The topic of antibiotics by pharmacology. Antibiotics and their pharmacological action. Side Effects of Antibacterial Therapy

Antibiotics are a group of medicines that can coherent the growth and development of living cells. The most commonly used to treat infectious processes caused by various bacteria strains. The first drug was discovered in 1928 by British bacteriologist Alexander Fleming. However, some antibiotics are also prescribed during cancer pathologies as a component of combined chemotherapy. For viruses, this group of medicines practically does not act, with the exception of some tetracyclines. In modern pharmacology, the term "antibiotics" is increasingly replaced by "antibacterial drugs".

The first was synthesized drugs from the penicillin group. They helped significantly reduce the mortality of such diseases such as pneumonia, sepsis, meningitis, gangrene and syphilis. Over time, due to the active use of antibiotics, many microorganisms began to have resistance to them. Therefore, an important task was to search for new groups of antibacterial drugs.

Gradually, pharmaceutical companies were synthesized and began to produce cephalosporins, macrolides, fluoroquinolones, tetracyclines, leftomycetin, nitrofurans, aminoglycosides, carbapenes and other antibiotics.

Antibiotics and their classification

The main pharmacological classification of antibacterial drugs is separation for the action on microorganisms. For this characteristic, two groups of antibiotics distinguish:

bactericidal - drugs cause death and lysis of microorganisms. This action is due to the ability of antibiotics to inhibit the synthesis of membranes or suppress the production of DNA components. This property own penicillins, cephalosporins, fluoroquinolones, carbapenes, monobactams, glycopeptides and phosphomycin.
bacteriostatic - antibiotics are able to inject the synthesis of proteins by microbial cells, which makes it impossible to reproduce. As a result, the further development of the pathological process is limited. This action is characteristic of tetracyclines, macrolides, aminoglycosides, lincosamines and aminoglycosides.

The spectrum of action also distinguishes two groups of antibiotics:

with a wide - the drug can be used to treat pathologies caused by a large number of microorganisms;
with narrow - medicine affects individual strains and types of bacteria.

There is also a classification of antibacterial drugs by their origin:

natural - get from living organisms;
semi-synthetic antibiotics are modified natural analogue molecules;
synthetic - they are completely artificial in specialized laboratories.

Description of various groups of antibiotics

Beta lactama

Penicillins

Historically, the first group of antibacterial drugs. It has a bactericidal effect on a wide range of microorganisms. Penicillins distinguish the following groups:

natural penicillins (synthesized under normal conditions mushrooms) - benzylpenicillin, phenoxymethylpenicillin;
semi-synthetic penicillins that have greater resistance to penicillins, which significantly expands their range of action - oxacillin medicines, methicillin;
with an extended effect - Ampesicillin, ampicillin preparations;
penicillins with a wide effect on microorganisms - Meslocillin medicines, azlotsillin.

To reduce the resistance of bacteria and increase the chance of the success of antibiotic therapy, penicillinase-clavulanic acid, tazobactam and sulbactams are actively added to penicillins. Thus appeared drugs "Augmentin", "Tazochim", "Tazrobid" and others.

These drugs are used in respiratory infections (bronchitis, sinusite, pneumonia, pharyngitis, laryngitis), urogenital (cystitis, urethritis, prostatitis, gonor), digestive (cholecystitis, dysentery) systems, syphilis and leather lesions. From side effects, allergic reactions are most often found (urticaria, anaphylactic shock, angioedema edema).

Penicillins are also the safest means for pregnant and babies.

Cephalosporins

This group of antibiotics owns a bactericidal effect on a large number of microorganisms. Today, the following generations of cephalosporins are distinguished:

The overwhelming majority of these medications exist only in the injection form, so they are used mainly in clinics. Cephalosporins are the most popular antibacterial agents for use in hospitals.

These drugs are used to treat a huge amount of diseases: pneumonia, meningitis, generalization of infections, pyelonephritis, cystite, inflammation of bones, soft tissues, lymphangitis and other pathologies. When using cephalosporins, hypersensitivity is often found. Sometimes there is a transient reduction in creatinine clearance, pain in the muscles, cough, an increase in bleeding (due to a decrease in vitamin K).

Carbapenes

They are a rather new group of antibiotics. Like the remaining beta lactams, the carbapenes have a bactericidal effect. A huge number of different bacteria strains remains sensitive to this group of medicines. Also, the carbapenes show resistance to enzymes that synthesize microorganisms. Data properties led to the fact that they are considered to be rescue preparations when the remaining antibacterial agents remain ineffective. However, their use is strictly limited due to the concerns of the development of bacteria resistance. This group of drugs belong to Meropenem, Doripenem, Ertapenem, and impediment.

Carbapenes are used to treat sepsis, pneumonia, peritonitis, acute surgical pathologies of the abdominal cavity, meningitis, endometritis. Also prescribe these drugs with immunodeficiency patients or against neutropenia.

Among the side effects it is necessary to note dyspeptic disorders, headache, thrombophlebitis, pseudo-membrane colitis, cramps and hypokalemia.

Monobaktama

Monobactams act mainly only on the gram-negative flora. The clinic uses only one active ingredient from this group - Azitreon. With its advantages, resistance to most bacterial enzymes is distinguished, which makes it a drug of choice in the ineffectiveness of treatment with penicillins, cephalosporins and aminoglycosides. In clinical recommendations, the aztreon is recommended for enterobacter infection. It applies only intravenously or intramuscularly.

Among the testimony, it is necessary to highlight sepsis, community-acquired pneumonia, peritonitis, infections of the pelvis, leather and musculoskeletal system. The use of aztreonam sometimes leads to the development of dyspepsic symptoms, jaundice, toxic hepatitis, headaches, dizziness and allergic rash.

Macrolids

Medicines are also noted low toxicity, which allows them to be applied during pregnancy and at the early age of the child. They are divided into the following groups:

natural, which were synthesized in the 50s-60s of the last century - Erythromycin, Spiramycin, Josamicina, Midekamycin;
prodrugs (transformed into an active form after metabolism) - Toleandomycin;
semi-synthetic - azithromycin medicine, clarithromycin, diritromycin, telitromycin.

Macrolides are used with many bacterial pathologies: peptic diseases, bronchitis, pneumonia, ENT infections, dermatosis, Lyme disease, urethritis, Cervicitis, Roger, Impregno. It is impossible to use this group of medicines during arrhythmias, lack of renal function.

Tetracyclines

For the first time, tetracyclines were synthesized for more than half a century. This group owns a bacteriostatic effect against many strains of microbial flora. In high concentrations, they show a bactericidal action. A feature of tetracycline is their ability to accumulate in bone tissue and enamel of teeth.

On the one hand, this allows clinicians to actively use them in chronic osteomyelitis, and on the other disrupts the development of a skeleton in children. Therefore, they are categorically impossible to apply during pregnancy, lactation and under the age of 12 years. Tetracycles, except for the drug of the same name, include doxycycline, oxytetracycline, minocycline and tigecycline.

Use them with various intestinal pathologies, brucellosis, leptospirosis, tularemia, actinomycosis, trachoma, lime disease, gonducting infection and rickettsiosis. Among the contraindications are also distinguished by porphyria, chronic liver diseases and individual intolerances.

Fluoroquinolones

Fluoroquinolones are a large group of antibacterial agents with a wide bactericidal effect on the pathogenic microflora. All drugs are hiking nanidixic acid. The active use of fluoroquinolones began with the 70s of the last century. Today they are classified for generations:

I - drugs nodidix and oxolinic acid;
II - medicines with offloxacin, ciprofloxacin, norfloxacin, peffloxacin;
III - levofloxacin preparations;
IV - medicines with gatifloxacin, moxifloxacin, hemifloxacin.

The last generations of Fluoroquinolones were called "respiratory", due to their activity against microflora, which most often causes the development of pneumonia. They are also used to treat sinusites, bronchitis, intestinal infections, prostatitis, gonorrhea, sepsis, tuberculosis and meningitis.

Among the disadvantages it is necessary to allocate that fluoroquinolones are able to influence the formation of the musculoskeletal system, so in childhood, during pregnancy and during the lactation period they can be prescribed only on life indications. The first generation of drugs is also characterized by high hepato and nephrotoxicity.

Aminoglycosides

Aminoglycosides found an active use in the treatment of bacterial infection caused by gram-negative fluoro. They have a bactericidal action. Their high efficiency, which does not depend on the functional activity of the patient's immunity, made them indispensable means in its violations and neutropenia. The following generations of aminoglycosides distinguish:

Aminoglycosides are prescribed in infections of the respiratory system, sepsis, infectious endocarditis, peritonitis, meningitis, cystitis, pyelonephritis, osteomyelitis and other pathologies. Among the side effects are of great importance to the toxic effect on the kidneys and a decrease in hearing.

Therefore, during the course of therapy, it is necessary to regularly carry out a biochemical blood test (creatinine, SKF, urea) and audiometry. Pregnant women, during lactation, patients with chronic kidney disease or on hemodialysis aminoglycosides are prescribed only on life indications.

Glycopeptides.

Glixopeptide antibiotics own a bactericidal effect of a wide range of action. The most famous from them - Bleomycin and Vancomycin. In the clinical practice of glycopeptides are reserve drugs that are prescribed in the ineffectiveness of other antibacterial agents or specific sensitivity to the infection pathogen.

They are often combined with aminoglycosides, which makes it possible to increase the cumulative effect on golden staphylococcus, enterococcus and streptococcus. On mycobacteria and mushrooms, glycopeptide antibiotics do not act.

Assigns this group of antibacterial agents with endocarditis, sepsis, osteomyelitis, phlegmon, pnegumonia (including complicated), abscess and pseudomambranous colitis. It is impossible to use glycopeptide antibiotics in renal failure, increased sensitivity to drugs, lactation, nerupting auditory nerve, pregnancy and lactation.

Lincoosamida

Lincoosamides include Lincomicin and Clindamycin. These drugs show a bacteriostatic effect on gram-positive bacteria. We use them mainly in combination with aminoglycosides, like a second line tools for heavy patients.

Lincoosamides are prescribed with aspiration pneumonia, osteomyelitis, diabetic foot, necrotic fasci and other pathologies.

Quite often during their admission, candidal infection is developing, headache, allergic reactions and inhibition of blood formation.

Clinical - pharmacological characteristics

beta - lactam antibiotics

Penicillins, cephalosporins, carbapenes and monobactams in their structure have β - a lactam ring, which causes their strong bactericidal effect, and the possibility of developing cross-allergies. Penicillins and cephalosporins can be inactivated by microorganisms (including intestinal flora) producing an enzyme β - lactamase (penicillinase), which destructsβ - a lactam ring. Due to the high clinical efficacy and low toxicity, the lactam antibiotics occupy a leading place in the treatment of most infections.

Penicillins

Classification.

1. Natural (natural) penicillins - benzylpenicillins, phenoxymethylpenicillin and prolonged penicillins (Durant Penicillins).

2. Semi-synthetic penicillins:

● isoxazolpenicillins - antistaphococcal penicillins (oxacillin, chloxacillin, fluxacoccillin);

● amidinopenicillins (amidinocyllin, pivamdinocyllin, bacamidinocyllin, acidocillin);

● aminopenicillins - penicillins of the expanded spectrum of action (ampicillin, amoxicillin, tamplanicillin, bakakopicillin, pivampicillin);

● antisingenic antibiotics:

- carboxyzylinicillins (carbenicillin, carindacyllin, carindacillin, ticarcillin),

- ureidopenicillins (azlocillin, meslocillin, pepactorin);

● Inhibitory-protected penicillins (amoxicillin + clavulanic acid, ampicillin + sulbactam, ticarcillin + clavulanic acid, peperingillin + pelvis).

BenzylPenicillins low-toxic and not expensive, create rapidly high concentrations in many organs and tissues, including inside cells (therefore are a means of emergency); Worse penetrate into bone and nervous fabric, do not penetrate the BC. At the same time, with meningitis and hypoxic states of the brain, they can penetrate the BEB due to inflammatory capillary vasodilation of cerebral vessels, and therefore are used to treat meningoencephalitis.

Sodium salt of benzylpenicillin is introduced intramuscularly, intravenously, endoomumboral (under the brain shell - intrate) And in the body cavity. Benzylpenicillin potassium and novocaine salt are introduced only intramuscularly. The potassium salt can not be administered intravenously, since potassium ions released from the drug can cause heartfelt oppression and convulsions. The novocaine salt of the drug is badly soluble in water, forms a suspension with water and it is unacceptable to enter the vessel.

The multiplicity of administration of benzylpenicillins is 6 times a day (after 1 month of life), and the novocaine salt of the drug (benzylpenicillin plosen) - 2 times a day.

Phenoxymethylpenicillin (FOMP) Acid resistant and applied by Per OS, but does not create high blood concentrations, therefore, it is not taken to treat severe infections. Usually the FOMP is not used for monotherapy, but combine it with other antibiotics. For example, in the morning and in the evening, benzylпenicillin can be introduced intramuscularly, and the day (2 - 3 times) is prescribed per os FOMP.

Prolonged preparations of Penicillin Apply with a prophylactic goal. Bicyllin - 1 (benzatin benzylpenicillin or benzinenicillin G) is poorly soluble in water, which is used only for intramuscular administration 1 - 2 times a week. Bicyllin - 3 is a combination of potassium or novocaine bezylpenicillin novocaine salts - 1 in equal proportions of 100 thousand units of each. The drug is injected intramuscularly 1 - 2 times a week. Bicyllin - 5 is also a combination of benzylpenicillin novocaine salt and bicillin - 1 in proportion of 1 to 4. Its intramuscular administration produce 1 time in 4 weeks.

Due to the slow suction of Bicyllin - 1 its action begins only 1 - 2 days after administration. Bicyllins - 3 and - 5 Due to the presence of benzylpenicillin in them, antimicrobial action is already in the first hours.

The most frequent side effect of natural penicillins is allergic reactions (anaphylactic shock is possible). Therefore, when prescribing drugs, careful collection of allergological history and monitoring of the patient for 30 minutes is required. After the first introduction of the drug. In some cases, skin samples are carried out.

Preparations show antagonism with sulfanimamides and synergism with aminoglycosides against gram-positive coils (except pneumococci!), But are not compatible with them in one syringe or in one infusion system.

Isoksazolpenicillins(antistaphococcal penicillins) resistant to the action of penicillinase, i.e. active in relation penicillin-resistant stamps Staphilococci - Staphylococcus aureus. (PRSA), Besides methicillin-resistant staphylococci strains (MRSA).PRSA - Staphilococci play a major role in the problem nosokomial(in-community, hospital) infections. In relation to other microorganisms, the spectrum of their activity is the same as natural penicillins, but antimicrobial efficacy is significantly less. Preparations are introduced both parenterally and inwards in 1 - 1.5 hours before meals, since they are little resistant to hydrochloric acid.

Amidoenicillinsactive in relation to gram-negative enterobacteria. To increase their spectrum of action, these antibiotics are combined with isoxazolpenicillins and natural penicillins.

Aminopenicillins - Wide spectral antibiotics, but they are stable PRSA, which is why these LS do not solve the problem of hospital infection. Therefore, combined drugs were created: ampiox (ampicillin + oxacillin), clonac - P (ampicillin + keloxylin), sulmbillin (ampicillin + sulbactam, which is an inhibitor of β - lactamases), clonacom (amoxicillin + chloxacillin), agguntin and its analog amoxiclav ( Amoxicillin + Clawulanic acid).

Antsingenic penicillins prescribed only in the absence of other antsingenic drugs and only in the case of a confirmed sensitivity to them with a cinema stick, since they are toxic, and they develop rapidly secondary (induced by an antibiotic itself) resistance causative agent. Preparations do not act on staphylococci. Therefore, if necessary, they are combined with ochesazolpenicillins. There are combined drugs: Timemitin (ticarcillain + clavulanic acid) and tazocin (peperacylin + tazobactama as a β-lactamase inhibitor).

● Inhibitors of penicillins - Combined preparations containing β-lactamase inhibitors (clavulanic acid, sulbactam, pelvic acids). The most powerful of them is a tazocin. These LS are well distributed in the body, creating high concentrations in tissues and liquids (including light, pleural and peritoneal cavities, middle ear, sinuses), but do not penetrate the BGB. Clawulanic acid may be acute liver damage: increasing the activity of transaminases, fever, nausea, vomiting.

Natural penicillins, isoxazolpenicillins, amidoenicillins, aminopenicillins - small-toxic, have a greater latitude of therapeutic action. Danger represents only allergic reactions of both immediate and slow-motion types in treating them.

Carboxyzenicillins and ureidopenicillins - drugs with low latitude of therapeutic action, i.e. drugs of strict dosing mode. Their use may be accompanied by the emergence of allergic reactions, symptoms of neuro and hematotoxicity, jade, dysbiosis, hypokalemia.

All penicillins are incompatible with many substances, so their introduction should be made by a separate syringe.

Cephalosporins

These LS are widely used in clinical practice, since they have a strong bactericidal action, a wide therapeutic range, resistance of varying degrees to β - lactamases of staphylococcal and low toxicity.

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Introduction

1. Classification of antibiotics

2. Beta-lactam antibiotics

3. Penicillins

4. Cephalosporins group

5. Group of carbapenes

6. Group of Monobakatam

7. A group of tetracycline

8. Group of aminoglycoside

9. Levomycetina

10. Glycopeptide Group

11. Lincoosamide group

12. Anti-tuberculosis chemotherapy

13. Classification of anti-tuberculosis drugs of the International Union of Tuberculosis

14. Polypeptides

Literature

Introduction

Antibiotics - These are substances that suppress the growth of living cells, most often prokaryotic and simplest. Antibiotics can be natural (natural) origin and artificial (synthetic and semi-synthetic).

Antibiotics of natural origin are most often produced by actinomycetes and mold mushrooms, but they can also be obtained from bacteria (polymyxins), plants (phytoncides) and animal tissues and fish.

Antibiotics that suppress the growth and reproduction of bacteria are used as drugs. The widespread use of antibiotics and oncological practice, as cytostatic (antitumor) drugs. In the treatment of diseases of viral etiology, the use of antibiotics is not advisable, as they are not able to influence viruses. However, it was noted that a number of antibiotics (tetracycles) are able to influence large viruses.

Antibacterial drugs are synthetic preparations that do not have natural analogues and providing an overwhelming effect on the growth of bacteria.

The invention of antibiotics can be called a revolution in medicine. The first antibiotics were Penicillin and Streptomycin.

1. Classification of antibiotics

By the nature of the impact on the bacterial cell:

1. Bacteriostatic preparations (stop and reproduction of bacteria)

2. Bactericidal preparations (destroy bacteria)

By the method of obtaining distinguishes antibiotics:

1. Natural

2. Synthetic

3. Polysintetic

In the direction of action distinguish:

1. Antibacterial

2. Antitumor

3. Antifungal

The spectrum is distinguished by:

1. Wide spectrum antibiotics

2. Antibiotics of the narrow spectrum of action

By chemical structure:

1. Beta-lactam antibiotics

Penicillins - are produced by the colonies of the mold fungus Penicillinum. Breaks: biosynthetic (Penicillin G - benzylpenicillin), aminopenicillin (amoxicillin, ampicillin, bakampicillin) and semi-synthetic (oxacillin, methicillin, chloxacillin, dyloxicillin, fluklocylin) penicillins.

Cephalosporins are used in relation to penicilline bacteria. Cefalosporins distinguish: 1st (Zefenin, Cephalexin), 2nd (cefazoline, Cefhamesin), 3rd (Cefriaxone, Cefotaxim, Cefuroxime) and 4th (cefepim, cefpir) generations.

Carbapenes - broad spectrum antibiotics. The structure of the carbapenes determines their high resistance to beta lactamases. Carbapenes include: Meropenem (Merone) and Imphene.

MONOBACTAMA (Azitreon)

2. Macrolids - antibiotics with a complex cyclic structure with a bacteriostatic action. Compared with other antibiotics are less toxic. These include: erythromycin, oleandomycin, roxitromycin, azithromycin (Sumamed), Clarithromycin, etc. Also among macrolides include: azalida and ketolides.

3. Tetracyclines - are used to treat infections of respiratory and urinary tract, treatment of severe infections such as Siberian ulcers, Tularemia, Brucellia. It has a bacteriostatic action. Refer to the class of polyketides. Among them are distinguished: natural (tetracycline, oxytetracycline) and semi-synthetic (metacycline, chlorotter, doxycycline) tetracyclines.

4. Aminoglycosides - drugs of this group of antibiotics are highly toxic. Used to treat heavy infections such as blood infection or peritonitis. It has a bactericidal action. AminoglycosidyActive in relation to gram-negative aerobic bacteria. These include: streptomycin, gentamicin, kanamycin, neomycin, amikacin, etc.

5. Levomycetins - with the use of antibiotics of this group, there is a risk of serious complications - the damage to the bone marrow generating blood cells. It has a bacteriostatic action.

6. Glixopeptide antibiotics disrupt the synthesis of the cell wall of bacteria. It has a bactericidal effect, however, the bacteriostatic effect of antibiotics of this group is possible in relation to enterococcal, streptococci and staphylococcal. These include: Vancomycin, Teicoplast, Daptomicin, etc.

7. Lincoosamids have a bacteriostatic action. In high concentrations with respect to highly sensitive microorganisms, a bactericidal effect may be exhibited. These include: Lincomicin and Clindamycin

8. Anti-tuberculosis drugs - isoniazide, fivazide, salub, metaside, etionamide, protionamide.

9. Polypeptides - antibiotics of this group in its molecule contain residues of polypeptide compounds. These include: gramicidine, polymixines M and B, Bacitrazin, Kolistin;

10. To polyenams include: amphotericin in, nystatin, Lev Room, Natamicin

11. Antibiotics of different groups - rifamycin, ristomycin sulfate, fusidin-sodium, etc.

12. Antifungal drugs - cause the death of the cells of fungi, destroying their membrane structure. Possess a lithic action.

13. Anti-persons - diaphenylsulfophone, solidfone, diucifon.

14. Anthracycline antibiotics - they include antitumor antibiotics - doxorubicin, carmineomycin, regulation, Aklaurubicin.

2. Beta-lactam antibiotics

To B-lactam antibiotics (B-lactamam), which combines the presence in the structure of the B-Lactam ring, includes penicillins, cephalosporins, carbapenes and monobactams with a bactericidal action. The similarity of the chemical structure predetermines the same mechanism of action of all B-lactam (violation of the synthesis of the cell wall of bacteria), as well as cross allergies to them in some patients.

Penicillins, cephalosporins and monobactams are sensitive to hydrolyzing action of special enzymes - in lactamas produced by a number of bacteria. Carbapenes are characterized by significantly higher resistance to V-lactamases.

Given the high clinical efficacy and low toxicity, B-lactam antibiotics form the basis of antimicrobial chemotherapy at the present stage, occupying a leading place in the treatment of most infections.

3. Penicillins

Penicillins are the first antimicrobial preparations developed on the basis of biologically active substances produced by microorganisms. The source of all penicillins, benzylpenicillin, was obtained at the beginning of the 40s of the 20th century. Currently, the penicillin group includes more than ten antibiotics, which, depending on the sources of production, the characteristics of the structure and antimicrobial activity are divided into several subgroups (Table 1).

General properties:

1. Bactericidal action.

2. Low toxicity.

3. Extinguishing mainly through the kidneys.

4. Wide dosage range.

Cross allergies between all penicillins and partially cephalosporins and carbapenes.

Natural penicillins. Natural penicillins include essentially, only benzylpenicillin. However, based on the spectrum of activity, prolonged (benzylpenicillinproter, benzyl benzylpenicillin), imperorated (phenoxymethylpenicillin, benzatinfenoxymethylpenicillin) derivatives can also be attributed to this group. All of them are destroyed in lactamases, so they cannot be used for therapy of staphylococcal infections, since in most cases staphylococci produces in lactamases.

Semi-synthetic penicillins:

Antistaphococcal penicillins

Penicillins with an extended activity spectrum

Antsingenic penicillins

4. Group cephalosporins

Cephalosporins are representatives of V-Lactamov. They are considered one of the most extensive class of AMP. Due to its low toxicity and high efficiency, cephalosporins use much more often than other AMPs. Antimicrobial activity and pharmacokinetic characteristics determine the use of one or another antibiotic group of cephalosporins. Since cephalosporins and penicillins have a structural similarity, these group drugs are characterized by the same antimicrobial mechanism, as well as cross-allergies in some patients.

There are 4 generations of cephallosporins:

I generation - cefazoline (parenteral use); Cephalexin, Cefadroxyl (oral use)

II generation - cefuroxime (parenteral); Cefuroxime Axietyl, cefaclor (oral)

III generation - cefotaxim, ceftriaxone, ceftazidim, cefoperazazon, cefoperazone / sulbactam (parenteral); Zefisim, Cefibutene (oral)

IV generation - cefepim (parenteral).

Mechanism of action. The effect of cephalosporins Bactricidal. References of cephalosporins include penicillin-binding bacteria proteins that perform the role of enzymes at the final stage of the synthesis of peptideoglycan (biopolymer is the main component of the cell wall of bacteria). As a result of blocking the synthesis of peptidoglycan bacterium dies.

Spectrum of activity. Cephalosporins from I to III generation are characterized by a tendency to expand the circle of activity, as well as an increase in the level of antimicrobial activity in terms of gram-negative microorganisms and a decrease in the level of activity with respect to gram-positive bacteria.

Total for all cephalosporins - This is a lack of weighty activity in relation to L.monocytogenes, MRSA and Enterococci. Cefalosporins show a smaller sensitivity of the CNS, compared with S.Aureus.

Cephalosporins I generation. They have a similar antimicrobial spectrum of activity with the following difference: there are more preparations intended for parenteral administration (cefazoline), rather than preparations for oral administration (cefadroxyl, cephalexin). The action of antibiotics is subject to meticilla-sensitive Staphylococcus SPP. and Streptococcus SPP. (S.pneumoniae, S.pyogenes). The cephalosporins of the II generation are characterized by less antiphenococcal activity, compared with aminopenicillins and the majority of the cephalosporins of subsequent generations. Cephalosporins do not act at all on letteria and enterococci, which is a clinically important feature of this class of antibiotics. The cephalosporins revealed resistance to the action of staphylococcal B-lactamas, but despite this in individual strains (hyperproduces of these enzymes), moderate sensitivity may appear. Cephalosporins I am generation and penicillins are not active in relation to pneumococci. In cephalosporins I generation, a narrow spectrum of action and a low level of activity in relation to gram-negative bacteria. Their action will apply to Neisseria SPP. However, the clinical significance of this fact is limited. Clinically insignificant activity of cephalosporins I am generation against M.Satarrhalis and H.INFLUENZAE. On M.Satarrhalis, naturally actively actively actively, but show sensitivity to hydrolysis in lactamases, producing almost 100-% of strains. Confused by the influence of cephalosporins I am generation of representatives of the Enterobacteriaceae family: p.mirabilis, Salmonella SPP., Shigella SPP., E. coli, and the clinical significance is absent in activity in relation to Schigell and Salmonella. P.MiraBilis and E. coli strains that provoke community-acquired (especially nosocomial) infections are characterized by widespread acquired resistance due to the production of in-lactamas of an extended and wide range of action.

In other enterobacteria, non-enmented bacteria and Pseudomonas SPP. Revealed resistance.

B.Fragilis and related microorganisms show stability, and representatives of a number of anaerobes are sensitivity to the action of cephalosporins I am generation.

CephalosporinsII.generation. Cefuroxime and cefaclor are two representatives of this generation - differ among themselves: having a similar antimicrobial spectrum of action, at cefuroxime, compared to cefaclorom, has a large activity with respect to Staphylococcus SPP. and Streptococcus SPP. Both drugs do not show activity regarding layeries, enterococci and MRSA.

Pneumococcus is manifested in penicillin and generation cephalosporins. Representatives of cephalosporins II generation are characterized by a more advanced spectrum of influence on gram-negative microorganisms than the cephalosporins of the first generation. Both cefuroxime and cefaclor show activity in relation to Neisseria SPP., But only the action of cefuroxime on the gonococci is marked by clinical activity. On Haemophilus SPP. and M. Catarrhalis affects more strongly cefuroxime, since it shows resistance to hydrolysis of them in lactamases, and these enzymes partially destroy the cefaclor. From representatives of the Enterobacteriaceae family are exposed to drugs not only P.Mirabilis, Salmonella SPP., Shigella SPP., E. coli, but also c.diversus, p.Vulgaris, Klebsiella SPP. During the production of microorganisms listed above, the wide spectrum in the lactamas of them remains the sensitivity to cefuroxime. Cefaclore and cefuroxime have a feature: they are destroyed by in-lactamases of the expanded spectrum. Some p.rettgeri strains, P.Stuartii, M.Morganii, Serratia SPP., C.Freundii, Enterobacter SPP. In vitro moderate sensitivity to cefuroxime can manifest itself, but it makes no sense to use this drug in the treatment of infections whose pathogens are the above bacteria. The effect of cephalosporins II of generation does not apply to the anaeros of the B.Fragilis Group, Pseudomonads and other non-enzyme microorganisms.

Cephalosporins III generation. Cefalosporins III generations are along with general features there are certain features. Ceftriaxone and Cefotaxim are the basic AMP of this group and practically do not differ from each other in their antimicrobial actions. Both drugs actively act on the Streptococcus SPP., At the same time, at the essential part of the pneumococci, as well as in the green streptococci, showing resistance to penicillin, the sensitivity to ceftriaxone and cefotaxim are preserved. The effect of cefotaxim and ceftriaxone is subject to S.Aureus (except MRSA), in a slightly lesser extent - the KNS. Corynebacteria (except C.JeIKEIUM), as a rule, manifests sensitivity. Stability exhibit B.Sereus, B.antracis, L.monocytogenes, MRSA and Enterococci. The high activity of ceftriaxone and cefotaxim demonstrate with respect to H.INFLUENZAE, M.Catarrhalis, Gonococcal and Montingokokkov, including strains with reduced sensitivity to the action of penicillin, regardless of the stability mechanism. Almost all representatives of the Enterobacteriaceae family, incl. Microorganisms that produce B-lactamases of a wide spectrum are subject to active natural effects of ceftaxim and ceftriaxone. E.Coli and Klebsiella SPP. They have stability, most often due to BRS products. Hyperproduction of chromosomal B-lactamas class C is usually caused by the stability of P.rettgeri, P.Stuartii, M.Morganii, Serratia SPP., C.Freundii, Enterobacter SPP.

Sometimes the activity of Cefotaxim and Ceftriaxone in vitro is manifested in relation to certain P.aeruginosa strains, other non-enzyme microorganisms, as well as B.Fragilis, but this is not enough to ensure that they can be used in the treatment of relevant infections.

Between ceftazidim, cefoperazone and cefotaxime, ceftriaxone there are similarities on the main antimicrobial properties. Distinctive characteristics of ceftazidim and cefoperazone from Cefotaxim and Ceftriaxone:

Show high sensitivity to hydrolysis BRS;

There are significantly less activity in relation to streptococci, primarily S.pneumoniae;

Pronounced activity (especially at ceftazidim) in relation to P.aeruginosa and others. Nefernizing microorganisms.

The differences between Cefixima and Cefybutene from Cefotaxim and Ceftriaxone:

Both drugs do not act or act on P.rettgeri, P.Stuartii, M.Morganii, Serratia SPP., C.Freundii, Enterobacter SPP.;

Cefibutene is low-effective in relation to greening streptococci and pneumococcis are little exposed to CEFTIBUTEN;

There is no significant activity in relation to Staphylococcus SPP.

Cephalosporins IV generation. Between the cefepim and cephalosporins III of generation a lot in common in many parameters. However, the features of the chemical structure allow the cefpin to penetrate with greater confidence through the external membrane of gram-negative microorganisms, as well as to have relative resistance to hydrolysis of chromosomal B-lactamases of class C. Therefore, together with its properties that distinguish the basic cephalosporins of the III generation (Ceftriaxone, Cefotaxim), the cefpinim has the following features:

High activity in relation to non-enzyme microorganisms and P.aeruginosa;

Increased resistance to hydrolysis in lactamas of an extended spectrum (this fact does not fully determine its clinical value);

Effect on the following microorganisms-hyperproducers of chromosomal V-lactamas class C: p.rettgeri, P.Stuartii, M.Morganii, Serratia SPP., C.Freundii, Enterobacter SPP.

Inhibitory-proof cephalosporins. Cefoperazone / Sulbaktam is the only representative of this group in Laktam. Compared to the cefoperazone, the combined drug has an expanded spectrum of action by influencing anaerobic microorganisms. Also, the action of the drug is subject to the majority of enterobacteria strains, which produce in lactamases of an extended and wide spectrum. The antibacterial activity of Sulbactam allows this AMP to exhibit high activity with the ACINETOBACTER SPP.

Pharmacokinetics. Operal cephalosporins have a good suction in the gastrointestinal tract. A specific drug is distinguished by its bioavailability, varying between 40-50% (in cue) and 95% (at cefaclor, cefadroxyl and cephalexin). The presence of food can slightly slow down the reels of Cefibutene, Cephixima and Cefaclorian. Food helps during the absorption of Cefuroxime Axietyl release the active cefuroxime. Under the introduction of V / m, there is a good absorption of parenteral cephalosporins. The distribution of cephalosporins is carried out in many organs (except for the prostate gland), tissues and secrets. In the peritoneal, pleural, pericardial and synovial fluids, in the bones, soft tissues, skin, muscles, liver, kidneys and lungs, high concentrations are marked. Cepoperazon and ceftriaxone create the highest levels in bile. In cephalosporins, in particular ceftazidim and cefuroxime, the ability to penetrate into the intraocular fluid is well, and not to create therapeutic levels in the rear eye chamber. Cephalosporins III generation (ceftazidim, ceftriaxone, cefotaxim) and the IV generation (cefepim) have the most ability to pass through the BGB, as well as to create therapeutic concentrations in the Code. Cefuroxime moderately overcomes the BGB solely in the case of inflammation of the brain shells.

In most cephalosporins (except cefotaxim, biotracting with the formation of active metabolite) there is no ability to be metabolized. The conclusion of drugs is carried out mainly through the kidneys, while creating very high concentrations in the urine. Ceftriaxone and cefoperason have a double path of removal - liver and kidneys. Most cephalosporins have a half-life from 1 to 2 hours. Cefibutene, Zefisim differ in a longer period - 3-4 hours, at ceftriaxone it increases to 8.5 hours. Thanks to this indicator, these drugs can be taken 1 time per day. Renal failure entails the correction of the dosing mode of antibiotics of the cephalosporins group (except cefopezone and ceftriaxone).

Cephalosporins I generation. Mostly today cefasoline Used as perioperative prophylaxis in surgery. It is also used in infections of soft tissues and skin.

Since Cefhazoline has a narrow spectrum of activity, and among potential pathogens, resistance to the action of cephalosporins is common, then recommendations for the use of cefazoline for the treatment of respiratory tract infections and MVP today there are no sufficient justifications.

Cephalexin is used in the treatment of streptococcal tonsilotlopharygitis (as a preparation of the second row), as well as over-hospital infections of soft tissues and skin of light and moderate severity.

Cephalosporins II generation

Cefuroxime used:

Under community-hospital pneumonia requiring hospitalization;

Under community-friendly infections of soft tissues and skin;

With IWE infections (pyelonephritis of medium and severe severity); Antibiotic Cephalosporin Tetracycline anti-tuberculosis

As perioperative prophylaxis in surgery.

Cefaclor, Cefuroxime Axetil Used:

In infections of the VDI and NDP (community-acquired pneumonia, the exacerbation of chronic bronchitis, acute sinusitis, iso);

Under community-friendly infections of soft tissues and skin of light, moderate severity;

IMP infections (acute cystitis and pyelonephritis in children, pyelonephritis in women during lactation, pyelonephritis of light and moderate severity).

Cefuroxime Axietyl and cefuroxime can be used as stepped therapy.

Cephalosporins III generation

Ceftriakson, Cefotaxim Apply with:

Non-hospital infections - acute gonorrhea, iso (ceftriaxone);

Heavy nosocomial and community-friendly infections - sepsis, meningitis, generalized salmonelles, infections of small pelvis organs, intraabdominal infections, severe forms of infections of joints, bones, soft tissues and skin, heavy forms of IWE infections, NDP infections.

Cefoperasazon, Ceftazidim prescribe with:

Treatment of severe community-friendly and nosocomial infections of various localization in the case of a confirmed or possible etiological effect of P.aeruginosa and others. Nefermenting microorganisms.

Treatment of infections against the background of immunodeficiency and neutropenia (including neutropenic fever).

Cephalosporins III generation can be applied parenterally in the form of monotherapy or together with antibiotics etc. groups.

Cefibutene, Zefisim effective:

PRIINFECTIONS OF MVP: acute cystitis and pyelonephritis in children, pyelonephritis in women during pregnancy and breastfeeding, pyelonephritis of light and moderate severity;

As an oral stage of the stepwise therapy of different heavy nosocomial and community-acquired infections caused by gram-negative bacteria, after obtaining a resistant effect from drugs intended for parenteral reception;

In case of infections of the DPI and NDP (receiving Cefibutene in the case of possible pneumococcal etiology is not recommended).

Cefoperazazon / Sulbaktam apply:

In the treatment of severe (mainly nosocomial) infections caused by mixed (aerobic anaerobic) and a poly-resistant microflora - sepsis, NDP infections (pulmonary abscess, lung abscess, pneumonia), complicated MWP infections, intraabdominal infections of a small pelvis;

In case of infections against neutropenia, as well as other immunodeficiency states.

Cephalosporins IV generation. Used with severe, mainly nosocomial, infections, provoked by a poly-resistant microflora:

Intraabdomominal infections;

Infections of joints, bones, leather and soft tissues;

Complicated inapplications

NDP infections (empty pleura, lung abscess, pneumonia).

Also cephalosporins IV generation are effective in the treatment of infections on the background of neutropenia, as well as other immunodeficiency states.

Contraindications

It is impossible to use with allergic reactions to cephalosporins.

5. Group of carbapenem

Carbapenes (impedite and meropenem) belong to V-lactams. Compared with penicillins and cephalosporins, they are more resistant to hydrolyzing effects of bacterial in-lactamaz, including BLRS.and have a broader spectrum of activity. Used in severe infections of various localization, including nosocomialMore often as reserve preparations, but in case of threatening life, infections can be considered as a priority empirical therapy.

Mechanism of action. Carbapenes have a powerful bactericidal effect due to disruption of the cell wall of bacteria. Compared to other B-lactams, the carbapens are able to penetrate the outer membrane of gram-negative bacteria and, in addition, to have a pronounced PE with respect to them.

Spectrum of activity. Carbapenes act on many gram-positive, gram-negative and anaerobic microorganisms.

The carbapenes are sensitive staphylococci (except MRSA.), streptococci, including S.pneumoniae. (according to activity in relation to armp carbapenams are inferior vancomycin), Gonococci, Meningococci. The imipenem acts on E.Faecalis.

Carbapenes are highly active in relation to most gram-negative bacteria Enterobacteriaceae. (Intestinal wand, Klebsiella, Protea, Enterobacter, Citrobacter, Asinobacter, Morganla), including in relation to strains resistant to cephalosporins III-IV generations and inhibitors of penicillins. Somewhat lower activity in relation to the protea, serration, H.INFLUENZAE.. Most strains P.aeruginosa. Initially sensitive, but in the process of applying carbapes, there is an increase in resistance. So, according to a multicenter epidemiological study conducted in Russia in 1998-1999, resistance to imipenem of nosocomial strains P.aeruginosa. In the Orit amounted to 18.8%.

Carbapenes are relatively poorly acting on B.cepaacia.Sustainable is S.maltophilia.

Carbapenes are highly active with respect to spore-forming (except C.difficile) and dislike (including B. Fragilis) Anaerobov.

Secondary stability of microorganisms (except P.aeruginosa.) It rarely develops to the carbapenes. For sustainable pathogens (except P.aeruginosa.) It is characterized by cross-resistance to imipenem and meropenem.

Pharmacokinetics. Carbapenes apply only parenterally. Well distributed in the body, creating therapeutic concentrations in many tissues and secrets. With inflammation of the brain shells penetrate through the BGB, creating concentrations in the CME equal to 15-20% of the blood plasma level. Carbapenes are not metabolized, derived mainly by the kidneys unchanged, therefore, with renal failure, there is a significant slowdown in their elimination.

Due to the fact that the imparency is inactivated in the kidney channels of the enzyme dehydropptidase I and at the same time therapeutic concentrations in the urine are not created, it is used in combination with cilastatin, which is a selective inhibitor of dehydropptidase I.

When conducting hemodialysis, carbapenams and cilastatin are quickly removed from the blood.

Indications:

1. Heavy infections, predominantly nosocomial caused by poly-resistant and mixed microflora;

2. ANDnFECS NDP (pneumonia, lung abscess, pleural empyema);

3. Complicated infections MVP;

4. ANDnTRABdomominal infections;

5. ANDnFECTIONS OF A LAST PAZA;

6. FROMePSIS;

7. ANDskin and soft tissue;

8. I. nFECS OF BACKES AND JOINS (only by imipenem);

9. E.ndocarditis (only by imipenem);

10. Bacterial infections in patients with neutropenia;

11. Meningitis (Meropene only).

Contraindications. Allergic reaction to carbapenes. The imipenem / cilastatin cannot be used as an allergic reaction to cilastatin.

6. Group of Monobakatam

From the monobactam, or monocyclic V-lactam, in clinical practice one antibiotic is applied - aztreonam. It has a narrow spectrum of antibacterial activity and is used to treat infections caused by aerobic gram-negative flora.

Mechanism of action.Azitreons have a bactericidal effect, which is associated with a violation of the formation of the cell wall of bacteria.

Spectrum of activity. The originality of the antimicrobial spectrum of the aztreonam is due to the fact that it is resistant to many V-lactamases produced by aerobic gram-negative flora, and at the same time destroyed in lactamases of staphylococcus, bacteroids and BRS.

Clinical importance is the activity of aztreonam in relation to many microorganisms of the family Enterobacteriaceae. (E.Coli., Enterobacter, Klebsiella, Protea, Sergery, Citrobacter, Providence, Morganla) and P.aeruginosa., with respect to nosocomial strains resistant to aminoglycosides, ureidopenicillins and cephalosporins.

Aztreonam does not act on asinobacter, S.maltophilia, B.cepaacia., gram-positive coils and anaerobes.

Pharmacokinetics.Azitreon applies only parenterally. It is distributed in many tissues and environmental environments. It passes through the BC with inflammation of the brain shells, through the placenta and penetrates into breast milk. It is very slightly metabolized in the liver, excreted mainly by the kidneys, by 60-75% unchanged. The half-life during the normal function of the kidneys and the liver is 1.5-2 hours, under the cirrhosis of the liver may increase to 2.5-3.5 hours, with renal failure - up to 6-8 hours. When conducting hemodialysis, the concentration of aztreonam in the blood decreases 25-60%.

Indications.Aztreonam is a reserve preparation for the treatment of infections of various location caused by aerobic gram-negative bacteria:

1. NDP infections (community-acquired and nosocomial pneumonia);

2. intraabdominal infections;

3. infections of small pelvis organs;

4. Infectilation of MVP;

5. Skin infections, soft tissues, bones and joints;

6. Sepsis.

Considering the narrow antimicrobial spectrum of the aztreonma action, during empirical therapy of heavy infections should be prescribed in combination with AMP, active against gram-positive cookers (oxacillin, cephalosporins, lincoosamides, vancomycin) and anaerobov (metronidazole).

Contraindications.Allergic reactions to aztreona in history.

7. A group of tetracycline

Tetracyclines are one of the early class of AMP, the first tetracycles were obtained in the late 40s. Currently, due to the emergence of a large number of microorganisms resistant to tetracycles and numerous HP, which are characteristic of these drugs, their use is limited. The largest clinical value of tetracycline (natural tetracycline and semi-synthetic doxycycline) are preserved with chlamydial infections, rickettsiosis, some zoonoses, severe acne.

Mechanism of action. Tetracyclines have a bacteriostatic effect, which is associated with a disruption of protein synthesis in a microbial cell.

Spectrum of activity. Tetracyclines are considered an AMP with a wide range of antimicrobial activity, however, in the process of their many years of use, many bacteria have acquired resistance to them.

Among gram-positive Cockks is the most sensitive to the pneumococcus (with the exception of an ARP). At the same time, more resistant more than 50% of strains S.pyogenes, more than 70% of staphylococci nosocomial strains and the vast majority of enterococci. From gram-negative cocci, meningococci and M.CatarRhalisAnd many gonococci is resistant.

Tetracycles act on some gram-positive and gram-negative sticks - Listeria, H.INFLUENZAE, H.DUCREYI., Iracinia, Campylobacter (including H.pylori.), Brucella, Bartonella, Vibrihrines (including Holera), causative agents of granuloma, Siberian ulcers, plague, tularemia. Most of the strains of intestinal sticks, Salmonella, Shigell, Klebsiell, Enterobacter are stable.

Tetracyclines are active against spirochete, leptospir, borrelius, rickettsies, chlamydia, mycoplasmas, actinomycetes, some simplest.

Among the anaerobic flora to tetracycles are sensitive to Klostridia (except C.difficile), fuzobacteria, P.acnes. Most bacteroid strains are stable.

Pharmacokinetics. When taking inside, tetracycline is well absorbed, and doxycycline is better than tetracycline. Doxycycline bioavailability does not change, and tetracycline - 2 times decreases under the influence of food. The maximum concentrations of blood serum preparations are created in 1-3 hours after intake. When in / in the introduction, significantly higher concentrations in the blood are rapidly achieved than when ingestion.

Tetracyclines are distributed in many organs and environmental environments, and doxycycline creates higher tissue concentrations than tetracycline. Concentrations in the CMF are 10-25% of serum levels, concentrations in bile 5-20 times higher than in blood. Tetracycles have a high ability to pass through the placenta and penetrate into breast milk.

The excretion of hydrophilic tetracycline is carried out mainly by the kidneys, so with renal failure, its elimination is significantly violated. More lipophilic doxycycline is excreted not only by the kidneys, but also the gastrointestinal tract, and in patients with impaired kidney function, this path is the main one. Doxycycline has 2-3 times longer half-life compared to tetracycline. In hemodialysis, tetracycline is removed slowly, and doxycycline is not deleted at all.

Indications:

1. Chlamydial infections (psychez, trachoma, urethritis, prostatitis, cervicitis).

2. Mycoplasma infections.

3. Borreliosis (Lyme Disease, Return Tiff).

4. Rickesciosis (ku-fever, spotted fragile rocky mountains, raw tit).

5. Bacterial zoonoses: brucellosis, leptospirosis, Siberian ulcers, plague, tularemia (in the last two cases - in combination with streptomycin or gentamicin).

6. NDP infections: aggravation of chronic bronchitis, community-hospital pneumonia.

7. Intestinal infections: cholera, yersiniosis.

8. Gynecological infections: adnexitis, salpingooforitis (with severe flow, in combination with in lactams, aminoglycosides, metronidazole).

9. Angry rash.

10. Pink acne.

11. Wound infection after animal bites.

12. STIs: syphilis (with allergies to penicillin), granuloma, venereal lymphogranul.

13. Eye infections.

14. Aktinomikosis.

15. Bacillry angiomatosis.

16. Eradication H.pylori. For ulcerative diseases of the stomach and duodenum (tetracycline, in combination with antisecretory drugs, bismuth subcitrate and other AMP).

17. Prevention of tropical malaria.

Contraindications:

Age up to 8 years.

Pregnancy.

Lactation.

Heavy liver pathology.

Renal failure (tetracycline).

8. Group of aminoglycosides

Aminoglycosides are one of the early classes of antibiotics. The first aminoglycoside - streptomycin was obtained in 1944. Currently, three generations of aminoglycosides are distinguished.

The main clinical meaning of aminoglycosides has in the treatment of nosocomial infections caused by aerobic gram-negative pathogens, as well as infectious endocarditis. Streptomycin and Canamycin are used in the treatment of tuberculosis. Neomycin as the most toxic among aminoglycosides is applied only inside and locally.

Aminoglycosides have potential nephrotoxicity, output and can cause neuromuscular blockade. However, the accounting of risk factors, one-time introduction of the entire daily dose, short courses of therapy and TLM can reduce the degree of manifestation of HP.

Mechanism of action. Aminoglycosides have a bactericidal effect, which is associated with violation of the synthesis of protein ribosomes. The degree of antibacterial activity of aminoglycosides depends on their maximum (peak) serum concentration. When combined with penicillins or cephalosporine, synergism for some gram-negative and gram-positive aerobic microorganisms.

Spectrum of activity. For aminoglycosides II and III generation, dose-dependent bactericidal activity against gram-negative microorganisms of the family is characterized Enterobacteriaceae. (E.Coli, Proteus. SPP., Klebsiella. SPP., Enterobacter. SPP., Serratia. SPP. et al.), as well as non-enzyme gram-negative sticks ( P.aeruginosa, Acinetobacter. SPP.). Aminoglycosides are active with respect to staphylococcus, except MRSA. Streptomycin and kanamycin act on M.TUBERCULOSIS, while amikacin is more active in relation to M.Avium and other atypical mycobacteria. Streptomycin and gentamicin act on enterococci. Streptomicin is active against the pathogens of the plague, Tularemia, Brucellize.

Aminoglycosides inactive in relation S.pneumoniae., S.maltophilia, B.cepaacia., anaerobov ( Bacteroides. SPP., Clostridium. SPP. and etc.). Moreover, resistance S.pneumoniae., S.maltophilia and B.cepaacia. Aminoglycosides can be used when identifying these microorganisms.

Despite the fact that aminoglycosides iN. vitro. Active in relation to Hemophil, Shigell, Salmonella, Legionell, clinical efficacy in the treatment of infections caused by these pathogens has not been established.

Pharmacokinetics. When taken inside, the aminoglycosides are practically not absorbed, therefore parenterally applied (except neomycine). After the I / M of the introduction is absorbed quickly and completely. Peak concentrations are developing 30 minutes after the end of the infusion and 0.5-1.5 hours after the introduction.

Peak concentrations of aminoglycosides varies from different patients, as they depend on the volume of distribution. The volume of distribution, in turn, depends on body weight, liquid volume and adipose tissue, patient state. For example, in patients with extensive burns, ascites, the volume of the distribution of aminoglycosides is increased. On the contrary, with dehydration or muscle dystrophy, it decreases.

Aminoglycosides are distributed in extracellular fluid, including blood serum, exudate abscesses, ascitic, pericardial, pleural, synovial, lymphatic and peritoneal fluids. Create high concentrations in organs with good blood supply: liver, lungs, kidneys (where they accumulate in cortical matter). Low concentrations are marked in sputum, bronchial secrete, bile, breast milk. Aminoglycosides are poorly passing through the BGB. With inflammation of brain shells, permeability increases slightly. In newborns, higher concentrations are achieved in the SMM than adults.

Aminoglycosides are not metabolized, are removed by the kidneys by glomerular filtration unchanged, creating high concentrations in the urine. The speed of excretion depends on the age, the functions of the kidneys and the concomitant pathology of the patient. In patients with fever, it can increase, when the kidney function decreases significantly slows down. In the elderly, as a result of decreasing glomerular filtration, the excretion can also slow down. The half-life of all aminoglycosides in adults with a normal kidney function is 2-4 hours, in newborns - 5-8 hours, in children - 2.5-4 hours. In renal failure, the half-life can increase to 70 hours or more.

Indications:

1. Empirical therapy (In most cases, they are prescribed in combination with B-lactams, glycipeptides or anti-indesses, depending on the intended pathogens):

Sepsis unclear etiology.

Infectious endocarditis.

Post-traumatic and postoperative meningitis.

Fever in patients with neutropenia.

Nosocomial pneumonia (including ventilation).

Pyelonephritis.

Intraabdominal infections.

Infectness of small pelvis organs.

Diabetic stop.

Postoperative or post-traumatic osteomyelitis.

Septic arthritis.

Local therapy:

Eye infection - bacterial conjunctivitis and keratitis.

2. Specific therapy:

Plague (streptomycin).

Tularemia (streptomycin, gentamicin).

Brucellosis (streptomycin).

Tuberculosis (streptomycin, kanamycin).

Antibiotic pyrofilax

Deconptamination of the intestine in front of planned operations on the colon (neomycin or canamycin in combination with erythromycin).

Aminoglycosides cannot be used for the treatment of community-hospital pneumonia both in the outpatient and inpatient conditions. This is due to the lack of activity of this group of antibiotics in relation to the main pathogen - pneumococcus. With therapy of nosocomial pneumonia, aminoglycosides are prescribed parenterally. Endotracheal administration of aminoglycosides due to unpredictable pharmacokinetics does not lead to an increase in clinical efficacy.

It is erroneous is the purpose of the aminoglycoside for therapy of cinellosis and salmonellosis (both inside and parenterally), since they are clinically ineffective with respect to pathogens localized intracellularly.

Aminoglycosides should not be used to treat uncomplicated MWP infections, except when the causative agent is resistant to other, less toxic antibiotics.

Aminoglycosides should also not be used for local applications in the treatment of skin infections due to the rapid formation of resistance in microorganisms.

It is necessary to avoid using aminoglycosides for flow drainage and irrigation of the abdominal cavity due to their pronounced toxicity.

Dosing rules of aminoglycosides. In adult patients, two aminoglycoside appointment modes can be carried out: traditionalwhen they are injected 2-3 times a day (for example, streptomycin, kanamycin and amikacin - 2 times; gentamicin, tobramycin and neutylmicin - 2-3 times), and single introduction of the whole daily dose.

The one-time introduction of the entire daily dose of aminoglycoside allows you to optimize therapy with drugs of this group. Numerous clinical trials have shown that the effectiveness of treatment in one-time assignment of aminoglycosides is the same as in the traditional, and nephrotoxicity is less expressed. In addition, with a single introduction of a daily dose, economic costs decrease. However, this mode of appointment of aminoglycosides should not be used in the treatment of infectious endocarditis.

The choice of the dose of aminoglycosides is influenced by such factors as the mass of the patient's body, localization and severity of infection, the kidney function.

In parenteral administration, the dose of all aminoglycosides should be calculated on a kilogram of body weight. Considering that aminoglycosides are poorly distributed in adipose tissue, in patients with a body weight exceeding an ideal by more than 25%, a dose correction must be carried out. At the same time, a daily dose designed for the actual body weight should be empirically reduced by 25%. At the same time, exhausting patients dose increases by 25%.

Under meningitis, sepsis, pneumonia and other severe infections, the maximum doses of aminoglycosides are prescribed, with minimum or medium infections. Maximum doses should not be prescribed to the elderly people.

In patients with renal failure, the dose of aminoglycosides must be understood. This is achieved or a decrease in a single dose, or an increase in the intervals between the introductions.

Therapeutic medicinal monitoring. Since the pharmacokinetics of aminoglycosides is unstable and depends on a number of reasons, to achieve the maximum clinical effect while reducing the risk of HP development, TLM is carried out. At the same time, the peak and residual concentrations of aminoglycosides in serum are determined. Peak concentrations (60 minutes after a / m or 15-30 minutes after the end of the Introduction), on which the effectiveness of therapy depends, under normal dosing mode, it should be for gentamicin, tobramycin and nonylmicin at least 6-10 μg / ml , for kanamycin and amikacin - at least 20-30 μg / ml. Residual concentrations (before the next administration), which indicate the degree of cumulation of aminoglycosides and allow to control the safety of therapy, for gentamicin, tobramycin and nonylmicin, should be less than 2 μg / ml, for Canamycin and amikacin - less than 10 μg / ml. TLM is primarily necessary in patients with severe infections and in the presence of other risk factors for the toxic effect of aminoglycosides. When the daily dose is prescribed in the form of one-time administration, the residual concentration of aminoglycosides is usually controlled.

Contraindications: Allergic reactions to aminoglycosides.

9. Levomycetina

Levomycetins - antibiotics with a wide range of action. The levomycenetin group includes levomycetin and syntomicin. The first natural levomycetin antibiotic was obtained from the culture of the radiant fungus Streptomyces Venezualae in 1947, and in 1949 a chemical structure was established. In the USSR, this antibiotic was called "Levomycetin" due to the fact that it is a leaving isomer. With respect to bacteria, an expulsive isomer is not effective. The antibiotic of this group, obtained by the synthetic path in 1950, was called "syntomicin". The composition of the syntomicin includes a mixture of levieving and re-engraving isomers, which is why the action of syntomicine is weaker than 2 times, compared with the leftomycetin. Synthomycin is used solely externally.

Mechanism of action. Levomycenetine acraiserizable bacteristatic effects, and specifically disrupt protein synthesis, fixed on ribosomes, which leads to the oppression of the microbial cell reproduction function. This property in the bone marrow becomes the cause of the formation of erythrocytes and leukocytes (can lead to anemia and leukopenia), as well as the oppression of blood formation. In the isomers there is an ability to provide the opposite effect on the central nervous system: the left-hander isomer inhibits the central nervous system, and the releger - it excites it moderately.

Circle activity. Antibiotics-Levomycetins exhibit activity in relation to many gram-negative and gram-positive bacteria; Viruses: Chlamydia Psittaci, Chlamydia trachomatis; Spirocaetales, Rickettsiae; Strains of bacteria that are not agencies of penicillin, streptomycin, sulfonamides. An insignificant action is available on acid-resistant bacteria (tuberculosis pathogens, some saprophytes, leprosy), Protozoa, Clostridium, Pseudomonas Aeruginosa. The development of drug resistance to antibiotics of this group is relatively slow. Levomycetins are not able to cause cross-resistance to other chemotherapeutic LS.

Pprovision. Levomycetins are used in the treatment of trachomas, gonorrhea, various types of pneumonia, meningitis, cough, ricketersiosis, chlamydia, tularemia, brucellosis, salmonellosis, dysentery, parathy, abdominal typhoids, etc.

10. Group of glycopeptide

Glixopeptides include natural antibiotics - vancomycin and teicoplan. Vancomycin is used in clinical practice since 1958, Teicoplast - from the mid-80s. Recently, interest in glycopeptide has increased due to increasing frequency nosocomial infectionscaused by gram-positive microorganisms. Currently, glycopeptides are drugs for infections caused by MRSA., MRSE, as well as enterococci resistant to ampicillin and aminoglycosidam.

Mechanism of action. Glycopeptides violate the synthesis of the cell wall of bacteria. Have a bactericidal action, however, in relation to enterococci, some streptococci and KNS. Bacteriostatically act.

Spectrum of activity. Glycopeptides are active against gram-positive aerobic and anaerobic microorganisms: staphylococci (including MRSA., MRSE), streptococci, pneumococci (including armp), enterococci, peptopulationococci, sheets, corenebacteria, clostridium (including C.difficile). Gram-negative microorganisms are resistant to glycopeptides.

According to the spectrum of antimicrobial activity, Vancomycin and Teicoplanine are similar, however there are some differences in the level of natural activity and acquired resistance. Teicoplan in vitro. more active in relation S.Aureus. (including MRSA.), streptococci (including S.pneumoniae.) And enterococci. Vancomycin iN. vitro. more active in relation KNS..

In recent years, in several countries allocated S.Aureus. with reduced sensitivity to vancomycin or to vancomycin and teiquotlap.

For enterococci, a faster development of vancomycin resistance is characterized by: currently in the USI in the US level of resistance E.Faecium. Vancomycin is about 10% or more. In this case, it is clinically important that some Vre. Keep sensitivity to teiquotlap.

Pharmacokinetics. Glycopeptides are practically not absorbed when taking inside. Bioavailability Teicoplane at the I / M administration is about 90%.

Glycopeptides are not metabolized, removed by the kidneys unchanged, so when renal failure requires dose correction. Preparations are not removed during hemodialysis.

Half-life Vancomycin with a normal kidney function is 6-8 h, the teiquotoplanine is from 40 hours to 70 hours. The long-lasting period of the teicoplanine makes it possible to assign it once a day.

Indications:

1. Infections caused by MRSA., MRSE.

2. Staphylococcal infections with allergies to V-lactams.

3. Heavy infections caused by Enterococcus SPP., C.JeIikeium, B.Cereus, F.Meningosepticum.

4. Infectious endocarditiscaused by green streptococci and S.BOVIS, with allergies to V-lactams.

5. Infectious endocarditiscaused E.Faecalis (in combination with gentamicin).

6. Meningitiscaused S.pneumoniae.resistant to penicillins.

Empirical therapy of life-threatening infections in suspected staphylococcal etiology:

Infective endocarditis of a tricuspid valve or prosthetized valve (in combination with gentamicin);

What is antibiotic

This is a group of drugs that have the ability to block proteins synthesis and thereby coagulate reproduction, height of living cells. All types of antibiotics are used to treat infectious processes that are caused by various strains of bacteria: Staphylococcus, Streptococcus, Meningokok. For the first time, medication was developed in 1928 Alexander Fleming. Antibiotics of some groups are prescribed in the treatment of oncological pathology as part of combined chemotherapy. In modern terminology, this type of medication is often called antibacterial drugs.

Classification of antibiotics by the mechanism of action

Penicillin-based medicines were the first drugs of this species. There is a classification of antibiotics by groups and the mechanism of action. Some of the drugs have a narrow orientation, others - a wide range of action. This parameter determines how much the medicine will affect human health (both in positive and negative terms). Medicines help to cope or reduce mortality of such serious diseases:

sepsis;
gangrene;
meningitis;
pneumonia;
syphilis.

Bactericidal

This is one of the species from the classification of antimicrobial means of pharmacological action. Bactericidal antibiotics are a drug that cause lysis, the death of microorganisms. The medication inhibits the synthesis of membranes, suppress the products of DNA components. These properties have the following groups of antibiotics:

carbapenes;
penicillins;
fluoroquinolones;
glycopeptides;
monobactam;
phosphomycin.

Bacteriostatic

The action of this group of medications is aimed at the oppression of protein synthesis by cells of microorganisms, which does not allow them to continue to multiply and develop. The result of the drug action is to limit the further development of the pathological process. This impact is characteristic of the following groups of antibiotics:

lincosamines;
macrolides;
aminoglycosides.

Classification of antibiotics for chemical composition

The main separation of drugs is carried out in the chemical structure. Each of them is based on different active substance. Such a separation helps to fight purposefully with a specific type of microbes or provide a wide range of action for a large number of varieties. This does not give bacteria to develop resistance (resistance, immunity) to a specific type of medication. The main types of antibiotics are described below.

Penicillins

This is the very first group that was created by a person. Antibiotics of the penicillin group (Penicillium) has a wide range of exposure to microorganisms. Inside the group there is an additional division on:

natural penicillin facilities - are produced by mushrooms under normal conditions (phenoxymethylpenicillin, benzylpenicillin);
semi-synthetic penicillins, have a greater resistance against penicillinases, which significantly expands the spectrum of the effect of antibiotic (meticillin, oxacillin medicines);
expanded action - Ampicillin preparations, amoxicillin;
medicines with a wide range of action - agenicillin medication, Meslocillin.

In order to reduce the resistance of bacteria in this type of antibiotics, penicillinase inhibitors are added: sulbacts, pelvobactam, clavulanic acid. Bright examples of such medicines are: Tazocin, Augmentin, Tazrobide. Assign funds under the following pathologies:

respiratory system infections: pneumonia, sinusitis, bronchitis, laryngitis, pharyngitis;
urogenital: urethritis, cystitis, gonorrhea, prostatitis;
digestive: dysentery, cholecystitis;
syphilis.

Cephalosporins

The bactericidal property of this group has a wide range of action. The following generations of ceflufosporins are distinguished:

I-e, Cefradin, Cephalexin, Cefhazolina;
II, funds with cefaclor, cefuroxime, cefoxytin, cefotiam;
Iii-e, ceftazidim, cefotaxim, cefoperason, cefriaxone, cefodizma;
IV-e, remedies with cefpir, cefepim;
V-e, Fethobiprola, Ceftarolina, Fetolosan.

There is a large part of the antibacterial medicines of this group only in the form of injections, therefore they are used more often in clinics. Cephalosporins are the most popular type of antibiotics with inpatient treatment. Assign this class of antobacterial means at:

pyelonephritis;
generatization of infection;
inflammation of soft tissues, bones;
meningitis;
pneumonia;
lymphangitis.

Macrolids

Natural. It was synthesized for the first time in the 60s of the 20th century, they include spiramycin, erythromycin, Midekamycin, Josamycin.
Prodrugs, the active form is accepted after metabolism, for example, Toleandomycin.
Semi-synthetic. These are clarithromycin, telitromycin, azithromycin, diritromycin.

Tetracyclines

This species was created in the second half of the 20th century. Antibiotics of the tetracycline group have antimicrobial effects against a large number of strains of microbial flora. At high concentration, a bactericidal effect is manifested. The peculiarity of tetracycline is the ability to accumulate in the enamel of teeth, bone tissue. It helps in the treatment of chronic osteomyelitis, but also violates the development of a skeleton in young children. This group is prohibited for receiving pregnant girls, children under 12 years old. These antibacterial medicines are represented by the following drugs:

Oxytetracycline;
Tigecycline;
Doxycycline;
Minocycline.

Contraindications include hypersensitivity to components, chronic liver pathologies, porphyria. The following pathologies are indicated for use:

lyme disease;
intestinal pathology;
leptospirosis;
brucellosis;
gonococcal infections;
ricketsiosis;
trachoma;
actinomycosis;
tulara'yia.

Aminoglycosides

The active use of this number of medicines is carried out in the treatment of infections that caused a gram-negative flora. Antibiotics have a bactericidal action. Preparations show high efficiency, which is not associated with an indicator of the activity of the patient's immunity, makes these medicines indispensable when it is weakened and neutropenia. There are the following generations of these antibacterial agents:

Drugs of Canamycin, neomycin, leftomycetin, streptomycin belong to the first generation.
The second includes funds with gentamicin, tobramycin.
The third belongs to the preparations of amikacin.
The fourth generation is represented by ispamycin.

The following pathologies become indications for the use of this group of medicines.

Antibiotics are a huge group of bactericidal preparations, each of which is characterized by its spectrum of action, indications for the use and availability of certain consequences

Antibiotics - substances capable of suppressing the growth of microorganisms or destroy them. According to the definition of GOST, the antibiotics include substances of vegetable, animal or microbial origin. Currently, this definition is somewhat outdated, as a huge number of synthetic preparations have been created, but natural antibiotics were a prototype for their creation.

The history of antimicrobial preparations begins from 1928, when A. Fleming was first open penicillin. This substance was precisely open, and not created, as it always existed in nature. In the wilderness of it produces microscopic mushrooms of the genus Penicillium, protecting itself from other microorganisms.

Less than 100 years have created more than a hundred different antibacterial drugs. Some of them are already outdated and are not used in treatment, and some are entered into clinical practice.

How to act antibiotics

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All antibacterial drugs on the effect of exposure to microorganisms can be divided into two large groups:

bactericidal - directly cause death of microbes;
bacteriostatic - prevent the reproduction of microorganisms. Not able to grow and multiply, bacteria are destroyed by the immune system of a patient person.

Its effects of antibiotics are realized by many ways: some of them prevent the synthesis of microbes nucleic acids; Others prevent the synthesis of the cell wall of the bacteria, the third disturb the synthesis of proteins, and the fourth block the functions of the respiratory enzymes.

Groups of antibiotics

Despite the diversity of this group of drugs, they can be attributed to several main types. The basis of this classification is a chemical structure - drugs from the same group have a similar chemical formula, differing from each other by the presence or absence of certain fragments of molecules.

The classification of antibiotics implies the presence of groups:

Penicillin derivatives. This includes all drugs created on the basis of the first antibiotic itself. In this group, the following subgroups or generation of penicillin preparations are distinguished:

Natural benzylpenicillin, which is synthesized by mushrooms, and semi-synthetic drugs: methicillin, nafcillin.
Synthetic preparations: Carbenicillin and ticarcillin, with a broader spectrum of exposure.
Mixillas and azlocyllin, having an even wider range of action.

Cephalosporins - Nearest relatives of Penicillins. The very first antibiotic of this group - cefazolin C, is produced by the mushrooms of the genus Cephalosporium. Preparations of this group for the most part have a bactericidal action, that is, microorganisms kill. Several generations of cephalosporins are distinguished:

I generation: Cefazoline, Cephalexin, Cefradin, etc.
II generation: Cefsulodin, Cephamandol, cefuroxime.
III generation: cefotaxim, ceftazidim, cepodizim.
IV generation: cefpir.
V Generation: Ceftolozan, Ceftopibrol.

The differences between different groups consist mainly in their effectiveness - later generations have a larger spectrum of action and more efficient. Cephalosporins 1 and 2 generations in clinical practice are now used extremely rare, most of them are not even produced.

- Preparations with a complex chemical structure that have a bacteriostatic effect on a wide range of microbes. Representatives: azithromycin, rovamicine, josamicin, leucomycin and a number of others. Macrolids are considered one of the safest antibacterial drugs - they can be applied even pregnant women. Azalides and Ketolides are varieties of macorloids having differences in the structure of active molecules.

Another advantage of this group of drugs is capable of penetrating the cells of the human body, which makes them effective in the treatment of intracellular infections: ,.

Aminoglycosides. Representatives: Gentamicin, Amicacin, Canamycin. Effective with respect to a large number of aerobic gram-negative microorganisms. These drugs are considered the most toxic, can lead to sufficiently serious complications. Apply to the treatment of urinary tract infections ,.
Tetracyclines. Basically, this semi-synthetic and synthetic drugs that include: tetracycline, doxycycline, minocycline. Effective with respect to many bacteria. The disadvantage of these drugs is cross-stability, that is, microorganisms that have developed resistance to one drug will also be completely well-sensitive to another of this group.
Fluoroquinolones. These are fully synthetic preparations that do not have their own natural analog. All drugs of this group are divided into the first generation (pofloxacin, ciprofloxacin, norfloxacin) and second (levofloxacin, moxifloxacin). It is used most often for the treatment of ENT infections (,) and respiratory tract (,).
Lincoosamide. This group includes the natural antibiotic of Lincomicin and its derivative of clindamycin. Bacteriostatic, and bactericidal action, effect depends on the concentration.
Carbapenes. This is one of the most modern antibiotics acting on a large number of microorganisms. Preparations of this group belong to the antibiotics of the reserve, that is, applied in the most difficult cases when other medicines are ineffective. Representatives: imipenem, Meropenem, Ertapenem.
Polymixin. These are highly specialized drugs used to treat infections caused. Polymixinam includes Polymixin M and B. Lack of these drugs - toxic effects on the nervous system and kidneys.
Anti-tuberculosis means. This is a separate group of drugs with a pronounced action on. These include rifampicin, isoniazide and Pask. Other antibiotics are also used to treat tuberculosis, but only if resistance has been developed to the above-mentioned drugs.
Antifungal agents. This group includes drugs used for the treatment of micaoses - fungal lesions: ampothirecine B, nystatin, flukonazole.

Methods of use of antibiotics

Antibacterial drugs are available in different forms: tablets, powder, from which a solution for injection, ointments, drops, sprays, syrup, candles are prepared. Main ways of using antibiotics:

Oral - Reception through the mouth. You can take the medicine in the form of tablets, capsules, syrup or powder. The multiplicity of reception depends on the type of antibiotics, for example, azithromycin is taken once a day, and tetracycline - 4 times a day. For each type of antibiotic, there are recommendations in which it is indicated when it needs to be taken to meals, during or after. The effectiveness of the treatment and severity of side effects depends on this. Little children antibiotics are sometimes prescribed in the form of syrup - children are easier to drink fluid than swallowing a tablet or capsule. In addition, syrup can be sweetened to get rid of the unpleasant or bitter taste of the medicine itself.
Injection- in the form of intramuscular or intravenous injections. In this method, the drug enters the focus of infection and actively acts. The disadvantage of this method of administration is painfulness in the checker. Use injections with a moderate and severe diseases.

Important:making injections should exclusively medical sister under the conditions of clinic or hospital! At home, antibiotics prick is categorically not recommended.

Local- Application of ointments or creams directly to the focus of infection. This method of delivering the drug is mainly used in skin infections - face inflammation, as well as in ophthalmology - with infectious eye damage, for example, tetracycline ointment during conjunctivitis.

Only the doctor defines the path of administration. At the same time, many factors are taken into account: the absorption of the drug in the gastrointestinal tract, the state of the digestive system as a whole (in some diseases, the absorption rate is reduced, and the effectiveness of treatment decreases). Some drugs can be administered only in one way.

When injecting introduction, you need to know what can dissolve powder. For example, Abaktal can only be breeding only glucose, since when using sodium chloride, it is destroyed, which means that the treatment will be ineffective.

Sensitivity to antibiotics

Any organism is sooner or late to get used to the most severe conditions. It is fair to this statement and in relation to microorganisms - in response to the long-term effects of microbic antibiotics produce resistance to them. In medical practice, the concept of sensitivity to antibiotics was introduced - with what efficiency one or another drug on the causative agent affects.

Any assignment of antibiotics should be based on the knowledge of the sensitivity of the pathogen. Ideally, before appointing the drug, the doctor must analyze the sensitivity, and appoint the most effective drug. But the time of this analysis at the best case is a few days, and during this time an infection can lead to a sadder one.

Therefore, with infection with an unexplained causative agent, doctors prescribe drugs empirically - taking into account the most likely pathogen, with the knowledge of the epidemiological situation in a particular region and the medical institution. For this use the antibiotics of a wide range of action.

After analyzing the sensitivity, the doctor has the ability to change the drug to more efficiently. Replacing the drug can be produced and in the absence of an effect from treatment by 3-5 days.

More efficiently etiotropic (target) appointment of antibiotics. It turns out that the disease is caused by a bacteriological study, the type of pathogen is established. The doctor then selects a specific drug to which the microbe does not have resistance (stability).

Antibiotics are always effective

Antibiotics act only on bacteria and mushrooms! Bacteria is one-cell microorganisms. There are several thousand types of bacteria, some of which are quite normally coexist with a person - more than 20 types of bacteria live in a thick intestine. Part of the bacteria is a conditional pathogenic - they become the cause of the disease only under certain conditions, for example, when inhibiting the habitat for them. For example, very often prostatitis causes an intestinal wand falling ascending in from the rectum.

Note: absolutely ineffective antibiotics in viral diseases. Viruses are many times less bacteria, and antibiotics simply have no point of application of its ability. Therefore, antibiotics do not have an effect with a cold, since the cold in 99% of cases is caused by viruses.

Antibiotics with cough and bronchitis can be effective if these phenomena are caused by bacteria. To understand that only a doctor can be caused by a disease - for this, he prescribes blood tests, if necessary, a study of sputum, if it is departed.

Important:assign antibiotics yourself is unacceptable! This will only lead to the fact that part of the pathogens will develop resistance, and the next time the disease will cure much more difficult.

Of course, antibiotics are effective when this disease has an exclusively bacterial nature, it causes its streptococci or staphylococcal. For the treatment of angina use the most simple antibiotics - Penicillin, erythromycin. The most important angina in treating is the observance of the multiplicity of drug intake and the duration of treatment - at least 7 days. It is impossible to stop taking medication immediately after the state of the state, which is usually noted for 3-4 days. It should not be confused by a true thounded anchine, which may be viral origin.

Note: the unfit angina may cause acute rheumatic fever or!

Inflammation of the lungs () can have both bacterial and viral origin. Bacteria cause pneumonia in 80% of cases, therefore, even with empirical imposition, antibiotics at pneumonia have a good effect. In the viral pneumonia, antibiotics do not possess therapeutic effect, although they prevent the attachment of the bacterial flora to the inflammatory process.

Antibiotics and alcohol

The simultaneous admission of alcohol and antibiotics in a short period of time does not lead to anything good. Some drugs are destroyed in the liver, like alcohol. The presence of an antibiotic and alcohol in the blood gives a strong load on the liver - it simply does not have time to neloit ethyl alcohol. As a result, the likelihood of the development of unpleasant symptoms increases: nausea, vomiting, intestinal disorders.

Important: a number of drugs interact with alcohol at the chemical level, as a result of which the therapeutic effects are directly reduced. These drugs include metronidazole, Levomycetin, cefoperazone and a number of others. The simultaneous admission of alcohol and these drugs can not only reduce therapeutic effect, but also lead to shortness of breath, cramps and death.

Of course, some antibiotics can be taken against the background of alcohol use, but why risk health? It is better to refrain from alcoholic beverages for a while - the course of antibacterial therapy rarely exceeds 1.5-2 weeks.

Antibiotics during pregnancy

Pregnant women are hurting infectious diseases no less often than everyone else. But the treatment of pregnant antibiotics is very difficult. In the body of a pregnant woman grows and the fruit is growing - the future child is very sensitive to many chemicals. Incoming the emerging organism of antibiotics can provoke the development of malformations of the fetus development, toxic damage to the central nervous system of the fetus.

In the first trimester, it is advisable to avoid the use of antibiotics at all. In the second and third trimesters, their appointment is safer, but also, if possible, should be limited.

It is impossible to refuse to appoint antibiotics to a pregnant woman with the following diseases:

Pneumonia;
angina;
infected wounds;
specific infections: brucellosis, bulliosis;
sex infections: ,.

What antibiotics can be prescribed pregnant?

Almost no effect on the fruit of Penicillin, drugs of cephalosporine series, erythromycin, josamamicin. Penicillin, although it passes through the placenta, does not have a negative impact on the fetus. Cephalosporin and other named drugs penetrate the placenta in extremely low concentration and are not able to harm the future child.

Conditionally safe preparations include metronidazole, gentamicin and azithromycin. They are prescribed only on life indications when the benefit for a woman outweighs the risk for the child. These situations include heavy pneumonia, sepsis, other severe infections, in which a woman can simply die without antibiotics.

Which of the drugs can not be prescribed during pregnancy

It is impossible to use the following drugs in pregnant women:

aminoglycosides - able to lead to congenital deafness (exception - gentamicin);
clarithromycin, Roxitromycin - In the experiments, a toxic effect on animal embryos was rendered;
fluoroquinolones;
tetracycline - disrupts the formation of the bone system and teeth;
levomycetin - It is dangerous in late pregnancy due to the oppression of bone marrow functions in a child.

For some antibacterial drugs, there is no data on the negative impact on the fruit. It is explained simply - on pregnant women do not conduct experiments, allowing to find out the toxicity of drugs. Experiments on animals do not allow with 100% confidence to exclude all negative effects, since the metabolism of drugs in humans and animals can differ significantly.

It should be noted that before you should also refuse to receive antibiotics or change plans for conception. Some drugs have a cumulative effect - are able to accumulate in the body of a woman, and some time after the end of the course of treatment are gradually metabolized and output. Pregnant recommended no earlier than 2-3 weeks after the end of the antibiotics.

The effects of taking antibiotics

Antibiotics in the human body leads not only to the destruction of pathogenic bacteria. Like all foreign chemicals, antibiotics have a systematic action - to one way or another affect all organism systems.

Several groups of the side effects of antibiotics can be distinguished:

Allergic reactions

Almost any antibiotic can cause allergies. The severity of the reaction is different: a rash on the body, swelling of quinque (angioedema edema), anaphylactic shock. If an allergic rash is practically not dangerous, the anaphylactic shock may result in death. The risk of shock is much higher in the injections of antibiotics, which is why injections should be made only in medical institutions - emergency assistance can be provided.

Antibiotics and other antimicrobial drugs causing cross-allergic reactions:

Toxic reactions

Antibiotics can damage many organs, but most of all are subject to their exposure to the liver - against the background of antibacterial therapy, a toxic hepatitis may occur. Separate drugs have a selective toxic effect on other organs: aminoglycosides - on the auditory unit (cause deafness); Tetracyclines oppress the growth of bone tissue in children.

note: the toxicity of the drug usually depends on its dose, but at individual intolerance, sometimes enough smaller doses, so that the effect manifested itself.

Impact on the gastrointestinal tract

When taking some antibiotics, patients often complain about pain in the stomach, nausea, vomiting, chair disorders (diarrhea). These reactions are most often due to the local remedy effects of drugs. The specific effects of antibiotics on the intestinal flora leads to functional disorders of its activities, which is accompanied most often by diarrhea. This condition is also called antibiotic diarrhea, which in the people is more known under thermal dysbacteriosis after antibiotics.

Other side effects

Other adverse consequences include:

depression of immunity;
the emergence of antibiotic-resistant strains of microorganisms;
superinfection is a condition in which the microbes-resistant to this antibiotic are activated, leading to the emergence of a new disease;
violation of vitamins - due to the oppression of the natural flora of the colon, which synthesizes some group vitamins;
bacteriolism Yarisha-Gersheimer is a reaction. It occurs when the use of bactericidal drugs occurs when a large number of toxins are thrown into the blood as a result of the one-time death of a large number of bacteria. The reaction is similar to the clinic with shock.

Is it possible to use antibiotics with preventive purpose

Self-forming in the field of treatment led to the fact that many patients are especially true of young mothers, try to appoint themselves (or their child) an antibiotic with the slightest signs of colds. Antibiotics do not have a prophylactic action - they treat the cause of the disease, that is, the microorganisms are eliminated, and in the absence there are only side effects of drugs.

There is a limited number of situations where antibiotics are introduced to clinical manifestations of infection, to prevent it:

surgery - In this case, the antibiotic in the blood and tissues prevents the development of infection. As a rule, a rather single dose of the drug introduced 30-40 minutes before intervention. Sometimes even after appendectomy in the postoperative period, antibiotics do not bother. After "clean" surgical operations, antibiotics are not prescribed at all.
large injuries or wounds (Open fractures, earth wound pollution). In this case, it is absolutely obvious that an infection has got into a wound and it should be "criticized" before it appears;
emergency prevention of syphilisa It is carried out with unprotected sexual contact with a potentially sick person, as well as in health workers who have the blood of an infected person or other biological fluid hit the mucous membrane;
penicillin can be assigned to children For the prevention of rheumatic fever, which is an complication of an angina.

Antibiotics for children

The use of antibiotics in children as a whole does not differ from their use of other groups of people. Children of small age pediatricians most often prescribe antibiotics in syrup. This dosage form is more convenient for reception, in contrast to the injections completely painless. Antibiotics in tablets and capsules can be assigned to children older age. In case of severe, infection is transferred to the parenteral route of administration - injections.

Important: the main feature in the use of antibiotics in pediatrics is the dosages - children are prescribed smaller doses, since the calculation of the drug is carried out in terms of a kilogram of body weight.

Antibiotics are very effective preparations that have a large number of side effects at the same time. To recover with their help and do not harm your body, take them only to appoint a doctor.

What are the antibiotics? In which cases, the reception of antibiotics is necessary, and in what is dangerous? The main rules of treatment with antibiotics tells the pediatrician, Dr. Komarovsky:

Gudkov Roman, a renexcatyologist

Antibiotics and their classification

Beta lactama

Penicillins

Cephalosporins

Carbapenes

Monobaktama

Macrolids

Tetracyclines

Fluoroquinolones

Aminoglycosides

Glycopeptides.

Lincoosamida

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6. Group of Monobakatam

Mechanism of action.Azitreons have a bactericidal effect, which is associated with a violation of the formation of the cell wall of bacteria.

Spectrum of activity. The originality of the antimicrobial spectrum of the aztreonam is due to the fact that it is resistant to many V-lactamases produced by aerobic gram-negative flora, and at the same time destroyed in lactamases of staphylococcus, bacteroids and BRS.

Indications.Aztreonam is a reserve preparation for the treatment of infections of various location caused by aerobic gram-negative bacteria:

Contraindications.Allergic reactions to aztreona in history.

7. A group of tetracycline

Mechanism of action. Tetracyclines have a bacteriostatic effect, which is associated with a disruption of protein synthesis in a microbial cell.

Spectrum of activity. Tetracyclines are considered an AMP with a wide range of antimicrobial activity, however, in the process of their many years of use, many bacteria have acquired resistance to them.

Indications:

Contraindications:

Similar documents

What is antibiotic

Classification of antibiotics by the mechanism of action

Bactericidal

Bacteriostatic

Classification of antibiotics for chemical composition

Penicillins

Cephalosporins

Macrolids

Tetracyclines

Aminoglycosides

How to act antibiotics

Groups of antibiotics

Methods of use of antibiotics

Sensitivity to antibiotics

Antibiotics are always effective

Antibiotics and alcohol

Antibiotics during pregnancy

What antibiotics can be prescribed pregnant?

Which of the drugs can not be prescribed during pregnancy

The effects of taking antibiotics

Allergic reactions

Toxic reactions

Impact on the gastrointestinal tract

Other side effects

Is it possible to use antibiotics with preventive purpose

Antibiotics for children