Sulfonamides drugs new generation list. Sulfanilamide (Sulfanilamide)

international name: Sulfadiazine (Sulfadiazine)

Dosage form:

Pharmachologic effect:

Indications:

Kelfizin

International name: Sulfalene (Sulfalene)

Dosage form: solution for intravenous and intramuscular injection, tablets

Pharmachologic effect: Antimicrobial bacteriostatic agent, ultra-long-acting sulfanilamide. The mechanism of action is due to competitive antagonism ...

Indications: Infections caused by susceptible microorganisms: pneumonia, bronchitis, gonorrhea, sepsis, toxoplasmosis, sinusitis, otitis media, inflammatory diseases...

mafenide acetate

International name: Mafenide (Mafenide)

Dosage form: ointment for external use

Pharmachologic effect: Mafenide acetate is a sulfanilamide, a broad-spectrum antimicrobial drug, active in vitro against gram-positive and gram-negative ...

Indications: Infected burns, purulent wounds, bedsores, trophic ulcers.

norsulfazol

International name: Sulfathiazole (Sulfathiazole)

Dosage form: tablets

Pharmachologic effect:

Indications: Infections caused by susceptible microorganisms: diseases of the respiratory and biliary tract.

Salazodimethoxine

Dosage form: tablets

Pharmachologic effect: Antibacterial agent, has an anti-inflammatory effect. It breaks down in the intestine, forming 5-aminosalicylic acid and sulfadimethoxin, ...

Indications: non-specific ulcerative colitis, Crohn's disease; rheumatoid arthritis (basic therapy).

Silvederm

International name: Sulfadiazine (Sulfadiazine)

Dosage form: topical aerosol, topical cream, topical ointment

Pharmachologic effect: Sulfonamide drug for local application. It has a wide spectrum of antibacterial action, which includes almost all microorganisms, ...

Indications: Infected superficial wounds and burns with weak exudation, bedsores, trophic and long-term non-healing ulcers (including stump wounds), abrasions, skin grafting.

Silverdin

International name: Sulfadiazine (Sulfadiazine)

Dosage form: topical aerosol, topical cream, topical ointment

Pharmachologic effect: Sulfanilamide drug for topical use. It has a wide spectrum of antibacterial action, which includes almost all microorganisms, ...

Indications: Infected superficial wounds and burns with weak exudation, bedsores, trophic and long-term non-healing ulcers (including stump wounds), abrasions, skin grafting.

streptocide

International name:

Dosage form:

Pharmachologic effect: Antimicrobial bacteriostatic agent, sulfanilamide. The mechanism of action is due to competitive antagonism with PABA, inhibition of dihydropteroate synthetase, ...

Indications:

Streptocid soluble

International name: Sulfanilamide (Sulfanilamide)

Dosage form: liniment, topical ointment, topical powder, tablets

Pharmachologic effect: Antimicrobial bacteriostatic agent, sulfanilamide. The mechanism of action is due to competitive antagonism with PABA, inhibition of dihydropteroate synthetase, ...

Indications: Local treatment: tonsillitis, infected wounds of various etiologies, burns (stage I-II), folliculitis, furuncle, carbuncle, acne vulgaris, impetigo, other purulent-inflammatory processes of the skin, erysipelas.

Preparations of this group are synthetic antimicrobial agents, derivatives of sulfanilic acid. All of them have a common formula.

Sulfanilamide drugs suppress the vital activity of both various cocci (streptococci, except for the green one, staphylococci, pneumococci, gonococci, meningococci), and rods (enteropathogenic Escherichia coli, shigella, salmonella, klebsiella, yersinia, etc.). Sulfamonometoxin and sulfapyridazine also affect Toxoplasma, Chlamydia, Proteus, Plasmodium malaria, Nocardia. Sulfonamide preparations often cause healing effect, in the treatment of diseases caused by antibiotic-resistant strains of these pathogens.

Sulfonamides are bacteriostatic drugs. They are chemically similar to para-aminobenzoic acid (PABA) and can be taken up by microbes instead. At the same time, the formation of folic acid, which ensures the vital activity of cells (the synthesis of nucleic acids and proteins), is disrupted. Sulfonamides have no effect on microorganisms that themselves synthesize PABA, as well as on resting forms of microbes. Folic acid is not synthesized in human tissues, therefore, sulfonamides do not interfere with its metabolism.

The affinity of microorganisms for para-aminobenzoic acid is higher than for sulfonamides, so the concentration of these drugs in the blood should exceed that of PABA by tens and hundreds of times. The use of insufficient doses of sulfonamides can lead to the selection of microbial strains resistant to them.

For practical purposes, the following classification of sulfonamides can be used.

1. Sulfonamides used in systemic infections:

Short-acting: streptocid, etazol, norsulfazol, sulfadimezin, sulfacyl (albucid);

Medium duration of action: sulfazine, sulfamethoxazole;

Long-acting: sulfapyridazine, sulfamonometoxin, sulfadimethoxine;

Superlong action: sulfalene (kelfisin);

Combined preparations with trimethoprim: bactrim (biseptol), groseptol, poteseptil, etc.

2. Used for gastrointestinal infections: sulgin, ftalazol, phtazine, salazosulfapyridazine, salazosulfapyridine, salazosulfadimethoxin.

3. Used for urinary tract infections: urosulfan, sulfadimethoxine, sulfalene.

4. Used in eye practice: sodium sulfacyl, sodium sulfapyridazine.

For parenteral administration, sulfonamides, which dissolve well in water, can be used. For this purpose, short-acting preparations are used: sodium etazol, sodium sulfacyl, soluble streptocide and a super-long-acting drug - sulfalene-meglumine.

Most sulfonamides are well absorbed from the intestines (with the exception of specially weighted drugs used to treat gastrointestinal infections). In plasma, they are associated with proteins, but relatively easily penetrate into various tissues.

The excretion of sulfonamides is carried out mainly by glomerular filtration, therefore, the more the drug is bound to plasma proteins, the slower its elimination occurs. Some sulfonamides, especially sulfalene, may be reabsorbed from the urine. These features determine the rate of excretion of drugs from the body.

The choice of the drug depends on its pharmacokinetic characteristics, as well as on the pathogen, localization and course of the infectious process.

For the treatment of systemic infections, sulfonamides are used, which are well absorbed from the intestine. They easily penetrate from blood plasma into tissues, creating effective concentrations in them, including in the lungs, in pleural, synovial, ascitic fluids. Sulfapyridazine penetrates into the cerebrospinal fluid better than other drugs, sulfadimethoxine practically does not penetrate. The remaining sulfonamides penetrate moderately into the cerebrospinal fluid. Sulfonamides penetrate the placenta well, creating concentrations in the amniotic fluid, blood and tissues of the fetus and newborn that are sufficient for the manifestation of an antimicrobial effect. In mother's milk, the concentration of drugs is equal to that in her blood plasma, and infant may receive sulfanilamide in an amount sufficient to cause undesirable effects.

In the liver, sulfonamides undergo biotransformation by acetylation and (or) glucuronidation. Acetylated metabolites are poorly soluble in water, so they can precipitate in the urine, disrupting the patency of the kidney tubules. To prevent this complication, it is necessary to drink each portion of sulfanilamide with a glass of alkaline water (soda solution, borzhom) to alkalize urine and increase the solubility of acetylated metabolites. This rule must be observed when prescribing streptocide, norsulfazol, sulfadimezin, etazol, sulfacyl, sulfazin. When prescribing long-acting and super-long-acting drugs, crystalluria is rarely observed, which is associated with taking these drugs in smaller doses, and also with the fact that these sulfonamides partially form esters with glucuronic acid, which are highly soluble in water. Sulfadimetoksin undergoes glucuronidation and is excreted in the urine unchanged, so there is no danger of the formation of its crystals in the urine. Urosulfan is excreted unchanged by the kidneys, creating high concentrations in the urine, so it is used to treat urinary tract infections. For the treatment of biliary tract infections, sulfadimethoxine, sulfapyridazine and sulfalene are used, which are found in bile in an active form and in high concentration.

Sulfonamides, well absorbed from the intestines, are used to treat diseases respiratory tract, tonsillitis, pharyngitis, otitis, meningitis, infectious lesions of the skin.

Currently widely used combined preparations sulfonamides containing trimethoprim bactrim (biseptol, cotrimoxazole, bacterial), groseptol, poteseptil, sulfatone, etc. Trimethoprim is an inhibitor of dihydrofolate reductase, which converts dihydrofolic acid into active tetrahydrofolic (folinic) acid, which transports one-carbon fragments necessary for the synthesis of purine and pyrimidine bases, some amino acids and proteins. (In human tissues, dihydrofolate reductase is less sensitive to trimethoprim than the enzyme in a microorganism.) Trimethoprim has a pronounced antimicrobial effect and is an active synergist of sulfonamides. All combined preparations, in which it is included together with sulfonamides, are characterized by a wide spectrum of action. They inhibit the activity of gram-positive and gram-negative microorganisms: various cocci, rods (including Haemophilus influenzae and legionella), chlamydia, pneumocysts, actinomycetes and some anaerobes. Mycobacterium tuberculosis, pale treponema, Pseudomonas aeruginosa, mycoplasmas are resistant to them.

Poorly absorbed from the intestines sulfonamides (sulgin, ftalazol, phtazin) are used to treat fetal infections: salmonellosis, typhoid fever, dysentery, gastroenteritis, etc. These drugs are retained in the intestine, where they undergo hydrolysis with the elimination of the active sulfanilamide part of the molecule, which has an antimicrobial effect. Salazosulfanilamide - drugs used mainly for ulcerative colitis and Crohn's disease. They accumulate in the connective tissue of the intestine, where they are gradually broken down, forming active sulfanilamide and aminosalicylic acid, which has an anti-inflammatory effect.

The use of sulfonamides in normal doses is rarely accompanied by complications. The undesirable effect of drugs often occurs in people with impaired renal excretory function, in children of the first months of life, as well as when prescribing excessively high doses and (or) with their long-term use.

Sulfonamides can displace difenin, synthetic antidiabetic agents (sulfonylurea derivatives), indirect anticoagulants (neodicoumarin, etc.) from the connection with blood plasma proteins, which leads to an increase in the free fraction of drugs. As a result, conventional doses of these medicinal substances may cause undesirable effects.

Sulfonamides should not be prescribed to newborns with hyperbilirubinemia, as they can prevent the binding of bilirubin to plasma proteins, which increases the risk of bilirubin encephalopathy. Sometimes in newborns and infants, sulfonamides lead to the oxidation of the iron ion of fetal hemoglobin, which causes the appearance of methemoglobin, impaired oxygen transport, hypoxia and acidosis. To prevent this complication, it is simultaneously necessary to prescribe drugs with antioxidant properties, for example, ascorbic acid with glucose.

In addition to these complications, sulfonamides can cause allergic reactions, usually occurring in the form of rashes, dermatitis, leukopenia. Sometimes the appearance of polyneuritis and dysfunction of the central nervous system are noted.

Combined preparations containing trimethoprim in children with folic acid deficiency can disrupt the conversion of folic acid into its active metabolite - tetrahydrofolic acid, which leads to a deficiency of the named vitamin and is accompanied by neutro- and (or) thrombocytopenia, disorders of the gastrointestinal tract (nausea, vomiting, diarrhea), sometimes glossitis, stomatitis, pseudomembranous colitis are observed. To eliminate and prevent complications, you can take the drug folinic acid - calcium folinate.

Sulfonamides are a broad group antimicrobials. The first drug of the group - streptocide, is considered the world's first synthetic antibacterial agent.

By modifying the original compound, many antibiotic derivatives were obtained, most of which have lost their significance today due to the developed resistance of microorganisms.

Nonetheless, modern drugs groups of sulfonamides are widely used to treat various infections, especially combined ones such as Biseptol, external creams and ointments or eye drops Albucid. Many drugs that were previously used to treat human diseases are now relevant for veterinary practice.

Yes, sulfonamides are a separate group of antibiotics, although initially, after the invention of penicillin, they were not included in the classification. For a long time, only natural or semi-synthetic compounds were considered “real”, and the first sulfanilamide synthesized from coal tar and its derivatives were not. But later the situation changed.

Today, sulfonamides are a large group of bacteriostatic antibiotics, active against a wide range of pathogens of infectious and inflammatory processes. Previously, sulfonamide antibiotics were often used in various fields of medicine. But over time, most of them have lost their significance due to mutations and bacterial resistance, and combined drugs are now used more often for medicinal purposes.

Classification of sulfonamides

It is noteworthy that sulfa drugs were discovered and began to be used for medicinal purposes much earlier than penicillin. The therapeutic effect of some industrial dyes (in particular, prontosil or "red streptocide") was discovered by the German bacteriologist Gerhard Domagk in 1934. Thanks to this compound, active against streptococci, he cured his own daughter, and in 1939 he won the Nobel Prize.

The fact that it is not the coloring part of the prontosil molecule that has a bacteriostatic effect, but aminobenzenesulfamide (aka “white streptocide” and the simplest substance in the group of sulfonamides) was discovered in 1935. It was by modifying it that all other drugs of the class were subsequently synthesized, many of which are widely used in medicine and veterinary medicine. Possessing a similar spectrum of antimicrobial action, they differ in pharmacokinetic parameters.

Some drugs are quickly absorbed and distributed, while others take longer to digest. There is a difference in the duration of excretion from the body, due to which the following types of sulfonamides are isolated:

• Short-acting, half-life of which is less than 10 hours (streptocide, sulfadimidine).
• Medium duration, whose T 1 / 2 10-24 hours - sulfadiazine, sulfamethoxazole.
• Long-acting (T half-life from 1 to 2 days) - sulfadimethoxine, sulfamonomethoxine.
• Ultra-long - sulfadoxine, sulfamethoxypyridazine, sulfalene - which are excreted for longer than 48 hours.

This classification is used for oral medicines, however, there are also sulfonamides that are not adsorbed from the gastrointestinal tract (phthalylsulfathiazole, sulfaguanidine), as well as silver sulfadiazine intended exclusively for topical use.

Complete list of sulfonamides

List of used in modern medicine sulfonamide antibiotics with trade names and indicating the release form is presented in the table:

All antibiotics sulfonamides from the list of drugs are currently being produced. Some sources also mention other drugs in this group (for example, Urosulfan), which have long been discontinued. In addition, there are sulfonamide antibiotics used exclusively in veterinary medicine.

The mechanism of action of sulfonamides

Indications for the use of sulfonamides

Stopping the growth of pathogens (gram-negative and gram-positive microorganisms, some protozoa) is carried out due to the similarity of the chemical structure of para-aminobenzoic acid and sulfanilamide. PABA is necessary for the cell to synthesize the most important developmental factors - folate and dihydrofolate. However, when its molecule is replaced by a sulfanilamide structure, this process is disrupted and the growth of the pathogen stops.

All drugs are absorbed in the digestive tract at different rates and degrees of assimilation. Those that are not adsorbed in the gastrointestinal tract are indicated for treatment intestinal infections. Distribution in tissues is quite uniform, metabolism is carried out in the liver, excretion - mainly through the kidneys. In this case, depo-sulfonamides (acting for a long time and super-long) are absorbed back into the renal tubules, which explains the long half-life.

Allergy to sulfonamides

The high degree of allergenicity of combined preparations-sulfonamides is the main problem of their use. Of particular difficulty in this regard is the treatment of pneumocystis pneumonia in HIV-infected people, since Biseptol is the drug of choice for them. However, it is in this category of patients that the likelihood of developing allergic reactions on co-trimoxazole increases tenfold.

Therefore, if the patient is allergic to sulfonamides, Biseptol and other combined preparations based on co-trimoxazole are contraindicated. Intolerance is manifested most often by a small generalized rash, fever may also occur, the composition of the blood (neutro- and thrombocytopenia) may change. In especially severe cases - Lyell and Stevens-Johnson syndromes, erythema multiforme, anaphylactic shock, angioedema.

Allergy to sulfonamides requires the abolition of the drug that caused it, as well as the use of antiallergic drugs.

Other side effects of sulfonamides

Many drugs in this group are toxic and poorly tolerated, which was the reason for the reduction in their use after the discovery of penicillin. In addition to allergies, they can cause dyspeptic disorders, headaches and abdominal pain, apathy, peripheral neuritis, hematopoietic disorders, bronchospasm, polyuria, renal dysfunction, toxic nephropathy, myalgia and arthralgia. In addition, the risk of developing crystalluria increases, so it is necessary to drink plenty of medicine and drink more alkaline water.

Interaction with other drugs

Cross-resistance with other antibiotics in sulfonamides is not observed. At joint admission with oral hypoglycemic agents and indirect coagulants, their action is enhanced. It is not recommended to combine sulfonamide antibiotics with thiazide diuretics, rifampicin and cyclosporine.

What is the difference between sulfonamides and sulfonamides

Despite the consonant names, these chemical compounds are fundamentally different. Sulfonamides (ATX code C03BA) are diuretics - diuretics. The drugs of the group are prescribed for hypertension, edema, gestosis, diabetes insipidus, obesity and other pathologies accompanied by the accumulation of fluid in the body.

ANTRIMA (Antrima)

Pharmachologic effect. Combined sulfanilamide drug. Sulfadiazine and trimethoprim have bacteriostatic (preventing the growth of bacteria) and bactericidal (destroying bacteria) effects, 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 susceptible microorganisms, including respiratory tract infections, urinary tract infections, gastrointestinal tract infections (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 used in patients with diabetes it should be borne in mind 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, Primazole, 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.

Combination preparation containing two active ingredients: sulfanilamide drug sulfamethoxazole and 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, coli, protea; 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 Bladder), pyelitis (inflammation of the renal pelvis), chronic pyelonephritis (inflammation of the tissue of the kidney and renal pelvis), prostatitis (inflammation of the prostate gland), 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. At 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. Possible nausea, vomiting, diarrhea (diarrhea), allergic reactions, nephropathy ( common name some kidney diseases). 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 children. early age. 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 to disappear acute manifestations infections (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 old - 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 down), 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 a burn or wound surface, burning, pain can be observed, lasting from "/2 to 1-3 hours; with severe pain prescribe analgesics (painkillers).

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 dosage form, dehydrated by freezing in a vacuum) 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); at 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. Intravenously administered in cases where the possibility of introducing nosulfazole into the stomach is excluded (for example, after surgery on the gastrointestinal intestinal 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).

Also used in the form eye drops(10% solution, 2 drops 3-4 times a day) with 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 ulceration of unknown cause) in the active stage, mainly in mild to moderate severe forms 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 drugs in therapy 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. Sick with light forms diseases, the drug is prescribed 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 available therapeutic effect continue treatment at this dose for 5-7 days, then reduce the dose by 2 times and continue treatment 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 common methods treatment 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 in case of damage to the rectum and sieve, in the preoperative period and after subtogal colectomy (after removal of part 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. AT acute stage diseases are prescribed 1 suppository 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 that when using sulfonamides and salicylates: allergic phenomena, leukopenia (decrease in the level of leukocytes in the blood), dyspeptic disorders (digestive disorders), sometimes a slight decrease in the level of hemoglobin (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 rectal administration 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 nonspecific ulcerative colitis ( chronic inflammation colon with ulceration of unknown cause). 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 the subsidence clinical symptoms diseases are prescribed maintenance doses (1.5-2.0 g per day) for several months.

For children, salazosulfapyridine is prescribed in smaller doses: at the age of 5-7 years - 1/2-1 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 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 preparation. 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(disease thyroid gland), 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 adjacent 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 ulcers that dry out with the formation of crusts) and other purulent-inflammatory 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. Sharp 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: streptocide - 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, sore throat, cystitis (inflammation of the bladder), pyelitis (inflammation of the renal pelvis), colitis (inflammation of the colon), 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. Is effective tool for the treatment of intestinal infections. Similar in action to phthalazole.

Indications for use. Bacterial 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 prevention postoperative complications on the intestines at 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. It is 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 antimicrobial agents, derivatives of para (π)-aminobenzenesulfamide - sulfanilic acid amide (para-aminobenzenesulfonic acid). Many of these substances have been used as antibacterial drugs since the mid-twentieth century.

Aminobenzenesulfamide - the simplest compound of the class - is also called white streptocide and is still used in medicine. A somewhat more complex sulfanilamide prontosil (red streptocide) was the first drug in this group and, in general, the world's first synthetic antibacterial drug.

The antibacterial properties of prontosil were discovered in 1934 by G. Domagk. In 1935, scientists at the Pasteur Institute (France) found that it was the sulfanilamide part of the prontosil molecule that had the antibacterial effect, and not the structure that gave it color. It was found that the "active principle" of red streptocide is a sulfanilamide, which is formed during metabolism (streptocide, white streptocide). The red streptocide went out of use, and based on the sulfanilamide molecule, it was synthesized a large number of its derivatives, some of which are widely used in medicine.

pharmachologic effect

Sulfonamides have a bacteriostatic effect. Being similar in chemical structure to PABA, they competitively inhibit the bacterial enzyme responsible for the synthesis of dihydrofolic acid, a precursor of folic acid, which is the most important factor in the vital activity of microorganisms. In environments containing a large amount of PABA, such as pus or tissue decay products, the antimicrobial effect of sulfonamides is significantly weakened.

Some topical sulfonamide preparations contain silver (silver sulfadiazine, silver sulfathiazole). As a result of dissociation, silver ions are slowly released, providing a bactericidal effect (due to binding to DNA), which is independent of the concentration of PABA at the site of application. Therefore, the effect of these drugs persists in the presence of pus and necrotic tissue.

Activity spectrum

Initially, sulfonamides were active against a wide range of gram-positive (S.aureus, S.pneumoniae, etc.) and gram-negative (gonococci, meningococci, H.influenzae, E.coli, Proteus spp., Salmonella, Shigella, etc.) bacteria. In addition, they act on chlamydia, nocardia, pneumocysts, actinomycetes, malarial plasmodia, toxoplasma.

Currently, many strains of staphylococci, streptococci, pneumococci, gonococci, meningococci, enterobacteria are characterized by a high level of acquired resistance. Enterococci, Pseudomonas aeruginosa and most anaerobes are naturally resistant.

Preparations containing silver are active against many pathogens of wound infections - Staphylococcus spp., P.aeruginosa, E.coli, Proteus spp., Klebsiella spp., Candida fungi.

Pharmacokinetics

Sulfonamides are well absorbed in the gastrointestinal tract (70-100%). Higher concentrations in the blood are observed when using short drugs (sulfadimidine, etc.) and medium duration(sulfadiazine, sulfamethoxazole) action. Long-term sulfonamides (sulfadimethoxine, etc.) and super-long-term (sulfalene, sulfadoxine) action are bound to blood plasma proteins to a greater extent.

Widely distributed in tissues and body fluids, including pleural effusion, peritoneal and synovial fluid, exudate of the middle ear, chamber moisture, tissues of the urogenital tract. Sulfadiazine and sulfadimethoxine pass through the BBB, reaching 32-65% and 14-30% serum concentrations in the CSF, respectively. Pass through the placenta and enter breast milk.

Metabolized in the liver, mainly by acetylation, with the formation of microbiologically inactive, but toxic metabolites. Excreted by the kidneys about half unchanged, with an alkaline urine reaction, excretion increases; small amounts are excreted in the bile. At kidney failure cumulation of sulfonamides and their metabolites in the body is possible, leading to the development of a toxic effect.

With topical application of sulfonamides containing silver, high local concentrations are created. active components. Systemic absorption through the damaged (wound, burn) surface of the skin of sulfonamides can reach 10%, silver - 1%.

Kinds

Sulfonamides are divided into the following groups:

1. Drugs that are completely absorbed in the gastrointestinal tract and rapidly excreted by the kidneys: sulfatiazole (norsulfazol), sulfatidol (etazol), sulfadimidine (sulfadimezin), sulfacarbamide (urosulfan).
2. Drugs that are completely absorbed into gastrointestinal tract, but slowly excreted by the kidneys (long-acting): sulfamethoxypyridazine (sulfapyridazine), sulfamonometoxin, sulfadimethoxine, sulfalene.
3. Drugs that are poorly absorbed from the gastrointestinal tract and act in the intestinal lumen: phthalylsulfathiazole (phthalazole), sulfaguanidine (sulgin), phthalylsulfapyridazine (phtazine), as well as sulfonamides conjugated with salicylic acid Salazosulfapyridine, tesalazine (salazopyridazine), salazodimethoxine.
4. Topical preparations: sulfanilamide (streptocid), sulfacetamide (sulfacyl sodium), silver sulfadiazine (sulfargin) - the latter, dissolving, releases silver ions, which provide an antiseptic and anti-inflammatory effect.
5. Combined preparations: co-trimoxazole (bactrim, biseptol) containing trimethoprim with sulfamethoxazole or sulfamonomethoxin with trimethoprim (sulfatone) are also antimicrobial agents with a wide spectrum of action.

The first and second groups, well absorbed in the gastrointestinal tract, are used to treat systemic infections; the third - for the treatment of intestinal diseases (drugs are not absorbed and act in the lumen of the digestive tract); the fourth - locally, and the fifth (combined drugs with trimethoprim) are effective in respiratory and urinary tract infections, gastrointestinal diseases.

Indications for the use of sulfonamides

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• respiratory tract infections (acute and chronic bronchitis, bronchiectasis, lobar pneumonia, bronchopneumonia, pneumocystis pneumonia, pleural empyema, lung abscess)
• ENT infections ( otitis media sinusitis, laryngitis, tonsillitis, pharyngitis, tonsillitis)
• scarlet fever
• urinary tract infections (pyelonephritis, pyelitis, epididymitis, cystitis, urethritis, salpingitis, prostatitis, gonorrhea in men and women, chancre, lymphogranuloma venereum, inguinal granuloma)
• gastrointestinal infections (dysentery, cholera, typhoid fever, salmonella carriers, paratyphoid fever, cholecystitis, cholangitis, gastroenteritis caused by enterotoxic strains of E. coli)
• skin and soft tissue infections (acne, furunculosis, pyoderma, abscess, wound infections)
• osteomyelitis (acute and chronic)
• brucellosis (acute)
• sepsis
• peritonitis
• meningitis
• brain abscess
• osteoarticular infections
• South American blastomycosis
• malaria
• whooping cough (as part of complex therapy).
• folliculitis, erysipelas
• impetigo
• burns 1 and 2 degrees
• pyoderma, carbuncles, boils
• purulent-inflammatory processes on the skin
• infected wounds of various origins
• tonsillitis
• eye diseases.

Instructions for use Sulfanilamide (method and dosage)

10% and 5% ointment, liniment or powder is applied to the affected surfaces or to a gauze bandage. Dressings are done once a day.

In the treatment of deep wounds, the agent is introduced into the wound cavity in the form of a crushed (to dust) sterilized powder. Dosage from 5 to 15 grams. Parallel carry out systemic treatment prescribed oral antibiotics.

Also, the drug is often combined with ephedrine, sulfathiazole and benzylpenicillin for the treatment of rhinitis. It is used in powder form. The powder (thoroughly ground) is inhaled through the nose.

Inside Sulfanilamide can be used in a daily dosage of 0.5 to 1 gram, distributed over 5-6 doses. For children, it is recommended to adjust the daily dosage depending on age.

The maximum amount of antibiotic that can be taken per day is 7 grams, at a time - 2 grams.

Side effects of sulfa drugs

Of the sometimes observed side effects, dyspeptic and allergic are more often noted.

Allergy

For allergic reactions prescribed antihistamines and calcium preparations, especially gluconate and lactate. With minor allergic phenomena, sulfonamides are often not even canceled, which is necessary with more pronounced symptoms or more persistent complications.

Impact on the Central Nervous System

Possible phenomena from the central nervous system:

• headache;
• dizziness, etc.

Blood disorders

Sometimes there are changes in the blood:

• anemia;
• agranulocytosis;
• leukopenia, etc.

crystalluria

All side effects may be more persistent with the introduction of long-acting drugs that are more slowly excreted from the body. Because these poorly soluble drugs are excreted in the urine, they may form crystals in the urine. Acid urine may cause crystalluria. To prevent this phenomenon, sulfa drugs should be taken with a significant amount of alkaline drink.

Sulfonamides contraindications

The main contraindications to the use of sulfa drugs are: increased individual sensitivity of individuals to sulfonamides (usually to the entire group).

This may be indicated by anamnestic data on previous intolerance to other drugs of various groups.

Toxic effect on the blood with other drugs

Do not take sulfonamides with other medicines that have a toxic effect on the blood:

• chloramphenicol;
• griseofulvin;
• amphotericin preparations;
• arsenic compounds, etc.

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), as well as 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. AT experimental studies in rats and mice treated during pregnancy with certain short, medium 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 malformations has been shown bones in the fetus. Penetrates into breast milk, can cause nuclear jaundice in newborns.

What can not be consumed with sulfonamides?

Sulfonamides are incompatible with such drugs, due to the fact that they increase their toxicity:

• amidopyrine;
• phenacetin;
• nitrofuran derivatives;
• salicylates.

Sulfonamides are incompatible with certain foods containing the following chemicals:

• sulfur:
• eggs.
• folic acid:
• tomatoes;
• beans;
• beans;
• liver.

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. Domestic sulfonamides will be inexpensive, while imported drugs are much more expensive. Approximate price for sulfa drugs:

• Sulfanilamide (White streptocide) 250 g Switzerland 1900 rub.
• Biseptol 20 pcs. 120 mg Poland 30 rub.
• Sinersul 100 ml Republic of Croatia 300 rub.
• Sumetrolim 20 pcs. 400 mg Hungary 115 rub.