Sulfanilamide (Sulfanilamide). Side effects of sulfonamides sulfonamides and sulfonamides list of drugs

Sulfonamides are the first class of AMPs for widespread use. In recent years, the use of sulfonamides in clinical practice has significantly decreased, since in terms of activity they are significantly inferior to modern antibiotics and are highly toxic. It is also significant that due to the long-term use of sulfonamides, most microorganisms have developed resistance to them.

Mechanism of action

Sulfonamides have a bacteriostatic effect. Being analogs of PABA in chemical structure, 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 life of microorganisms. In environments containing a large amount of PABA, such as pus or tissue degradation 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 does not depend on the concentration of PABA at the site of application. Therefore, the effect of these drugs persists in the presence of pus and necrotic tissue.

Spectrum of activity

Initially, sulfonamides were active against a wide range of gram-positive ( S.aureus, S.pneumoniae and others) and gram-negative (gonococci, meningococci, H.influenzae, E.coli, Proteus spp., salmonella, shigella, etc.) bacteria. In addition, they act on chlamydia, nocardia, pneumocystis, actinomycetes, malaria 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., mushrooms Candida.

Pharmacokinetics

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

They are widely distributed in tissues and body fluids, including pleural effusion, peritoneal and synovial fluids, middle ear exudate, chamber moisture, and 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 pass into 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 reaction of urine, excretion is enhanced; small amounts are excreted in the bile. With renal failure, the accumulation of sulfonamides and their metabolites in the body is possible, leading to the development of toxic effects.

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

Adverse reactions

Systemic drugs

Allergic reactions: fever, skin rash, itching, Stevens-Johnson and Lyell syndromes (more often with the use of long-acting and ultra-long-acting sulfonamides).

Hematological reactions: leukopenia, agranulocytosis, hypoplastic anemia, thrombocytopenia, pancytopenia.

Liver: hepatitis, toxic dystrophy.

CNS: headache, dizziness, lethargy, confusion, disorientation, euphoria, hallucinations, depression.

Gastrointestinal tract: abdominal pain, anorexia, nausea, vomiting, diarrhea, pseudomembranous colitis.

Kidneys: crystalluria, hematuria, interstitial nephritis, tubular necrosis. Crystalluria is more often caused by poorly soluble sulfonamides (sulfadiazine, sulfadimethoxine, sulfalene).

Thyroid: dysfunction, goiter.

Others: photosensitivity (increased skin sensitivity to sunlight).

Local preparations

Local reactions: burning, itching, pain at the site of application (usually short-term).

Systemic reactions: allergic reactions, rash, skin flushing, rhinitis, bronchospasm; leukopenia (with prolonged use on large surfaces).

Indications

Systemic drugs

Local preparations

Trophic ulcers.

Bed sores.

Contraindications

Allergic reactions to sulfa drugs, furosemide, thiazide diuretics, carbonic anhydrase inhibitors and sulfonylurea derivatives.

Should not be used in children under 2 months of age. The exception is congenital toxoplasmosis, in which sulfonamides are used for health reasons.

Renal failure

Warnings

Allergy. It is crossover to all sulfa drugs. Given the similarity in chemical structure, sulfonamides should not be used in patients allergic to furosemide, thiazide diuretics, carbonic anhydrase inhibitors, and sulfonylurea derivatives.

Pneumocystis pneumonia (treatment and prevention).

Contraindications

Allergic reactions to sulfonamide drugs, furosemide, thiazide diuretics, carbonic anhydrase inhibitors, sulfonylureas.

Should not be used in children under 2 months of age, except for children born to HIV-infected mothers.

Pregnancy.

Severe renal failure.

Severe liver dysfunction.

Megaloblastic anemia associated with a deficiency of folic acid.

Warnings

Allergy. If any rash occurs during the use of co-trimoxazole, it should be immediately canceled in order to avoid the development of severe skin toxic-allergic reactions. Co-trimoxazole should not be used in patients allergic to furosemide, thiazide diuretics, carbonic anhydrase inhibitors and sulfonylurea derivatives.

Pregnancy. The use of co-trimoxazole during pregnancy (especially in the first and third trimesters) is not recommended, since the sulfanilamide component can cause kernicterus and hemolytic anemia, and trimethoprim disrupts the metabolism of folic acid.

Lactation . Sulfamethoxazole passes into breast milk and may cause kernicterus in babies who are breastfeedingand hemolytic anemia in children with glucose-6-phosphate dehydrogenase deficiency. Trimethoprim disrupts the metabolism of folic acid.

Pediatrics. Sulfonamides compete with bilirubin for binding to plasma proteins, increasing the risk of kernicterus in newborns. In addition, since the liver enzyme systems are not fully formed in the newborn, elevated concentrations of free sulfamethoxazole may further increase the risk of developing kernicterus. In this regard, sulfonamides are contraindicated in children under 2 months of age. However, co-trimoxazole can be used in children from 4 to 6 weeks of age born to HIV-infected mothers.

Geriatrics. Elderly people have an increased risk of developing severe adverse skin reactions, generalized depression of hematopoiesis, thrombocytopenic purpura (the latter, especially when combined with thiazide diuretics). In case of impaired renal function, the risk of developing hyperkalemia increases. Strict monitoring is required and long-term courses of co-trimoxazole should be avoided if possible.

Impaired renal function. A slowdown in renal excretion leads to the accumulation of co-trimoxazole components in the body, which increases the risk of toxic effects. Co-trimoxazole should not be used in severe renal failure (creatinine clearance less than 15 ml / min). With impaired renal function, the risk of developing hyperkalemia increases.

Liver dysfunction. Slowing down the metabolism of sulfonamides with an increased risk of toxic effects. Possible development of toxic liver dystrophy.

Thyroid dysfunction. Caution is required when using in connection with the possible aggravation of thyroid dysfunction.

Hyperkalemia. The co-trimoxazole component, trimethoprim, can cause hyperkalemia, the risk of which increases in the elderly, with impaired renal function, with the simultaneous use of potassium preparations or potassium-sparing diuretics. In these groups of patients, the serum potassium content should be monitored, and if hyperkalemia develops, co-trimoxazole should be canceled.

Pathological changes in the blood. The risk of developing hematological adverse reactions increases.

Deficiency of glucose-6-phosphate dehydrogenase. High risk the development of hemolytic anemia.

Porphyria. The development of an acute attack of porphyria is possible.

AIDS patients. The risk of developing adverse reactions increases significantly in patients with AIDS.

Drug interactions

The sulfanilamide component can enhance the effect and / or toxic effect of indirect anticoagulants (coumarin or indandione derivatives), anticonvulsants (hydantoin derivatives), oral antidiabetic agents and methotrexate due to their displacement from the connection with proteins and / or weakening of their metabolism.

With simultaneous use with other drugs that cause bone marrow suppression, hemolysis, hepatotoxic effects, the risk of developing the corresponding toxic effects may increase.

When combined with co-trimoxazole, the effect of oral contraceptives may weaken and the frequency of uterine bleeding may increase.

With the simultaneous use of cyclosporine, it is possible to increase its metabolism, accompanied by a decrease in serum concentrations and effectiveness. At the same time, the risk of nephrotoxicity increases.

Phenylbutazone, salicylates and indomethacin can displace the sulfanilamide component from the bond with blood plasma proteins, thereby increasing its concentration in the blood.

Should not be combined with penicillins, as sulfonamides weaken their bactericidal effect.

Information for patients

Co-trimoxazole must be taken on an empty stomach with a full glass of water. Correctly use liquid dosage forms for oral administration (suspension, syrup).

Strictly adhere to the regimen of appointments throughout the course of treatment, do not skip the dose and take it at regular intervals. If a dose is missed, take it as soon as possible; do not take if it is almost time for the next dose; do not double the dose.

Do not use expired or degraded drugs as they may be toxic.

You should consult your doctor if there is no improvement within a few days or new symptoms appear.

Do not take any other medications without the advice of your doctor during treatment with co-trimoxazole.

Observe the storage rules, keep out of the reach of children.

Table. Preparations of the sulfonamide group and co-trimoxazole.
Main characteristics and application features

INN	Lecform LS	T ½, h *	Dosage regimen	Features of drugs
Sulfadimidine	Tab. 0.25 g and 0.5 g	3-5	Inside Adults: 2.0 g for the first dose, then 1.0 g every 4-6 hours Children older than 2 months: 100 mg / kg for the first dose, then 25 mg / kg every 4-6 hours For the prevention of plague (adults and children): 30-60 mg / kg / day in 4 divided doses	The drug is highly soluble, therefore it was previously widely used for infections with MEP
Sulfadiazine	Tab. 0.5 g	10	Inside Adults: 2.0 g for the first dose, then 1.0 g every 6 hours Children older than 2 months: 75 mg / kg for the first dose, then 37.5 mg / kg every 6 hours or 25 mg / kg every 4 hours (but not more than 6.0 g per day) For the prevention of plague (adults and children): 30-60 mg / kg / day in 4 steps	Better than other sulfonamides it penetrates the BBB, therefore it is preferable for toxoplasmosis. Not recommended for use with MEP infections, as it is poorly soluble
Sulfadimethoxine	Tab. 0.2 g	40	Inside Adults: 1.0-2.0 g on the first day, on the next 0.5-1.0 g, at one time Children over 2 months old: 25-50 mg / kg on the first day, then 12.5-25 mg / kg	High risk of developing Stevens-Johnson and Lyell's syndrome
Sulfalen	Tab. 0.2 g	80	Inside Adults: 1.0 g on the first day, on the next 0.2 g; or 2.0 g once a week	High risk of developing Stevens-Johnson and Lyell's syndrome. Not assigned to children
Silver sulfadiazine	Ointment 1% in tubes of 50 g	ND	Locally Apply to the affected surface 1-2 times a day	Indications: burns, trophic ulcers, bedsores
Silver sulfathiazole	Cream 2% in tubes of 40 g and in jars of 400 g	ND	Also	The same
Co-trimoxazole (Trimethoprim / sulfamethoxazole)	Tab. 0.12 g; 0.48 g and 0.96 g Sir., 0.24 g / 5 ml in a bottle. Rr d / in. 0.48 g in amp. 5 ml each	Trime- toprim 8-10 Sulfa- tags- sazol 8-12	Inside Adults: for infections of mild to moderate severity - 0.96 g every 12 hours; for the prevention of pneumocystis pneumonia - 0.96 g once a day Children over 2 months old: for infections of mild and moderate severity - 6-8 mg / kg / day ** in 2 divided doses; for the prevention of pneumocystis pneumonia - 10 mg / kg / day ** in 2 divided doses for 3 days every week I / O Adults: for severe infections - 8-10 mg / kg / day ** in 2-3 injections; with pneumocystis pneumonia - 20 mg / kg / day ** in 3-4 injections for 3 weeks Children older than 2 months: for severe infections, including pneumocystis pneumonia, - 15-20 mg / kg / day ** in 3-4 injections For intravenous administration, dilute at a ratio of 1:25 in 0.9% sodium chloride solution or 5% glucose solution. The introduction is carried out slowly - within 1.5-2 hours	Bactericidal action. The activity is mainly associated with the presence of trimethoprim. When prescribing, regional data on the sensitivity of microorganisms should be taken into account

* With normal liver function

** Calculation for body weight is based on trimethoprim

Chemically, sulfonamides are derivatives of sulfanilic acid amide. It is based on para-aminobenzenesulfonic acid.

All sulfonamides are odorless white or yellowish powders, some with a bitter taste. Most of them are poorly soluble in water, better in dilute acids and aqueous solutions of alkalis. Only sulfacil has good solubility.

Drugs in this group belong to chemotherapeutic agents with a wide antibacterial spectrum of action, because they suppress the vital activity of many species of Gr and Gr-bacteria: streptococci, staphylococci, meningococci, gonococci, bacteria of the entero-typhoid-dysentery group and many others. They are active against large viruses (pathogens of trachoma), coccidia, plasmodium malaria and toxoplasma, actinomycetes, etc.

Sulfanilamide preparations in low concentrations retard the growth and development of bacteria, that is, they act bacteriostatically. They have a bactericidal effect only when exposed to such high concentrations that are unsafe for the macroorganism.

The mechanism of the antimicrobial action of sulfonamides is associated with their competitive antagonism with para-aminobenzoic acid (PABA). PABA is incorporated into the structure of dihydrofolic acid, which is synthesized by many microorganisms. Due to its chemical affinity for PABA, sulfonamides prevent its inclusion in dihydrofolic acid. In addition, they competitively inhibit dihydropteroate synthetase. Violation of the synthesis of dihydrofolic acid reduces the formation of tetrahydrofolic acid from it, which is necessary for the synthesis of purine and pyrimidine bases. As a result, the synthesis of nucleic acids is inhibited, as a result of which the growth and reproduction of microorganisms is suppressed.

Some sulfonamides exhibit competitive antagonism in relation to other enzyme systems, in particular, they disrupt the process of decarboxylation of pyruvic acid, glucose oxidation.

Protein substances (pus, dead tissue) containing a large amount of PABA, as well as some drugs, the molecule of which contains the remainder of PABA (novocaine, anestezin), are inhibitors of the activity of sulfonamides.

To obtain a therapeutic effect, they must be prescribed in doses sufficient to prevent the possibility of using PABA contained in tissues by microorganisms. Taking sulfonamides in insufficient doses or stopping treatment too early can lead to the emergence of resistant strains of pathogens.

The effect of sulfonamides on the macroorganism (antipyretic effect, anti-inflammatory, stimulates the process of phagocytosis, increases the body's resistance to toxins) and the microorganism complement each other, providing a well-expressed therapeutic effect.

Most sulfonamides are readily absorbed from the gastrointestinal tract and rapidly accumulate in the blood, organs and tissues in bacteriostatic concentrations. The sodium salts of the preparations are very well absorbed. Some, difficult to absorb, are relatively long in the intestine in high concentrations and are excreted mainly with feces.

In the blood, organs and tissues, sulfonamides are in the form of free compounds and in a state bound to plasma proteins.

They are unevenly distributed in various organs and tissues. Most of them are found in the kidneys, lungs, walls of the stomach and intestines, heart, liver. Sulfonamides penetrate well through the placenta.

Most sulfonamides are relatively quickly eliminated from the body of animals. They are eliminated mainly by the kidneys, mammary, sweat, salivary, bronchial and intestinal glands, as well as the liver.

Sulfonamides are used to treat infectious diseases respiratory tract (tracheitis, bronchitis, pneumonia, purulent pleurisy, etc.), gastrointestinal diseases of various etiologies (dyspepsia, eimeriosis, dysentery, gastroenterocolitis, etc.); erysipelas, myt, postpartum sepsis, pyelitis, cystitis, salmonellosis, colibacillosis, pasteurellosis, wound and other infections.

Sulfanilamide preparations are low-toxic. However, long-term use of them in overestimated doses can lead to the development of undesirable, i.e., toxic effects: inhibition of the beneficial microflora of the gastrointestinal tract, cyanosis, leukopenia, anemia, B-avitaminosis, agranulocytosis, and general depression. With insufficient renal function or with the appointment of large doses of drugs, crystalluria phenomena may occur.

Contraindications for use: general acidosis, diseases of the hematopoietic system, hepatitis.

Classification of sulfonamides:

• 1. Drugs quickly and completely absorbed from the gastrointestinal tract (resorptive sulfonamides). They include streptocide, norsulfazole, sulfazine, sulfadimezin, etc.
• 2. Drugs that are poorly absorbed from the gastrointestinal tract and create a high concentration in the intestinal lumen (acting in the intestinal lumen). Phthalazole, sulgin, phtazine are referred to.
• 3. Drugs used topically (prevention and treatment of eye infections, wound infections, burns and wounds) - sodium sulfacyl, sulfargin.
• 4. Sulfonamides for special purposes - salazosulfapyridine, salazopyridazine (used in ulcerative colitis), sulfanthrol (antipyroplasmidic agent), diacarb (diuretic).
• 5. Combined preparations of sulfonamides with trimethoprim (trimethosul, trimerazine, etc.).

Sulfonamides of resorptive action differ in the duration of the antibacterial effect.

• 1. Preparations of short duration of action (4-6 hours). Streptocid norsulfazole, etazole, sulfadimezin;
• 2. Medium duration drugs (12 hours) Sulfazine;
• 3. Long-acting drugs (24 - 48 hours) Sulfapyridazine, sulfamonomethoxin, sulfadimethoxine;
• 4. Ultra-long-acting drugs (5 - 7 days) Sulfalene.

Streptocid Streptocidum.

A white crystalline powder, odorless and tasteless. Slightly soluble in water, easily in boiling water, solutions of acids and alkalis.

Used for tonsillitis, wash, bronchopneumonia, etc.

Soluble streptocide Strepticidum solubile.

White crystalline powder, soluble in water, sterilized. Incompatible with novocaine, anesthesin, barbiturates.

Assign i / m and s / c in the form of a 5% solution prepared with water for injection or isotonic sodium chloride solution. In / in - 10% on isotonic sodium chloride solution, or 1 - 5% glucose solution.

Norsulfazole Norsulfazolum.

White or slightly yellowish powder, slightly soluble in water. Incompatible with novocaine, anesthesin. This is one of the most active CA drugs, but toxicity can manifest itself after 7 to 9 days - hematuria, agranulocytosis.

Assign inside 2 - 3 times a day:

Norsulfazole sodium Norsulfazolum natrium.

Lamellar, shiny, colorless or with a slightly yellowish shade, odorless crystals. Let's easily dissolve in water. Withstands sterilization.

Due to its good solubility in water, it can be used not only internally, but also parenterally, as well as in the form of eye drops.

It is prescribed for septic processes, when it is necessary to quickly create a high concentration of the drug in the blood IV in the form of 5 - 15% solutions (injected slowly). S / c and i / m injected solutions not higher than 0.5 - 1% concentration (hitting s / c stronger solutions causes tissue irritation, up to necrosis.

Etazole Aethazolum.

White or white with a slightly yellowish sheen, odorless powder. Insoluble in water.

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

Surpasses many sulfonamides in antibacterial action

It is not acetylated in the body of dogs, and in other animals it is subjected to acetylation to a small extent (5 - 10%), therefore its use does not lead to the formation of crystals in the urinary tract.

For the prevention of wound infection, 5% ointment is injected into the wound cavity in the form of a powder. At the same time, the drug is administered orally.

Contraindications: acidosis, acute hepatitis, hemolytic anemia, agranulocytosis.

Sulfadimezin Sulfadimezinum.

Flavourless white or slightly yellowish powder. Insoluble in water.

Release form - powder, tablets of 0.25 and 0.5 g;

Excreted from the body slowly, mainly by the kidneys. Due to the relatively low rate of elimination, it is safer compared to rapidly released drugs.

In the treatment of wounds, ulcers, burns, the drug is used externally in the form of the smallest powder.

Urosulfan Urosulfanum.

Flavourless white crystalline powder, sour taste, slightly soluble in water.

Possesses high antibacterial activity against staphylococci and Escherichia coli.

It is slightly acetylated, circulates and is excreted mainly in free form. The rapid release ensures the creation of high concentrations of the free form of the drug in the urine, which contributes to the manifestation of its antimicrobial properties in urinary tract infections; complications in the urinary tract are not observed.

It is especially effective in treating pyelitis and cystitis without urinary disturbance.

Long-acting sulfonamides.

Sulfamonomethoxin Sulfamonomethoxinum.

White or white with a yellowish sheen, crystalline powder, slightly soluble in water.

Foma release - powder and tablets of 0.5 g.

The drugs are used for respiratory tract infections, purulent infections of the ear, throat, nose, dysentery, enterocolitis, infections of the bile and urinary tract, purulent meningitis.

Sulfadimethoxin Sulfadimethoxinum.

White crystalline powder, tasteless and odorless.

It is slightly toxic to animals, has a wide range of therapeutic action. The application is similar.

Ultra-long acting CA (5 - 7 days).

Sulfalene Sulfalenum.

White crystalline powder, slightly soluble in water.

Release form - powder, 0.2 tablets; 0.5 and 2.0 g,

bottles of 60 ml of 5% suspension.

It is excreted from the body very slowly.

Well tolerated by animals.

CA poorly absorbed from the gastrointestinal tract (intestinal drugs).

Phthalazole Phthalazolum.

White or white powder with a slightly yellowish sheen, insoluble in water.

Release form - powder, tablets of 0.5 g.

The high concentration of phthalazole in the digestive tract ensures its effective effect on the intestinal microflora. Differs in low toxicity, well tolerated by animals.

Used for dysentery, gastroenteritis, colitis, neonatal dyspepsia, coccidiosis.

Sulgin Sulginum.

White crystalline powder, odorless, slightly soluble in water.

Release form - powder, tablets of 0.5 g.

Possesses high antimicrobial activity against the intestinal group of microorganisms and some Gy forms.

Phtazine Phtazinum.

White or white with a slightly yellowish sheen, crystalline powder, insoluble in water.

Release form - powder, tablets of 0.5 g.

Applied for therapeutic and prophylactic purposes for dysentery, dyspepsia, newborns, enterocolitis, colitis, coccidiosis.

sulfonamide chemotherapy antimicrobial trimethoprim

Sulfanilamide preparations I Sulfanilamide preparations (synonym)

After absorption in S., the item is reversible, but to an unequal extent it binds to blood plasma proteins. In a bound form, they do not have an antimicrobial effect and show it only as the drugs are released from this connection. The rate of S.'s release of the item from the body is not affected by the degree of their binding to blood plasma proteins. S. of the item is metabolized in the liver mainly by acetylation. The resulting acetylated S. of the item do not possess antimicrobial activity and are excreted from the body through. In the urine, these metabolites can precipitate in the form of crystals, causing the appearance of crystalluria. The severity of crystalluria is determined not only by the degree of conversion of individual S. of the item into acetylated metabolites and the magnitude of doses of drugs, but also by the reaction of urine, because these metabolites are poorly soluble in an acidic medium.

In accordance with the peculiarities of pharmacokinetics and use among S. of the item, there are corresponding subgroups. For example, a subgroup of S. of the item is distinguished. Well absorbed from the gastrointestinal tract. Such S. of the item is used for systemic treatment of infections and for this purpose is prescribed internally and parenterally. Depending on the rate of their release among S. p. Of this subgroup, they are distinguished: short-acting drugs (half-life less than 10 h) - streptocide, sulfacyl sodium, etazole, sulfadimezin, urosulfan, etc.; drugs of average duration of action (half-life 10-24 h) - sulfazine, sulfamethoxazole, etc.; long-acting drugs (half-life from 24 to 48 h) - ulfapyridazine, sulfadimethoxine, sulfayunomethoxin, etc.; ultra-long-acting drugs (half-life more than 48 h) - sulfalene.

Sulfonamides of prolonged action differ from S. of the item of short action by a higher lipophilicity and, therefore, they are reabsorbed in the renal tubules in significant quantities (up to 50-90%) and are excreted more slowly from the body.

The subgroup of S. of the item, poorly absorbed from the gastrointestinal tract, includes sulgin, phthalazol, and phtazin. These drugs are used to treat intestinal infections (colitis and enterocolitis of bacterial etiology, including bacterial dysentery).

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

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

In modern clinical practice, combined preparations containing sulfonamides and trimethoprim are also widely used. Some of these combination drugs include biseptol containing sulfamistoxazole and trimethoprim (in a ratio of 5: 1), and sulfatone containing sulfomonomethoxin and trimethoprim (in a ratio of 2.5: 1). Unlike S. of the item, biseptol and sulfaton act bactericidal, have a wider spectrum of antimicrobial activity and are effective against strains resistant to sulfa drugs.

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

Sulfonamides are used to treat infections caused by microorganisms susceptible to these drugs. The choice of drugs is made taking into account the characteristics of their pharmacokinetics. So, for systemic infections (bacterial infections of the respiratory tract, lungs, bile and urinary tract, etc.), S. of the item is used, which are well absorbed from the gastrointestinal tract. For the treatment of intestinal infections, S. of the item is prescribed, which are poorly absorbed from the gastrointestinal tract (sometimes in combination with well-absorbed S. of the item).

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

Side effect of S. of the item is manifested by dyspeptic disorders, allergic reactions, neuritis, disturbances on the part of c.n.s. (dizziness, etc.), leukopenia, methemoglobinemia, etc. Due to poor solubility in water, S. p. and the products of their acetylation in the body can drop out in the kidneys in the form of crystals and cause crystalluria (especially when urine is acidified). For the prevention of this complication, when taking S. of the item, it is advisable to recommend an abundant alkaline drink.

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

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

Biseptol (Biseptol; synonym for bactrim, septrin, etc.) is prescribed internally (after meals) for adults and children over 12 years old, 1-2 tablets (for adults) 2 times a day, in severe cases - 3 tablets 2 times a day; children aged 2 to 5 years, 2 tablets (for children); from 5 to 12 years old, 4 tablets (for children) 2 times a day. Method of production: tablets for adults, containing 0.4 r sulfamethoxazole and 0.08 r trimethoprim; tablets for children containing 0.1 r sulfamethoxazole and 0.02 r trimethoprim. Storage: List B.

Salazodimethoxin (Salazodimethoxinum) is taken orally (after meals). Adults are prescribed 0.5 r 4 times a day or 1 r 2 times a day for 3-4 weeks. With the onset of the therapeutic effect, the daily dose is reduced to 1-1.5 r (0.5 each r 2-3 times a day). Children aged 3 to 5 years are initially prescribed 0.5 r per day (in 2-3 doses). With the onset of a therapeutic effect, the dose is reduced by 2 times. Children aged 5 to 7 years are initially prescribed 0.75-1 r, from 7 to 15 years old, 1-1.5 r per day. Method of production: 0.5 tablets r

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

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

Soluble streptocide (Streptocidum solubile) is administered intramuscularly and subcutaneously in the form of 1-1.5% solutions prepared with water for injection or isotonic sodium chloride solution, up to 100 ml (2-3 times a day). Intravenously administered in the form of 2-5-10% solutions prepared in the same solvents or 1% glucose solution, up to 20-30 ml... Release form: powder. Storage: List B in well-sealed jars.

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

Silver sulfadiazine (Sulfadiazini argenti) is used topically. It is part of Dermazin ointment, which is applied to the burn surface with a layer of 2-4 mm 2 times a day, followed by sterile application. The ointment is not prescribed for premature and newborn babies; in pregnant women, it is used for health reasons (with a burn area of \u200b\u200bmore than 20% of the body surface). Release form: tubes of 50 r, banks of 250 r.

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

Sulfadimethoxine (Sulfadimethoxinum; synonym madribone, etc.) is used internally. Adults are prescribed on the 1st day 1-2 r, on the following days 0.5-1 r per day (at one time); children at the rate of 0.025 g / kg on the 1st day and 0.0125 each g / kg in the following days. Method of production: powder; tablets 0.2 and 0.5 r... Storage: List B; in a dark place.

Sulfazine (Sulfazinum) is used internally. Adults are prescribed for the 1st reception 2-4 r, within 1-2 days 1 r every 4 h, on the following days 1 r every 6-8 h; children at the rate of 0.1 g / kg for the first appointment, then 0.025 g / kg every 4-6 h... Method of production: powder; 0.5 tablets r... Storage: List B; in a dark place.

Sulfalen (Sulfalenum; synonym kelfizin, etc.) r once every 7-10 days or on the first day 1 r, then 0.2 r daily. Release form: tablets of 0.2 r... Storage: List B.

Sulfamonomethoxin (Sulfamonomethoxinum). The method of administration and doses are the same as for sulfadimethoxine. Method of production: powder; 0.5 tablets r... Storage: List B; in a dark place.

Sulfapyridazine (Sulfapyridazinum; synonym: spofazadin, sulamin, etc.). The method of administration and doses are the same as for sulfadimethoxine. Method of production: powder; 0.5 tablets r... Storage: List B; in a dark place.

Sulfaton (Sulfatonum) is prescribed for adults, 1 tablet 2 times a day. Higher doses for adults: single - 4 tablets, daily - 8 tablets. Release form: tablets containing 0.25 r sulfamonomethoxin and 0.1 r trimethoprim. Storage: List B; in a dry, dark place.

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

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

Ftazin (Phthazinum) is prescribed for adults on the first day for 1 r 1-2 times, on the following days 0.5 r 2 times a day. For children, the dose is reduced according to age. Method of production: powder; 0.5 tablets r... Storage: List B: well protected from light.

Phthalazole (Phthalazolum; synonym for phthalyl-sulfathiazole, etc.) is used internally for dysentery. Adults are prescribed on 1-2 days for 1 r every 4 h (by 6 r per day), for 3-4 days 1 r every 6 h (by 4 r per day), on days 5-6 for 1 r every 8 h (3 r per day). After 5-6 days, repeat: on days 1-2 - 5 r per day, on days 3-4 - 4 r per day, on the 5th day - 3 r per day. For other intestinal infections, adults are prescribed in the first 2-3 days for 1-2 r, on the following days 0.5-1 r every 4-6 h... Children under 3 years old with dysentery are prescribed at the rate of 0.2 g / kg per day (in 3 doses), for children over 3 years old - 0.4-0.75 r at the reception 4 times a day. Higher doses for adults inside are the same as for sodium sulfacyl. Method of production: powder; 0.5 tablets r... Storage: List B; in a well-closed container.

Etazol (Aethazolum; synonym for sulfaetidol, etc.) is administered orally for adults 1 r 4-6 times a day: for children under 2 years old, 0.1-0.3 r every 4 h, from 2 to 5 years - 0.3-0.4 each r every 4 h, from 5 to 12 years old - 0.5 each r every 4 h... Locally prescribed in the form of a powder (powder) or ointment (5%). Higher doses for adults inside are the same as for sodium sulfacyl. Method of production: powder; tablets of 0.25 and 0.5 r... Storage: List B; in a well-closed container.

Etazole sodium (Aethazolum-natrium; synonym etazole soluble) is administered intravenously (slowly) in 5-10 ml 10% or 20% solution. In children's practice, they are used orally in granules, which are dissolved in water before use and prescribed to children at the age of 1 year - 5 each ml (0,1 r), 2 years - 10 ml (0,2 r), 3-4 years - 15 each ml (0,3 r), 5-6 years - 20 ml every 4 h... Method of production: powder; ampoules of 5 and 10 ml 10% and 20% solutions; granules in bags of 60 r... Storage: List B; in a well-closed container, protected from light.

II Sulfanilamide preparations (sulfanilamida;. Sulfonamides)

chemotherapeutic agents that are derivatives of sulfanilic acid; used to treat a number of infectious diseases.

1. Small Medical Encyclopedia. - M .: Medical encyclopedia. 1991-96 2. First health care... - M .: Great Russian Encyclopedia. 1994 3. Encyclopedic Dictionary of Medical Terms. - M .: Soviet encyclopedia. - 1982-1984.

A group of chemically synthesized compounds used for the treatment of infectious diseases, mainly bacterial origin... Sulfonamides were the first medicinesallowing successful prevention and ... ... Collier's Encyclopedia

sulfa drugs - sulfanilamidiniai preparatai statusas T sritis chemija apibrėžtis Sulfanilamido dariniai, pasižymintys antimikrobiniu veikimu. atitikmenys: angl. sulfanilamides rus. sulfa drugs; ryšiai sulfonamides: sinonimas - sulfamidiniai ... ... Chemijos terminų aiškinamasis žodynas

sulfa drugs - sulfa drugs ... Dictionary of Chemical Synonyms I

- (sulfanilamida; syn. sulfonamides) chemotherapeutic agents, which are derivatives of sulfanilic acid; are used to treat a number of infectious diseases ... Big Medical Dictionary

Sulfanilamides, a group of antimicrobial drugs derived from sulfanilic acid. Their antibacterial properties were discovered by the German scientist G. Domagk in 1934 35. S. p. Are close in chemical structure to para-aminobenzoic acid ... ... Great Soviet Encyclopedia

SULPHANYLAMIDE PREPARATIONS - sulfa drugs, sulfonamides, synthetic chemotherapeutic agents with predominantly bacteriostatic action; derivatives of para-aminobenzenesulfonic (sulfanilic) acid. All S. p. Are similar to each other in ... ... Veterinary encyclopedic dictionary

Sulfonamides - antimicrobial agents, derivatives of the pair (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. Sulfanilamide prontosil (red streptocid), which is somewhat more complex in structure, was the first drug in this group and generally the first synthetic antibacterial drug in the world.

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

pharmachologic effect

Sulfonamides have a bacteriostatic effect. Being analogs of PABA in chemical structure, 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 life of microorganisms. In environments containing a large amount of PABA, such as pus or tissue degradation 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 does not depend on the concentration of PABA at the site of application. Therefore, the effect of these drugs persists in the presence of pus and necrotic tissue.

Spectrum of activity

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, pneumocystis, actinomycetes, malaria 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 causative agents 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 blood concentrations are observed when using drugs of short (sulfadimidine, etc.) and medium duration (sulfadiazine, sulfamethoxazole) action. Sulfonamides of long-term (sulfadimethoxine, etc.) and ultra-long (sulfalene, sulfadoxine) action are bound to blood plasma proteins to a greater extent.

They are widely distributed in tissues and body fluids, including pleural effusion, peritoneal and synovial fluids, middle ear exudate, chamber moisture, and 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 pass into 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 reaction of urine, excretion is enhanced; small amounts are excreted in the bile. With renal failure, the accumulation of sulfonamides and their metabolites in the body is possible, leading to the development of toxic effects.

With the local application of sulfonamides containing silver, high local concentrations of active components are created. 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 are rapidly excreted by the kidneys: sulfathiazole (norsulfazole), sulfaetidol (etazole), sulfadimidine (sulfadimezine), sulfacarbamide (urosulfan).
2. Drugs that are completely absorbed in the gastrointestinal tract, but are slowly excreted by the kidneys (long-acting): sulfamethoxypyridazine (sulfapyridazine), sulfamonomethoxin, 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 (salicylic acid, salicylic acid, salazalazalazo), (salazalazalazalazine).
4. Preparations for topical use: sulfonamide (streptocid), sulfacetamide (sodium sulfacyl), silver sulfadiazine (sulfargin) - the latter, dissolving, releases silver ions, providing an antiseptic and anti-inflammatory effect.
5. Combination drugs: 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, which are 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 - topically, and the fifth (combined preparations with trimethoprim) are effective for infections of the respiratory and urinary tract, gastrointestinal diseases.

Indications for the use of sulfonamides

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

• respiratory tract infections (acute and chronical bronchitis, bronchiectasis, croupous pneumonia, bronchopneumonia, pneumocystis pneumonia, pleural empyema, lung abscess)
• eNT infections (otitis media, sinusitis, laryngitis, tonsillitis, pharyngitis, tonsillitis)
• scarlet fever
• infections of the genitourinary organs (pyelonephritis, pyelitis, epididymitis, cystitis, urethritis, salpingitis, prostatitis, gonorrhea in men and women, chancre, lymphogranuloma venereal, inguinal granuloma)
• gastrointestinal infections (dysentery, cholera, typhoid fever, salmonella, paratyphoid fever, cholecystitis, cholangitis, gastroenteritis caused by enterotoxic strains of E. coli)
• infections of the skin and soft tissues (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
• 1st and 2nd degree burns
• pyoderma, carbuncles, boils
• purulent-inflammatory processes on the skin
• infected wounds of different origins
• tonsillitis
• eye diseases.

Instructions for the use of 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.

When treating deep wounds, the agent is introduced into the wound cavity in the form of a crushed (into dust) sterilized powder. The dosage is 5 to 15 grams. In parallel, systemic treatment is carried out, antibiotics are prescribed for oral administration.

It is also often combined with ephedrine, sulfathiazole, and benzylpenicillin to treat rhinitis. It is used in powder form. The powder (finely ground) is inhaled through the nose.

Inside Sulfanilamide can be used in a daily dosage of 0.5 to 1 gram, distributed in 5-6 doses. For children, it is recommended to adjust the daily dosage according to 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 side effects observed sometimes, dyspeptic and allergic ones are more often noted.

Allergy

For allergic reactions, antihistamines and calcium preparations are prescribed, 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.

Effects on the Central Nervous System

Phenomena from the central nervous system are possible:

• headache;
• dizziness, etc.

Blood disorders

Sometimes there are changes in the blood:

• anemia;
• agranulocytosis;
• leukopenia, etc.

Kristallouria

All side effects can be more persistent with the introduction of long-acting drugs that are more slowly excreted from the body. Since these slightly soluble drugs are excreted in the urine, they can form crystals in the urine. With an acidic reaction of urine, crystalluria is possible. To prevent this phenomenon, sulfa drugs should be taken with a significant amount of alkaline drink.

Contraindications for sulfonamides

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

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

Toxic effect on blood with other drugs

Do not take sulfonamides in conjunction with others medicinesthat have a toxic effect on the blood:

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

Application during pregnancy and lactation

With systemic absorption, sulfonamide can quickly pass through the placenta and be found in the fetal blood (the concentration in the fetal blood is 50–90% of that in the mother's blood), and also cause toxic effects. The safety of using sulfonamide during pregnancy has not been established. It is not known if sulfonamide can have fetal harmful effects when taken by pregnant women. In experimental studies in rats and mice that received during pregnancy some sulfonamides (including sulfonamide) of short, medium and long-acting orally in high doses (7-25 times higher than the therapeutic oral dose for humans), a significant increase in the incidence of cleft palate and other malformations of bones in the fetus. It passes into breast milk, may cause kernicterus in newborns.

What should not be consumed with sulfonamides?

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

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

Sulfonamides are incompatible with some foods that contain the following chemicals:

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

The price of sulfa drugs

It is not a problem to buy medicines of this group in an online store or in a 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 single drug, you will have to pay extra for delivery. Domestically produced sulfonamides will be inexpensive, while imported medicines are much more expensive. The approximate price of sulfa drugs:

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

A series of short-acting sulfonamides, it is also called streptocide ... It is one of the first representatives of this series of antibacterial agents. Possesses a wide spectrum of antimicrobial activity.

The drug is synthesized in the form of a white crystalline powder, without a specific odor, bitter taste, the powder has a sweet aftertaste. The substance dissolves well in boiling water, it is difficult - in ethyl alcohol, soluble - in solution salt to-you , caustic alkalis , acetone , propylene glycol ... The product does not dissolve in, air , benzene , petroleum . Molecular mass compound is 172.2 grams per mole.

Antibiotic also sold as sodium sulfonamide ... It is a white powder, readily soluble in water. Practically insoluble in various organic solvents. Also available in pill form.

Sulfanilamide preparations are mainly used externally, in the form of ointments, powders for external use, liniment, aerosols, as part of vaginal suppositories. However, the medicine can also be taken by mouth.

pharmachologic effect

Antimicrobial.

Pharmacodynamics and pharmacokinetics

The mechanism of action of the substance

The agent acts as an antagonist para-aminobenzoic acid , due to its chemical similarity with it. The microbial cell captures the Sulfanilamide molecule instead of PABA, the bacterial enzyme is suppressed dihydropteroate synthetase by a competitive mechanism. Synthesis processes are disrupted dihydrofolic acid and tetrahydrofolic acid which, in turn, are essential for education pyrimidines and purines , growth and development of harmful microorganisms. Thus, the substance has a bacteriostatic effect.

Antibiotics Sulfonamides are active against gram-positive and gram-negative cocci, streptococci, meningococci, pneumococcus, gonococci, Vibrio cholerae, Bacillus anthracis, Yersinia pestis, Actinomyces israelii, Shigella spp., Clostridium perfringens, Corynebacterium diphtheriae, Chlamydia spp., Toxoplasma gondii, Shigella spp... When used topically, it significantly speeds up wound healing.

After the substance enters the digestive tract, the maximum concentration of the agent in the blood is observed after 1-2 hours. The half-life is less than 8 hours. The remedy overcomes everything histohematogenous barriers , including the BBB and the placental barrier. 4 hours after ingestion, the substance can be found in the cerebrospinal fluid. Metabolized in the liver, metabolites do not have antibacterial properties. Displayed antibiotic mainly with the help of the kidneys (up to 95%).

The drug has not been studied for mutagenic and carcinogenic effects on the body.

Indications for the use of Sulfanilamide

The antibiotic is used topically:

• for treatment;
• at ulcers , cracks and infected wounds of various origins;
• in patients with purulent-inflammatory skin lesions;
• at boils , carbuncles , pyoderma ;
• sick folliculitis , with erysipelas, with vulgar;
• at;
• for the treatment of first and second degree burns.

At the moment, the agent is practically not used for oral administration. Previously, it was used to treat erysipelas , pyelitis , enterocolitis , for the prevention and treatment of wound infections. Also Sulfanilamide was injected in dissolved form (5% solution on water) intravenously, ex tempore.

Contraindications

Preparations based on this antibiotic do not appoint:

• for substance and others sulfonamides ;
• at anemia , diseases of the hematopoietic system;
• patients with hepatic and renal insufficiency;
• at porphyrias , ;
• patients with congenital deficiency glucose-6-phosphate dehydrogenase ;
• at.

Patients should be especially careful during breastfeeding and during pregnancy.

Side effects

When used topically, Sulfanilamide most often does not cause any side reactions. May occur allergic rashes .

When taken orally or locally in large quantities, there are:

• , paresthesias ;
• , nausea,;
• , crystalluria .

Rarely may appear:

• thrombocytopenia , hypoprothrombinemia , leukopenia ;
• decreased visual acuity, ataxia , hypothyroidism .

Instructions for use of Sulfanilamide (Way 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.

When treating deep wounds, the agent is introduced into the wound cavity in the form of a crushed (into dust) sterilized powder. The dosage is 5 to 15 grams. In parallel, systemic treatment is carried out, antibiotics for oral administration.

Also, the remedy is often combined with, sulfathiazole and for treatment. It is used in powder form. The powder (finely ground) is inhaled through the nose.

Inside Sulfanilamide can be used in a daily dosage of 0.5 to 1 gram, distributed in 5-6 doses. For children, it is recommended to adjust the daily dosage according to age.
The maximum amount of antibiotic that can be taken per day is 7 grams, at a time - 2 grams.

Overdose

There is no evidence of an overdose of the drug when used topically.

Interaction

When combined with myelotoxic drugs, the hematotoxicity of the drug increases.

Terms of sale

A recipe is usually not required.

Storage conditions

Depending on the dosage form, there are different requirements for the storage of Sulfanilamide preparations.

Medicines are stored in a cool place, protected from direct sunlight. Away from children.

Shelf life

special instructions

Patients with renal failure ... Drink plenty of fluids during treatment.

During prolonged intake of the drug inside, it is recommended to monitor the functioning of the liver and kidneys, the peripheral blood picture.

If, during therapy with sulfonamide, the patient experiences allergy on the remedy, then the treatment must be interrupted.

For children

Children under 12 months are prescribed 50-100 mg of the drug at a time. From 2 to 5 years old - 0.2-03 grams. From 6 to 12 years old, 0.3-0.5 grams of the drug are prescribed. The frequency of admission is 5-6 times.

With alcohol

Preparations that contain (Analogues)

Matching ATX level 4:

List of drugs Sulfonamides: Streptocid-LekT , powder for external use, Streptocid white soluble, Streptocide tablets, 10%.

The names of the drugs in which FROMtreptocide in combination with other substances: suppositories Osarcid , Ingalipt-VIAL , spray can, Newingalipt spray, (combination with trimethoprim), etc.