New macrolide preparations. Macrolide antibiotics for children. Mechanism of action and list of drugs

Distinctive feature Klacida is its activity against a wide range of microbes, including atypical pathogenic bacteria that cause infectious and inflammatory diseases. respiratory tract. In addition, the antibiotic is highly effective in the treatment of acute otitis media, acute bronchitis, pneumonia, pharyngitis or tonsillitis in children.

Varieties, names, composition and forms of release

• Klacid;
• Klacid SR.

Klacid SR is available in a single dosage form - these are tablets of prolonged (long-term) action, and Klacid - in three dosage forms, such as:

• Lyophilisate for solution for infusion;
• Powder for suspension for oral administration;
• Tablets.

In everyday life, various dosage forms, varieties and dosages of Klacid are called short and capacious names, reflecting their main characteristics. So, tablets are often called Klacid 250 or Klacid 500, where the number next to the name reflects the dosage of the drug. Suspension, taking into account the same principle, is called Klacid 125 or Klacid 250, etc.

Tablets of both dosages Klacid and prolonged action Klacid SR have the same biconvex, oval shape and are covered with a yellow-colored shell. Tablets are available in packs of 7, 10, 14, 21 and 42 pieces.

Powder for suspension for oral administration is a small granules, painted white or almost white in color and having a fruity odor. The powder is available in 42.3 g vials, complete with dosing spoon and syringe. When the powder is dissolved in water, an opaque suspension is formed, colored white and having a fruity aroma.

Lyophilisate for solution for infusion is available in hermetically sealed vials and is a white powder with a slight aroma.

Therapeutic action of Klacid

Klacid has a wide spectrum of action and harmful to the following types of microorganisms:

• Chlamydia pneumoniae (TWAR);
• Chlamydia trachomatis;
• Enterobacteriaceae and Pseudomonas;
• haemophilus influenzae;
• Haemophilus parainfluenzae;
• Helicobacter (Campilobacter) pylori;
• Legionella pneumophila;
• Listeria monocytogenes;
• Moraxella catarrhalis;
• Mycobacterium leprae;
• Mycobacterium kansasii;
• Mycobacterium chelonae;
• Mycobacterium fortuitum;
• Mycobacterium avium complex (MAC) - a complex including: Mycobacterium avium, Mycobacterium intracellulare;
• Mycoplasma pneumoniae;
• Neisseria gonorrheae;
• Staphylococcus aureus;
• Streptococcus pneumoniae;
• Streptococcus pyogenes.

With regard to the following microorganisms, it is detrimental the action of Klacid is shown only during laboratory tests, but not confirmed by clinical practice:

• Bacteroides melaninogenicus;
• Bordetella pertussis;
• Borrelia burgdorferi;
• Campylobacter jejuni;
• Clostridium perfringens;
• Pasteurella multocida;
• Peptococcus niger;
• Propionibacterium acnes;
• Streptococcus agalactiae;
• Streptococci (groups C, F, G);
• Treponema pallidum;
• Viridans group streptococci.

Indications for use

• Lower site infections respiratory system(bronchitis, pneumonia, bronchiolitis, etc.);
• infections upper divisions respiratory system (pharyngitis, tonsillitis, sinusitis, otitis, etc.);
• Infections of the skin and soft tissues (folliculitis, erysipelas, infectious cellulitis, furunculosis, impetigo, wound infection etc.);
• Infections caused by mycobacteria;
• Prevention of infection caused by the Mycobacterium avium complex (MAC) in HIV-infected people;
• Eradication of H. pylori to cure gastritis and peptic ulcer of the stomach or twelve duodenal ulcer;
• Treatment and reduction in the frequency of recurrence of duodenal ulcers;
• Infections of the teeth and oral cavity (tooth granuloma, stomatitis, etc.);
• Infections caused by Chlamydia trachomatis, Ureaplasma urealyticum (urethritis, colpitis, etc.).

The drug is effective against many microorganisms - gram-negative (meningococci, gonococci, Haemophilus influenzae, Helicobacter pylori, etc.) and gram-positive (staphylococci, streptococci, pneumococci, corynebacterium diphtheria, etc.). It is also prescribed to fight intracellular microorganisms (chlamydia, mycoplasma, ureaplasma, etc.), as well as some anaerobic bacteria(Peptococci, Peptostreptococci, Bacteroids and Clostridia).

Vilprafen is rapidly absorbed from the digestive tract. Within an hour, its maximum concentration in the blood is reached. At the same time, Vilprafen has a long-term therapeutic effect.

The drug crosses the placental barrier and can be excreted in breast milk.

The drug is inactive against enterobacteria, therefore, it practically does not affect the intestinal microflora.

80% of Vilprafen is excreted in the bile, 20% in the urine.

Macrolides are not only safe, but also quite effective. They are inherent huge potential antimicrobial activity, as well as excellent pharmacokinetic action, which makes it much easier to transfer their effects into childhood. The very first macrolide antibiotic was erythromycin. After another 3 years, two more drugs were released - spiramycin and oleandomycin. To date, there are the best antibiotics of this group for children in the face azithromycin, roxithromycin, clarithromycin, spiramycin and some others. It is these antibiotic drugs that are used by modern pediatricians to fight infections in children.

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Erythromycin is an antibiotic that should be taken for legionellosis, in order to prevent acute rheumatic fever (if penicillin is not possible), intestinal decontamination before colorectal surgery.

Clarithromycin is used for the treatment and prevention of opportunistic infections in AIDS caused by some atypical mycobacteria, including for eradication Helicobacter pylori in diseases of the gastrointestinal tract.

Spiramycin is used to treat toxoplasmosis, particularly in pregnant women.

Josamycin is suitable for the treatment of various respiratory diseases, soft tissue infections, odontogenic infections.
The use of josamycin during pregnancy and during breastfeeding is allowed if indicated. The WHO European Office recommends josamycin for the correct treatment of chlamydial infection in women who are expecting a child.

All macrolides are allowed to be taken orally.

The advantages in the direction of clarithromycin, spiramycin, roxithromycin, midecamycin and josamycin over erythromycin are better pharmacokinetics, better tolerance and less frequency of use.

Contraindications to the use of macrolides are hypersensitivity, pregnancy (josamycin, roxithromycin, midecamycin, clarithromycin), breastfeeding (josamycin, spiramycin, clarithromycin, midecamycin, roxithromycin).

Macrolides pass through the placenta and are absorbed into breast milk.

Side effects. These drugs are well tolerated and are one of the most harmless groups of antimicrobial drugs.

This group of macrolides is natural antibiotics(oleandomycin, erythromycin, spiramycin, etc.), as well as semi-synthetic drugs (azithromycin, roxithromycin, clarithromycin, etc.).
The base of the chemical structure of these drugs is the lactone ring, which consists of 14-16 carbon atoms in various antibiotics. A variety of substituents are attached to lactone rings, which strongly affect the quality of individual compounds.

The main feature of semi-synthetic macrolides has become high-quality pharmacokinetic properties with increased (wide spectrum) antibacterial activity. They are well absorbed and form a long-lasting high concentration in the blood and tissues, which helps to reduce the number of injections per day to one or two times, reduce the duration of the course, the frequency and severity of side effects. They are effective in respiratory tract infections, diseases of the genital organs and urinary tract, soft tissues, skin and other diseases that have arisen due to gram-negative and gram-positive microorganisms, atypical bacteria, and various anaerobes.
penicillin. A distinctive feature of these antibiotics was that various gram-positive microorganisms that were not subject to penicillin, tetracycline, etc. became sensitive to them. It is not for nothing that macrolides in the clinical field have received the place of “reserve” antibiotics. The emergence of new generations of these drugs has only strengthened the position of this pharmacological group antibacterial drugs. But, nevertheless, it did not speak of complete failure from the use of erythromycin, well known in the clinical setting. In fact, erythromycin is still usable for a large number types of microorganisms.

However, the antimicrobial activity of erythromycin in vitro is high. Do not ignore the bioavailability of the antibiotic, which is not so great compared to the new macrolides / azalides, high opportunity undesirable effects, as well as the formation of resistant microorganisms.

Of particular importance is the choice of macrolide antibiotics, taking into account the pathogen, the characteristics of clinical manifestations and the course of the disease.

A necessary feature of these first generation drugs was the lack of effectiveness against gram-negative bacteria, including fungi, brucella, nocardia. New generations of these drugs are more effective in the fight against gram-negative microorganisms and are constantly attracting attention.

Macrolides are some kind of lactones, in which the number of atoms in the cycle is eight or more; they can include various substituents, namely functional groups, including 1 or 2 C=C bonds. They exist with 2 or more lactone groups. These are, as a rule, solid substances that dissolve quite well in organic solutions and solvents, but are poorly soluble in water. In terms of their chemical qualities, they are similar to lower lactones, but they do not have such a strong reactivity.

Most macrolides are produced by strains of bacteria, mainly actinomycetes and streptomycetes. Of these substances, oleandomycin, erythromycin, tetranactin and rosamycin are better known.
From culture filtrates, such macrolides are obtained by extraction of organic solvents and purified by chromatographic methods. There are also similar substances that are obtained through bacteria, after which they are converted biochemically or chemically, for example, triacetyloleandomycin. By chemical means, as a rule, synthesize unsubstituted macrolides. They can be made by lactonization of w-halo acids or various esters of hydroxy acids.

The chemical synthesis of these substances, similar to that produced by bacteria, is very difficult. It includes obtaining a hydroxy acid, which has some substituents, and its direct lactonization. Thus, tylosin and some derivatives of erythromycin were synthesized. Macrolide antibiotics stop the growth of gram-positive penicillin allergy to penicillin, legionella and rickettsial infections. At community-acquired pneumonia macrolides can become first aid antibiotics.

Lincomycin (not a macrolide) has bacteriostatic properties that are similar to those of erythromycin.

Tetracyclines are now used mainly in the treatment of patients with atypical pneumonia due to the formation of microbial resistance to them. Tetracyclines affect bacterial ribosomes by stopping bacterial protein synthesis. Doxycycline properly enters the lungs (alveolar macrophages), leukocytes and is therefore suitable in the fight against intracellular pathogens (eg Legionella).

The presence of toxicity in tetracyclines becomes a great difficulty. Thus, tetracyclines often provoke the appearance of gastrointestinal diseases in patients, affect the appearance of candidiasis and liver and kidney damage, mainly in the elderly. It is not correct to start therapy of patients with ambulatory pneumonia with tetracyclines.

Geriatrics. There are no prohibitions for the use of macrolides for the elderly, but one should remember the fact that age-related changes in liver function are likely, as well as high risk hearing loss with erythromycin.

Impaired kidney function. With a decrease in creatinine clearance less than 30 ml / min, the half-life of clarithromycin can rise to twenty hours, and its active metabolite - up to forty hours. The half-life of roxithromycin can increase to fifteen hours with a decrease in creatinine clearance to 10 ml / min. In such cases, it may be necessary to change the dosing regimen of such macrolides.

Many believe that antibiotics should be used only in extreme cases. However, this is not an entirely correct opinion, since the list of such drugs is replenished with drugs that are relatively safe - macrolides. Such antibiotics, basically, without having a negative impact on the human body, are able to overcome the infection “in no time”. The safe profile allows prescribing macrolides to patients undergoing outpatient and inpatient treatment, as well as children aged 6 months (under medical supervision).

Few people know about the properties, origin and effect of such "harmless" remedies. And if you want to get acquainted with such drugs and find out in more detail what a macrolide antibiotic is, we suggest reading our article.

It should be noted right away that macrolides belong to the group of antibiotic drugs that are the least toxic to the human body and are well tolerated by patients.

Antibiotics such as macrolides, from the point of view of biochemistry, are complex compounds of natural origin, which consist of carbon atoms, which in different amount are in the macrocyclic lactone ring.

If we take this criterion, which is responsible for the number of carbon atoms, as the basis for the classification of drugs, then we can divide all such antimicrobial agents into:

Erythromycin, an antibiotic of the macrolide group, was one of the first to be discovered, in 1952. New generation drugs appeared a little later, in the 70s. Since they showed excellent results in the fight against infections, studies of this group medicines actively continued, thanks to which we currently have a fairly extensive list of drugs that can be used to treat both adults and children.

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Mechanism of action and scope

The antimicrobial effect is achieved by affecting the ribosomes of microbial cells, disrupting protein synthesis. Of course, under such an attack of macrolides, the infection weakens and “surrenders”. In addition, antibiotics of this group of drugs are able to regulate immunity, providing immunomodulatory activity. Also, these drugs have anti-inflammatory properties, affecting both the body of adults and children, quite moderately.

Group Tools antibacterial agents new generation are able to cope with atypical microbacteria, gram-positive cocci and similar misfortunes, which often become the causative agents of diseases such as bronchitis, whooping cough, diphtheria, pneumonia, etc.

No less popular are macrolides in the situation that has developed over the past few years, due to addiction. a large number microbes to antibiotics (resistance). This is due to the fact that new generation drugs belonging to this group are able to maintain their activity against a variety of pathogens.

In particular, macrolide preparations are widely used in the treatment and as prophylactic from the following diseases:

• Chronical bronchitis;
• acute sinusitis;
• periostitis;
• periodontitis;
• rheumatism;
• endocarditis;
• gastroenteritis;
• severe forms of toxoplasmosis, acne, mycobacteriosis.

The list of diseases that can be overcome using new generation antibiotics, which have a common name - macrolides, can be supplemented by sexually transmitted infections - syphilis, chlamydia and infections that affect soft tissues and skin - furunculosis, folliculitis, paronychia.

Contraindications for use

If your doctor prescribes a similar antibiotic for you, immediately read its contraindications indicated in the instructions for the drug. Unlike most conventional antibiotics, new generation drugs - macrolides are safe, including for children, and less toxic. Therefore the list unwanted effects the antibiotics of this group are not as large as those of similar drugs.

First of all, it is not recommended to use macrolides for pregnant women and mothers during lactation. The use of such drugs in children under 6 months is contraindicated, since the reaction to the drug has not yet been studied. You should not use such drugs as a treatment for people who have individual sensitivity.

macrolide antibiotics with special attention should be prescribed by physicians to patients middle age. This is due to the fact that most of the older generation have disorders in the functioning of the kidneys, liver and heart.

Side effects may also occur with the use of macrolides in mild form- weakness and malaise, manifested after their intake. But there may also be:

• vomit;
• nausea;
• headache and pain in the abdomen;
• impaired vision, hearing;
• an allergic reaction in the form of a rash, urticaria (most often occurs in children).

In order to avoid problems and undesirable consequences after the use of drugs of the macrolide group, it is necessary to strictly follow the doctor's recommendations, strictly observe the dosage and refrain from drinking alcohol. It is also strictly forbidden to combine the intake of new generation antibiotics with antacids. It is also important not to skip appointments.

Basically, new generation antibiotics should be taken 1 hour before a meal, or 2 hours after a meal. Take the tablets with a whole glass of water. If the doctor has prescribed you an antibiotic of the macrolide group, the release form of which is a powder for the preparation of a suspension, strictly follow the instructions for preparing the medicine and strictly follow the doctor's instructions.

Application and appointment to children

In the fight against bacterial and other diseases that have arisen in children, the first place today is occupied by antibiotics - macrolides. This is one of the few groups of drugs that have earned the respect of specialists and are boldly used in pediatrics. The advantage of such medications, unlike other similar ones, is that they practically do not cause allergic reactions in young patients. In particular, this applies to drugs that have names - "Penicillin" and "Cefalosporin".

Despite the fact that macrolides are safe for children, they have enough effective action. Their impact in a mild form on children's body provide pharmacokinetic properties inherent in drugs. Some of the most popular means that represent the macrolide group are:

• Clarithromycin;
• Roxithromycin;
• Spiramycin etc.

The dosage of the use of such drugs for children depends on the type of disease and the weight of the child. Therefore, try to follow the doctor's recommendations. In general, the produced forms of such funds are very convenient to use. Some of them are in the form of ointments for external use, and are also intended for parenteral use of the form, which, in turn, is relevant for children in emergency situations.

Summing up, we can safely say that macrolides, like antibiotics, are “white and fluffy”. Virtually non-exciting side effects and undesirable consequences, these new generation drugs have found their acceptance among many doctors and specialists. Effective, and able to cope even with severe forms of diseases, such antibiotics are used even in the treatment of children.

Antibiotics are the waste products (of natural or synthetic origin) of viral, bacterial or fungal cells that can inhibit the growth and reproduction of other cells or microorganisms. Drugs may have antibacterial, anthelmintic, antifungal, antiviral and antitumor activity. They are divided into groups depending on the chemical structure.

Macrolide antibiotics are relatively safe representatives of antimicrobial agents. They look like complex compounds consisting of carbon atoms that are attached in various ways to the macrocyclic lactone ring. The drugs are well tolerated by patients.

Classification

The macrolide group has several divisions:

1. Depending on the number of attached carbon atoms:
   • preparations having 14 carbon atoms (for example, Erythromycin, Clarithromycin, Oleandomycin);
   • means with 15 carbon atoms ();
   • macrolides with 16 carbons attached (eg Josamycin, Spiramycin, Roxithromycin);
   • 23 atoms - belong to the only drug (Tacrolimus), which simultaneously belongs to the list of macrolide drugs and immunosuppressants.
2. According to the method of obtaining antibiotics: natural and synthetic origin.
3. Effect duration:
   • short-acting (Erythromycin, Spiramycin, Oleandomycin, Roxithromycin);
   • average duration (Clarithromycin, Josamycin, Flurithromycin);
   • "Long" drugs (Azithromycin, Dirithromycin).
4. Depending on the generation of drugs:
   • means of the 1st generation;
   • macrolides of the 2nd generation;
   • 3rd generation antibiotics (macrolides latest generation);
   • ketolides - means, chemical structure which consists of a traditional ring with the addition of a keto group.

The effectiveness of drugs

Antibiotics of this group, especially new generation macrolides, have a wide spectrum of action. They are used to control gram-positive microorganisms ( and ). On the present stage there is a decrease in the sensitivity of pneumococci and some types of streptococci to antibiotics having 14 and 15 carbon atoms in the composition, however, 16-membered preparations retain their activity against these bacteria.

The drugs are effective against the following pathogens:

• some strains of Mycobacterium tuberculosis;
• gardnerella;
• chlamydia;
• pathogen;
• mycoplasma;
• bacillus that causes the development of hemophilic infection.

Mechanism of action and benefits

Macrolides are tissue preparations, since their use is accompanied by the fact that the concentration of active substances in soft tissues is much higher than in the bloodstream. This is due to the ability of the substance to penetrate into the middle of the cells. The drugs bind to plasma proteins, but the degree of such action varies from 20 to 90% (depending on the antibiotic).

The mechanism of action is due to the fact that macrolides inhibit the process of protein production by microbial cells, disrupt the functionality of their ribosomes. In addition, they have a predominantly bacteriostatic effect, that is, they inhibit growth and reproduction. pathogenic microorganisms. The drugs have low toxicity, do not cause the development allergic reaction when combined with other groups of antibiotics.

Additional benefits of the latest generation products:

• long half-life of drugs from the body;
• transportation to the site of infection with the help of leukocyte cells;
• no need for a long course of treatment and frequent use drugs;
• absence toxic effect on the digestive system;
• when using tablet forms, absorption from the gastrointestinal tract is more than 75%.

Macrolides in ENT practice

The drugs act on a wide range of pathogens of ENT diseases. Antibiotics are recommended for the treatment of bacterial tonsillitis, acute inflammation middle ear and paranasal sinuses as well as bronchitis and pneumonia.
Macrolides are not used in the treatment of inflammation of the epiglottis and abscess of the pharynx.

Azithromycin has found the greatest prevalence in the treatment of the upper respiratory tract. The results of the studies confirmed the effectiveness of the drug in children with mild and medium degree severity of inflammatory processes. Clinical manifestations The effectiveness of treatment consists in the normalization of body temperature, the elimination of leukocytosis, and the subjective improvement in the condition of patients.

Reasons for choosing macrolides in otorhinolaryngology

Doctors prioritize this group of antibiotics based on the following points:

1. Sensitization to penicillins. In patients with rhinosinusitis or otitis media allergic rhinitis or bronchial asthma penicillin preparations, which are put in the first place, cannot be used because of the allergenic properties. They are replaced by macrolides.
2. The group has an anti-inflammatory effect and a wide range actions.
3. The presence of infections caused by atypical bacteria. Against such pathogens, causing development some types of tonsillopharyngitis, chronic adenoiditis, nasal pathologies, macrolides are effective.
4. A number of microorganisms can form specific films under which pathogens “live”, causing the development chronic processes ENT organs. Macrolides are able to act on pathological cells during their stay under such films.

Contraindications

Macrolides are considered relatively safe drugs, which can be prescribed for the treatment of children, but even they have some contraindications for use. It is undesirable to use the funds of this group during pregnancy and lactation. The use of macrolides in children under 6 months of age is not recommended.

Means are not prescribed in the presence of individual hypersensitivity to active components, with severe pathologies liver and kidneys.

Side effects

Adverse reactions develop infrequently. There may be attacks of nausea and vomiting, diarrhea, abdominal pain. At negative impact on the liver, the patient complains of an increase in body temperature, yellowing skin and sclera, weakness, dyspeptic manifestations.

From the side of the central nervous system, cephalgia can be observed, slight dizziness, job change auditory analyzer. Local reactions can develop with parenteral administration of drugs (inflammation of the veins with the formation of blood clots in them).

Group representatives

Most macrolides should be taken an hour before a meal or a few hours after it, because when interacting with food, the activity of the drugs decreases. Liquid dosage forms are taken according to the scheme prescribed by the attending physician.

Be sure to observe even intervals between doses of antibiotics. If the patient missed a dose, the medicine should be taken as soon as possible. Doubling the dosage of the drug at the time of the next dose is prohibited. During the period of treatment, you should definitely stop drinking alcohol.

Erythromycin

Produced in the form of oral forms, suppository, powder for injection. This representative can be used during pregnancy and lactation, but under the strict supervision of the attending physician. For the treatment of newborns, it is not prescribed because of the possibility of developing a narrowing of the output section of the stomach (pyloric stenosis).

Roxithromycin

Produced in the form of tablets. The spectrum of activity is similar to the previous representative of the group. Its analogues are Rulid, Roxithromycin Lek. Differences from Erythromycin:

• the percentage of the drug entering the blood is higher, does not depend on the intake of food in the body;
• longer withdrawal period;
• better tolerability of the drug by patients;
• interacts well with drugs of other groups.

It is prescribed to combat inflammation of the tonsils, larynx, paranasal sinuses of a streptococcal nature, infection caused by mycoplasmas and chlamydia.

Clarithromycin

Available in tablets and powders for injection. Analogues - Fromilid, Klacid. Clarithromycin has a high bioavailability and is well tolerated by patients. Not used for the treatment of newborns, pregnant and lactating mothers. The drug is effective against atypical microorganisms.

Azithromycin (Sumamed)

Macrolide belonging to the class of antibiotics with 15 carbon atoms. Available in the form of tablets, capsules, powders for injection and syrup. Differs from Erythromycin in a large percentage of entry into the bloodstream, less dependence on food, long-term preservation therapeutic effect after the end of therapy.

Spiramycin

Antibiotic of natural origin, having 16 carbon atoms in the composition. Effective in the fight against pneumonia pathogens that are resistant to other representatives of macrolides. It can be prescribed for the treatment of women during the period of bearing a child. Introduced orally or into a vein drip.

The active substance is midecamycin. Macrolide of natural origin, acting on those staphylococci and pneumococci that are resistant to other drugs. The agent is well absorbed from the intestinal tract and interacts well with representatives of other groups of medicines.

Josamycin

It has a slightly different spectrum of action than Erythromycin. Josamycin fights those microorganisms that are resistant to a number of macrolides, but is not able to suppress the reproduction of a number of erythromycin-sensitive bacteria. Available in the form of tablets and suspensions.

Conditions for prescribing drugs

For macrolide treatment to be effective, a number of rules must be observed:

1. staging accurate diagnosis, which allows you to clarify the presence of local or general inflammation in the body.
2. Determination of the causative agent of pathology using bacteriological and serological diagnostics.
3. Choice required drug based on antibiogram, localization inflammatory process and the severity of the disease.
4. The choice of the dosage of the drug, the frequency of administration, the duration of the course of treatment based on the characteristics of the drug.
5. The appointment of macrolides with a narrow spectrum of action for relatively mild infections and with a wide spectrum for severe diseases.
6. Monitoring the effectiveness of therapy.

The list of drugs is quite wide. Only a qualified specialist can select necessary remedy, which will be most effective for each specific clinical case.

Macrolides are antibiotics natural origin having a complex structure and having a bacteriostatic effect. Inhibition of the growth of 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 activity indicators, drug interactions with other drugs, pharmacokinetic properties, tolerability, etc. Mechanisms of influence on microbiocenosis in the presented pharmacological agents are identical.

Group of antibiotics macrolides: a list of drugs

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 from the body unchanged.

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 of the upper respiratory tract, 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 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, inner lining of the heart, upper respiratory tract infections, purulent pleurisy, furunculosis, the entry 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 appointed 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 skin lesions, 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 acidic environment and increases in alkaline. 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. NLR in children are manifested by pain in the abdomen, discomfort in the epigastrium, vomiting. In general, the 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 revealed that this antibiotic acts as an immunomodulator, stimulating protective functions organism.

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 of injection, in which the drug bypasses the gastrointestinal tract. It becomes necessary in emergency cases. 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 note frequent bowel movements, pain in the abdomen, impaired 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. The situation is aggravated by advanced age, heart disease, overdose, water and electrolyte disorders.

Structural and functional disorders of the liver

A long course of treatment, excess dosage are the main causes of hepatoxicity. Macrolides have different effects on cytochrome, an enzyme involved in the metabolism of foreign to the body chemical substances: 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 macrolide antibiotic that this is a direct threat to human mental health. 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 macrolides therapeutic effect 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 replenished the international American innovative company Eli Lilly and 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.

Macrolides are antibiotics of natural origin, having a complex structure and bacteriostatic action. Inhibition of the growth of 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.

Macrolides are classified according to the method of preparation and the chemical structural basis.

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 and high bioavailability. They are acid resistant.

The classification implies the division of macrolides into 3 groups:

* ex. - Natural.
*pol.- Semi-synthetic.

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

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

Consider the main representatives of the group separately.

Er. inhibits the growth of chlamydia, legionella, staphylococci, mycoplasmas and legionella, Pseudomonas aeruginosa, Klebsiella.
Bioavailability can reach sixty percent, it depends on meals. Partially absorbed in the digestive tract.

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 skin lesions, chlamydia, Pittsburgh pneumonia, etc.
Treatment with erythromycin during pregnancy and lactation is excluded.

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.

Inhibits the growth of aerobes and anaerobes. There is low activity in relation to the Koch stick. Clarithromycin is 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 of the stomach and 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 of the upper respiratory tract, purulent rashes, furunculosis, mycoplasmosis, mycobacteriosis against the background of the immunodeficiency virus.
Clarithromycin should not be taken in early pregnancy. Infant age up to six months is also a contraindication.

Ol. 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 of the meninges, the inner lining of the heart, infections of the upper respiratory tract, purulent pleurisy, furunculosis, the ingress of pathogenic microorganisms into the bloodstream.

The antibiotic demonstrates high rates of activity against Helicobacter pylori, Haemophilus influenzae, gonococcus. Azithromycin is 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.

It is effective in the eradication of streptococcus, the treatment of lobar pneumonia, infectious lesions of the pelvic organs, the genitourinary system, tick-borne borreliosis, and sexually transmitted diseases. During the period of bearing a child, it is prescribed according to vital indications.
The intake of azithromycin by HIV-infected patients can prevent the development of mycobacteriosis.

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.

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, and 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.

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 permissible to take it during childbearing. The antibiotic affects breastfeeding, so during lactation it is worth finding an alternative drug.

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

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. In general, the 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.

Clirithromycin deserves special attention, surpassing 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 of 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.

Therapy with macrolides rarely causes anatomical and functional changes, but the occurrence of side effects is not excluded.

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.

Dyspeptic phenomena occur due to the prokinetic effect inherent in macrolides. Most patients note frequent bowel movements, pain in the abdomen, impaired taste sensations, and vomiting. Newborns develop pyloric stenosis, a disease in which the evacuation of food from the stomach into the small intestine is difficult.

Pirouette ventricular tachycardia, cardiac arrhythmia, long QT interval syndrome are the main manifestations of cardiotoxicity of this group of antibiotics. The situation is aggravated by advanced age, heart disease, overdose, water and electrolyte disorders.

A long course of treatment, excess dosage are the main causes of hepatoxicity. Macrolides have different effects 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.

Few doctors know when prescribing a macrolide antibiotic that this is a direct threat to a person's mental health. Neuropsychiatric disorders most often occur when taking clarithromycin.

Video about the group in question:

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. Eli Lilly & Company, an international American innovative company, has replenished its portfolio of the latest pharmaceuticals. 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-lactim antibiotics;
• creating high and stable concentrations in tissues.

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lifetab.ru

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.

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 schemes. AT modern medicine the first of these drugs is more often used as the drug of choice in patients with individual intolerance to penicillins, the second - as a highly effective agent, characterized by a long 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.

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.

To natural, in addition to those already mentioned in historical background medicines include Midecamycin and Josamycin; to artificially synthesized - Azithromycin, Clarithromycin, Roxithromycin, etc. From general group prodrugs are isolated that have a slightly modified structure:

• 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).

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), oral diseases that have 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 meningococcal carriers, during surgical procedures in lower section intestines.

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.

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, 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.

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 in relation to pathogens that cause inflammatory processes in gastrointestinal tract(including 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.

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.

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.

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.

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.

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:

• disturbances in the work of the gastrointestinal tract (nausea, vomiting, dysbacteriosis), kidneys, liver and central nervous system;
• allergic reactions;
• visual and hearing disorders;
• arrhythmia, tachycardia.

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.

med-antibiotics.ru

Antibiotics are the waste products (of natural or synthetic origin) of viral, bacterial or fungal cells that can inhibit the growth and reproduction of other cells or microorganisms. Drugs may have antibacterial, anthelmintic, antifungal, antiviral and antitumor activity. They are divided into groups depending on the chemical structure.

Macrolide antibiotics are relatively safe representatives of antimicrobial agents. They have the form of complex compounds consisting of carbon atoms, which are attached in various ways to the macrocyclic lactone ring. The drugs are well tolerated by patients.

Classification

The macrolide group has several divisions:

1. Depending on the number of attached carbon atoms:
   • preparations having 14 carbon atoms (for example, Erythromycin, Clarithromycin, Oleandomycin);
   • means with 15 carbon atoms (Azithromycin);
   • macrolides with 16 carbons attached (eg Josamycin, Spiramycin, Roxithromycin);
   • 23 atoms - belong to the only drug (Tacrolimus), which simultaneously belongs to the list of macrolide drugs and immunosuppressants.
2. According to the method of obtaining antibiotics: natural and synthetic origin.
3. Effect duration:
   • short-acting (Erythromycin, Spiramycin, Oleandomycin, Roxithromycin);
   • average duration (Clarithromycin, Josamycin, Flurithromycin);
   • "Long" drugs (Azithromycin, Dirithromycin).
4. Depending on the generation of drugs:
   • means of the 1st generation;
   • macrolides of the 2nd generation;
   • 3rd generation antibiotics (latest generation macrolides);
   • Ketolides are agents whose chemical structure consists of a traditional ring with the addition of a keto group.

The effectiveness of drugs

Antibiotics of this group, especially new generation macrolides, have a wide spectrum of action. They are used to combat gram-positive microorganisms (staphylococci and streptococci). At the present stage, there is a decrease in the sensitivity of pneumococci and some types of streptococci to antibiotics that have 14 and 15 carbon atoms in the composition, however, 16-membered preparations retain their activity against these bacteria.

The drugs are effective against the following pathogens:

• some strains of Mycobacterium tuberculosis;
• gardnerella;
• chlamydia;
• the causative agent of whooping cough;
• mycoplasma;
• bacillus that causes the development of hemophilic infection.

Mechanism of action and benefits

Macrolides are tissue preparations, since their use is accompanied by the fact that the concentration of active substances in soft tissues is much higher than in the bloodstream. This is due to the ability of the substance to penetrate into the middle of the cells. The drugs bind to plasma proteins, but the degree of such action varies from 20 to 90% (depending on the antibiotic).

The action of various antibiotics on the bacterial cell

The mechanism of action is due to the fact that macrolides inhibit the process of protein production by microbial cells, disrupt the functionality of their ribosomes. In addition, they have a predominantly bacteriostatic effect, that is, they inhibit the growth and reproduction of pathogenic microorganisms. The drugs have low toxicity, do not cause the development of an allergic reaction when combined with other groups of antibiotics.

Additional benefits of the latest generation products:

• long half-life of drugs from the body;
• transportation to the site of infection with the help of leukocyte cells;
• no need for a long course of treatment and frequent use of drugs;
• no toxic effect on the digestive system;
• when using tablet forms, absorption from the gastrointestinal tract is more than 75%.

Macrolides in ENT practice

The drugs act on a wide range of pathogens of ENT diseases. Antibiotics are recommended for the treatment of bacterial tonsillitis, tonsillopharyngitis, acute inflammation of the middle ear and paranasal sinuses, as well as bronchitis and pneumonia. Macrolides are not used in the treatment of paratonsillitis, inflammation of the epiglottis and abscess of the pharynx.

Azithromycin has found the greatest prevalence in the treatment of the upper respiratory tract. The results of the studies confirmed the effectiveness of the drug in children with mild and moderate severity of inflammatory processes. Clinical manifestations of the effectiveness of treatment are the normalization of body temperature, the elimination of leukocytosis, the subjective improvement in the condition of patients.

Doctors prioritize this group of antibiotics based on the following points:

1. Sensitization to penicillins. In patients with rhinosinusitis or otitis media on the background of allergic rhinitis or bronchial asthma, penicillin preparations, which are put in the first place, cannot be used due to allergenic properties. They are replaced by macrolides.
2. The group has an anti-inflammatory effect and a wide spectrum of action.
3. The presence of infections caused by atypical bacteria. Macrolides are effective against such pathogens that cause the development of certain types of tonsillopharyngitis, chronic adenoiditis, nasal pathologies.
4. A number of microorganisms can form specific films under which pathogens “live”, causing the development of chronic processes in the ENT organs. Macrolides are able to act on pathological cells during their stay under such films.

Contraindications

Macrolides are considered relatively safe drugs that can be prescribed for the treatment of children, but even they have some contraindications for use. It is undesirable to use the funds of this group during pregnancy and lactation. The use of macrolides in children under 6 months of age is not recommended.

Means are not prescribed in the presence of individual hypersensitivity to active components, with severe pathologies of the liver and kidneys.

Side effects

Adverse reactions develop infrequently. There may be attacks of nausea and vomiting, diarrhea, abdominal pain. With a negative effect on the liver, the patient complains of an increase in body temperature, yellowing of the skin and sclera, weakness, and dyspeptic manifestations.

From the side of the central nervous system, cephalgia, slight dizziness, and a change in the functioning of the auditory analyzer can be observed. Local reactions can develop with parenteral administration of drugs (inflammation of the veins with the formation of blood clots in them).

Group representatives

Most macrolides should be taken an hour before a meal or a few hours after it, because when interacting with food, the activity of the drugs decreases. Liquid dosage forms are taken according to the scheme prescribed by the attending physician.

Be sure to observe even intervals between doses of antibiotics. If the patient missed a dose, the medicine should be taken as soon as possible. Doubling the dosage of the drug at the time of the next dose is prohibited. During the period of treatment, you should definitely stop drinking alcohol.

Produced in the form of oral forms, suppository, powder for injection. This representative can be used during pregnancy and lactation, but under the strict supervision of the attending physician. For the treatment of newborns, it is not prescribed because of the possibility of developing a narrowing of the output section of the stomach (pyloric stenosis).

Produced in the form of tablets. The spectrum of activity is similar to the previous representative of the group. Its analogues are Rulid, Roxithromycin Lek. Differences from Erythromycin:

• the percentage of the drug entering the blood is higher, does not depend on the intake of food in the body;
• longer withdrawal period;
• better tolerability of the drug by patients;
• interacts well with drugs of other groups.

It is prescribed to combat inflammation of the tonsils, larynx, paranasal sinuses of a streptococcal nature, infection caused by mycoplasmas and chlamydia.

Available in tablets and powders for injection. Analogues - Fromilid, Klacid. Clarithromycin has a high bioavailability and is well tolerated by patients. Not used for the treatment of newborns, pregnant and lactating mothers. The drug is effective against atypical microorganisms.

Macrolide belonging to the class of antibiotics with 15 carbon atoms. Available in the form of tablets, capsules, powders for injection and syrup. It differs from Erythromycin in a large percentage of entry into the bloodstream, less dependence on food, and a long-term preservation of the therapeutic effect after the end of therapy.

Antibiotic of natural origin, having 16 carbon atoms in the composition. Effective in the fight against pneumonia pathogens that are resistant to other representatives of macrolides. It can be prescribed for the treatment of women during the period of bearing a child. Introduced orally or into a vein drip.

The active substance is midecamycin. Macrolide of natural origin, acting on those staphylococci and pneumococci that are resistant to other drugs. The agent is well absorbed from the intestinal tract and interacts well with representatives of other groups of medicines.

It has a slightly different spectrum of action than Erythromycin. Josamycin fights those microorganisms that are resistant to a number of macrolides, but is not able to suppress the reproduction of a number of erythromycin-sensitive bacteria. Available in the form of tablets and suspensions.

Conditions for prescribing drugs

For macrolide treatment to be effective, a number of rules must be observed:

1. Making an accurate diagnosis, which allows you to clarify the presence of local or general inflammation in the body.
2. Determination of the causative agent of pathology using bacteriological and serological diagnostics.
3. The choice of the necessary drug based on the antibiogram, the localization of the inflammatory process and the severity of the disease.
4. The choice of the dosage of the drug, the frequency of administration, the duration of the course of treatment based on the characteristics of the drug.
5. The appointment of macrolides with a narrow spectrum of action for relatively mild infections and with a wide spectrum for severe diseases.
6. Monitoring the effectiveness of therapy.

The list of drugs is quite wide. Only a qualified specialist can choose the necessary remedy that will be most effective for each specific clinical case.

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Many believe that antibiotics should be used only in extreme cases. However, this is not an entirely correct opinion, since the list of such drugs is replenished with drugs that are relatively safe - macrolides. Such antibiotics, basically, without having a negative impact on the human body, are able to overcome the infection “in no time”. The safe profile allows prescribing macrolides to patients undergoing outpatient and inpatient treatment, as well as to children aged 6 months and older (under medical supervision).

Few people know about the properties, origin and effect of such "harmless" remedies. And if you want to get acquainted with such drugs and find out in more detail what a macrolide antibiotic is, we suggest reading our article.

It should be noted right away that macrolides belong to the group of antibiotic drugs that are the least toxic to the human body and are well tolerated by patients.

Antibiotics such as macrolides, from the point of view of biochemistry, are complex compounds of natural origin, which consist of carbon atoms, which are in different amounts in the macrocyclic lactone ring.

If we take this criterion, which is responsible for the number of carbon atoms, as the basis for the classification of drugs, then we can divide all such antimicrobial agents into:

• 14-membered, which include semi-synthetic drugs - Roxithromycin and Clarithromycin, as well as natural - Erythromycin;
• 15-membered, represented by a semi-synthetic agent - Azithromycin;
• 16-membered, including a group of natural drugs: Midecamycin, Spiramycin, Josamycin, as well as semi-synthetic Midecamycin acetate.

Erythromycin, an antibiotic of the macrolide group, was one of the first to be discovered, in 1952. New generation drugs appeared a little later, in the 70s. Since they showed excellent results in the fight against infections, research on this group of drugs has continued actively, so that today we have a fairly extensive list of drugs that can be used to treat both adults and children.

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The antimicrobial effect is achieved by affecting the ribosomes of microbial cells, disrupting protein synthesis. Of course, under such an attack of macrolides, the infection weakens and “surrenders”. In addition, antibiotics of this group of drugs are able to regulate immunity, providing immunomodulatory activity. Also, these drugs have anti-inflammatory properties, affecting both the body of adults and children, quite moderately.

Means of the group of antibacterial agents of the new generation are able to cope with atypical microbacteria, gram-positive cocci and similar misfortunes, which often become the causative agents of such diseases as: bronchitis, whooping cough, diphtheria, pneumonia, etc.

No less popular are macrolides in the situation that has developed over the past few years, due to the addiction of a large number of microbes to antibiotics (resistance). This is due to the fact that new generation drugs belonging to this group are able to maintain their activity against a variety of pathogens.

In particular, macrolide preparations are widely used in the treatment and as prophylactic agents for the following diseases:

• Chronical bronchitis;
• acute sinusitis;
• periostitis;
• periodontitis;
• rheumatism;
• endocarditis;
• gastroenteritis;
• severe forms of toxoplasmosis, acne, mycobacteriosis.

The list of diseases that can be overcome using new generation antibiotics, which have a common name - macrolides, can be supplemented by sexually transmitted infections - syphilis, chlamydia and infections that affect soft tissues and skin - furunculosis, folliculitis, paronychia.

If your doctor prescribes a similar antibiotic for you, immediately read its contraindications indicated in the instructions for the drug. Unlike most conventional antibiotics, new generation drugs - macrolides are safe, including for children, and less toxic. Therefore, the list of undesirable effects of antibiotics in this group is not as large as that of similar drugs.

First of all, it is not recommended to use macrolides for pregnant women and mothers during lactation. The use of such drugs in children under 6 months is contraindicated, since the reaction to the drug has not yet been studied. You should not use such drugs as a treatment for people who have individual sensitivity.

Antibiotics of the macrolide group with special attention should be prescribed by doctors to patients of mature age. This is due to the fact that most of the older generation have disorders in the functioning of the kidneys, liver and heart.

Side effects can also occur when using macrolides in a mild form - weakness and malaise that appear after taking them. But there may also be:

• vomit;
• nausea;
• headache and pain in the abdomen;
• impaired vision, hearing;
• an allergic reaction in the form of a rash, urticaria (most often occurs in children).

In order to avoid problems and undesirable consequences after the use of drugs of the macrolide group, it is necessary to strictly follow the doctor's recommendations, strictly observe the dosage and refrain from drinking alcohol. It is also strictly forbidden to combine the intake of new generation antibiotics with antacids. It is also important not to skip appointments.

Basically, new generation antibiotics should be taken 1 hour before a meal, or 2 hours after a meal. Take the tablets with a whole glass of water. If the doctor has prescribed you an antibiotic of the macrolide group, the release form of which is a powder for the preparation of a suspension, strictly follow the instructions for preparing the medicine and strictly follow the doctor's instructions.