Antibacterial drugs for pneumonia

The basis for the treatment of acute pneumonia is the appointment of antibacterial agents. Etiotropic treatment should satisfy the following conditions:

• treatment should be prescribed as soon as possible, before identification and identification of the pathogen;
• treatment should be carried out under clinical and bacteriological control with the definition of the pathogen and its sensitivity to antibiotics;
• antibacterial agents should be given in optimal doses and at such intervals to ensure the creation of a therapeutic concentration in the blood and lung tissue;
• treatment with antibacterial drugs should continue until the disappearance of intoxication, normalization of body temperature (at least 3-4 days of persistently normal temperature), physical data in the lungs, resorption of inflammatory infiltration in the lungs according to X-ray study. The presence of clinical and radiological "residual" phenomena of pneumonia is not a basis for the continuation of antibiotic therapy. According to the Consensus on pneumonia of the Russian National Congress of Pulmonology (1995), the duration of antibiotic therapy is determined by the type of pathogen of pneumonia. Uncomplicated bacterial pneumonia is treated 3-4 days after the normalization of body temperature (under the condition of normalization of the leukocyte formula) and 5 days if azithromycin is used (not prescribed for signs of bacteremia). The duration of antibiotic therapy for mycoplasmal and chlamydial pneumonia is 10-14 days (5 days if azithromycin is used). Legionellosis pneumonia is treated with antilegionellar drugs for 14 days (21 days in patients with immunodeficiency states).
• in the absence of the effect of the antibiotic for 2-3 days, it is changed, in case of severe pneumonia, antibiotics are combined;
• unacceptable uncontrolled use of antibacterial agents, as this increases the virulence of the pathogens of infection and forms that are resistant to drugs;
• with prolonged use of antibiotics in the body, a deficiency of B vitamins can result in a violation of their synthesis in the intestines, which requires correction of vitamin imbalance by additional administration of appropriate vitamins; it is necessary to diagnose candidomycosis and intestinal dysbacteriosis in time, which can develop in the treatment with antibiotics;
• in the course of treatment, it is advisable to monitor the immune status indicators, since antibiotic treatment can cause inhibition of the immune system, which contributes to the long-term existence of the inflammatory process.

Criteria for the effectiveness of antibiotic therapy

Criteria for the effectiveness of antibiotic therapy are primarily clinical signs: a decrease in body temperature, a decrease in intoxication, an improvement in the general condition, normalization of the leukocyte formula, a decrease in the amount of pus in the sputum, a positive dynamics of auscultatory and roentgenological data. Efficacy is assessed after 24-72 hours. Treatment does not change if there is no impairment.

Fever and leukocytosis may persist for 2-4 days, physical data - more than a week, radiographic signs of infiltration - 2-4 weeks from the onset of the disease. X-ray data often deteriorate during the initial treatment period, which is a serious predictor of patients with severe disease.

Among the antibacterial agents used as etiotropic in acute pneumonia, we can distinguish:

• penicillins;
• cephalosporins;
• monobactams;
• carbapenems;
• aminoglycosides;
• tetracyclines;
• macrolides;
• levomycetin;
• lincosamines;
• anamycin;
• polypeptides;
• fuzidine;
• novobiocin;
• phosphomycin;
• quinolones;
• nitrofurans;
• imidazoles (metronidazole);
• phytoncides;
• sulfonamides.

[1], [2], [3], [4], [5],

Beta-lactam antibiotics

[6], [7], [8], [9], [10]

Group of penicillins

The mechanism of action of penicillins is to suppress the biosynthesis of the peptidoglycan of the cell membrane, which protects the bacteria from the surrounding space. The beta-lactam antibiotic fragment serves as a structural analog of alanyl aniline, a component of murano acid that cross-links with peptide chains in the peptidoglycan layer. Violation of the synthesis of cell membranes leads to the inability of the cell to resist the osmotic gradient between the cell and the environment, so the microbial cell swells and breaks. Penicillins have a bactericidal effect only on multiplying microorganisms, because in resting, no new cell membranes are built. The main protection of bacteria from penicillins is the production of the enzyme beta-lactamase, which opens the beta-lactam ring and the inactivating antibiotic.

Classification of beta-lactamases depending on their effect on antibiotics (Richmond, Sykes)

• I-class β-lactamase, cleavage of cephalosporins
• II-class β-lactamase, cleavage penicillins
• II-class β-lactamase, splitting various broad-spectrum antibiotics
• lV-class
• V-class β-lactamase, cleavage of isoxazolylpenicillins (oxacillin)

In 1940, Abraham and Chain discovered in E. Coli, an enzyme that cleaves penicillin. Since that time, a large number of enzymes have been described that cleave the beta-lactam ring of penicillin and cephalosporins. They are called beta-lactamase. This is a more correct name than penicillinase. β-Lactamases differ in molecular weight, isoelectric properties, sequence of amino acids, molecular structure, relationships with chromosomes and plasmids. The harmlessness of penicillins for humans is due to the fact that human cell membranes differ in structure and are not exposed to the action of the drug.

The first generation of penicillins (natural, natural penicillins)

The spectrum of action: gram-positive bacteria ( staphylococcus aureus, streptococcus, pneumococcus, anthrax, gangrene, diphtheria, lerella); Gram-negative bacteria (meningococci, gonococci, proteus, spirochetes, leptospira).

Resistant to the action of natural penicillins: Gram-negative bacteria (enterobacteria, pertussis, Pseudomonas aeruginosa, Klebsiella, hemophilic rod, legionella, and staphylococci, which produce the enzyme beta-lactamase, brucellosis, tularemia, plague, cholera), tubercle bacilli.

Benzylpenicillin sodium salt is available in vials of 250,000 units, 500,000 units, 1,000,000 units. The average daily dose is 6,000,000 units (1,000,000 every 4 hours). The maximum daily dose is 40,000,000 units or more. The drug is administered intramuscularly, intravenously, intraarterially.

Benzylpenicillin potassium salt - the form of release and dosage are the same, the drug can not be administered intravenously and endolumbally.

Benzylpenicillin novocaine salt (novocillin) - the form of release is the same. The drug is administered only intramuscularly, has an extended action, can be administered 4 times a day for 1 million units.

Phenoxymethylpenicillin - tablets of 0.25 g. It is applied inside (not destroyed by gastric juice) 6 times a day. The average daily dose is 1-2 g, the maximum daily dose is 3 g or more.

The second generation of penicillins (semisynthetic penicillin-resistant anti-staphylococcal antibiotics)

The second generation of penicillins was obtained by adding to the 6-aminopenicillanic acid an acyl side chain. Some staphylococci produce an enzyme β-lactamase, which interacts with the β-lactam ring of penicillins and opens it, which leads to the morning antibacterial activity of the drug. The presence in the preparations of the second generation of the side acyl chain protects the beta-lactam ring of the antibiotic from the action of beta-lactamase bacteria. Therefore, second-generation drugs are primarily intended for the treatment of patients with penicillinase-producing staphylococcus infection. These antibiotics are also active against other bacteria in which penicillin is effective, but it is important to know that benzylpenicillin is significantly more effective in these cases (more than 20 times with pneumococcal pneumonia). In this regard, with a mixed infection, it is necessary to prescribe benzylpenicillin and a drug resistant to β-lactamase. To penicillins of the second generation are resistant pathogens resistant to the action of penicillin. Indications for the appointment of penicillins of this generation are pneumonia and other infectious diseases of staphylococcal etiology.

Oxacillin (prostaflin, resistin, stapenor, bristopen, bactoacyl) is available in 0.25 and 0.5 g bottles, as well as in tablets and capsules at 0.25 and 0.5 g. It is administered intravenously, intramuscularly, orally every 4-6 hours. The average daily dose at The pneumonia is 6 g. The highest daily dose is 18 g.

Dikloxacillin (dinapen, dicill) - an antibiotic, close to oxacillin, containing in its molecule 2 chlorine atoms, penetrates well into the cell. It is used intravenously, intramuscularly, inside every 4 hours. The average daily therapeutic dose is 2 g, the maximum daily dose is 6 g.

Cloxacillin (tegopen) is a drug close to dicloxacillin, but contains one chlorine atom. It is applied intravenously, intramuscularly, inside every 4 hours. The average daily therapeutic dose is 4 g, the maximum daily dose is 6 g.

Flukloxacillin - an antibiotic, close to dicloxacillin, contains in its molecule one atom of chlorine and fluorine. It is applied intravenously, intramuscularly every 4-6 h, the average daily therapeutic dose is 4-8 g, the maximum daily dose is 18 g.

Cloxacillin and flucloxacillin, in comparison with oxacillin, produce a higher concentration in the serum. The ratio of blood concentrations after the administration of high doses of oxacillin, cloxacillin, dicloxacillin into the vein is 1: 1.27: 3.32

Dicloxacillin and oxacillin are metabolized predominantly in the liver, so they are more preferred for use in renal failure.

Nafcillin (nafzil, unipen) is administered intravenously, intramuscularly every 4-6 hours. The average daily dose is 6 g. The highest daily dose is 12 g.

The third generation of penicillins is a semi-synthetic penicillin with a broad spectrum of action

Penicillins of the third generation actively suppress Gram-negative bacteria. With regard to gram-negative bacteria, their activity is lower than that of benzylpenicillin. But somewhat higher than that of the second generation penicillins. The exception is staphylococcus, producing beta-lactamase, for which penicillin of a wide spectrum does not work.

Ampicillin (pentrexil, omnipen) - is available in tablets, capsules of 0.25 g and in bottles of 0.25 and 0.5 g. It is administered intramuscularly, intravenously every 4-6 hours. The average daily dose of the drug is 4-6 g. The highest daily dose - 12 g. Ampicillin is resistant to Pseudomonas aeruginosa, penicillinase-forming staphylococci and indole-positive strains of Proteus.

Ampicillin penetrates well into the bile, sinuses of the nose and accumulates in the urine, its concentrations in the sputum and lung tissue are low. The drug is most indicated for urogenital infections, and it does not have a nephrotoxic effect. However, in renal failure, the dose of ampicillin is recommended to reduce or increase the intervals between drug administrations. Ampicillins in optimal doses are also effective for pneumonia, but the duration of treatment is 5-10 days or more.

Cyclacillin (cyclopen) is a structural analogue of ampicillin. Assigned inside every 6 hours. The average daily dose of the drug is 1-2 g.

Pivampticillin - pivaloyloxymethyl ester of ampicillin - is hydrolyzed by nonspecific esterases in the blood and intestines to ampicillin. The drug is absorbed from the intestine better than ampicillin. It is administered internally in the same doses as ampicillin.

Bacampicillin (penglab, spectrobide) refers to the precursors that release ampicillin in the body. Assigned inside every 6-8 hours. The average daily dose is 2.4-3.2 g.

Amoxicillin is an active metabolite of ampicillin and is taken internally every 8 hours. The average daily dose is 1.5-3 g. The drug is more easily absorbed in the intestine compared to ampicillin and administered at the same dose creates a doubled concentration in the blood, its activity against sensitive bacteria in 5 -7 times higher, by the degree of penetration into the lung tissue it exceeds ampicillin.

Augmentin - a combination of amoxicillin and clavulanic acid.

Clavulanic acid is a β-lactam derivative produced by Streptomyces clavuligerus. Clavulanic acid binds (inhibits) β-lactamase (penicillinase) and, thus, competitively protects penicillin, potentiating its action. Amoxicillin, potentiated with clavulanic acid, is suitable for the treatment of respiratory and urinary tract infections caused by β-lactamase-producing microorganisms, as well as in the case of an infection resistant to amoxicillin.

Produced in tablets, one tablet contains 250 mg of amoxicillin and 125 mg of clavulanic acid. It is prescribed for 1-2 tablets 3 times a day (every 8 hours).

Unazine is a combination of sodium sulbactam and ampicillin in a 1: 2 ratio. It is used for intramuscular, intravenous injection. It is produced in 10 ml vials containing 0.75 g of substance (0.25 g of sulbactam and 0.5 g of ampicillin); in vials of 20 ml containing 1.5 g of the substance (0.5 g of sulbactam and 1 g of ampicillin); in vials of 20 ml with 3 g of substance (I g of sulbactam and 2 g of ampicillin). Sulbactam irreversibly suppresses the majority of β-lactamases responsible for the resistance of many bacterial species to penicillins and cephalosporins.

Sulbactam prevents the destruction of ampicillin by resistant microorganisms and has a pronounced synergism when administered with it. Sulbactam also inactivates the penicillin-binding proteins of bacteria such as Staph. Aureus, E. Coli, P. Mirabilis, Acinetobacter, N. Gonorrheae, H. Influenzae, Klebsiella, which leads to a sharp increase in the antibacterial activity of ampicillin. The bactericidal component of the combination is ampicillin. Spectrum of the drug: staphylococci, including penicillinase-producing), pneumococcus, enterococcus, certain types of streptococci, hemophilic rod, anaerobes, E. Coli, Klebsiella, Enterobacter, Neisseria. The drug is diluted with water for injection or 5% glucose, injected slowly intravenously for 3 minutes or drip for 15-30 minutes. The daily dose of unazine is from 1.5 to 12 g for 3-4 injections (every 6-8 hours). The maximum daily dose is 12 g, which is equivalent to 4 g of sulbactam and 8 g of ampicillin.

Ampioks - a combination of ampicillin and oxacillin (2: 1), combines the spectra of the action of both antibiotics. It is produced in tablets, capsules C for oral ingestion of 0.25 g and in vials of 0.1, 0.2 and 0.5 g. It is administered by mouth, intravenously, intramuscularly every 6 hours. The average daily dose is 2-4 g. The maximum daily dose is 8 g.

The fourth generation of penicillins (carboxypenicillins)

The spectrum of action of penicillins of the fourth generation is the same as that of ampicillin, but with the additional property of destroying the Pseudomonas aeruginosa, pseudomonas and indolpositive proteasis. The remaining microorganisms are weaker than ampicillin.

Carbenicillin (pyopen) - the spectrum of action: the same non-positive bacteria that are sensitive to penicillin, and gram-negative bacteria that are sensitive to ampicillin, in addition, the drug acts on Pseudomonas aeruginosa and Proteus. Carbenicillin is resistant to: penicillinase-producing staphylococci, causative agents of gas gangrene, tetanus, protozoa, spirochetes, fungi, rickettsia.

It is produced in vials of 1 g. It is administered intravenously, intramuscularly every 6 hours. The average daily dose is 20 g intravenously, the maximum daily dose is 30 g. The average daily dose is intramuscular - 4 g, the highest daily dose is 8 g.

Carindacillin - carbenicillin indanyle ester, applied internally by 0.5 g 4 times a day. After absorption from the intestine it quickly hydrolyses to carbenicillin and indole.

Carpencilin phenyl ester of carbenicillin, administered orally 0.5 g 3 times a day, in severe cases the daily dose rises to 3 g. Effective for pneumonia and urinary tract infections.

Ticarcillin (ticar) - is similar to carbenicillin, but 4 times more active against Pseudomonas aeruginosa. It is administered intravenously and intramuscularly. Intravenously administered every 4-6 hours, the average daily dose is 200-300 mg / kg, the maximum daily dose is 24 grams. Intramuscularly injected every 6-8 hours, the average daily dose is 50-100 mg / kg, the maximum daily dose - 8 g. Ticarcillin is destroyed by beta-lactamases produced by Pseudomonas aeruginosa, hemophilic, Escherichia coli, proteus, Maracella (Neisseria). The spectrum of action of ticarcillin increases with a combination of ticarcillin and clavulanic acid (timentin). Timentin is highly effective against β-lactamase-producing and beta-lactamase-negative strains of non-negative bacteria.

The fifth generation of penicillins - ureido- and piperazinopenicillins

In ureidopenicillins, a side chain with a urea residue is attached to the ampicillin molecule. Ureidopenicillins penetrate the walls of bacteria, suppress their synthesis, but are destroyed by β-lactamases. The drugs have a bactericidal action and are especially effective against Pseudomonas aeruginosa (8 times more active than carbenicillin).

Azlotsimin (azlin, secular) - a bactericidal antibiotic, is available in 0.5, 1, 2 and 5 g vials, is administered intravenously in the form of a 10% solution. It dissolves in distilled water for injection: 0.5 g dissolves in 5 ml, 1 g in 10 ml, 2 g in 20 ml, 5 g in 50 ml, is intravenously injected slowly or intravenously drip. 10% glucose can be used as the solvent.

The spectrum of the drug: gram-positive flora (pneumococcus, streptococcus, staphylococcus, enterococcus, corynebacteria, clostridia), gram-negative flora (pseudomonas, klebsiella, enterobacter, E. Coli, salmonella, shigella, Pseudomonas aeruginosa, Neisseria, Proteus, Hemophilus rod).

The average daily dose is from 8 g (4 times 2 grams) to 15, (3 times 5 grams each). The maximum daily dose is from 20 g (4 times 5 g) to 24 g.

Mesocillin - in comparison with azlocillin less active against Pseudomonas aeruginosa, but more active against normal Gram-negative bacteria. It is administered intravenously every 4-6 hours, intramuscularly every 6 hours. The average daily dose intravenously is 12-I6 g, the maximum daily dose is 24 g. The average daily dose intramuscularly is 6-8 g, the maximum daily dose is 24 g.

Piperacillin (piprazyl) - has a piperazine grouping in the structure and refers to piperazinopenicillins. The spectrum of action is close to carbenicillin, it is active against Pseudomonas aeruginosae, Klebsiellae, Enterobacter, H.influenzae, Neisseriae, Pseudomonas aeruginosa. β-lactamases produced by S. Aureus destroy piperacillin. Piperacillin is administered intravenously every 4-6 hours, with an average daily therapeutic dose of 12-16 grams, the maximum daily dose is 24 grams. Intramuscularly the drug is injected every 6-12 hours, with an average daily therapeutic dose of 6-8 grams, the maximum daily i dose - 24 g.

It is reported on the release of a combined preparation of piperacillin with a beta-lactamase inhibitor tazobactam, which is most successfully used in the treatment of purulent abdominal lesions.

The sixth generation of penicillins - amidipenicillin and tetracycline

Penicillins of the sixth generation have a wide spectrum of action, but are especially active against gram-negative bacteria, including those resistant to ampicillin.

Amdinotsillin (coactin) - is administered intravenously, intramuscularly at intervals of 4-6 hours. The average daily dose of the drug is 40-60 mg / kg.

Temocillin is a semisynthetic beta-lactam antibiotic. The most effective against enterobacteria, hemophilic rod, gonococcus. To temotsillinu are resistant P. Aeruginosae and B. Fragilis. Resistant to the action of most β-lactamases. When administered intravenously, 1-2 g every 12 hours.

The drug in the body is not metabolized, in the unchanged form is excreted by the kidneys. It often changes with gram-negative sepsis and urinary infection.

All penicillins can cause allergic reactions: bronchospasm, Klinke edema, hives, itching rashes, anaphylactic shock.

Drugs used inside may cause dyspeptic phenomena, pseudomembranous colitis, intestinal dysbacteriosis.

Group of cephalosporins

Preparations of the group cephalosporins are based on 7-aminocephalosporinic acid, the spectrum of antimicrobial effects is wide, now they are increasingly considered as a drug of choice. Antibiotics of this group were first obtained from a cephalosporium fungus isolated from seawater taken in Sardinia near the wastewater discharge site.

The mechanism of action of cephalosporins is close to the mechanism of action of penicillins, since both groups of antibiotics contain a β-lactam ring: a violation of the synthesis of the cell wall of fissile microorganisms due to acetylation of membrane transpeptidases. Cephalosporins have a bactericidal effect. The spectrum of cephalosporins is wide: Gram-positive and non-negative microorganisms (streptococci, staphylococci, including penicillinase-producing, pneumococci, meningococci, gonococci, diphtheria and anthrax, gas gangrene, tetanus, treponema, borellia, a number of Escherichia coli strains, Shigella, Salmonella, klebsiella, individual types of proteas). The bactericidal effect of cephalosporins is enhanced in an alkaline environment.

Classification of cephalosporins used parenterally

1st generation	2nd generation	3rd generation	IV generation
Cefazolin (kefzol) Cephalothin (keflin) Cefradine Cephaloridine (chains) Cefapyrine (cefadil) Cefatón Cephzedon Cefadroxil (duracef)	Cefuroxime sodium (ketoceph) Cefuroxime-acoetyl (zinnate) Cefamandol Tsefanid (preceph) Tsefonitsid (monocid) Cefmenoxime	Cefotaxime sodium (claforan) Cefoperazone (cefobide) Cefsulodin (cefomonide) Cefduaperase Ceftazidime (fortune) Tseftrksson (longacef) Ceftieoxm (cefizone) Cefazidime (Modified) Ceflamizol	Cephazaflur Tsefpyrom (kaiten) Cefemetazole Cefotetan Cefoxytin Cefsulodin (cefomonide) Moxalactam (latamoxef)
High activity against gram-positive bacteria	High activity against Gram-negative bacteria	High activity against Pseudomonas aeruginosa	High activity against bacteroides and other anaerobes

Some new cephalosporins are effective against mycoplasmas, Pseudomonas aeruginosa. They do not act on mushrooms, rickettsia, tubercle bacilli, protozoa.

Cephalosporins are resistant to penicillinase, although many of them are destroyed by cephalosporinase beta-lactamase, produced in contrast to penicillinase by non-Gram positive, and by separate non-negative pathogens).

Cephalosporins used parenterally.

The first generation of cephalosporins

Cephalosporins of the first generation have a high activity against gram-positive cocci, including golden and coagulase-negative staphylococci, beta-hemolytic streptococcus, pneumococcus, green streptococcus. Cephalosporins of the first generation are resistant to the action of staphylococcal beta-lactamase, but are hydrolysed by β-lactamase of gram-negative bacteria, and therefore preparations of this group are not very active against gram-negative cerebral flora (Escherichia coli, Klebsiella, Proteus, etc.).

Cephalosporins of the first generation penetrate well into all tissues, easily pass through the placenta, are found in high concentrations in the kidneys, pleural, peritoneal and synovial exudates, in smaller amounts in the prostate gland and bronchial secretion and practically do not penetrate the blood-brain barrier;

Cefoloridine (chainin, loridine) - is available in vials of 0.25, 0.5 and 1 g. It is administered intramuscularly, intravenously every 6 hours. The average daily dose is 1-2 g, the maximum daily dose is 6 g or more.

Cefaolin (kefzol, cefamezin, acef) - is available in vials of 0.25, 0.5, 1, 2 and 4 grams, is administered intravenously, intramuscularly at intervals of 6-8 hours. The average daily dose is 3-4 g, the maximum daily dose

Cephalotin (keflin, zeffin) - is available in 0.5, 1 and 2 g. Bottles. It is administered intramuscularly, intravenously at intervals of 4-6 hours. The average daily dose is 4-6 g, the maximum daily dose is 12 g.

Tsefapirin (cefadil) - is administered intravenously, intramuscularly every 6 hours. The average daily dose of the drug is 2-4 g, the maximum daily dose is 6 g or more.

The second generation of cephalosporins

Cephalosporins of the second generation have predominantly high activity against Gram-negative bacteria (Escherichia coli, Klebsiella, Proteus, Enterobacter, Hemophilus rod, etc.), as well as gonococci, Neisseria. Preparations of this group are resistant to several or all of the resulting beta-lactamases and to several chromosomal beta-lactamases produced by Gram-negative bacteria. Some cephalosporins of the second generation are resistant to the action of beta-lactamases and other bacteria.

Cefamandol (mandol) - is available in vials of 0.25; 0.5; 1.0 g, is administered intravenously, intramuscularly at intervals of 6 hours. The average daily dose is 2-4 g, the maximum daily dose is 6 g or more.

Tsefanid (preceph) - is administered intravenously, intramuscularly at intervals of 12 hours. The average daily dose is 1 g, the maximum daily dose is 2 g.

Cefuroxime sodium (ketocef) - is available in vials containing 0.75 g and 1.5 g of dry matter. It is administered intramuscularly or intravenously after dilution with the applied solvent at intervals of 6-8 hours. The average daily dose is 6 g, the maximum is 9 g.

Tsefonitsid (monitsid) - used intravenously, intramuscularly once a day in a dose of 2 g.

The third generation of cephalosporins

Preparations of the third generation have a large Gram-negative activity, i.e. Highly active against indolpositive strains of the protein, Pseudomonas aeruginosa, bacteroides (anaerobes, which play an important role in the development of aspiration pneumonia, wound infections, osteomyelitis), but are inactive for coccal infections, in particular staphylococcal and enterococcal. Highly resistant to the action of β-lactamases.

Cefotaxime (claforan) - is available in 1 g vials, used intravenously, intramuscularly at intervals of 6-8 hours. The average daily dose is 4 g, the maximum daily dose is 12 g.

Ceftriaxone (longatef) is used intravenously, intramuscularly at intervals of 24 hours. The average daily dose is 2 g, the maximum is 4 g. Sometimes it is applied at intervals of 12 hours.

Ceftizoksim (cefizone, epocelin) - is available in 0.5 and 1 g bottles, it is administered at intervals of 8 hours. The average daily dose is 4 g, the maximum daily dose is 9-12 g. Epocelin is recommended by the manufacturer of its company (Japan) in daily a dose of 0.5-2 g in 2-4 injections, in severe cases - up to 4 g per day.

Cefadizim (mod.) Is a broad-spectrum preparation due to the presence in the cephalosporin nucleus of the iminomethoxy and aminothiazole group and the dihydrotiazine ring. Effective against non-positive and gram-negative microorganisms, including both aerobes and anaerobes (Staphylococcus aureus, pneumococcus, Streptococcus, Neisseria, Escherichia coli, Proteus, Salmonella, Haemophilus influenzae). It is resistant to the action of most beta-lactamases, is not metabolized, is excreted mainly through the kidneys, it is recommended for use in urology and pulmonology. Modivid significantly stimulates the immune system, increases the number of T-lymphocytes-helleras, as well as phagocytosis. The drug is ineffective against pseudomonas, mycoplasmas, chlamydia.

The drug is administered intravenously or intramuscularly 2 times a day in a daily dose of 2-4 g.

Cefoperazone (cefobide) - is administered intravenously, intramuscularly every 8-12 hours, the average daily dose is 2-4 g, the maximum daily dose is 8 g.

Ceftazidime (kefadim, fortum) - is released in ampoules of 0.25, 0.5, 1 and 2 g. It dissolves in water for injection. It is administered intravenously, intramuscularly at intervals of 8-12 hours. You can prescribe 1 g of the drug every 8-12 hours. The average daily dose is 2 g, the maximum daily dose is -6 g.

Ceftazidime (fortum) is well combined in one injection with metrogil: 500 mg of Fortum in 1.5 ml of water for injection + 100 ml of 0.5% solution (500 mg) of metrogyl.

The fourth generation of cephalosporins

Preparations of the fourth generation are resistant to the action of β-lactamases, characterized by a wide spectrum of antimicrobial activity (Gram-positive bacteria, non-negative bacteria, bacteroides), as well as antipseudomonas activity, but enterococci are resistant to them.

Moxalactom (moksam, latamokcef) - has a high activity against most Gram-positive and Gram-negative aerobes, anaerobes, Klebsiella, Escherichia coli, Pseudomonas aeruginosa, moderately active against Staphylococcus aureus. It is used intravenously, intramuscularly every 8 hours, the average daily dose of 2 g, the maximum daily dose of 12 g. Possible side effects are diarrhea, hypoprothrombinemia.

Cefoxytin (mefoksin) - is active mainly against bacteroids and bacteria close to them. In relation to non-positive and Gram-negative microorganisms is less active. Apply most often with anaerobic infection intramuscularly or intravenously every 6-8 hours for 1-2 g.

Cefotetan - is quite active against gram-positive and gram-negative microbes, is inactive against enterococci. It is used intravenously, intramuscularly 2 g 2 times a day, the highest daily dose is 6 g.

Tsefpyrom (kaiten) - is characterized by a well-balanced activity in both gram-positive and gram-negative microorganisms. Tsefpyrom is the only one of cephalosporin antibiotics, which possess significant activity against enterococci. The drug is significantly superior in activity to all the third generation cephalosporins with respect to staphylococci, enterobacteria, klebsiella, escherichia, comparable to ceftazidime in activity against Pseudomonas aeruginosa, has a high activity against the hemophilic rod. Cephpir is highly resistant to major beta-lactamases, including broad-spectrum plasmid β-lactamases, inactivating cefazidime, cefotaxime, ceftriaxone and other third generation cephalosporins.

Tsefpirom is used for severe and extremely severe infections of various locations in patients in intensive care and resuscitation departments, with infectious inflammatory processes that have developed against neutropenia and immunosuppression. With septicemia, severe infections of the bronchopulmonary system and urinary tract.

The drug is used only intravenously struino or drip.

The contents of the vial (1 or 2 g of cefpyrom) are dissolved respectively into 10 or 20 ml of water for injection and the resulting solution is injected into the vein for 3-5 minutes. The drip introduction into the vein is carried out as follows: the contents of the vial (1 or 2 g of cefpyrom) are dissolved in 100 ml of isotonic sodium chloride solution or 5% glucose solution and injected into the drip for 30 minutes.

Drug tolerance is good, however, in rare cases, allergic reactions, skin rashes, diarrhea, headache, drug fever, pseudomembranous colitis are possible.

Oral cephalosporins of the first generation

Cefalexin (chainex, ceflex, oraccef) - is released in capsules of 0.25 g, applied internally every 6 hours. The average daily dose is 1-2 g, the maximum daily dose is 4 g.

Cefradine (anspora, velotsef) - is administered internally at intervals of 6 h (according to some data - 12 h). The average daily dose is 2 g, the maximum daily dose is 4 g.

Cefadroxil (duracef) - is available in capsules of 0.2 g, is administered orally at intervals of 12 hours. The average daily dose is 2 g, the maximum daily dose is 4 g.

Oral cephalosporins of the second generation

Cefaclor (tseklor, panorel) - is available in capsules of 0.5 g, applied internally at intervals of 6-8 hours. For pneumonia, 1 capsule is prescribed 3 times a day, in severe cases - 2 capsules 3 times a day. The average daily dose of the drug is 2 g, the maximum daily dose is 4 g.

Cefuroxime-aksetil (zinnat) - is available in tablets at 0.125; 0.25 and 0.5 g. It is used for 0.25-0.5 g 2 times a day. Cefuroxime-axetil is a prodrug form, which after absorption is converted into an active cefuroxime.

Lorakarbef - applied inside of 0.4 g 2 times a day.

Oral cephalosporins of the third generation

Cefsulodin (monaspora, cefomonid) - is administered internally at intervals of 6-12 hours. The average daily dose is 2 g, the maximum daily dose is 6 g.

Ceftibuten - applied inside of 0.4 g 2 times a day. Has a pronounced activity against gram-negative bacteria and is resistant to the action of beta-lactamases.

Cefpodoxime proksetil - applied inside of 0.2 g 2 times a day.

Cepetamet pivoksil - applied internally on 0.5 g 2 times a day. Effective against pneumococcus, streptococcus, hemophilic rod, moraxella; Ineffective against staphylococci, enterococci.

Cefixime (suprax, cefspane) - applied internally by 0.2 g 2 times a day. To cefixime pneumococci, streptococci, hemophilic rod, intestinal daddy, Neisseria are highly sensitive; resistant - enterococci, Pseudomonas aeruginosa, staphylococci, enterobacter.

Cephalosporins can cause the following adverse reactions: a cross-allergy with penicillins in 5-10% of patients;

• allergic reactions - urticaria, korepodobnoyu rash, fever, eosinophilia, serum sickness, anaphylactic shock;
• in rare cases - leukopenia, hypoprothrombinemia and bleeding;
• increase in the content of transaminases in the blood; dyspepsia.

Group of monobactams

Monobactams are a new class of antibiotics derived from Pseudomonas acidophil and Chromobacterinum violaceum. At the heart of their structure is a simple beta-lactam ring, unlike related penicillins and cephalosporins, constructed from a beta-lactam ring conjugated with a thiazolidine, in this connection, new compounds have been called monobactams. They are exceptionally resistant to the action of β-lactamases produced by a non-negative flora, but are destroyed by beta-lactamase produced by staphylococci and bacteroides.

Aztreonam (azactam) - the drug is active against a large number of Gram-negative bacteria, including Escherichia coli, Klebsiella, Proteus and Pseudomonas aeruginosa, may be active if infected with resistant microorganisms or hospital infections caused by them; However, the drug does not have significant activity against staphylococci, streptococci, pneumococci, bacteroides. It is administered intravenously, intramuscularly at intervals of 8 hours. The average daily dose is 3-6 g, the maximum daily dose is 8 g.

Group of carbapenems

Imipenem-cilostine (thienam) is a broad-spectrum beta-lactam drug consisting of two components: tienamycin antibiotic (carbapenem) and cilastine, a specific enzyme that inhibits the metabolism of imipenem in the kidneys and significantly increases its concentration in the urinary tract. The ratio of imipenem and cilastine in the preparation is 1: 1.

The drug has a very wide range of antibacterial activity. It is effective against gram-negative flora (enterobacter, hemophilic rod, klebsiella, neisseria, proteus, pseudomonas, salmonella, iersinia, acinethobacter, gram-positive flora (all staphylococci, streptococci, pneumococci), as well as anaerobic flora .Imipenem has a pronounced stability to action β-lactamases (penicillinases and cephalosporinases) produced by Gram-positive and Gram-negative bacteria The drug is used for severe Gram-positive and Gram-negative infections caused by plaque Resistant and intrahospital strains of bacteria: sepsis, peritonitis, staphylococcal destruction of lungs, peritoneal pneumonia caused by klebsiella, acitetobacter, enterobacter, hemophilic rod, serration, Escherichia coli. Especially effective is imipenem in the presence of polymicrobial flora.

Group of aminoglycosides

Aminoglycosides contain in their molecule aminosugars, connected by a glycosidic bond. These features of the structure of aminoglycosides explain the name of this group of antibiotics. Aminoglycosides have bactericidal properties, they act inside the cell of microorganisms, bind to ribosomes and break down the amino acid sequence in the peptide chains (the resulting abnormal proteins are fatal to microorganisms). They can have varying degrees of nephrotoxicity (in 17% of patients) and ototoxic effect (in 8% of patients). According to DR Lawrence, hearing loss often occurs in the treatment of amikacin, neomycin and kanamycin, vestibular toxicity is characteristic of streptomycin, gentamicin, tobramischin. Ringing in the ears can serve as a warning about the defeat of the auditory nerve. The first signs of involvement in the process of the vestibular apparatus are a headache associated with movement, dizziness, nausea. Neomycin, gentamicin, amikacin are more nephrotoxic than tobramycin and netilmicin. The least toxic drug is netilmicin.

To prevent side effects of aminoglycosides, monitor serum aminoglycoside levels and record the audiogram once a week. For the early diagnosis of nephrotoxic action of aminoglycosides, it is recommended to determine the fractional excretion of sodium, N-acetyl-beta-D-glucosaminidase and beta2-microglobulin. If there is a violation of kidney function and hearing, aminoglycosides should not be prescribed. Aminoglycosides have a bactericidal effect, the severity of which depends on the concentration of the drug in the blood. In recent years, it has been suggested that a single dose of aminoglycoside at a higher dose is effective in connection with an increase in bactericidal activity and an increase in the duration of the postantibacterial effect, while the incidence of side effects decreases. According to Tulkens (1991), the single administration of netilmicin and amikacin was not inferior in effectiveness to a 2-3-fold administration, but less frequently was accompanied by impaired renal function.

Aminoglycosides are wide-spectrum antibiotics: they affect gram-positive and gram-negative flora, but their high activity in relation to the majority of Gram-negative bacteria is of the greatest practical importance. They have a pronounced bactericidal effect on Gram-negative aerobic bacteria (pseudomonas, enterobacter, Escherichia coli, Proteus, Klebsiella), but are less effective against the hemophilic rod.

The main indications for the administration of aminoglycosides are rather severe infections (in particular, hospital infections caused by non-negative bacteria (pneumonia, urinary tract infections, septicemia), in which they are the means of choice .In severe cases, aminoglycosides are combined with anti-synergic penicillins or cephalosporins.

In the treatment with aminoglycosides, the development of microflora resistance to them is possible, which is due to the ability of microorganisms to produce specific enzymes (5 types of aminoglycosidase acetyltransferases, 2 types of aminomycosphosphate transferases, aminoglycoside nucleotide transferase) that inactivate aminoglycosides.

Aminoglycosides II and III generations have higher antibacterial activity, a broader antimicrobial spectrum and greater resistance to enzymes that inactivate aminoglycosides.

The resistance to aminoglycosides in microorganisms is partially cross-linked. Microorganisms resistant to streptomycin and kanamycin are also resistant to monomycin, but are sensitive to neomycin and all other aminoglycosides.

Flora, resistant to aminoglycosides of the first generation, is sensitive to gentamycin and III aminoglycosides. Gentamycin resistant strains are also resistant to monomycin and kanamycin, but are sensitive to aminoglycosides of the third generation.

There are three generations of aminoglycosides.

The first generation of aminoglycosides

Of the first-generation drugs, kanamycin is most commonly used. Kanamycin and streptomycin are used as anti-tuberculosis drugs, neomycin and monomycin because of high toxicity, they are not used parenterally, they are prescribed inside. And intestinal infections. Streptomycin - available in 0.5 and 1 g bottles is given intramuscularly every 12 hours. The average daily vine is 1 g. The maximum daily dose is 2 g. For the treatment of pneumonia, it is almost not currently used, it is used mainly for tuberculosis.

Kanamycin - is available in tablets of 0.25 g and in vials for intramuscular injection of 0.5 and I g. Just like streptomycin, it is used primarily for tuberculosis. It is administered intramuscularly at intervals of 12 hours. The average daily dose of the drug is 1-1.5 g, the maximum daily dose is 2 g.

Monomycin - is released in tablets of 0.25 g, bottles of 0.25 and 0.5 g. It is administered intramuscularly at intervals of 8 hours. The average daily dose is 0.25 g, the maximum daily dose is 0.75 g. Pneumococci acts poorly, it is used mainly for intestinal infections.

Neomycin (kolomitsin, mizirin) - is available in tablets of 0.1 and 0.25 g and 0.5 g bottles. It is one of the most active antibiotics that suppress the intestinal bacterial flora in liver failure. It is applied internally by 0.25 g 3 times a day inside or intramuscularly at 0.25 g 3 times a day.

The second generation of aminoglycosides

The second generation of aminoglycosides is represented by gentamycin, which unlike first-generation drugs has a high activity against Pseudomonas aeruginosa and acts on strains of microorganisms that developed resistance to first-generation aminoglycosides. The antimicrobial activity of gentamicin is higher than that of kanamycin.

Gentamicin (Garamycin) - is issued in ampoules of 2 ml of 4% solution, bottles of 0.04 g of dry matter. It is used intramuscularly, in severe cases intravenously at intervals of 8 hours. The average daily dose is 2.4-3.2 mg / kg, the maximum daily dose is 5 mg / kg (this dose is prescribed in case of a severe condition of the patient). Usually used in a dose of 0.04-0.08 g intramuscularly 3 times a day. Gentamicin is active against aerobic Gram-negative bacteria, Escherichia coli, enterobacteria, pneumococcus, Proteus, Pseudomonas aeruginosa, but is weakly active against streptococci, enterococci and is inactive in anaerobic infection. In the treatment of septicemia, gentamicin is combined with one of beta-lactam antibiotics or antianaerobic drugs, for example, metronidazole or with one and / or another.

The third generation of aminoglycosides

The third generation of aminoglycosides is stronger than gentamicin, inhibits Pseudomonas aeruginosa, the secondary resistance of flora to these drugs is much less common than to gentamicin.

Tobramycin (brulamycin, obrazin) - is issued in ampoules of 2 ml in the form of a ready-made solution (80 g of the drug). It is used intravenously, intramuscularly at intervals of 8 hours. The doses are the same as gentamycin. The average daily dose for pneumonia is 3 mg / kg, the maximum daily dose is 5 mg / kg

Sizomycin - available in ampoules of 1, 1.5 and 2 ml of a 5% solution. It is administered intramuscularly at intervals of 6-8 hours, intravenous administration should be drip in a 5% glucose solution. The average daily dose of the drug is 3 mg / kg. The maximum daily dose is 5 mg / kg.

Amikacin (amikin) - is released in ampoules of 2 ml, which contain 100 or 500 mg of the drug, is administered intravenously, intramuscularly at intervals of 8-12 hours. The average daily dose is 15 mg / kg, the maximum daily dose is 25 mg / kg. Amikacin is the most effective preparation among aminoglycosides of the third generation, unlike all other aminoglycosides, it is sensitive to only one inactivating enzyme, while the rest is at least five. Strains resistant to amikacin are resistant to all other aminoglycosides.

Nethylmicin is a semisynthetic aminoglycoside, it is active in infection with some strains resistant to gentamicin and tobramycin, it is less oto- and nephrotoxic. It is administered intravenously, intramuscularly at intervals of 8 hours. The daily dose of the drug is 3-5 mg / kg.

By the degree of decrease in the antimicrobial effect, the aminoglycosides are arranged as follows: amikacin-netilmicin-gentamicin-tobramycin-streptomycin-neomycin-kanamycin-monomycin.

Group of tetracyclines

Antibiotics of this group have a wide spectrum of bacteriostatic action. They affect protein synthesis by binding to ribosomes and stopping the access of complexes consisting of transport RNA with amino acids to complexes of information RNA with ribosomes. Tetracyclines accumulate inside the bacterial cell. By origin, they are divided into natural (tetracycline, oxytetracycline, chlortetracycline or biomycin) and semisynthetic (metacyclin, doxycycline, minocycline, morphocycline, rolitetracycline). Tetracyclines are active in almost all infections caused by gram-negative and gram-positive bacteria, with the exception of most strains of proteium and Pseudomonas aeruginosa. If the stability of microflora develops in the treatment with tetracyclines, then it has a complete cross-type character (with the exception of minocycline), therefore all tetracyclines are prescribed by single indications. Tetracyclines can be used in many common infections, especially mixed infections, or in cases where treatment begins without identification of the pathogen, i.e. With bronchitis and bronchopneumonia. Tetracyclines are especially effective in mycoplasmal and chlamydial infections. In average therapeutic concentrations, tetracyclines are found in the lungs, liver, kidneys, spleen, uterus, tonsils, prostate gland, accumulate in inflamed and tumor tissues. In a complex with calcium are deposited in bone tissue, enamel of teeth.

Natural tetracyclines

Tetracycline - is released in tablets of 0.1 and 0.25 g, appointed at intervals of 6 hours. The average daily dose is 1-2 g, the maximum daily dose is 2 g. Intramuscularly administered 0.1 g 3 times a day.

Oxytetracycline (terramycin) - is administered by mouth, intramuscularly, intravenously. For oral administration is available in tablets of 0.25 g. Inside the drug is used at intervals of 6 h, the average daily dose is 1-1.5 g, the maximum daily dose is 2 g. Intramuscularly the drug is administered at intervals of 8-12 h, the average daily dose is 0.3 g , the maximum dose is 0.6 g. Intravenously the drug is administered at intervals of 12 h, the average daily dose is 0.5-1 g, the maximum dose is 2 g.

Chlortetracycline (biomycin, aureomycin) is used internally, there are forms for intravenous administration. Inside is applied at intervals of 6 hours, the average daily dose of the drug is 1-2 g, maximum -3 g. Intravenously applied at intervals of 12 hours, the average and maximum daily doses - 1 g.

Semisynthetic tetracyclines

Metacyclin (rondomycin) - is available in capsules of 0.15 and 0.3 g, administered internally at intervals of 8-12 hours. The average daily dose is 0.6 g, the maximum is 1.2 g.

Doxycycline (vibramycin) - is released in capsules of 0.5 and 0.1 grams, in ampoules for intravenous administration of 0.1 g. Inside is applied to 0.1 g 2 times a day, in the following days - 0.1 g / day, in severe cases, the daily dose to the first and the next days is 0.2 g.

For intravenous infusion, 0.1 g of vial powder is dissolved in 100-300 ml of isotonic sodium chloride solution and administered intravenously drip for 30-60 minutes 2 times a day.

Minocycline (clinomycin) is administered internally at intervals of 12 hours. On the first day, the daily dose is 0.2 g, in the following days - 0.1 g, a brief daily dose can be increased to 0.4 g.

Morfocycline - is available in vials for intravenous administration of 0.1 and 0.15 g, is administered intravenously at intervals of 12 hours in a 5% solution of glucose. The average daily dose of the drug is 0.3 g, the maximum daily dose is 0.45 g.

Roilititracycline (velacycline, reverin) - the drug is administered intramuscularly 1-2 times a day. The average daily dose is 0.25 g, the maximum daily dose is 0.5 g.

The incidence of side effects with tetracyclines is 7-30%. The toxic complications due to the catabolic action of tetracyclines predominate: hypotrophy, hypovitaminosis, liver, kidney, gastrointestinal ulcer, photosensitivity of the skin, diarrhea, nausea; complications associated with the suppression of saprophytes and the development of secondary infections (candidiasis, staphylococcal enterocolitis). Children up to 5-8 years of tetracyclines are not prescribed.

In the treatment of tetracyclines, VG Kukes recommends the following:

• between them there is a cross allergy, patients with allergies to local anesthetics can react to oxytetracycline (often injected on lidocaine) and tetracycline hydrochloride for intramuscular injection;
• tetracyclines can cause increased catecholamine excretion in the urine;
• they cause an increase in the level of alkaline phosphatase, amylase, bilirubin, residual nitrogen;
• it is recommended to take tetracyclines inwards on an empty stomach or 3 hours after eating, squeezing 200 ml of water, which reduces the irritating effect on the wall of the esophagus and intestines, improves absorption.

Group of macrolides

Preparations of this group contain in the molecule a macrocyclic lactone ring linked to carbohydrate residues. These are predominantly bacteriostatic antibiotics, but depending on the type of pathogen and concentration, they may exhibit a bactericidal effect. The mechanism of their action is analogous to the mechanism of action of tetracyclines and is based on binding to ribosomes and preventing access of a complex of transport RNA with an amino acid to a complex of information RNA with ribosomes, which leads to suppression of protein synthesis.

Highly sensitive to macrolides are non-positive cocci (pneumococcus, pyogenic streptococcus), mycoplasma, legionella, chlamydia, whooping cough stick Bordetella pertussis, diphtheria bacillus.

Moderately sensitive to macrolides, hemophilic rod, staphylococcus, resistant - bacteroides, enterobacteria, rickettsia.

The activity of macrolides against bacteria is related to the structure of the antibiotic. There are macrolides 14-membered (erythromycin, oleandomycin, fluoritromycin, clarithromycin, megalomycin, dirithromycin), 15-membered (azithromycin, roxitramycin), 16-membered (spiramycin, yozamycin, rozamycin, tourimycin, myocamecin). 14-member macrolides possess a higher bactericidal activity than the 15-membered ones, with respect to streptococci and pertussis. Clarithromycin has the greatest effect against streptococci, pneumococci, diphtheria bacillus, azithromycin is highly effective against hemophilic rod.

Macrolides are highly effective in respiratory infections and pneumonia, as they penetrate well into the mucous membrane of the bronchopulmonary system, bronchial secretions and sputum.

Macrolides are effective against pathogens located intracellularly (in tissues, macrophages, leukocytes), which is especially important in the treatment of legionella and chlamydia infection, since these pathogens are located intracellularly. Macrolides can develop resistance, so they are recommended to be used as part of combination therapy for severe infection, for resistance to other antibacterial drugs, for allergic reactions or hypersensitivity to penicillins and cephalosporins, and for mycoplasmal and chlamydial infections.

Erythromycin - is available in tablets of 0.1 and 0.25 g, capsules of 0.1 and 0.2 g, vials for intramuscular and intravenous administration of 0.05, 0.1 and 0.2 g. It is administered by mouth, intravenously, intramuscularly.

Inside is applied at intervals of 4-6 hours, the average daily dose is 1 g, the maximum daily dose is 2 g. Intramuscularly and intravenously is applied at intervals of 8-12 hours, the average daily dose is 0.6 g, the maximum is 1 g.

The drug, like other macrolides, manifests its effect more actively in the alkaline environment. There is evidence that in the alkaline environment, erythromycin is converted into a broad-spectrum antibiotic that actively suppresses gram-negative bacteria highly resistant to many chemotherapeutic agents, in particular, Pseudomonas aeruginosa, Escherichia, Proteus, Klebsiella. This can be used for infections of the urinary, biliary tract and local surgical infection.

DR Lawrence recommends the use of erythromycin in the following cases:

• with mycoplasmal pneumonia in children - the drug of choice, although for the treatment of adults, tetracycline is preferable;
• for the treatment of patients with legionella pneumonia as a first-line drug alone or in combination with rifampicin;
• with chlamydial infection, diphtheria (including with carriage) and whooping cough;
• with gastroenteritis caused by campylobacteria (erythromycin promotes the elimination of microorganisms from the body, although it does not necessarily shorten the duration of clinical manifestations);
• in patients infected with Pseudomonas aeruginosa, pneumococcus, or with allergies to penicillin.

Ericycline - a mixture of erythromycin and tetracycline. Issued in capsules of 0.25 g, prescribed 1 capsule every 4-6 hours, the daily dose of the drug is 1.5-2 g.

Oleandomycin - is released in tablets of 0.25 g. Take every 4-6 hours. The average daily dose is 1-1.5 g, the maximum daily dose is 2 g. There are forms for intravenous, intramuscular injection, daily doses are the same.

Oletetrin (tetraolyn) is a combined preparation consisting of oleandomycin and tetracycline in a ratio of 1: 2. It is produced in capsules of 0.25 g and in vials of 0.25 g for intramuscular, intravenous administration. Assigned inside by 1-1.5 grams per day in 4 divided doses with 6-hour intervals.

For intramuscular injection, the contents of the vial are dissolved in 2 ml of water or isotonic sodium chloride solution and 0.1 g of the drug is administered 3 times a day. For intravenous administration, 1% solution is used (0.25 or 0.5 g of the drug is dissolved in 25 or 50 ml of isotonic sodium chloride solution or water for injection, respectively, and injected slowly). You can apply intravenous drip infusion. The average daily dose intravenously is 0.5 g 2 times a day, the maximum daily dose is 0.5 g 4 times a day.

In recent years, there have appeared so-called "new" macrolides. Their characteristic feature is a broader spectrum of antibacterial action, stability in an acidic environment.

Azithromycin (sumamed) - refers to the antibiotic group of azamide, close to macrolides, is available in tablets of 125 and 500 mg, 250 mg capsules. Unlike erythromycin, it is a bactericidal antibiotic with a wide spectrum of activity. It is highly effective against gram-positive microbes (pyogenic streptococci, staphylococci, including those producing beta-lactamase, a pathogen of diphtheria), moderately active against enterococci. Effective against gram-negative pathogens (hemophilia, pertussis, E. Coli, shigella, salmonella, iersiniosis, legionella, Helicobacter, chlamydia, mycoplasmas), causative agent of gonorrhea, spirochaetes, many anaerobes, toxoplasm. Azithromycin is administered orally, usually on the first day, 500 mg once, from 2 to 5 days - 250 mg once a day. The duration of treatment is 5 days. When treating acute urogenital infections, a single dose of 500 mg of azithromycin is sufficient.

Midekamycin (macropen) - is produced in tablets of 0.4 g, has a bacteriostatic effect. The spectrum of antimicrobial action is close to sumamed. It is administered orally at a daily dose of 130 mg / kg body weight (3-4 times).

Iozamycin (josamycin, vilprafen) - is available in tablets at 0.05 g; 0.15 g; 0.2 g; 0.25 g; 0.5 g. Bacteriostatic drug, antimicrobial spectrum is close to the spectrum of azithromycin. Assigned to 0.2 g 3 times a day for 7-10 days.

Roxithromycin (rulid) - a macrolide antibiotic of bacteriostatic action, is produced in tablets of 150 and 300 mg, the antimicrobial spectrum is close to the spectrum of azithromycin, but weaker in the case of helikobacteria, pertussis sticks. Resistant to roksitromitsinu pseudomonas, E. Coli, Shigella, Salmonella. It is administered orally 150 mg twice a day, in severe cases, a dose increase of 2 times is possible. The course of treatment lasts 7-10 days.

Spiramycin (rovamycin) - is manufactured in tablets of 1.5 million ME and 3 million ME, as well as in suppositories containing 1.3 million ME (500 mg) and 1.9 million ME (750 mg) of the drug. Antimicrobial spectrum is close to the spectrum of azithromycin, but compared with other macrolides is less effective against chlamydia. Resistant to spiramycin enterobacteria, pseudomonas. Assigned inside 3-6 million ME 2-3 times a day.

Kitazamycin is a bacteriostatic macrolide antibiotic, produced in 0.2 g tablets, 0.25 g capsules in 0.2-g ampoules for intravenous administration. The spectrum of antimicrobial action is close to the spectrum of azithromycin. Assigned to 0.2-0.4 g 3-4 times a day. In severe infectious and inflammatory processes, intravenously administered 0.2-0.4 g 1-2 times a day. The drug is dissolved in 10-20 ml of 5% glucose solution and injected into the vein slowly for 3-5 minutes.

Clarithromycin is a bacteriostatic macrolide antibiotic, produced in tablets of 0.25 g and 0.5 g. The spectrum of antimicrobial activity is close to the spectrum of azithromycin. The drug is considered to be most effective against Legionella. Assigned to 0.25 g 2 times a day, with severe disease, the dose can be increased.

Dirithromycin - is available in tablets of 0.5 g. When administered orally, dirithromycin is subjected to non-enzymatic hydrolysis to erythromycylamine, which has an antimicrobial effect. The antibacterial effect is similar to that of erythromycin. Assigned inside by 0.5 g once a day.

Macrolides can cause side effects (not often):

• dyspepsia (nausea, vomiting, abdominal pain);
• diarrhea;
• skin allergic reactions.

There are also antifungal macrolides.

Amphotericin B - is administered only intravenously drip at intervals of 72 hours, the average daily dose is 0.25-1 mg / kg, the maximum daily dose is 1.5 mg / kg.

Flucytosine (ankoban) - is administered internally at intervals of 6 hours. The average daily dose is 50-100 mg / kg, the maximum daily dose is 150 mg / kg.

Group of Levomycetin

Mechanism of action: inhibits the synthesis of protein in microorganisms, inhibiting the synthesis of the enzyme that carries the peptide chain to a new amino acid on the ribosome. Levomycetin exhibits bacteriostatic activity, but most strains of hemophilic rod, pneumococcus, and some Shigella species are bactericidal. Levomycetin is active against non-positive, gram-negative. Aerobic and anaerobic bacteria, mycoplasmas, chlamydia, rickettsia, but Pseudomonas aeruginosa is resistant to it.

Levomycetin (chlorocide, chloramphenicol) - is available in tablets of 0.25 and 0.5 g, tablets of prolonged action of 0.65 g, capsules of 6.25 g. It is taken by mouth at intervals of 6 hours, the average daily dose is 2 g, the maximum daily dose is 3 g.

Levomycetin succinate (chlorocide C) - a form for intravenous and intramuscular injection, is available in 0.5 and 1 g. Vials. It is administered intravenously or intramuscularly at intervals of 8-12 hours, the average daily dose of the drug is 1.5-2 g, the maximum daily dose is 4 g .

Preparations of the group of levomycetin can cause the following side effects: dyspeptic disorders, aplastic states of the bone marrow, thrombocytopenia, agranulocytosis. Preparations of Levomycetin are not prescribed for pregnant women and children.

Group of lincosamines

Mechanism of action: Lincosamines bind to ribosomes and inhibit protein synthesis like erythromycin and tetracycline, in therapeutic doses have a bacteriostatic effect. Preparations of this group are effective against gram-positive bacteria, staphylococcus, streptococcus, pneumococcus, diphtheria rods and some anaerobes, including agents of gas gangrene and tetanus. The drugs are active against microorganisms, especially staphylococci (including those producing beta-lactamase), resistant to other antibiotics. Do not act on gram-negative bacteria, fungi, viruses.

Lincomycin (Lincocin) - is available in capsules of 0.5 g, in ampoules of 1 ml with 0.3 g of substance. Assigned inside, intravenously, intramuscularly. Inside is applied at intervals of 6-8 hours, the average daily dose is 2 g, the maximum daily dose is 3 g.

Intravenous and intramuscularly applied at intervals of 8-12 hours, the average daily dose is 1-1.2 g, the maximum daily dose is 1.8 g. With rapid intravenous administration of the drug, especially in high doses, the development of collapse and respiratory failure is described. Contraindicated in severe liver and kidney diseases.

Clindamycin (Dalacin C) - is available in capsules of 0.15 g and in ampoules of 2 ml with 0.3 g of substance in one ampoule. It is used inside, intravenously, intramuscularly. The drug is a chlorinated derivative of lincomycin, has a large antimicrobial activity (2-10 times more active against gram-positive staphylococci, mycoplasma, bacteroides) and is more easily absorbed from the intestine. At low concentrations, it exhibits bacteriostatic, and in high concentrations bactericidal properties.

Inside is taken at intervals of 6 hours, the average daily dose is 0.6 g, the maximum is 1.8 g. Intravenous or intramuscularly administered at intervals of 6-12 hours, the average daily dose is 1.2 grams, the maximum is 2.4 g.

Group of anzamycins

The group of anamycins includes anamycin and rifampicins.

Anamycin - is administered orally at an average daily dose of 0.15-0.3 g.

Rifampicin (rifadin, benemycin) kills bacteria by binding to DNA-dependent RNA polymerase and suppressing RNA biosynthesis. It is active against mycobacteria tuberculosis, leprosy, and also non-positive flora. Has bactericidal action, but does not affect non-negative bacteria.

Produced in capsules at 0.05 and 0.15 g, applied orally 2 times a day. The average daily dose is 0.6 g, the highest daily intake is 1.2 g.

Rifamycin (rifotsin) - the mechanism of action and spectrum of antimicrobial influence is the same as that of rifampicin. Produced in ampoules of 1.5 ml (125 mg) and 3 ml (250 mg) for intramuscular injection and 10 ml (500 mg) for intravenous administration. Intramuscularly administered at intervals of 8-12 hours, the average daily dose is 0.5-0.75 g, the maximum daily dose is 2 g. Intravenously injected at intervals of 6-12 hours, the average daily dose is 0.5-1.5 g, the maximum daily dose is 1.5 g.

Rifamethoprim (rifaprim) - is available in capsules containing 0.15 g of rifampicin and 0.04 g of trimethoprim. The daily dose is 0.6-0.9 g, taken in 2-3 doses for 10-12 days. Effective against mycoplasmal and legionella pneumonia, as well as pulmonary tuberculosis.

The drugs rifampicin and rifotsin can cause the following side effects: flu-like syndrome (malaise, headache, fever), hepatitis, thrombocytopenia, hemolytic syndrome, skin reactions (reddening of the skin, itching, rashes), diarrhea (diarrhea, abdominal pain, nausea, vomiting). In the treatment of rifampicin, urine, tears, sputum acquire an orange-red color.

Group of polypeptides

Polymyxin

They act mainly on gram-negative flora (intestinal, dysentery, typhoid, paratyphoid flora, pseudomonas, Pseudomonas aeruginosa), but do not affect protaeus, diphtheria, clostridia, fungi.

Polymyxin B - is issued in vials of 25 and 50 mg. It is used for sepsis, meningitis (injected intralumbnally), pneumonia, urinary tract infections caused by pseudomonas. In infections caused by another non-negative flora, polymyxin B is used only in the case of multidrug resistance of the pathogen to other less toxic preparations. It is administered intravenously and intramuscularly. Intravenously administered at intervals of 12 hours, the average daily dose is 2 mg / kg, the maximum daily dose is 150 mg / kg. Intramuscularly administered at intervals of 6-8 hours, the average daily dose is 1.5-2.5 mg / kg, the maximum daily dose is 200 mg / kg.

Side effects of polymyxin: with parenteral administration has nephro- and neurotoxic effects, it is possible to block neuromuscular conduction, allergic reactions.

Glycopeptides

Vancomycin - derived from Streptomyces oriental is fungus, acts on fissile microorganisms, suppressing the formation of the peptidoglycan component of the cell membrane and DNA. It has a bactericidal action against most pneumococci, non-positive cocci and bacteria (including beta-lactamase-forming staphylococci), and does not develop.

Vancomycin is applied:

• with pneumonia and enterocolitis caused by clostridia or less often staphylococci (pseudomembranous colitis);
• in severe infections caused by staphylococci, resistant to conventional antistaphylococcal antibiotics (multiple resistance), streptococci;
• with severe staphylococcal infections in people with allergies to penicillins and cephalosporins;
• with streptococcal endocarditis in patients with an allergy to penicillin. In this case, vancomycin is combined with an aminoglycoside antibiotic;
• in patients with Gram-positive infection with allergic to β-lactams.

Vancomycin is administered intravenously at intervals of 8-12 hours, the average daily dose is 30 mg / kg, the maximum daily dose is 3 g. The main side effect: damage to the VIII pair of cranial nerves, nephrotoxic and allergic reactions, neutropenia.

Ristomycin (ristocetin, spontin) - acts bactericidal against gram-positive bacteria and on staphylococci, resistant to penicillin, tetracycline, levomycetin. Gram-negative flora has no significant effect. Introduced only intravenously drip on 5% glucose solution or isotonic sodium chloride solution 2 times a day. The average daily dose is 1,000,000 units, the maximum daily dose is 1,500,000 units.

Teicoplanin (teycomycin A2) is a glycopeptide antibiotic, close to vancomycin. Effective only in relation to gram-positive bacteria. The highest activity is shown in relation to Staphylococcus aureus, pneumococcus, green streptococcus. It is able to act on staphylococci, which are inside neutrophils and macrophages. Intramuscular injection of 200 mg or 3-6 mg / kg of body weight 1 time per day. Oto- and nephrotoxic effects are possible (rarely).

Fuzidine

Fusidine is an antibiotic active against non-negative and Gram-positive cocci, many strains of listeria, clostridia, mycobacteria are susceptible to it. Has a weak antiviral effect, but does not affect streptococcus. Fusidine is recommended for use in the infection of staphylococcus, producing β-lactamase. In normal doses, it acts bacteriostatically, with an increase in dose 3-4 times the bactericidal effect. The mechanism of action is suppression of protein synthesis in microorganisms.

Produced in tablets of 0.25 g. Used internally at intervals of 8 hours, the average daily dose is 1.5 g, the maximum daily dose of -3 g. There is also a form for intravenous administration. Intravenously applied at intervals of 8-12 hours, the average daily dose is 1.5 g, the maximum daily dose is 2 g.

Novobiocin

Novobiocin is a bacteriostatic drug intended mainly for the treatment of patients with stable staphylococcal infection. The main spectrum of action: gram-positive bacteria (especially staphylococci, streptococci), meningococci. The majority of gram-negative bacteria are resistant to the action of novobiocin. Assigned inside and intravenously. Inside is applied at intervals of 6-12 hours, the average daily dose is 1 g, the maximum daily dose is 2 g. Intravenously applied at intervals of 12-24 h, the average daily dose is 0.5 g, the maximum daily dose is 1 g.

Phosphomycin

Fosfomycin (phosphocin) is a broad-spectrum antibiotic that has a bactericidal effect on gram-positive and gram-negative bacteria and microorganisms resistant to other antibiotics. Virtually devoid of toxicity. Active in the kidneys. It is used primarily for inflammatory diseases of the urinary tract, but also for pneumonia, sepsis, pyelonephritis, endocarditis. It is produced in vials of 1 and 4 grams, is injected intravenously slowly or better with a drop of water at intervals of 6-8 hours. The average daily dose is 200 mg / kg (ie 2-4 g every 6-8 hours), the maximum daily dose - 16 g. 1 g of the drug is dissolved in 10 ml, 4 g in 100 ml of isotonic sodium chloride solution or 5% glucose solution.

Preparations of fluoroquinolones

Currently, fluoroquinolones along with cephalosporins occupy one of the leading places in the treatment of bacterial infections. Fluoroquinolones have a bactericidal effect, which is caused by the suppression of bacterial topoisomerase type 2 (DNA gyrase), which leads to disruption of genetic recombination, DNA repair and replication, and when using large doses of preparations, inhibition of DNA transcription. The consequence of these influences of fluoroquinolones is the death of bacteria. Fluoroquinolones are antibacterial agents of a wide spectrum of action. They are effective against gram-positive and gram-negative bacteria, including streptococci, staphylococcus, pneumococcus, pseudomonas, hemophilic rod, anaerobic bacteria, campylobacteria, chlamydia, mycoplasmas, legionella, gonococcus. With regard to gram-negative bacteria, the effectiveness of fluoroquinolones is more pronounced compared with the effect on gram-positive flora. Fluoroquinolones are usually used to treat infectious inflammatory processes in the bronchopulmonary and urinary systems in connection with the ability to penetrate well into these tissues.

Resistance to fluoroquinolones develops rarely and is associated with two causes:

• structural changes in DNA-gyrase, in particular, topoisomer-A (for pefloxacin, ofloxacin, ciprofloxacin)
• change in the permeability of the bacterial wall.

Fluorescinolone resistant strains of serrations, tsitrobacter, E. Coli, pseudomonas, Staphylococcus aureus are described.

Ofloxacin (tarivid, zanocin, flobocin) - is available in tablets of 0.1 and 0.2 g, for parenteral administration - in vials containing 0.2 g of the drug. Most often it is administered internally by 0.2 g 2 times in laziness, with a heavy recurrent infection the dose can be doubled. In very serious infections, sequential (sequential) treatment is used, i.e. Begin therapy with intravenous administration of 200-400 mg, and after the improvement of the state go to oral intake. Intravenous ofloxacin is administered dropwise in 200 ml of isotonic sodium chloride solution or 5% glucose solution. The drug is well tolerated. Possible allergic reactions, skin rashes, dizziness, headache, nausea, vomiting, increased blood levels of alanine amyotransferase.

High doses negatively affect articular cartilage and bone growth, therefore it is not recommended to take Tariqid to children under 16, pregnant and lactating women.

Ciprofloxacin (ciprobay) - the mechanism of action and spectrum of antimicrobial effects are similar to those of utaravid. Forms of release: tablets of 0.25, 0.5 and 0.75 g, bottles of 50 ml of an infusion solution containing 100 mg of the drug; vials of 100 ml of an infusion solution containing 200 mg of the drug; ampoules of 10 ml of a concentrate of an infusion solution containing 100 mg of the drug.

It is applied intravenously and intravenously 2 times a day, intravenously can be injected slowly by jet or drip.

The average daily dose for ingestion is 1 g, with intravenous injection - 0.4-0.6 g. With severe infection, you can increase the oral dose to 0.5 g 3 times a day.

The same side effects as ofloxacin are possible.

Norfloxacin (nolycin) - is available in tablets of 0.4 g. It is administered orally before meals at 200-400 mg 2 times a day. Reduces the clearance of theophylline, H2-blockers, may increase the risk of side effects of these drugs. Simultaneous with norfloxacin reception of non-steroidal anti-inflammatory drugs can cause convulsions, hallucinations. Dyspeptic phenomena, arthralgia, photosensitivity, elevation in the blood level of transaminases, abdominal pain are possible.

Enoxacin (penetrax) - is available in tablets of 0.2-0.4 g. It is administered orally by 0.2-0.4 g 2 times a day.

Pefloxacin (abaktal) - is available in tablets of 0.4 g and in ampoules containing 0.4 g of the drug. Assign inside of 0.2 g 2 times a day, with a severe condition, first use intravenous drip (400 mg in 250 ml of 5% glucose solution), and then switch to oral administration.

In comparison with other fluoroquinolones it is distinguished by high biliary excretion and reaches high concentrations in bile, is widely used for the treatment of intestinal infections and infectious and inflammatory diseases of bile ducts. In the process of treatment, headache, nausea, vomiting, abdominal pain, diarrhea, thirst, photodermatitis are possible.

Lomefloxacin (maksakvin) - available in tablets of 0.4 g. Has a pronounced bactericidal effect on most gram-negative, many non-positive (staphylococcus, streptococcus) and intracellular (chlamydia, mycoplasma, legionella, brucella) pathogens. Assigned to 0.4 grams I once a day.

Sparfloxacin (zagam) is a new difluorinated quinolone, has a ciprofloxacin-like structure, but contains additional 2 methyl groups and a second fluorine atom, which significantly increases the activity of this drug against gram-positive microorganisms, as well as intracellular anaerobic pathogens.

Fleoxycin is highly active against gram-negative bacteria, especially enterobacteria, and against gram-positive microorganisms, including staphylococci. Streptococci and anaerobes are less sensitive or resistant to fleoxaxin. Combination with phosphomycin increases activity against pseudomonas. It is prescribed 1 time per day inside 0.2-0.4 g. Side effects are rare.

The derivatives of quinoxoline

Hinoksidin - a synthetic bactericidal antibacterial drug, active against the proteus, Klebsiella (Friedlander sticks), Pseudomonas aeruginosa, intestinal and dysentery bacillus, Salmonella, Staphylococcus, Clostridium. Assigned inside after eating to 0.25 g 3-4 times a day.

Side effects: dyspepsia, dizziness, headache, muscle cramps (more often gastrocnemius).

Dioxydin - the spectrum and bactericidal mechanism of action of dioxidine are similar to those of quinoxidine, but the drug is less toxic and can be administered intravenously. It is used for severe pneumonia, sepsis intravenously drops of 15-30 ml of 0.5% solution in 5% glucose solution.

Nitrofuran preparations

The bacteriostatic effect of nitrofurans is provided by an aromatic nitro group. There is also evidence of a bactericidal effect. The spectrum of action is wide: drugs suppress the activity of non-positive and non-negative bacteria, anaerobes, many protozoa. The activity of nitrofurans is preserved in the presence of pus and other products of tissue decay. With pneumonia, furazolidone and furagin are most widely used.

Furazolidonum - is appointed or nominated inside by 0.15-0.3 g (1-2 tablets) 4 times a day.

Furagin - prescribed in tablets 0.15 g 3-4 times a day or intravenously drip 300-500 ml 0.1% solution.

Solafur is a water-soluble drug of furagin.

Imidazole preparations

Metronidazole (trichopolum) - in anaerobic microorganisms (but not in aerobic microorganisms, into which it also penetrates) is converted to an active form after the reduction of the nitro group, which binds to DNA and prevents the formation of nucleic acids.

The drug has a bactericidal effect. Effective in anaerobic infection (the specific gravity of these microorganisms in the development of sepsis has increased significantly). Metronidazole is sensitive to Trichomonas, Giardia, Amoeba, Spirochaete, Clostridium.

Assigned in tablets of 0.25 g 4 times a day. For intravenous drip infusion, metrogyl - metronidazole is used in 100 ml vials (500 mg).

Phytoncidal preparations

Chlorophyllipt is a phytoncid with a broad spectrum of antimicrobial action, it has an anti-staphylococcal action. Obtained from the leaves of eucalyptus. It is used in the form of 1% alcohol solution for 30 drops 3 times a day for 2-3 weeks or intravenously drip 2 ml 0.25% solution in 38 ml isotonic sodium chloride solution.

Sulfanilamide preparations

Sulfanilamides are derivatives of sulfanilic acid. All sulfanilamides are characterized by a single mechanism of action and a virtually identical antimicrobial spectrum. Sulfanilamides are competitors of paraaminobenzoic acid, which is necessary for most bacteria for the synthesis of folic acid, which is used by the microbial cell to form nucleic acids. By the nature of the action of sulfonamides - bacteriostatic drugs. The antimicrobial activity of sulfonamides is determined by the degree of their affinity for the receptors of microbial cells, i.e. Ability to compete for receptors with paraaminobenzoic acid. Since most bacteria can not utilize folic acid from the external environment, sulfonamides are a broad-spectrum drug.

Spectrum of action of sulfonamides

Highly sensitive microorganisms:

• streptococcus, staphylococcus, pneumococcus, meningococcus, gonococcus, E. Coli, salmonella, cholera vibrio, anthrax, hemophilic bacteria;
• chlamydia: causative agents of trachoma, psittacosis, ornithosis, inguinal lymphogranulomatosis;
• protozoa: plasmodium malaria, toxoplasma;
• pathogenic fungi, actinomycetes, coccidia.

Moderately sensitive microorganisms:

• microbes: enterococci, green streptococcus, proteus, clostridia, pasteurellas (including pathogens of tularemia), brucellae, mycobacterium leprosy;
• protozoa: leishmania.

Sulfonylamide resistant species of pathogens: salmonella (some species), pseudomonas, pertussis and diphtheria bacillus, mycobacterium tuberculosis, spirochetes, leptospira, viruses.

Sulfanilamides are divided into the following groups:

1. Short-acting drugs (T1 / 2 less than 10 hours): norsulfazole, ethazole, sulfadimezine, sulfazoxazole. They are taken orally 1 g every 4-6 hours, for the first dose, 1 g is often recommended. Ethazol is available in ampoules in the form of sodium salt for parenteral administration (10 ml of a 10% solution in an ampoule), the sodium salt of norsulfazole is also administered intravenously via 5- 10 ml of 10% solution. In addition, these drugs and other short-acting sulfanilamides are produced in tablets of 0.5 g.
2. Drugs of average duration of action (T1 / 2 10-24 h): sulfazin, sulfamethoxazole, sulfomoxal. Wide application have not received. Produced in tablets of 0.5 g. Adults on the first dose give 2 grams, then for 1-2 days for 1 g every 4 hours, then 1 g every 6-8 hours.
3. Long-acting drugs (T1 / 2 24-48 h): sulfapyridazine, sulfadimethoxin, sulfamonomethoxin. Produced in tablets of 0.5 g. Assigned to adults on the first day of I-2 g, depending on the severity of the disease, the next day give 0.5 or 1 g 1 time per day and spend the entire course on this maintenance dose. The average duration of treatment is 5-7 days.
4. Drugs of super long-duration action (T _1/2 more than 48 hours): sulfalene, sulfadoxine. Produced in tablets of 0.2 g. Sulfalen is prescribed orally daily or 1 time per 7-10 days. Daily appoint with acute or rapid infections, I once every 7-10 days - with chronic, long-lasting. With daily intake appoint an adult on the 1st day of 1 g, then 0.2 g per day, take 30 minutes before meals.
5. Topical preparations that are poorly absorbed in the gastrointestinal tract: sulgin, phthalazole, phtazine, disulformin, salazosulfapyridine, salazopyridazine, salazodimethoxin. Applied with intestinal infections, with pneumonia are not prescribed.

Highly effective combination of sulfonamides with an antifolia drug trimethoprim. Trimethoprim enhances the action of sulfonamides, disrupting the reduction of trihydrophosphate to tetrahydrofolic acid, responsible for protein metabolism and division of the microbial cell. The combination of sulfonamides with trimethoprim provides a significant increase in the degree and spectrum of antimicrobial activity.

The following preparations containing sulfonamides in combination with trimethoprim are produced:

• Biseptol-120 - contains 100 mg of sulfamethoxazole and 20 mg of trimethoprim.
• Biseptol-480 - contains 400 mg of sulfamethoxazole and 80 mg of trimethoprim;
• Biseptol for intravenous infusions of 10 ml;
• proteseptil - contains sulfadimezin and trimethoprim in the same doses as biseptol;
• sulfaten - a combination of 0.25 g of sulfonamethoxin with 0.1 g of trimethoprim.

The most widely used biseptol, which unlike other sulfonamides has not only bacteriostatic, but also bactericidal action. Biseptol is taken once a day for 0.48 g (1-2 tablets per reception).

Side effects of sulfonamides:

• crystallization of acetylated metabolites of sulfonamides in the kidneys and urinary tract;
• alkalinization of urine increases the ionization of sulfanilamides, which are weak acids, in ionized form, these preparations are much more soluble in water and urine;
• alkalinization of urine reduces the probability of crystalluria, helps maintain high concentrations of sulfonamides in urine. To ensure a stable alkaline urine reaction, it is sufficient to prescribe soda at 5-10 g per day. Crystalluria, caused by sulfonamides, can be asymptomatic or cause renal colic, hematuria, oliguria, and even anuria;
• Allergic reactions: skin rashes, exfoliative dermatitis, leukopenia;
• dyspeptic reactions: nausea, vomiting, diarrhea; in newborns and infants, sulfonamides can cause methemoglobinemia due to the oxidation of fetal hemoglobin, accompanied by cyanosis;
• in the case of hyperbilirubinemia, the use of sulfonamides is dangerous, since they displace bilirubin from binding to the protein and contribute to the manifestation of its toxic effect;
• when using biseptol, a picture of folic acid deficiency (macrocytic anemia, gastrointestinal tract damage) can develop, folic acid is needed to eliminate this side effect. Currently, sulfonamides are rarely used, especially if antibiotics are intolerant or resistant to microflora.

Combination of antibacterial drugs

Synergy occurs when the following drugs are combined:

Penicillins	+ Aminoglycosides, cephalosporins
Penicillins (penicillinase-resistant)	+ Penicillins (penicillinase-unstable)
Cephalosporins (other than cephaloridine)	+ Aminoglycosides
Macrolides	+ Tetracyclines
Levomycetin	+ Macrolides
Tetracycline, macrolides, lincomycin	+ Sulfonamides
Tetracyclines, lincomycin, nystatin	+ Nitrofurans
Tetracyclines, nystatin	+ Oxyquinolines

Thus, the synergy of action is noted when combining bactericidal antibiotics with a combination of two bacteriostatic antibacterial drugs. Antagonism occurs when a combination of bactericidal and bacteriostatic drugs.

The combined use of antibiotics is performed in severe and complicated pneumonia (pneumonia subscription, pleural empyema), when monotherapy may be ineffective.

The choice of antibiotic in various clinical situations

Clinical situation	Probable pathogen	Antibiotic of the 1st series	Alternative drug
Primary lobe pneumonia	Pneumococcus	Penicillin	Erythromycin and other macrolides, azithromycin, cephaloslorins
Primary atypical pneumonia	Mycoplasma, legionella, chlamydia	Erythromycin, semisynthetic macrolides, erythromycin	Fluoroquinolones
Pneumonia in the background of chronic bronchitis	Hemophilus rods, streptococci	Ampicillin, macrolides, erythromycin	Leaomycetin, fluoroquinolones, cephaloslorins
Pneumonia on the background of influenza	Staphylococcus, pneumococcus, hemophilic rods	Ampioks, penicillins with beta-lactamase inhibitors	Fluoroquinolones, cephaloslorins
Pneumonia aspiration	Enterobacteria, anaerobes	Aminoglycosides + metronidazole	Cephaloslorins, fluoroquinolones
Pneumonia on the background of artificial ventilation	Enterobacteria, Pseudomonas aeruginosa	Aminoglycosides	Imipenem
Pneumonia in persons with immunodeficiency states	Enterobacteria, staphylococcus, caprofits	Penicillins with beta-lactamase inhibitors, ampiox, aminoglycosides	Cephaloslorins, fluoroquinolones

Features of antibiotic therapy of atypical and intrahospital (nosocomial) pneumonia

Atypical pneumonia refers to pneumonia caused by mycoplasma, chlamydia, legionella, and characterized by certain clinical manifestations that differ from typical out-of-hospital pneumonia. Legionella causes pneumonia in 6.4%, chlamydia - in 6.1% and mycoplasma - in 2% of cases. A feature of atypical pneumonia is the intracellular location of the causative agent of the disease. In this regard, for the treatment of "atypical" pneumonia should be used such antibacterial drugs, which penetrate well into the cell and create high concentrations there. These are macrolides (erythromycin and new macrolides, in particular, azithromycin, roxithromycin, etc.), tetracyclines, rifampicin, and fluoroquinolones.

Intrahospital nosocomial pneumonia is a pneumonia developing in a hospital provided that during the first two days of hospitalization there were no clinical and radiological signs of pneumonia.

Intrahospital pneumonia differs from outpatients in that they are more often caused by gram-negative flora: Pseudomonas aeruginosa, hemophilic daddy, legionella, mycoplasmas, chlamydia, occur more heavily and more often result in death.

About half of all cases of nosocomial pneumonia develops in intensive care units, in postoperative departments. Intubation with mechanical ventilation of the lungs increases the incidence of intra-hospital infection by 10-12 times. In this case, 50% of patients who are on ventilator are allocated pseudomonas, 30% - acinetobacter, 25% - klebsiela. Less often, the pathogens of nosocomial pneumonia are E. Coli, Staphylococcus aureus, serratus, and tsitrobacter.

Hospital aspiration also includes aspiration pneumonia. They are most often found in alcoholics, in people with impaired cerebral circulation, with poisoning, chest injuries. Aspiration pneumonia is almost always due to gram-negative flora and anaerobes.

Nosocomial pneumonia is treated with broad-spectrum antibiotics (third generation cephalosporins, ureidopenicillins, monobactams, aminoglycosides), fluoroquinolones. In the severe course of nosocomial pneumonia, the combination of aminoglycosides with cephalosporins of the third generation or monobactams (aztreonam) is considered to be the 1 st line. In the absence of effect, the drugs of the second series are used - fluoroquinolones, it is also effective by imipynem.

[11], [12], [13], [14], [15], [16],