Macrolids contain a macrocyclic lactone ring in its structure, produced with radiant mushrooms. These include erythromycin. The spectrum of its antimicrobial action: the spectrum of benzylpenicillin, including staphylococci producing penicillinase, as well as the pathogens of a rapid typhoid, returning typhoid, cattlefloral pneumonia, causative agents of brucellosis, chlamydia: the pathogens of ornithosis, trachomas, inguinal lymphogranulum, etc.
The mechanism of action of erythromycin: Due to the glocade of peptidranslochase, protein synthesis disrupts.
Type of action: bacteriostatic
Pharmacokinetics. When taken inside is absorbed, it is not completely and partially inactivated, so it must be administered in capsules or in the tablets covered with a shell. Well penetrates the fabric, including through the placenta, bad - through the BC. It is highlighted mainly with bile, in a small amount with urine, it is allocated with milk, but such milk can be fed, because In children until the year he is not absorbed.
The disadvantages of erythromycin are the fact that drug stability is rapidly developing rapidly and it is less active, therefore refers to the antibiotics of the reserve.
Indications for use: Erythromycin is used for diseases caused by sensitive microorganisms to it, but lost sensitivity to penicillins and other antibiotics or in the intolerance of penicillins. Erythromycin is introduced inside 0.25, in more severe cases of 0.5-6 times a day, it is local in ointment. For in / in administration, erythromycin phosphate is used. This group includes oleandomycin phosphate, which is even less active, therefore it is rarely applied.
In recent years, new macrolides have been introduced into practical medicine: spiramycin, Roxitromycin, Clarithromycin and etc.
Azithromycin - antibiotic from the group of macrolides allocated to a new subgroup of azalides, because He has a somewhat different structure. All new macrolides and azalids of a wider spectrum of antimicrobial action are more active, it is better absorbed from the gastrointestinal tract, except forzitromycin, are slower slower (they are injected 2-3 times, and azithromycin 1 time per day) is better tolerated.
Roxitromycin is introduced inside 0.15 g 2 times a day.
Side effects: Can cause allergic reactions, superinfection, dyspeptic phenomena, some of them cause damage to the liver, etc. Side effects. They are not prescribed to nursing women, except erythromycin and azithromycin. In general, these are low-toxic antibiotics.
Tetracyclines - produced with radiant mushrooms. The basis of their structure is four hexted cycles, the system under the general name "Tetracycline"
Antimicrobial spectrum: Benzylpenicillin spectrum, including staphylococci producing penicillinase, rapid typhoid pathogens, return title, Qatarral pneumonia (freedland stick), plague, tularemia, brucellosis, intestinal wand, chiegella, cholera vibrion, dysenteric amoeba, influenza wand, coat and soft Shankra , trachomas, ornithosis, inguinal lymphogranulomytosis, etc. Do not act on a cinema stick, protea, salmonella, tuberculosis wand, viruses and mushrooms. On the gram-positive microflora, they act less actively than penicillins.
Mechanism of action:Tetracyclines violate the synthesis of protein ribosomes of bacteria, together with the tetracyclines form chelate compounds with magnesium and calcium, inhibiting enzymes.
Type of action: Bacteriostatic.
Pharmacokinetics: They are well absorbed from the gastrointestinal tract, bind from 20 to 80% with plasma proteins, penetrate the tissue well, through the placenta, poorly through the Gab. Stand out with urine, brya, feces and milk, such milk can not feed!
Preparations: Depending on the addition of various radicals to the four-cyclic structure, natural: tetracycline, tetracycline hydrochloride, oxytetracycline dihydrate, oxytetracycline hydrochloride; semi-synthetic: metacycline hydrochloride (rondomycin), doxycycline hydrochloride (vibramicin).
All tetracycles are produced cross-stability, therefore semi-synthetic tetracycles are not a reserve of natural tetracyclines, but they are longer. In activity, all tetracyclines are similar.
Indications for use: Tetracyclines are used for diseases caused by an unknown microflora; In case of diseases caused by microorganisms, resistant to penicillins, etc. Antibiotics or in sensitizing the patient to these antibiotics: for the treatment of syphilis, gonorrhea, bacillire and amoebic dysentery, cholera, etc. (See antimicrobial spectrum).
Ways of administration: The main route of administration is inside, some, well-soluble chloride hydrogen salts - in / m and in / in, in the cavity, are widely used in ointments. Doxycycline hydrochloride inside and in / in 0.2 g (0.1 g 2 times or 0.2 1 time) on the first day, in the following days 0.1 1 time; With severe diseases in the first and subsequent days of 0.2 g / in drip, prescribed with severe purulent necrotic processes, as well as with difficulty administration of the drug inside.
Side effects:
Tetracyclines, forming complexes with calcium, are postponed in the bones, teeth and their meetings, breaking the synthesis of protein, which leads to a violation of their development, detention to the appearance of teeth up to two years, they are irregular shape, yellow. If the pregnant and child under 6 months have taken tetracycline, then dairy teeth are affected, and if after 6 months and up to 5 years, then the development of permanent teeth is disturbed. Therefore, pregnant women and children up to 8 years old tetracyclines are contraindicated. They have teratogenic action. Candidiasis can be caused, so they are used with antifungal antibiotics, superinfection with a blue rod, staphylococcal and protematics. Hypovitaminosis, therefore, applied with vitamins of Group V. due to the anti-analyzic effect of tetracycline in children can cause hypotrophy. Can increase intracranial pressure in children. Increase skin sensitivity to ultraviolet rays (photosensitization), in connection with which dermatitis arise. Cumulating in the mucous membrane of the gastrointestinal tract, breaking food suction. Possess hepatotoxicity. The mucous membranes irritate and cause pharyngitis, gastritis, esophagitis, ulcerative lesion of the gastrointestinal tract, so they are applied after meals; At the I / M Introduction - Infiltrates, with / in - Flebites. Cause allergic reactions and others. Side effects.
Combined drugs: eribisculin - combination of oxytetracycline of dihydrate and erythromycin, yATETRIN and loved ones tetraolean - Combination of tetracycline and phosphate oleandomycin.
Tetracyclines due to a decrease in the sensitivity of microorganisms and pronounced side effects at present began to be applied less frequently.
Pharmacology of Levomycetin Group
Levomycetin is synthesized with radiant mushrooms and is obtained by a synthetic path (chloramphenicol).
the same as tetracycline, but in contrast to them it does not act on the simplest, cholera vibrion, anaeroba, but is highly active in relation to Salmonel. Also, as well as tetracycles do not act on a protein, a cinema wand, tuberculous wand, true viruses, mushrooms.
Mechanism of action. Levomycetin inhibits peptidyltransferase and disrupts protein synthesis.
Type of action bacteriostatic.
Pharmacokinetics:it is well absorbed from the gastrointestinal tract, much of it is associated with the albumin plasma, penetrates well in the tissue, including through the placenta, well - through the BC, unlike most antibiotics. Turns mainly in the liver and is excreted mainly kidneys in the form of conjugates and 10% unchanged, partly with bile and feces, as well as with mother's milk and it is impossible to feed such milk.
Preparations.Levomycetin, Levomycetin Stearat (Unlike Levomycetin is not bitter and less active), Levomycetin Succinate soluble for parenteral administration (p / k, in / m, in / c), for local use of Levomikol ointment, syntomicin liniment, etc.
Indications for use.If earlier, Levomycetin was widely used, now due to high toxicity, primarily due to the oppression of blood formation, it is used as a reserve antibiotic with the ineffectiveness of other antibiotics. It is mainly used at salmonellosis (abdominal typhoid, food toxicoinfection) and rickettsiosis (raw tit). Sometimes it is used in meningitis caused by a stick of influenza and hemophilic stick, brain abscess, because It penetrates well through the BC and other diseases. Levomycetin is widely used to prevent and treat infectious and inflammatory diseases of the eyes and purulent wounds.
Side effects.
Levomycetin depresses the blood formation, accompanied by agranulocytosis, reticulocyteopenia, in severe cases there is an aplastic anemia with a fatal outcome. The cause of severe bleeding disorders are sensitization or idiosyncrasy. The oppression of blood formation depends on the dose of levelscetin, therefore it cannot be applied for a long time. Levomycetin is prescribed under blood pattern control. In newborns and in children up to one year due to the insufficiency of liver enzymes and slow removal of Levomycetin through the kidneys, intoxication is developing, accompanied by acute vascular weakness (gray collapse). It causes irritation of the mucous membranes of the gastrointestinal tract (nausea, diarrhea, pharyngitis, anorectal syndrome: irritation around the anus). Dysbacteriosis (candidiasis, infection with a blue rod, protemat, staphylococcal); Hypovitaminosis of the group V. Gipotrophy in children in connection with the violation of the seizure of iron and a decrease in iron-containing enzymes that stimulate protein synthesis. Neurotoxic, may cause psychomotor disorders. Causes allergic reactions; adversely affects myocardium.
Due to the high toxicity of Levomycetin, it is impossible to be prescribed uncontrollable and in easy cases, especially children.
Pharmacology aminoglycoside
They are called, because in their molecule contains an amino-mahor, connected by a glycoside association with an agalicon fragment. Are products of vital activity of various mushrooms, and are also created by a semi-synthetic path.
Antimicrobial spectrumwide. These antibiotics are effective in relation to many aerobic gram-negative and a number of gram-positive microorganisms. The most actively affect the gram-negative microflora and differ in each other by the spectrum of antimicrobial action. Thus, in the spectrum of streptomycin, kanamycin and a derivative of amikacin, there is a tuberculous stick, monomocrine - some simplest (degenerates of toxoplasmosis, amoebic dysentery, skin leishmaniosis, etc.), gentamicin, tobramycin, cozyomycin and amikacin - protein and a cinema wand. Effective with respect to microbes not sensitive to penicillins, tetracycline, leftomycetin, etc. Antibiotics. Aminoglycosides do not act on the anaerobes, mushrooms, spirochetes, rickettsia, true viruses.
Resistance to them develops slowly, but the crossover, except for amikacin, which is resistant to the action of enzymes inactivating aminoglycosides.
Mechanism of action.The synthesis of protein is disturbed, as well as there is reason to believe that they violate the synthesis of the cytoplasmic membrane (see Mashkovsky 2000)
Type of actionbactericidal.
Pharmacokinetics. They are not absorbed from the gastrointestinal tract, that is, poorly absorbed, so when taking inside, they have a local action, with parenteral administration (the main way to / m, but widely entered into / c) they penetrate well in the tissue, including through the placenta, worse In the pulmonary tissue, therefore, with the diseases of the lungs, along with injections, they are injected and intrachechically. Does not penetrate the BC. Displays with different speeds mainly through the kidneys unchanged, creating a valid concentration here, when administered inside - with a fellow. Milk stand out, it is possible to feed, because Not absorbed from the gastrointestinal tract.
Classification.Depending on the spectrum of antimicrobial action and activity, they are divided into three generations. By the first generation includes streptomycin sulfate, monomitial sulfate, kanamycin sulfate and monosulfate. To the second - gentamicin sulfate. By the third generation - Tobramycin sulfate, sizomycin sulfate, amikacin sulfate, neutylmicin. By the fourth generation - izepamycin (Markova). The second and third-generation preparations act on a blue chopstick and protea. According to activity, they are located as follows: amikacin, sizomycin, gentamicin, kanamycin, monomitial.
Indications for use. Appointed inside of all aminoglycosides, only monosulfate monosulfate monosulfate canamycinoma in infections of the gastrointestinal tract: bacillomic dysentery, dysentero carrier, salmonellosis, etc., as well as for the bowel reservation when preparing for the operation on the tract. The resorbative effect of aminoglycosides due to their high toxicity is used mainly as reserve antibiotics with severe infections caused by a gram-negative microflora, including a blue row and proteate; mixed microflora, which lost sensitivity to less toxic antibiotics; Sometimes used in the fight against polyesistant staphylococcis, as well as in diseases caused by an unknown microflora (pneumonia, bronchitis, abscess of lungs, pleurisites, peritonites, wound infection, urinary tract infections, etc.).
Dose and Rhythm Introductiongentamicin sulfate. It is introduced in / m and in / in (drip), depending on the severity of the disease, a single dose for adults and children over 14 years old 0.4-1 mg / kg 2-3 times a day. The highest daily dose is 5 mg / kg (calculate).
Side effects: First, the dyotoxic, striking the auditory and vestibular branch of 8 pairs of cranopy brain nerves, because They accumulate in the lycvore and the structures of the inner ear, causing degenerative changes in them, as a result of which the irreversible deafness may be. In early age children, deafness, therefore, in large doses and do not use them for a long time (no more than 5-7-10 days), if reused, then after 2-3-4 weeks). Aminoglycosides are not prescribed in the second half of pregnancy, because A child can be born deaf-and-and-day, carefully newborn and young children.
According to the isotoxicity, drugs are located (descending) monomicine, so kanamycin, amikacin, gentamicin, tobramycin are not administered to children to one year.
Secondly, they have nephrotoxicity, accumulating in the kidneys, they violate their function, this effect is irreversible, after their cancellation, the kidney function is restored after 1-2 months, but if there was a kidney pathology, then the function violations can be aggravated and preserved. For nephrotoxicity, drugs are located descending: gentamicin, amikacin, kanamycin, tobramycin, streptomycin.
Thirdly, they inhibit neuromuscular conductivity, because Reduce the release of calcium and acetylcholine from the endings of the cholinergic nerves and reduce the sensitivity to the acetylcholine of n-cholinoreceptors of skeletal muscles. Due to the weakness of the respiratory muscles, there may be a weakening of breathing or its stop in weakened children of the first months of life, so when these antibiotics can not be left without supervision. To eliminate the neuromuscular block, it is necessary to introduce in / in prozero and gluconate or calcium chloride with the preliminary administration of sulfate atropine. They are cumulated in the gastrointestinal mucous membrane, the angry of its transport mechanisms and disturb the suction from the intestine of food and some medicines (digoxin, etc.). Allergic reactions, dysbacteriosis (candidiasis), hypovitaminosis of the group B, etc. Side effects. Consequently, aminoglycosides are very toxic antibiotics and are used mainly in the fight against severe diseases caused by a poly-resistant gram-negative microflora.
Polymixin Pharmacology.
They are produced BacillusPolimixa.
Antimicrobial spectrum.In the spectrum, gram-negative microorganisms: causative agents of Qatarral pneumonia, plague, tularemia, brucellosis, intestinal sticks, Schigella, Salmonellosis, a stick of influenza, causative agents of a cough, soft Shankra, a blue chopstick, etc.
Mechanism of action. Disrupts the permeability of the cytoplasmic membrane, contributing to the elimination of many components of the cytoplasm into the environment.
Type of actionbactericidal.
Pharmacokinetics. Poor absorbed from the gastrointestinal tract, creating a valid concentration here. When I / in and in / m, the injection paths penetrates well in the tissue, poorly through the BBB, metabolized in the liver, stand out with urine in a relatively high concentration and partially with bile.
Preparations.Polymixin M Sulfat is very toxic, therefore it is prescribed only inside with intestinal infections caused by sensitive microorganisms to it, as well as for the intestinal retention before the operations on the gastrointestinal tract. They are used locally in ointment for the treatment of purulent processes mainly caused by gram-negative microorganisms, and which is very valuable with a cinema wand. The resorbative effect of this drug is not used. The dose and the rhythm of administration inwards 500,000 cells 4-6 times a day.
Polymixin in sulfate is less toxic, therefore introduced in / m and in / in (drip), only in hospital in severe diseases caused by gram-negative microflora, which has lost sensitivity to less toxic antibiotics, including a sysegnaya stick (sepsis, meningitis, pneumonia, infection, infection Urinary tract, infected burns, etc.) under the control of urine analysis.
Polymixinas stability develops slowly.
Side effects. When orally and local use of these antibiotics, side effects are usually not noted. In parenteral administration, the polymixin in sulfate can have an nephro- and neurotoxic effect, in rare cases - cause the blockade of neuromuscular conductivity, at the Introduction Introduction - infiltrates, when in / in - phlebitis. Polymixin B causes allergic reactions. Polymixins cause dyspeptic phenomena, sometimes superinfection. Pregnant Polymixin in sulfate apply only on life indications.
Preventive use of antibiotics.To this end, they are used to prevent diseases when contacting people with patients with plates, rickettsiosis, tuberculosis, scarletina, venance: syphilif, etc.; for the prevention of rheumatism attacks (Bicyllins); with streptococcal lesions of nasopharynses, apparent cavities, which reduces the frequency of acute glomerulonephritis; In obstetrics, with premature existence of waters and other states, threatening mothers and the fetus, they are prescribed by a gildrency and newborn; with a decrease in the body's resistance to infection (hormone therapy, radiation therapy, malignant neoplasms, etc.); elderly persons with a decrease in reactivity, it is especially important to quickly appoint in the threat of infection; In the oppression of blood formation: agranulocytosis, reticulose; in diagnostic and therapeutic endoscopy of urinary tract; with open bone fractures; extensive burns; when transplanting organs and tissues; with operations on knowingly infected areas (dentistry, lororgans, light, gastrointestinal tract); With operations on the heart, vessels, the brain (prescribed before the operation, during and after surgery 3-4 days), etc.
Principles of chemotherapy (the most common rules). The use of antibacterial chemotherapeutic agents has its own characteristics.
1. It is necessary to determine whether chemotherapy is shown, for this you should put a clinical diagnosis. For example, Cort, bronchopneumonia. The cause of measles is a virus, which does not act chemotherapeutic agents, and therefore it does not make sense. At bronchopneumonia, it is necessary to carry out chemotherapy.
2. Selection of the drug. To do this, it is necessary: \u200b\u200ba) highlight the pathogen and determine its sensitivity to the tool that will be used for this; b) determine whether there are no contraindications to this tool. Apply a means to which a microorganism that caused the disease is sensitive, and the patient has no contraindications to it. With an unknown pathorator, it is advisable to use a means with a wide spectrum of antimicrobial action or a combination of two to three drugs, the total spectrum of which includes probable pathogens.
3. Communication Chemotherapeutic agents are a concentration tools, it is necessary to create and maintain the current concentration of the drug in the lesion focus. For this it is necessary: \u200b\u200ba) when choosing a drug to take into account its pharmacokinetics and choose the path of administration, which can provide the necessary concentration in the lesion. For example, in diseases, the gastrointestinal tract is injected inside the drug is not suction. In the diseases of the urinary tract, the drug is used that is allocated unchanged with urine and with the corresponding route of administration can create a necessary concentration in them; b) To create and maintain the acting concentration, the drug is prescribed in the appropriate dose (sometimes starting with a shock dose that exceeds the subsequent) and the corresponding administration rhythm, that is, the concentration must be strictly constant.
4. It should be combined to combine chemotherapeutic agents, simultaneously assign 2-3 drugs with a different mechanism of action in order to strengthen their effect and slow down the accurate microorganisms to chemotherapeutic agents. It should be borne in mind that with a combination of drugs, not only synergism, but also antagonism of substances in relation to antibacterial activity, as well as the summation of their side effects is possible. It should be noted that synergism is more often manifested if the combined means of the same kind of antimicrobial action and antagonism, if funds with various types of action (in each case, it is necessary to use literature on this issue). It is impossible to combine funds with the same side effects, which is one of the main rules of pharmacology !!!
5. Treatment is necessary as early as possible, because At the beginning of the disease microbial bodies less and they are in a state of energetic growth and reproduction. In this stage, they are most sensitive to chemotherapeutic means. And until more pronounced changes from macroorganism (intoxication, destructive changes) occurred.
6. Very important is the optimal duration of treatment. It is impossible to stop the reception of the chemotherapeutic drug immediately after the disappearance of clinical symptoms of the disease (temperature, etc.), because There may be a relapse of the disease.
7. The prevention of dysbacteriosis preparations are prescribed together with means of destructive on white candid and other microorganisms that can cause superinfection.
8. The field with chemotherapeutic means is used by the drugs of pathogenetic effects (anti-inflammatory drugs), stimulating the body's resistance to infection immunomodulators: Timaline; Vitamin preparations carry out disinfecting therapy. Assign full nutrition.
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, Josamicin, 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.
The conditions of action of antibiotics 1) The system is biologically important for the life of bacteria should react to the effect of low concentrations of the drug through a specific point of the application (the presence of the "target") 2) an antibiotic must have the ability to penetrate the bacterial cell and affect the application point; 3) The antibiotic should not be inactivated earlier than entering the interaction with the biologically active system of bacteria. T D.
The principles of rational assignment of antibiotics (4-5) General principles 6. M Aximal doses to complete overcoming of the disease; Preferred method of administration of preparations parenteral. The local and inhalation use of antibacterial drugs should be reduced to a minimum. 7. Periodic replacement of drugs recently created or rarely appointed (reserve).
The principles of rational assignment of antibiotics (5-5) General principles 8. Conduct the cyclic substitution program of the antibacterial drug. 9. Combined use of drugs to which stability is developing. 10. One antibacterial drug should not be replaced on another, to which there is cross-stability.
Semisynthetic: 1. Izoksazolilpenitsilliny (penitsillinazosta- stably, anti-staphylococcal): oxacillin 2. aminopenicillin: ampicillin, amoxicillin 3. Karboksipenitsilliny (pseudomonas): carbenicillin, ticarcillin 4. Ureidopenitsilliny: azlocillin, piperacillin 5. Ingibitorozaschischennye penicillins: amoxicillin / clavulanate, ampicillin / sulbactam GR "+" gr "-"
The mechanism of action -lockamines The target of the action is the penicillin-binding proteins of bacteria that perform the role of enzymes at the final stage of the synthesis of peptideoglycan - a biopolymer, which is the main component of the cell wall of bacteria. Blocking the synthesis of peptidoglycan leads to the death of the bacterium. The effect of bactericidal. Peptideoglycan and penicillin-binding proteins are absent in mammals \u003d\u003e Specific toxicity against macroorganism for -lactam is not characteristic. Specific toxicity against macroorganism for -lactam is not characteristic. "\u003e 
To overcome the acquired stability of microorganisms that produce special enzymes ---lactamases (destructive-shall), irreversible inhibitors are developed - clavulanic acid (clavulanate), sulbactams, pelvis. They are used when creating combined (inhibitor-crumbling) penicillins.
Drug interactions (1-2) of penicillins can not be mixed in one syringe or in one infusion system with aminoglycosides due to their physico-chemical incompatibility. With a combination of ampicillin with allopurinol, the risk of "ampicillin" rashes increases. The use of high doses of benzylpenicillin potassium salts in combination with potassium-saving diuretics, potassium drugs or ACE inhibitors predetermines the increased risk of hypercalemia.
Medicinal interactions (2-2) are required to be taken care of the combination of penicillins active with respect to the sysegnaya stick, with anticoagulants and antiagregants due to the potential risk of increased bleeding. The use of penicillins in combination with sulfanyamides should be avoided, since it is possible to weaken their bactericidal effect.
IV generation of parenteral cefepim, cefpir active for some strains resistant to the III generation of cephalosporins. Higher resistance to -lktamazamas of a wide and extended spectrum of action. Indications - Treatment of severe nosocomial infections caused by poly-resistant flora; infections on the background of neutropenia.
Medicinal interactions in combination with aminoglycosides and / or loop diuretics, especially in patients with impaired kidney function, it is possible to increase the risk of nephrotoxicity. Antacids reduce the absorption of oral cephalosporins in the gastrointestinal tract. There must be intervals of at least 2 hours between the techniques of these drugs. With a combination of cefoperazone with anticoagulants, thrombolytic and antiagregants increase the risk of bleeding, especially gastrointestinal. In the case of alcohol consumption against the background of treatment with cefoperazone, a disulfira-like reaction may develop.
Lactam antibiotics of the carbapenes: imipenem, Meropene Reserve preparations, more resistant to bacterial -lotamas, are more quickly penetrated through the outer membrane of gram-negative bacteria, have a broader spectrum of activity and are used in severe infections of various localization, including nosocomial (internal hospitality). GR "+" gr "-" Anaeroba
Lactam antibiotics of the monobactam: (monocyclic-lactams) Azitreons The preparation of the reserve, a narrow spectrum of action, should be prescribed in combination with drugs active against gram-positive Cocktles (oxacillin, cephalosporins, linkosamides, vancomycin) and anaerobov (metronidazole) ~ ~ ~ gr "- "Aerobes
The mechanism of action is bactericidal action, violation of the synthesis of protein ribosomes. The degree of antibacterial activity of aminoglycosides depends on their concentration. When combined with penicillins or cephalosporins, synergism is observed against gram-negative and gram-positive aerobic microorganisms.
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.
Drug interactions can not be mixed in one syringe or one infusion system with -laction antibiotics or heparin due to physicochemical incompatibility. Strengthening toxic effects while prescribing two aminoglycosides or combined with other nephrome and outlook drugs: polymixine B, amphotericin B, etcrinic acid, furosemide, vancomycin. Strengthening neuromuscular blockade with simultaneous use of funds for inhalation anesthesia, opioid analgesics, magnesium sulfate and transfusion of large amounts of blood with citrate preservatives. Indomethacin, PhenylButazone and other NSAIDs, disturbing renal blood flow, slow down the removal rate of aminoglycosides.
Amino cyclitol group (structurally similar to aminoglycosides) Natural: spectinomycin mechanism of action bacteriostatic action, suppression of protein synthesis ribosomes of bacterial cells. A narrow spectrum of antimicrobial activity - gonococci, including strains resistant to penicillin
Hinolon / fluoroquinolone group I am generation (oafelled quinolones): 3 acids - nodidix, oxolin and pipemeid (pephemidium) narrow spectrum, drugs of 2nd row with infections of MVP and intestines II generation (fluoroquinolones): SUPLOXCIN, NORFLOXACIN, OFFLOXACIN, PERFLOXACIN, CIPROFLOSCINSACIN . GR "-" gr "+"
Medicinal interactions (1-4) with simultaneous use with antacids and other drugs containing magnesium ions, zinc, iron, bismuth can decrease, the bioavailability of quinolones may be reduced due to the formation of non-supersonic chelate complexes. May slow down the elimination of methylksantines and increase the risk of their toxic effects. With the concomitant use of NSAIDs, nitroimidazole derivatives and methylksantins increases the risk of neurotoxic effects.
Drug interactions (2-4) quinolone show antagonism with nitrofuran derivatives, so combinations of these drugs should be avoided. Hinolona I generation, Ciprofloxacin and Norfloxacin may violate the metabolism of indirect anticoagulants in the liver, which leads to an increase in prothrombin time and risk of bleeding. With simultaneously use, the dose correction of the anticoagulant may be needed.
Medicinal interactions (3-4) increase the cardiotoxicity of drugs lengthening the Qt interval on the electrocardiogram, since the risk of developing heart arrhythmia is increasing. With simultaneous appointment with glucocorticoids, the risk of tendons breaks, especially in the elderly.
Medicinal interactions (4-4) When appointing ciprofloxacin, norfloxacin and peffloxacin, together with preparations that are leaning urine (carbonithihrose inhibitors, citrates, sodium bicarbonate), the risk of crystalluria and nephrotoxic effects increases. With simultaneous use with azlocyllin and cimetidine, due to the decrease in the channel secretion, the elimination of fluoroquinolones slows down and their concentrations in the blood increase.
Group of Macrolides 14-membered: natural - erythromycin semi-synthetic - Clarithromycin, Roxitromycin 15-membered (azalida): semi-synthetic - azithromycin 16-membered: natural - spiramsycin, Josamamicin, Midcamicine semi-synthetic - Midcamicine Acetate GR "+"
The mechanism of action of the macrolide temporarily stop the reproduction of gram-positive cookers. The effect is due to a violation of the synthesis of protein by the microbial cell ribosomes. As a rule, macrolides have a bacteriostatic effect, but in high concentrations, bactericidial on beta hemolytic streptococcus groups A, pneumococcus, causative agents and diphtheria are capable of acting. Have moderate immunomodulatory and anti-inflammatory activity. Unebeat cytochrome R-450 in the liver.
Drug interactions (1-2) of macrolides inhibit metabolism and increase the blood concentration of indirect anticoagulants, theophylline, carbamazepine, valproic acid, dyspeyramide, disputes, cyclosporin. It is dangerous to combine macrolides with terpheneenadine, asthemisol and cisapride due to the danger of the development of severe heart rate disorders due to the elongation of the Qt interval. Macrolids increase the bioavailability of digoxin when taking inside due to the weakening of its inactivation of intestinal microflora.
Medicinal interactions (2-2) antacids reduce the absorption of macrolides, especially azithromycin, in the gastrointestinal tract. Rifampicin enhances the metabolism of macrolides in the liver and reduces their concentration in the blood. Macrolids should not be combined with linkosamides due to the similar mechanism of action and possible competition. Erythromycin, especially when in / in administration, is able to strengthen the absorption of alcohol into the gastrointestinal tract and increase its concentration in the blood.
Natural tetracycline groups: Tetracycline semi-synthetic: doxycycline retain clinical importance in chlamydial infections, rickettsiosis, borreliosis and some particularly dangerous infections, severe acne. The mechanism of action has a bacteriostatic effect, disturbing protein synthesis in a microbial cell. GR "+" gr "-"
Medicinal interactions (1-2) when taking inside, simultaneously with antacids containing calcium, aluminum and magnesium, with sodium hydrocarbonate and cholestyramine, their bioavailability may decrease due to the formation of non-quasive complexes and increase the pH of gastric content. Therefore, intervals of 1-3 hours should be observed between the receptions of the listed drugs and antacids. It is not recommended to combine tetracycles with iron preparations, since it may be disturbed by their mutual absorption.
Drug interactions (2-2) carbamazepine, phenytoin and barbiturates enhance the hepatic metabolism of doxycycline and reduce its blood concentration, which may require the dose correction of this drug or replace it with tetracycline. When combined with tetracycles, it is possible to reduce the reliability of estrogen-containing oral contraceptives. Tetracyclines can enhance the effect of indirect anticoagulants due to inhibiting their metabolism in the liver, which requires careful control of prothrombin time.
Linkosamide Group Natural: Lincomycin Its semi-synthetic analogue: Clindamycin mechanism Action has a bacteriostatic effect, which is due to inhibiting the synthesis of protein ribosomes. In high concentrations, there may be a bactericidal effect. A narrow spectrum of antimicrobial activity - (gram-positive coils (as the second-row preparations) and a non-relative anaerobic flora. GR "+"
Medicinal interactions Antagonism with chloramphenicol and macrolides. With simultaneous use with opioid analgesics, inhalation drugs or muscle relaxants, breathing is possible. Kaolin and attapulgite-containing anti-diagram preparations reduce the absorption of linkosamides in the gastrointestinal tract, therefore the intervals of 3-4 h are required between the receptions of these drugs.
Glycopeptide Group Natural: Vancomycin and Teicoplast The mechanism of action disrupt the synthesis of the cell wall of bacteria. Bactericidal action has, however, with respect to enterococci, some streptococci and coagulategable staphylococci, bacteriostatically act. Preparations of selection with infections caused by MRSA, as well as enterococci, resistant to ampicillin and aminoglycosides gr "+"
Medicinal interactions while simultaneously use with local anesthetics increases the risk of developing hyperemia and other symptoms of histamine reaction. Aminoglycosides, amphotericin B, Polymixin B, Cyclosporin, loop diuretics increase the risk of neurotoxic effects of glycopeptides. Aminoglycosides and stacrifice acid increase the risk of glycopeptide output.
Polymixin Polymixin B Polymixin Polymixin M - the oral action mechanism is a bactericidal effect, which is associated with a violation of the integrity of the cytoplasmic membrane of the microbial cell. A narrow spectrum of activity, high toxicity. Polymixin B is a reserve preparation used in the treatment of a cinema infection, Polymixin M - GTS infection. Gr "-"
Natural RFAMICIN: RFAMICIN SV, RFAMICIN S semi-synthetic: rifampicin, rifabutin mechanism of action bactericidal effect, specific RNA synthesis inhibitors. Wide spectrum of activity. Rifampicin - PTP (anti-tuberculosis drug) of the first row, rifabutin - PTP of the second row. GR "-" gr "+"
Drug interactions Rifampicin - inductor microsomal enzymes of the cytochrome system P-450; Accelerates the metabolism of many drugs: indirect anticoagulants, oral contraceptives, glucocorticoids, oral antidiabetic agents; Digitoxine, quinidine, cyclosporine, chloramphenicol, doxycycline, ketoconazole, itraconazole, fluconazole. Pyrazinamide reduces the concentration of rifampicin in the blood plasma as a result of the impact on the hepatic or renal clearance of the latter.
Chloramphenicol Natural: Chloramphenicol (Levomycetin) mechanism of action Bacteriostatic action, due to violation of the synthesis of protein ribosomes. In high concentrations, has a bactericidal effect against pneumococcus, meningococcus and h.influenzae. It is used as a preparation II of a series in the treatment of meningitis, ricketersiosis, salmonellosis and anaerobic infections.
Medicinal interactions of the antagonist of macrolides and libosamids. Reduces the effectiveness of iron, folic acid and vitamin preparations at 12 due to the weakening of their stimulating effect on hemopoies. The inhibitor of microsomal liver enzymes, enhances the effects of oral antidiabetic preparations, phenytoin, warfarin. Inductors of liver microsomal enzymes (rifampicin, phenobarbital and phenytoin) reduce chloramphenicol concentration in serum.
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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 Cefalosporins
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 - cefazolin (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 BLRSand 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 neomycin). 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.
Infective 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);
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The antibiotic is the substance "against life" - a drug that is used to treat diseases caused by alive agents, as a rule, by various pathogenic bacteria.
Antibiotics are divided into many species and groups on the most different reasons. The classification of antibiotics allows you to most effectively determine the scope of the use of each type of preparation.
1. Depending on the origin.
- Natural (natural).
- Semi-synthetic - at the initial stage of production, the substance is obtained from natural raw materials, and then continues to artificially synthesize the drug.
- Synthetic.
Strictly speaking, actually antibiotics are only drugs obtained from natural raw materials. All other medicines are called "Antibacterial drugs". In the modern world, the concept of "antibiotic" implies all types of drugs that can fight alive causative agents of the disease.
What do natural antibiotics produce?
- from mold fungi;
- from actinomycetes;
- from bacteria;
- from plants (phytoncides);
- fish and animal fabrics.
2. Depending on the impact.
- Antibacterial.
- Antitumor.
- Antifungal.
3. According to the spectrum of impact on a number of different microorganisms.
- Antibiotics with a narrow spectrum of action.
These drugs are preferred for treatment, since it acts purposefully on a certain type (or group) of microorganisms and do not suppress the patient's healthy microflora. - Antibiotics with a wide range of impact.
4. By the nature of the influence on the bacterium cell.
- Bactericidal preparations - destroy the causative agents of the disease.
- Bacteriostatics - suspend the growth and reproduction of cells. Subsequently, the body's immune system must independently cope with the remaining bacteria.
5. By chemical structure.
For those who study antibiotics, the classification by the chemical structure is determined, since the structure of the drug determines its role in the treatment of various diseases.
1. Beta lactam drugs
1. Penicillin is a substance produced by the colonies of mold mushrooms of Penicillinum. Natural and artificial derivatives of penicillin have a bactericidal effect. The substance destroys the walls of the cells of bacteria, which leads to their death.
The pathogenic bacteria adapt to medicines and become resistant to them. The new generation of penicillins is supplemented with a tazobactam, sulbactam and clavulanic acid that protect the drug from destruction inside the cells of bacteria.
Unfortunately, penicillins are often perceived by the body as an allergen.
Penicillin antibiotics groups:
- Penicillins of natural origin are not protected from penicillos - enzymes that produce modified bacteria and which destroy the antibiotic.
- Semi-synthetic - resistant to the effects of a bacterial enzyme:
Biosynthetic penicillin G - benzylpenicillin;
aminopenicillin (amoxicillin, ampicillin, bakampitelin);
Semi-synthetic penicillin (preparations of meticillin, oxacillin, chloxacillin, dcloxacillin, flukoxacillin).
2. Cephalosporin.
It is used in the treatment of diseases caused by bacteria, resistant to the impact of penicillins.
Today there are 4 generations of cephalosporins.
- Cefalelexin, Cefadroxyl, Charin.
- CefaMesin, Cefuroxime (Axietyl), Cefasalin, Cefaclor.
- Cefotaxim, Ceftriakson, Cefitisadim, Ceftibutene, Cefoperasazon.
- Cefpir, cefepim.
Cephalosporins also cause organism allergic reactions.
Cephalosporins are used in surgical interventions to prevent complications, in the treatment of ENT diseases, gonorrhea and pyelonephritis.
2. Macrolids
Have a bacteriostatic effect - prevent growth and division of bacteria. Macrolides affect directly on the focus of inflammation.
Among modern antibiotics, macrolides are considered the least toxic and give a minimum of allergic reactions.
Macrolids accumulate in the body and are applied short courses 1-3 days. It is used in the treatment of inflammation of internal LOR-organs, lungs and bronchi, infections of the small pelvis organs.
Erythrocin, Roxitromycin, Clarithormicin, Azithromycin, Azaldides and Ketolides.
3. Tetracycline
A group of drugs of natural and artificial origin. Have a bacteriostatic action.
Tetracyclines are used in the treatment of severe infections: brucellosis, Siberian ulcers, tularemia, respiratory and urinary tract organs. The main disadvantage of the drug - bacteria very quickly adapt to it. Tetracycline is most effective under local use in the form of ointments.
- Natural tetracyclines: Tetracycline, oxytetracycline.
- Sedentate tetracycles: chloretritis, doxycycline, metacycline.
4. Aminoglycosides
Aminoglycosides belong to bactericidal high-tech drugs active with respect to gram-negative aerobic bacteria.
Aminoglycosides quickly and effectively destroy pathogenic bacteria even with weakened immunite. To start the mechanism for the destruction of bacteria, aerobic conditions are required, that is, antibiotics of this group do not "work" in dead tissues and organs with weak blood circulation (cavity, abscesses).
Aminoglycosides are used in the treatment of the following states: sepsis, peritonitis, furunculosis, endocarditis, pneumonia, bacterial kidney damage, urinary tract infections, inflammation of the inner ear.
Preparations - Aminoglycosides: Streptomicin, Kanamycin, Amikaqin, Gentamicin, Neoamycin.
5. Levomycetin
The drug with a bacteriostatic mechanism of impact on bacterial causative agents of the disease. It is used to treat serious intestinal infections.
An unpleasant side effect of treatment with levomycenetin is the damage to the bone marrow, in which the process of the production of blood cells occurs.
6. Fluoroquinolones
Preparations with a wide range of exposure and powerful bactericidal effect. The mechanism of exposure to the bacterium is to violate the synthesis of DNA, which leads to their death.
Fluoroquinolones are used for local treatment of eyes and ears, due to a strong side effect. Preparations have an impact on joints and bones, contraindicated in the treatment of children and pregnant women.
Fluoroquinolone is used in relation to the following pathogens of diseases: Gonokokk, Schigella, Salmonella, Cholera, Mycoplasma, Chlamydia, Sinygnaya Wand, Legionella, Meningokok, tuberculosis mycobacterium.
Preparations: Levofloxacin, hemifloxacin, sparfloxacine, Moxifloxacin.
7. Glycopeptides
Antibiotic mixed type effect on bacteria. In relation to most species, it has a bactericidal effect, and in relation to streptococci, enterococci and staphylococci - bacteriostatic impact.
Glycopeptide preparations: Teicoplast (Targocid), Daptomycin, Vancomycin (Vankacin, Dialatcin).
8. Antiberculse antibiotics
Preparations: fatzide, metaside, caululzide, ethionamide, simpleness, isoniazide.
9. Antibiotics with antifungal effect
Destroy the membrane structure of mushroom cells, causing their death.
10. Anti-collect drugs
Used for the treatment of leprosy: Solusulfon, Diucifon, diaphenylsulfone.
11. Antitumor drugs - anthracycline
Doxorubicin, Rub Doc, Carminomycin, Aklaubitsin.
12. Lincoosamida
According to their healing properties, it is very close to macrolids, although the chemical composition is a completely different group of antibiotics.
Preparation: Decin S.
13. Antibiotics, which are used in medical practice, but do not apply to any of the known classifications..
Phosphomycin, Fusidin, Rifampicin.
Table of drugs - antibiotics
The classification of antibiotics by groups, the table distributes some types of antibacterial drugs depending on the chemical structure.
| Group of drugs | Preparations | Scope of application | Side effects |
| Penicillin | Penicillin. AMINOPENYCILLIN: ampicillin, amoxicillin, beckhampicillin. Semi-synthetic: methecillin, oxacillin, chloxylin, dyloxacillin, fluklooxacillin. |
Antibiotic with a wide range of impact. | Allergic reactions |
| Cephalosporin | 1 generation: Cephalexin, Cefadroxyl, Zepenin. 2: Cefhamesin, Cefuroxime (Axetil), Cephazolin, Cefaclor. 3: Cefotaxim, Ceftriaxon, Cefitisadim, Cefibutene, Cefoperasazon. 4: Cefpir, cefepim. |
Surgical operations (to prevent complications), ENT diseases, gonorrhea, pyelonephritis. | Allergic reactions |
| Macrolids | Erythromycin, roxitromycin, clarithromycin, azithromycin, azalida and ketolides. | ENT organs, lungs, bronchi, infection of small pelvis organs. | The least toxic, do not cause allergic reactions. |
| Tetracycline | Tetracycline, oxytetracycline, Chlortotrin, doxycycline, metacycline. |
Brucellosis, Siberian ulcers, tularevia, respiratory infections and urinary organs. | Causes rapid addiction |
| Aminoglycosides | Streptomycin, Canamycin, amikacin, gentamicin, neomycin. | Treatment of sepsis, peritonitis, furunculez, endocarditis, pneumonia, bacterial kidney damage, urinary tract infections, inflammation of the inner ear. | High toxicity |
| Fluoroquinolones | Levofloxacin, hemifloxacin, sparfloxacin, moxifloxacin. | Salmonella, Gonokokk, Cholera, Chlamydia, Mycoplasma, Sinneva, Meningokokok, Shigella, Legionella, Tuberculous mycobacterium. | Affect the musculoskeletal system: joints and bones. Contraindicated to children and pregnant women. |
| Levomycetin | Levomycetin | Intestinal infections | Bone marrow damage |
The main classification of antibacterial drugs is carried out depending on their chemical structure.
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