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Sulfonamides are broad-spectrum bacteriostatic drugs, competitive antagonists of para-aminobenzoic acid (PABA), which is necessary for most microorganisms to synthesize folic acid. They bind pterin and inhibit folate synthetase, resulting in a bacteriostatic effect.

The antimicrobial properties of sulfanilamide preparations are significantly (20-100 times) potentiated and approach in severity to bactericidal action when combined with trimethoprim, which is a specific inhibitor of bacterial folate reductase. It should be taken into account that in environments with a high content of PABA, for example, in the focus of purulent fusion of tissues, the antimicrobial activity of sulfonamides is sharply reduced.

The spectrum of antimicrobial activity of sulfa drugs includes:

- gram-positive microorganisms (streptococci, staphylococci, clostridia, anthrax, actinomycetes). It should be noted that at present a significant number of strains of staphylococci have acquired resistance to these drugs;
- Gram-negative microorganisms (E. coli, Shigella, Salmonella, Haemophilus influenzae, bacteroids, Vibrio cholerae, meningococci, gonococci, chlamydia - causative agents of urogenital infections);
- protozoa (plasmodia malaria, toxoplasma, trypanosomes).

The spectrum of action of drugs combined with trimethoprim approaches the spectrum of action of the antibiotic chloramphenicol. Up to 50-90% of strains of staphylococci, Escherichia coli, enterobacteria, salmonella, shigella, pseudomonads are sensitive to them.

When taken systemically, sulfa drugs can cause dyspeptic symptoms (nausea, vomiting), headache, allergic reactions (rash, dermatitis, fever). With prolonged use, the development of leukopenia, thrombocytopenia, agranulocytosis is possible. probable side effect is the precipitation of crystals in the kidneys (especially for the drugs sulfadimezin, norsulfazol, sulfapyridazine, sulfamonometoxin). The danger of crystalluria is greatly reduced by using an alkaline drink. Therefore, it is advisable to simultaneously prescribe alkaline mineral waters or sodium bicarbonate (up to 5-10 g per day).

The toxicity of preparations combined with trimethoprim is higher than that of monocomponent agents, especially in folate-deficient conditions (diseases of the hematopoietic organs, pregnancy, old age).

General classification of sulfa drugs

Drugs well absorbed from the gastrointestinal tract:

A) short-term action: streptocide (sulfanilamide, white streptocide); sulfadimezin (sulfadimidine); etazol (sulfaetidol); norsulfazol (sulfathiazole); urosulfan (sulfa-carbamide);

B) medium duration of action: sulfazine (sulfadiazine); sulfamethoxazole;

C) long-acting: sulfadimethoxine; sulfapyridazine (sulfamethoxypyridazine); sulphamonomethoxin;

D) ultra-long action: sulfalene; sulfalene-meglumine.

Drugs that are poorly absorbed from the gastrointestinal tract (acting in the intestinal lumen): ftalazol (phthalyl-sulfathiazole); sulgin (sulfaguanidine); phthazine (phthalylsulfapyridazine); salazopyridazine (salazodin); salazosulfapyridine (sulfasalazine, salazopyrin).

Topical preparations: sulfacyl sodium (sulfaietamide); silver sulfadiazine (dermazin, flamazin).

IV. Combined sulfa drugs:

A) preparations containing sulfamethoxazole and trimethoprim: Co-trimoxazole (bactrim, biseptol, berlocid, septrin, groseptol);

B) preparations containing sulfadimezin and trimethoprim: proteseptil (potesetta);

C) preparations containing sulfamonomethoxin and trimethoprim: sulfatone.

In dentistry, sulfanilamide drugs are used for various inflammatory diseases of the pulp, periodontium, and for the prevention of infectious complications after surgery. These indications include:

— pharmacotherapy of deep caries. Streptocid and norsulfazol, together with antibiotics and enzymes, are part of the pastes for covering the bottom of the carious cavity before filling;

- pharmacotherapy of pulpitis with a biological method of treatment;

- covering the pulp stump during amputation in the surgical treatment of pulpitis (norsulfazol or streptocide in combination with antibiotics monomycin or neomycin);

- acute periodontitis (30% solution of albucid together with antibiotics and antiseptics);

- periodontitis of milk teeth (pastes with norsulfazole, astringents and enzyme preparations for filling the root canals of milk teeth);

- treatment of acute odontogenic infection (locally - 30% sodium sulfacyl solution; systemically - any sulfanilamide well absorbed in the intestine, for 5-7 days);

- treatment of periodontal disease (pastes and emulsions with sulfonamides for the treatment of pathological periodontal pockets);

- aphthous and ulcerative stomatitis (30% solution of sodium sulfacyl for irrigation of aphthae and ulcerative surface).

Ingalipt(Inhalyptum).

pharmachologic effect: is a combined preparation containing soluble streptocide - 0.75 g, thymol, eucalyptus oil and peppermint oil - 0.015 g each, ethyl alcohol 95% - 1.8 g, sugar - 1.5 g, glycerin - 2.1 g , tween-80 - 0.9 g, water - up to 30 ml. It has an antiseptic and anti-inflammatory effect.

Indications: used for infectious and inflammatory lesions of the oral mucosa and periodontal tissues (aphthous and ulcerative stomatitis, ulcerative necrotic gingivitis).

Mode of application: irrigation of the oral mucosa. Before irrigation, it is recommended to rinse your mouth, remove plaque from erosive surfaces. In the oral cavity should be held for 5-7 minutes; irrigation to produce 34 times a day.

Side effect: Allergic reactions are possible.

Release form: aerosol cans containing 30 ml of the drug.

Storage conditions: at temperatures from +3 to +35°C.

Co-trimoxazole(Co-Trimoxazole). Synonyms: Bactrim (Bactrim), Sinersul (Sinersul), Biseptol (Biseptolitm), Berlocid (Veglocid), Groseptol (Groseptol), Septrin (Septrin), Sumetrolim (Sumetrolim).

pharmachologic effect: is a combined preparation containing sulfamethoxazole and trimethoprim in a 5:1 ratio. Both drugs have a bacteriostatic effect. In combination, they provide a pronounced bactericidal effect against gram-positive and gram-negative microbes, including those resistant to sulfanilamide preparations. The drug is effective against coccal flora, but ineffective against Pseudomonas aeruginosa, spirochetes.

Indications: used for surgical infections.

Mode of application: appoint inside. A tablet for adults contains 400 mg of sulfamethoxazole and 80 mg of trimethoprim, for children - 100 and 20 mg, respectively. Recommended dosage: adults and children over 12 years old, 2 tablets 2 times a day after meals, for chronic infections - 1 tablet 2 times a day. Children from 2 to 5 years old are recommended for a single dose of 2 tablets (0.12 g each), 5-12 years old - 4 tablets 2 times a day. The course of treatment is 5-14 days.

Side effect: possible nausea, vomiting, diarrhea, allergic reactions, nephropathy, leukopenia, agranulocytosis. : see Streptocide.

Contraindications: similar to those of long-acting sulfa drugs. Limit use in children younger age. Do not use in pregnant women, with diseases of the hematopoietic system.

Release form: tablets of 0.12 and 0.48 g, in a package of 20 pcs (each tablet contains 100 mg of sulfamethoxazole and 20 mg of trimethoprim or 400 mg and 80 mg, respectively); forte tablets, in a package of 10 pcs (content of sulfamethoxazole and trimethoprim 800 mg and 160 mg); 100 ml syrup in a vial complete with a dosing spoon (5 ml of syrup contains 200 mg of sulfamethoxazole and 40 mg of trimethoprim).

Storage conditions: list B.

Sulfadimethoxine(Sulfadimethoxin).

According to the pharmacological action, Indications m, method of administration and side effects similar to sulfapyridazine.

Interaction with other drugs: can be combined with antibiotics of the penicillin group, erythromycin. See: Streptocid, Norsulfazol, Sulfapyridazine.

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

Storage conditions: list B.

Sulfanilamide(Sulfanilamide). Synonym: Streptocide (Streptocidum).

pharmachologic effect: is an antimicrobial drug that is active against cocci (streptococcus, meningococcus, pneumococcus, gonococcus), as well as coli coli. Recently, many types of staphylococci are resistant.

Indications: in dentistry, it is used topically in the treatment of infected ulcers of the oral mucosa or infected wounds of the maxillofacial region.

Mode of application: in dentistry, they are mainly used topically in the form of a powder, ointment or liniment. Apply to the affected surface or injected into the wound 5-15 g of sterile powder. It is rarely used systemically.

Side effect: when applied topically in conditions of sensitization, allergic reactions are possible. With systemic use: nausea, vomiting, diarrhea, allergic skin reactions, impaired leukopoiesis.

Interaction with other drugs: joint application with acids, hexamethylenetetramine, adrenaline solution is impractical, since they are chemically incompatible. When combined with esters of para-aminobenzoic acid (novocaine, anestezin, dikain), the antibacterial activity of streptocide decreases by a competitive mechanism.

Contraindications: for topical use - a known allergy to sulfonamides. For systemic use - hypersensitivity to sulfonamides, pregnancy, lactation, blood diseases. Systemically should be used with caution in diseases of the liver, kidneys (requires dynamic monitoring of liver and kidney function).

Release form: powder, ointment 5 and 10% in glass jars, liniment 5% in glass jars or tubes.

Storage conditions: in a cool, dark place.

Sulfapyridazine(Sulfapyridazinum), Synonym: Sulfamethoxypyridazine.

pharmachologic effect: long-acting sulfanilamide drug with antibacterial activity against gram-positive (streptococcus, pneumococcus, staphylococcus, enterococcus) and gram-negative (E. coli, Proteus, etc.) microbes, some protozoa. Does not affect bacteria resistant to other sulfonamides.

Indications: used for acute purulent-inflammatory lesions of the maxillofacial region, for the prevention of infectious complications after surgery.

Mode of application: appoint inside. Doses for adults are at the first dose of 1-2 g, depending on the severity of the disease, in the following days - 0.5-1 g. The interval between doses is 24 hours. The average duration of treatment is 5-7 days. The drug is used within 2-3 days after the temperature drops. For children under 13 years of age, the initial dose is 25 mg / kg of body weight, in the following days - 12.5 mg / kg.

Side effect: in isolated cases, dyspeptic symptoms, allergic reactions are possible.

Interaction with other drugs: when taken simultaneously with erythromycin, lincomycin, novobiocin, fusidine, tetracycline, antibacterial activity is mutually enhanced, the spectrum of action is expanded; with rifampicin, streptomycin, monomycin, kanamycin, gentamicin, nitroxylin - the antibacterial effect of the drug does not change; sometimes there is antagonism with nevigramon; with ristomycin, chloramphenicol, nitrofurans - a decrease in the total effect. In combination with antimalarial drugs, it has a pronounced effect on drug-resistant forms of malaria pathogens.

Release form: powder, tablets of 0.5 g.

Storage conditions: in a place protected from light.

Sulfathiazole(Sulfathiazole). Synonym: Norsulfazol (Norsulfasolum).

pharmachologic effect: has antibacterial properties against hemolytic streptococcus, pneumococcus, staphylococcus, gonococcus, Escherichia coli.

Indications: used for purulent-inflammatory diseases of the maxillofacial region, for the prevention and treatment of inflammatory diseases of periodontal tissues, the treatment of complicated forms of caries.

Mode of application: prescribed externally for applications on the mucous membrane and as part of gum dressings, pastes for the treatment of pulpitis and periodontitis. Inside taken in acute infectious and inflammatory diseases.

With staphylococcal infections, adults are prescribed 2 g for the first dose, in severe cases - up to 3-4 g, then 1 g every 6-8 hours. The duration of treatment is 3-6 days. For children, single doses are: from 4 months to 2 years - 0.1-0.25 g. 2-5 years - 0.3-0.4 g, 6-12 years - 0.4-0.5 g. At the first dose, give a double dose.

Side effect: possible nausea, vomiting, allergic reactions, leukopenia, neuritis, crystalluria.

Interaction with other drugs: when combined with PAS and barbiturates, the activity of the drug increases, with salicylates - activity and toxicity, with methotrexate and diphenin - toxicity, with phenacetin - hemolytic properties, with chloramphenicol - the possibility of developing agranulocytosis increases, with nitrofuran - the risk of anemia and methemoglobinemia, with anticoagulants indirect action increases the effect of the latter, with oxacillin - the activity of the antibiotic decreases. Incompatible with salts of iron and heavy metals. See also Sulfanilamide.

Contraindications: do not use with increased individual sensitivity to sulfonamides, diseases of the blood system, diffuse toxic goiter, kidney disease, acute hepatitis, intestinal obstruction.

Release form: powder, tablets of 0.25 and 0.5 g.

Storage conditions: list B.

Sulfacyl sodium(Sulfacilum-natrium). Synonyms: Albucid (Albucid-natricLim), Sulfacetamid.

pharmachologic effect: the drug is effective against streptococci, gonococci, pneumococci, Escherichia coli.

Indications: in dentistry, it is used topically for the treatment of infected wounds, infectious and inflammatory lesions of the oral mucosa and periodontal tissues.

Mode of application: used in the form of a powder - 5-6 times a day before epithelization, in the form of a solution - for washing periodontal pockets.

Side effect: rare. Possible local irritant effect at high concentrations.

Contraindications: do not prescribe if there is a history of allergic reactions to sulfa drugs.

Release form: powder; 30% solution in vials; ointment 30%.

Storage conditions: store the powder in a place protected from light. Solutions and ointment - in a cool, dark place. List B (except ointment).

Dentist's guide to medicines
Edited by Honored Scientist of the Russian Federation, Academician of the Russian Academy of Medical Sciences, Professor Yu. D. Ignatov

The sulfonamides familiar to people have long established themselves, as they appeared even before the history of the discovery of penicillin. To date, these drugs in pharmacology have partially lost their significance, since they are inferior to modern medicines in terms of efficiency. However, in the treatment of certain pathologies, they are indispensable.

Sulfonamides (sulfonamides) are synthetic antimicrobial drugs that are derivatives of sulfanilic acid (aminobenzenesulfamide). Sulfanilamide sodium inhibits the vital activity of cocci and rods, affects nocardia, malaria, plasmodia, proteus, chlamydia, toxoplasma, has a bacteriostatic effect. Sulfanilamide preparations are drugs that are prescribed for the treatment of diseases caused by pathogens resistant to antibiotics.

Classification of sulfa drugs

In their activity, sulfa drugs are inferior to antibiotics (not to be confused with sulfonanilide). These drugs have a high toxicity, so they have a limited range of indications. The classification of sulfa drugs is divided into 4 groups, depending on the pharmacokinetics and properties:

1. Sulfonamides, rapidly absorbed from the gastrointestinal tract. They are prescribed for systemic treatment of infections caused by susceptible microorganisms: Etazol, Sulfadimetoksin, Sulfametizol, Sulfadimidine (Sulfadimezin), Sulfacarbamide.
2. Sulfonamides, incompletely or slowly absorbed. They create a high concentration in the large and small intestines: Sulgin, Ftalazol, Phtazin. Etazol sodium
3. topical sulfonamides. Well proven in eye therapy: Sulfacyl sodium (Albucid, Sulfacetamide), Silver sulfadiazine (Dermazin), Mafenide acetate ointment 10%, Streptocide ointment 10%.
4. Salazosulfanamides. This classification of compounds of sulfonamides with salicylic acid: Sulfasalazine, Salazomethoxin.

The mechanism of action of sulfa drugs

The choice of a drug for treating a patient depends on the properties of the pathogen, because the mechanism of action of sulfonamides is to block sensitive microorganisms in the cells of folic acid synthesis. For this reason, some drugs, for example, Novocaine or Methionomixin, are incompatible with them, as they weaken their effect. The key principle of action of sulfonamides is a violation of the metabolism of microorganisms, the suppression of their reproduction and growth.

Indications for the use of sulfonamides

Depending on the structure, sulfide preparations have a common formula, but unequal pharmacokinetics. There are dosage forms for intravenous administration: Sodium Sulfacetamide, Streptocide. Some drugs are administered intramuscularly: Sulfalen, Sulfadoxin. Combination drugs are used in both ways. For children, sulfonamides are used topically or in tablets: Co-trimoxazole-Rivofarm, Cotrifarm. Indications for the use of sulfonamides:

• folliculitis, acne vulgaris, erysipelas;
• impetigo;
• burns 1 and 2 degrees;
• pyoderma, carbuncles, boils;
• purulent-inflammatory processes on the skin;
• infected wounds of various origins;
• tonsillitis;
• bronchitis;
• eye diseases.

List of sulfa drugs

According to the circulation period, antibiotics sulfonamides are divided into: short, medium, long-term and extra-long exposure. It is not possible to list all drugs, so this table presents long-acting sulfonamides used to treat many bacteria:

Name		Indications
	silver sulfadiazine	infected burns and superficial wounds
Argosulfan	silver sulfadiazine	burns of any etiology, minor injuries, trophic ulcers
norsulfazol	norsulfazole	pathologies caused by cocci, including gonorrhea, pneumonia, dysentery
	sulfamethoxazole	infections of the urinary canal, respiratory tract, soft tissues, skin
Pyrimethamine	pyrimethamine	toxoplasmosis, malaria, primary polycythemia
Prontosil (Red streptocide)	sulfanilamide	streptococcal pneumonia, puerperal sepsis, erysipelas

Combined sulfa drug

Time does not stand still, and many strains of microbes have mutated and adapted. Doctors found new way fight bacteria - they created a combined sulfanilamide drug, in which antibiotics are combined with trimethoprim. The list of such sulfo drugs:

Titles		Indications
	sulfamethoxazole, trimethoprim	gastrointestinal infections, uncomplicated gonorrhea and other infectious pathologies.
Berlocid	sulfamethoxazole, trimethoprim	chronic or acute bronchitis lung abscess, cystitis bacterial diarrhea and others
Duo-Septol	sulfamethoxazole, trimethoprim	broad spectrum antibacterial, antiprotozoal, bactericidal agent
	sulfamethoxazole, trimethoprim	typhoid fever, acute brucellosis, brain abscess, inguinal granuloma, prostatitis and others

Sulfanilamide preparations for children

Since these drugs are broad-spectrum drugs, they are also used in pediatrics. Sulfanilamide preparations for children are available in tablets, granules, ointments and injection solutions. List of medicines:

Name		Application
	sulfamethoxazole, trimethoprim	from 6 years: gastroenteritis, pneumonia, wound infections, acne
Etazola tablets	sulfaetidol	from 1 year: pneumonia, bronchitis, tonsillitis, peritonitis, erysipelas
Sulfargin	silver sulfadiazine	from 1 year: non-healing wounds, bedsores, burns, ulcers
trimezol	co-trimoxazole	from 6 years: infections of the respiratory tract, genitourinary system, skin pathologies

Instructions for use of sulfonamides

Antibacterial agents are prescribed, both inside and locally. Instructions for the use of sulfonamides states that children will use the drug: up to a year, 0.05 g, from 2 to 5 years - 0.3 g, from 6 to 12 years - 0.6 g for the entire intake. Adults take 5-6 times / day for 0.6-1.2 g. The duration of treatment depends on the severity of the pathology and is prescribed by a doctor. According to the annotation, the course is no more than 7 days. Any sulfa drug should be taken with an alkaline liquid and foods that contain sulfur to maintain the urine reaction and prevent crystallization.

Side effects of sulfa drugs

With prolonged or uncontrolled use, side effects of sulfonamides may occur. These are allergic reactions, nausea, dizziness, headaches, vomiting. With systemic absorption, sulfo drugs can pass through the placenta and then be found in the blood of the fetus, causing toxic effects. For this reason, the safety of the use of drugs during pregnancy is questionable. The doctor should take into account such a chemotherapeutic effect when prescribing them to pregnant women and during lactation. A contraindication to the use of sulfonamides is:

• hypersensitivity to the main component;
• anemia;
• porphyria;
• liver or kidney failure;
• pathology of the hematopoietic system;
• azotemia.

The price of sulfa drugs

Medicines of this group are not a problem to buy in an online store or pharmacy. The difference in cost will be noticeable if you order several drugs from the catalog on the Internet at once. If you buy a medicine in a single version, you will have to pay extra for delivery. Domestically produced sulfonamides will be inexpensive, while imported drugs are much more expensive. Approximate price for sulfa drugs:

Video: what are sulfonamides

Sulfanilamide drugs - a list. The mechanism of action of sulfonamides, use and contraindications - all about medicines and health on the site

Sulfanilamide preparations(synonymous with sulfonamides) - synthetic broad-spectrum chemotherapeutic agents from the group of derivatives of sulfanilic acid amide (sulfanilamide).

Streptococci are sensitive to sulfanilamide preparations, and, diplococci (gonococci, meningococci, pneumococci), intestinal, dysenteria, diphtheria and anthrax sticks, brucella, cholera vibrions, actinomycetes, chlamydia (pathogens of trachomas, ornithosis, etc.), as well as pathogens) anaerobic infection ( clostridia), some protozoal infections (malaria, a). Besides, separate activators of deep ov (nocardin, actinomycetes) are sensitive to S. of the item. Some S. items (sulfadimethoxine, sulfapyridazine, sulfalene) are active against mycobacteria leprosy (see. Anti-leprosy drugs ). Salmonella, Pseudomonas aeruginosa, mycobacterium tuberculosis, spirochetes, leptospira, and viruses are among the items resistant to S.. S.'s microorganisms, sensitive to them, in concentrations in which they accumulate in the body in therapeutic doses, act bacteriostatically.

The mechanism of the antimicrobial action of S. p. is due to the fact that they block the synthesis of dihydrofolic acid at the stage of formation of dihydropteroic acid from dihydropteridine and para-aminobenzoic acid (PABA) with the participation of the enzyme dihydropteroate synthetase (dihydrofolate synthetase). It is believed that the violation of the synthesis of dihydropteroic acid occurs primarily as a result of the inclusion of S. p. instead of PABA as a substrate for dihydropteroate synthetase, tk. according to the chemical structure of S. p., they are similar to PABA. As a result, the formation of analogues of dihydrofolic acid, which do not have its inherent biological activity, occurs. In addition, when S. p. interacts with dihydropteridine in the presence of ATP and magnesium ions, an intermediate metabolite is formed that inhibits dihydropteroate synthetase, which leads to inhibition of the formation of dihydrofolic acid. It is also possible that S. p. prevent the inclusion of dihydropteridine in the synthesis of dihydrofolic acid. Ultimately, the violation of the formation of dihydrofolic acid under the influence of S. p. leads to a decrease in the formation of tetrahydrofolic acid and the resulting inhibition of nucleotide biosynthesis and a delay in the development and reproduction of microorganisms. These features of the mechanism of action explain the fact that only those microorganisms in which the process of dihydrofolic acid synthesis occurs are sensitive to S. p. Microorganisms and macroorganism cells that utilize ready-made dihydrofolic acid from the external environment are not sensitive to the action of S. p.

With an excess of PABA and its derivatives in the environment, for example, novocaine, anesthesin, etc., as well as methionine, folic acid, purine and pyrimidine bases, the antimicrobial activity of S. p. decreases. A decrease in the activity of S. p. in the presence of pus and wound discharge is associated with a high content of PABA and other antagonists of sulfanilamide preparations in these substrates.

The antimicrobial effect of S. p. is enhanced by drugs (for example, trimethoprim) that inhibit the conversion of dihydrofolic acid to folic (tetrahydrofolic) acid by inhibiting the enzyme dihydrofolate reductase. With the simultaneous use of S. p. with trimethoprim, the synthesis of tetrahydrofolic acid is disturbed at two successive stages - at the stage of formation of dihydrofolic acid (under the influence of S. p.) and at the stage of transformation of the latter into tetrahydrofolic acid (under the influence of trimethoprim), as a result of which a bactericidal effect develops .

After absorption into the blood, S. p. reversibly, but to a different extent, binds to plasma proteins. In a bound form, they do not have an antimicrobial effect and show it only as the drugs are released from this connection. The degree of their binding to blood plasma proteins does not affect the rate of S.'s release from the body. Metabolized by S. p. in the liver mainly by acetylation. The resulting acetylated metabolites of S. p. have no antimicrobial activity and are excreted from the body through the kidneys. In the urine, these metabolites can precipitate in the form of crystals, causing the appearance of crystalluria. The severity of crystalluria is determined not only by the degree of conversion of individual S. p. into acetylated metabolites and the magnitude of the doses of drugs, but also by the reaction of urine, tk. these metabolites are poorly soluble in an acidic environment.

According to features of pharmacokinetics and application among S. of the item distinguish the corresponding subgroups. For example, allocate a subgroup of S. items well absorbed from the gastrointestinal tract. Such S. items are used for systemic treatment of infections and for this purpose are prescribed orally and parenterally. Depending on the rate of their release among S. p. of this subgroup, there are: short-acting drugs (half-life less than 10 h) - streptocide, sulfacyl sodium, etazol, sulfadimezin, urosulfan, etc .; intermediate-acting drugs (half-life 10-24 h) - sulfazine, sulfamethoxazole, etc.; long-acting drugs (half-life from 24 to 48 h) - ulfapiridazine, sulfadimethoxine, sulfayunomethoxine, etc.; long-acting drugs (half-life more than 48 h) - sulfalene.

Long-acting sulfonamides differ from short-acting S.'s in their higher lipophilicity and, therefore, they are reabsorbed in significant amounts (up to 50-90%) in the renal tubules and are more slowly excreted from the body.

Sulgin, ftalazol, and ftazin belong to the subgroup of S.'s poorly absorbed from the gastrointestinal tract. These drugs are used to treat intestinal infections (colitis and enterocolitis of bacterial etiology, including bacillary dysentery).

The subgroup of S. items intended for topical use usually include soluble sodium salts of drugs that are well absorbed from the gastrointestinal tract, for example, etazol sodium, sulfapyridazine sodium, soluble streptocide, etc., as well as silver sulfadiazine. Preparations of this subgroup in the appropriate dosage forms (solutions, ointments, etc.) are used topically for the treatment of purulent infections of the skin and mucous membranes, infected wounds, etc.

In addition, among S. p., the so-called salazosulfanilamides are distinguished - azo compounds synthesized on the basis of some S. p. of systemic action and salicylic acid. These include salazopyridazine, salazodimethoxin, and salazosulfapyridine, which are used primarily for the treatment of non-specific ulcerative a. The effectiveness of salazosulfanamides in this disease is associated with the presence of not only antimicrobial activity, but also pronounced anti-inflammatory properties, which are due to the formation of aminosalicylic acid in the intestine during the biotransformation of drugs of this group, which has an anti-inflammatory effect.

In modern clinical practice Combination preparations containing sulfonamides and trimethoprim are also widely used. These combined preparations include biseptol containing sulfamstoxazole and trimethoprim (5:1 ratio) and sulfatone containing sulfomonomethoxine and trimethoprim (2.5:1 ratio). Unlike S. p. biseptol and sulfatone act bactericidal, have a broader spectrum of antimicrobial activity and are effective against strains resistant to sulfanilamide drugs.

In practice, other combinations of S. p. with diaminopyrimidine derivatives are also used. For example, combinations of sulfalene with chloridine are used to treat drug-resistant forms of malaria, and combinations of sulfazine with chloridine are used to treat a.

Sulfonamides are used to treat infections caused by microorganisms sensitive to these drugs. The choice of drugs is made taking into account the peculiarities of their pharmacokinetics. So, for systemic infections (bacterial infections of the respiratory tract, lungs, bile and urinary tract, etc.), S. p. are used, which are well absorbed from the gastrointestinal tract. For the treatment of intestinal infections, S.

items that are poorly absorbed from the gastrointestinal tract (sometimes in combination with well-absorbed S. p.).

Single and course doses of S. p., as well as the schemes for their appointment, are established in accordance with the duration of action of the drugs. So, short-acting S. p. is used in daily doses of 4-6 G, appointing them in 4-6 doses (course doses 20-30 G); drugs of medium duration of action - in daily doses 1-3 G, appointing them in 2 doses (course doses 10-15 G); long-acting drugs are prescribed in one dose at a daily dose of 0.5-2 G(course doses up to 8 G). Ultra-long-acting sulfonamides are prescribed according to two schemes: daily at the initial dose (on the first day) 0.8-1 G and further in maintenance doses of 0.2 G 1 time per day; 1 time per week at a dose of 1.5-2 G. For children, doses are reduced according to age.

The side effect of S. p. is manifested by dyspeptic disorders, allergic reactions ami, violations on the part of c.n.s. (headache, dizziness, etc.), leukopenia, methemoglobinemia, etc. Due to poor solubility in water, S. p. and their acetylation products in the body can precipitate in the kidneys in the form of crystals and cause crystalluria (especially when urine is acidified). For the prevention of this complication when taking S. p., it is advisable to recommend a plentiful alkaline drink.

S. items are contraindicated if there is a history of data on toxic-allergic reactions to any drugs in this group. In diseases of the liver and kidneys, S. p. should be prescribed in reduced doses under the control of the functional state of these organs.

Methods of application, doses, forms of release and storage conditions of the main S. items are given below.

Biseptol(Biseptol; a synonym for Bactrim, Septrin, etc.) is prescribed orally (after meals) for adults and children over 12 years old, 1-2 tablets (for adults) 2 times a day, in severe cases - 3 tablets 2 times a day; children aged 2 to 5 years, 2 tablets (for children); from 5 to 12 years old, 4 tablets (for children) 2 times a day. Release form: tablets for adults containing 0.4 G sulfamethoxazole and 0.08 G trimethoprim; tablets for children containing 0.1 G sulfamethoxazole and 0.02 G trimethoprim. Storage: list B.

Salazodimethoxine(Salazodimethoxinum) is used orally (after meals). Adults are prescribed 0.5 G 4 times a day or 1 G 2 times a day for 3-4 weeks. Upon the onset of a therapeutic effect, the daily dose is reduced to 1-1.5 G(by 0.5 G 2-3 times a day). Children aged 3 to 5 years are initially prescribed 0.5 G per day (in 2-3 doses). At the onset of a therapeutic effect, the dose is reduced by 2 times. Children aged 5 to 7 years are initially prescribed 0.75-1 G, from 7 to 15 years, 1-1.5 G per day. Release form: powder, tablets of 0.5 G. Storage: list B; in a place protected from light.

Salazopyridazine(Salazopyridazinum). Methods of application, doses. release forms and storage conditions are the same as for salazodimethoxine.

streptocide(Streptocidum, a synonym for white streptocide) is administered orally to adults at 0.5-1 G at the reception 5-6 times a day; children under the age of 1 year at 0.05-0.1 G, from 2 to 5 years by 0.2-0.3 G, from 6 to 12 years 0.3-0.5 G appointment. Higher doses for adults orally single 2 G, daily 7 G. Topically applied in the form of powders, ointments (10%) or liniments (5%). Release form: powder, tablets of 0.3 and 0.5 G; 10% ointment; 5% liniment. Storage: list B: in a well-closed container.

Streptocid soluble(Streptocidum solubile) is administered intramuscularly and subcutaneously in the form of 1-1,

5% solutions prepared with water for injection or isotonic sodium chloride solution, up to 100 ml(2-3 times a day). Intravenously administered in the form of 2-5-10% solutions prepared in the same solvents or 1% glucose solution, up to 20-30 ml. Release form: powder. Storage: List B in well-closed jars.

Sulgin(Sulginum) is prescribed inside for adults 1-2 times a day. G at the reception: on the 1st day 6 times a day, on the 2nd and 3rd days 5 times, on the 4th day 4 times, on the 5th day 3 times a day. The course of treatment is 5-7 days. Other schemes are used to treat acute dysentery. Higher doses for adults single 2 G, daily 7 G. release forms: powder; tablets 0.5 G

Silver sulfadiazine(Sulfadiazini argenti) is applied topically. Included in the composition of the ointment "Dermazin", which is applied to the oval surface with a layer of 2-4 mm 2 times a day, followed by the imposition of a sterile dressing. Ointment is not prescribed to premature and newborn children; in pregnant women, they are used according to health indications (with an area of ​​\u200b\u200bmore than 20% of the body surface). Release form: tubes of 50 G, cans of 250 G.

Sulfadimezin(Sulfadimezinum; synonymous with sulfadimidine, etc.) is administered orally to adults at the first dose 2 G, then 1 G every 4-6 h(until the body temperature drops), then 1 G after 6-8 h. Children inside at the rate of 0.1 g/kg at the first appointment, then 0.025 g/kg every 4-6-8 h. For the treatment of dysentery, adults are prescribed according to the following scheme: on the 1st and 2nd days, 1 G every 4 h(6 G per day), on the 3rd and 4th days 1 G every 6 h(4 G per day), on the 5th and 6th days 1 G every 8 h(3 G per day). After a break (within 5-6 days), a second cycle is carried out, appointing on the 1st and 2nd days 5 G per day, on the 3rd and 4th days 4 G per day, on the 5th day 3 G per day. For the same purpose, children under 3 years of age are prescribed at the rate of 0.2 g/kg per day (in 4 divided doses) for 7 days, children over 3 years old 0.4-0.75 G(depending on age) 4 times a day. Release form: powder; tablets of 0.25 and 0.5 G

Sulfadimethoxine(Sulfadimethoxinum; synonymous with madribon, etc.) is used orally. Adults are prescribed on the 1st day 1-2 G, in the following days, 0.5-1 G per day (in one dose); children at the rate of 0.025 g/kg on the 1st day and at 0.0125 g/kg in the following days. Release form: powder; tablets of 0.2 and 0.5 G. Storage: list B; in a place protected from light.

Sulfazin(Sulfazinum) is used internally. Adults are prescribed for the 1st appointment 2-4 G, within 1-2 days 1 G every 4 h, in the following days 1 G every 6-8 h; children at the rate of 0.1 g/kg at the first appointment, then 0.025 g/kg every 4-6 h. Release form: powder; tablets 0.5 G. Storage: list B; in a place protected from light.

Sulfalen(Sulfalenum; synonymous with kelfisin, etc.) is prescribed by mouth for adults, 2 G once every 7-10 days or on the first day 1 G, then by 0.2 G daily. Release form: tablets of 0.2 G. Storage: list B.

Sulfamonomethoxin(Sulfamonomethoxin). The method of administration and doses are the same as those of sulfadimethoxine. Release form: powder; tablets 0.5 G

Sulfapyridazine(Sulfapyridazinum; synonym: spofazadin, sulamine, etc.). The method of administration and doses are the same as those of sulfadimethoxine. Release form: powder; tablets 0.5 G. Storage: list B; in a place protected from light.

Sulfatone(Sulfatonum) is prescribed by mouth for adults, 1 tablet 2 times a day. Higher doses for adults: single - 4 tablets, daily - 8 tablets. Release form: tablets containing 0.25 G sulfamonomethoxine and 0.1 G trimethoprim. Storage: list B; in a dry, dark place.

Sulfacyl sodium(Sulfacylum-natrium; synonym: soluble sulfacyl, sulfacetamide-sodium, etc.) is administered orally to adults at 0.5-1 G, children 0.1-0.5 G 3-5 times a day. Intravenously (slowly) 3-5 ml 30% solution 2 times a day. In eye practice, they are used in the form of 10-20-30% solutions and ointments. Higher doses for adults orally single 2 G, daily 7 G. Release form: powder; 30% solution for injection in ampoules of 5 ml; 30% solution in vials of 5 and 10 ml; 20% and 30% solutions (eye drops) in dropper tubes of 1.5 ml; 30% ointment 10 G. Storage: list B; in a cool, dark place.

Urosulfan(Urosulfanum) is used internally. Adults are prescribed in the same doses as sodium sulfacyl, children 1-2.5 G per day (in 4-5 doses). The higher daily doses for adults are the same as sodium sulfacyl. Release form: powder, tablets of 0.5 G

Phtazin(Phthazinum) is administered orally to adults on the first day, 1 G 1-2 times, in the following days, 0.5 G 2 times a day. For children, the dose is reduced according to age. Release form: powder; tablets 0.5 G. Storage: list B: in a place well protected from light.

Ftalazol(Phthalazolum; synonymous with phthalyl-sulfathiazole, etc.) is used orally for dysentery. Adults are prescribed on the 1-2nd day 1 G every 4 h(6 G per day), on the 3rd-4th days, 1 G every 6 h(4 G per day), on the 5-6th day, 1 G every 8 h(3 G per day). After 5-6 days, the treatment is repeated: on the 1st-2nd days - 5 G per day, on the 3rd-4th days - 4 G per day, on the 5th day - 3 G per day. For other intestinal infections, adults are prescribed in the first 2-3 days 1-2 G, in the following days, 0.5-1 G every 4-6 h. Children under 3 years old with dysentery are prescribed at the rate of 0.2 g/kg per day (in 3 divided doses), children over 3 years old 0.4-0.75 G at the reception 4 times a day. The highest oral doses for adults are the same as for sulfacyl sodium. Release form: powder; tablets 0.5 G. Storage: list B; in a well sealed container.

Etazol(Aethazolum; synonymous with sulfaetidol, etc.) is administered orally to adults, 1 G 4-6 times a day: children under 2 years old 0.1-0.3 G every 4 h, from 2 to 5 years - 0.3-0.4 G every 4 h, from 5 to 12 years old - 0.5 each G every 4 h. Locally prescribed in the form of a powder (powder) or ointment (5%). The highest oral doses for adults are the same as for sulfacyl sodium. Release forms: powder; tablets of 0.25 and 0.5 G. Storage: list B; in a well sealed container.

Etazol sodium(Aethazolum-natrium; synonymous with etazol soluble) is administered intravenously (slowly) 5-10 ml 10% or 20% solution. In pediatric practice, the drug is used orally in granules, which are dissolved in water before use and prescribed to children at the age of 1 year - 5 ml (0,1 G), 2 years - 10 ml (0,2 G), 3-4 years - 15 ml (0,3 G), 5-6 years - 20 ml every 4 h. Release forms: powder; ampoules of 5 and 10 ml 10% and 20% solutions; granules in bags of 60 G. Storage: list B; in a well-closed container, protected from light.