Sulfonamide ointments. Sulfanilamide preparations - a list. Mechanism of action of sulfonamides, use and contraindications. Interaction of sulfanilamide with other substances

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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, E. 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. A likely side effect is the precipitation of crystals in the kidneys (especially for the drugs sulfadimezin, norsulfazol, sulfapiridazine, sulfamonomethoxine). 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 drugs combined with trimethoprim is higher than that of monocomponent drugs, 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); sulphamonomethoxine;

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 young children. 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: combined use with acids, hexamethylenetetramine, adrenaline solution is impractical, as 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, it should be prescribed with caution in diseases of the liver, kidneys (dynamic monitoring of liver and kidney function is necessary).

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).

The 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

ANTRIMA (Antrima)

Pharmachologic effect. Combined sulfanilamide drug. Sulfadiazine and trimethoprim have a bacteriostatic (preventing the growth of bacteria) and bactericidal (destroying bacteria) action, in combination their antimicrobial effect is enhanced. Highly sensitive to the drug: E. coli, Klebsiella, Enterobacter, Proteus, Citrobacter, Salmonella, Shigella, Haemophilus, Vibriocholerae, Listeria, Pneumocystiscarinii.

Indications for use. Bacterial infections caused by microorganisms sensitive to the drug, including respiratory tract infections, urinary tract infections, infections of the gastrointestinal tract (especially typhoid fever).

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Adults are prescribed 1 tablet 2 times a day with meals. For children, the drug is usually prescribed in the form of a suspension (suspension of solid particles of the drug in a liquid) - 1 attached measuring spoon (2.5 ml) per 5 kg of body weight 2 times a day with meals. The maximum daily dose is 8 scoops. For patients with creatinine clearance (the rate of blood purification from the end product of nitrogen metabolism - creatinine) from 30 to 15 ml / min, the drug is prescribed only in the case of hemodialysis (blood purification method), 1 time per day.

In the case of prolonged treatment with the drug, systematic monitoring of the picture of peripheral blood, kidney and liver function is necessary. When using the drug in patients with diabetes, it should be taken into account that 2.5 ml of the drug contains 1 g of sucrose.

Side effect. Nausea, abdominal pain, thrombocytopenia (a decrease in the number of platelets in the blood),

neutropenia (decrease in the number of neutrophils in the blood), allergic reactions.

Contraindications. Deficiency of the enzyme glucose-6-phosphate dehydrogenase in erythrocytes (risk of increased hemolysis /destruction of erythrocytes/); pregnancy, breastfeeding; hypersensitivity to the components of the drug. The drug is not prescribed to premature and newborn children.

Release form. Tablets containing 0.4 g of sulfadiazine and 0.08 g of trimethoprim; oral suspension for children (2.5 ml - 0.1 g sulfadiazine and 0.02 g trimethoprim) in 50 ml vials.

Storage conditions. List B. In a dry, cool, dark place.

BISEPTOL (Biseptol)

Synonyms: Bactrim, Septrin, Abacin, Abactrim, Andoprim, Bacterial, Bacticel, Bactifer, Bactramin, Bactramel, Bactrizol, Berlocid, Hemitrin, Doctonil, Ectapprim, Ekspektrin, Falprin, Gantrin, Infectrim, Metomid, Microcetim, Nola "ps, Oradin, Oribact, Potecept, Primazol, Resprim, Septocid, Sumetrolim, Trimexazole, Trixazole, Uroxen, Vanadil, Aposulfatrin, Bactecod, Bactreduct, Blackson, Groseptol, Cotribene, Cotrim, Cotrimol, Eriprim, Primotren, Rancotrim, Sulfatrim, Trimezol, Expazole, Novotrimed, Oriprim, Sinersul, Cotrimaxol, Cotrimaxazole, Sulotrim, Trimosul, etc.

A combined preparation containing two active ingredients: the sulfanilamide drug sulfamethoxazole and a diaminopyrimidine derivative - trimethoprim.

Pharmachologic effect. The combination of these two drugs, each of which has a bacteriostatic (preventing the reproduction of bacteria) effect, provides a high bactericidal (destroying

bacteria) activity against gram-positive and gram-negative microorganisms, including bacteria resistant to sulfanilamide preparations.

The bactericidal effect is associated with a double blocking effect of bactrim on the metabolism (metabolism) of bacteria. Sulfamethoxazole disrupts the biosynthesis of dihydrofolic acid, and trimethoprim blocks the next stage of metabolism - the restoration of dihydrofolic acid to tetrahydrofolic acid, which is necessary for the development of microorganisms. The choice of sulfamethoxazole as a component of bactrim is due to the fact that it has the same elimination rate (removal rate) with trimethoprim.

The drug is effective against streptococci, staphylococci, pneumococci, dysentery bacillus, typhoid fever, Escherichia coli, Proteus; ineffective against Mycobacterium tuberculosis, spirochetes, Pseudomonas aeruginosa.

The drug is rapidly absorbed when taken orally. The maximum concentration in the blood is observed 1-3 hours after ingestion and persists for 7 hours. High concentrations are created in the lungs and kidneys. It is excreted in a significant amount in the urine (40-50% of trimethoprim and about 60% of sulfamethoxazole are excreted within 24 hours, mainly in acetylated form).

Indications for use. Biseptol is used for respiratory tract infections: acute and chronic bronchitis (inflammation of the bronchi), pleural empyema (accumulation of pus between the membranes of the lungs), bronchiectasis (bronchial disease associated with the expansion of their lumen), abscess (abscess) of the lung, pneumonia (pneumonia) ; urinary tract: urethritis (inflammation of the urethra), cystitis (inflammation of the bladder), pyelitis (inflammation of the renal pelvis), chronic pyelonephritis (inflammation of the tissue of the kidney and renal pelvis), prostatitis (inflammation of the prostate), gonococcal urethritis. It is also used for infections of the gastrointestinal tract, surgical infection and other infectious diseases. The drug is also effective in septicemia (a form of blood infection by microorganisms) caused by bacteria sensitive to the drug. The high efficacy of the drug in uncomplicated gonorrhea has been established.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Adults and children over 12 years of age are usually prescribed 4 tablets (or 2 forte tablets, or 8 measuring spoons of syrup) in a daily dose. The minimum daily dose for long-term therapy (more than 14 days) is 2 tablets (or 1 forte tablet, or 4 measuring spoons of syrup). The maximum daily dose (for the treatment of particularly severe cases) is 6 tablets (or 3 forte tablets, or 12 measuring spoons of syrup). The daily dose is divided into 2 doses (morning and evening). The drug is taken after meals with a sufficient amount of liquid. In acute infections, treatment with the drug is carried out for 5 days or until the patient has no symptoms of an infectious disease for 2 days.

For gonorrhea, the drug is prescribed for one day in a daily dose of 10 tablets (5 forte tablets, or 20 measuring beds of syrup), divided into 2 doses (morning and evening). In acute uncomplicated urinary tract infections in women, it is recommended to prescribe 2-3 forte tablets once. It is advisable to take the tablets in the evening after meals or before going to bed.

In pneumocystosis (an acute form of pneumonia; observed more often in weakened children of the first months of life) caused by Pneumocystiscarinii, sulfamethoxazole is prescribed in a daily dose of up to 0.1 g / kg of body weight and

trimethoprim up to 0.02 g/kg. Assign every 6 hours. The course of treatment is 14 days.

For children under 12 years of age, the drug is prescribed as a syrup in a daily dose of sulfamethoxazole 0.03 g and trimethoprim 0.006 g. The syrup is taken 2 times a day (morning and evening). In severe infections, the daily dose can be increased by about 50%.

For patients with impaired renal function, the dose is set depending on the amount of creatinine clearance (the rate of blood purification from the end product of nitrogen metabolism - creatinine). With a creatinine clearance greater than 30 ml / min, dose adjustment is not required; at 15-30 ml / min, half the usual dose is used; with a creatinine clearance of less than 15 ml / min, the drug is not recommended. Elderly patients may also require dose adjustment.

The drug should be used under close medical supervision.

Side effect. Nausea, vomiting, diarrhea (diarrhea), allergic reactions, nephropathy (a common name for some kidney diseases) are possible. Leukopenia (a decrease in the level of leukocytes in the blood) and agranulocytosis (a sharp decrease in the number of granulocytes in the blood) may develop.

Contraindications. Hypersensitivity to sulfonamides, diseases of the hematopoietic system, impaired liver and kidney function, pregnancy. The drug should not be given to premature babies and newborns. Bactrim should be used with caution in young children. When treating with the drug, it is necessary to carefully monitor the blood picture.

Release form. Tablets in a package of 20 pieces. The drug is available in tablets in two dosages: for adults, containing 0.4 g (400 mg) of sulfamethoxazole and 0.08 g (80 mg) of trimethoprim in one tablet; for children containing 100 mg of sulfamethoxazole and 20 mg of trimethoprim in one tablet.

For adults, tablets "bactrim forte" are also produced, containing 800 mg of sulfamethoxazole and 160 mg of trimethoprim, and for children - a syrup, 1 ml of which contains 40 mg of sulfamethoxazole and 8 mg of trimethoprim (suspension of white with a yellowish tinge in 100 ml vials ).

Storage conditions.

BACTRIM SUSPENSION (Bactrim)

Synonyms: Biseptol, Septrin, etc.

Pharmachologic effect. Combined drug. The combination of sulfamethoxazole and trimethoprim provides high efficiency against gram-positive and gram-negative microorganisms, including those resistant to sulfanilamide preparations. Bactrim is rapidly absorbed when taken orally. The maximum concentration in the blood is observed after 1-3 hours and persists for 7 hours.

Indications for use. Septicemia (a form of blood poisoning by microorganisms), infections of the respiratory, urinary tract and gastrointestinal tract caused by microorganisms sensitive to the drug, etc.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Assign inside after meals (morning and evening). Doses are set depending on the age of the child: from 6 weeks. up to 5 months - "/2 teaspoons 2 times a day; from 6 months to 5 years - 1 teaspoon 2 times a day; from 5 to 12 years - 2 teaspoons 2 times a day.

Side effect. Nausea, vomiting, allergic reactions, leukopenia (a decrease in the level of leukocytes in the blood) and agranulocytosis (a sharp decrease in the number of granulocytes in the blood). Treatment is carried out under the control of the blood picture.

Contraindications.

Release form. Suspension (syrup) in vials of 100 ml. The composition of the suspension (based on 5 ml) includes the following substances: sulfamethoxazole-3 (paminobenzenesulfamido) -5-methylisoxazole - 0.2 g; trimethoprim - 2,4-diamino-5-(3,4,5-trimethoxybenzyl) -pyrimidine - 0.04 g.

Storage conditions. List B. In a dry cool dark place.

Lidaprim (Lidaprim)

Pharmachologic effect. Combined preparation containing sulfametrol and trimethoprim. Sulfametrol has a high antibacterial activity, and in combination with trimethoprim (see Biseptol) provides a bactericidal (destroying bacteria) effect against gram-positive and gram-negative microorganisms, including bacteria that are resistant to conventional sulfanilamide drugs.

Indications for use. Indications for the use of lidaprim basically coincide with the indications for the use of biseptol.

Lidaprim is effective for infections of the respiratory tract, ear, throat and nose of the kidneys and urinary tract and gastrointestinal tract, for prostatitis (inflammation of the prostate gland), gonorrhea, gynecological infectious diseases and other infections caused by pathogens sensitive to the drug.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Adults and children over 12 years of age are prescribed the drug orally, usually starting with 2 tablets of lidaprim or 1 tablet of lidaprim forte 2 times a day (morning and evening). Take until the disappearance of acute manifestations of infection (at least 5 days); then 1 tablet or V2 tablets of lidaprim forte 2 times a day.

Patients with chronic pyelonephritis (inflammation of the tissue of the kidney and renal pelvis) and with chronic salmonella carriage are prescribed 2 tablets of lidaprim or 1 tablet of lidaprim forte 2 times a day for a long time (on average 3 months).

In case of gonorrhea, 4 tablets of lidaprim forte are usually prescribed once a day.

In acute infections, you can start with an intravenous infusion of a solution of lidaprim; enter slowly 250 ml (1 vial) 2 times a day.

Children under the age of 2 years are prescribed "/ 2 teaspoons of suspension 2 times a day, from 2 to 3 years - 1 teaspoon of suspension or 2 tablets for children 2 times a day; 3-6 years - 1 "/ 2 teaspoons or 3 tablets for children per day; 6-12 years - 2 teaspoons or 4 tablets for children 2 times a day.

Side effects and contraindications are the same as Biseptol.

Release form. Lidaprim is available in different dosage forms: a) Lidaprim tablets containing 400 mg of sulfametrol and 80 mg of trimethoprim, in a package of 20 or 100 pieces; b) tablets of lidaprim forte, coated, containing 800 mg of sulfametrol and 160 mg of trimethoprim, in a package of 10; 25 or 50 pieces; c) lidaprim tablets for children, containing 100 mg of sulfametrol and 20 mg of trimethoprim, in a package of 20 pieces; d) suspension of lidaprim (for children), containing 5 ml (1 teaspoon) of 200 mg of sulfametrol and 40 mg of trimethoprim, in vials of 50 and 100 ml; e) solution for injection (infusion) in 250 ml glass vials containing 800 mg of sulfametrol and 160 mg of trimethoprim.

Storage conditions.

MAFENID (Maphenidum)

Synonyms: Ambamide, Bensulfamidine, Homosulfamidine, Sulfamilone, Mafenide acetate, etc.

Sulfanilamide antibacterial drug for external use. Available as mafenide acetate.

Pharmachologic effect. Mafenide acetate has a wide spectrum of action, effective against gram-positive and gram-negative bacteria and pathogenic (pathogenic) anaerobes (microorganisms that can exist in the absence of oxygen), pathogens of gas gangrene. It is not inactivated by para-aminobenzoic acid and does not change activity in an acidic environment.

Indications for use. It is used to treat infected burns, purulent wounds, bedsores (tissue necrosis caused by prolonged pressure on them due to lying), trophic ulcers (slowly healing skin defects).

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Ointment (10%) is applied directly to the affected surface, swabs soaked in ointment are introduced into the cavity, napkins smeared with ointment with a layer of 2-3 mm are also applied to the wounds. Usually, 30-70 g of ointment is used per bandage. Before applying a bandage, the wound is cleaned of purulent-necrotic masses (inflamed necrotic / dead / tissues). Dressings are changed daily or 2-3 times a week, depending on the amount of purulent discharge. The duration of treatment is from 1 to 4-5 weeks.

For second-degree burns, a single dressing may be applied.

Side effect. When applying the ointment to the burn or wound surface, burning, pain can be observed, lasting from "/2 to 1-3 hours; with severe pain, analgesics (painkillers) are prescribed.

Contraindications. The use of the ointment is contraindicated if there is a history (medical history) of data on toxic-allergic reactions to sulfanilamide preparations.

Release form. 10% ointment in light-protective glass jars of 50 g and 2 kg.

Storage conditions.

ALGIMAF (Algimafum)

Lyophilized gel (iron-like dosage form, dehydrated by freezing in a vacuum) of sodium-calcium salt of alginic acid containing mafenide and other substances.

Pharmachologic effect. Shows adsorbing (absorbing) and antimicrobial activity, cleans wounds, promotes regeneration (recovery) of tissues.

Indications for use. Applied with superficial burns of 2 and 3 degrees, long-term non-healing ulcers and wounds.

Method of application and dose. Impose on the affected surface (after treatment) a plate of the appropriate size. Fix with a gauze bandage or bandage. It can be left in the wound until the end of epithelialization (recovery of the skin surface or mucous membrane).

Side effect. Passing burning sensation.

Release form. Sterile porous sheets from 50x50 to 135x250 mm and 10 mm thick in bags,

Storage conditions. List B. In a dry, dark place, without bending the packages and protecting them from mechanical damage.

NORSULFAZOL (Norsulfazolum)

Synonyms: Sulfathiazole, Amidothiazole, Aseptosil, Azoseptal, Cibazol, Eleudron, Polyseptil, Pirisulfone, Thiazamide, etc.

Pharmachologic effect. Sulfanilamide drug. It is effective in infections caused by hemolytic streptococcus, pneumococcus, gonococcus, staphylococcus, and also Escherichia coli.

Indications for use. Pneumonia (pneumonia), cerebral meningitis (purulent inflammation of the meninges), gonorrhea, staphylococcal and streptococcal sepsis (blood infection with microbes / streptococci / from the focus of purulent inflammation), dysentery, etc.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Taken inside. For pneumonia and meningitis, the first dose is 2 g, then 1 g every 4-6 g (course dose 20-30 g); with staphylococcal infections at the first dose 3-4 g, then 1 g 4 times a day for 3-6 days. In the treatment of dysentery, 6-4-3 g per day according to a special scheme.

Norsulfazol is prescribed to children every 4-6-8 hours in the following single doses: at the age of 4 months. up to 2 years - 0.1-0.25 g each, from 2 to 5 years - 0.3-0.4 g each, from 6 to 12 years old - 0.4-0.5 g each. double dose.

Side effect. Possible dyspeptic disorders (digestive disorders), allergic reactions, leukopenia (decrease in the level of leukocytes in the blood), neuritis (nerve inflammation), impaired renal function (crystalluria - the presence of salt crystals in the urine).

Contraindications. Hypersensitivity to sulfa drugs.

Release form. Powder; tablets in packs of 10 pieces of 0.25 g and 0.5 g with a score.

Storage conditions. List B. In a dry, dark place.

Norsulfazol is also included in the preparations of inhalipt, sunoref ointment.

NORSULFAZOL-SODIUM (Norsulfazolum-natrium)

Synonyms: Sulfathiazole sodium, Sulfathiazole sodium, Norsulfazol soluble.

Sodium salt of norsulfazole.

Indications for use. The same as for norsulfazole. In addition, with infectious diseases of the eyes.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. It is administered intravenously in cases where the possibility of introducing nosulfazole into the stomach is excluded (for example, after surgery on the gastrointestinal tract, with vomiting and unconsciousness of the patient) and if it is necessary to quickly create a high concentration of the drug in the blood. As soon as the patient's condition allows, they switch to taking the drug inside.

A 5% or 10% solution is injected into a vein; appoint at the rate of 0.5-1.0-2.0 g per infusion (10-20 ml of a 5% or 10% solution; pour slowly). It is advisable to further dilute solutions of norsulfazole soluble in 5% glucose solution or in isotonic sodium chloride solution. When using concentrated solutions, the possibility of phlebitis (inflammation of the vein) at the injection site should be considered. Subcutaneous and intramuscular solutions are not prescribed, as they can cause tissue irritation up to necrosis (tissue necrosis).

It is also used in the form of eye drops (10% solution, 2 drops 3-4 times a day) for conjunctivitis (inflammation of the outer shell of the eye), blepharitis (inflammation of the edges of the eyelids) and other infectious eye diseases. Can be taken orally.

Higher doses for adults inside: single - 2 g, daily - 7 g.

Side effects and contraindications. Same as for norsulfazole.

Release form. Powder.

Storage conditions. List B. In a dry, dark place.

Salazodimethoxin (Salazodimethoxintun)

Pharmachologic effect. Sulfanilamide of the prolonged (long) action. - Like salazopyridazine, the drug breaks down in the intestines, with the formation of 5-aminosalicylic acid and sulfadimethoxin, which have anti-inflammatory and antibacterial effects. The drug has low toxicity.

Indications for use. Non-specific ulcerative colitis (chronic inflammation of the colon with the formation of ulcers, caused by unclear reasons) in the active stage, mainly in mild and moderate forms of the disease, poor tolerance or ineffectiveness of salazopyridazine.

Method of application and dose. Assign inside (after eating) in approximately the same doses and for the same period as salazopyridazine. Usually give adults 0.5 g 4 times a day (1 g 2 times a day) for 3-4 weeks, and then (if a therapeutic effect has occurred during this period) 0.5 g 2-3 times a day day for the next 2-3 weeks. In severe forms of the disease, the daily dose is increased in the first days to 4 g, and after a decrease in the frequency of stools, the dose is reduced. In mild forms of the disease, you can start with a dose of 1.5 g per day, and if there is no effect, go to 2 g per day.

Children aged 3 to 5 years in the first 7-14 days are prescribed 0.5 g per day, in the next 2 weeks. - 0.25 g per day, on other days (until the 40th - 50th day from the start of treatment) - 0.125 g per day; children from 5 to 7 years old - respectively, 0.8-1.0 g each; 0.4-0.5 g and 0.2-0.25 g; from 7 to 15 years - 1.0-1.5 g; 0.5-0.75 g and 0.25-0.375 g. Daily doses are given in 2-3 doses.

If during the first 14 days from the start of treatment it is not possible to obtain a therapeutic effect, salazodimethoxine is canceled; you can switch to the use of salazopyridazine or salazosulfapyridine.

To prevent recurrence (reappearance of signs of the disease) of ulcerative colitis and Crohn's disease (a disease of unknown cause, characterized by inflammation and narrowing of the lumen of certain sections of the intestine), salazodimethoxine is prescribed for a long time in gradually decreasing doses: for adults, 0.5 g 1-2 times a day, daily for 2-6 months, then 0.25-0.5 g daily or every other day for 6-12 months. For children, the drug is prescribed in smaller

doses, taking into account age and doses used in the acute period of the disease. In case of deterioration of health, the dose of salazodimethoxin is increased,

Side effect. Allergic reactions, leukopenia (decrease in the level of leukocytes in the blood), dyspeptic disorders (digestive disorders).

Contraindications. Hypersensitivity to sulfonamides.

Release form.

Storage conditions. List B. In a dark place.

Salazopyridazine (Salazopyridazinum)

Synonyms: Salazodin.

Pharmachologic effect. Sulfanilamide drug. It has anti-inflammatory and immunosuppressive (suppressing the body's defenses) effect.

Indications for use. Non-specific ulcerative colitis (chronic inflammation of the colon with the formation of ulcers, caused by unclear reasons), as well as in diseases that occur with autoimmune disorders (disorders based on allergic reactions to the body's own tissues or waste products), including as a basic means in the treatment of rheumatoid arthritis (an infectious-allergic disease from the group of collagenoses, characterized by chronic progressive inflammation of the joints).

Method of application and dose. In ulcerative colitis, salazopyridazine is prescribed for adults inside (after meals) in tablets of 0.5 g 4 times a day for 3-4 weeks. If during this period a therapeutic effect is manifested, the daily dose is reduced to 1.0-1.5 g (0.5 g 2-3 times a day) and treatment is continued for another 2-3 weeks. If there is no effect, the drug is stopped. Patients with mild forms of the disease are prescribed the drug first at a daily dose of 1.5 g, and if there is no effect, the dose is increased to 2 g per day.

For children aged 3 to 5 years, salazopyridazine is prescribed, starting with a dose of 0.5 g per day (2-3 doses). If there is no effect within 2 weeks. the drug is canceled, and if there is a therapeutic effect, treatment is continued at this dose for 5-7 days, then the dose is reduced by 2 times and treatment is continued for another 2 weeks. In the case of clinical remission (temporary weakening or disappearance of the manifestations of the disease), the daily dose is again halved and prescribed until the 40-50th day, counting from the start of treatment.

Children aged 5 to 7 years are prescribed the drug, starting with 0.75-1.0 g per day; from 7 to 15 years - with a dose of 1.0-1.2-1.5 g per day. Treatment and dose reduction are carried out according to the same scheme as in children from 3 to 5 years.

The use of salazopyridazine is combined with the general treatments and diet recommended for ulcerative colitis.

Salazopyridazine can also be used rectally (into the rectum) in the form of suspensions (suspensions of solid particles in a liquid) and suppositories.

Suspension of salazopyridazine 5% is used for rectal administration with damage to the rectum and sieve, in the preoperative period and after subtogal colectomy (after removal of part of the colon), with poor tolerance of the drug in the form of tablets. The suspension is slightly warmed up and injected as an enema into the rectum or into the stump of the intestine, 20-40 ml each.

1-2 times a day. Children are administered 10-20 ml (depending on age). Rectal administration can be combined with oral administration.

Candles are used rectally. In the acute stage of the disease, 1 suppository is prescribed 2-4 times a day for 2 weeks. up to 3 months The duration of the course depends on the effectiveness of treatment and tolerability of the drug. The maximum daily dose is 4 suppositories (2 g). At the same time, you can take salazopyridazine tablets (not exceeding a total daily dose of 3 g) and other drugs for the treatment of ulcerative colitis.

In order to prevent relapses (reappearance of signs of the disease), 1-2 suppositories are prescribed per day for 2-3 months.

Doses and regimen of the drug in other forms of colitis with ulcerative lesions are the same as in nonspecific ulcerative colitis.

Side effect. When taking salazopyridazine tablets orally, the same adverse reactions are possible as with the use of sulfonamides and salicylates: allergic phenomena, leukopenia (decrease in the level of leukocytes in the blood), dyspeptic disorders (digestive disorders), sometimes a slight decrease in hemoglobin levels (the functional structure of the erythrocyte, which ensures its interaction with oxygen). In such cases, the dose should be reduced or the drug discontinued. After the introduction of the suspension, a burning sensation in the rectum and the urge to defecate (empty bowel) may appear, especially with rapid administration. When using salazopyridazine in suppositories, there may be a burning sensation and soreness in the rectum, sometimes an increase in stool. In case of severe pain during rectal administration of salazopyridazine in suppositories, it is recommended to prescribe the drug rectally in the form of a 5% suspension and orally in tablets.

Contraindications. The drug is contraindicated in the presence of a history (medical history) of data on toxic-allergic reactions in the treatment of sulfonamides and salicylates.

Release forms. Tablets of 0.5 g in a package of 50 pieces; 5% suspension in 250 ml vials containing salazopyridazine, tween-80, benzyl alcohol and polyvinyl alcohol (the drug after shaking is an orange suspension, which then settles); candles (brown) 0.5 g per pack of 10 pieces.

Storage conditions. List B. In a place protected from light at room temperature.

Salazosulfaliridine (Salazosulfapyridinum)

Synonyms: Sulfasalazine, Azopyrine, Azufidin, Salazopyridine, Salazopyrin, Salicylazosulfapyridine, Salisulf.

Pharmachologic effect. The drug has an antibacterial effect against diplococci, streptococci, gonococci, Escherichia coli. A feature of the drug is that it has a pronounced therapeutic effect in patients with ulcerative colitis (chronic inflammation of the colon with the formation of ulcers caused by unclear reasons). The mechanism of this action is not fully understood. A certain role is played by the ability of the drug to accumulate in the connective tissue (including intestinal tissue) and gradually separate 5-aminosalicylic acid and sulfapyridine, which have anti-inflammatory and antibacterial properties.

Indications for use. Nonspecific ulcerative colitis, rheumatoid arthritis (an infectious-allergic disease from the group of collagenoses, characterized by chronic progressive inflammation of the joints).

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Assign inside. It is recommended on the 1st day for adults 1 tablet (0.5 g) Phrase per day (at regular intervals), on the 2nd day - 2 tablets 4 times and on subsequent days in case of good tolerance of the drug - 3-4 times tablets 4 times a day. After subsiding of the clinical symptoms of the disease, maintenance doses (1.5-2.0 g per day) are prescribed for several months.

For children, salazosulfapyridine is prescribed in smaller doses: at the age of 5-7 years - 2-1 tablet (0.25-0.5 g) 3-6 times a day, over 7 years old - 1 tablet (0.5 g ) 3-6 times a day.

Salazosulfapyridine is also effective in mild to moderate forms of Crohn's disease (a disease of unknown cause, characterized by inflammation and narrowing of the lumen of certain sections of the intestine)

Salazosulfapyridine is also used as a basic agent in the treatment of rheumatoid arthritis due to the presence of immunocorrective properties in the drug (restoring immunity / body defenses /). Assign 2-3 g per day (40 mg / kg per day) for 2-6 months.

Treatment should be carried out under close medical supervision; it is necessary to systematically monitor the blood picture.

Side effect. Nausea, vomiting, headache, dizziness may occur. In such cases, cancel the drug, and after 2 days gradually, within 3 days, again increase the dose. Allergic reactions in the form of skin rashes, drug fever (a sharp rise in body temperature in response to taking the drug); leukopenia (decrease in the level of leukocytes in the blood). In these cases, the drug should be discontinued. The drug is excreted in the urine and, with an alkaline reaction, stains it in a yellow-orange color.

Contraindications. Severe toxic-allergic reactions in history (previously) to sulfonamides.

Release form. Tablets of 0.5 g in a package of 50 pieces.

Storage conditions. List B. In a dry, dark place.

Streptocid (Streptocidum)

Synonyms: Sulfanilamide, Streptocid white, Ambezid, Deseptil, Dipron, Prontalbin, Prontalin, Prontoin, Prontosil white, Streptamine, Streptozol, Sulfamidil, etc.

Pharmachologic effect. Sulfanylamide drug. It has an antimicrobial effect against streptococci, meningococci, gonococci, pneumococci, Escherichia coli and some other bacteria.

Indications for use. Erysipelas, tonsillitis, epidemic cerebrospinal meningitis (purulent inflammation of the membranes of the brain), cystitis (inflammation of the bladder), pyelitis (inflammation of the renal pelvis), colitis (inflammation of the colon:), wound infection.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Inside, 0.5-1 g 5-6 times a day. Doses for children

decrease according to age. Higher doses for adults inside: single - 2 g, daily - 7 g.

Locally injected into the wound 5-15 g of sterile powder; externally in the form of 5% liniment or 10% ointment.

Side effect. Headache, dizziness, nausea, vomiting, cyanosis (blue skin and mucous membranes), allergic reactions, leukopenia (decrease in the level of leukocytes in the blood), agranulocytosis (a sharp decrease in the number of granulocytes in the blood), paresthesia (numbness in the extremities), tachycardia ( palpitations).

Contraindications. Diseases of the hematopoietic system, kidneys, Graves' disease (thyroid disease), hypersensitivity to sulfonamides.

Release form. Powder; tablets in a package of 10 pieces of 0.3 g and 0.5 g; 5% liniment in a package of 50 g; ointment 10% in a package of 30 g.

Storage conditions. List B. In a dry, dark place.

STREPTOCIDA LINIMENT 5% (LinimentumStreptocidi5%)

Indications for use. To accelerate the healing of infected wounds, burns of I and II degrees, boils (purulent inflammation of the hair follicle of the skin that has spread to surrounding tissues), carbuncles (acute diffuse purulent-necrotic inflammation of several nearby sebaceous glands and hair follicles), with superficial pyoderma (purulent inflammation of the skin) , acne vulgaris, impetigo (superficial inflammation of the skin, characterized by the appearance of abscesses that dry out with the formation of crusts) and other pyoinflammatory skin diseases.

Method of application and dose. Before prescribing the drug to the patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Liniment is applied to the lesion (under a gauze bandage) 1-2 times a day.

Side effects and contraindications are the same as for streptocide.

Release form. In tubes or glass jars of 30 g.

Storage conditions. In a dry, cool place; banks - in a place protected from light.

"SUNOREF" OINTMENT (Unguentum "Sunoreph")

Indications for use. Acute and chronic rhinitis (inflammation of the nasal mucosa).

Method of application and dose. Locally (lubricate the mucous membranes of the nose).

Side effect. Allergic reactions are possible.

Contraindications. Hypersensitivity to sulfa drugs.

Release form. Ointment of the composition: streptocid - 5 g, norsulfazol - 5 g, sulfadimezin - 5 g, ephedrine hydrochloride - 1 g, camphor - 3 g, eucalyptus oil - 5 drops, ointment base - up to 100 g, in a package of 15 g.

Storage conditions. In a cool place.

Streptocid is also part of the drug osarcid.

STREPTOCID SOLUBLE (Streptocidumsolubile)

Pharmachologic effect. Sulfanilamide drug. (See Streptocide).

Indications for use. Epidemic, cerebrospinal meningitis (purulent inflammation of the meninges), erysipelas, tonsillitis, cystitis (inflammation of the bladder), pyelitis (inflammation of the renal pelvis), colitis (inflammation of the large intestine), wound infection. The purpose of the drug is especially indicated for vomiting or unconsciousness of the patient.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity of the microflora to it that caused the disease in this patient. Subcutaneously, intramuscularly up to 100 ml of 1-1.5% solution 2-3 times a day; intravenously up to 20-30 ml of 2%, 5% or 10% solution.

Side effects and contraindications are the same as for streptocide.

Release form. Powder.

Storage conditions. List B. In a dry, dark place.

Streptocide soluble is also part of the drug inhalipt.

SULGIN (Sulginum)

Synonyms: Sulfaguanidine, Abiguanil, Aseptiguamidine, Ganidan, Guamid, Guanicil, Guasept, Neosulfonamide, Resulfon, Sulfaguanisan, etc.

Pharmachologic effect. Sulfanilamide drug. Sulgin is very slowly absorbed. The main amount of the drug taken orally is retained in the intestine and excreted in the feces. It is an effective remedy for the treatment of intestinal infections. Similar in action to phthalazole.

Indications for use. Bacillary dysentery, colitis (inflammation of the large intestine) and enterocolitis (inflammation of the small and large intestine) with diarrhea, carriage of shigella and typhoid fever bacillus, preparation for intestinal surgery.

Method of application and dose. Inside, 1-2 g 6-5-4-3 times a day (on the first day - 6 times; in 2 and 3 - 5; in 4 - 4, and in 5 - 3 times a day).

Children under 3 years old - 0.2 g / kg per day in 3 divided doses for 7 days; children over 3 years old - 0.4-0.75 g (depending on age) 4 times a day.

For the prevention of postoperative complications in the intestines, 0.05 g / kg every 8 hours for 5 days before surgery and 7 days after surgery.

Higher doses for adults inside: single 2 g, daily 7 g.

Side effect. Possible nausea, vomiting, crystalluria (the presence of salt crystals in the urine).

Contraindications. Hypersensitivity to sulfonamides, impaired renal function.

Release form.

Storage conditions. List B. In a dry, light-protected place.

SULFADIMESIN (Sulfadimezinum)

Synonyms: Sulfadimidine, Diazyl, Diazol, Dimetazil, Dimethyldebenal, Dimethylsulfadiazine, Dimethylsulfapyrimidine, Primazine, Sulfadimerazine, Sulfamethazine, Sulfamesatil, Sulfamesatin, Sulmet, Sulfadimethylpyrimidine, Superseptil.

Pharmachologic effect. Sulfanilamide drug. Active against pneumococci, meningococci, streptococci, gonococci, Escherichia coli and some other microorganisms.

Method of application and dose. Before prescribing a drug to a patient, it is desirable to determine the sensitivity

to him the microflora that caused the disease in this patient. Inside, 1 g 4-6 times a day. With pneumonia and meningitis, 2 g is prescribed for the first appointment; children at the rate of 0.1 g / kg for the first dose, then 0.25 g / kg every 4, 6, 8 hours. Higher doses for adults inside: single 2 g, daily 7 g.

For the treatment of dysentery in adults on the 1st-2nd day - 1 g 6 times; on the 3rd-4th day - 1 g 4 times; on the 5-6th day - 1 g 3 times a day. The course dose is 25-30 g. After a 5-6 day break, repeat the course of treatment for 5 days, the course dose is 21 g of the drug. With dysentery for children under 3 years old - up to 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.

Side effect. Nausea, vomiting, allergic reactions, leukopenia (a decrease in the level of leukocytes in the blood), agranulocytosis (a sharp decrease in the number of granulocytes in the blood), crystalluria (the presence of salt crystals in the urine) are possible.

Contraindications. Hypersensitivity to sulfonamides, diseases of the hematopoietic system, impaired renal function.

Release form. Powder; tablets of 0.5 g in a package of 10 pieces.

Storage conditions. List B. In a place shielded from the light.

Sulfonamides are synthetic chemotherapeutic agents that are derivatives of sulfanilic acid. They were the first highly effective antibacterial agents.

Mechanism of action:

Sulfonamides are structurally similar to para-aminobenzoic acid (PABA) and are its competitive antagonists.

As a result, the synthesis of nucleic acids is inhibited, as a result, the growth and reproduction of microorganisms is suppressed (bacteriostatic effect). With prolonged use of SA, resistance of microorganisms develops to them. Cross Stability.

The antibacterial effect of sulfonamides decreases or disappears in the presence of blood, pus, tissue decay products, where there are noticeable amounts of PABA.

Spectrum of antimicrobial action:

real spectrum(as a result of resistance of microorganisms) antimicrobial action of sulfonamides: many strains of pneumococci (not all!), pathogens of dysentery, paratyphoid, chlamydia, pneumocystis.

They are practically do not work for infections caused by staphylococci, most strains of streptococci, gonococci, meningococci, Haemophilus influenzae, Pseudomonas aeruginosa, Proteus, Enterococci, Klebsiella, Escherichia coli.

Classification of sulfonamides:

Depending on the pharmacokinetics, sulfonamides are divided into four groups.

1. Sulfonamides, which are well absorbed from the gastrointestinal tract (resorbable):

1.1. Short-acting drugs (T 0.5 less than 10 hours):

Sulfadimezin

Sulfacyl

norsulfazol

streptocide

1.2. Intermediate-acting drugs (10-24 hours):

Sulfazin

Sulfamethoxazole

1.3. Long-acting drugs (more than 24 hours):

Sulfadimethoxine

Sulfapyridazine

1.4. Extra long acting drugs (60 - 120 hours):

Sulfalen

2. Sulfonamides, slowly and incompletely absorbed in the gastrointestinal tract (non-resorbable):

Ftalazol

Sulgin

3. Sulfonamides for local use:

Sulfacil - sodium (sulfacetamide, albucid)

Sulfapyridazine - sodium

Sulfargin (Sulfadiazine, Dermazin)

4. Combined sulfonamides

A) Salazosulfanamides

Salazopyridazine (salazodine)

Salazosulfapyridine

Salazodimethoxine

Mesalazine (salofalk)

B) Combined preparations with trimetaprim:

Co-trimoxazole (biseptol, septrin, bactrim, etc.)

Fansidar

Pharmacokinetics:

All sulfonamides are partially absorbed in the stomach, most - in the small intestine. In the blood, peak concentrations are usually created after 2-6 hours.

In high concentrations, sulfonamides are found in the kidneys, lungs, liver, skin; they are not found in the bones. Sulfonamides penetrate well through the BBB. In sufficiently high concentrations (50-80% of the content in the blood), they are present in liquid media, as well as fetal tissues (a teratogenic effect is possible). Sulfonamides are poorly soluble in the usual acid reaction of urine. In the renal tubules, they can precipitate as crystals and block the lumen. This complication can be prevented and significantly accelerate the excretion of drugs by artificially increasing the pH of the urine by taking soda, alkaline mineral waters.

Indications for use:

1) infections of the eyes, respiratory tract, genital tract caused by chlamydia (erythromycin and tetracyclines remain the drugs of choice);

2) primary (previously untreated) acute urinary tract infections, especially in non-pregnant women (uroantiseptics and bactericidal antibiotics are still considered the drugs of choice);

3) ulcerative colitis, enteritis and other inflammatory bowel diseases, most strains of dysentery pathogens have developed resistance, and antibiotics are preferred;

4) shallow burns, wounds - only in liniments and ointments (mafenide or silver sulfadiazine).

In the treatment of pneumococcal and other pneumonias, meningitis - only after confirmation of the sensitivity of the flora and in combination with other chemotherapeutic agents.

Complications:

1. An overdose of the drug is more common in children and the elderly, especially after 10-14 days of treatment.

Symptoms of CNS intoxication - dizziness, headaches, depression, nausea, vomiting (outpatient admission is contraindicated for drivers of transport);

Kidney damage - pain in the lumbar region, oliguria, protein and red blood cells in the urine, microcrystals of drugs and their metabolites

On the part of the blood: hemolytic or aplastic anemia, granulocytopenia, thrombocytopenia.

2. Hypersensitivity occurs in an average of 5% of patients. Drugs can cause allergic reactions by any route of administration, but faster and brighter - after taking well-absorbed drugs. The most common skin manifestations of allergies (various rashes, limited dermatitis, generalized dermatitis, exudative erythema, necrotic lesions, etc.). Other manifestations include fever, vascular lesions, and anaphylactic shock.

Group characteristics:

1. SA, well absorbed from the gastrointestinal tract - are prescribed for systemic treatment of infections caused by susceptible microorganisms.

2. Sulfonamides, slowly and incompletely absorbed in the gastrointestinal tract and creating a high concentration in the small and large intestines, are prescribed only inside. It is used to treat acute enteritis, bacillary dysentery, colitis and enterocolitis caused by sensitive aerobic flora. Prescribed according to the schemes, the course of treatment is on average 5-7 days.

3. Sulfonamides for topical use - they are most successfully used in eye practice. Albucid is used in the form of 30% eye drops, eye ointment. The drug is prescribed for inflammatory diseases of the conjunctiva, blepharitis, purulent corneal ulcers, trachoma caused by chlamydia.

For local use, a large number of soluble sodium salts of sulfonamides are produced: streptocide, norsulfazol, etazol, sulfapyridazine, etc. In the form of solutions, in aerosols, in liniments, ointments, powders, they are used to treat purulent wounds, long-term non-healing ulcers, burns, pustular skin diseases , bedsores, etc. Pre-wounds and the affected surface must be washed from pus and treated with an antiseptic. Most solutions of sulfonamides have a strongly alkaline reaction and, when applied to damaged tissues, cause sharp and prolonged (within 1-3 hours) pain. Better tolerated and more effective than others 10% mafenide ointment and 1% sulfargin ointment (silver sulfadiazine, dermazin). Contraindication: history of allergic reactions to sulfonamides. The duration of treatment is from 1 to 3 weeks.

Powdering wounds and burns with sulfonamide powders is not only ineffective, but also undesirable, since pus accumulates under the resulting crust, and the process develops in depth.

4. Salazosulfanamides - compounds of a number of drugs with salicylic acid. Most widely used salazopyridazine (salazodin) in the form of tablets, suppositories, suspensions. They are used to treat polymicrobial (nonspecific) colitis, including ulcers.

5. Combined SA with trimethaprim. As a result of the combination, not only the mutual potentiation of the antimicrobial action occurs, but the spectrum also expands; in high therapeutic doses, combined preparations exhibit a bactericidal effect against a number of microbes. The resistance of microorganisms to combined preparations develops slowly.

Its optimal ratio in combination with sulfamethoxazole (biseptol drug) is 1: 5. At the same time, peak concentrations of drugs in the blood are reached after 1-4 hours.

Indications for the use of biseptol and its analogues:

1) bacterial infections of the respiratory tract - pneumonia, acute bronchitis and exacerbation of chronic; used for the treatment and prevention of secondary infections;

2) pneumonia caused by pneumocysts - biseptol is considered the drug of choice; in severe cases, an intravenous infusion of the solution is indicated;

3) infections of the lower and upper urinary tract (in the absence of bacteriuria);

4) enteritis and enterocolitis caused by dysenteric bacillus, bacteria of the typhoid paratyphoid group, cholera vibrios and other microflora, including those that have acquired resistance to ampicillin and levomycetin;

5) inflammation of the middle ear, meningitis (in combination with other chemotherapeutic agents), sepsis (in / in);

Side effects.

- allergic reactions.

Hematopoietic disorders.

Principles of sulfanilamide therapy:

1. Start treatment as early as possible with a loading dose.

2. Assign confirmation doses following the shock according to the scheme, based on the pharmacokinetics of the drug.

3. Conduct a course of treatment lasting at least 5-10 days, without interrupting or shortening the course of treatment.

Gross formula

Pharmacological group of the substance Sulfanilamide

Nosological classification (ICD-10)

CAS code

Characteristics of the substance Sulfanilamide

Refers to short-acting sulfa drugs. Sulfanilamide is a white, odorless, crystalline powder with a slightly bitter taste and a sweet aftertaste. Easily soluble in boiling water (1:2), difficult - in ethanol (1:37), soluble in solutions of hydrochloric acid, caustic alkalis, acetone (1:5), glycerin, propylene glycol; practically insoluble in ether, chloroform, benzene, petroleum ether. Molecular weight - 172.21.

It is also used in the form of sodium methane sulfate (Streptocide soluble) - white crystalline powder; soluble in water, practically insoluble in organic solvents.

Pharmacology

The mechanism of the antimicrobial action of sulfanilamide is associated with the antagonism of PABA, with which it has a chemical similarity. Sulfanilamide is captured by the microbial cell, prevents the incorporation of PABA into dihydrofolic acid and, in addition, competitively inhibits the bacterial enzyme dihydropteroate synthetase (the enzyme responsible for the incorporation of PABA into dihydrofolic acid), as a result, the synthesis of dihydrofolic acid is disrupted, the formation of metabolically active tetrahydrofolic acid from it, which is necessary for the formation of purines and pyrimidines, stops the growth and development of microorganisms (bacteriostatic effect).

Active against gram-positive and gram-negative cocci (including streptococci, pneumococci, meningococci, gonococci), Escherichia coli, Shigella spp., Vibrio cholerae, Clostridium perfringens, Bacillus anthracis, Corynebacterium diphtheriae, Yersinia pestis, Chlamydia spp., Actinomyces israelii, Toxoplasma gondii.

When applied topically, it promotes rapid healing of wounds.

When taken orally, it is rapidly absorbed from the gastrointestinal tract. C max in the blood is created in 1-2 hours and decreases by 50%, usually in less than 8 hours. Passes through histohematic, including the BBB, placental barriers. It is distributed in tissues, after 4 hours it is found in the cerebrospinal fluid. It is acetylated in the liver with loss of antibacterial properties. It is excreted mainly (90-95%) by the kidneys.

There is no information on carcinogenic, mutagenic and fertility effects during long-term use in animals and humans.

Previously, sulfanilamide was used orally for the treatment of tonsillitis, erysipelas, cystitis, pyelitis, enterocolitis, prevention and treatment of wound infection. Sulfanilamide (Streptocide soluble) has been used in the past as 5% aqueous solutions for intravenous administration, which were prepared ex tempore; currently used only in the form of liniment for external use.

Application of the substance Sulfanilamide

locally: tonsillitis, purulent-inflammatory skin lesions, infected wounds of various etiologies (including ulcers, cracks), furuncle, carbuncle, pyoderma, folliculitis, erysipelas, acne vulgaris, impetigo, burns (I and II degrees).

Contraindications

Hypersensitivity (including to other sulfone and sulfonamides), diseases of the hematopoietic system, anemia, renal / hepatic insufficiency, congenital deficiency of glucose-6-phosphate dehydrogenase, azotemia, porphyria.

Application restrictions

Pregnancy, breastfeeding.

Use during pregnancy and lactation

With systemic absorption, sulfanilamide can quickly pass through the placenta and be found in the blood of the fetus (the concentration in the blood of the fetus is 50-90% of that in the mother's blood), and also cause toxic effects. The safety of sulfanilamide during pregnancy has not been established. It is not known whether sulfonamide can cause fetal harm when taken by pregnant women. In experimental studies in rats and mice treated during pregnancy with certain short, intermediate and long-acting sulfonamides (including sulfanilamide) orally at high doses (7-25 times the therapeutic oral dose for humans), a significant increase in the incidence of cleft palate and other fetal bone malformations.

Penetrates into breast milk, can cause nuclear jaundice in newborns.

Side effects of the substance Sulfanilamide

allergic reactions; with prolonged local use in large quantities - a systemic effect: headache, dizziness, paresthesia, tachycardia, nausea, vomiting, dyspepsia, leukopenia, agranulocytosis, crystalluria, cyanosis.

Interaction

Myelotoxic drugs increase hematotoxicity.

Routes of administration

locally.

Substance Precautions Sulfanilamide

With prolonged use, it is necessary to periodically conduct a peripheral blood test.

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