barrier and BBB. penetrate into breast milk and pass through the placenta.
Metabolism of macrolides occurs in the liver, in which the microsomal cytochrome P-450 system takes part. The excretion of metabolites is carried out mainly with bile. One of the metabolites of clarithromycin showed antimicrobial activity. Metabolism is predominantly excreted with bile, and through the kidneys - 5-10%. The half-life of macrolides is from 1 (for midecamycin) to 55 hours (for azithromycin). kidney failure in most macrolides (except roxithromycin and clarithromycin) does not affect this indicator. Cirrhosis of the liver can provoke a significant increase in the half-life of josamycin and erythromycin.
Adverse reactions
Macrolides are one of the safest groups of AMPs. In general, adverse reactions are rare.
Heart: rarely - prolongation of the QT interval on the electrocardiogram.
CNS: dizziness, headache, hearing loss (in rare cases - with the introduction of / in large doses clarithromycin and erythromycin).
Liver: cholestatic hepatitis, transient increase in liver transaminase activity - manifested by nausea, vomiting, abdominal pain, weakness, general malaise, fever, jaundice (more often as a result of the use of clarithromycin and erythromycin, in isolated cases - from josamycin and spiramycin).
GIT: diarrhea, vomiting, nausea, discomfort or pain in the abdomen (most often manifested by taking erythromycin, which has a prokinetic effect, in rare cases - from josamycin and spiramycin).
allergic reactions: in very rare cases, urticaria, rash, etc.
Local reactions: phlebitis and thrombophlebitis in the case of intravenous administration, caused by local irritant action (macrolide antibiotics are prohibited to be administered in a stream and in a concentrated form - administration is carried out by slow infusion).
Indications
NDP infections: community-acquired pneumonia (including atypical), exacerbation of chronic bronchitis.
URT infections: acute sinusitis, streptococcal tonsillopharyngitis, CCA in children (taking azithromycin).
Skin and soft tissue infections.
Diphtheria (a combination of erythromycin and antidiphtheria serum).
Oral infections: periostitis, periodontitis.
STIs: syphilis (except neurosyphilis), chlamydia, lymphogranuloma venereum, chancre.
Campylobacter gastroenteritis (reception of erythromycin).
heavy acne(taking azithromycin, erythromycin).
Toxoplasmosis (often taking spiramycin).
H.pylori eradication in case peptic ulcer stomach and 12 duodenal ulcer(combination of clarithromycin with antisecretory drugs, metronidazole and amoxicillin).
Cryptosporidiosis (spiramycin, roxithromycin).
Prevention and treatment of mycobacteriosis provoked by M.avium in patients with AIDS (clarithromycin, azithromycin).
Preventive use:
- prevention of whooping cough in people who are in contact with patients (prescription of erythromycin);
- Sanitation of carriers of meningococcus (appointment of spiramycin);
- year-round prevention of rheumatism in case of allergic reactions to penicillin (prescription of erythromycin);
- prevention of endocarditis in dentistry (appointment of clarithromycin, azithromycin);
- bowel decontamination before colon surgery (combination of erythromycin and kanamycin).
Contraindications
It is forbidden to use if allergic reactions to macrolides are detected, during pregnancy (roxithromycin, midecamycin, clarithromycin), during breastfeeding (spiramycin, roxithromycin, midecamycin, clarithromycin, josamycin).
Warnings
Pregnancy. It has been proven that clarithromycin can have an undesirable effect on the fetus. There are no data on the safety of midecamycin and roxithromycin during pregnancy, so they should also not be prescribed in given period. Pregnant women can take spiramycin, josamycin and erythromycin as they do not affect the fetus. Azithromycin can be prescribed only for vital indications.
Lactation. Most macrolides have the ability to pass into breast milk (no data on azithromycin). Only erythromycin does not affect the baby through breast milk. It is not recommended to use other macrolides for nursing mothers.
Pediatrics. Information about the safety of clarithromycin in children under 6 months of age. missing. The half-life of roxithromycin in younger patients may be extended up to 20 hours.
Geriatrics. Elderly people are not limited to taking macrolides, but when prescribing erythromycin, the likely age-related changes liver function, increased risk of hearing loss.
Heart disease. Exercise caution when prescribing macrolides in case of prolongation of the QT interval on the electrocardiogram.
Impaired liver function. Severe illnesses liver require increased attention when prescribing macrolides, since with impaired liver function, the half-life may increase, and the risk of hepatotoxicity of drugs, especially erythromycin and josamycin, also increases.
Impaired kidney function. A decrease in creatinine clearance of less than 30 ml / min may cause an increase in the half-life of clarithromycin up to 20 hours, its active metabolite - up to 40 hours. A decrease in creatinine clearance to 10 ml / min can cause an increase in the half-life of roxithromycin up to 15 hours. Such cases suggest a correction of the dosing regimen of these macrolides.
Drug Interactions
At the heart of most drug interactions of antibiotics of the macrolide group is their inhibition of cytochrome P-450 in the liver. The distribution of macrolides according to the severity of its inhibition occurs in the following order: midecamycin> roxithromycin> azithromycin> spiramycin = clarithromycin> erythromycin> josamycin. With the help of macrolides, metabolism is inhibited and the concentration in the blood of indirect anticoagulants, cyclosporine, ergot preparations, disopyramide, valproic acid, carbamazepine, theophylline increases, which entails an increased risk of developing adverse reactions caused by this group of antibiotics, and it may be necessary to correct their dosing regimen. The combination of macrolides (exception: spiramycin) with cisapride, astemizole and terfenadine is not recommended, as it may lead to the development of severe disorders heart rate as a result of prolongation of the QT interval.
Absorption of macrolides (especially azithromycin) in the gastrointestinal tract decreases with simultaneous reception with antacids.
Due to weakening of digoxin inactivation intestinal microflora macrolides may increase its oral bioavailability.
When taken simultaneously with rifampicin, the metabolism of macrolides in the liver increases, and a decrease in their concentration in the blood is also observed.
Erythromycin, especially when administered intravenously, has the ability to enhance the absorption of alcohol into the gastrointestinal tract, as well as increase its concentration in the blood.
Information for patients
Clarithromycin, josamycin, and spiramycin can be taken with or without food, and other macrolides can be taken 2 hours after or 1 hour before meals.
Erythromycin should be taken with a full glass of water (when taken orally).
It is necessary to follow the instructions when preparing and taking liquid lek. forms intended for oral administration.
Do not take drugs that have expired.
During treatment with erythromycin, it is forbidden to drink alcohol.
Strict adherence to the regimen is recommended throughout the course of treatment, especially in the treatment of streptococcal infections. Do not skip a dose. Take the dose at regular intervals. If a dose is missed for any reason, take it as soon as possible, but if it is almost time for the next dose, do not take the missed dose. Doubling the dose is prohibited.
A doctor's consultation is required if there is no improvement within a few days or if new symptoms appear.
generation:
- Spiramycin (rovamycin);
- Roxithromycin (rulide);
- Josamycin (Vilprafen);
- Clarithromycin (clacid);
- Midecamycin (macrofoam);
- Dirithromycin (dynabac).
generation:
- Azithromycin (Sumamed).
Azithromycin by chemical structure referred to as azalides. Their division is based on the spectrum of action, pharmacokinetic characteristics and undesirable effects. The spectrum of action of dirithromycin coincides with that of erythromycin.
Macrolides a group of antibiotics for children
Indications for the use of macrolides
Pharmacodynamics: Macrolides for children inhibit RNA synthesis at the level of the 50-S subunit of ribosomes. Pharmacological effect - bacteriostatic. It should be noted that the drugs are capable of exerting an immunomodulating effect on the functions of peripheral blood phagocytes (increased chemotaxis, etc.). This effect associated with the anti-inflammatory effect of certain macrolides (erythromycin, roxithromycin and clarithromycin), due to their antioxidant activity and the ability to reduce the processes of oxidative metabolism ("oxidative burst") in phagocytes, reducing the formation of superoxide ion. "Oxidative burst" is one of the most powerful mechanisms of intracellular digestion of bacteria.
However, in a number of cases, the processes of oxidative metabolism, reaching their maximum manifestation, themselves have a damaging effect on the human body, making the inflammation reaction inadequate to the cause that causes it. On an experimental model of inflammation, it was shown that the anti-inflammatory effect of drugs is due to a decrease in the activity of cyclooxygenase and lipoxygenase of cells.
How to use macrolides
The spectrum of action of this group of antibiotics is wide. Moreover, antibiotics have a bactericidal effect on some microorganisms that are highly sensitive to macrolides: Gr. "+" cocci (methicillin-sensitive staphylococci, streptococci, pneumococci), Gr. "+" rods (corynebacteria), Gr. "-" sticks (moraxella), chlamydia, ureaplasma and mycoplasma. Macrolides affect other microorganisms bacteriostatically: Neisseria, Legionella, Haemophilus influenzae, Brucella, Treponema, Clostridia (except CI. difficile), Bacteroids (except Bact. fragilis) and Rickettsia.
Macrolides of II and III generations have more wide range. So, to drugs of the second generation: josamycin and clarithromycin, high sensitivity of Helicobacter pylori was revealed; to spiramycin and roxithromycin - toxoplasma. Preparations of the II and III generations were effective against Campylobacter, Listeria, Gardnerella and some mycobacteria.
The secondary resistance of microorganisms to macrolides develops rapidly, so the course of treatment of the child should be short (up to 7 days), otherwise they must be combined with other antibiotics. It should be emphasized that in the event of secondary resistance to one of the macrolides, it applies to all other antibiotics of this group and even to drugs from other groups: lincosamides (lincomycin, clindamycin) and penicillins, which are destroyed by staphylococcal beta-lactamase.
Pharmacokinetics of macrolides
Some macrolides can be given intravenously to children (erythromycin phosphate, spiramycin, and clarithromycin), others parenteral administration(subcutaneous, intramuscular) - do not use, since injections are painful and local tissue damage occurs. These drugs can be administered orally. The bioavailability of drugs ranges from 30% to 70%. More acid-resistant are oleandomidin and antibiotics of the II and III generation, so they can be taken regardless of the meal. It is recommended to take pills mineral water"Borjomi" or a solution of sodium bicarbonate. There are preparations (ointments) for topical use.
The time of occurrence of the maximum concentration of drugs in the blood plasma is 1.5 - 2 hours (when taken orally). At the same time, most macrolides bind to plasma proteins by 60-70%. However, these antibiotics have low affinity for blood proteins, so they are very quickly and easily cleaved from them, entering various tissues. In preparations of the II and III generation, the penetrating ability is higher than that of erythromycin and oleandomycin.
These drugs penetrate well into the adenoids and tonsils of the child; tissues and fluids of medium and inner ear; lung tissue, bronchi, bronchial secretion and sputum; pleural, peritoneal, synovial fluid; skin. They are able to accumulate in phagocytic cells (polymorphonuclear leukocytes, pulmonary macrophages), where their concentration can be 13-20 times greater than in the extracellular fluid. Thus, macrolides help fight intracellular infection (legionella, chlamydia, mycoplasma, listeria, brucella, toxoplasma, etc.), which is manifested by a protracted, recurrent and atypical course of the inflammatory process.
This is very important for debilitated patients, to prevent recurrence of the disease. It should be noted that capture of macrolides by macrophages promotes the transport of antibiotics to the foci of infection. Moreover, the release of macrolides from phagocytes occurs only in the presence of an infectious factor, which makes these drugs safe for uninfected tissue cells of the patient.
Macrolides cross the placenta, but their concentration in the blood of the fetus is only 20-25% of the level in the mother's blood. Since these are low-toxic antibiotics, if necessary, they can be used in pregnant women. The drugs pass into the mother's milk, where they accumulate intensively, so it is necessary to interrupt breastfeeding. All drugs of this group of antibiotics penetrate the blood-brain barrier very poorly, so sanitation of the cerebrospinal fluid does not occur during meningitis.
With urine after ingestion, only 2-3% of the antibiotic from the administered dose is excreted. However, when intravenous administration the amount of the drug in the urine can reach 12 - 15%. This concentration is sufficient to suppress microflora sensitive to macrolides, but urine must be alkalized.
Macrolide Interactions
Macrolides should not be administered in the same syringe with B vitamins, ascorbic acid, cephalothin, tetracyclines, chloramphenicol, heparin, diphenylhydantoin (difenin), as complexes are formed that precipitate. Macrolides are not prescribed simultaneously with terfenadine and astemizole because of the risk of hepatotoxicity and the occurrence of ventricular arrhythmias.
The interaction of macrolides with levomycetin is contraindicated, since it also disrupts RNA synthesis at the level of the SO-S subunit of ribosomes, so antagonism occurs between them (1+1=0.75). It is known that I generation macrolides can more often cause the so-called transient effects: ototoxicity and neuromuscular block. Therefore, the summation of the above undesirable effects is possible when macrolides are combined with aminoglycosides, polymyxins, glycopeptide and polyene antibiotics, which also cause these effects.
Macrolides of the 1st generation and, to a lesser extent, of the 2nd generation inhibit the activity of enzymes of the monooxygenase system in the liver due to the formation of stable compounds with some P-450 cytochromes. As a result, biotransformation in the liver of a number of simultaneously named medicines and the rate of their elimination decreases. This is accompanied by the accumulation of these substances in the body and the occurrence of undesirable effects, sometimes life-threatening. These drugs include: theophylline, chloramphenicol, bromocriptine, warfarin, cimetidine, carbamazepine, dihydroergotamine, antipyrine, methylprednisolone, etc.
The interaction of macrolides with bacteriostatic drugs with a different mechanism of action is possible. For example, with tetracyclines that disrupt RNA synthesis at the level of the 30-S-ribosomal subunit; or with sulfonamides, which compete with para-aminobenzoic acid.
Side effects of macrolides
Side effects of macrolides
Macrolides are low-toxic drugs. Complications with the use of drugs of the first generation occur on average in 4.1% of patients, with the use of the second generation - in 2.6% of patients, with the use of the third generation - in 0.7% of patients.
- Dyspeptic symptoms (nausea, vomiting, diarrhea);
- Stomatitis, gingivitis;
- cholestasis;
- With intravenous administration - phlebitis. In order to avoid irritation and inflammation of the veins, it is recommended to dilute 1 mg of the antibiotic in 1 ml. isotonic solution sodium chloride or 5% glucose solution and infusion over 30-60 minutes;
- Rarely - cardiac arrhythmias, lengthening Q-T interval; and with intravenous administration - temporary deafness.
Most antibiotics, while suppressing the development of infectious agents, simultaneously have a negative impact on the internal microbiocenosis. human body, but, unfortunately, a number of diseases without the use antibacterial agents it is simply impossible to cure.
The best way out of the situation is the preparations of the macrolide group, which occupy a leading position in the list of the safest antimicrobial drugs.
History reference
The first representative of the class of antibiotics under consideration was Erythromycin, obtained from soil bacteria in the middle of the last century. As a result of research activities, it was found that the basis of the chemical structure of the drug is a lactone macrocyclic ring, to which carbon atoms are attached; this feature determined the name of the entire group.
The new tool almost immediately gained wide popularity; 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 Spiramycin.
The development of the next generations of antibiotics of this series was due to the discovery of activity early drugs groups against campylobacter, chlamydia and mycoplasmas.
Today, almost 70 years after their discovery, Erythromycin and Spiramycin are still present in therapeutic regimens. AT modern medicine first of specified medicines often used as the drug of choice in the presence of 
in patients with individual intolerance to penicillins, the second - as a highly effective agent, characterized by a long-term antibacterial effect and the absence of teratogenic effects.
Oleandomycin is used much less often: many experts consider this antibiotic to be outdated.
AT this moment there are three generations of macrolides; drug research is ongoing.
Systematization principles
The classification of drugs included in the described group of antibiotics is based on the chemical structure, method of preparation, duration of exposure and generation of the drug.
Details of the distribution of drugs - in the table below.
This classification should be supplemented with three points:
The list of group drugs includes Tacrolimus, a drug that has 23 atoms in the structure and simultaneously belongs to immunosuppressants and to the series under consideration.
The structure of Azithromycin includes a nitrogen atom, so the drug is azalide.
Macrolide antibiotics are of both natural and semi-synthetic origin.
Natural, in addition to the medicines already indicated in the historical reference, include Midecamycin and Josamycin; artificially synthesized - Azithromycin, Clarithromycin, Roxithromycin, etc. Prodrugs with a slightly modified structure stand out from the general group:
- esters of Erythromycin and Oleandomycin, their salts (propionyl, troleandomycin, phosphate, hydrochloride);
- ester salts of the first representative of a number of macrolides (estolate, acistrat);
- Midecamycin salts (Myokamicin).
general description
All drugs under consideration have a bacteriostatic type of action: they inhibit the growth of colonies of infectious agents by disrupting protein synthesis in pathogen cells. In some cases, clinic specialists prescribe an increased dosage of medications to patients: the drugs involved in this way acquire a bactericidal effect.
Antibiotics of the macrolide group are characterized by: 
- a wide range of effects on pathogens (including drug-sensitive microorganisms - pneumococci and streptococci, listeria and spirochetes, ureaplasma and a number of other pathogens);
- minimal toxicity;
- high activity.
As a rule, the drugs in question are used in the treatment of genital infections (syphilis, chlamydia), diseases of the oral cavity with bacterial etiology (periodontitis, periostitis), diseases respiratory system(whooping cough, bronchitis, sinusitis).
The effectiveness of medicines related to macrolides has also been proven in the fight against folliculitis and furunculosis. In addition, antibiotics are prescribed for:
- gastroenteritis;
- cryptosporidiosis;
- atypical pneumonia;
- acne (severe course of the disease).
For the purpose of prevention, a group of macrolides is used to sanitize meningococcal carriers, during surgical procedures in lower section intestines.
Macrolides - drugs, their characteristics, a list of the most popular forms of release
Modern medicine actively uses Erythromycin, Clarithromycin, Iloson, Spiramycin and a number of other representatives of the considered group of antibiotics in therapy regimens. The main forms of their release are shown in the table below.
| Drug names | Packing type | |||
| Capsules, tablets | Granules | Suspension | Powder | |
| Azivok | + | |||
| + | + | |||
| Josamycin | + | |||
| Zitrolide | + | |||
| Ilozon | + | + | + | + |
| + | + | + | ||
| + | + | |||
| Rovamycin | + | + | ||
| Rulid | + | |||
| Sumamed | + | + | ||
| Hemomycin | + | + | ||
| Ecomed | + | + | ||
| + | + | |||
Pharmacy chains also offer consumers Sumamed in the form of an aerosol, lyophilisate for infusion, Hemomycin - in the form of a powder for preparation injection solutions. Erythromycin-liniment is packed in aluminum tubes. Ilozon is available in the form of rectal suppositories.
A brief description of popular tools is in the material below.
Resistant to alkalis, acids. It is prescribed mainly for diseases of the ENT organs, genitourinary system, skin.
It is contraindicated in pregnant and lactating women, as well as in small patients under the age of 2 months. The half-life is 10 hours.
Under the strict supervision of a doctor, it is allowed to use the medication in the treatment of pregnant women (in difficult cases). The bioavailability of the antibiotic is directly dependent on food intake, so the drug should be drunk before meals. In list side effects - allergic reactions, disruption of the functioning of the gastrointestinal tract (including diarrhea).
Another name for the drug is Midecamycin.
It is used when the patient has an individual intolerance to beta-lactams. It is prescribed to suppress the symptoms of ailments that affect skin, respiratory system.
Contraindications - pregnancy, the period of breastfeeding. Involved in pediatrics.
Josamycin
It is used in the treatment of pregnant, lactating women. In pediatrics, it is used in the form of a suspension. May lower the patient's blood pressure. It is taken regardless of the time of eating.
Stops the symptoms of diseases such as tonsillitis, bronchitis, furunculosis, urethritis, etc.
Characterized increased activity towards pathogens that cause inflammatory processes in the gastrointestinal tract (among them Helicobacter pylori).
Bioavailability does not depend on the time of eating. Among the contraindications are the first trimester of pregnancy, infancy. The half-life is short, less than five hours.
Oleandomycin
The effect of the use of the drug increases when it enters the alkaline environment.
Activated when:
- bronchiectasis;
- purulent pleurisy;
- brucellosis;
- diseases of the upper respiratory tract.
New generation drug. Acid resistant.
The structure of the antibiotic differs from most medicines belonging to the described group. When involved in the treatment of HIV-infected patients, it prevents mycobacteriosis.
The half-life is more than 48 hours; this feature reduces the use of the drug to 1 r./day.
Ilozon
Incompatible with Clindamycin, Lincomycin, Chloramphenicol; reduces the effectiveness of beta-lactams and hormonal contraceptives. At severe course disease is administered intravenously. It is not used during pregnancy, hypersensitivity to the components of the drug, during lactation.
Features the ability to adjust immune system. Does not affect the fetus during the gestation period, is involved in the treatment of pregnant women.
Safe for children (the dosage is determined by the doctor, taking into account the weight, age of the patient and the severity of his disease). Does not undergo cellular metabolism, does not break down in the liver.
Zatrin, Lincomycin, Clindamycin, Sumamed
Low toxicity macrolides latest generation. They are actively used in the treatment of adults and small (from 6 months) patients, since they do not have a significant negative impact on the body. They are characterized by the presence of a long half-life, as a result of which they are used no more than 1 time for 24 hours.
Macrolides of the new generation have practically no contraindications, are well tolerated by patients when involved in therapeutic regimens. The duration of treatment with these drugs should not exceed 5 days.
Application features
It is impossible to use macrolides in the treatment of diseases on their own.
It should be remembered: to use antibiotics without first consulting a doctor means to be irresponsible about your health.
Most of the drugs in the group are characterized by slight toxicity, but the information contained in the instructions for the use of macrolide medications should not be ignored. According to the annotation, when using drugs, you may experience:
If the patient has a history of individual intolerance to macrolides, use medical goods this series cannot be treated.
Forbidden:
- drink alcohol during treatment;
- increase or decrease the prescribed dosage;
- skip taking pills (capsules, suspensions);
- stop taking without retesting;
- use medicines with expired validity.
In the absence of improvement, the appearance of new symptoms should immediately contact your doctor.
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Macrolides are naturally occurring antibiotics complex structure and have a bacteriostatic effect. growth inhibition pathogenic microorganisms occurs due to inhibition of protein synthesis in ribosomes.
Increasing the dosage helps to achieve a bactericidal effect.
Macrolides belong to the class of polyketides. Polyketides are polycarbonyl compounds that are metabolic intermediates in animal, plant, and fungal cells.
When taking macrolides, there were no cases of selective dysfunction of blood cells, its cellular composition, nephrotoxic reactions, secondary dystrophic damage to the joints, photosensitivity, manifested by hypersensitivity of the skin to ultraviolet radiation. Anaphylaxis and the occurrence of antibiotic-associated conditions occur in a small percentage of patients.
Macrolide antibiotics occupy a leading position among the safest antimicrobial drugs for the body.
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 little background information will help us systematize information and determine which antibiotics are macrolides.
Modern medicine has about ten antibiotics - macrolides. They are similar in structure to their ancestor - erythromycin, the differences appear only in the nature of the side chains and in the number of carbon atoms (14, 15 and 16). Side chains determine the activity against Pseudomonas aeruginosa. The basis of the chemical structure of macrolides is the macrocyclic lactone ring.
Macrolides are classified according to the method of preparation and the chemical structural basis.
How to obtain
In the first case, they are divided into synthetic, natural and prodrugs (erythromycin esters, oleandomycin salts, etc.). Prodrugs have a modified structure compared to the drug, but in the body, under the influence of enzymes, they turn into the same active drug, which has a characteristic pharmacological effect.
Prodrugs have improved palatability, high rates bioavailability. They are acid resistant.
Chemical structural basis
The classification implies the division of macrolides into 3 groups:
* pr.- Natural.
** semi-synthetic.
It should be noted that azithromycin ® is an azalide, since its ring contains a nitrogen atom.
Features of the structure of each macro. affect the performance, drug interaction with other drugs, pharmacokinetic properties, tolerability, etc. The mechanisms of influence on microbiocenosis in the presented pharmacological agents are identical.
Group of antibiotics macrolides: a list of drugs
| № | Name and release form |
| 1 | Azivok ® - capsule form |
| 2 | Azimicin ® - tablet form |
| 3 | Azitral ® - capsule form |
| 4 | Azitrox ® - capsule form |
| 5 | Azithromycin ® - capsules, powders |
| 6 | AzitRus ® — capsule form, powder form, tablet form |
| 7 | Azicide ® - tablet form |
| 8 | Binoclair ® - tablet form |
| 9 | Brilid ® - tablet form |
| 10 | Vero-Azithromycin ® - capsule form |
| 11 | Vilprafen ® (Josamycin ®) - tablet form |
| 12 | Grunamycin syrup ® - granules |
| 13 | ZI-Factor ® - tablets, capsules |
| 14 | Zitrolide ® - capsule form |
| 15 | Ilozon ® - suspension |
| 16 | Klabaks ® - granules, tablets |
| 17 | Clarithromycin ® - capsules, tablets, powder |
| 18 | Clarithrosin ® - tablet form |
| 19 | Klacid ® - lyophilizate |
| 20 | Klacid ® - powder, tablets |
| 21 | Rovamycin ® - powder form, tablets |
| 22 | RoxyGEKSAL ® - tablet form |
| 23 | Roxid ® - tablet form |
| 24 | Roxilor ® - tablet form |
| 25 | Roksimizan ® - tablet form |
| 26 | Rulid ® - tablet form |
| 27 | Rulicin ® - tablet form |
| 28 | Seidon-Sanovel ® — tablet form, granules |
| 29 | SR-Claren ® - tablet form |
| 30 | Sumazid ® - capsules |
| 31 | Sumaklid ® - capsules |
| 32 | Sumamed ® - capsules, aerosols, powder |
| 33 | Sumamycin ® - capsules, tablets |
| 34 | Sumamox ® - capsules, tablet form |
| 35 | Sumatrolide solutab ® - tablet form |
| 36 | Fromilid ® - granules, tablet form |
| 37 | Hemomycin ® - capsules, tablets, lyophilisate, powder |
| 38 | Ecositrin ® - tablet form |
| 39 | Ecomed ® — tablet form, capsules, powder |
| 40 | Erythromycin ® - lyophilisate, eye ointment, ointment for external use, powder, tablets |
| 41 | Ermiced ® - liquid form |
| 42 | Esparoxy ® - tablet form |
Characteristics of each macrolide
Consider the main representatives of the group separately.
Erythromycin ®
Er. inhibits the growth of chlamydia, legionella, staphylococci, mycoplasmas and legionella, Pseudomonas aeruginosa, Klebsiella.
Bioavailability can reach sixty percent, it depends on meals. Absorbed in digestive tract partially.
Among the side effects noted: dyslepsy, dyspepsia, narrowing of one of the sections of the stomach (diagnosed in newborns), allergies, "shortness of breath syndrome."
Prescribed for diphtheria, vibriosis, infectious lesions skin, chlamydia, Pittsburgh pneumonia, etc. Treatment with erythromycin during pregnancy and lactation is excluded.
Roxithromycin ®
Inhibits the growth of microorganisms that produce an enzyme that breaks down beta-lactams, has an anti-inflammatory effect. R. is resistant to acids and alkalis. The bactericidal effect is achieved by increasing the dosage. The half-life is about ten hours. Bioavailability is fifty percent.
Roxithromycin ® is well tolerated and excreted unchanged from the body.
Prescribed for inflammation of the mucous membrane of the bronchi, larynx, paranasal sinuses, middle ear, palatine tonsils, gallbladder, urethra, vaginal segment of the cervix, infections of the skin, musculoskeletal system, brucellosis, etc.
Pregnancy, lactation and age up to two months are contraindications.
Clarithromycin ®
Inhibits the growth of aerobes and anaerobes. Observed low activity in relation to the Koch stick. superior to erythromycin in microbiological parameters. The drug is acid-resistant. Alkaline environment affects the achievement of antimicrobial action.
Clarithromycin ® is the most active macrolide against Helicobacter pylori, which infects various areas stomach, and 12 - duodenum. The half-life is about five hours. The bioavailability of the drug does not depend on food.
K. is prescribed for infection of wounds, infectious diseases ENT organs, purulent rashes, furunculosis, mycoplasmosis, mycobacteriosis against the background of the immunodeficiency virus.
Taking clarithromycin® for early dates pregnancy is prohibited. Infant age up to six months is also a contraindication.
Oleandomycin ®
Oleandomycin ® inhibits protein synthesis in pathogen cells. The bacteriostatic effect is enhanced in an alkaline environment.
To date, cases of the use of oleandomycin are rare, as it is outdated.
Ol. prescribed for brucellosis, abscess pneumonia, bronchiectasis, gonorrhea, inflammation meninges, the inner lining of the heart, infections of the upper respiratory tract, purulent pleurisy, furunculosis, the ingress of pathogenic microorganisms into the bloodstream.
Azithromycin ®
It is an azalide antibiotic, which differs in structure from classical macrolides. K - n inhibits gram +, gram-flora, aerobes, anaerobes and acts intracellularly.
The antibiotic demonstrates high rates of activity in relation to, Haemophilus influenzae, gonococcus. three hundred times more acid-resistant than erythromycin. Digestibility rates reach forty percent. Like all erythromycin antibiotics, azithromycin ® is well tolerated. A long half-life (more than 2 days) allows you to prescribe the drug once a day. The maximum course of treatment does not exceed five days.
Effective in the eradication of streptococcus, the treatment of lobar pneumonia, infectious lesions of the pelvic organs, the genitourinary system, tick-borne borreliosis, sexually transmitted diseases. During the period of bearing a child, it is prescribed according to vital indications.
Taking azithromycin ® by HIV-infected patients prevents the development of mycobacteriosis.
Josamycin ® (Vilprafen Solutab ®)
A natural antibiotic derived from the radiant fungus Streptomyces narbonensis. Bactericidal action is achieved at high concentrations in the focus of infection. J - n inhibits protein synthesis and inhibits the growth of pathogens.
Therapy with josamycin ® often leads to a decrease in blood pressure. The drug is actively used in otorhinolaryngology (tonsillitis, pharyngitis, otitis), pulmonology (bronchitis, ornithosis, pneumonia), dermatology (furunculosis, erysipelas, acne), urology (urethritis, prostatitis).
Approved for use during lactation, it is prescribed for the treatment of pregnant women. Newborns and children under fourteen years of age are shown a suspension form.
Midecamycin ® (Macropen ®)
Differs in high indicators of microbial activity and good pharmacokinetic properties. The bactericidal effect is achieved by a significant increase in the dose. The bacteriostatic effect is associated with the inhibition of protein synthesis.
Pharmacological action depends on the type of harmful microorganism, the concentration of the drug, the size of the inoculum, etc. Midecamycin ® is used for infectious lesions of the skin, subcutaneous tissue, respiratory tract.
Midecamycin ® is a reserve antibiotic and is prescribed for patients with hypersensitivity to beta-lactams. Actively used in pediatrics.
The period of lactation (penetrates into breast milk) and pregnancy are contraindications. Sometimes m-n is prescribed for vital indications and if the benefit to the mother outweighs the potential risk to the fetus.
Spiramycin ®
It differs from other macrolides in that it regulates the immune system. The bioavailability of the drug reaches forty percent.
The activity of the drug decreases in an acidic environment and increases in an alkaline one. Alkali contributes to an increase in penetrating ability: the antibiotic gets better inside the cells of pathogens.
It has been scientifically proven that spiramycin ® does not affect embryonic development, so it is acceptable to take it during childbearing. The antibiotic affects breast-feeding, therefore, during lactation, it is worth finding an alternative drug.
Macrolide antibiotics for children should not be administered by intravenous infusion.
Antibiotics of the macrolide group: drug names for children
In the treatment of macrolides, the occurrence of life-threatening drug reactions is excluded. NLR in children are manifested by pain in the abdomen, discomfort in the epigastrium, vomiting. Generally, children's body tolerates macrolide antibiotics well.
Drugs, invented relatively recently, practically do not stimulate the motility of the gastrointestinal tract. Dyspeptic manifestations as a result of the use of midecamycin ® , midecamycin acetate ® are not observed at all.
Special attention deserves clarithromycin ® , which is superior to other macrolides in many respects. As part of a randomized controlled trial, it was found that this antibiotic acts as an immunomodulator, having a stimulating effect on the protective functions of the body.
Macrolides are used for:
- treatment of atypical mycobacterial infections,
- hypersensitivity to β-lactams,
- diseases of bacterial origin.
They have become popular in pediatrics due to the possibility injection in which the drug bypasses the gastrointestinal tract. This becomes necessary in emergencies. A macrolide antibiotic is what the pediatrician most often prescribes when treating infections in young patients.
Adverse drug reactions
Therapy with macrolides rarely causes anatomical and functional changes, but the occurrence of side effects is not excluded.
Allergy
In the course of a scientific study, in which about 2 thousand people took part, it was found that the likelihood of anaphylactoid reactions when taking macrolides is minimal. No cases of cross-allergy have been reported. Allergic reactions are manifested in the form of nettle fever and exanthema. In rare cases, anaphylactic shock is possible.
gastrointestinal tract
Dyspeptic phenomena occur due to the prokinetic effect inherent in macrolides. Most patients report frequent defecation, pain in the abdomen, violation taste sensations, vomiting. Newborns develop pyloric stenosis, a disease in which the evacuation of food from the stomach into the small intestine is difficult.
The cardiovascular system
pirouette ventricular tachycardia, cardiac arrhythmia, long QT interval syndrome are the main manifestations of cardiotoxicity of this group of antibiotics. make things worse old age, heart disease, overdosing, fluid and electrolyte disturbances.
Structural and functional disorders of the liver
A long course of treatment, excess dosage are the main causes of hepatoxicity. Macrolides act differently on cytochrome, an enzyme involved in the metabolism of chemicals foreign to the body: erythromycin inhibits it, josamycin ® affects the enzyme a little less, and azithromycin ® does not have any effect at all.
CNS
Few doctors know when prescribing a macrolide antibiotic that this is a direct threat mental health person. Neuropsychiatric disorders most often occur when taking clarithromycin ® .
Video about the group in question:
History and development
Macrolides are a promising class of antibiotics. They were invented more than half a century ago, but are still actively used in medical practice. The uniqueness of the therapeutic effect of macrolides is due to 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 favorably distinguish macrolides against the background of β-lactams.
Erythromycin ® marked the beginning of the macrolide class.
The first acquaintance with erythromycin occurred in 1952. Portfolio of the latest pharmaceuticals joined the international American innovative company "Eli Lilly & Company ®" (Eli Lilly & Company ®). Her scientists derived erythromycin from a radiant fungus that lives in the soil. Erythromycin has become an excellent alternative for patients with hypersensitivity to penicillin antibiotics.
Expansion of the scope, development and introduction into the clinic of macrolides, modernized in terms of microbiological indicators, dates back to the seventies and eighties.
The erythromycin series is different:
- high activity against Streptococcus and Staphylococcus and intracellular microorganisms;
- low rates of toxicity;
- no cross-allergy with beta-lactam antibiotics;
- creating high and stable concentrations in tissues.
On our site you can get acquainted with most groups of antibiotics, complete lists of the drugs included in them, classifications, history and other important information. For this, a section "" has been created in the top menu of the site.
Most antibiotics, while suppressing the development of infectious agents, simultaneously have a negative impact on the internal microbiocenosis of the human body, but, unfortunately, a number of diseases cannot be cured without the use of antibacterial agents.
The best way out of the situation is the preparations of the macrolide group, which occupy a leading position in the list of the safest antimicrobial drugs.
History reference
The first representative of the class of antibiotics under consideration was Erythromycin, obtained from soil bacteria in the middle of the last century. As a result of research activities, it was found that the basis of the chemical structure of the drug is a lactone macrocyclic ring, to which carbon atoms are attached; this feature determined the name of the entire group.
The new tool almost immediately gained wide popularity; 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 Spiramycin.
The development of the next generations of antibiotics of this series was due to the discovery of the activity of early drugs of the group against campylobacter, chlamydia and mycoplasmas.
Today, almost 70 years after their discovery, Erythromycin and Spiramycin are still present in therapeutic regimens. In modern medicine, the first of these drugs is more often used as the drug of choice in the presence of in patients with individual intolerance to penicillins, the second - as a highly effective agent, characterized by a long-term antibacterial effect and the absence of teratogenic effects.
Oleandomycin is used much less often: many experts consider this antibiotic to be outdated.
There are currently three generations of macrolides; drug research is ongoing.
Systematization principles
The classification of drugs included in the described group of antibiotics is based on the chemical structure, method of preparation, duration of exposure and generation of the drug.
Details of the distribution of drugs - in the table below.
This classification should be supplemented with three points:
The list of group drugs includes Tacrolimus, a drug that has 23 atoms in the structure and simultaneously belongs to immunosuppressants and to the series under consideration.
The structure of Azithromycin includes a nitrogen atom, so the drug is azalide.
Macrolide antibiotics are of both natural and semi-synthetic origin.
Natural, in addition to the medicines already indicated in the historical reference, include Midecamycin and Josamycin; artificially synthesized - Azithromycin, Clarithromycin, Roxithromycin, etc. Prodrugs with a slightly modified structure stand out from the general group:
- esters of Erythromycin and Oleandomycin, their salts (propionyl, troleandomycin, phosphate, hydrochloride);
- ester salts of the first representative of a number of macrolides (estolate, acistrat);
- Midecamycin salts (Myokamicin).
general description
All drugs under consideration have a bacteriostatic type of action: they inhibit the growth of colonies of infectious agents by disrupting protein synthesis in pathogen cells. In some cases, clinic specialists prescribe an increased dosage of medications to patients: the drugs involved in this way acquire a bactericidal effect.
Antibiotics of the macrolide group are characterized by:
- a wide range of effects on pathogens (including drug-sensitive microorganisms - pneumococci and streptococci, listeria and spirochetes, ureaplasma and a number of other pathogens);
- minimal toxicity;
- high activity.
As a rule, the drugs in question are used in the treatment of genital infections (syphilis, chlamydia), diseases of the oral cavity with bacterial etiology (periodontitis, periostitis), diseases of the respiratory system (whooping cough, bronchitis, sinusitis).
The effectiveness of medicines related to macrolides has also been proven in the fight against folliculitis and furunculosis. In addition, antibiotics are prescribed for:
- gastroenteritis;
- cryptosporidiosis;
- atypical pneumonia;
- acne (severe course of the disease).
For the purpose of prevention, a group of macrolides is used to sanitize carriers of meningococcus, during surgical procedures in the lower intestine.
Macrolides - drugs, their characteristics, a list of the most popular forms of release
Modern medicine actively uses Erythromycin, Clarithromycin, Iloson, Spiramycin and a number of other representatives of the considered group of antibiotics in therapy regimens. The main forms of their release are shown in the table below.
| Drug names | Packing type | |||
| Capsules, tablets | Granules | Suspension | Powder | |
| Azivok | + | |||
| + | + | |||
| Josamycin | + | |||
| Zitrolide | + | |||
| Ilozon | + | + | + | + |
| + | + | + | ||
| + | + | |||
| Rovamycin | + | + | ||
| Rulid | + | |||
| Sumamed | + | + | ||
| Hemomycin | + | + | ||
| Ecomed | + | + | ||
| + | + | |||
Pharmacy chains also offer consumers Sumamed in the form of an aerosol, lyophilizate for infusions, Hemomycin - in the form of a powder for the preparation of injection solutions. Erythromycin-liniment is packed in aluminum tubes. Ilozon is available in the form of rectal suppositories.
A brief description of popular tools is in the material below.
Resistant to alkalis, acids. It is prescribed mainly for diseases of the ENT organs, the genitourinary system, and the skin.
It is contraindicated in pregnant and lactating women, as well as in small patients under the age of 2 months. The half-life is 10 hours.
Under the strict supervision of a doctor, it is allowed to use the medication in the treatment of pregnant women (in difficult cases). The bioavailability of the antibiotic is directly dependent on food intake, so the drug should be drunk before meals. Among the side effects are allergic reactions, disruption of the functioning of the gastrointestinal tract (including diarrhea).
Another name for the drug is Midecamycin.
It is used when the patient has an individual intolerance to beta-lactams. It is prescribed to suppress the symptoms of ailments that affect the skin, respiratory organs.
Contraindications - pregnancy, the period of breastfeeding. Involved in pediatrics.
Josamycin
It is used in the treatment of pregnant, lactating women. In pediatrics, it is used in the form of a suspension. May lower the patient's blood pressure. It is taken regardless of the time of eating.
Stops the symptoms of diseases such as tonsillitis, bronchitis, furunculosis, urethritis, etc.
It is characterized by increased activity against pathogens that cause inflammation in the gastrointestinal tract (among them Helicobacter pylori).
Bioavailability does not depend on the time of eating. Among the contraindications are the first trimester of pregnancy, infancy. The half-life is short, less than five hours.
Oleandomycin
The effect of the use of the drug increases when it enters the alkaline environment.
Activated when:
- bronchiectasis;
- purulent pleurisy;
- brucellosis;
- diseases of the upper respiratory tract.
New generation drug. Acid resistant.
The structure of the antibiotic differs from most medicines belonging to the described group. When involved in the treatment of HIV-infected patients, it prevents mycobacteriosis.
The half-life is more than 48 hours; this feature reduces the use of the drug to 1 r./day.
Ilozon
Incompatible with Clindamycin, Lincomycin, Chloramphenicol; reduces the effectiveness of beta-lactams and hormonal contraceptives. In severe cases of the disease, it is administered intravenously. It is not used during pregnancy, hypersensitivity to the components of the drug, during lactation.
It is characterized by the ability to regulate the immune system. Does not affect the fetus during the gestation period, is involved in the treatment of pregnant women.
Safe for children (the dosage is determined by the doctor, taking into account the weight, age of the patient and the severity of his disease). Does not undergo cellular metabolism, does not break down in the liver.
Zatrin, Lincomycin, Clindamycin, Sumamed
Low-toxic macrolides of the latest generation. They are actively used in the treatment of adults and small (from 6 months) patients, since they do not have a significant negative effect on the body. They are characterized by the presence of a long half-life, as a result of which they are used no more than 1 time for 24 hours.
Macrolides of the new generation have practically no contraindications, are well tolerated by patients when involved in therapeutic regimens. The duration of treatment with these drugs should not exceed 5 days.
Application features
It is impossible to use macrolides in the treatment of diseases on their own.
It should be remembered: to use antibiotics without first consulting a doctor means to be irresponsible about your health.
Most of the drugs in the group are characterized by slight toxicity, but the information contained in the instructions for the use of macrolide medications should not be ignored. According to the annotation, when using drugs, you may experience:
If there is an individual intolerance to macrolides in the patient's history, it is impossible to use medical products of this series in the treatment.
Forbidden:
- drink alcohol during treatment;
- increase or decrease the prescribed dosage;
- skip taking pills (capsules, suspensions);
- stop taking without retesting;
- use medicines that have expired.
In the absence of improvement, the appearance of new symptoms should immediately contact your doctor.
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