Macrolide antibiotics for children. How to take macrolides

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, high rates 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 the performance, drug interaction with other drugs, pharmacokinetic properties, tolerability, etc. 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. Absorbed in digestive tract partially.

Among side effects note: 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. Observed 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 12 - duodenal ulcer. 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.

Ol. 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, hit 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.

Effective in the eradication of streptococcus, the treatment of lobar pneumonia, infectious lesions of the pelvic organs, genitourinary system, tick-borne borreliosis, 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 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.

Lactation period (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.

Differs from other macrolides in that it regulates 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 permissible to take it while carrying a child. 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 motor skills. 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 protective functions organism.

Macrolides are used for:

  • therapy for atypical mycoses bacterial 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 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.

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 disturbances.

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.

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:

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-lactim antibiotics;
  • creating high and stable concentrations in tissues.

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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 exerting on the human body negative impact, are capable of "in no time" to overcome the infection. 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 natural origin, which consist of carbon atoms, which are in different numbers 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 the group natural preparations: 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.

http://youtu.be/-PB2xZd-qWE

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 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 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 toxoplasmosis, acne, mycobacteriosis.

List of diseases that can be overcome using new generation antibiotics that have common name- macrolides, can supplement 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 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 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).

To avoid problems and undesirable consequences after the use of drugs of the macrolide group, it is necessary to strictly follow the recommendations of the doctor, 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.

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 medicines, which have earned the respect of specialists, and are boldly used in pediatrics. The advantage of such treatments, unlike other similar ones, is that they practically do not cause allergic reactions in small patients. In particular, this applies to drugs that have names - "Penicillin" and "Cefalosporin".

Despite the fact that macrolides are safe for children, they have a fairly effective effect. Their impact in a mild form on the child's body is provided by the pharmacokinetic properties inherent in the preparations. Some of the most popular means that represent the macrolide group are:

  • Erythromycin;
  • 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 no 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.

Macrolide antibiotics are antibacterial agents widely used in modern medical practice for the treatment of infectious diseases. This group of drugs belongs to the least toxic antibiotics, which have less pronounced side effects than other antibacterial drugs.

Clinical studies confirm that macrolides have a persistent post-antibiotic effect, that is, for a long time after ingestion, they suppress the vital activity of bacterial microorganisms. In addition, the drugs of this group have non-antibacterial activity, which is expressed in the form of anti-inflammatory and prokinetic action (the ability to stimulate the motility of the gastrointestinal tract).

Most often, macrolide antibiotics are used in the treatment of the following diseases:

  • respiratory infections (whooping cough, diphtheria, sinusitis, tonsillitis, exacerbation of chronic bronchitis);
  • skin and soft tissue infections (furunculosis, folliculitis);
  • bacterial infections of the oral cavity (periodontitis, periostitis);
  • sexually transmitted infections (chlamydia, syphilis);
  • gastroenteritis;
  • urinary tract infections;
  • severe forms of acne.

In addition, macrolide antibiotics can be used to prevent infectious diseases in rheumatological and dental practices. They are also used to prevent post-operative infections after certain surgeries.

Macrolide antibiotics are classified according to their chemical structure and method of preparation. Depending on the chemical structure, macrolides are divided into:

  • 14-membered (erythromycin, clarithromycin, roxithromycin, oleandomycin, dirithromycin);
  • 15-membered (azithromycin);
  • 16-membered (spiramycin, midecamycin, josamycin).

This classification is necessary to assess the safety of drugs, which largely depends on the characteristics of their chemical structure. For example, 14-mer macrolides have a stimulating effect on the motility of the gastrointestinal tract, which can provoke various intestinal disorders. 15-membered and 16-membered macrolides can also cause this undesirable effect, however, it is much less pronounced.

Depending on the method of preparation, preparations of the macrolide group are divided into natural and synthetic. The list of natural antibacterial agents includes erythromycin, midecamycin, oleandomycin, spiramycin, josamycin. Semi-synthetic drugs include clarithromycin, azithromycin, roxithromycin.

Antibiotics from the macrolide group are among the safest types of antibacterial agents. They have a relatively low toxicity, do not have a pronounced effect on the body's immune system and are well tolerated by patients. Compared with antibiotics of other groups, macrolides are less likely to cause allergic reactions. Currently, they are widely used in the treatment of infectious diseases in newborns, children and pregnant patients.

At the same time, this type of antimicrobial drugs can cause a number of undesirable effects:

  • gastrointestinal disorders (nausea, vomiting, diarrhea, abdominal pain);
  • increased risk of severe cardiac disorders;
  • pressure drop;
  • abnormal liver function (cholestatic hepatitis);
  • reversible hearing loss;
  • allergic reactions.

Roxithromycin has the best tolerance among macrolides. It is followed by azithromycin, then by spiramycin and clarithromycin, and after them by erythromycin. As for contraindications for use, they are established in individually depending on the type and characteristics of the course of the disease, the patient's condition and the form of release of the drug.

Some macrolide antibiotics should not be used in children, pregnant or lactating women, or in patients with severe hepatic impairment.

Other medicines in this group may be used in the elderly, neonates, young children and women during pregnancy and breastfeeding. However, such an appointment is allowed only if there are strict indications and requires careful medical supervision during the entire period of treatment.

International name:

Dosage form:

Pharmachologic effect:

Indications:

International name:

Dosage form:

Pharmachologic effect:

Indications:

International name: Roxithromycin (Roxithromycin)

Dosage form: dispersible tablets, coated tablets

Pharmachologic effect: Semi-synthetic macrolide antibiotic for oral administration. Has a bacteriostatic effect: binding to the 50S subunit of ribosomes.

Indications: Infections of the upper and lower respiratory tract (pharyngitis, bronchitis, pneumonia, bacterial infections in COPD, panbronchiolitis, bronchiectasis.

International name: Clarithromycin (Clarithromycin)

Dosage form: granules for suspension for oral administration, capsules, lyophilisate for solution for infusion, powder for suspension for oral administration, film-coated tablets, long-acting film-coated tablets

Pharmachologic effect: Semi-synthetic macrolide antibiotic a wide range actions. Violates protein synthesis of microorganisms (binds to the 50S subunit of the membrane.

Indications: Bacterial infections caused by susceptible microorganisms: infections of the upper respiratory tract (laryngitis, pharyngitis, tonsillitis, sinusitis).

International name: Roxithromycin (Roxithromycin)

Dosage form: dispersible tablets, coated tablets

Pharmachologic effect: Semi-synthetic macrolide antibiotic for oral administration. Has a bacteriostatic effect: binding to the 50S subunit of ribosomes.

Indications: Infections of the upper and lower respiratory tract (pharyngitis, bronchitis, pneumonia, bacterial infections in COPD, panbronchiolitis, bronchiectasis.

International name: Josamycin (Josamycin)

Dosage form:

Pharmachologic effect:

Indications:

International name: Erythromycin (Erythromycin)

Dosage form: granules for the preparation of a suspension for oral administration, granules for the preparation of a suspension for oral administration, lyophilizate for the preparation of a solution for intravenous administration, powder for solution for injection, rectal suppositories [

Pharmachologic effect: A bacteriostatic antibiotic from the macrolide group, reversibly binds to the 50S subunit of ribosomes, which disrupts the formation of peptide bonds.

Indications: Bacterial infections caused by susceptible pathogens: diphtheria (including bacterial carriage), whooping cough (including prevention), trachoma.

International name: Josamycin (Josamycin)

Dosage form: oral suspension, coated tablets

Pharmachologic effect: An antibiotic from the group of macrolides, acts bactericidal. It binds to the 50S subunit of the ribosomal membrane and prevents fixation of the transport membrane.

Indications: Infectious and inflammatory diseases caused by susceptible microorganisms: otitis media, sinusitis, tonsillitis, pharyngitis, laryngitis, diphtheria.

International name: Dirithromycin (Dirithromycin)

Pharmachologic effect: Macrolide antibiotic. Suppresses intracellular protein synthesis in sensitive microorganisms. Active against gram-positive.

Indications: Infectious and inflammatory diseases caused by sensitive pathogens: pharyngitis; tonsillitis; bronchitis (acute and exacerbation); pneumonia; skin and soft tissue infections; cholecystitis, cholangitis.

Macrolides are a new generation of antibacterial agents. The basis of the structure of this type of antibiotics is the macrocyclic lactone ring. This fact gave the name to the whole group of drugs. Depending on the number of carbon atoms contained in the ring, all macrolides are: 14, 15, and 15-membered.

Antibiotics - macrolides are active against gram-positive cocci, as well as against intracellular pathogens: mycoplasmas, chlamydia, campylobacter, legionella. This group of drugs belongs to the least toxic antibiotics, and the list of drugs included in it is quite extensive.

Today we will talk about antibiotics macrolides, names, use, indications for use, we are considering - you will also find out all this, find out and discuss:

Names of macrolide antibiotics

The group of these drugs includes many drugs - antibiotics of the new generation. The most famous of them:

Natural macrolides: Oleandomycin phosphate, Erythromycin, Erycycline spiramycin, as well as midecamycin, leukomycin and josamycin.

Semi-synthetic macrolides: Roxithromycin, Clarithromycin, Dirithromycin. This group also includes: Flurithromycin, Azithromycin and Rokitamycin.

Often prescribed drugs such as: Vilprafen, Kitazamicin, Midecamycin. In a pharmacy, you will most likely be recommended the following names: Roxithromycin, Sumamed, Tetraolean and Eriderm.

It must be said that the names of antibiotic drugs often differ from the names of the macrolides themselves. For example, the active ingredient of the well-known drug "Azitrox" is the macrolide Azithromycin. Well, the drug "Zinerit" contains the antibiotic macrolide Erythromycin.

What are macrolide antibiotics good for? Indications for use

This group of drugs has a wide spectrum of action. Most often they are prescribed in the treatment of the following diseases:

Infectious diseases of the respiratory system: diphtheria, whooping cough, acute sinusitis. They are prescribed for the treatment of atypical pneumonia, used for exacerbations of chronic bronchitis.

Infectious diseases of soft tissues, skin: folliculitis, furunculosis, paronychia.

Sexual infections: chlamydia, syphilis.

Bacterial infections of the mouth: periostitis, periodontitis.

In addition, drugs of this group are prescribed in the treatment of toxoplasmosis, gastroenteritis, cryptosporidiosis, as well as in the treatment of severe acne. Assign for other infectious diseases. They may also be recommended for the prevention of infections in dental practice, rheumatology, as well as surgical treatment on the large intestine.

How and how much to take macrolide antibiotics? Application, dosage

The group of macrolide antibiotics is represented by different dosage forms: tablets, granules, suspensions. Pharmacies will also offer: suppositories, powder in vials and a preparation in the form of a syrup.

Regardless of the dosage form, drugs intended for internal use are prescribed to drink by the hour, observing an equal period of time. Usually they are taken 1 hour before a meal, or 2 hours after it. Only a small number of these antibiotics are not dependent on food intake. Therefore, before starting treatment, carefully read the package leaflet.

In addition, any drug in this group can be used only for medical indications by doctor's prescription. After establishing the diagnosis, the doctor will prescribe the remedy that will help with your disease, and exactly the dosage that you need. The dosage regimen takes into account the age, body weight of the patient, the presence of chronic diseases and so on.

Who are macrolide antibiotics dangerous for? Contraindications, side effects

Like most serious drugs, macrolides have a number of contraindications for use. They also have side effects. However, it should be noted that their number is significantly less than that of antibiotics of other groups. Macrolides are less toxic and therefore safer than other antibiotics.

However, they are contraindicated in pregnant women, nursing mothers, babies under 6 months. They can not be used in case of individual sensitivity of the body to the components of the drug. With caution, these drugs are prescribed to people with serious violations of the liver and kidneys.

With improper use or uncontrolled use, side effects may occur: headache, dizziness. Hearing may be disturbed, often there is nausea, vomiting, discomfort in the abdomen, and diarrhea appears. Observed allergic manifestations: rash, urticaria.

Remember that self-prescribing, taking antibiotics without a doctor's prescription, can seriously aggravate the patient's condition. Be healthy!


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.

Table of contents [Show]

Macrolide antibiotics: classification

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 and high bioavailability. They are acid resistant.

Chemical structural basis

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.

Group of antibiotics macrolides: a list of drugs

Name and release form
Azivok - capsule form
Azimicin - tablet form
Azitral - capsule form
Azitrox - capsule form
Azithromycin - capsules, powders
AzitRus - capsule form, powder form, tablet form
Azicide - tablet form
Binoclair - tablet form
Brilid - tablet form
Vero-Azithromycin - capsule form
Vilprafen (Josamycin) - tablet form
Grunamycin syrup - granules
ZI-Factor - tablets, capsules
Zitrolide - capsule form
Ilozon - suspension
Klabaks - granules, tablets
Clarithromycin - capsules, tablets, powder
Clarithrosin - tablet form
Klacid - lyophilizate
Klacid - powder, tablets
Rovamycin - powder form, tablets
RoxyGEKSAL - tablet form
Roxid - tablet form
Roxilor - tablet form
Roksimizan - tablet form
Rulid - tablet form
Rulicin - tablet form
Seidon-Sanovel - tablet form, granules
SR-Claren - tablet form
Sumazid - capsules
Sumaclide - capsules
Sumamed - capsules, aerosols, powder
Sumamycin - capsules, tablets
Sumamox - capsules, tablet form
Sumatrolid solutab - tablet form
Fromilid - granules, tablet form
Hemomycin - capsules, tablets, lyophilisate, powder
Ecositrin - tablet form
Ecomed - tablet form, capsules, powder
Erythromycin - lyophilisate, eye ointment, ointment for external use, powder, tablets
Ermiced - liquid form
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. 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.

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. 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.

Oleandomycin

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.

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 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.

Effective in the eradication of streptococcus, the treatment of lobar pneumonia, infectious lesions of the pelvic organs, the genitourinary system, tick-borne borreliosis, venereal 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.


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, 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.

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 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.

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. 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.

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, and 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 disturbances.

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 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 to a person's 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 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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In severe pneumonia, macrolides are also used, the list of drugs of which is indicated in the standard treatment protocols. However, they contain information about the need to combine with other antimicrobials. Most often they are used together with cephalosporins. This combination allows you to mutually increase the effectiveness of both drugs without increasing their toxicity.

Macrolide classification

The most competent and convenient classification of this group of drugs is chemical. It reflects the differences in the structure and origin of the antibiotics of the group called "Macrolides". The list of drugs will be given below, and the substances themselves are distinguished by:

  1. 14-mer macrolides:
  • natural origin - erythromycin and oleandomycin;
  • semi-synthetic - clarithromycin and roxithromycin, dirithromycin and flurithromycin, telithromycin.

2. Azalide (15-mer) macrolides: azithromycin.

3. 16-mer macrolides:

  • natural origin - midecamycin, spiramycin and josamycin;
  • semi-synthetic - midecamycin acetate.

This classification reflects only the structural features of the drugs of the class. The list of trade names is presented below.

List of drugs

Macrolides are drugs, the list of which is very wide. In total, as of 2015, there are 12 medicinal substances of this class. And the number of preparations containing data active ingredients, much higher. Many of them can be found in the pharmacy network and taken to treat a number of diseases. Moreover, some drugs are not available in the CIS, as they are not registered in the pharmacopoeia. Examples of trade names for preparations containing macrolides are as follows:

  • Erythromycin is often produced in preparations with the same name, and is also included in the complex medicines Zinerit and Isotrexin.
  • Oleandomycin - medicinal substance drug "Oletetrin".
  • Clarithromycin: "Klabaks" and "Claricar", "Clerimed" and "Klacid", "Cleron" and "Lecoclar", "Pylobact" and "Fromilid", "Ekozitrin" and "Erasid", "Zimbaktar" and "Arvitsin", "Kispar" and "Clarbakt", "Claritrosin" and "Claricin", "Klasine" and "Coater", "Clerimed" and "Romiclar", "Seydon" and "SR-Claren".
  • Roxithromycin is often found in the form of a generic trade name, and is also included in the following drugs: Xitrocin and Romic, Elrox and Rulicin, Esparoxy.
  • Azithromycin: Azivok and Azidrop, Azimycin and Azitral, Azitrox and Azitrus, Zetamax and Zi-Factor, Zitnob and Zitrolid, Zitracin and Sumaklid ”, “Sumamed” and “Sumamoks”, “Sumatrolid” and “Tremax-Sanovel”, “Hemomycin” and “Ecomed”, “Safocid”.
  • Midecamycin is available in the form of the drug "Macropen".
  • Spiramycin is available as Rovamycin and Spiramycin-Vero.
  • Dirithromycin, flurithromycin, as well as telithromycin and josamycin are not available in the CIS.

The mechanism of action of macrolides

This specific pharmacological group- macrolides - has a bacteriostatic effect on the susceptible cell of the causative agent of infectious diseases. Only in high concentrations is it possible to provide a bactericidal effect, although this has only been proven in laboratory studies. The only mechanism of action of macrolides is the inhibition of protein synthesis of microbial cells. This disrupts all the vital processes of a virulent microorganism, as a result of which it dies after a while.

The mechanism of inhibition of protein synthesis is associated with the attachment of bacterial ribosomes to the 50S subunit. They are responsible for building up the polypeptide chain during DNA synthesis. Thus, the synthesis of structural proteins and virulence factors of the bacterium is disrupted. At the same time, the high specificity to the bacterial ribosome determines the relative safety of macrolides for the human body.

Comparison of macrolides and antibiotics of other classes

Macrolides are similar in properties to tetracyclines, but safer. They do not disrupt the development of the skeleton in childhood. Like tetracyclines with fluoroquinolones, macrolides (the list of drugs is presented above) are able to penetrate into the cell and create therapeutic concentrations in three compartments of the body. This is important in the treatment of mycoplasmal pneumonia, legionellosis, campylobacteriosis and chlamydial infection. At the same time, macrolides are safer than fluoroquinolones, although they are less effective.

All macrolides are more toxic than penicillins, but the safest in terms of the likelihood of developing allergies. Wherein penicillin antibiotics are champions in safety, but tend to cause allergies. Thus, having a similar spectrum of antimicrobial activity, macrolides can replace aminopenicillins in infections. respiratory system. And laboratory research show that macrolides reduce the effectiveness of penicillins when taken together, although modern treatment protocols allow their combination.

Macrolides during pregnancy and in pediatric therapy

Macrolides are safe drugs along with cephalosporins and penicillins. This allows them to be used during pregnancy and in the treatment of children. They do not disrupt the development of the bone and cartilage skeleton, do not have teratogenic properties. Only azithromycin should be limited in use in the third trimester of pregnancy. In pediatric therapy, both penicillins, and cephalosporins, and macrolides, the list of which is indicated in the standard protocols for the treatment of diseases, can be used without risk. toxic lesions organism.

Description of some macrolides

Macrolides (drugs, we listed above) in clinical practice widely used, including in the CIS. Most often, 4 of their representatives are used: clarithromycin and azithromycin, midecamycin and erythromycin. Spiramycin is used much less frequently. The effectiveness of macrolides is approximately the same, although it is achieved in different ways. In particular, clarithromycin and midecamycin to achieve clinical effect must be taken twice a day, while azithromycin acts for 24 hours. One dose per day is enough for the treatment of infectious diseases.

Erythromycin is the shortest of all macrolides. It should be taken 4-6 times a day. Therefore, it is most often used in the form of topical forms for the treatment of acne and skin infections. It is noteworthy that macrolides for children are safe, although they can cause diarrhea.

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 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.

Historical 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 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.

IN 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 chemical structure, method of preparation, duration of exposure and generation of the drug.

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

Number of attached carbons
14 15 16
Oleandomycin;

Dirithromycin;

Clarithromycin;

Erythromycin.

Azithromycin Roxithromycin;

Josamycin;

Midecamycin;

Spiromycin.

The duration of the therapeutic effect
short average long
Roxithromycin;

Spiramycin;

Erythromycin.

Flurithromycin (not registered in our country);

Clarithromycin.

Dirithromycin;

Azithromycin.

Generation
first second third
Erythromycin;

Oleandomycin.

Spiramycin;

Roxithromycin;

Clarithromycin.

Azithromycin;

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 reference 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).

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 meningococcal carriers, 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 +
Azithromycin + +
Josamycin +
Zitrolide +
Ilozon + + + +
Clarithromycin + + +
macrofoam + +
Rovamycin + +
Rulid +
Sumamed + +
Hemomycin + +
Ecomed + +
Erythromycin + +

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.

Roxithromycin

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.

Erythromycin

Under the strict supervision of a physician, the use of the drug in the treatment of pregnant women is allowed (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).

macrofoam

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, period 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.

Clarithromycin

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.

Azithromycin

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.

Spiramycin

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 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. Are characterized by the presence long period 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:

  • 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 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 that have expired.

In the absence of improvement, the appearance of new symptoms should immediately contact your doctor.

Medical terms are often incomprehensible to the general population, unfamiliar with narrow concepts. It can be difficult for a non-specialist to figure out what a doctor prescribes, since the name of the drug or group of drugs does not tell the patient anything. What is hidden behind the word "macrolides", what drugs are included in this group and what they are for - all this is in the article.

What are macrolides

Macrolides are a group of antibiotics. They are the latest generation of drugs.

Chemical structure of macrolides:

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

Macrolides are classified according to their origin into 3 groups:

  • natural(derived from various kinds bacteria Streptomyces - living microorganisms that live in the soil and layers of sea water);
  • semi-synthetic(derivatives from natural macrolides);
  • azalides(15-membered macrolides obtained by inserting a nitrogen atom between 9 and 10 carbon atoms).

The list of drugs included in the group of macrolides is wide. Below is a description existing medicines from this group.

The first drug representative of the azalide class. Active ingredient: azithromycin. Release form: tablets, capsules, powder for suspension.

Indications for use: many diseases associated with ENT organs (bronchitis, tonsillitis, pharyngitis, sinusitis and others), infections of the skin and soft tissues (beshiha, infectious dermatitis), cervicitis or urethritis, occurring without complications, initial stages borreliosis, scarlet fever, diseases of the gastrointestinal tract and duodenum caused by bacterium Helicobacter pylori.

Contraindications: for all forms of release: intolerance to azithromycin or other components, as well as severe liver and kidney disease. Tablets and capsules should not be used for children weighing up to 45 kilograms, suspension - for children up to 5 kilograms in weight.

Side effects: visual and hearing impairment, diarrhea, nausea, vomiting. Less commonly, there are problems with heart rhythm, allergic reactions and disruption of the central nervous system.

Analogues: Azivok, Azitral, Zitrolid, Hemomycin, Sumaklid 1000 and others.

The name of an antibiotic is also the name of its active ingredient. In fact, it is a powder consisting only of the active ingredient. Indications for use: dental infections, diseases of the upper respiratory tract (including tonsillitis caused by an atypical pathogen), respiratory diseases, erysipelas and scarlet fever (if penicillin cannot be used), ophthalmic inflammations, anthrax, syphilis, prostatitis, urethritis, furunculosis, gonorrhea.

Contraindications: severe liver damage, allergy to the drug.

Side effects: disorders of the gastrointestinal tract, plaque on the tongue, jaundice, general weakness, allergies, swelling of the feet, candidiasis and others.

Analogues: Vilprafen and Vilprafen Solutab.

Macrolide with a wide range of activities. Release form: capsules, tablets. Active ingredient: clarithromycin. Indications: mycobacterial infections, diseases (infectious) of ENT organs and upper and lower respiratory tract, infectious diseases of the skin.

Contraindications: I trimester of pregnancy and the period of breastfeeding, allergy to the drug, simultaneous reception with Terfenadine, Pimozide and Cisapride.

Side effects: disorders of the central nervous system (dizziness, panic conditions, hand tremors), gastrointestinal tract disorders, allergic manifestations, disturbances in the functioning of the sense organs (impaired vision or hearing), the appearance of resistance of microorganisms to the active substance.

Analogues: Arvicin, Clarexide, Klacid and others.

Belongs to natural macrolides. Active ingredient: midecamycin. Release form: tablets, powder. Corresponding pharmacological drug is called Macropen.

It is indicated for infectious diseases, when it is not possible to take penicillin, in the treatment of whooping cough, legionnaires' disease, otitis media, enteritis, scarlet fever, diphtheria, trachoma, pneumonia.

Contraindications: allergy to the drug, severe kidney and liver disease.

Side effects: heaviness in the abdomen, allergies, anorexia, increased levels of bilirubin and liver enzymes.

Produced in the form of a powder for the preparation of suspensions. Based on it, capsules and tablets are produced. Indications for use: lung abscess, pneumonia, pleurisy, otitis media, tonsillitis, whooping cough, trachoma, diphtheria, endocarditis, meningitis, sepsis, enterocolitis, osteomyelitis, gonorrhea, furunculosis.

Contraindications: allergies, pregnancy, liver failure is also not recommended for patients with a history of jaundice.

Side effects: diarrhea, vomiting, itching, nausea, liver failure, allergies.

Preparations produced on the basis of Oleandomycin: Oletetrin, Oleandomycin phosphate.

Semi-synthetic macrolide. Produced in the form of tablets. Active substance: roxithromycin. Indications: bacterial lesions of the ENT organs, infectious diseases upper and lower respiratory tract, skin, genitourinary system (except gonorrhea, urethritis, cervicitis, endometritis), skeletal system.

Contraindications: simultaneous use with Dihydroergotamine and Ergotamine, pregnancy and lactation, age up to 12 years, allergy to the drug.

Side effects: taste changes, gastrointestinal disorders, pancreatitis, vaginal or oral candidiasis, hepatitis (cholestatic or acute hepatocellular).

Analogues: Rulid, Elroks, Esparoxy.

A drug based on Spiramycin is called Spiramycin-Vero. Produced in the form of tablets and a special liquid (lyophilizate) for the preparation of a solution for intravenous injection. Indications: toxoplasmosis, rheumatism, bronchitis, urethritis, skin infections, prevention of meningitis, rheumatism, otitis media, sinusitis, tonsillitis, sexually transmitted diseases, carriage of pertussis and diphtheria bacteria.

Contraindications: lactation period, liver failure, childhood, deficiency of glucose-6-phosphate dehydrogenase.

Side effects: nausea, vomiting, allergic manifestations, cholestatic hepatitis, thrombocytopenia, transient paresthesia, acute hemolysis, ulcerative esophagitis.

Analogues: Rovamycin, Spiramycin Adipate, Spiramisar.

The first isolated macrolide of natural origin. Release form: tablets, solution, ointment (including eye). Active ingredient: erythromycin. Indications for use: used as a reserve antibiotic for allergies to penicillin. It is prescribed for the treatment of infectious diseases caused by bacteria (trachoma, erythrasma, pneumonia in children, cholecystitis, tonsillitis, otitis media, acne vulgaris).

Contraindications: hearing loss, pregnancy, taking terdenacin and astemizole, allergy to the drug. Alcohol is strictly contraindicated.

Side effects: abdominal pain, thrush oral cavity), pancreatitis, atrial fibrillation, dysbacteriosis, vomiting.

Analogues: Altrocin-S, Erythromycin ointment.

Preparations from the group of macrolides are prescribed for:

  • infectious diseases of the upper and lower respiratory tract;
  • sexually transmitted infections;
  • acne;
  • toxoplasmosis;
  • compylobacter gastroenteritis;
  • prevention and treatment of mycobacteriosis in patients with AIDS;
  • prevention of rheumatism, whooping cough, endocarditis;
  • as reserve antibiotics when it is impossible to use penicillin.

Macrolides destroy the structure of the microbe, penetrating into the ribosomes and stopping protein synthesis on them. Thus, the antimicrobial effect of the drugs is manifested.

Sometimes substances from this group exhibit a bacteriostatic effect, however, due to their large number, a bactericidal effect is exerted in relation to such organisms as whooping cough and diphtheria pathogens, pneumococci.

In addition to the antibacterial action, macrolides have a moderate anti-inflammatory and immunomodulatory effect.

Spiramycin, josamycin, and clarithromycin are taken with or without food. The remaining drugs are taken either 2 hours after a meal, or an hour before. Dosage and frequency of administration depends on the specific disease and doctor's prescriptions. Particular attention should be paid to this if macrolides are prescribed for children or during pregnancy. The duration of the course is also determined by the attending physician.

Erythromycin, when taken orally, is washed down with a full glass of water. When preparing solutions for oral administration, it is important to follow the proportions and recommendations indicated in the annotation to the drug.

Ointments are applied externally, thin layer over the affected area. Macrolide solutions for injections are prepared and placed only by medical workers. Since most drugs are prescription drugs, they should not be taken lightly.

Absolutely all drugs from the macrolide group have 2 contraindications:

  • individual intolerance to the components of the drug;
  • severe liver dysfunction.

Macrolides are considered a safe group of medicines for use.

At long-term treatment macrolides are possible:

  • violations of the liver;
  • allergic reactions;
  • frequent defecation;
  • taste disturbance, vomiting;
  • torsades de pointes ventricular tachycardia, cardiac arrhythmia, long QT syndrome;
  • neuropsychiatric disorders.

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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:

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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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.

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.

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 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.

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 a fairly effective effect. Their impact in a mild form on the child's body is provided by the pharmacokinetic properties inherent in the preparations. 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 no 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.

In severe pneumonia, macrolides are also used, the list of drugs of which is indicated in the standard treatment protocols. However, they contain information about the need to combine with others. They are most often used together with cephalosporins. This combination allows you to mutually increase the effectiveness of both drugs without increasing their toxicity.

Macrolide classification

The most competent and convenient classification of this group of drugs is chemical. It reflects the differences in structure and origin with the name "Macrolides". The list of drugs will be given below, and the substances themselves are distinguished by:

  1. 14-mer macrolides:
  • natural origin - erythromycin and oleandomycin;
  • semi-synthetic - clarithromycin and roxithromycin, dirithromycin and flurithromycin, telithromycin.

2. Azalide (15-mer) macrolides: azithromycin.

3. 16-mer macrolides:

  • natural origin - midecamycin, spiramycin and josamycin;
  • semi-synthetic - midecamycin acetate.

This classification reflects only the structural features of the drugs of the class. The list of trade names is presented below.

List of drugs

Macrolides are drugs, the list of which is very wide. In total, as of 2015, there are 12 medicinal substances of this class. And the number of drugs containing these active substances is much higher. Many of them can be found in the pharmacy network and taken to treat a number of diseases. Moreover, some drugs are not available in the CIS, as they are not registered in the pharmacopoeia. Examples of trade names for preparations containing macrolides are as follows:

  • Erythromycin is often produced in preparations with the same name, and is also included in the complex drugs "Zinerit" and "Isotrexin".
  • Oleandomycin is the drug substance of the drug Oletetrin.
  • Clarithromycin: "Klabaks" and "Clarikar", "Clerimed" and "Klacid", "Cleron" and "Lecoclar", "Pylobact" and "Fromilid", "Ekozitrin" and "Erasid", "Zimbaktar" and "Arvitsin", "Kispar" and "Clarbakt", "Claritrosin" and "Claricin", "Klasine" and "Coater", "Clerimed" and "Romiclar", "Seidon" and "SR-Claren".
  • Roxithromycin is often found in the form of a generic trade name, and is also included in the following drugs: Xitrocin and Romic, Elrox and Rulicin, Esparoxy.
  • Azithromycin: Azivok and Azidrop, Azimycin and Azitral, Azitrox and Azitrus, Zetamax and Zi-Factor, Zitnob and Zitrolid, Zitracin and Sumaklid ", "Sumamed" and "Sumamoks", "Sumatrolid" and "Tremax-Sanovel", "Hemomycin" and "Ecomed", "Safocid".
  • Midecamycin is available in the form of the drug "Macropen".
  • Spiramycin is available as Rovamycin and Spiramycin-Vero.
  • Dirithromycin, flurithromycin, as well as telithromycin and josamycin are not available in the CIS.

The mechanism of action of macrolides

This specific pharmacological group - macrolides - has a bacteriostatic effect on the susceptible cell of the causative agent of infectious diseases. Only in high concentrations is it possible to provide a bactericidal effect, although this has only been proven in laboratory studies. The only mechanism of action of macrolides is the inhibition of protein synthesis of microbial cells. This disrupts all the vital processes of a virulent microorganism, as a result of which it dies after a while.

The mechanism of inhibition of protein synthesis is associated with the attachment of bacterial ribosomes to the 50S subunit. They are responsible for building up the polypeptide chain during DNA synthesis. Thus, the synthesis of structural proteins and virulence factors of the bacterium is disrupted. At the same time, the high specificity to the bacterial ribosome determines the relative safety of macrolides for the human body.

Comparison of macrolides and antibiotics of other classes

Macrolides are similar in properties to tetracyclines, but safer. They do not disrupt the development of the skeleton in childhood. Like tetracyclines with fluoroquinolones, macrolides (the list of drugs is presented above) are able to penetrate into the cell and create therapeutic concentrations in three compartments of the body. This is important in the treatment of mycoplasmal pneumonia, legionellosis, campylobacteriosis, and at the same time, macrolides are safer than fluoroquinolones, although they are less effective.

All macrolides are more toxic than penicillins, but the safest in terms of the likelihood of developing allergies. At the same time, they are champions in safety, but tend to cause allergies. Thus, having a similar spectrum of antimicrobial activity, macrolides can replace aminopenicillins in infections of the respiratory system. Moreover, laboratory studies show that macrolides reduce the effectiveness of penicillins when taken together, although modern treatment protocols allow their combination.

Macrolides during pregnancy and in pediatric therapy

Macrolides are safe drugs along with cephalosporins and penicillins. This allows them to be used during pregnancy and in the treatment of children. They do not disrupt the development of the bone and cartilage skeleton, do not have teratogenic properties. Only azithromycin should be limited in use in the third trimester of pregnancy. In pediatric therapy, both penicillins, and cephalosporins, and macrolides, the list of which is indicated in the standard protocols for the treatment of diseases, can be used without the risk of toxic damage to the body.

Description of some macrolides

Macrolides (preparations listed above) are widely used in clinical practice, including in the CIS. Most often, 4 of their representatives are used: clarithromycin and azithromycin, midecamycin and erythromycin. Spiramycin is used much less frequently. The effectiveness of macrolides is approximately the same, although it is achieved in different ways. In particular, clarithromycin and midecamycin must be taken twice a day to achieve a clinical effect, while azithromycin acts for 24 hours. One dose per day is enough for the treatment of infectious diseases.

Erythromycin is the shortest of all macrolides. It should be taken 4-6 times a day. Therefore, it is most often used in the form of topical forms for the treatment of acne and skin infections. It is noteworthy that macrolides for children are safe, although they can cause diarrhea.