Sulfonamides antibiotics. See what "Sulfanilamide preparations" are in other dictionaries.

A group of compounds with the general formula belongs to sulfa drugs. One of the hydrogen atoms of the amino group in position 4 can also be substituted by various radicals.
The chemotherapeutic activity of sulfa drugs was discovered in the early 1930s. This is the first group of modern chemotherapeutic antibacterial agents.
The first drug in this group to receive practical use in medicine, there was Kprontosil [Domagk, 1934], or red streptocide. It was soon established that> red streptocide is a Ksulfanilamide formed during metabolism (streptocid, white streptocide). Therefore, red streptocide went out of use, and on the basis of the sulfanilamide molecule it was synthesized a large number of its derivatives, of which some have received wide application in medicine.
With the advent of penicillin and other antibiotics, and in recent times fluoroquinolones, the use of sulfonamides has somewhat decreased, however, the values ​​of the drugs of this group have not lost and in some cases are successfully used for infectious diseases caused by microorganisms sensitive to them.
Sulfanilamide preparations have chemotherapeutic activity in infections caused by gram-positive and gram-negative bacteria, some protozoa (causative agents of toxoplasmosis malaria), chlamydia (with trachoma, paratrachoma).
Their action is mainly associated with a violation of the formation of growth factors necessary for their development by microorganisms - folic and dihydrofolic acids and other substances, the molecule of which includes para-aminobenzoic acid. Sulfonamides are close in chemical structure to para-aminobenzoic acid, they are captured by the microbial cell instead of para-aminobenzoic acid and thereby disrupt the course of metabolic processes in it.
Sulfonamides have a bacteriostatic effect. To receive therapeutic effect they must be administered in doses sufficient to prevent microorganisms from using para-aminobenzoic acid contained in tissues. U Taking sulfa drugs in insufficient doses or stopping treatment too early can lead to the emergence of resistant strains of pathogens that are not susceptible to further action sulfonamides. It should be borne in mind that some medications, the molecule of which includes the residue of para-aminobenzoic acid (for example, novocaine), can have a pronounced antisulfanilamide effect.
Available sulfa drugs differ in pharmacological parameters. Streptocid, norsulfazole, sulfazine, sulfadimezine, etazole, sulfapyridazine, sulfadimethoxine, etc. are relatively easily absorbed and rapidly accumulate in the blood and organs in bacteriostatic concentrations, penetrate the histohematological barriers (blood-brain, placental, etc.); they find application in the treatment of various infectious diseases. Other drugs, such as phthalazol, phtazin, sulgin, are difficult to absorb, are in the intestines for a relatively long time in high concentrations and are excreted mainly in the feces. Therefore, they are mainly used for infectious diseases. gastrointestinal tract... Urosulfan is excreted in significant quantities by the kidneys; it is used mainly for infections urinary tract.
According to the time of excretion from the body, sulfonamides can be divided into 4 groups: a) short-acting drugs (streptocid, norsulfazole, etazole, sulfadimezin, etc.); b) medium action (sulfazine, etc.); v) long acting(sulfapyridazine, sulfamonomethoxin, sulfadimethoxine, etc.); d) ultra-long-term action (sulfalene, etc.).
Drugs that are slowly released from the body are called. Their slow excretion is largely due to the ability to be reabsorbed (reabsorbed) in the renal tubules after glomerular filtration.
Absorption and the rate of excretion from the body largely determine the size of the dose and the frequency of drug intake.
The maximum blood concentration of short-acting drugs decreases by 50%, usually in less than 8 hours, and 50% of them are excreted in the urine in less than 16 hours. 16 and 24 - 48 hours, excretion of 50% with urine - after 16 - 24 and 24 - 56 hours, which makes it possible to prescribe these drugs less often and in smaller doses. Ultra-long-acting drugs are released even more slowly: maximum concentration in the blood lasts up to 7 days.
Sulfanilamide preparations can, if necessary, be used in different combinations... Poorly absorbed drugs can be administered concurrently with well-absorbed drugs. You can combine sulfonamides with antibiotics.
In the 70s, a highly effective combination drug was developed containing a sulfa drug (sulfamethoxazole) in combination with trimethoprim (see Bactrim and Sulfaton). The drug has a wide spectrum of antibacterial activity and is widely used.
Some sulfa drugs have special application as local antimicrobial agents for the treatment of purulent wounds (see Sulfazine silver salt) and eye infections - in the form of solutions (see Sulfacil sodium, Sulfapyridazine sodium).
Of the sulfonamide drugs of systemic action, Bactrim (Biseptol) is currently widely used, which is fully consistent with the effectiveness of the domestic drug sulfaton. Sulfadimethoxine, sulfalene, sulfapyridazine, mafenide, etazole, salazopyridazine are also used.
Sulfanilamide drugs can cause allergic reactions and other side effects: nausea, vomiting, dermatitis, leukopenia, neuritis, etc. Sometimes there are dysfunctions of the central nervous system. Renal dysfunction is relatively common. Due to poor solubility, sulfonamides and especially their acetylation products, formed in the body by replacing the amino group hydrogen with a residue acetic acid, can fall out in the kidneys in the form of crystals (crystalluria) and block the urinary tract. Sulfonamides and their acetyl derivatives are especially poorly soluble in acidic urine.
U To prevent the listed complications, patients while taking sulfanilamide drugs should receive abundant alkaline drink. When using long-acting drugs, side effects are usually less pronounced, which is explained by the intake of these drugs in lower doses. At the same time, it should be borne in mind that due to the slow release from the body and the possibility of cumulation, side effects (dyspeptic symptoms, allergic reactions, blood changes, etc.) may be more persistent than when taking short-acting sulfa drugs.
Given the possibility of the development of side effects and the resistance of microorganisms to sulfa drugs, it is necessary to use these funds only as directed by a doctor.

Sulfanilamide drugs are antibacterial substances that have shown nice results in the treatment of diseases caused by bacteria in humans. Sulfonamides familiar to many have long established themselves with positive side, because they were invented even before the appearance penicillin antibiotics, as well as fluoroquinols.

In connection with the release modern drugs sulfanilamide are produced in a smaller volume, but their importance in practical official medicine did not shake at all. Still, with sensitivity to sulfonamides of bacterial flora and harmful microorganisms, which are shown by analyzes, they choose this particular active ingredient, which has been tested over the years.

How sulfa drugs work

It was revealed that sulfa drugs cope with certain types bacteria, including:

• gram-positive and negative bacteria;
• protozoa that cause malaria and toxoplasma;
• chlamydia.

Effective action is achieved by disrupting the formation process necessary conditions for reproduction and the existence of infection in human body... The microbial cell lives by feeding on para-aminobenzoic acid, with which sulfa drugs are similar in structure. As a result, the bacterium begins to feed on another substance that destroys the metabolic processes of the microbe, after which the latter dies.

Types of sulfa drugs

Sulfonamides are distinguished by the circulation period:

• short action;
• medium action;
• long-acting;
• ultra-long.

Time does not stand still, and, unfortunately, many strains of microbes were able to mutate and adapt to sulfonamides. V in this case doctors have found the next effective way to deal with bacteria - by combining the sulfanilamide group of antibiotics with trimethoprim. Combined medicines also help, which also include a sulfanilamide component.

What types of sulfonamides are currently used to treat microbial ailments:

1. Co-trimoxazole.
2. Sulfadimethoxine.
3. Sulfalene.
4. Sulfaetidol.

In terms of chemical content, the agents are similar to sulfones, which exhibit excellent activity against leprosy mycobacteria, and therefore are used to treat a serious disease - leprosy.

Sulfaminalamide preparations in pure form: list

It is impossible to list absolutely all sulfa drugs found in pharmacies, so we have compiled a list of the most basic medicines used in modern times to cure many strains of bacteria:

1. Argidin.
2. Argosulfan.
3. Bactrim.
4. Berlocid.
5. Biseptol.
6. Dermazin.
7. Duo-Septol.
8. Co-trimoxazole-Rivopharm.
9. Kotrifarm.
10. Mafenide acetate ointment 10%.
11. Oriprim.
12. Septrine
13. Sinersul.
14. Streptocide.
15. Streptocide ointment 10%.
16. Sulgin.
17. Sulfadimezin.
18. Sulfadimethoxine.
19. Sulfalene.
20. Sulfargin.
21. Sulfacetamide.
22. Sulfacetamide sodium.
23. Sumetrolim.
24. Trimezole.
25. Phthalazol.
26. Tsiplin.
27. Etazole sodium.
28. Etazole tablets.

Sulfonamides in combinations

There are not so many sulfa drugs in combinations:

1. Ingalipt - used as a remedy for inflammation of the tonsils, which is characterized by sore throat, swelling, pain. An otolaryngologist (ENT) prescribes Ingalipt if patients, including children, are diagnosed with one of the following ailments: tonsillitis, pharyngitis, laryngitis, stomatitis, expressed in ulcers. The pharmacological action of the spray is based on anti-inflammatory and antimicrobial principles. Plant extracts not only are powerful antiseptics, but also refresh the larynx. Children can be taken from the age of 12, because medicated oils can cause an allergic reaction in babies.
2. A variation of Ingalipt is another sulfa drug - Ingalipt-Vial.
3. Lidaprim - helps in the treatment of many bacterial diseases, complete list which can be found in the instructions for use. They are mainly associated with inflammatory ailments of the throat, nose and ear, complicated by infections of the skin, urinary system. The antibiotic is also useful as a maintenance therapy after surgery. To prevent the bacteria from Candida, it is shown to orally consume tablets to maintain the intestinal microflora, women can insert suppositories into the vagina.
4. Streptonitol - helps cleanse the skin and organs from bacteria. Doctors prescribe a drug for the treatment of wounds, burns from 1 to 4 degrees, bedsores, trophic ulcers, gangrene formed against the background of diabetes. The remedy saves from erysipelas, dermatitis of various etiologies and pyoderma. Also attributed to acne. However, with the use of Streptonitol, you need to be careful in patients who have wounds with profuse purulent discharge.

Indications for the use of basic sulfa drugs

Doctors note the following features of the main sulfa drugs:

1. Argosulfan - acts not only against bacteria, but also against microbes of different strains. It can be applied openly or with an occlusive dressing on the wound. If a bandage is applied, it is important to cleanse the affected area with particular care. The thickness of the application of the ointment is at least 2-3 mm, it is allowed to use it 3 times a day.

It is considered inappropriate to leave individual areas uncovered, the cream must be placed tightly so that it is not visible skin... You can cover the wound or leave it uncovered with a bandage, the cream will not spread.

How long does Argosulfan treatment last? Before complete healing area or before a skin graft is planned. Do not be alarmed if exudate appears in the wound - this is normal phenomenon with internal infection. Before use, doctors recommend washing the wound from ichor and other secretions with Chlorhexidine 0.1%.

The ointment must not be frozen, otherwise it will lose its medicinal properties.

1. Biseptol is an antibiotic of the sulfanilamide class, which is directed against bacteria, the advantage is that today it is effective against many types of microbes. Therefore, the course of Biseptol will relieve such ailments as bronchitis, sinusitis, whooping cough, scarlet fever, syphilis, gonorrhea, chlamydia, malaria, meningitis, otitis media, pneumonia, peritonitis, osteomyelitis, cystitis and urethritis, both chronic and primarily indicated.

Biseptol can be stored for up to 5 years at a temperature not exceeding 25 degrees with a plus sign.

1. Berlocid - the unique composition of the drug allows you to fight against microorganisms that are resistant to other representatives of the sulfanilamide group. Berlocid is prescribed for infections involving respiratory tract, ear, throat and nose. The antibiotic is active against microbes found in the kidneys, genitourinary tract and organs of the gastrointestinal tract. Among the contraindications in the instructions, the manufacturer indicated: hypersensitivity to individual components of the medication, Stevens-Johnson syndrome, severe complications associated with kidney and liver dysfunction, prematurity. Pregnant women should not use the active ingredient in this composition in the 1st trimester of pregnancy.
2. Dermazin - helps to heal burns, bedsores and wounds that have affected the deep layers of the skin. Among side effects itching, burning and baking of the treated area may occur. The ointment is applied no more than 2 times a day after surgical treatment of the wound and disinfection. The remedy is not applicable to newborns. Dermazin is designed for external use only.
3. Co-trimoxazole-Rivopharm. Tablets are available with content active substance volume of 120 mg, 480 mg, 960 mg. Also on sale are suspensions for oral administration, packaged in 100 ml vials. With the help of an antibiotic, therapy is carried out for streptococci, staphylococci, pathogens of gonorrhea, salmonella, which cause in humans severe forms poisoning.
4. With the help of Streptocide, wounds are treated; for this, the tablets should be rubbed into powder. The powder is applied both wet and dry alone. Allergic reactions may occur very rarely.

SULPHANYLAMIDE PREPARATIONS

Sulfonamides (SA) are called large group chemotherapy medicinal substances a wide spectrum of action, based on the structure of sulfanilic (para-aminobenzosulfanoic) acid.

The first reports about SA, or rather about derivatives of sulfanilic acid, were made in 1908 in Germany by the German scientist Gelno. In 1932, chemists Mitchell and Klarer obtained a red dye for fabrics, which in 1935 was tested by the German scientist Domagk as an antimicrobial agent and showed good results. Domagk called this drug prantosil. Thus, in 1935, the use of CA drugs began. In the same year, in the USSR, Magidson and Rubtsov obtained red streptocide, an analogue of prantazil. Currently, about 10,000 different sulfonamides have been synthesized. In practice veterinary medicine applies to about forty.

All sulfonamides are white or slightly yellowish powders. Most of them are poorly soluble in water, better in dilute acids and alkalis. Sodium salts of individual CAs dissolve well and can be used orally, intravenously (5-10% solutions) and very rarely subcutaneously (1-1.5% solutions). They suppress the vital activity of many types of gram-positive and gram-negative bacteria, streptococci, staphylococci, meningococci, bacteria of the entero-typhoid group, large viruses. In normal concentrations, they act bacteriostatically, and in high concentrations, they are bactericidal.

The mechanism of the bacteriostatic action of sulfonamides is due to the competitive relationship between sulfonamide and PABA, which in some microorganisms takes part in the synthesis folic acid and is necessary for the synthesis of purine and pyrimidine bases with further formation of DNA and RNA, which cause the growth and reproduction of microorganisms. Such competition is possible due to the similarity of the geometric configuration and sizes of sulfonamide and PABA molecules.

At a high concentration of sulfanilamide in the blood (at least 300 times higher than the concentration of PABA), the microorganism instead of PABA assimilates the sulfanilamide drug, which cannot replace it. For the manifestation of antimicrobial activity, the concentration of free sulfanilamide in plasma must be at least 40 μg / ml.

Most CAs are readily absorbed from the gastrointestinal tract and rapidly accumulate in the blood, organs and tissues at therapeutic concentrations, penetrate through the blood-brain and placental barrier... Some CAs (phthalazole, sulgin and phtazin) are poorly absorbed and remain in the intestine for a long time in high concentrations. They are excreted mainly in feces, therefore they are usually used for diseases of the gastrointestinal tract. Most drugs in this group are excreted through the kidneys. With various pathologies (dystrophic, inflammatory processes) and with an acidic reaction of urine, CA form acetylated compounds, which can lead to the development of urolithiasis... To prevent this, CA is recommended to be prescribed with a large amount of water. alkaline reaction... CA can be secreted by the mammary, sweat, salivary, bronchial and other glands.

To create a therapeutic concentration of sulfonamides, the first dose is assigned a double (shock). The course of treatment lasts 3-8 days. Short-acting drugs are prescribed 4-6 times a day, medium - 2 times, long-term and ultra-long - 1 time per day. Treatment with small doses, non-compliance with the frequency of use and the course of treatment lead to the development of sulfanamide-resistant microorganisms. Resistance acquired to one sulfonamide extends to other drugs, and can also be genetically inherited.

Sulfonamides are low-toxic compounds. However, long-term use of them in overestimated doses can lead to the development of undesirable phenomena: allergic reactions, dysbiosis, vitamin deficiency (group B), crystalluria, violation of the morphological and biochemical composition of the blood.

SA is used for infectious diseases of the respiratory tract, gastrointestinal diseases different etiology, in obstetric and gynecological practice, surgery, etc. All CAs are divided into a number of groups by action. The first group - SA of general (resorptive) action. They are well absorbed from the gastrointestinal tract. According to the duration of action, these drugs can be divided into several groups: CA with short term actions (6-8 hours) - streptocide, norsulfazole, etazole, sulfacil, sulfadimezin; CA with a medium duration of action (12 hours) - sulfazine; CA with long-term and ultra-long action (24 hours or more) - sulfadimethoxine, sulfamonomethoxin, sulfapyridazine, sulfalene. The second group is CA of intestinal action. Poorly absorbed from the intestines (sulgin, phthalazole, phtazin, disulformin). The third group - CA for external use - sulfacil and sodium sulfacil.

Streptocid (white streptocid, prontosil, ambesid, etc.) -Streptocidum.

White crystalline powder, tasteless, poorly soluble in water (1: 170), well in boiling water, difficult in alcohol (1:35), well soluble in solutions of caustic alkalis. The solutions are stable during storage.

Release form. Powder; tablets of 0.3 and 0.5 g; 10% ointment and 5% liniment.

Soluble streptocid - Streptocidum solubile.

White crystalline powder, readily soluble in water.

Release form. Powder; liniment 5% in tubes of 30 g.

Storage. According to the "B" list. Shelf life is 10 years.

Action. Bacteriostatic for coccal forms (except for staphylococci), Escherichia coli, the causative agent of gas gangrene, etc.

After entnral administration, streptocide is well absorbed by the mucous membrane. Maximum concentration in the blood, various bodies and tissues appears in 1-2 hours and lasts 4-6 hours. The drug easily passes all barriers, binds to proteins by 20%. The acetylation process occurs 25-60% in the urine.

Application. With streptococcal tonsillitis, tonsillar abscesses, bronchopneumonia, sepsis, wash, cystitis, pyelitis, enterocolitis, wounds, ulcers, burns, and other pathological processes. Assign enterally 4-6 times a day for 5-7 days in doses (g per animal): horses and cattle - 5-10; small ruminants and pigs - 0.5-2; dogs -0.5-2. Intravenous streptocide soluble in the form of a 10% solution: for horses and cattle -3-6; small ruminants - 1-2; dogs - 0.3-0.5; 5% solution of soluble streptocide can be administered subcutaneously or intramuscularly. In case of mastitis, 3-5% solutions are injected into the affected milk cistern, 25-40 ml 2-3 times a day. Outwardly, the drug is used to treat wounds, pyoderma, burns, in the form of powders, 10% ointment and 5% liniment. The preparations are applied to surfaces after mechanical cleaning. The use of streptocide is contraindicated in general acidosis, hepatitis, hemolytic anemia, agronulocytosis, nephritis and nephrosis.

Norsulfazole (amidothiazole, polyseptyl, sulfatazole) - Norsulfasolum.

White or white with a slightly yellowish sheen, crystalline powder, odorless. We will dissolve very little in water, little in alcohol, we will dissolve in diluted mineral acids and solutions of caustic and carbonic alkalis.

Release form. Powder, tablets of 0.25-0.5 g.

Norsulfazole sodium (soluble norsulfazole) - Norsulfasolum natrium.

White powder, readily soluble in water (1: 2).

Storage. According to the "B" list. In a dry, dark place. Shelf life: non-dissolving - 5 years; soluble - 3 years.

Action. Highly active in relation to hemolytic streptococcus, pneumococci, gonococci, staphylococci, Escherichia coli, Pasteurella and Salmonella are also sensitive. After enteral administration, the therapeutic concentration in the blood is reached after 3-6 hours and is maintained for 6-12 hours, 60-70% bound to blood proteins.

Application. With bronchopneumonia, pleurisy, streptococcal sepsis, endometritis, mastitis, gastroenteritis, necrobacteriosis, diplococcal septicemia, poultry pasteurellosis, coccidiosis. Assign enterally in doses (g per animal): horses and cattle - 10-25; small ruminants and pigs -2-5; chickens - 0.5. With bronchopneumonia, calves are injected with an 8-10% solution intratracheally at the rate of 0.05 g / kg of weight. In case of poultry pasteurellosis, norsulfazole is administered intramuscularly in the form of a 20% oil suspension or aqueous solution at the rate of 1 ml per 1 kg of weight. Norsulfazole sodium is administered intravenously in the form of 5-10% solutions in doses (g per animal): horses and cattle - 6-10; sheep - 1-2; dogs - 0.5-1 g.

Etazol (globucid, setadil, etc.) - Aethazolum.

White or white powder with a slightly yellowish sheen. Practically insoluble in water, hardly soluble in alcohol, easily in alkali solutions.

Release form. Powder, tablets of 0.25 and 0.5 g.

Etazole sodium (soluble etazole) - Aethazolum natrium.

White crystalline powder, easily soluble in water.

Release form. Powder, solution 10% and 20% in ampoules of 5 and 10 ml.

Storing. According to the "B" list. Powder in a well sealed container, protected from light. The shelf life of etazole is 3 years, sodium ethazole is 5 years.

Action. Antimicrobial against streptococci, pneumococci, meningococci, colibacillus and dysentery bacilli, uterine anaerobes. The therapeutic concentration in the blood of cattle after enteral administration is created after 5-8 hours, in dogs after 2-3 hours and is kept up to 10 hours.

Application. For bronchopneumonia, pneumonia, dyspepsia, dysentery, pyelitis, cystitis, postpartum sepsis, endometritis, pulorosis of chickens, pasteurellosis, pig erysipelas, wound infection, etc. Assign enterally (g per animal): horses - 10-25; KRS - 15-25; small ruminants -2-3; pigs -2-5; dogs - 0.3-0.5; rabbits -1-1.5; poultry - 0.5 g 3-4 times a day. Etazole sodium is administered intravenously (10-20% solution) (rarely intramuscularly) in doses (g per animal): horses and cattle - 5-10; small ruminants -1-2; pigs -2-3; dogs - 0.1-0.3 - 2-3 times a day. Powders or 5% ointment are applied externally.

Sulfadimesin (dimetrazyl, sulfamezatil, superseptyl) -Sulfadimesinum.

White or slightly yellowish crystalline powder. Practically insoluble in water, readily soluble in solutions of acids and alkalis. Release form. Powder, tablets of 0.25-0.5 g.

Storage. According to the "B" list. In a well sealed container, protected from light. Shelf life is 10 years.

Action. Broad antimicrobial spectrum. Pneumococci, staphylococci are sensitive to the drug, colibacillus, salmonella, pasteurella. After enteral administration, the maximum concentration of the drug in the blood is created after 6-8 hours, 75% binds to blood proteins and accumulates in it in large quantities.

Application. For pneumonia, bronchopneumonia, tonsillitis, pharyngitis, sepsis, endometritis, mastitis, dyspepsia, gastroenteritis, salmonellosis, pasteurellosis, respiratory mycoplasmosis, urinary tract infections, etc. Prescribe enterally 2 times a day in doses of horses and animals (g per animal): 15-20; small ruminants -2-3; pigs -1-2; chickens -0.3-0.5. In case of pasteurellosis, birds are fed with compound feed at the rate of 0.05 g per 1 kg of weight 1-3 times a day for 4 days.

Sulfapyridazine (quintoseptil, microcide, depovermil) -Sulfapyridasinum.

Crystalline powder, white with a slightly yellowish sheen, odorless, bitter in taste. Practically insoluble in water, slightly soluble in alcohol, easily in diluted acids and alkalis.

Sulfapyridazine sodium - Sulfapyridasinum natrium.

Release form. Powder, 10% solution in 7% polyvinyl alcohol, 10 and 100 ml each.

Storage. According to the "B" list. In a dry, dark place. Shelf life is 2 years.

Action. Bacteriostatic against most coccal microorganisms, colibacillus and dysentery bacillus, toxoplasma, coccidia, etc. It is rapidly absorbed. The therapeutic concentration in the blood is created 1 hour after application and is maintained for a day.

Application. For pneumonia, bronchitis, pharyngitis, mycoplasmosis, enterocolitis, dysentery, salmonellosis, colibacillosis, endometritis, mastitis, urinary tract infections, surgical pathology... Assign enterally in doses (mg / kg of animal weight): cattle - 50-75; piglets - 75-100; dogs -25-30; rabbits -250-500; chickens - 100-120 once a day. Sulfapyridazine sodium is used intravenously (less often intramuscularly) in the form of 5-10% solutions in isotonic NaCl solution or 2-5% polyvinyl alcohol solution. Intravenous doses (mg / kg of animal weight): cattle -25-30; small ruminants - 50-75 once a day.

Sulfadimetoxin (deposul, madroxin, madribone) - Sulfadimetoxinum.

White or white with a cream shade, crystalline powder, odorless. Practically insoluble in water, little in alcohol. Let's well dissolve in solutions of acids and alkalis.

Release form. Powder, tablets of 0.2 and 0.5 g.

Storage. According to the "B" list. In a dark place. Shelf life is 4 years.

Action. A wide range of antimicrobial action against gram-positive and gram-negative microorganisms, especially on meningo-, strepto- and staphylococci, Escherichia coli, shigela, dysentery pathogens. It is absorbed slowly. The therapeutic concentration in the blood is created: in cattle after 8-12 hours; sheep - 5-6 hours; dogs - 2-5 and kept for 2448 hours. Almost does not penetrate through barriers.

Sulfamonometoxin (diameton, dufadin, etc.) - Sulfamonometoxinum.

Crystalline powder, white with a cream shade. Let's very little dissolve in water, alcohol, well - in solutions of acids and alkalis. Release form. Powder, tablets of 0.5.

Storage. According to the "B" list. In a dark place. Shelf life is 2 years.

Action. The spectrum of action is close to sulfapyridazine. Well absorbed. The therapeutic concentration in the blood and tissues is created in 4-6 hours and lasts for 24-48 hours. Penetrates the blood-brain barrier.

Application. Similar to sulfapyridazine.

Sulfalen (Kelfisin, Dalisep, Policidal, etc.) - Sulfalenum.

White crystalline powder, almost insoluble in water and readily soluble in solutions of acids and alkalis.

Release form. Tablets of 0.2 and 0.5 g; soluble form sulfalene-methemoglobin - 10% solution in ampoules of 2 and 5 ml.

Storage. According to the "B" list. The shelf life is 5 years.

Action. In terms of antimicrobial action, it is close to other sulfonamides. Differs in an ultra-long period of validity. The therapeutic concentration of the drug in the blood is created after 4-6 hours and is retained by 60% for 3-5 days, 9 days are excreted from the body.

Application. For bronchopneumonia, colibacillosis, salmonellosis, pasteurellosis, toxoplasmosis, respiratory mycoplasmosis, mastitis, endometritis, etc. Prescribed enterally once every 5-7 days for chronic pathology and once a day for acute in doses (mg / kg animal weight): to calves - dairy producers - 20-25; suckling pigs - 40-50; chickens -100-150.

Sulfacil sodium (albucid, sobizon, ophthalmide) - Sulfacilum natrium.

Flavourless white crystalline powder. It dissolves well in water, poorly in alcohol.

Release form. Powder; solution of 30% in ampoules of 5 ml; solution of 30% in vials of 5 and 10 ml; solution of 20% in dropper tubes of 1.5 ml; 10% solution with methylcellulose and 30% ointment in tubes of 10 g.

Action. Antimicrobial for staphylococcal, streptococcal, pneumococcal, colibacillary and salmonella infections. It is rapidly absorbed, the maximum concentration in the blood is kept for 25 hours.

Application. With tonsillitis, pharyngitis, bronchopneumonia, postpartum sepsis, streptococcal infections, escherichiosis, salmonellosis, dyspepsia, enterocolitis, etc. Prescribed enterally 1-2 times a day in doses (g per animal): horses and cattle -3-10; small ruminants and pigs -1-2; dogs - 0.3-0.5. Topically for the treatment of conjunctivitis, blepharitis in the form of 10, 20 and 30% solutions or ointments.

Mafenid - Maphenidum.

Sulfanilamide preparation for external use.

Release form. Ointment 10% in orange glass jars of 50 g and 2 kg.

Action and application. A wide range of actions. Topically for the treatment of infected wounds, burns, bedsores, etc.

Phtalazol (talidin, talisulfazole, talazol, etc.) - Phtalazolum.

Powder, white with a slightly yellowish sheen. Practically insoluble in water and alcohol, soluble in sodium carbonate solution.

Release form. Powder, tablets of 0.5 g.

Storage. According to the "B" list. Shelf life is 10 years.

Action. Antimicrobial against the intestinal group of pathogenic microorganisms and some gram-negative. Very little is absorbed from the gastrointestinal tract and creates in the lumen high concentration drug.

Application. With dysentery, salmonellosis, gastroenterocolitis, for prevention postoperative complications... Assign enterally in doses (g per animal): horses - 10-15; KRS -10-20; pigs - 2-5; dogs - 0.5-1; chickens -0.1-0.2 two to four times a day.

Sulgin (guanicil, guamid, guacept, etc.) - Sulginum.

White fine crystalline powder. We will dissolve very little in water and alkali solutions, little - in alcohol.

Release form. Powder, tablets.

Storage. According to the "B" list. In a well-sealed container. Shelf life is 5 years.

Action. Like phthalazole, salmonella are slightly sensitive to it.

Application. For dyspepsia, gastroenterocolitis for the prevention of postoperative complications. Assign enterally in doses (g per animal): for horses -19-20; cattle - 15-25; pigs - 1-5; dairy calves - 2-3; suckling pigs - 0.3-0.5; chickens - 0.2-0.3 twice a day.

Phtazin - Phtazinum.

Flavourless white crystalline powder. Practically insoluble in water and alcohol. Easily soluble in alkali solutions. Release form. Powder, tablets of 0.5 g.

Storage. According to the "B" list. In a dry, dark place. Shelf life is 2 years.

Action. The spectrum of antimicrobial action is similar to that of sulfapyridazine. In the intestine, it gradually decomposes to sulfapyridazine, which is absorbed, therefore the drug acts in the intestinal lumen and is resorptive.

Application. For dysentery, dyspepsia, enterocolitis, coccidiosis, etc. Assign enterally in doses (mg / kg of animal weight): KRS-10-15; calves, lambs -15-20; pigs - 8-12; piglets - 12-16; chickens -30-50 twice a day.

Salazopyridazine - Salazopyridasinum.

Fine crystalline powder, orange... Practically insoluble in water, slightly soluble in alcohol. Contains sulfapyridazine and salicylic acid.

Release form. Powder, tablets of 0.5; suspension 5% in bottles of 250 ml; candles 0.5 g each.

Storage. According to the "B" list. In a cool, dark place. Shelf life is 5 years.

Action. Antimicrobial, anti-inflammatory. In the intestine, the drug disintegrates with the release of sulfapyridazine, which is absorbed and maintains a therapeutic concentration for 12 hours. In addition, 5-aminosalicylic acid is released, which has an anti-inflammatory effect.

Application. The indications are the same as for sulfapyridazine, but are more often used for intestinal pathology. Assign enterally to young animals (calves, piglets, lambs) at a dose of 25-50 mg / kg body weight, to chickens -60-90 mg / kg body weight 2 times a day.

Salazodimetoxin - Salazodimetoxinum.

Orange powder. Odorless, practically insoluble in water and alcohol.

Release form. According to the "B" list. Shelf life is 2 years.

Action and application. Similar to salazopyridazine.

Combined preparations with trimethoprim Co-trimoxazole (bactrim, biseptol, oriprim, etc.) - Co-Trimoxasole.

White crystalline powder, practically insoluble in water and alcohol. Combined preparation containing two active principles: sulfamethoxazole and trimethoprim.

Release form. Tablets containing 400 mg of sulfamethoxazole and 80 mg of trimethoprim; tablets containing 100 and 20 mg each, respectively.

Storage. According to the "B" list. In a dark place.

Action. Bactericidal against gram-positive and gram-negative microorganisms, including bacteria resistant to sulfa drugs. The bactericidal effect is associated with a double blocking effect on the metabolism of bacteria: sulfamethoxazole disrupts the synthesis of dehydrofolic acid, and trimethoprim blocks the next stage of metabolism - the reduction of dehydrofolic acid to the tetrahydrofolic acid necessary for microorganisms. This disrupts the synthesis of pyridine and purine bases of DNA and RNA. After enteral administration, the drug is rapidly absorbed and after 1-3 hours it creates a therapeutic concentration, which is retained in the blood and tissues for about 7 hours.

Application. With pathology of the respiratory tract (bronchitis, bronchopneumonia, pneumonia), urinary system(urethritis, cystitis, pyelitis, pyelonephritis, etc.), gastrointestinal tract, in surgery, etc. Prescribed enterally, more often young animals: calves, piglets, lambs, as well as carnivores, at the rate of 50 mg per 1 kg of weight 3 times in a day.

Trimerazin - Trimerazinum.

White crystalline powder, practically insoluble in water and alcohol. It contains 0.1 sulfamerazine and 0.02 trimethoprim. Release form. Powder in bags of 300 and 100 g; pills. Storage. According to the "B" list. In a dark place. Action. A wide range of antimicrobial action.

Application. For the treatment of young animals, as well as adult pigs with various pathologies of the respiratory, urinary, digestive and other systems. Assign enterally with feed (powder) at the rate of 2.5 g of the drug per 20 kg of feed; poultry with feed 1 kg per 1 kg of feed, tablets at the rate of 1 tablet per 15 kg - 1 time per day.

In the practice of veterinary medicine, other combined sulfonamides with trimethoprim are also used: trimethosul, tribrisen, co-sulfazine, ditrivet-480, sulfaton, co-sumix-plus, trisulmix, etc.

Sulfanilamide preparations- antimicrobial agents that are derivatives of sulfanilic acid.

With the advent of antibiotics and their widespread distribution, sulfonamides, which were previously the main antimicrobial drugs, began to be used much less frequently due to the greater effectiveness of antibiotics, their more choice and better patient tolerance. However, if there are contraindications to the use of antibiotics, sulfa drugs are used.

Doses of sulfa drugs are largely determined by the rate of their elimination from the body.

According to the duration of maintaining the therapeutic concentration in the blood after a single dose, sulfonamides are divided into 4 groups: short-term action (, etc.), action average duration(and others), long-acting (, etc.) and super-long-acting (and others).

Contraindications for use

Individual intolerance to sulfonamides, kidney and liver diseases, diseases of the hematopoietic system.

Side effects

The most frequent side effects arising from the appointment of sulfa drugs are: a feeling of general weakness, headaches, nausea, vomiting, fever, cyanosis. Sometimes liver dysfunctions, agranulocytosis and hemolytic anemia occur. Dysfunction of the kidneys (up to anuria) due to blockage of the crystals of sulfonamides of the urinary tract.

Complications in the treatment of sulfonamides can also manifest as hemorrhagic vasculitis, widespread and fixed scarlet fever and measles erythema, Stevens-Johnson syndrome and Lyell's syndrome. On open areas of the skin, rashes may occur due to photosensitization of the body.

special instructions

The effectiveness of sulfa drugs is reduced if, at the same time, the patient is administered medicines containing the residue of para-aminobenzoic acid (for example).

To prevent renal dysfunction during treatment with sulfa drugs (deposition of sulfonamide crystals in urinary tract) it is imperative to prescribe an abundant alkaline drink during the course of treatment, as well as a clinical study of urine and blood at least 1 time per week.

Properties

Spectrum of action

Sulfanilamide drugs have an antibacterial effect on many gram-positive and gram-negative bacteria, in particular meningococci.

At early termination treatment with sulfanilamide drugs or prescribing them in small, subtherapeutic doses, microorganisms can adapt to them and form sulfonamide-resistant (sulfonamide-resistant) strains.

Pharmacodynamics

The antibacterial effect of sulfonamides is due to the similarity of their structure with (PABA), as a result of which sulfonamide preparations enter into competition with it, blocking the metabolic processes of microorganisms.

Pharmacokinetics

Sulfonamides are excreted mainly through the kidneys, and poorly soluble drugs through the gastrointestinal tract. Some sulfa drugs bind to blood proteins and their excretion is slowed down, which makes it possible to maintain their therapeutic concentration in the blood for a long time.

Karaganda State Medical University

Department of General Pharmacology

Topic: Sulfanilamide preparations.

Completed: Art. group 2085 Savitskaya T.

Checked by: teacher Nikolaeva T.L.

Karaganda 2013

1. Introduction

2.sulfanilamide drugs (pharmacodynamics, pharmacokinetics, contraindications and indications for use, classification)

3. Sulfanilamide preparations. Name. Forms of release, average therapeutic doses, methods of administration.

4.

5. Derivatives of sulfa drugs.

6. Used literature.

Sulfanilamide drugs are synthetic chemotherapeutic agents, derivatives of sulfanilic acid, capable of to a large extent suppress the development of gram-positive and gram-negative bacteria, chlamydia, some protozoa and pathogenic fungi. The first sulfonamide was synthesized in 1908 by P. gel, a graduate of the pharmaceutical faculty of the University of Vienna. However, the medicinal properties of the new chemical compound have not been investigated. In 1932 German chemists of the Far-Benindustri company synthesized red paint, the antimicrobial properties of which were investigated by G. Domagk. He showed that red dye has a pronounced antimicrobial effect in mice infected with hemolytic streptococcus. Proptosil (this is the name given to the red paint) prevented the death of mice, which were injected with a 1000-fold dose of hemolytic streptococcus. Experimental studies had to be confirmed by clinical observation. A dramatic incident in the family of G. Domagka accelerated these observations. His daughter fell ill with a severe form of septicemia with an unfavorable prognosis at the time. Mr. Domagk was forced to give her proptosil, although this substance had not yet been used for treatment. The daughter was saved from certain death. G. Domagk agreed to test prontosil in different clinics in Germany. The scientist received positive reviews from everywhere. The common dye has proven to be an effective antimicrobial agent. Summarizing the experimental, clinical studies, G. Domagk in 1935 published in the magazine "Deutsche medi-cinishe wochenschrifft" an article "Contribution to the chemotherapy of bacterial infections." For the discovery of the medicinal properties of prontosil, G. Domagk received the Nobel Prize in 1938. However, prontosil was patented by Farbenindustry, which had an exclusive right to the drug and established high prices... Employees of the Pasteur Institute in Paris showed that the effective principle of prontosil, or red streptocide, is its white fraction - aminobenzenesulfamide, which was synthesized in 1908 by P. gel. It was streptocide (white streptocide). Since white streptocide was not patented, everyone could use it. The discovery of the medicinal properties of streptocide and other drugs of this group began a new stage in the treatment of patients with infectious diseases - sulfonamide therapy. The product for the synthesis of sulfonamides is sulfanilic acid obtained from PABA. Sulfonamides have one general formula. To date, more than 15,000 derivatives of sulfanilic acid have been synthesized, of which about 40 have been introduced into medical practice as antibacterial agents. Under the influence of sulfa drugs, a bacteriostatic effect is observed in vivo and in vitro only in relation to bacterial cells that multiply. Antimicrobial activity requires the presence of a free amine NH2 group at the 4-position. The spectrum of antimicrobial action of sulfa drugs is quite wide: gram-positive and gram-negative cocci, Escherichia coli, Shigella, cholera vibrio, clostridia, protozoa (causative agents of malaria, pneumocystis, toxoplasma), chlamydia (causative agents of psittacosis), causative agents, diphtheria pathogens, plague fungi (actinomycetes, coccidia), large viruses (causative agents of trachoma, inguinal granulomas). The mechanism of the chemotherapeutic action of sulfa drugs is based on general structure them with para-aminobenzoic acid (PABA), due to which they, competing with it, are attracted to the metabolism of bacteria. By competing with PABA, sulfonamides prevent its use by microorganisms for the synthesis of dihydrofolic acid. Dihydrofolic acid with the participation of reductase is converted into metabolically active coenzyme tetrahydrofolic acid, which is involved in the synthesis of pyrimidine bases of DNA and RNA. The microbial cell has a certain amount of accumulated PABA, therefore, the effect of sulfonamides is observed after a certain latency period, during which 5.5 ± 0.5 generation occurs. Thus, the competitive antagonism between sulfonamides and PABA largely predominates towards PABA. Therefore, for antimicrobial action, it is necessary that the concentration of sulfanilamide in the medium exceeds the concentration of PABA by a factor of 2000 - 5000. Only in this case will microbial cells absorb sulfanilamide instead of PABA. That is why sulfa drugs are administered in rather significant doses. First, 0.5 - 2 g of the drug is prescribed to create a sufficient concentration in the body, and then it is systematically administered in doses that will provide a bacteriostatic concentration. As a result, the synthesis of purine and pyrimidine compounds, nucleotides and nucleic acids is disrupted, which leads to inhibition of the exchange of proteins of microorganisms, disrupts the development and division of their cells. The use of sulfa drugs in reduced doses promotes the formation of strains of microorganisms that are resistant to the action of drugs. The antibacterial effect of sulfa drugs is reduced in the presence of pus, blood, decay products of body tissues, which contain sufficient amounts of PABA and folic acid. Means that, due to their biotransformation in the body, form PABA (for example, novocaine), as well as compounds containing purine and pyrimidine bases, reduce the antibacterial effect of sulfonamides. Conversely, those compounds that are capable of inhibiting dihydrofolic acid reductase are synergists of sulfonamides, since they disrupt the next stage of metabolism - the synthesis of tetrahydrofolic acid with dihydrofolic. An example is, for example, trimethoprim, which is used to create effective antimicrobial agents. The sensitivity of microorganisms to sulfa drugs is due to their ability to synthesize PABA. Nichutlnvish to streptocid hemolytic streptococcus. Microorganisms that do not require PABA (assimilate dihydrofolic acid) are not sensitive to the action of sulfonamides. Staphylococcus, enterococcus, proteus, tularemia causative agent are less sensitive to sulfonamides. In the early years of widespread use, sulfa drugs were highly effective against staphylococcus, meningococcus, gonococcus, etc. Now, most clinical strains of these microorganisms have acquired resistance to the action of sulfa drugs due to the ability to synthesize PABA or as a result of mutation. Most sulfanilamide preparations are obtained on the basis of a streptocide molecule by introducing aliphatic, aromatic and heterocyclic radicals. Substitution of hydrogen at the nitrogen of the sulfanilamide group makes it possible to obtain antimicrobial compounds with aliphatic groups (sulfacil), aromatic radicals (sulfadimezine, etazole, norsulfazole). If we replace hydrogen at the nitrogen of the amine group in the 4-position, the antibacterial activity of the compound decreases significantly. This is due to a decrease in the similarity of sulfonamides to PABA. Phthalazole, for example, acquires antibacterial activity after the reduction of the amino group, which occurs in the intestine. The spectrum of antibacterial action of various sulfanilamide drugs is somewhat different due to their ability to suppress other enzyme systems. Norsulfazole has a thiazole ring, mimics the action of thiamine and inhibits the synthesis of cocarboxylase, which is involved in the decarboxylation of pyruvic acid. According to norsulfazole acts on gonococcus, staphylococcus, intestinal group of bacteria, weaker - on pneumo-, meningo- and especially streptococcus. Sulfadimezin is active against cocci and gram-negative rods, less active against gono-and staphylococcus. Etazole has a moderate bacteriostatic effect on most cocci, active against the intestinal flora. Sulfanilamide is a white powder, slightly soluble in water, soluble in aqueous solutions of bases. The choice of sulfa drugs is determined by the properties of the pathogen, the spectrum of antimicrobial action, as well as the characteristics of pharmacokinetics. Classification. Depending on the characteristics of pharmacokinetics (absorption in the gastrointestinal tract and the duration of excretion from the body) sulfa drugs are divided into the following groups: I. Drugs that are well absorbed from digestive tract, in connection with which they are prescribed for systemic treatment of diseases caused by sensitive microorganisms. T1 / 2 of these drugs in the blood is different, so they can be divided into separate subgroups. 1. Preparations

short-term action from T1 / 2 to 10 hours (etazole, norsulfazole, sulfadimezin). they are prescribed 4-6 times a day, the daily dose is 4-6 g, the course dose is 20-30 g. 2. Drugs with an average duration of action TU / and 10-24 hours (sulfazine, methylsulfazine). they are prescribed 1-3 g per day 2 times; course dose of 10 - 15 g. Preparations of short and medium duration of action are used mainly in acute infectious processes. 3. Long-acting drugs with T1 / 2 more than 24 hours (sulfapyridazine, sulfadimethoxine, sulfamonodimethox-son). Prescribe the first days 1-2 g, then 0.5 - 1 g 1 time per day. 4. Drugs Increased action with T, / 2 60 - 120 h (sulfalene). Sulfalene is prescribed in a dose of 1 g of the first day, then 2 g once a week or 0.2 g per 30 minutes before meals, daily for chronic diseases. II. Drugs that are practically not absorbed in the alimentary canal (phtazin, phthalazol, sulgin) are prescribed for colitis, enterocolitis only inside. These drugs form a significant concentration of the active substance in the intestine (phthalazole decomposes to form norsulfazole). With prolonged use, sulfonamides suppress saprophytic microflora, which plays a significant role in the synthesis of vitamin K2, an imbalance of which can lead to hypoprothrombinemia. III. Topical preparations (streptocid, etazole, sodium sulfacyl). Streptocide, etazole as the smallest powders are used for powders, in the form of liniment, sodium sulfacyl - for eye drops, which penetrate well into all eye tissues. Sulfonamides are found in many ointments. IV. Salazosulfonamides - nitrogen compounds of sulfonamides with salicylic acid (salazosulfapyridine, salazopyridazine, salazodimethoxin) have antibacterial and anti-inflammatory properties. In the intestine, they break down with the release of active sulfonamides and 5-aminosalicylic acid. Prescribed mainly to patients with ulcerative colitis, 0.5 - 1 g 4 times a day. V. Combined preparations of sulfonamides with trimethoprim (bactrim - biseptol). Sulfonamides, which are well absorbed into the blood, are able to form complexes with plasma albumin, and partially circulate in a free state. The connection with proteins is unstable. The degree of bond increases with an increase in the hydrophobicity of the molecules. Acetylated forms are more associated with proteins than free compounds. With a decrease in the level of protein in the blood plasma, the content of the free fraction of sulfonamides in it significantly increases. From the blood, sulfonamides penetrate well into various fabrics and body fluids. Sulfapyridazine has the highest permeability. Sulfonamides are found in significant quantities in the kidneys, liver, lungs, skin, in smaller quantities in adipose tissue, and in bones they are not detected. The concentration of sulfonamide in the pleural, peritoneal, synovial and other fluids is 50 - 80% of it in the blood. The process of inflammation greatly facilitates the penetration of sulfonamides through the blood-brain barrier into the brain tissue. Quite easily, they pass through the placenta, are determined in saliva, sweat, in the mother's milk, in the tissues of the fetus. The biotransformation of sulfonamides is different for different drugs. Sulfonamides in the body are partially acetylated, oxidized, form inactive glucaronides or do not change. Acetylation in the liver and depends not only on the drug, but also on the acetylative ability of the liver. Etazole, urosulfan are less acetylated, and sulfidine, streptocid, norsulfazole, sulfadimezin are more acetylated. With acetylation, the activity of the drug is lost and its toxicity increases. Acetylated sulfonamides have low solubility and in an acidic environment can form calculi that can precipitate (crystalluria), injure or even block the renal tubules. Drugs that are slightly acetylated are excreted from the body in active form and have significant antimicrobial activity in the urinary tract (etazole, urosulfan). The formation of inactive glucuronides is characteristic of sulfadimethoxine. Glucuronides are highly soluble and do not precipitate. Sulfonamide metabolites have no antimicrobial activity. Excreted by the kidneys by glomerular filtration and partly tubular secretion. Long-term and increased-action drugs are little inactivated in the body and are reabsorbed in significant quantities in the tubules, which explains the duration of their action. Side effects when using sulfa drugs can be different and dangerous, but rarely happens with proper treatment. Complications are common for the entire group: allergic reactions, effects on the blood, and the like. They are caused by an overdose of drugs or hypersensitivity of the patient. Overdose is more common in children and the elderly, especially after 10-14 days of treatment with long-acting drugs. Signs of intoxication (nausea, vomiting, dizziness), damage to the epithelium of the renal tubules, the formation of crystals in them (oliguria, protein, erythrocytes in the urine), hepatitis may develop. To prevent the formation of crystals in the urinary tract, a significant amount of alkaline drink (up to 3 liters) or sodium hydrogencarbonate, mineral alkaline waters should be prescribed. Prescribing sulfa drugs requires caution in kidney and liver diseases. Complications associated with increased sensitivity of the body can be of an allergic nature (rash, dermatitis, exudative erythema, serum sickness, vascular damage, sometimes anaphylactic shock). There are blood lesions - hemolytic anemia, leukopenia, agranulocytosis, rarely - aplastic anemia, a depressing effect on the central nervous system. Indications for the use of sulfonamides- diseases caused by microorganisms sensitive to them. Sulfonamides, well absorbed, are used for infectious diseases of the urinary system, biliary tract, ear, throat, nose, lungs, patients are prescribed trachoma, actinomycosis, toxoplasmosis, malaria, meningitis, etc. If the pathogen is sensitive to the drug, the therapeutic effect is manifested in within 1 - 3 days: signs of infectious toxicosis (fever, impaired blood circulation, respiration) disappear, the general condition improves. Sulfonamides, poorly absorbed, are used for intestinal infections (enteritis, colitis, dysentery, typhoid fever, etc.). The antibacterial activity of sulfa drugs is much weaker than antibiotics. Taking this into account, and also taking into account the increase in the number of resistant strains, in recent years, sulfa drugs have been used less. they can be given along with antibiotics. To prevent the formation of sulfanil-midostiic strains of microorganisms, combinations of sulfa drugs with other chemotherapeutic agents are used. For example, the combined preparation bactrim (biseptol, trimoxazole) contains 5 parts of the sulfa drug sulfamethoxazole and 1 part of trimethoprim. Sulfamethoxazole and trimethoprim each separately carry out a bacteriostatic effect. Simultaneous use in the form of a combined preparation enhances the antimicrobial effect and provides a high bactericidal effect even against microorganisms resistant to sulfa drugs. Sulfamethoxazole blocks the biosynthesis of the acid of dihydrofolic bacteria at the PABA level. Trimethoprim blocks the next phase of metabolism - the reduction of dihydrofolic acid to tetrahydrofolic acid by inhibition of dihydrofolic acid reductase. Trimethoprim is 5,000 - 10,000 times more related to microorganism dihydrofelate reductase than with functionally analogous mammalian reductases. Trimethoprim has an antimicrobial spectrum similar to other sulfonamides, but it is 20-100 times more active. Bactrim inhibits the development of most (about 95%) strains of staphylococcus, pyogenic and green streptococcus, different types protea, Escherichia coli, Salmonella, Shigella. Resistance to Bactrim develops rather slowly. When administered orally, the maximum concentration in the blood is determined after 1 to 3 hours and lasts for 7 hours. T1 / 2 of trimethoprim is 16 hours, sulfamethoxazole - 10 hours. In the presence of sulfamethoxazole, trimethoprim in a small amount binds to plasma proteins and quickly enters the tissues, where the concentration exceeds the concentration in the blood serum. Sulfamethoxazole binds up to 65% to blood plasma albumin. Sulfamethoxazole and trimethoprim are found in significant quantities in bile, sputum, mother's milk, amniotic fluid, eye media, bone marrow, intracellularly. During the day, 60% of trimethoprim and 25-50% of sulfamethoxazole are excreted in the urine, and more than 60% is excreted unchanged. Indications. Bactrim is prescribed for infectious diseases of the genitourinary system, biliary tract, ear, throat, nose, upper respiratory tract, lungs, for the prevention of meningitis in groups where there are carriers of meningococcus, for the treatment of infectious diseases caused by hemophilus influenzae, patients with brucellosis, typhoid fever , cholera, etc. Therapeutic doses for adults - 1 g (2 tab.) Twice a day for 9-14 days and then 0.5 g twice a day in case of longer treatment. Contraindications Sulfanilamide drugs, especially bactrim, are contraindicated in pregnant women due to the possibility of impaired fetal development, for mothers, since sulfonamides that come with milk can cause the child to develop methemoglobinemia. It should not be prescribed to children with hyper-bilirubinemia: the risk of bilirubin encephalopathy (especially in children in the first 2 months of life), as well as to children with a deficiency of glucose-6-phosphate dehydrogenase in erythrocytes. Side effects are rare. These are dyspeptic symptoms in 3-4% of patients (nausea, anorexia, diarrhea, vomiting), skin rash, urticaria, itching (in 3-5% of patients). Sometimes there are also severe skin-allergic reactions (Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis, etc.). Occasionally, leukopenia, agranulocytosis, thrombocytopenia, eosinophilia may develop. Possible megablastic reaction of the bone marrow in pregnant women with alcoholism (eliminated by folic acid). This reaction occurs as a hypersensitivity and is usually a contraindication to the appointment. Possible allergy cross-reactions in persons sensitized to sulfonamides. Cases of reproductive dysfunction in men are described. Sometimes candidiasis develops oral cavity and dysbiosis, especially in seriously ill and elderly people. Sulfanilamide preparations. Name. Forms of release, average therapeutic doses, methods of administration.

Sulfadimezin Sulfadimezinum Etazole Aethazolum Sulfacil sodium Sulfacylum-natrium Sulfadimethoxin Sulfadimethoxinum Sul lfap irndazin Sulfapyridazinum Phthalazol Phthalazolum Biseptol-480 (120; 240; 960 g) Biseptol-480 (120; 240; 960) tablets : 1st intake - 2 g, then take but 1 g 4 - 6 times a day, with alkaline water. Children - 0.1 g / kg - 1st dose, then 0.025 g / kg every 4 - 6, or 4 - 8 hours. Powder tablets of 0.25 and 0.5 g. Inside, 1 g 4-6 times a day. In the wound - up to 5 g of the drug. Powder in ampoules of 5 ml of 30% solution; in vials of 5 and 10 ml ZO% difference; eye drops - a dropper tube with a 20% solution of 1.5 ml. Inside powder, 0.5-1 g 3 - 5 times a day, children 0.1 - 0.5 g 3-5 times a day, externally ZO% ointment. Powder tablets of 0.2 and 0.5 g. Inside the 1st day - 1-2 g, then 0.5 - 1 g per day. Children: 1st day - 25 mg / kg, then 12.5 mg / kg. Powder tablets, 0.5 g. Inside the 1st day-1 g, then 0.5 g; severe infections - 1st day - 1 g 2 times a day, then 1 -0.5 g 1 time per day Powder tablets but 0.5 g Inside the 1st and 2nd day, 6 g per day, 3 th and 4 th day - 4 g, 5 th and 6 th day - 3 g. Tablets, 20 pcs. Inside, 2 tablets 3 times a day after meals.

Pharmacology: Synthetic antimicrobial agents of various chemical structures.

This group includes various chemical compounds synthesized later than sulfa drugs, which differ from them and antibiotics in structure, mechanism and spectrum of antibacterial action. All of them have high antibacterial activity and a predominant effect on pathogens. intestinal infections and diseases of the urinary tract, including infections that are difficult to treat with other antimicrobial agents. The drugs presented in this section are represented by the following chemical groups 1. Quinolone derivatives of the 1st generation, derivatives of 8-hydroxyquinoline (nitroxoline, chlorquinaldone, quiniophone, intetrix). 2. Quinolone derivatives of the second generation, naphthyridine derivatives (nalidixic acid, oxolinium acid, pipemidium acid). 3. Quinolone derivatives of the third generation, fluoroquinolones (ciprofloxacin, ofloxacin, norfloxacin, pefloxacin, lomefloxacin, sparfloxacin). 4. Quinoxaline derivatives (quinoxidine, dioxidine). 5. Derivatives of nitrofuran (furacilin, furazolidone, furazolin, furadonin, fura-gon, soluble furagin). 6. Derivatives of imidazole (metronidazole). Quinoline derivatives (8-hydroxyquinoline and 4-quinolones). The drugs of this group are represented by halogen (nitroxoline, mexazand mexaform, quiniophone) and nitro derivatives. They suppress the vital activity of microorganisms, forming complex compounds with metal ions, reducing their enzymatic processes and functional activity. Pipemidic acid, for example, selectively inhibits the synthesis of bacterial DNA, has a wide spectrum of antimicrobial action, which spreads to gram-negative bacteria, causative agents of protozoal diseases (dysentery amoeba, lamblia, Trichomonas, balantidia). Drugs in this group are effective against antibiotic-resistant bacteria due to their lack of cross-resistance. The effect of the drugs is determined by the varying degrees of absorption in the digestive tract: enteroseptol and intestopan are poorly absorbed, which contributes to the creation of a high concentration in the intestine and is used for infectious intestinal diseases. Nitroxoline, pipemidium and oxolinium acids are well absorbed and excreted by the kidneys unchanged, which provides an antibacterial effect in the urinary tract. Chlorquinaldone has antibacterial, protimycosis, antiprotozoal activity. The greatest activity is shown by gram-positive and some gram-negative bacteria. It is prescribed for intestinal infectious diseases (dysentery, salmonellosis, foodborne diseases, infections caused by staphylococcus, proteus, enterobacteria), as well as for dysbiosis. In terms of chemical structure, Intetrix is ​​close to Nitroxoline and Chlorquinaldone, and contains a surfactant. Possesses antimicrobial, antiamebna, antimycotic action. Prescribed in cases of acute infectious diarrhea, dysbiosis, amebiasis. Hiniophone is not widely used. Prescribed for amoebic dysentery. Prescribing drugs of this group inside, it should be borne in mind that in the case of prolonged use of them, as well as in people with increased sensitivity to them, side effects may occur: peripheral neuritis, myelopathy, damage to the optic nerve, impaired liver and kidney function, allergic reactions. Therefore, despite their significant antibacterial activity, their treatment is very limited. For infectious diseases of the intestine, Chlorquinaldol and Intestopan are used, for the urinary tract, nitroxoline. Nitroxoline (5-NOK, uritrol -