home Auditorium 8 The effect of sulfonamide drugs. Sulfonamide drugs for children. Cost of sulfa drugs

The effect of sulfonamide drugs. Sulfonamide drugs for children. Cost of sulfa drugs

The familiar sulfonamides have proven themselves since ancient times, because they were discovered even before the advent of penicillin. Currently, these drugs are medical activities have lost some of their value as they have been replaced by more effective modern medicines. However, they are still indispensable for the treatment of some diseases.

What are sulfonamides?

Sulfonamides are antimicrobial drugs manufactured using modern technologies and related to sulfanilic acid derivatives.

Antibiotic of this series short acting- streptocide. He is one of the first representatives of this group antibacterial agents. Has a wide spectrum of action. The drug is synthesized in the form of a white crystalline powder, odorless and tasteless, with a sweet aftertaste.

The antibiotic can also be found in the form of sodium sulfonamide - white powder, highly soluble in water. Also available in tablet form. Sodium sulfanilamide is capable of inhibiting the vital functions of rods and cocci, influencing malaria, Proteus, nocardia, plasmodia, toxoplasma, chlamydia, and has a bacteriostatic effect. Sulfonamide drugs are used to treat diseases caused by resistant to antibacterial drugs pathogens.

Classification of sulfonamides

Sulfonamides - which are inferior in activity to modern antibacterial drugs. They are highly toxic, which means that their range of indications is very limited. Sulfonamide drugs Depending on their properties and pharmacokinetics, they are classified into 4 groups:

Sulfonamides, which are quickly and easily absorbed from gastrointestinal tract. They are used for systemic antibacterial therapy infectious diseases caused by microorganisms sensitive to sulfonamides: “Sulfadimethoxin”, “Etazol”, “Sulfadimizin”, “Sulphaurea”, “Sulfamethizole”.

Sulfonamides, which are slowly and incompletely absorbed from the gastrointestinal tract, creating high concentration in the small and large intestines: “Ftazin”, “Sulgin”, “Etazol-sodium”, “Ftalazol”.
Sulfonamides, which are used superficially or externally to obtain a local effect. For treatment eye diseases have proven themselves to be effective: sulfacyl sodium (“Sulfacetamide”, “Albucid”), silver sulfadiazine (“Dermazin”), “Streptocidal ointment 10%”, “Mafenide acetate ointment 10%”.
Salazosulfonamides, which are nitrogen compounds of sulfonamides and salicylic acid: “Salazomethoxin”, “Sulfasalazine”. The list of sulfonamide drugs is quite extensive.

Main mechanisms of action

The choice of a drug for treating a patient is determined by the properties of the pathogen, because the main mechanism of action of sulfonamides is the inhibition of sensitive microorganisms in cells that synthesize folic acid. It is because of this that some medications, such as Methionomix or Novacon, cannot be combined with them, because they can weaken the effect of sulfonamides. The key action is to disrupt the metabolism of microorganisms, as well as block their growth and reproduction.

Release forms

All sulfonamide drugs have the same formula, but different pharmacokinetics depending on the structure. There are release forms in the form of a solution for intravenous administration: “Streptocide”, “Sodium sulfacetamide”. Some are for intramuscular injection: “Sulfadoxin”, “Sulfalene”. Combination dosage forms of sulfonamides can be administered by both routes. Children are prescribed sulfa drugs local application or in the form of tablets: “Cotripharm”, “Co-trimoxazole-Rivopharm”.

Indications

The main indications for the use of the sulfonamides group are:

acne ( acne vulgaris), inflammation hair follicle, erysipelas;
burns of I and II degrees;
pyoderma, boils, carbuncles;
of different nature;
purulent-inflammatory skin diseases;
tonsillitis;
eye diseases;
bronchitis.

List of sulfa drugs

Sulfonamides are drugs that, depending on the period of circulation, are divided into drugs: fast, medium, long-acting (long-term) and extra-long-acting. It is very difficult to compile a list of all drugs in this group, so below we provide a table with only long-acting sulfonamides:

"Arghedin" - main active substance: silver sulfadiazine. Indications for use are superficial infected burns and wounds, abrasions.

"Argosulfan" is the main active substance: silver sulfadiazine. Burns of various etiologies and all degrees, purulent wounds, frostbite, abrasions, cuts, infected dermatitis, bedsores, trophic ulcers.
"Norsulfazole" - the main active substance: norsulfazole. Infectious diseases caused by pneumococcus, staphylococcus, hemolytic streptococcus, Escherichia coli, gonococcus, gonorrhea, pneumonia, dysentery, cerebral meningitis.
"Oriprim" - the main active substance: sulfamethoxazole. Indications - infectious diseases genitourinary organs, ENT organs, gastrointestinal tract, respiratory organs, skin and soft tissues.
"Pyrimethamine" - the main active substance: pyrimethamine. Preventive and curative therapy malaria, primary polycythemia, toxoplasmosis.
"Prontosil" (red streptocide) - main active substance: sulfonamide. Indications will be puerperal sepsis, streptococcal pneumonia, erysipelas epidermis.

List of combination sulfonamide drugs

The use of sulfonamides is quite common. Many strains of microorganisms have learned to mutate and adapt to antibiotics. And therefore, representatives of medicine have created combined sulfonamide drugs, in which the main active ingredient is combined with trimethoprim. Here is a table of these sulfodrugs:

How to treat with sulfonamides? Data can be prescribed both locally and internally. The instructions for the use of sulfonamide drugs state that children under one year of age should take the drug 0.05 g, children from two to five years old - 0.3 g, children from six to twelve years old - 0.6 g. Adults are advised to take 0.5-1.3 g about five times a day. The general course of therapy is prescribed by a doctor and depends on the severity of the disease. Most often, the duration of use of the drug is a week. Each sulfonamide drug should be taken with alkaline water. Also, the patient's diet should include foods containing sulfur to prevent crystallization and maintain general reaction urine.

The effect of sulfonamides is not always positive. There may also be negative reactions from the body.

Side effects

During prolonged and uncontrolled use of sulfonamide drugs, side effects may occur. These include various allergic reactions of the body, headaches, dizziness, nausea, vomiting. When absorbed systemically into the blood, sulfonamide drugs are able to pass through the placenta and then penetrate into the blood of the pregnant child, thereby causing toxic effect. It is because of this that pregnant women are advised to be very careful when using it and strictly follow the treatment regimen prescribed by a specialist.

Contraindications to the use of sulfonamide medicines are:

individual increased sensitivity mostly active active substance drug;
low hemoglobin content;
violation of hemoglobin synthesis;
liver or kidney dysfunction;
diseases hematopoietic organs and blood;
azotemia.

We discussed the mechanism of sulfonamides above.

Cost of sulfa drugs

Sulfonamide drugs can be purchased at a pharmacy or ordered through an online store. The advantage of the latter method of purchase is that when ordering several drugs at the same time, the difference in price will be noticeable, because to purchase one drug you will have to overpay for delivery. Sulfa drugs are much cheaper domestic production. Here is the approximate price:

“Sulfanilamide” (white streptocide) with a volume of 250 g of Swiss production will cost about 1900 rubles.
"Biseptol" (pack of 20 tablets of 120 mg each) produced in Poland will cost about 30 rubles.

"Sinersul" with a volume of 100 ml of Croatian production will cost 300 rubles.
“Sumetrolim” (pack of 20 tablets of 400 mg each) produced in Hungary will cost 115 rubles.

Now we know that these are sulfonamides.

Sulfonamides, familiar to people, have long proven themselves, since they appeared even before the history of the discovery of penicillin. Today, these drugs in pharmacology have partially lost their importance, since they are inferior in effectiveness modern medicines. However, they are indispensable in the treatment of certain pathologies.

What are sulfa drugs

Sulfanilamide (sulfonamides) include synthetic antimicrobial drugs that are derivatives of sulfanilic acid (aminobenzenesulfamide). Sodium sulfanilamide suppresses the vital activity of cocci and bacilli, affects nocardia, malaria, plasmodia, proteus, chlamydia, toxoplasma, and has a bacteriostatic effect. Sulfonamide drugs are medications prescribed to treat diseases caused by pathogens that are resistant to antibiotics.

Classification of sulfonamide drugs

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

Sulfonamides are rapidly absorbed from the gastrointestinal tract. They are prescribed for systemic treatment of infections that are caused by sensitive microorganisms: Etazol, Sulfadimethoxine, Sulfamethizole, Sulfadimidine (Sulfadimezin), Sulfcarbamide.
Sulfonamides, incompletely or slowly absorbed. They create in thick and small intestine high concentration: Sulgin, Ftalazol, Ftazin. Etazol sodium
Topical sulfonamides. Have proven themselves well in eye therapy: Sulfacyl sodium (Albucid, Sulfacetamide), Silver sulfadiazine (Dermazin), Mafenide acetate ointment 10%, Streptocide ointment 10%.
Salazosulfonamides. This classification of sulfonamide compounds with salicylic acid: Sulfasalazine, Salazomethoxine.

Mechanism of action of sulfonamide drugs

The choice of medication to treat a patient depends on the properties of the pathogen, because the mechanism of action of sulfonamides is to block sensitive microorganisms in the cells of folic acid synthesis. For this reason, some medications, for example, Novocaine or Methionomixin, are incompatible with them, since they weaken their effect. Key Principle the effects of sulfonamides - disruption of the metabolism of microorganisms, suppression of their reproduction and growth.

Indications for the use of sulfonamides

Depending on their structure, sulfide drugs have a common formula, but different pharmacokinetics. There are dosage forms for intravenous administration: Sodium sulfacetamide, Streptocide. Some drugs are administered intramuscularly: Sulfalen, Sulfadoxine. Combination drugs are used in both ways. For children, sulfonamides are used topically or in tablets: Co-trimoxazole-Rivopharm, Cotripharm. Indications for the use of sulfonamides:

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

List of sulfa drugs

According to the period of circulation, sulfonamides antibiotics are divided into: short, medium, long and extra long exposure. It is impossible to list all drugs, so this table shows long-acting sulfonamides used to treat many bacteria:

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

Combined sulfonamide drug

Time does not stand still, and many strains of microbes have mutated and adapted. Doctors found new way fight against bacteria - they created a combined sulfonamide drug in which antibiotics are combined with trimethoprim. List of such sulfopreparations:

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

Sulfonamide drugs for children

Since these drugs are broad-spectrum drugs, they are also used in pediatrics. Sulfonamide preparations for children are produced in tablets, granules, ointments and solutions for injections. List of medications:

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

Instructions for use of sulfonamides

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

Side effects of sulfonamide drugs

With prolonged or uncontrolled use, side effects of sulfonamides may occur. These are allergic reactions, nausea, dizziness, headaches, vomiting. When absorbed systemically, sulfodrugs can cross the placenta and then be found in the fetal blood, causing toxic effects. For this reason, the safety of medications during pregnancy is questionable. The physician should take into account this chemotherapeutic effect when prescribing them to pregnant women and during lactation. Contraindications to the use of sulfonamides are:

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

Price for sulfonamide drugs

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

Video: what are sulfonamides

The information presented in the article is for informational purposes only. The materials of the article do not call for self-treatment. Only a qualified doctor can make a diagnosis and make recommendations for treatment based on individual characteristics specific patient.

Sulfonamides, familiar to people, have long proven themselves, since they appeared even before the history of the discovery of penicillin. Today, these drugs have partially lost their importance in pharmacology, since they are inferior in effectiveness to modern medicines. However, they are indispensable in the treatment of certain pathologies.

Classification of sulfonamide drugs

Sulfonamides are rapidly absorbed from the gastrointestinal tract. They are prescribed for systemic treatment of infections that are caused by sensitive microorganisms: Etazol, Sulfadimethoxine, Sulfamethizole, Sulfadimidine (Sulfadimezin), Sulfcarbamide.
Sulfonamides, incompletely or slowly absorbed. They create a high concentration in the large and small intestines: Sulgin, Ftalazol, Ftazin. Etazol sodium
Topical sulfonamides. Well proven in eye therapy: Sulfacyl sodium (Albucid, Sulfacetamide), Silver sulfadiazine (Dermazin), Mafenide acetate ointment 10%, Streptocide ointment 10%.
Salazosulfonamides. This classification of sulfonamide compounds with salicylic acid: Sulfasalazine, Salazomethoxine.

Mechanism of action of sulfonamide drugs

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

Indications for the use of sulfonamides

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

List of sulfa drugs

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

Combined sulfonamide drug

Time does not stand still, and many strains of microbes have mutated and adapted. Doctors have found a new way to fight bacteria - they have created a combined sulfonamide drug, which combines antibiotics with trimethoprim. List of such sulfopreparations:

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

Sulfonamide drugs for children

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

Instructions for use of sulfonamides

Side effects of sulfonamide drugs

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

Price for sulfonamide drugs

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

Video: what are sulfonamides

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

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

The antimicrobial properties of sulfonamide drugs are significantly (20-100 times) potentiated and approach the bactericidal effect when combined with trimethoprim, which is a specific inhibitor of bacterial folate reductase. It must be taken into account that in environments with a high content of PABA, for example, in the focus of purulent tissue melting, the antimicrobial activity of sulfonamides sharply decreases.

Range antimicrobial action sulfa drugs include:

— gram-positive microorganisms (streptococci, staphylococci, clostridia, anthrax bacillus, actinomycetes). It should be noted that currently a significant number of staphylococcal strains have acquired resistance to these drugs;
- gram-negative microorganisms ( coli, Shigella, Salmonella, Haemophilus influenzae, Bacteroides, 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, and pseudomonads are sensitive to them.

When taken systemically, sulfonamide drugs can cause dyspepsia (nausea, vomiting), headache, and allergic reactions (rash, dermatitis, fever). At long-term use possible development of leukopenia, thrombocytopenia, agranulocytosis. A likely side effect is the loss of crystals in the kidneys (especially for the drugs sulfadimezin, norsulfazole, sulfapyridazine, sulfamonomethoxine). The danger of crystalluria is greatly reduced by using an alkaline drink. Therefore, it is advisable to simultaneously administer 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 deficiency conditions (diseases of the hematopoietic organs, pregnancy, old age).

General classification of sulfonamide drugs

Drugs that are well absorbed from the gastrointestinal tract:

A) short-acting: streptocide (sulfanilamide, white streptocide); sulfadimezin (sulfadimidine); etazol (sulfaethidol); norsulfazole (sulfathiazole); urosulfan (sulfa-urea);

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

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

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

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

Preparations for topical use: sulfacyl sodium (sulfaietamide); silver sulfadiazine (dermazin, flamazin).

IV. Combined sulfonamide drugs:

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

B) drugs containing sulfadimezin and trimethoprim: proteceptil (potesetta);

C) drugs containing sulfamonomethoxine and trimethoprim: sulfatone.

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

— pharmacotherapy of deep caries. Streptocide and norsulfazole, together with antibiotics and enzymes, are included in 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 surgical method treatment of pulpitis (norsulfazole or streptocide in combination with antibiotics monomycin or neomycin);

— acute periodontitis(30% solution of albucid along with antibiotics and antiseptics);

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

- treatment of acute odontogenic infection (locally - 30% sodium sulfacyl solution; systemically - any sulfonamide that is 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% sodium sulfacyl solution for irrigation of aphthous and ulcerative surfaces).

Inhalipt(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. 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 and remove plaque from eroded surfaces. It should be kept in the oral cavity for 5-7 minutes; Irrigation should be carried out 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, Sinersul, Biseptol, Berlocid, Groseptol, Septrin, Sumetrolim.

pharmachologic effect: is a combination drug containing sulfamethoxazole and trimethoprim in a ratio of 5:1. 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 sulfonamide drugs. The drug is effective against coccal flora, but is ineffective against Pseudomonas aeruginosa and spirochetes.

Indications: used for surgical infections.

Mode of application: prescribed internally. The 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, with chronic infections- 1 tablet 2 times a day. Children from 2 to 5 years old are recommended to take 2 tablets (0.12 g each) per single dose, 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, nephropathies, leukopenia, agranulocytosis. : see Streptocide.

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

Release form: tablets of 0.12 and 0.48 g, in a package of 20 pieces (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 pieces (content of sulfamethoxazole and trimethoprim 800 mg and 160 mg); 100 ml syrup in a bottle complete with a dosage spoon (5 ml of syrup contains 200 mg of sulfamethoxazole and 40 mg of trimethoprim).

Storage conditions: list B.

Sulfadimethoxine(Sulfadimethoxinum).

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

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

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

Storage conditions: list B.

Sulfanilamide(Sulfanilamidum). Synonym: Streptocidum.

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

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

Mode of application: in dentistry it is used mainly topically in the form of powder, ointment or liniment. Apply 5-15 g of sterile powder to the affected surface or inject into the wound. Currently, it is rarely used systemically.

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

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

Contraindications: For topical use - known allergy to sulfonamides. For systemic use- hypersensitivity to sulfonamides, pregnancy, lactation, blood diseases. Systemic use should be used with caution in patients with liver and kidney diseases (necessary dynamic observation for indicators of liver and kidney function).

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

Storage conditions: in a cool place, protected from light.

Sulfapyridazine(Sulfapyridazinum), Synonym: Sulfamethoxypyridazine.

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

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

Mode of application: prescribed internally. Doses for adults are 1-2 g for the first dose, depending on the severity of the disease, in subsequent 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 for 2-3 days after the temperature drops. For children under 13 years of age, the initial dose is 25 mg/kg body weight, in subsequent days - 12.5 mg/kg.

Side effect: in isolated cases, dyspepsia and allergic reactions are possible.

Interaction with other drugs: at simultaneous administration with erythromycin, lincomycin, novobiocin, fusidine, tetracycline, antibacterial activity is mutually enhanced, the spectrum of action is expanded; with rifampicin, streptomycin, monomycin, kanamycin, gentamicin, nitroxyline - 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 0.5 g.

Storage conditions: in a place protected from light.

Sulfathiazole(Sulfathiazole). Synonym: Norsulfazole (Norsulfasolum).

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

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

Mode of application: prescribed externally for applications to the mucous membrane and as part of gingival dressings, pastes for the treatment of pulpitis and periodontitis. Taken orally for acute infectious and inflammatory diseases.

At 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. Duration of treatment - 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. For the first dose, a double dose is given.

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 the effect of the latter increases; with oxacillin, the activity of the antibiotic decreases. Incompatible with iron salts and heavy metals. See also Sulfanilamide.

Contraindications: do not use in case of increased individual sensitivity to sulfonamides, diseases of the blood system, diffuse toxic goiter, kidney diseases, 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, E. 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 until epithelization, in the form of a solution - for washing periodontal pockets.

Side effect: Rarely appears. Possible local irritation when using high concentrations.

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

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

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

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

Sulfonamides instructions for children

Pharmacological action of sulfonamides:

Depending on the chemical structure, sulfonamides are characterized by unequal pharmacokinetics. All drugs can be prescribed orally. Sulfonamide drugs used for gastrointestinal infections are practically not absorbed, so their kinetic parameters are not considered. By the way, according to the instructions, they are prescribed in a frequency of 4–6 times a day.

There are dosage forms of sulfonamides for intravenous (streptocide, sulfacyl, norsulfazole, etazol, sulfalene) and intramuscular (streptocide, sulfalene) administration. Drugs combined with trimethoprim can be administered by both routes. Sometimes sulfonamides are used topically for children (eye practice, burns, etc.).

Indications for the use of sulfonamides:

Absorption of sulfonamides occurs from small intestine, they have high bioavailability (70-90%). Time of occurrence maximum concentration in the blood plasma - 2-4 hours. At the same time, they are 50-90% bound to blood plasma proteins (the exceptions are streptocide - 12% and sulfacyl - 22%). Moreover, sulfonamide drugs have a very high affinity for blood proteins, so they can displace other drugs, increasing their free, “working” fraction.

These drugs (especially long- and extra-long-acting drugs) penetrate well into the lungs, adenoids and tonsils, tissues and fluids of the middle and inner ear, pleural, synovial and ascitic fluid, through the placental barrier and into mother's milk. IN cerebrospinal fluid The best sulfonamide is sulfapyridazine, and the worst is sulfadimethoxine. In purulent and necrotic foci, the effectiveness of sulfonamides is significantly lower, since they contain a lot of PABA.

Biotransformation of sulfonamides occurs at all stages: epithelium of the gastrointestinal tract, liver, kidneys. It should be noted that the resulting metabolites do not have antimicrobial activity, but can provoke side effects.

Classification of drugs by duration of action

Sulfonamide drugs of short and medium duration of action undergo a process of acetylation in the mucous membrane of the gastrointestinal tract, liver and kidneys. In this case, metabolites are formed, which are acidic environment crystallize and precipitate, irritating the intestinal mucosa and damaging the epithelium of the kidney tubules. To reduce the crystallization of metabolites, these medications should be taken with water. alkaline drinking(5-10 g of sodium bicarbonate per day).

Long- and extra-long-acting sulfonamides undergo a process of glucuronidation in the liver. These metabolites do not precipitate in an acidic environment, but the diversion of liver enzymes to their formation can interfere with the glucuronidation of other drugs and endogenous substances (for example, bilirubin).

Excretion of sulfonamides

Excretion of short- and medium-acting sulfonamides in unchanged and acetylated forms is carried out mainly by the renal route due to glomerular filtration. If endogenous creatinine clearance is less than 20 ml/min, these drugs cannot be used.

Long- and ultra-long-acting drugs are almost completely reabsorbed in the kidneys. This main reason explaining them long stay in blood plasma. Thus, their half-life of elimination from the blood averages 36 and 48 hours, while for drugs with short and medium duration of action, an average of 8 and 16 hours, respectively.

Excretion of long- and extra-long-acting sulfonamides in modified and unchanged form is carried out by the liver. Moreover, sulfalene, sulfapyridazine and sulfadimethoxine are quite large quantities are in the bile in an active state. Multiplicity of appointment:

short-acting drugs – 4-6 times a day;
medium action – 3-4 times a day;
long-acting – 2 (sometimes 1) times a day;
extra-long-acting – 1 time per day.

Side effects of sulfonamides

Sulfanilamide drugs cannot be prescribed together with nephrotoxic and hematotoxic drugs, and they are also not recommended to be administered together with novocaine and novocainamide, since the latter are converted in the body into PABA, which enters into a competitive relationship with them.

Sulfonamides should be used very carefully together with drugs that they displace from binding to plasma proteins.

Side effects sulfonamides in this case can be quite serious. For example, with indirect anticoagulants (phenyline, neodicoumarin) there is a risk of bleeding; with methotrexate – risk of agranulocytosis; with synthetic antidiabetic agents (butamide, glibenclamide, bucarban) - the risk of hypoglycemic coma, etc.

In order to increase the spectrum of action and increase efficiency, sulfonamides can be combined with other bacteriostatic agents, and the free fraction of the latter in the blood, as a rule, increases, which in this case should be regarded as a positive phenomenon.

Sulfonamides in their own way chemical structure are similar to furosemide, butamide, diacarb, so if the patient reacts poorly to the above drugs, then one can expect intolerance to sulfonamide drugs.

Undesirable effects sulfonamides for children:

Nephrotoxicity. It may occur when using short-acting sulfonamides (except urosulfan, since it is not subject to acetylation).

Methemoglobinemia. It occurs more often in newborns and children in the first year of life, since they have special fetal hemoglobin and low activity of reducing enzymes (methemoglobin reductase, glutathione reductase, etc.). With this complication, the oxygen capacity of the blood decreases (hypoxia occurs, metabolic acidosis). To convert methemoglobin (ferric ion) into oxyhemoglobin (ferrous ion), reducing substances (methylene blue, ascorbic acid and etc.).

Methemoglobinemia and hemolytic anemia may occur in patients with congenital forms enzymopathies (glucose-6-phosphate dehydrogenase deficiency), especially when taking sulfonamides simultaneously with other oxidizing drugs (paracetamol, phenacetin, acetylsalicylic acid, furadonin, furazolidone, vikasol, butamide, quinidine, etc.).

Hyperbilirubinemia. Observed when using long- and extra-long-acting sulfonamides, more often:

in young children;
patients suffering from liver diseases;
patients with uridine diphosphoglucuronic transferase deficiency;
patients receiving simultaneously with sulfonamides other drugs that undergo glucuronidation reactions in the liver (for example, vikasol, a nicotinic acid, chloramphenicol, paracetamol, glucocorticoids, estrogens, androgens, triiodothyronine, adrenaline, etc.).

With this complication, there is a danger of developing bilirubin encephalopathy (convulsions, hyperkinesis, paralysis, possible death).

“Lupus erythematosus syndrome” can occur in people with genetically determined acetyltransferase deficiency. Clinical manifestations syndrome are as follows: headache, nausea, vomiting, tachycardia, rash, fever, effusion in pleural cavity, antinuclear antibodies are detected in the blood. This complication occurs when using sulfonamides that undergo acetylation, especially often when using sulfadimezine.

Allergic reactions: urticaria, itching, skin photosensitivity, rarely – Stevens-Johnson, Lyell and Lefller syndrome.

Neuritis (may occur muscle weakness without loss of sensitivity).

Folic acid deficiency syndrome:

neutropenia, leukopenia, thrombocytopenia;
dysfunctions of the gastrointestinal tract (nausea, vomiting, anorexia, diarrhea, stomatitis, etc.);
malnutrition;
disturbance of spermatogenesis.

This group of complications is most often caused by combination sulfonamide drugs with trimethoprim. These effects of sulfonamides can be prevented by taking folinic acid (calcium folinate, leucovorin), which is the active form of vitamin B.

Teratogenicity, especially when using drugs with trimethoprim.

Provoking porphyria - an atypical reaction that occurs when hereditary disorders metabolism. In patients, the formation of aminolevulenic acid and porphobilinogen in the liver increases, and their concentration in the urine of patients increases. The disease manifests itself in attacks intestinal colic, polyneuritis, muscle paralysis, mental disorders, epileptiform seizures, etc. In this case, sulfonamides must be discontinued.

List of sulfonamide drugs

There are 2 groups of sulfonamides:

I. Sulfonamide drugs used for systemic infections

Based on their duration of action they are divided into:

Short-acting drugs:

streptocide;
sulfacyl (albucid);
norsulfazole;
etazol;
urosulfan;
sulfadimezin;
sulfazoxazole;
sulfamerazine (not used independently, part of combination drugs).

Medium-acting drugs:

sulfazine;
sulfamethoxazole;
sulfamoxal.

Long-acting sulfa drugs for children:

sulfapyridazine;
sulfamonomethoxine;
sulfadimethoxine.

Ultra-long-acting drugs:

sulfalene (kelfisin, meglumine);
Sulfadoxine.

Drugs of different durations actions combined with trimethoprim:

poteseptil (sulfadimezin + trimethoprim);
groseptol (sulfamerazine + trimethoprim);
cotrimoxazole (synonym: bactrim, biseptol; consists of sulfamethoxazole + trimethoprim);
lidaprim (sulfametrol + trimethoprim);
sulfatone (sulfamonomethoxine + trimethoprim).

II. Medicines used for gastrointestinal tract infections:

sulgin;
phthalazole;
phthazine;
disulformine;
drugs combined with 5-aminosalicylic acid (salazosulfapyridine, salazopyridazine, salazodimethoxine).

Pharmacodynamics of sulfonamides

Sulfonamides are similar in their chemical structure to para-aminobenzoic acid (PABA), which, together with glutamic acid and pteridine, is part of folic acid (vitamin Bc), the role of which is to transfer one-carbon residues used for the formation nucleic acids and proteins. Some microorganisms can only use their own, independently synthesized (endogenous) folic acid for their life activity; such microorganisms make the mistake of including a sulfonamide drug in the structure of folic acid instead of PABA, so they synthesize defective vitamin B6.

Thus, sulfonamides have a mechanism of action that is competitive with PABA. It must be emphasized that it is not folic acid itself that works, but its reduced form - tetrahydrofolic (foleic, folinic) acid; turning into active form occurs under the influence of the enzyme dihydrofolate reductase. Trimethoprim, which is part of some combination drugs, inhibits the named enzyme. Therefore, the spectrum of action of such drugs is greater, since they can also influence microorganisms that can use exogenous folic acid for their vital functions.

The pharmacological effect is bacteriostatic. For drugs combined with trimethoprim, pharmacological effect– bactericidal. The spectrum of action is wide. Most sulfonamides affect Gr. “ – ” enterobacteria (Escherichia, some strains of Salmonella, Shigella, Yersinia, Klebsiella), Gr. “+” cocci (except enterococci and viridans streptococcus) and neisseri.

Sulfapyridazine and sulfamonomethoxine additionally have an effect on chlamydia, toxoplasma, proteus, nocardia and plasmodia malaria. Sulfonamide drugs combined with trimethoprim affect, in addition to the above-mentioned microorganisms, Haemophilus influenzae, Aeromonas, Legionella, actinomycetes and pneumocystis (the latter special microorganisms for a long time they were classified as protozoa; nowadays they are said to belong to yeast-like fungi).