Synthetic antimicrobials. Antimicrobial drugs: overview, application and reviews

Sulfonamides

Preparations of this group are prescribed for intolerance to antibiotics or microflora resistance to them. In terms of activity, they are significantly inferior to antibiotics, and in recent years their importance for the clinic has been declining. Sulfonamides are similar in structure to para-aminobenzoic acid. The mechanism of action of drugs is associated with their competitive antagonism with para-aminobenzoic acid, which is used by microorganisms for the synthesis of dihydrofolic acid. Violation of the synthesis of the latter leads to blockade of the formation of purine and pyrnmidine bases and suppression of the reproduction of microorganisms (bacternostagic effect).

Sulfanilamides are active against Gram-positive and Gram-negative cocci, Escherichia coli, Shigella, Vibrio cholerae, Clostrndia, protozoa (malarial Plasmodium and Toxoplasma), Chlamydia; causative agents of anthrax, diphtheria, plague, as well as Klebsiella, active bacteria and some other microorganisms.

Depending on absorption from the gastrointestinal tract and the duration of excretion from the body, the following groups of sulfonamides are distinguished:

A. Sulfonamides with good absorbability:

short-term action (T1 / 2 - 8 hours); norsulfazol, sulfadimezin, urosulfan, etazol, sodium sulfacyl;

medium duration of action (T1 / 2 - 8-20 hours): sulfazine and other drugs (these drugs are not widely used);

long-acting (T1 / 2 - 24-48 hours): sulfapridazn,

sulfadimethoxine (sulfamethoxazole), sulfamonomethoxine and other drugs;

ultra-long action (T1 / 2 - 65 hours); sulfalene.

B. Sulfonamides, poorly absorbed from the gastrointestinal tract and slowly excreted from the body: sulgin, fthalazol, phthalazine, salazopyridazine and other drugs. ^^ ^

The duration of the action of sulfonamides depends on the occurrence of labile bonds with albumin. From the blood, sulfonamides penetrate quite well into various tissues and body fluids. Sulfapyrndazine has the highest penetrating power. Sulfadimetoksin accumulates in significant amounts in bile. All sulfonamides cross the placenta well. Sulfonamides are metabolized (acetylated) in the liver. At the same time, their activity is lost and toxicity increases, in some of them the solubility in a neutral and especially in an acidic environment decreases sharply, which can contribute to their precipitation in the urinary tract (crystalluria). The degree and rate of acetyl-lnrovaniya different sulfonamides are not the same. Those drugs that are acetylated to a small extent are excreted from the body in an active form, and this determines their greater antimicrobial activity in the urinary tract (etazol, urosulfan). Sulfanilamides can be absorbed in the body by the formation of inactive glucuronides. This inactivation pathway is especially characteristic of sulfadimethoxine. Sulfonamide glucuronides are highly soluble in water and do not precipitate in the kidneys. Sulfonamides and their metabolites are excreted by the kidneys.

The sensitivity of microbes to sulfonamides is sharply reduced in those environments where there is a high concentration of para-aminobenzoic acid, for example, in a purulent focus. The activity of long-acting drugs decreases in the presence of folic acid, methionine, purine and pnrimidine bases. The competitive mechanism of action of these drugs requires the creation of a high concentration of sulfonamides in the patient's blood for successful treatment of infections. To do this, you should prescribe the first loading dose, 2-3 times higher than the average therapeutic dose, and at certain intervals (depending on the half-life of the drug) prescribe maintenance doses.

Side effects in the treatment of sulfa drugs are common to the entire group: effects on the blood and central nervous system; dysbacteriosis. Taking drugs can cause methemoglobinemia and hyperbilirubinemia, especially in newborns. Therefore, it is not recommended to prescribe these drugs, especially long-acting ones, to pregnant women shortly before delivery and to newborns.

Biseptol (sulfatene, co-trnmoxazole) - is a combination of sulfanilamide - sulfamethoxazole with the drug trimethoprim. Trimethoprim inhibits the activity of an enzyme important for the synthesis of folvic acids - dagndrofola reductase. This combination drug has a bactericidal effect. In patients, it can cause a violation of hematopoiesis (leukopenia, agranulocytosis),

Salazo compounds of sulfonamides

Salazosulfapirishchi (sulfasalazine) - nitrogen compound of sulfetyryadin (sulfadn-na) with salicylic acid. High activity of this drug against diplococcus, streptococcus, gonococcus "E. coli" is noted. The determining role in the mechanism of action is played by the ability of the drug to accumulate in the connective tissue (including the intestines) and gradually break down into 5-salicylic acid (which is excreted in the faeces) and eulfaliride, which have anti-inflammatory and antibacterial effects in the intestines. The medicine is used for nonspecific ulcerative colitis. Salazopyrndazine and salshodimetoksin have a similar mechanism of action and indications.

4- and 8-hydroxyquinoline derivatives

Prepshch? You this group are halo- and nitro-derivatives of oxnhinolnia. They act mainly on the gram-negative flora, and also have an anti-rotozoic effect (dysentery amoeba, giardia, thrnchomonads, balantidia). According to pharmacokinetic properties, oxyquinol derivatives are divided into two groups; poorly absorbed (enteroseptol, mexaform, mekease "intestopaya) and well absorbed from the gastrointestinal tract (nntroxoln),

Enteroseptol is active against Escherichia coli, putrefactive bacteria, causative agents of amoebic and batsnlpyarnoy dysentery. It is practically not absorbed from the gastrointestinal tract, therefore, its high concentration in the intestinal lumen is created, which is also used in surgical practice. 1st or 3rd day of admission Enteroseptol contains iodine, so symptoms of iodine are possible: runny nose, cough, joint pain, skin rashes, anti-inflammatory drug! with hyperthyroidism, Enteroseptol is included in the combination * of complex prepfaggs; dermozolon, mexaform, meksat

Due to side effects (dyasneptic disorders, neuritis, myelopathy, damage to the optic nerve), oxysynthetic derivatives have become less commonly used.

Nntroxolnn (5-NOC) . a drug that is considered the least toxic compared to other oxnquinolines. It has a wide spectrum of activity against gram-positive (S, aureus, S. pyogenes, Enterococcus, Diplococcus, Corinebaeterium) and gram-negative (P. vulg^is, Salmonella, Shigella, P. aeruginosa) pathogens, as well as fungi (C. albicans). Nntroxoline is well absorbed. The drug penetrates well into the prostate tissue. Almost the entire amount of the drug is excreted unchanged by the kidneys, which, taking into account the spectrum of action (yashroksoln acts on all pathogens of the urogenital tract infection), allows it to be used exclusively as a uroseptic

Quinolones

Quinolones are a large group of a ^ r t h s f o b g ^ p "enarates, united by a single mechanism of action: inhibition of the enzyme of a bacterial cell - DNA gyrase. First Syntchem 3

a drug from the class of quinolones was nalidixic acid (Negram), used since 1962. This drug, due to the peculiarities of pharmacokinetics (excreted by the kidneys in active form) and the spectrum of antimicrobial action, is indicated for the treatment of urinary tract infections and some intestinal infections (bacterial enterocolitis, dysentery)

Antibacterial preparations of the fluoroquinol group

Preparations belonging to this group were obtained by introducing a fluorine atom into the 6th position of the quinolone molecule. Depending on the number of fluorine atoms, monofluorinated (cnprofloxacin, ofloxacin, pefloxacin, norfloxacin), difluorinated (lomefloxacin) and trifluorinated (fleroxacin) compounds are isolated.

The first drugs of the fluoroquinolone group were proposed for clinical practice in 1978-1980. The intensive development of the fluoroquinolone group is due to a wide spectrum of action, high antimicrobial activity, bactericidal action, optimal pharmacokinetic properties, and good tolerance for long-term use.

Fluoroquinolones are drugs with a broad antimicrobial spectrum, covering Gram-negative and Gram-positive aerobic and anaerobic microorganisms.

Fluoroquinolones are highly active against most gram-negative bacteria (Neisseria spp., Haemophiius spp., E. coli, Shigella spp., Salmonella spp.).

Sensitive microorganisms include Klebsiella spp., Proteus spp., Enterobacter spp., Legionella spp., Yersinia spp., Campylobacter spp, Staphylococcus spp. (including strains resistant to ieticillin), some strains of Clostridiuni (C. perfringens). Among Psedomonas strains, including P. aerugmosa, as well as Streptococcus spp. (including S. pneumonias) there are both sensitive and moderately sensitive strains

As a rule, Brocella spp., Corynebacterim spp., Chlamydiaspp, Mycobacterium tuberculosis, anaerobic streptococci are moderately sensitive.

Fungi, viruses, treponemas and most protozoa are resistant to fluoroquinolones.

The activity of fluoroquinolones against gran-positive microbes is less pronounced than against gram-negative ones. Streptococci are less sensitive to fluoroquinolones than staphylococci.

Among the fluoroquinolones, ciprofloxacin exhibits the highest in vitro activity against gram-negative microorganisms, and ciprofloxacin and ofloxacin against gram-positive microorganisms.

The mechanism of action of fluoroquinolones is associated with an effect on DNA gyrase. This enzyme is involved in the processes of replication, genetic recombination and DNA repair. DNA enzyme causes negative superspinning, converting DNA into a covalently closed circular structure, and also leads to reversible binding of DNA coils. Binding of fluoroquinolones to DNA gnrase leads to the death of bacteria.

Pharmacokinetics, Fgorquinolones are rapidly absorbed in the gastrointestinal tract, reaching maximum concentrations in the blood after 1-3 hours. Eating somewhat slows down the absorption of drugs, without affecting the amount of absorption. Fluoroquinolones are characterized by high oral bioavailability, which for most drugs reaches 80–100% (the exception is norfloxacin, whose bioavailability after oral administration is 35–45%). The duration of the circulation of fluoroquinolones in the human body (for most drugs, the T1 / 2 indicator is 5-10 hours) allows you to prescribe them 2 times a day. Fluoroquinolones are bound to a low degree by serum proteins (less than 30% in most cases). The preparations have a large volume of distribution (90 liters or more), which indicates their good penetration into various tissues, where concentrations are created that in many cases are close to short or exceed them. Fluoroquinolones penetrate well into the mucous membranes of the gastrointestinal tract, urogenital and respiratory tract, lungs, kidneys, synovial fluid, where concentrations are more than 150% relative to serum; the rate of penetration of fluoroquinolones into sputum, skin, muscles, uterus, inflammatory fluid and saliva is 50-150%, and into the cerebrospinal fluid, fat and tissues of the eye - less than 50%. The good diffusion of fluoroquinolones in tissues is due to high lipophilicity and low protein binding,

Fluoroquinolones metabolize in the body, while pefloxacin is more susceptible to biotransformation (50 - 85%), to the least - ofloxacin and lomefloxanine (less than 10%); other drugs in terms of the degree of metabolism occupy an intermediate position. The number of metabolites formed ranges from 1 to 6. A number of metabolites (oxo-, demetnl-v formnl-) have some antibacterial activity.

Elimination of fluoroquinolones in the body is carried out by renal and extrarenal (bnotransformation in the liver, excretion with bile, excretion with feces, etc.) pathways. With the excretion of fluoroquinolones (ofloxacyan and lomefloxacin) by the kidneys, concentrations are created in the urine that are sufficient to suppress the microflora sensitive to nm for a long time,

Clinical application. Fluoroquinolones are widely used in patients with urinary tract infections. Efficiency in jejunal and complicated infections is 70-100%, Good results were obtained in patients with bacterial and bacterial chlamydial prostatitis (55-100%),

Fluoroquinolones are effective in sexually transmitted infections, primarily gonorrhea. In acute uncomplicated gonorrhea of ​​various localizations (including the pharynx and rectum), the effectiveness of fluoroquinolones is 97%. 100% even with a single application. A less pronounced effect of fluoroquinolones is observed in urogenital infections caused by chlamydia (elimination of the pathogen is 45-100%) and Mnco-plasmas (33-100%). With syphilis, drepars of this group are not used,

Good results with the use of fluoroquinolones are observed in intestinal infections (salmonellosis, dysentery, various forms of bacterial diarrhea).

In cases of respiratory disease, fluoroquinolones are important in the treatment of lower respiratory tract infections (pneumonia, bronchitis, bronchoconstriction) caused by gram-negative microflora, including P. awuginosa.

The use of fluoroquinolones as first-line drugs for infections of the upper respiratory tract is inappropriate.

Fluoroquinolones are effective drugs for the treatment of severe forms of pyoinflammatory processes in the skin, soft tissues, purulent arthritis, chronic osteomyelitis caused by gram-negative aerobic bacteria (including P, aemgi-poaa) and S. ash-esh.

Given the good penetration of fluoroquinolones into gynecological tissues (uterus, vagina, fallopian tubes, ovaries), they are successfully used in the treatment of acute inflammatory diseases of the pelvic organs,

Fluoroquinolones (parenteral or oral) are effective in septic processes accompanied by bacteremia caused by gram-negative and gram-positive aerobic microorganisms

Fluoroquinolones (ciprofloxac, ofloxacian, nephthocyanin) are successfully used in the treatment of secondary bacterial meningitis.

Adverse reactions. Adverse reactions with the use of fluoroquinolones occur mainly in the gastrointestinal tract (up to 10%) (nausea, vomiting, anorexia, gastric discomfort) and the central nervous system (0.5. b%) (headache, dizziness, upset sleep or mood, agitation, tremor, depression), allergic reactions caused by fluoroquinolone occur in no more than 2% of patients, skin reactions are noted in 2% > in addition, photosensitization is observed ; it is not known whether they affect bone tissue in children. However, these drugs are not recommended for use in children under 12 years of age and pregnant women.

Ciprofloxacin (schrobay, cnfloxinal) is one from the most active and widely used preparations of this group. It penetrates well into various organs and tissues, cells. Hiccups up to 100% into sputum, 90-80% into pleural fluid, up to 200-1000% of the drug into lung tissue. The drug is used for infections of the respiratory tract, urinary tract, osteomyelitis, abdominal infection, skin lesions and appendages

Pefloxacin (peflacin, abakgal) is a fluoroquinolone with high activity against Enterobacteriaceae, gram-negative cocci. Gram-positive staphylococci and streptococci are less sensitive to pefloxacin than gram-negative bacteria. Pefloxacin exhibits high activity against intracellularly located bacteria (Hpamnidae, Legionella, Mncoplasmas). It is well absorbed when taken orally, in high concentrations it is determined in organs and tissues, including bones, it accumulates well in the skin, muscles, fascia, pertoneal fluid, in the abdominal organs, prostate, and penetrates through the BBB.

Pefloxacin is actively metabolized in the liver with the appearance of active compounds: N-demethylpefloxacin (norfloxacin), N-oxidepefloxacin, oxodemetshsheflox-cn and others. The drug is eliminated by the kidneys and partially excreted in the bile.

Ofloxacin (floksnn, tarivid) refers to monofluorinated hennolones. Its antimicrobial activity is close to that of ciprofloxacin, however, there is a higher activity against Staphylococcus aureus. At the same time, ofloxacin has better pharmacological parameters, better bioavailability, a longer half-life and higher concentrations in serum and tissues. It is used mainly for infections of the urogenital region, as well as for respiratory infections, 200-400 mg 2-3 times a day.

Lomefloxadine (Moxaquin) is a difluoroquinolone. It is rapidly and easily absorbed when taken orally. Bioavailability exceeds 98%. Very well accumulates in the tissues of the prostate gland. Apply 1 tablet of 400 mg per day for infections of the respiratory and urinary tract, prevention of urogenital infection in the postoperative period, lesions of the skin and soft tissues, gastrointestinal tract

Nitrofurans

Nntrofurans are active against gram-positive and gram-negative flora: intestinal, dysentery bacillus, paratyphoid, salmonella, vibrio cholerae, giardia, thrnchomonads, staphylococci, large viruses, causative agents of gas gangrene are sensitive to them. Preparations of this group are effective in the resistance of microorganisms to other antimicrobial agents. Nntrofurans have anti-inflammatory activity, rarely cause dnsbacternosis and candida. The drugs have a bactericidal effect by inhibiting the formation of nucleic acids. They are well absorbed from the gastrointestinal tract, quickly penetrate and are evenly distributed in fluids and tissues. Their main transformation in the body is the reduction of the ntro group. Nitrofurans and their metabolites are excreted by the kidneys, partly with bile and into the intestinal lumen

Side effects include dyspepsia and allergic reactions, methemoglobinemia, decreased platelet aggregation and, in connection with this, bleeding, disruption of the ovarian-menstrual cycle, embryotoxicity, impaired renal function, with prolonged use, neuritis, pulmonary interstitial infiltrates may occur. To prevent side effects, it is recommended to drink plenty of fluids, prescribe ai-tngnstamin drugs and vitamins of group B. A large number of side effects limits the use of drugs in this group.

Furazolidone acts on nashngella, salmonella, vibrio cholerae, giardia, trn-chomonas, paratyphoid bacillus, proteus. It is used for gastrointestinal infections. FurazolidoneSy'tchem6

increases sensitivity to alcoholic beverages, that is, it has a teturam-like action. It is prescribed orally after meals, 0.1-0.15 g 4 times a day. It is not recommended to take it for more than 10 days.

Furadonin (nitrofuranton) has an antimicrobial spectrum of action similar to that of furazolndone, but more active against intestinal daddy, staphylococci and proteus. When taken orally, furadonnn is rapidly absorbed from the gastrointestinal tract. 50% of furadonin is excreted in the urine in an unchanged state, and 50% in the form of inactive; metabolites. A high concentration of the drug in the urine lasts up to 12 hours. Furadonnn is eliminated in large quantities in the bile. The drug crosses the placenta. The drug is used for infections of the urinary system.

Furognn (solafur) is the most widely used of the drugs in this group. For oral administration, a single dose is 0.1-0.2 g, it is taken 3 times a day for 7-10 days. Primary use as uroantiephenka Locally used for washings (in surgery) and douching (in obstetric and gynecological practice).

Thiosemicarbazone derivative

Pharyngosept (ambazone) is a bacteriostatic drug, which is 1,4-benzoquino-guayyl-hydrozontosemicarbazone. Active against hemolytic streptococcus, pneumococcus, viridescent streptococcus Indications for the use of the drug are limited to diseases of the nasopharynx; treatment and prevention of cataracts, gingivitis, stomatitis caused by: a pathogen sensitive to this drug, as well as treatment of complications after operations in the nasopharynx. Apply sublinshaglio from 3 to 5 tablets per day 15-30 minutes after eating.

Quinoxaline derivatives

Hnnoxndin is a derivative of quinoxalin, a synthetic antibacterial agent. It is active against Frieddender's bacillus, Pseudomonas aeruginosa, Escherichia and dysentery bacilli, Salmonella, Staphylococcus aureus, Clostridae (especially pathogens of gas gangrene). Quinoxidine is indicated for severe forms of inflammatory processes in the abdominal cavity.

In terms of pharmacodynamics and pharmacokinetics, dioxidine is similar to quinoxin, but lower toxicity and the possibility of intracavitary and intravenous administration of daoxin-diyaa significantly increased the effectiveness of the treatment of sepsis, especially caused by staphylococcus aureus and papillomavirus.

synthetic antibacterial agents

Sulfonamides.

quinolone derivatives.

Nitrofuran derivatives.

Derivatives of 8-hydroxyquinoline.

Quinoxaline derivatives.

Oxazolidinones.

Sulfanilamide preparations

Classification

1. Sulfonamides for resorptive action

Short action:

Sulfanilamide (Streptocid), sulfathiazole (Norsulfazol).

Average duration of action:

Sulfadiazine (Sulfazin), sulfamethoxazole.

Long acting: Sulfadimetoksin, sulfamonometoksin.

Extra long acting: Sulfamethoxypyrazine (Sulfalene).

2. Sulfonamides acting in the intestinal lumen

Phthalylsulfathiazole (Ftalazol), sulfaguanidine (Sulgin).

3. Sulfonamides for topical use

Sulfacetamide (Sulfacyl sodium, Albucid), silver sulfadiazine.

4. Combined preparations of sulfonamides and salicylic acid: Salazosulfapyridine (Sulfasalazine), Salazopyridazine (Salazodine).

5. Combined preparations of sulfonamides with trimethoprim:

Co-trimoxazole (Bactrim, Biseptol).

SA have a wide range of activities:

Bacteria - gram-positive and gram-negative cocci, Escherichia coli, pathogens of dysentery, diphtheria, catarrhal pneumonia, cholera vibrio, clostridia;

Chlamydia;

Actinomycetes;

Protozoa (toxoplasmosis, malaria).

The nature of the action bacteriostatic.

Mechanism of action. They are structural analogues of PABA, competitively prevent its incorporation into dihydrofolic acid, and inhibit dihydropteroate synthetase. As a result, the formation of tetrahydrofolic acid, the synthesis of purines and pyrimidines, nucleic acids decreases, the growth and reproduction of microorganisms are suppressed.

SA of resorptive action. They are well absorbed in the gastrointestinal tract (70-100%), widely distributed in tissues and body fluids, pass through the BBB, placenta, and into breast milk. They are metabolized in the liver to form acetylated derivatives, which crystallize in acidic urine, blocking the renal tubules.

SA acting in the intestinal lumen poorly absorbed from the gastrointestinal tract, used to treat intestinal infections.

SA for topical use used to treat and prevent eye infections.

Combination drugs SA.

one). With trimethoprim - co-trimaxosole. Acts bactericidal.

Mechanism of action: violates the synthesis of dihydrofolic acid; trimethoprim blocks dihydrofolate reductase and disrupts the formation of tetrahydrofolic acid.

Well absorbed from the gastrointestinal tract.

2). With 5-aminosalicylic acid - Salazopyridazine, salazosulfapyridine have antimicrobial, anti-inflammatory and immunosuppressive effects.

Indications for use:

Respiratory and ENT infections

Infections of the biliary tract.

Urinary tract infections.

Chlamydia.

Infections of the gastrointestinal tract.

Eye infections.

Toxoplasmosis and malaria (+ pyrimethamine).

Treatment of a clean wound.

Side effects:

Nephrotoxicity (drink with alkaline drink), allergic reactions, hepatotoxicity (hyperbilirubinemia in young children), CNS (headache, dizziness, depression, hallucinations), dyspepsia, impaired hematopoiesis, methemoglobinemia (in newborns and children of the 1st year of life), malnutrition , thyroid dysfunction, teratogenicity.

Children of the 1st year of life are prescribed extremely rarely.

Synthetic antimicrobials

Sulfanilamide preparations

quinolone derivatives.

Synthetic antibacterial agents of different chemical structure: derivatives of nitrofuran, nitroimidazole and 8-hydroxyquinoline

Sulfanilamide preparations

Sulfonamides were the first broad-spectrum chemotherapeutic drugs that found application in practical medicine.

After the discovery in 1935 of the antimicrobial properties of streptocide, about 6,000 sulfanilamide substances have been synthesized and studied to date. Of these, about 40 compounds are used in medical practice. All of them have a common mechanism of action and differ little from each other in the spectrum of antimicrobial activity. Differences between individual drugs relate to the strength and duration of action.

Sulfanilamide drugs suppress the vital activity of various cocci (streptococcus, pneumococcus, meningococcus, gonococcus), some sticks (dysentery, anthrax, plague), cholera vibrio, trachoma virus. Less sensitive to sulfonamides are staphylococci, Escherichia coli, etc.

Chemically, sulfa drugs are weak acids. Taken orally, they are absorbed mainly in the stomach and ionized in the alkaline environment of the blood and tissues.

The mechanism of the chemotherapeutic action of sulfonamides is that they prevent the absorption by microorganisms of the substance necessary for their vital activity - para-aminobenzoic acid (PABA). With the participation of PABA in the microbial cell, folic acid and methionine are synthesized, which ensure the growth and development of cells (growth factors). Sulfonamides have a structural similarity with PABA and ways to delay the synthesis of growth factors, which leads to disruption of the development of microorganisms (bacteriostatic effect).

There is a competitive antagonism between PABA and a sulfanilamide preparation, and for the manifestation of an antimicrobial effect, it is necessary that the amount of sulfanilamide in the microbial environment significantly exceed the concentration of PABA. If the environment surrounding microorganisms contains a lot of PABA or folic acid (the presence of pus, tissue decay products, novocaine), then the antimicrobial activity of sulfonamides is markedly reduced.

For the successful treatment of infectious diseases, it is necessary to create high concentrations of sulfanilamide preparations in the patient's blood. Therefore, treatment is prescribed from the first increased dose (loading dose), after which the required concentration is maintained by repeated injections of the drug throughout the entire period of treatment. Insufficient concentrations of the drug in the blood can lead to the emergence of resistant strains of microorganisms. It is advisable to combine treatment with sulfanilamide preparations with some antibiotics (penicillin, erythromycin) and other antimicrobial agents.

Side effects of sulfonamides can be manifested by allergic reactions (itching, rash, urticaria) and leukopenia.

When urine is acidic, some sulfonamides precipitate and can cause blockage of the urinary tract. The appointment of plentiful drink (preferably alkaline) reduces or prevents complications from the kidneys.

According to the duration of action, sulfa drugs can be divided into three groups:

1) short-term drugs (streptocid, norsulfazol, sulfacyl, etazol, urosulfan, sulfadimezin; they are prescribed 4-6 times a day);

2) medium duration of action (sulfazine; it is prescribed 2 times a day);

3) long-acting (sulfapyridazine, sulfadimethoxine, etc.; they are prescribed 1 time per day);

4) an ultra-long-acting drug (sulfalene; about 1 week)

Drugs that are well absorbed from the gastrointestinal tract and provide stable blood concentrations (sulfadimezin, norsulfazol, long-acting drugs) are indicated for the treatment of pneumonia, meningitis, gonorrhea, sepsis and other diseases.

Sulfonamides, which are slowly and poorly absorbed and create high concentrations in the intestine (phthalazol, phtazin, sulgin, etc.), are indicated for the treatment of intestinal infections: dysentery, enterocolitis, etc.

Drugs that are rapidly excreted by the kidneys in unchanged form (urosulfan, etazol, sulfacyl, etc.) are prescribed for urological diseases.

The appointment of sulfonamides is contraindicated in severe diseases of the hematopoietic organs, in allergic diseases, hypersensitivity to sulfonamides, during pregnancy (possibly teratogenic effect).

The combination of some sulfonamides with trimethoprim in one dosage form made it possible to create very effective antimicrobial drugs: bactrim (biseptol), sulfatone, lidaprim, etc. Bactrim is available in tablets containing sulfamethoxazole and trimethoprim. Each of them individually has a bacteriostatic effect, and in combination they provide a strong bactericidal activity against gram-positive and gram-negative microbes, including those resistant to sulfanilamide drugs.

Bactrim is most effective for infections of the respiratory system, urinary tract, gastrointestinal tract, septicemia and other infectious diseases.

When using these drugs, side effects are possible: nausea, vomiting, diarrhea, allergic reactions, leukopenia and agranulocytosis. Contraindications: hypersensitivity to sulfonamides, diseases of the hematopoietic system, pregnancy, impaired renal and liver function.

Preparations:

Streptocide (Streptocidum)

Assign inside of 0.5 - 1.0 g 4 - 6 times a day.

Higher doses: single - 2.0 g, daily - ?.0 g.

Release form: powder, tablets of 0.3 and 0.5 g.

Norsulfazol (Norsulfazolum)

Assign inside of 0.5 - 10 g 4 -6 times a day. A solution (5-10%) of norsulfazole-sodium is injected intravenously at the rate of 0.5-1.2 g per infusion.

Higher doses: single - 2.0 g, daily - 7.0 g.

Storage: list B; in a well sealed container.

Sulfadimezin (Sulfadimezinum)

Assign inside 1.0 g 3-4 times a day.

Higher doses: single - 2.0 g, daily 7.0 g.

Storage: list B; in a place protected from light.

Urosulfan (Urosulfanum)

Assign inside of 0.5 - 1.0 g 3 - 5 times a day.

Higher doses: single - 2 g, daily - 7 g.

Storage: list B; in a well sealed container.

Ftalazol (Phthalazolum)

Assign inside of 1 - 2 g 3 - 4 times a day.

Higher doses: single - 2.0 g, daily - 7.0 g.

Release form: powder. Tablets of 0.5 g.

Storage: list B; in a well sealed container.

Sulfacyl - sodium (Sulfacylum - natrium)

Assign inside of 0.5 - 1 g 3 - 5 times a day. In eye practice, it is used in the form of 10-2 - 3% solutions or ointments.

Higher doses: single - 2 g, daily - 7 g.

Release form: powder.

Storage: list B.

Sulfadimethoxin (Sulfadimethoxinum)

Assign inside 1 - 2 g 1 time per day.

Release form: powder and tablets of 0.2 and 0.5 g.

Bactrim (Dfctrim)

Synonym: biseptol.

Release form: tablets.

Recipe Examples

Rp. Tab. Streptocidi 0.5 N 10

D.S. Take 2 tablets 4-6 times daily

Rp.: Sol. Norsulfazoli - sodium 5% - 20 ml

D.S. Administer intravenously 10 days 1-2 times a day

Rp.: Ung. Sulfacyli - sodium 30% - 10.0

D.S. Eye ointment. Lay behind the lower eyelid 2-3 times a day

Rp.: Sol. Sulfacyli - sodium 20% - 5 ml

D.S. Eye drops. Apply 2 drops 3 times a day.

Rep.: Tab. Urosulfani 0.5 N 30

D.S. Take 2 tablets 3 times a day

Quinolone derivatives

Quinolone derivatives include nalidixic acid (nevigramon, blacks). Effective in infections caused by gram-negative microorganisms. It is mainly used for urinary tract infections. It can be used for enterocolitis, cholecystitis and other diseases caused by microorganisms sensitive to the drug. Including resistant to other antibacterial drugs. Assign inside of 0.5 - 1 g 3 - 4 times a day. When using the drug, nausea, vomiting, diarrhea, headaches, allergic reactions are possible. The drug is contraindicated in violation of the function of the liver, kidneys, in the first 3 months. Pregnancy and children under 2 years of age.

Recently, fluoroquinolones, quinolone derivatives containing fluorine atoms in the structure, have attracted much attention. A significant number of such drugs have been synthesized: ciprofloxacin, norfloxacin, pefloxacin, lomefloxacin, ofloxacin. They are highly active broad-spectrum antibacterial agents. They have a bactericidal effect on gram-negative bacteria, including gonococci, E. coli, Shigella, Salmonella, Klebsiella, Enterobacter, Haemophilus influenzae, Pseudomonas aeruginosa, Mycoplasma, Chlamydia. They are less active against Gram-positive bacteria. They interfere with DNA replication and RNA formation. Fluoroquinolones are well absorbed from the gastrointestinal tract. Penetrates most tissues. They are used for infections of the urinary tract, respiratory tract, gastrointestinal tract. Tolerance to fluoroquinolones develops relatively slowly. Side effects include dyspeptic disorders, skin rashes, allergic reactions, headache, insomnia, photosensitivity. Contraindicated in pregnant and lactating women, as well as in patients under the age of 18 years.

One of the important directions in the creation of new fluoroquinolones is to increase the antimicrobial effect on gram-positive bacteria, in particular on pneumococci. These drugs include moxifloxacin, levofloxacin. In addition, these drugs are active against chlamydia, mycoplasmas, ureaplasmas, anaerobes. The drugs are prescribed 1 time per day, they are effective when administered enterally. They are very effective against pathogens of URT infections, they are active even against Mycobacterium tuberculosis.

Ofloxacin (Ofloxacinum)

Assign inside of 0.2 g 2 times a day.

Release form: tablets of 0.2 g.

Storage: list B; in a place protected from light.

Ciprofloxacin (Ciprofloxacin)

Inside and in / in 0.125-0.75 g.

Release form: tablets of 0.25; 0.5 and 0.75g; 0.2% solution for infusions of 50 and 100 ml; 1% solution in 10 ml ampoules (for dilution).

Moxifloxacin (Moxifloxacin)

Inside 0.4 g.

Release form: tablets of 0.4 g

Synthetic antibacterial agents: derivatives of nitrofuran, nitroimidazole and 8-hydroxyquinoline

Nitrofuran derivatives include furatsilin, furazolidone, etc.

Furacilin has an effect on many gram-positive and gram-negative microbes. It is used externally in solutions (0.02%) and ointments (0.2%) for the treatment and prevention of purulent-inflammatory processes: washing wounds, ulcers, burns, in eye practice, etc. Inside is prescribed for the treatment of bacterial dysentery. Furacilin, when applied topically, does not cause tissue irritation and promotes wound healing.

When ingested, nausea, vomiting, dizziness, and allergic reactions are sometimes noted. In case of impaired renal function, furatsilin is not prescribed orally.

Among nitrofuran derivatives, furadonin and furagin are used to treat urinary tract infections. They are prescribed orally, absorbed rather quickly and excreted in a significant amount by the kidneys, creating the necessary concentrations for the manifestation of bacteriostatic and bactericidal action in the urinary tract.

Furazolidone, in comparison with furatsilin, is less toxic and more active against Escherichia coli, the causative agent of bacterial dysentery, typhoid fever, and food poisoning. In addition, furazolidone is active against Giardia and Trichomonas. Furazolin is used orally for the treatment of infections of the gastrointestinal tract, giardiasis cholecystitis and trichomoniasis. Of the side effects, dyspeptic disorders and allergic reactions are sometimes observed.

Nitroimidazole derivatives include metronidazole and tinidazole.

Metronidazole (Trichopolum) - is widely used to treat trichomoniasis, giardiasis, amoebiosis and other diseases caused by protozoa. Recently, metronidazole has been found to be highly effective against Helicobacter pylori in gastric ulcers. Assign inside, parenterally and in the form of suppositories.

Side effects: nausea, vomiting, diarrhea, headache.

Contraindications: pregnancy, lactation, hematopoiesis. Incompatible with the intake of alcoholic beverages.

Tinidazole (Tinidazole). By structure, indications and contraindications, it is close to metronidazole. Both drugs are available in tablets. Storage: list B.

Nitroxoline (5 - NOC) has an antibacterial effect on gram-positive, gram-negative microbes, as well as against some fungi. Unlike other derivatives of 8-hydroxyquinoline, 5-NOC is rapidly absorbed from the gastrointestinal tract and excreted unchanged through the kidneys. Used for urinary tract infections.

Intestopan is used for acute and chronic enterocolitis, amoebic and bacillary dysentery.

Quiniofon (Yatren) is used orally mainly for amoebic dysentery. Sometimes it is prescribed intramuscularly for rheumatism.

Preparations…

Furacilin (Furacilinum)

Applied externally in the form of a 0.02 aqueous solution, 0.066% alcohol solution and 0.2% ointment.

Inside designate 0.1 g 4-5 times a day.

Higher doses inside: single - 0.1 g, daily - 0.5 g.

Release form: powder, tablets of 0.1 g.

Storage: list B; in a place protected from light.

Furazolidone

Applied inside of 0.1 - 0.15 g 3-4 times a day. Solutions of 1:25,000 are applied externally.

Higher doses inside: single - 0.2 g, daily - 0.8 g.

Release form: powder and tablets of 0.05 g.

Storage: list B; in a sheltered place.

Nitroxoline (Nitro, added 02/25/2014

The mechanism of action of sulfonamides; advantages of their application: low toxicity, low prices, bacteriostatic antimicrobial effect. Purpose, side effects and contraindications of nitrofuran derivatives, oxyquinoline and thiosemicarbazone.

presentation, added 11/02/2014

The principles of rational chemotherapy, as well as the main factors influencing the choice of drugs: antibiotics, sulfanilamide and antibacterial agents of various chemical structures, antisyphilitic. biosynthetic penicillins.

presentation, added 10/25/2014

Drugs for the correction of disorders of the reproductive system. Preparations of female and male sex hormones and their synthetic analogues. Classification of drugs of sex hormones. Release form and mechanism of action of hormonal preparations.

presentation, added 03/15/2015

General characteristics of sedative drugs, their classification and mechanism of action. Main indications for use, side effects and contraindications. Derivatives of benzodiazepine, drugs with antineurotic action, a group of combined drugs.

presentation, added 04/28/2012

Classification of sulfa drugs. Reactions due to aromatic amino group. Physical and chemical methods of identification. Nitritometry, neutralization, non-aqueous titration, acidimetry, iodine chlormetry, bromatometry. Purity tests.

term paper, added 07/01/2014

p-Aminophenol, p-Aminobenzoic and p-Aminosalicylic acids, their derivatives. Properties of paracetamol and features of its use. Anestezin and novocaine and the strength of their anesthetic action. The spectrum of antimicrobial activity of sulfanilamide (streptocide).

presentation, added 05/19/2015

The study of drugs under the general name "antibiotics". Antibacterial chemotherapeutic agents. The history of the discovery of antibiotics, their mechanism of action and classification. Features of the use of antibiotics and their side effects.

term paper, added 10/16/2014

Methods of using inhalation drugs for anesthesia. Clinical use of sulfa drugs, neurolepsy and analgesia. The value of inhalation anesthesia in veterinary medicine. Application of methods of anesthesia in surgical practice.

abstract, added 04/10/2014

Rapid development of polymer chemistry in the middle of the 20th century. Requirements for modern surgical suture material. Synthetic polymer bandages. Prosthetic heart valves. Synthetic joints, bones and skin. Synthetic vascular prostheses.

Sulfanilamide medicines

They are derivatives of sulfanilic acid amide. The chemotherapeutic activity of sulfonamides was discovered in the 30s of the twentieth century, when the German researcher Domagk discovered and proposed for medical use prontosil or red streptocide, for which he was awarded the Nobel Prize.

It was soon found that sulfanilic acid amide, which was called white streptocide, has an antimicrobial property in the prontosil molecule. On the basis of its molecule, a large number of derivatives of sulfanilamide drugs have been synthesized.

The mechanism of action of sulfonamides is associated with a specific antagonism with para-aminobenzoic acid (PABA), a factor in the growth and development of microbial cells. PABA is necessary for the synthesis of dihydrofolic acid by microorganisms, which is involved in the further formation of purine and pyrimidine bases, which are necessary for the synthesis of nucleic acids of microorganisms. Due to the similarity of the structure of PABA, sulfanilamide drugs displace it and instead of PABA are captured by the microbial cell, thereby inhibiting the growth and development of microorganisms. (Fig.28). To obtain a therapeutic effect, sulfonamides must be prescribed in doses sufficient to prevent the possibility of the use of PABA by microorganisms in the tissues.

The activity of sulfonamides decreases in purulent contents, blood, where high concentrations of PABA are observed. Their activity also decreases in the presence of substances that decompose with the formation of PABA (novocaine, benzocaine, sulfonylurea derivatives), when co-administered with folic acid and drugs involved in its synthesis.

Sulfonamides have a bacteriostatic effect. The spectrum of action of these compounds is quite wide and includes the following infectious agents: gram-positive and gram-negative bacteria (streptococci, pneumococci, gonococci, meningococci, E. coli, shigella, anthrax, plague, diphtheria, brucellosis, cholera, gas gangrene, tularemia), protozoa ( Plasmodium malaria, toxoplasma), chlamydia, actinomycetes.

Most sulfonamides are well absorbed from the gastrointestinal tract, mainly in the small intestine. The distribution in the body occurs evenly, they are found in the cerebrospinal fluid, penetrate into the joint cavity, and pass through the placenta.

In the body, sulfonamides undergo acetylation, and their chemotherapeutic activity is lost. Acetyl derivatives are less soluble in water and precipitate. The degree of acetylation for different drugs varies greatly. Sulfonamides are excreted from the body mainly by the kidneys.

Sulfanilamide drugs are used to treat infectious diseases of different localization. Means that are well absorbed from the intestines are used to treat pneumonia, meningitis, sepsis, urinary tract infections, tonsillitis, erysipelas, wound infections, etc. They are often used in combination with antibiotics.

Some sulfonamides are poorly absorbed from the intestine, create a high concentration in it and actively suppress the intestinal microflora (phthalazol, sulgin, ftazin).

Sulfanilamide drugs are considered low-toxic compounds, but they can cause the following undesirable side effects: allergic reactions (rash, dermatitis, fever), dyspeptic disorders (nausea, vomiting, loss of appetite), crystalluria (acetylated products can precipitate in the kidneys in the form of crystals and block the urinary tract ), impaired renal function, leukopenia, anemia, neuropsychiatric disorders. To prevent crystalluria, an abundant alkaline drink (up to 3 liters per day) is recommended.

Sulfonamides are contraindicated in case of hypersensitivity to them, impaired renal excretory function, diseases of the blood system, liver damage, pregnancy.

Sulfonamides of resorptive action

These drugs are well absorbed from the gastrointestinal tract, accumulate in all tissues and differ in the duration of the antibacterial effect and the rate of excretion from the body.

Short-acting drugs with a half-life (by 50%) up to 8 hours. To maintain bacteriostatic concentrations, they are prescribed after 4-6 hours.

Sulfadimezin (sulfamethazine) is practically insoluble in water. Relatively low toxicity, but causes crystalluria, a change in the blood picture.

Sulfaethylthiadiazole (etazol) is practically insoluble in water. Less acetylated than other sulfonamides, does not cause crystalluria and has less effect on the blood. Etazol sodium is readily water soluble and can be used parenterally for severe infections.

Sulfacetamide (sulfacyl sodium) is highly soluble in water. It is applied topically in eye practice in the form of drops, ointments for the treatment of conjunctivitis, blepharitis, purulent corneal ulcers, for the treatment of wounds. It is also used parenterally for systemic action in severe infections.

Sulfanilamide (streptocide) for systemic action is used in tablets and powders, while it is rapidly absorbed into the blood. For the treatment of purulent-inflammatory skin diseases, ulcers, wounds, streptocid ointment or streptocide liniment is used topically on the affected skin surface or on napkins for dressings. Included in the combined ointments "Sunoref", "Nitacid", aerosol "Ingalipt".

Long-acting drugs with a half-life of up to 24-48 hours. They are well absorbed from the gastrointestinal tract, but are slowly excreted from the body, they are prescribed 1-2 times a day.

Sulfadimethoxine (madribon), sulfamethoxazole are significantly reabsorbed in the renal tubules, accumulate in large quantities in bile, penetrate into the pleural fluid, but poorly and slowly penetrate the blood-brain barrier.

Sulfapyridazine (sulfamethoxypyridazine) is also reabsorbed in the kidneys. Penetrates into the cerebrospinal, pleural fluid, accumulates in bile. Effective against certain viruses and protozoa (causative agents of malaria, trachoma, leprosy).

Drugs of ultra-long (prolonged) action with a half-life of up to 84 hours.

Sulfamethoxypyridazine (sulfalene) is rapidly absorbed from the gastrointestinal tract, so its high concentrations are created in the intestinal lumen. They are used in the treatment of intestinal infections - bacillary dysentery, colitis, enterocolitis, for the prevention of intestinal infection, in the postoperative period.

Sulfonamides, not absorbed from the gastrointestinal tract

Phthalylsulfathiazole (phthalazol) is a powder that is practically insoluble in water. In the intestine, the sulfanilamide part of the molecule, norsulfazol, is cleaved off. Often, ftalazol is combined with antibiotics and well-absorbed sulfonamides. It has low toxicity and is well tolerated. Assign 4-6 times a day for intestinal infections.

Sulfaguanidine (Sulgin) acts similarly to phthalazole.

Phtazin is a longer-acting drug, it is prescribed 2 times a day for dysentery, salmonellosis and other intestinal infections.

Combination sulfonamide drugs

The most commonly used combination of sulfonamides with trimethoprim. Trimethoprim blocks the conversion of dihydrofolic acid to tetrahydrofolic acid. In such a combination, antimicrobial activity increases and the effect becomes bactericidal. (Fig. 28).

Co-trimaxazole (biseptol, septrin, groseptol, bactrim, oriprim, etc.) is a combination of sulfamethoxazole and trimethoprim. The drug is well absorbed from the gastrointestinal tract, the duration of the effect is about 8 hours. It is excreted mainly by the kidneys. Assign 2 times a day for infections of the respiratory tract, intestinal, ENT infections, genitourinary system, etc.

Side effects are the same as those of other sulfonamides.

Rice. 33 Mechanism of action of sulfonamides and trimethoprim

Similar drugs are Lidaprim (sulfametrol + trimethoprim), Sulfaton (sulfamonomethoxin + trimethoprim).

Drugs have been created that combine fragments of sulfanilamide and salicylic acid in their structure. These include Salazopyridazine (salazodin), Mesalazine (mesacol, salofalk, etc.). These drugs have antibacterial and anti-inflammatory effects. Applied with ulcerative colitis and Crohn's disease (granulomatous colitis) inside and rectally. When applied, allergic reactions, leukopenia, anemia are possible.

Nitrofuran derivatives

Nitrofuran derivatives are antimicrobial agents with a wide spectrum of activity, they are effective against many gram-positive and gram-negative bacteria, anaerobes, protozoa, rickettsia, fungi. Pseudomonas aeruginosa, Mycobacterium tuberculosis, viruses are resistant to them.

Nitrofurans disrupt the processes of tissue respiration in microorganisms and have a bacteriostatic effect. They are effective in the resistance of microorganisms to other antimicrobial agents.

Nitrofurans are well absorbed from the gastrointestinal tract, approximately evenly distributed in the tissues. Poor penetration into the cerebrospinal fluid. Excreted in the urine by the kidneys, partly with bile into the intestinal lumen.

They are mainly used to treat infections of the intestines and urinary tract, and some are applied topically as antiseptics (furatsilin).

The main undesirable side effects as a result of taking nitrofurans inside are dyspeptic and allergic reactions, dizziness. They have a teturam-like effect (increase the body's sensitivity to alcohol). In order to reduce side effects when taking nitrofuran derivatives, it is recommended to drink plenty of water, take drugs after meals, and B vitamins. Contraindicated in severe diseases of the kidneys, liver, heart, hypersensitivity to nitrofurans, pregnancy, lactation.

Nitrofurantoin (furadonin) has a wide spectrum of antimicrobial activity, is highly active against staphylococcus and Escherichia coli. It is found in high concentration in the urine, therefore it is used for urinary tract infections. In addition, furadonin is excreted in the bile and can be used for cholecystitis.

Furazidin (furagin) has a wide spectrum of action. Used for acute and chronic urethritis, cystitis, pyelonephritis and other infections of the urinary tract and kidneys in tablets. For the treatment of purulent wounds, burns, for douching and rinsing, a solution in isotonic sodium chloride solution is used topically.

Furazolidone inhibits the growth and reproduction of gram-positive and gram-negative microorganisms. Poorly absorbed from the gastrointestinal tract. It is especially active in relation to gram-negative microbes, in particular to causative agents of intestinal infections. It has antitrichomonas and antigiardia activity.

It is used for intestinal infections, sepsis, trichomonas colpitis, giardiasis, infected burns, etc. It is sometimes used to treat alcoholism. Nifuroxazide has the same effect.

Nitrofural (furatsilin) ​​is used in the form of aqueous, alcoholic solutions, ointments as an antiseptic for treating wounds, rinsing and washing cavities, with purulent-inflammatory processes on the skin. Orally in tablets can be used to treat dysentery, urinary tract infections.

Nitroimidazole derivatives

Show bactericidal action against all anaerobes, protozoa, Helicobacter pylori. They are inactive against aerobic bacteria and fungi. They are universal antiprotozoal agents. When taken orally, they are quickly and completely absorbed, penetrate into all tissues, including passing through the blood-brain and placental barriers. Metabolized in the liver, excreted in the urine unchanged and in the form of metabolites, staining it red-brown.

Metronidazole (trichopolum, flagyl, klion, metrogil) is prescribed for trichomoniasis, giardiasis, extracellular amoebiasis, gastric ulcer and other diseases. Assign inside, parenterally, rectally, topically.

Of the side effects, dyspeptic symptoms are most often noted (appetite disturbance, metallic taste, diarrhea, nausea), it can cause a violation of the central nervous system (impaired coordination of movements, convulsions). It has a teturam-like effect, is not compatible with alcohol.

Nitroimidazole derivatives also include Tinidazole (Fazigin), Ornidazole (Tiberal), Nimorazole (Naxogen). They last longer than metronidazole. Tinidazole is part of a complex drug in combination with norfloxacin "N-Flox-T". It has antibacterial and antiprotozoal activity.

Quinolones

1st generation - Non-fluorinated

Derivatives of 8-oxynoline

Intetrix

Nitroxoline

Drugs have a wide spectrum of antimicrobial activity, as well as antifungal and antiprotozoal activity.

The mechanism of antibacterial action is to disrupt protein synthesis of microbial cells. The drugs of oxyquinolines are used for intestinal infections, infections of the genitourinary system, etc.

There are drugs derivatives of 8-hydroxyquinoline that are poorly absorbed and well absorbed from the gastrointestinal tract.

Intetrix is ​​poorly absorbed from the alimentary canal. Effective against most gram-positive and gram-negative pathogenic intestinal bacteria, fungi of the genus Candida. Accepted for acute diarrhea, intestinal amebiasis. Low toxicity.

Nitroxoline (5-NOC, 5-nitrox) is rapidly absorbed from the gastrointestinal tract and excreted by the kidneys unchanged. It is used for urinary tract infections caused by various gram-positive and gram-negative microorganisms. Active against some yeast-like fungi. Assign inside. Of the side effects, dyspeptic phenomena, neuritis are possible. When taking nitroxoline, urine acquires a bright yellow color.

Derivatives of 8-hydroxyquinoline are contraindicated in case of hypersensitivity to them, impaired function of the kidneys, liver, lesions of the peripheral nervous system.

Naphthyridine derivatives

Nalidix acid

Pipemidic acid

Nalidixic acid (nevigramon, blacks) exhibits a strong antibacterial effect against gram-negative microorganisms. Pseudomonas aeruginosa, gram-positive pathogens and anaerobes are resistant to nalidixic acid.

Depending on the concentration, it acts bactericidal and bacteriostatically. Well absorbed when taken orally, excreted in the urine unchanged. It is used for urinary tract infections, especially acute forms, as well as for cholecystitis, otitis, enterocolitis.

The drug is usually well tolerated, sometimes dyspeptic disorders, allergic reactions, photodermatosis are possible.

Nalidixic acid is contraindicated in violation of the function of the liver, kidneys, pregnancy, children under 2 years of age.

Pipemidic acid (palin, pimidel, pipemidine, pipem) has a bactericidal effect against most gram-negative and some gram-positive microorganisms. It is well absorbed from the gastrointestinal tract, excreted by the kidneys unchanged, creating high concentrations in the urine. Used for acute and chronic diseases of the urinary tract and kidneys.

Dyspeptic symptoms and allergic reactions in the form of a rash are possible.

2nd generation - fluorinated (fluoroquinolones)

These drugs are quinolone derivatives containing fluorine atoms in the structure. They are highly active broad-spectrum antibacterial agents. Influence the metabolism of bacterial DNA. They have a bactericidal effect on aerobic gram-negative bacteria, they have a slightly weaker effect on gram-positive pathogens. Active against mycobacterium tuberculosis, chlamydia.

Fluoroquinolones are well absorbed and effective when taken orally, excreted by the kidneys more often unchanged. Penetrate into various organs and tissues, pass through the blood-brain barrier.

They are used for severe infections of the urinary tract, kidneys, respiratory tract, gastrointestinal tract, ENT infections, meningitis, tuberculosis, syphilis and other diseases caused by microorganisms sensitive to fluoroquinolones.

Habituation of microorganisms to fluoroquinolones develops relatively slowly.

Can cause unwanted side effects: dizziness, insomnia, photosensitivity, leukopenia, cartilage changes, dysbacteriosis.

Contraindicated in pregnancy, lactation, up to 18 years.

1st generation - systemic action:

Ciprofloxacin (ciprobay, tsifran, cyprinol), Pefloxacin (abaktal), Norfloxacin (norbactin, nolicin), Ofloxacin (tarivid, oflomax), Lomefloxacin (maksakvin, lomitas) are widely used in urology, pulmonology, ophthalmology, otolaryngology, dermatology for the treatment of infectious diseases of various kinds. They are used orally, by injection, topically.

2nd generation - respiratory fluoroquinolones:

They selectively accumulate in the respiratory tract. Levofloxacin (Tavanic), Moxifloxacin (Avelox) are used for respiratory tract infections, tuberculosis of the lungs, skin and soft tissues 1 time per day. Effective in infections resistant to β-lactam antibiotics, macrolides and other chemotherapeutic agents. Rarely cause unwanted effects.

Drug name, synonyms, storage conditions	Release form	Application methods
Sulfadimidinum (Sulfadimezinum) (B)		First dose 4 tablets then 2 tab. after 4 hours
Sulfanilamide (Streptocidum) (B)	Tab. 0.3; 0.5 Ointment 10% - 15.0; 20.0; 30.0; 50.0 Liniment 5% - 30.0	1-2 tables. 5-6 times a day Into the wound cavity Outwardly on affected areas of the skin Outwardly on affected areas of the skin
Sulfaaethylthiadizolum (Aethazolum) (B)	Tab. 0.5	2 tab. 4-6 times a day Into the wound cavity
Aethazolum-natrium (B)	Amp. 10% and 20% solution - 5ml and 10ml	into a muscle (into a vein) slowly) 3 times a day
(Sulfacylum-natrium) (B)	Flac. (tube- dropper) 10%, 20%, 30% solution - 1.5 ml, 5 ml and 10 ml Ointment 30% - 10.0 Amp. 30% solution - 5 ml	2 drops per cavity conjunctiva 3 times a day Lay behind the eyelid 3 times a day Into a vein slowly 2 times a day
Sulfadimethoxinum (Madribonum) (B)	Tab. 0.5	1-2 tables. 1 time per day (1 day - 4 tablets)
		1 tab. 1 time per day (1 day 5 tablets). at chronic infection 1 tab. 1 time per week
Phthalylsulfathiazidum (Phthalazolum)	Tab. 0.5	2 tab. 4-6 times a day
Sulraguanidinum (Sulginum)	Tab. 0.5	2 tablets 4-6 times a day
Co-Trimoxazolum Biseptolum, Septrinum, Oriprinum)	Tab. 0.12; 24; 0.48; 0.96 Susp. 80ml and 100ml	Pa 2 tab. morning and evening after meals 2 teas. spoon 2 times a day In a vein, 10 ml 2 times a day
Salazopyridazinum (Salazodinum)

A. Systemic action: (etazol, sulfadimesin, sulfapyridazine, sulfamonometoxin, sulfalene);

B. Combined drugs: groseptol (sulfamerazine + trimethoprim), co-trimoxazole (sulfamethoxazole + trimethoprim), sulfatone (sulfamonomethoxin + trimethoprim).

B. Local action: ftalazol, sulgin, ftazin, sodium sulfacyl.

D. Drugs for the treatment of nonspecific ulcerative colitis: sulfasalazine, salazopyridazine.

1. Nitrofuran derivatives:

- systemic action: furagin, furazolidone, nitrofurantoin (furadonin), furazolin.

- local action: nifuroxazide (ercefuril).

- for external use: furatsilin.

1. Quinolone derivatives: nalidixic acid (nevigramone), oxolinic acid (gramurine), pipemidic acid (paline).
2. 4 . 8-hydroxyquinoline derivatives: nitroxoline, intestopan.
3. Fluoroquinolone derivatives: ciprofloxacin, ofloxacin (tarivid), pefloxacin, nofloxacin, lomefloxacin.
4. Nitroimidazole derivatives: metronidazole, tinidazole

To characterize the preparations of each group: the mechanism of action, the spectrum of antimicrobial activity, the features of pharmacokinetics (absorption, distribution, metabolism, elimination), indications for use, side effects, contraindications.

Independent work

Make tables according to the pharmaco-clinical efficacy and safety of drugs: sulfadimezin, sulfapyridazine, sulfasalazine, co-trimoxazole, furagin, furazolidone, nalidixic acid, palin, nitroxoline, tarivid, ciprofloxacin, metronidazole.

Clinical and pharmacological efficacy of drugs

Group	Spectrum of antimicrobial activity	Indications for applications	Preparations
Sulfonamidessystemic actions	Active towards Gram-positive and Gram-negative cocci, E. coli, Shigella, Klebsiella, Vibrio cholerae, pathogens of gas gangrene, anthrax, diphtheria, catarrhal pneumonia, plague, as well as chlamydia, actinomycetes, pathogens of toxoplasmosis.		Sulfadimezin
	Active towards gram-positive and gram-negative microorganisms, as well as chlamydia, actinomycetes.	Pneumonia, bronchitis, purulent otitis, urinary and biliary tract infections, dysentery, enterocolitis, purulent meningitis (meningococcal and pneumococcal), purulent surgical infections; drug-resistant forms of malaria (in combination with antimalarial drugs, including chloridine); leprosy; infectious eye diseases (conjunctivitis, blepharitis, keratitis, trachoma, etc.); furunculosis, burns, bedsores, eczema, abscess. Infections of the upper and lower respiratory tract, ear, throat, nose, genitourinary tract, gastrointestinal tract caused by the specified microflora.	Sulfapyridazine
combined	Active against the following microorganisms: streptococci (hemolytic streptococci are more sensitive to penicillin), staphylococcus, pneumococcus, meningococcus, gonococcus, E. coli (including enterotoxigenic strains), salmonella (including S.typhi and paratyphi), vibrio cholerae, anthrax, Haemophilus influenzae (including ampicillin-resistant strains ), Listeria, Norcardia, Bordetella pertussis, Enterococcus, Klebsiella, Proteus, Clostridia, Pasteurella (including the causative agent of tularemia), Brucella, Mycobacterium, Leprosy, Citrobacter, Enterobacter, Legionella pneumopnia, Providencia, some types of Pseudomonas (except Ps. aeruginosa), Serratia marcescens, Shigella (flexneri and sonnei), Yersinia, Morganella, Pneumocystis carini; large viruses - pathogens, trachoma, psittacosis, ornithosis, inguinal lymphogranulomatosis; protozoa: Plasmodium malaria, toxoplasma, pathogenic fungi, actinomycetes, coccidia, histoplasma, leishmania. Resistant to the drug: Corynebacterium, Pseudomonas aeruginosa, Mycobacterium tuberculosis, spirochetes, leptospira, viruses.	Bacterial infections caused by sensitive microflora: urinary tract infections - urethritis, cystitis, pyelitis, pyelonephritis, prostatitis, gonorrhea (male and female). Respiratory tract infections: bronchitis (acute and chronic), bronchiectasis, lobar pneumonia, bronchopneumonia, pneumocystis pneumonia, inflammation of the middle ear, sinusitis. Infections of the gastrointestinal tract: typhoid, paratyphoid, salmonella, cholera and dysentery. Skin and soft tissue infections: pyoderma, abscesses and wound infections. Osteomyelitis (acute and chronic), brucellosis (acute), septicemia, intra-abdominal sepsis, meningitis, osteoarticular infections, childhood soft tissue and skeletal infections.	Co-trimoxazole
For the treatment of non-specific ulcerative colitis:	- has antimicrobial and anti-inflammatory effects. Able to selectively accumulate in the connective tissue of the intestinal wall with the release of 5-aminosalicylic acid, which has anti-inflammatory activity, and sulfapyridine, which has antimicrobial bacteriostatic activity, a competitive antagonist of para-aminobenzoic acid.		Sulfasalazine
local action	It is active against gram-positive and gram-negative cocci, Escherichia coli, as well as chlamydia, actinomycetes, etc.		Sulfacyl sodium
Nitrofurans systemic action	It has antibacterial activity against both gram-positive and gram-negative microbes. The drug remains active against pathogenic strains of staphylococci and other microorganisms resistant to antibiotics and other chemotherapeutic agents.	Furagin soluble is used in adults with severe forms of infectious and inflammatory diseases caused by pathogenic staphylococcus aureus, streptococcus and other pathogens sensitive to the drug. Furazidin capsules are also used to prevent infections during urological operations, cytoscopies, catheterization, etc. Infectious and inflammatory diseases: purulent wounds, burns, acute and chronic cystitis, urethritis, pyelonephritis; infections of the female genital organs; conjunctivitis.	Furagin
	Effective against gram-positive and gram-negative microbes, Trichomonas, Giardia. The causative agents of dysentery, abdominal and paratyphoid fever are most sensitive to furazolidone. It has little effect on pathogens of purulent infection and anaerobic infection. Microbial resistance develops slowly.		Furazolidone
local action	Effective against gram-positive (staphylococci, streptococci) and gram-negative (salmonella, shigella, proteus) microorganisms.	Diarrhea of ​​various origins (bacterial, in chronic colitis, in violation of intestinal enzymes).	Nifuroxazide (ercefuril)
for outdoor use	Active against gram-positive and gram-negative bacteria (Staphylococcus spp., Streptococcus spp., Shigella dysenteria spp., Shigella flexneri spp., Shigella boydii spp., Shigella sonnei spp., Escherichia coli, Clostridium perfringens, Salmonella spp., etc.).	Outwardly: purulent wounds, bedsores, burns II-III stage, blepharitis, conjunctivitis, furuncle of the external auditory canal; osteomyelitis, empyema of paranasal sinuses, pleura (washing of cavities); acute external and otitis media, stomatitis, gingivitis; minor skin damage (including abrasions, scratches, cracks, cuts). inside: dysentery of bacterial origin.	Furacilin
Quinolone derivatives	Effective against gram-negative microorganisms: Escherichia coli, Salmonella, Shigella, Proteus, Friedlander's bacillus. It acts bactericidal or bacteriostatic depending on the sensitivity of the microorganism and concentration. Strains of microorganisms resistant to antibiotics and sulfonamides are sensitive to the drug. The drug is not active against gram-positive microorganisms and anaerobes.
	It has a bactericidal effect on most gram-negative microorganisms (Pseudomonas aeruginosa and Escherichia coli, Proteus, Klebsiella, Shigella, Salmonella). It is active against some gram-positive microorganisms, in particular, Staphylococcus aureus.
8-hydroxyquinoline derivatives	The drug has an effect on gram-positive (staphylococci, streptococci, corynebacteria, etc.) and gram-negative (E. coli, Proteus, Klebsiella, Salmonella, Shigels, Enterobacteria, gonorrhea pathogens) microbes, is effective against certain types of fungi (Candida, dermatophytes, mold, some causative agents of deep mycoses).		Nitroxoline
Fluoroquinolones	Active against microorganisms producing beta-lactamase. Sensitive to the drug: Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitis, Escherichia coli, Citrobacter, Klebsiella, Enterobacteriaceae, Hafnia, Proteus (indole-positive and indole-negative), Salmonella, Shigella, Yersinis enterocolitica, Campylobacter jejuni, Aeromonas Plesiomonas , Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, chlamydia, legionella. Enterococci, Streptococcus pyogenes, pneumoniae and viridans, Serrratio marcescens, Pseudomonas aeruginosa, Acinetobacter, Mycoplasma hominis and pneumoniae, Mycobacterium tuberculosis, and Mycobacterium fortuim have different sensitivity to the drug. Mostly insensitive: Ureaplasma urealyticum, Nocardia asteroides, anaerobic bacteria (e.g. Bacteroides spp., Peptococci, Peptostreptococci, Eubacterium spp., Fusobacterium spp., Clostridium difficile). Does not work on Treponema pallidum.		Tarivid
	The following pathogens are highly sensitive to ciprofloxacin: E. coli, Shigella, Salmonella, Citrobacter, Klebsiella, Enterobacter, Serratia, Hafnia, Edwardsiella, Proteus (indole-positive and indole-negative), Providencia, Morganella, Yersinia; Vibrio, Aeromonas, Plesiomonas, Pasteurella, Haemophilus, Campylobacter, Pseudomonas, Legionella, Neisseria, Moraxella, Acinobacter, Brucella; Staphylococcus, Listeria, Corynebacterium, Chlamydia. The following microorganisms are moderately sensitive to ciprofloxacin: Gardnerella, Flavobacterium, Alcaligenes, Streptococcus agalactiae, Enterococcus faecalis, Streptococcus pyogenes, Streptococcus pneumoniae, the Viridans group of streptococci, Mycoplasma hominis, Mycobacterium tuberculosis and Mycobacterium fortuitum. The following organisms are considered generally sensitive to ciprofloxacin: Enterococcus faecium, Ureaplasma urealyticum, Nocardia asteroides. With few exceptions, anaerobic organisms are moderately sensitive (eg Peptococcus, Peptostreptococcus) or resistant (eg Bacteroides) to ciprofloxacin. Ciprofloxacin is not effective against Treponema pallidum.		Ciprofloxacin
Nitroimidazole derivatives	Antimicrobial bactericidal drug with high activity against obligate anaerobic bacteria (spore-forming and non-spore-forming), causative agents of some protozoal infections - Trichomonas, Giardia, dysenteric amoeba. Not active against aerobic bacteria. When combined with amoxicillin, it exhibits activity against Helicobacter pylori (amoxicillin inhibits the development of resistance to metronidazole).	Diseases caused by protozoa (amebiasis, trichomoniasis, giardiasis, balantiasis), trichomonas vaginitis, trichomonas urethritis, amoebic dysentery) and anaerobic bacteria (Bac.fragilis and other bacteroids, fusobacteria, eubacteria, clostridia, anaerobic cocci), incl. after surgical interventions on the abdominal organs, in gynecological practice: intra-abdominal infections, appendicitis, cholecystitis, peritonitis, liver abscesses, postoperative wound infections, postpartum sepsis, pelvic abscesses, peritonitis; respiratory tract infections - necrotizing pneumonia, lung abscess; other infections - septicemia, gas gangrene, osteomyelitis, tetanus, meningitis, brain abscess; prevention of postoperative anaerobic infections. Alcoholism. As a radiosensitizing agent - radiation therapy of patients with tumors (cancer, sarcoma) in cases where tumor resistance is due to hypoxia in tumor cells. For the gel: rosacea, acne vulgaris, bacterial vaginosis (intravaginal use), long-term non-healing wounds, trophic ulcers.	Metronidazole

Characteristics of the safety of the use of drugs

				Contraindications to the appointment
Sulfadimezin
Sulfapyridazine			Leukopenia. Anaphylactic shock. Quincke's edema. The formation of sulfo- and methemoglobin. Agranulocytosis. Necrotic angina. Acute renal failure (with repeated administration of large doses of more than 10 g, against the background of low diuresis and acidic urine crystalluria).
Co-trimoxazole (biseptol)
Sulfasalazine
Sulfacyl sodium
Furagin
Furazolidone
Nifuroxazide (ercefuril)
Furacilin
Nalidixic acid (nevigramon)
Pipemidic acid (palin)
Nitroxoline
Tarivid (ofloxacin)	Nausea. violations of taste, smell.
Ciprofloxacin	Nausea. violations of taste, smell.
Metronidazole	Nausea. "metallic" taste in the mouth

be able to choose group and specific drug, its dosage form, dose, route of administration, dosing regimen for the treatment of infectious diseases and write in prescriptions: co-trimoxazole, sulfadimezin, furazolidone, palin, nevigramon, nitroxoline, sulfasalazine, tarivid, ciprofloxacin, sodium sulfacyl.

№	Recipe	Indication for the use of the drug
1	Rp.:Tab. “Co-trimoxazoli” N.20 D.S. 2 tablets 2 times a day. In acute bronchitis, bacterial	Bacterial infections caused by sensitive microflora: urinary tract infections - urethritis, cystitis, pyelitis, pyelonephritis, prostatitis, gonorrhea (male and female). Respiratory tract infections: bronchitis (acute and chronic), bronchiectasis, lobar pneumonia, bronchopneumonia, pneumocystis pneumonia, inflammation of the middle ear, sinusitis. Infections of the gastrointestinal tract: typhoid, paratyphoid, salmonella, cholera and dysentery. Skin and soft tissue infections: pyoderma, abscesses and wound infections. Osteomyelitis (acute and chronic), brucellosis (acute), septicemia, intra-abdominal sepsis, meningitis, osteoarticular infections, childhood soft tissue and skeletal infections.
2	Rp.:Tab.Sulfadimezini 0.5 S. 2 tablets 6 times a day. For the treatment of pneumonia.	Infectious and inflammatory diseases caused by sensitive microflora: pneumonia, meningococcal infections, gonorrhea, sepsis, dysentery, toxoplasmosis, etc.
3	Rp.:Tab. Furazolidoni 0.05 N.20 D.S. 2 tablets 4 times a day. With dysentery.	Dysentery, paratyphoid, giardiasis, food poisoning; Trichomonas colpitis, urethritis; infected wounds and burns
4	Rp.: Palini 0.2 D.t.d. N.20 in caps. S. 2 capsules 2 times a day.	Pyelonephritis, urethritis, cystitis, prostatitis.
5	Rp.:Nevigramoni 0.5 D.t.d. N.56 in caps. S. Inside, 2 capsules 4 times a day in within 7 days. For the treatment of cystitis.	Pyelonephritis, cystitis, urethritis, prostatitis; gastrointestinal infections, cholecystitis, etc. - caused by microorganisms sensitive to the drug. Prevention of infections during operations on the kidneys, ureters, bladder.
6	Rp.:Tab.Nitroxolini 0.05 N.100 S. After meals, 2 tablets 4 times a day. Course 2 weeks. With chronic pyelonephritis.	Acute and chronic infections of the urogenital tract: pyelonephritis, cystitis, urethritis, epididymitis, infected adenoma or carcinoma of the prostate gland, prevention of infections during various interventions (catherization, cytoscopy; prevention of postoperative infections during operations on the kidneys and genitourinary tract).
7	Rp.:Tab.Sulfasalazini 0.5 N.100 D.S. 2 tablets 5 times a day for 2 weeks followed by gradual dose reduction by 0.5 g every 5–7 days; The course is 3 months.	Nonspecific ulcerative colitis; diseases of the broncho-pulmonary system and joints.
8	Rp.:Tab. Tarvidi 0.2 N.20 D.S. 1 tablet 2 times a day. AT within 7 days. For acute infections urinary tract.	Diseases caused by microorganisms sensitive to ofloxacin: infections of the respiratory tract, ear, throat, nose, skin, soft tissues, bones, joints, infectious and inflammatory diseases of the abdominal cavity (with the exception of bacterial enteritis), kidneys, urinary tract, pelvic organs, genitals, gonorrhea.
9	Rp.: Tab. Ciprofloxacini 0.25 N.20 D.S. 1 tablet 2 times a day. course For urinary tract infections.	Respiratory tract infections. The use of ciprofloxacin is indicated for so-called difficult pathogens (eg Klebsiella, Enterobacter, Proteus, Pseudomonas, Legionella, Staphylococcus, Escherichia coli). Infections of the middle ear, paranasal sinuses, especially if they are caused by gram-negative pathogens, including Pseudomonas, or Staphylococcus. Infections of the eyes, kidneys and (or) urinary tract, genital organs, including inflammation of the appendages, gonorrhea, prostatitis; infections of the abdominal cavity (for example, bacterial infections of the gastrointestinal tract, biliary tract, peritonitis), skin and soft tissues, bones and joints (for example, osteomyelitis), sepsis. Treatment and prevention of threatening infections in patients with weakened protective functions of the body, for example, during treatment with immunosuppressive agents or in patients with neutropenia. Selective intestinal decontamination in patients treated with immunosuppressive agents.
10	Rp.:Sol. Sulfacyli-natrii 20%-10.0ml. D.S. Eye drops, 2 drops 4 times a day day. With conjunctivitis.	Conjunctivitis, blepharitis, as well as some other eye diseases, prevention of blenorrhea in newborns.

Classroom work

1. Complete test tasks

1. Long-acting systemic sulfonamides include:

A. Etazol B. Sulfadimethoxin C. Phthalazol D. Urosulfan D. Sulfacyl sodium

1. The mechanism of action of oxyquinoline derivatives is:

A. Formation of complex compounds with metal ions B. Blockade of dehydrofolate reductase C. Competition with para-aminobenzoic acid D. Violation of microbial wall protein synthesis E. Binding of para-aminobenzoic acid

1. Sulfonamides block the synthesis of folic acid in the bacterial cell because they:

A. Compete with para-aminobenzoic acid B. Potentiate the action of para-aminobenzoic acid C. Bind para-aminobenzoic acid D. Disrupt the synthesis of microbial wall proteins E. Increase the osmotic pressure inside the microbial cell

1. Sulfonamides for the treatment of ulcerative colitis include:

A. Etazol B. Co-trimoxazole C. Phthalazol D. Salazopyridazine D. Sulfacyl sodium

1. Antitrichomonas and antilambliosis activity has:

A. Furazolidone B. Etazol C. Ofloxacin D. Ampicillin D. Ketoconazole

1. Specify the points of action of sulfonamides and trimethoprim

para-aminobenzoic

Dihydropteridine

Dihydropteorate synthetase

Dihydropteroic acid

Dehydrofolate reductase

Synthesis of purines

Synthesis

Topoisomerases Cellular DNA replication

walls

Nucleotide Synthesis Protein Synthesis

cell wall

cytoplasmic membrane

1. solve problems

Task #1

Dihydrofolate reductase activity inhibits:

Task #2

The activity of dihydropteroate synthetase inhibits:

1. Sulfadimezin 2. Trimethoprim 3. Sulfamethoxazole 4. Norsulfazol

Task #3

The activity of DNA gyrase of bacterial nuclei inhibits:

1. Dioxidin 2. Ciprofloxacin 3. Lomefloxacin 4. Metronidazole 5. Entefuril.

Task #4

Sulfonamides block the synthesis of folic acid in the bacterial wall, because:

1. They compete with para-aminobenzoic acid, which is a precursor to folic acid.
2. They potentiate the action of para-aminobenzoic acid, which is a natural folic acid antagonist.
3. They bind para-aminobenzoic acid and form an inactive complex

Task #5

Make a rational choice of a synthetic antimicrobial agent:

A. Ambulatory croupous pneumonia: 1. Co-trimoxazole 2. Ofloxacin. 3. Ercefuril

B. Hospital lobar pneumonia: 1. Co-trimoxazole 2. Ofloxacin. 3. Ercefuril

Propose a technology for the use of the selected means.

1. Solve problems on the choice of synthetic antimicrobial agents, taking into account the state of the organs and systems of the patient's body, side and toxic effects of drugs

Task #6

The following statements about sulfonamides are true:

1. Sulfadimethoxine has a long half-life 2. Salazosulfopyridine is commonly used for urinary tract infections 3. Sulgin is poorly absorbed from the gastrointestinal tract 4. Sulfacyl-Na is a suitable agent for topical application to the eye 5. If an allergic reaction occurs during treatment, the dose should be reduced during 2-3 days

Task #7

Sulfonamides:

1. Generally more soluble in alkaline urine 2. Achieve higher concentrations in blood than in urine 3. Are more active after being metabolized and acetylated in urine 4. Are more active in alkaline urine 5. May precipitate in urine to form crystals

Task #8

Sulfonamides can cause kidney damage, which may be due to the precipitation of crystals in the collecting tubules of the kidney. Factors predisposing to the formation of a crystalline precipitate are:

1. High concentration of the drug in the urine 2. Poor solubility of the drug in the urine 3. Urinary pH around 5.0 4. Simultaneous administration of several sulfonamides

Task #9

The most common causative agent of urinary tract infections is Proteus, which is highly sensitive to nitrofurantoin.

1. True 2. False

Task #10

The most common causative agent of intestinal infections is Escherichia coli, Salmonella, cholera, Enterobacter, dysentery bacillus: 1. True 2. False

Task #11

The causative agents of intestinal infections are highly sensitive to:

1. Ciprofloxacin 2. Nitroxalin 3. Entefuril.

Task #12

Sulfonamides are metabolized by:

1. Acetylation 2. Conjugation with glucuronic acid 3. Conjugation with sulfates

Task #13

Slowing down and accelerating the acetylation of sulfonamides:

1. Genetically determined 2. Depends on body temperature. 3. Depends on the dose of the drug. 4. Depends on the age of the patient

Task #14

In alkaline urine, sulfonamides:

1. Less soluble 2. More soluble 3. Insoluble 4. Stability of sulfonamides does not depend on urine pH

Task #15

For the treatment of urinary tract infections, the dose of sulfonamides should be:

1. Doubled compared to the dose required to treat a systemic infection 2. Equal to the required dose to treat a systemic infection 3. Less than the required dose to treat a systemic infection 4. Sulfonamides are not effective for treating a urinary tract infection

Task #16

The risk of developing crystalluria during sulfonamide therapy can be reduced by:

1. Prescription of more soluble sulfonamides 2. Alkalinization of urine 3. Treatment against the background of increased water load (diuresis up to 2 liters per day) 4. None of the above.

1. Substantiate a rational combined pharmacotherapy, taking into account the pharmacological and pharmaceutical interaction of drugs

Task #17

Combination of sulfonamides with trimethoprim:

1. Effective because sensitive enzyme reactions are inhibited

synthesis of folic acid 2. Safe, because no inhibitory reactions occur in humans

1. Can cause drug-induced anemia, which is successfully treated with folic acid without inhibiting the antibacterial effect 4. Bactericidal, although its components are bacteriostatic 5. Easily leads to drug resistance

Task #18

In co-trimoxazole, sulfamethoxazole is preferred over other sulfonamides because:

1. It is the least toxic 2. It acts in the same way as trimethoprim 3. The least resistance develops 4. Its half-life is similar to trimethoprim

Task #19

In acute urinary tract infection, with acidic urine, when the pathogen is not determined, treatment can be started with:

1. Chloramphenicol 2. Tetracycline 3. Co-trimoxazole 4. Furazolidone

Task #20

In acute urinary tract infection, with alkaline urine and lack of identification of the pathogen, treatment can begin with:

1. Co-trimoxazole 2. Nitrofurans 3. Sulfonamide 4. Entefuril

Task #21

Specify the drugs of choice for urinary tract infection caused by Pseudomonas aeruginosa:

1. Nitrofurans 2. Nalidixic acid 3. Ciprofloxacin 4. Ofloxacin

Task #22

What drugs are indicated for the treatment of chlamydial infection of the genitourinary tract:

1. Nitroxoline 2. Palin 3. Ofloxacin

Task #23

With long-term use, which uroantiseptics can develop polyneuritis?

1. Biseptol 2. Furagin 3. Nitroxoline

Task #24

Specify a uroantiseptic that does not cause intestinal dysbacteriosis:

1. Sulfadimezin 2. Palin 3. Furagin