Complications caused by sulfonamides. Sulfonamide drugs (sulfonamides). Short-acting drugs

Sulfanilamide and other drugs discussed in this part of the section are among the synthetic antimicrobial drugs that have a mainly bacteriostatic effect and are used to treat many infectious diseases.

• Sulfa drugs

All sulfonamide drugs are fundamentally similar to each other in chemical structure and mechanism antimicrobial action.

They differ from each other in pharmacokinetic parameters: some are easily absorbed from gastrointestinal tract, quickly accumulate in the blood, organs and tissues; others stay in the intestines for a long time and create a high concentration of drugs in it, sufficient to treat diseases of the stomach and intestines; still others accumulate in significant quantities in the kidneys and urinary tract, excreted unchanged from the body. Sulfonamide agents have a bacteriostatic effect on microorganisms. They suppress the vital activity of a large group of cocci, dysentery and E. coli, anthrax pathogens, Vibrio cholerae, Brucella and other pathogens.

The mechanism of action of sulfonamide drugs is based on the principle of antimetabolism, when a substance needed by a microorganism is replaced with a substance that is similar in chemical structure, but opposite in action. This action is called competitive antagonism. In this case, competitive antagonism is carried out on the structural similarity of the molecules of para-aminobenzoic acid (PABA) and sulfonamide (Fig. 4).

Para-aminobenzoic acid is directly involved in biotransformation folic acid, which, being converted into folinic acid, participates in the synthesis of nucleic acids (protein), which underlies the growth, development and reproduction of the microorganism. Replacing PABA with sulfonamide disrupts protein synthesis, leads to growth retardation and proliferation of pathogens. But to obtain such an effect, the concentrations of sulfonamide drugs must be many times higher than the concentration of PABA (the second principle of chemotherapy). That is why treatment with sulfonamide drugs begins with large (shock) doses of drugs in order to create a high concentration of a competitive drug in the body as quickly as possible.

Based on their duration of action, sulfonamide drugs are divided into short-, medium-, long- and extra-long-acting drugs.

To sulfonamides short acting include Streptocide, Norsulfazole, Sulfadimezin, Etazol, etc.

STREPTOCID (Streptocidum) is one of the first sulfonamide drugs used in medical practice. It is used to treat tonsillitis, pyelitis, cystitis, colitis, erysipelas, wound infections, etc.

Treatment with streptocide begins with a loading dose of 2 g, and then 0.5-1 g orally up to 5 times a day, gradually reducing the number of doses towards the end of treatment. Externally, streptocide is injected into the wound in the form of a sterile powder or its 5% liniment and 10% ointment are used.

Among side effects allergic reactions, leukopenia, agranulocytosis, tachycardia, etc. are possible. Streptocide is contraindicated in diseases of the hematopoietic system, impaired renal function, thyrotoxicosis and hypersensitivity the body to sulfonamide drugs.

Streptocide is produced in powder, tablets of 0.3 and 0.5 g, in the form of 5% liniment and 10% ointment in packages of 25-30 g.

NORSULFAZOL (Norsulfazolum) is active against gram-positive and gram-negative bacteria, is easily absorbed from the gastrointestinal tract and is quickly excreted from the body in the urine.

Norsulfazole is used to treat pneumonia, cerebral meningitis, streptococcal and staphylococcal sepsis, gonorrhea and other diseases. Treatment begins with a loading dose of 2 g, and then 1 g is taken every 4-6 hours, and then after 6-8 hours. In total, a course of treatment requires from 20 to 30 g of the drug.

When treating with Norsulfazole, it is recommended to increase fluid intake to 2-3 liters per day in order to prevent possible crystalluria. It is also recommended that after each dose of the drug, drink it with a glass of water with the addition of a small amount of baking soda.

Side effects when using Norsulfazole include allergic reactions, leukopenia, neuritis and intestinal upset.

The drug is produced in powder, tablets of 0.25 and 0.5 g. List B.

ETAZOL (Aethazolum) has antibacterial activity, which applies to all types of cocci, Escherichia coli, diphtheria pathogens and infections urinary tract. Etazol is used to treat pneumonia, erysipelas, sore throat, purulent urinary tract infections, wound infections and peritonitis.

The drug is prescribed orally, 1 g 4-6 times a day, depending on the nature of the disease. Etazol is low toxic, does not accumulate and almost does not cause crystalluria. Its side effects are the same as those of other sulfonamide drugs.

The drug is produced in powder and tablets of 0.25 and 0.5 g.

The sodium salts of the above drugs are highly soluble in water and are more often used for injection in cases where oral administration is not possible. It should also be noted that with the advent of more effective chemotherapeutic agents, the use of sulfonamide drugs has significantly decreased.

Sulfa drugs average duration actions are represented by the drug sulfazin and its silver salt.

Sulfazinum differs from other drugs in its longer action (up to 8 hours). Indications for use are the same as for Norsulfazole.

Sulfazine is prescribed orally, the first dose is 2 g, then within

• 2 days, 1 g every 4 hours and then 1 g every 6-8 hours.

It rarely causes side effects, and alkaline drinking is recommended to prevent kidney complications.

Sulfazine is produced in powder and tablets of 0.5 g.

Long-acting drugs are widely used in the treatment of infectious diseases, used in smaller doses per course of treatment, causing almost no crystalluria and prescribed 1-2 times a day after taking a loading dose.

SULFADIMETOXIN (Sulfadimethoxinum) is a long-acting drug, slowly absorbed from the gastrointestinal tract, reaching maximum concentration after 8-12 hours.

The antibacterial effect of the drug applies to all types of cocci, pathogens of dysentery, trachoma and some protozoa. It is used to treat acute respiratory diseases, pneumonia, bronchitis, sinusitis, otitis, inflammatory diseases of the biliary and urinary tract, wound infections, etc.

The drug is prescribed orally starting from 1-2 g on the first day and 0.5-1 g in subsequent days.

When using sulfadimethoxine, skin rashes, leukopenia and rarely intestinal upset are possible. The drug is contraindicated in case of individual intolerance.

Sulfadimethoxine is produced in tablets of 0.5 g in a package of 10 pieces.

SULFAPIRIDAZINE (Sulfapyridazinum) is absorbed in the intestine faster than sulfadimethoxine, but is excreted from the body more slowly, which explains its long-lasting effect.

Indications and contraindications for the use of sulfapyridazine are similar to sulfadimethoxine and other sulfonamide drugs. It is used with caution for diseases of the hematopoietic system, impaired renal function and decompensation of cardiac activity.

Sulfapyridazine is produced in tablets of 0.5 g. List B.

The highly soluble sodium salt of sulfapyridazine (Sulfapyridazinumnatrium) is often used for local treatment purulent infection, in the form of eye drops for trachoma and inhalations for chronic purulent processes in the bronchi and lungs.

The drug is produced in powder for the preparation of solutions and in the form of eye films in a package of 30 pieces.

SULFAMONOMETHOXINE (Sulfamonomethoxinum) according to indications and contraindications for use is close to long-acting drugs. It is easily soluble in water, quickly absorbed, penetrates the blood-brain barrier, and is relatively low-toxic.

It is prescribed orally in tablets on the first day, 1 g, and on subsequent days, 0.5 g per day. The daily dose is given 1 time per day.

The drug is produced in tablets of 0.5 g. Sulfamonomethoxin is part of the drug Sulfatone.

The group of ultra-long-acting drugs includes sulfalene and its methylglucamine salt.

SULFALEN (Sulfalenum) in antibacterial action is close to sulfapyridazine and other long-acting sulfonamides, but has an ultra-long-lasting effect, since it is very slowly excreted from the body through the kidneys (up to 72 hours).

When taken orally, it is well absorbed, easily penetrates fluids and tissues, is found in high concentrations in the liver, etc. Unlike other sulfonamide drugs, it almost does not bind to proteins and is in the blood in a free state, which ensures its long-term therapeutic effect.

Sulfalene is used for infectious diseases of the respiratory system, biliary and urinary tracts, purulent infections of various locations (abscesses, mastitis), osteomyelitis, otitis, etc.

Sulfalene is prescribed orally in tablets: on the first day, 1 g of the drug and on subsequent days - 0.2 g per day 30 minutes before meals. The duration of treatment depends on the nature of the disease and is approximately 7-10 days.

Sulfalene is usually well tolerated, but sometimes allergic reactions, nausea, headache and leukopenia.

Sulfalene is produced in tablets of 0.2 g in a package of 10 pieces.

Soluble sulfalene salt (Sulfalenum-megluminum) is used for parenteral administration for severe forms purulent infections in surgery, therapy, urology, pneumonia and meningitis. The drug is administered into a vein or intramuscularly. List B.

The combined sulfonamide drugs Sulfatone and Bactrim (Biseptol) have found widespread use in medical practice.

BACTRIM, synonym: Biseptol, is a broad-spectrum antibacterial drug. It contains sulfamethoxazole and trimethoprim. The bactericidal effect is explained by a double blocking effect on bacterial metabolism, which is associated with a violation of the synthesis of folic acid derivatives.

Bactrim is used for infectious and inflammatory diseases of the respiratory system, urinary tract, gastrointestinal diseases, diseases of the skin and soft tissues.

When taken orally, the drug is rapidly absorbed, reaches maximum concentration in the blood after 1-4 hours and persists for up to 7-8 hours. Bactrim is prescribed orally, 2 tablets in the morning and evening after meals. The course of treatment takes from 5 to 14 days depending on the nature of the disease. It is advisable to carry out treatment under the control of the blood picture.

Side effects when taking Bactrim include allergic reactions, nephropathy, some changes in the blood, nausea, vomiting, etc.

Bactrim (Biseptol) is produced in tablets of 480 mg for adults and 120 mg for children. In pediatric practice, starting from 1.5 months, the drug is used in the form of a suspension, which is produced in 100 ml bottles.

Sulfatonum contains two active ingredients: sulfamonomethoxine and trimethoprim, and is similar in action to Bactrim.

Indications for the use of the drug include infections of the respiratory tract, urinary and biliary tract, erysipelas, sepsis, meningitis, purulent surgical infection and etc.

Sulfatone is prescribed orally on the first day, 2 g in the morning and evening (loading dose), and on subsequent days, 1 tablet 2 times a day (maintenance dose). The course of treatment is 7-10 days.

Sulfatone is produced in tablets of 0.35 g.

For local application sulfonamides are used in the composition of Sunoref and Dermazin ointments, the complex drug Ingalipt and in the form of sulfacyl sodium eye drops.

SULFACYL-SODIUM (Sulfaciylum-natrium) is a drug with broad antimicrobial action, effective for coccal and colibacillary infections, purulent eye lesions, conjunctivitis, corneal ulcers and in the treatment of infected wounds. It is highly soluble in water, which allows it to be used not only in the form of eye drops, but also for injections.

Most wide application sodium sulfacyl solution was found in ophthalmology, where it is used in 20 and 30% concentrations or in the form of 10, 20 and 30% eye ointment. To prevent blenorrhea, newborns should instill 2 drops of a 30% solution into the eyes immediately after birth and 2 drops after 2 hours. For purulent eye lesions, sodium sulfacyl solution is instilled 2 drops up to 6 times a day. Orally, for diseases of the respiratory system and genitourinary system, the drug is prescribed at a dose of 0.5-1 g per dose 3-5 times a day. In severe cases, a 30% solution of the drug is injected into a vein.

They produce sodium sulfacyl in powder, in the form of 20 and 30% solutions in dropper tubes of 1.5 ml in a package of 2 pieces, a 30% solution in bottles of 5 ml and a 30% solution in ampoules of 5 ml in a package of 10 things. List B.

To treat infectious diseases of the gastrointestinal tract, sulfonamide drugs are used, which are poorly absorbed from it, creating a high antimicrobial concentration, leading to the death of pathogens. These include Sulgin, phthalazol, phtazin, etc.

SULGIN (Sulginum), synonym: sulfaguanidine, is a short-acting drug; after oral administration, the main amount of it is retained in the intestines, where its effect is manifested.

Sulgin is used for adults and children for all types of bacterial dysentery, colitis, enterocolitis and for preparing patients for surgery on the small and large intestines. For acute intestinal infections, the drug is used according to the following scheme: on the first day, 1-2 g 6 times a day, on the second and third - 5 times, on the fourth - 4 times and on the fifth day 3 times a day. The course of treatment is 5-7 days, and after a short break, it can be repeated if necessary.

To avoid side effects from the kidneys during treatment, it is recommended to maintain increased diuresis by taking

• 3 liters of fluid per day, and to prevent vitamin deficiencies it is recommended to use B vitamins.

Sulgin is produced in powder and tablets of 0.5 g in a package of 10 pieces.

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

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

Drugs in this group belong to chemotherapeutic agents with a broad antibacterial spectrum of action, because they suppress the vital activity of many types of Gr and Gr-bacteria: streptococci, staphylococci, meningococci, gonococci, bacteria of the enteric-typhoid-dysenteric group and many others. Active against large viruses (pathogens of trachoma), coccidia, plasmodium, malaria and toxoplasma, actinomycetes, etc.

Sulfonamide drugs in small concentrations they inhibit the growth and development of bacteria, i.e. they act bacteriostatically. They have a bactericidal effect only when exposed to such high concentrations that they are unsafe for the microorganism.

The mechanism of the antimicrobial action of sulfonamides is associated with their competitive antagonism with para-aminobenzoic acid (PABA). PABA is included in the structure of dihydrofolic acid, which is synthesized by many microorganisms. Due to their chemical affinity for PABA, sulfonamides prevent its incorporation into dihydrofolic acid. In addition, they competitively inhibit dihydropteroate synthetase. Impaired 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 and glucose oxidation.

Proteinous substances (pus, dead tissue) containing large amounts of PABA, as well as some medications, the molecule of which includes a PABA residue (novocaine, anesthesin), are inhibitors of the activity of sulfonamides.

To obtain a therapeutic effect, they must be prescribed in doses sufficient to prevent the possibility of microorganisms using PABA contained in tissues. 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, act anti-inflammatory, stimulate the process of phagocytosis, increase the body’s resistance to toxins) and the microorganism complement each other, providing a well-defined therapeutic effect.

Most sulfonamides are easily absorbed from the gastrointestinal tract and quickly accumulate in the blood, organs and tissues in bacteriostatic concentrations. The sodium salts of the drugs are very well absorbed. Some are difficult to absorb, remain in high concentrations in the intestine for a relatively long time and are excreted mainly in feces.

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

They are distributed unevenly in different organs and tissues. Largest quantity they are found in the kidneys, lungs, walls of the stomach and intestines, heart, and liver. Sulfonamides penetrate the placenta well.

Most sulfonamides are eliminated from the body of animals relatively quickly. 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, washout, postpartum sepsis, pyelitis, cystitis, salmonellosis, colibacillosis, pasteurellosis, wound and other infections.

Sulfonamide drugs are low toxic. However, long-term use of them in excessive doses can lead to the development of undesirable, i.e., toxic effects: inhibition of beneficial microflora of the gastrointestinal tract, cyanosis, leukopenia, anemia, B-vitaminosis, agranulocytosis, general depression. With insufficient renal function or when large doses of drugs are prescribed, crystalluria may occur.

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

Classification of sulfonamides:

• 1. Drugs that are quickly and completely absorbed from the gastrointestinal tract (resorptive sulfonamides). These 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). These include phthalazol, sulgin, phtazin.
• 3. Drugs used locally (prevention and treatment of eye infections, wound infections, burns and wounds) - sulfacyl sodium, sulfargin.
• 4. Sulfonamides special purpose- salazosulfapyridine, salazopyridazine (used for nonspecific ulcerative colitis), sulfantrol (antipyroplasmidosis agent), diacarb (diuretic).
• 5. Combined preparations of sulfonamides with trimethoprim (trimethosul, trimerazine, etc.).

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

• 1. Drugs with a short duration of action (4-6 hours). Streptocide norsulfazole, etazol, sulfadimezin;
• 2. Drugs with an average duration of action (12 hours) Sulfazin;
• 3. Long-acting drugs (24 - 48 hours) Sulfapyridazine, sulfamonomethoxine, sulfadimethoxine;
• 4. Ultra-long-acting drugs (5 - 7 days) Sulfalen.

Streptocide Streptocidum.

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

Used for sore throats, washing, bronchopneumonia, etc.

Soluble streptocide Strepticidum solubile.

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

Prescribed intramuscularly and subcutaneously in the form of a 5% solution prepared in water for injection or isotonic sodium chloride solution. IV - 10% in 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 SA drugs, but toxicity can appear after 7-9 days - hematuria, agranulocytosis.

Prescribed orally 2-3 times a day:

Norsulfazol-sodium Norsulfazolum-natrium.

Lamellar, shiny, colorless or odorless crystals with a slightly yellowish tint. Easily soluble in water. Withstands sterilization.

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

Prescribed for septic processes, when it is necessary to quickly create a high concentration of the drug in the blood intravenously in the form of 5 - 15% solutions (administered slowly). Solutions of no higher than 0.5 - 1% concentration are administered subcutaneously and intramuscularly (ingestion of stronger solutions subcutaneously causes tissue irritation, even necrosis.

Etazolum Aethazolum.

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

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

Superior to many sulfonamides in antibacterial action

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

To prevent wound infection, 5% ointment is injected into the wound cavity in the form of powder. At the same time, the drug is prescribed orally.

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

Sulfadimezinum Sulfadimezinum.

White or slightly yellowish powder, odorless. Insoluble in water.

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

It is excreted from the body slowly, mainly by the kidneys. Due to the relatively slow elimination rate, it is safer compared to rapidly released drugs.

When treating wounds, ulcers, and burns, the drug is used externally in the form of a tiny powder.

Urosulfan Urosulfanum.

White crystalline powder, odorless, sour taste, slightly soluble in water.

Has high antibacterial activity against staphylococci and Escherichia coli.

It is slightly acetylated, circulates and is excreted mainly in free form. 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; There are no complications in the urinary tract.

Its use is especially effective for pyelitis and cystitis without impaired urination.

Long-acting sulfonamides.

Sulfamonomethoxin Sulfamonomethoxinum.

White or white with a yellowish tint 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, biliary and urinary tract infections, purulent meningitis.

Sulfadimethoxin Sulfadimethoxinum.

White crystalline powder, tasteless and odorless.

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

Extra long-acting SA (5 - 7 days).

Sulfalene Sulfalenum.

White crystalline powder, slightly soluble in water.

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

bottles of 60 ml of 5% suspension.

It is eliminated from the body very slowly.

Well tolerated by animals.

CAs are poorly absorbed from the gastrointestinal tract (intestinal drugs).

Phthalazolum Phthalazolum.

White or white with a slightly yellowish tint powder, 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. It has low toxicity and is well tolerated by animals.

Used for dysentery, gastroenteritis, colitis, dyspepsia of newborns, coccidiosis.

Sulgin Sulginum.

White crystalline powder, odorless, slightly soluble in water.

Release form: powder, tablets of 0.5 g.

Has high antimicrobial activity in relation to the intestinal group of microorganisms and some Gr forms.

Phtazinum Phtazinum.

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

Release form: powder, tablets of 0.5 g.

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

sulfonamide chemotherapy antimicrobial trimethoprim

SYNTHETIC ANTIBACTERIAL PRODUCTS

Synthetic antibacterial agents represented by 6 main classes:

5. Sulfonamides.

6. Quinolone derivatives.

7. Nitrofuran derivatives.

8. 8-hydroxyquinoline derivatives.

9. Quinoxaline derivatives.

10. Oxazolidinones.

1. SULFANAMIDE DRUGS

Sulfonamides can be considered as derivatives of sulfanilic acid amide.

The main difference between sulfonamides lies in their pharmacokinetic properties.

11. Sulfonamides for resorptive action (well absorbed fromgastrointestinal tract)

a) Short-acting (half-life< 10 ч)

Sulfanilamide (Streptotsid), sulfathiazole (Norsulfazole), sulfaetidol (Etazol), sulfcarbamide (Urosulfan), sulfadimidine (Sulfadimezin). b) Medium duration of action (half-life 10-24 hours) Sulfadiazine (Sulfazine), sulfamethoxazole.

c) Long-acting (half-life 24-48 hours) Sulfadimethoxine, sulfamonomethoxine.

d) Ultra-long-acting (half-life >48 hours) Sulfamethoxypyrazine (Sulfalene).

12. Sulfonamides acting in the intestinal lumen (poorly absorbed fromgastrointestinal tract)

Phthalylsulfathiazole (Fthalazol), sulfaguanidine (Sulgin).

13. Sulfonamides for topical use

Sulfacetamide (Sulfacyl sodium, Albucid).

14. Combined preparations of sulfonamides and salicylic acid

Salazosulfapyridine (Sulfasalazine), salazopyridazine (Salazodin), Salazodimethoxine.

15. Combination preparations of sulfonamides with trimethoprim

Co-trimoxazole (Bactrim, Biseptol).

Sulfonamides have a bacteriostatic effect on microorganisms. The mechanism of the bacteriostatic effect of sulfonamides is that these substances, having a structural similarity to para-aminobenzoic acid, compete with it in the synthesis of folic acid, which is a growth factor for microorganisms.

Sulfonamides are mainly active against nocardia, toxoplasma, chlamydia, malarial plasmodia and actinomycetes.

The main indications for use are: nocardiosis, toxoplasmosis, tropical malaria resistant to chloroquine. In some cases, sulfonamides are used for coccal infections, bacillary dysentery, and infections caused by Escherichia coli. In some cases, sulfonamides are used for coccal infections, bacillary dysentery, and infections caused by Escherichia coli.

Systemic sulfonamides cause a large number of side effects. When using them, blood system disorders (anemia, leukopenia, thrombocytopenia), hepatotoxicity, allergic reactions ( skin rashes, fever, agranulocytosis), dyspeptic disorders. With acidic urine pH values, crystalluria occurs. To prevent it, sulfonamides must be taken with alkaline mineral water or soda solution.

Sulfonamides acting in the intestinal lumen are practically not absorbed in the gastrointestinal tract and create high concentrations in the intestinal lumen. They are used in the treatment of intestinal infections (bacillary dysentery, enterocolitis), as well as for the prevention of intestinal infections in the postoperative period.

Currently, many strains of intestinal pathogens have acquired resistance to sulfonamides. To increase the effectiveness of treatment, simultaneously with sulfonamides acting in the intestinal lumen, it is advisable to prescribe well-absorbed drugs (Etazol, Sulfadimezin, etc.), since the causative agents of intestinal infections are localized not only in the lumen, but also in the intestinal wall. When taking drugs of this group, B vitamins should be prescribed, since sulfonamides inhibit the growth of Escherichia coli, which is involved in the synthesis of B vitamins.

Sulfanilamide is one of the first antimicrobials sulfonamide structure. Currently, the drug is practically not used due to low efficiency and high toxicity.

Urosulfan is used to treat urinary tract infections, since the drug is excreted unchanged by the kidneys and creates high concentrations in the urine.

Sulfamethoxypyrazine used daily for acute or rapidly occurring infectious processes, once every 7-10 days for chronic, long-term infections.

Sulfacetamide is a sulfonamide for topical use. The drug is usually well tolerated. It is used in ophthalmic practice in the form of solutions and ointments for conjunctivitis, blepharitis, purulent corneal ulcers and gonorrheal eye diseases. When using more concentrated solutions, an irritating effect is observed; in these cases, solutions of lower concentrations are prescribed.

Trimethoprim is a pyrimidine derivative that has a bacteriostatic effect. The drug blocks the reduction of dihydrofolic acid to tetrahydrofolic acid due to inhibition of dihydrofolate reductase.

Co-trimoxazole is a combination of 5 parts sulfamethoxazole (medium-acting sulfonamide) and 1 part trimethoprim. The combination of trimethoprim with sulfonamides is characterized by a bactericidal effect and wide range antibacterial action, including microflora resistant to many antibiotics and conventional sulfonamides. Co-trimoxazole is well absorbed from the gastrointestinal tract, penetrates many organs and tissues, and creates high concentrations in bronchial secretions, bile, urine, and prostate gland. Penetrates through the BBB, especially during inflammation of the meninges. It is excreted mainly in the urine. The drug is used for respiratory and urinary tract infections, surgical and wound infections, brucellosis; Contraindicated in cases of severe dysfunction of the liver, kidneys and hematopoiesis. The drug should not be prescribed during pregnancy.

Sulfamethoxazole is part of the combination drug "Cotrimoxazole".

2. QUINOLONE DERIVATIVES

Quinolone derivatives are represented by non-fluorinated and fluorinated compounds. The latter have the greatest antibacterial activity.

Quinolone derivatives are presented:

6. Non-fluorinated quinolones

Nalidixic acid (Nevigramon, Negram), oxolinic acid (Gramurin). 7. Fluoroquinolones (first generation drugs)

Ciprofloxacin (Tsifran, Tsiprobay), lomefloxacin (Maxaquin), norfloxacin (Nomitsin), fleroxacin (Hinodis), ofloxacin (Tarivid).

8. Fluoroquinolones (new drugs of the second generation) Levofloxacin (Tavanic), sparfloxacin, moxifloxacin.

Nalidixic acid active only against some gram-negative microorganisms - Escherichia coli, Shigella, Klebsiella,

Salmonella Pseudomonas aeruginosa is resistant to nalidixic acid. Resistance of microorganisms to the drug occurs quickly.

The drug is well absorbed from the gastrointestinal tract, especially on an empty stomach. About 80% of the drug is excreted unchanged in the urine, resulting in high concentrations of nalidixic acid in the urine. Half-life

Indications for use: urinary tract infection (cystitis, pyelitis, pyelonephritis), prevention of infections during kidney and bladder operations.

Side effects: dyspeptic disorders, central nervous system stimulation, liver dysfunction, allergic reactions. Nalidixic acid is contraindicated in renal failure.

Fluoroquinolones have common properties:

4. drugs in this group inhibit a vital enzyme of the microbial cell

DNA gyrase;

5. the spectrum of antibacterial action is wide. They are active against gram-positive and gram-negative cocci, Escherichia coli, Salmonella, Shigella, Proteus, Klebsiella, Helicobacter, Pseudomonas aeruginosa. Selected drugs(ciprofloxacin, ofloxacin, lomefloxacin) act on mycobacterium tuberculosis. Spirochetes, Listeria and most anaerobes are not sensitive to fluoroquinolones;

6. fluoroquinolones act on extracellular and intracellular microorganisms;

4.resistance of microflora to fluoroquinolones develops relatively slowly;

5. Fluoroquinolones create high concentrations in the blood and tissues when taken orally, and bioavailability does not depend on food intake.

7. Fluoroquinolones penetrate well into various organs and tissues: lungs, kidneys, bones, prostates, etc.

Indications for use: infections of the urinary, respiratory tract, gastrointestinal tract. Fluoroquinolones are prescribed orally and intravenously.

Side effects: allergic reactions, dyspeptic symptoms, insomnia. Drugs in this group inhibit the development of cartilage tissue, so they are contraindicated for pregnant and nursing mothers; in children can be used only for health reasons. In rare cases

fluoroquinolones can cause the development of tendonitis (inflammation of the tendons), which physical activity may lead to their ruptures.

Second generation fluoroquinolones are more active against gram-positive bacteria, primarily pneumococci. They have an effect on staphylococci, and some drugs retain moderate activity against methicillin-resistant staphylococci. The activity of second generation fluoroquinolones does not differ in relation to penicillin-sensitive and penicillin-resistant strains of pneumococcus. Also, second generation drugs are highly active against chlamydia and mycoplasmas.

Indications for the use of second generation fluoroquinolones: community-acquired respiratory tract infections, skin and soft tissue infections, urogenital infections.

4. NITROFURANS

Nitrofurazone (Furacilin), nitrofurantoin (Furadonin), furazolidone, furazidin (Furagin).

TO general properties Nitrofuran derivatives include the following:

5. ability to disrupt DNA structure. Depending on the concentration, nitrofurans have a bactericidal or bacteriostatic effect;

6. a wide spectrum of antimicrobial action, which includes bacteria (Gram-positive cocci and gram-negative bacilli), viruses, protozoa (Giardia, Trichomonas).

7. high frequency of adverse reactions.

Nitrofurazone is used primarily as an antiseptic (for external use) for the treatment and prevention of purulent-inflammatory processes.

Nitrofurantoin creates high concentrations in urine, therefore it is used for urinary tract infections.

Furazolidone is poorly absorbed from the gastrointestinal tract and creates

high concentrations in the intestinal lumen. Furazolidone is used for intestinal infections of bacterial and protozoal etiology.

Furazidin is used orally for urinary tract infections and topically for rinsing and douching in surgical practice.

Side effects of nitrofuran derivatives: dyspeptic disorders, hepatotoxic, hematotoxic and neurotoxic effects. With prolonged use, nitrofuran derivatives can cause pulmonary reactions (pulmonary edema, bronchospasm, pneumonitis).

Contraindications: severe renal and liver failure, pregnancy.

5. OXAZOLIDINONES

Oxazolidinones are highly active against gram-positive microorganisms.

Linezolid - it is characterized by the following properties:

5. the ability to inhibit protein synthesis in a bacterial cell. Unlike other antibiotics that act on protein synthesis, linezolid acts at the early stages of translation and prevents the formation of the peptide chain. This mechanism of action prevents the development of cross-resistance with such

antibiotics such as macrolides, aminoglycosides, lincosamides, tetracyclines, chloramphenicol;

6. type of action - bacteriostatic.

7. spectrum of action: Bacteroides fragilis, Clostridium perfringens and some strains of streptococci, including Streptococcus pneumoniae and Streptococcus pyogenes; main gram-positive microorganisms,

including methicillin-resistant staphylococci, penicillin- and macrolide-resistant pneumococci and glycopeptide-resistant enterococci. Shows weak activity against gram-negative bacteria;

8. accumulates to a high degree in the bronchopulmonary epithelium. Penetrates well

V skin, soft fabrics, lungs, heart, intestines, liver, kidneys, central nervous system, synovial fluid, bones, gallbladder. Has 100% bioavailability;

9. resistance develops very slowly;

10. dosage regimen: 600 mg (orally or intravenously) every 12 hours. For the treatment of skin and soft tissue infections, the dose is 400 mg every 12 hours;

11. side effects: from the gastrointestinal tract (diarrhea, nausea, staining of the tongue), headache, skin rash.

Drugs

Sulfadimethoxinum Powder, tablets 0.2 and 0.5 g

Ciprofloxacin (Ciprofloxacinum) Tablets of 0.25, 0.5 and 0.75 g; 0.2% solution for infusion in bottles of 50 and 100 ml

Ofloxacin (Ofloxacinum) Tablets 0.2 g Lomefloxacin Tablets 0.4 g Furazolidonum Tablets 0.05 g

Control questions

intestinal infections of bacterial and protozoal etiology?

IX. What is the mechanism of antibacterial action of linezolid?

X. What is the spectrum of action of second generation fluoroquinolones?

TEST TASKS

3) WHICH CHEMOTHERAPEUTIC DRUGS ARE SULPHANAMIDES:

streptomycin

erythromycin

vancomycin

sulfadimezine

4) WHICH OF THE LISTED SULFANAMIDES IS USED FOR A RESORPTIVE EFFECT?

sulfadimidine

sulfacyl sodium

sulfaguanidine

phthalylsulfathiazole

5) WHEN USING SULPHANAMIDES WITH RESORPTIVE ACTION, THE FOLLOWING SIDE EFFECTS ARE POSSIBLE:

hemolytic anemia, methemoglobinemia

neuritis

ototoxicity

development of addiction.

6) TO PREVENT CRYSTALLURIA CAUSED BY SEDIMENTATION OF SULPHANAMIDES AND THEIR METABOLITES, IT IS NECESSARY:

drinking plenty of acidified water

drinking plenty of alkaline fluids

drinking plenty of salted water

restriction of fluid intake

7) HALF-LIFE OF SULPHAMETHOXAZOLE:

5 – 6 hours

40 – 50 hours

3) 10 – 24 hours

4) 30 minutes – 1 hour

8) UROSULPHAN IS USED FOR THE TREATMENT OF INFECTIONS:

Gastrointestinal tract

brain

urinary tract

respiratory tract

9) II GENERATION FLUOROQUINOLONES INCLUDE:

Levofloxacin

Nalidixic acid

fleroxacin

ofloxacin

10) NITROFURAZONE IS USED PRIMARILY AS:

drugs for the treatment of tuberculosis

antiseptic

drugs for the treatment of upper respiratory tract infections

drugs for the treatment of syphilis

11) TYPE OF ACTION OF LINEZOLID:

bacteriostatic

bactericidal

SULPHANAMIDES

Sulfonamides are one of the oldest classes of antibacterial drugs. Over the past decades, they have lost their importance and have very limited indications for use. Sulfonamides are significantly inferior in activity to modern antibiotics and at the same time are characterized by high toxicity. Most clinically important bacteria are currently resistant to sulfonamides.

Sulfonamides practically do not differ from each other in their spectrum of activity. The main difference between them lies in the pharmacokinetic properties, of which the most significant are the half-lives ().

Table 8. Classification of sulfonamides

* The main trade names are given in brackets.

GENERAL PROPERTIES

Mechanism of action

The bacteriostatic effect of sulfonamides is based on their structural similarity to para-aminobenzoic acid (PABA), which is necessary for the life of microorganisms. In environments where there is a lot of PABA (pus, a site of tissue decay), sulfonamides are ineffective. For the same reason, they have little effect in the presence of procaine (novocaine) and benzocaine (anesthesin), which hydrolyze to form PABA.

Activity spectrum

Initially, many gram-positive and gram-negative cocci, gram-negative rods ( E. coli, P.mirabilis etc.), however, they have now become stable.

Sulfonamides remain active against nocardia, toxoplasma, and malarial plasmodia.

Natural resistance is characteristic of enterococci, Pseudomonas aeruginosa and anaerobes.

Pharmacokinetics

Well absorbed from the gastrointestinal tract (except for non-absorbable ones), especially when taken on an empty stomach in crushed form. They are well distributed in the body and penetrate the blood-brain barrier (sulfazine is the best). The highest concentrations in the blood are created by drugs with short and medium duration of action. Metabolized in the liver. Excreted in urine and bile.

Adverse reactions

• Allergic reactions. In severe cases it is possible anaphylactic shock, Stevens-Johnson syndrome, Lyell's syndrome.
• Dyspeptic phenomena.
• Crystalluria due to acidic urine.
  Prevention measures: drink with alkaline mineral water or soda solution.
• Hematotoxicity: hemolytic anemia, thrombocytopenia.
• Hepatotoxicity.

Drug interactions

Sulfonamides enhance the effect indirect anticoagulants and oral antidiabetic drugs by displacing them from connection with plasma proteins.

Indications

• Nocardiosis.
• Toxoplasmosis (usually sulfadiazine in combination with pyrimethamine).
• Tropical malaria resistant to chloroquine (in combination with pyrimethamine).

Contraindications

• Age up to 2 months, since sulfonamides displace bilirubin from binding with plasma proteins and can cause kernicterus (with the exception of congenital toxoplasmosis).
• Severe liver dysfunction.
• Kidney failure.

CHARACTERISTICS OF INDIVIDUAL DRUGS

"SULPHANYLAMIDE"

Streptocide

One of the first antimicrobial drugs with a sulfonamide structure, from which the name of this entire class comes. Currently not used due to low efficiency and toxicity.

SULFADIMIDINE

Sulfadimezin

Dosage

Adults

Orally - 1st dose - 1.0-2.0 g, then 0.5-1.0 g every 4-6 hours 1 hour before meals.

Children over 2 months

Orally - 100-200 mg/kg/day in 4-6 divided doses 1 hour before meals.

Release forms

Tablets of 0.25 g and 0.5 g.

SULPHACARBAMIDE

Urosulfan

Its activity is similar to sulfadimidine. The highest concentrations of the drug are created in the urine. Previously used for urinary tract infections, but no longer used.

SULFADIAZINE

Sulfazine

More active than other sulfonamides, since it binds less to plasma proteins (10-20%) and, as a result, creates higher concentrations in the blood. It penetrates the BBB better than other sulfonamides, therefore it is preferable for toxoplasmosis.

Dosage

Adults

Orally - 1st dose - 1.0-2.0 g, then 0.5-1.0 g every 4-6 hours 1 hour before meals. For nocardiosis up to 8-12 g/day.

Children over 2 months

Orally - 100-150 mg/day in 4 divided doses 1 hour before meals.

Release form

Tablets 0.5 g.

SULPHAMETHOXAZOLE

Has an average degree of binding to plasma proteins (65%). Penetrates well into various organs and tissues. T 1/2 - 12 hours. Included in the combination drug "".

SULFAMONOMETHOXINE

SULPHADIMETOXINE

SULPHAMETHOXYPYRIDAZINE

Sulfapyridazine

They have similar pharmacokinetic properties. They are characterized by high degree binding to plasma proteins (96%) and long T1/2 (24-48 hours). When using these drugs, Stevens-Johnson or Lyell syndromes quite often develop, especially in children.

Dosage

Adults

Orally - on the 1st day 1.0-2.0 g, on subsequent days - 0.5-1.0 g in one dose 1 hour before meals.

Children over 2 months

Orally - on the 1st day 25-50 mg/kg, on subsequent days - 12.5-25 mg/kg 1 hour before meals.

Release form

Tablets 0.5 g.

SULPHALENE

Ultra-long-acting sulfanilamide (T 1/2 - 80 hours). As well as long-acting drugs, it often causes Stevens-Johnson or Lyell syndromes. Not used in children.

Dosage

Adults

Orally - on the 1st day 1.0 g, on subsequent days 0.2 g at a time, or 2.0 g once a week 1 hour before meals.

Release form

Tablets 0.2 g.

Sulfadoxine/pyrimethamine

Fansidar

Sulfadoxine has properties similar to sulfalene. The combination of sulfadoxine with the antimetabolite pyrimethamine is used to prevent and treat malaria.

Dosage

Adults

Orally - 3 tablets once.

Children over 2 months

Orally - up to 1 year: 1/4 tablet, 1-3 years: 1/2 tablet, 4-8 years: 1 tablet, 9-14 years: 2 tablets, once.

Prescribed during meals.

Release form

PHTHALYLSULPHATHIAZOLE

Phthalazole

Practically not absorbed into the gastrointestinal tract. Creates high concentrations in the intestinal lumen. Previously, it was widely used for intestinal infections, including shigellosis. Currently, most strains of Shigella and other pathogens of intestinal infections are resistant.

SILVER SULFADIAZINE

Dermazin

The drug is for local use. When used, as a result of dissociation, silver ions are slowly released, which have an antimicrobial effect that does not depend on the content of para-aminobenzoic acid at the site of application. In this regard, it remains active when penetrating exudates and necrotic tissue.

Active against many pathogens of wound infections - staphylococci, Pseudomonas aeruginosa, Escherichia coli, Proteus, Klebsiella and fungi Candida.

Adverse reactions

Skin burning and itching. Sometimes transient leukopenia is observed (with prolonged use on large surfaces).

Indications

• Burns.
• Trophic ulcers.
• Bedsores.

Release form and dosage

Cream 1%, applied in a thin layer to the affected surface 2 times a day.

COMBINED DRUGS
SULPHANAMIDES WITH TRIMETHOPRIM

With the reduction in the use of sulfonamides, combination drugs containing sulfonamide in combination with trimethoprim have become widespread. The latter is an antimetabolite of folic acid and has a slow bactericidal effect. According to the antimicrobial spectrum, it is close to sulfonamides, but the activity is 20-100 times higher.

Combinations of trimethoprim with sulfonamides are characterized by a bactericidal effect and a wide spectrum of activity, including microflora resistant to many antibiotics and conventional sulfonamides. It should be noted that the observed in vitro the synergism of the components has not been confirmed in clinical settings, and the effect combination drugs due mainly to the presence of trimethoprim. Therefore, in the treatment of respiratory tract infections, trimethoprim is equivalent in effectiveness to the sulfonamide/trimethoprim combination, but is better tolerated.

The most well-known drug from this group is sulfamethoxazole/trimethoprim (co-trimoxazole). Other drugs have no advantages over it and are now practically not used.

The main problems with the use of co-trimoxazole is the continued high potential for the development of severe allergic reactions, characteristic of sulfonamides (Stevens-Johnson and Lyell syndromes), and the widespread resistance of microflora. Resistance to co-trimoxazole in Russia (1998-2000) is S. pneumoniae more than 60%, H.influenzae and community-acquired uropathogenic strains E.coli- about 27%, nosocomial strains E.coli- about 30%, Shigella - about 100%.

SULPHAMETHOXAZOLE/TRIMETHOPRIM (CO-TRIMOXAZOLE)

Bactrim, Septrin, Biseptol

It is a combination of 5 parts sulfamethoxazole (medium-acting sulfonamide) and 1 part trimethoprim.

Activity spectrum

Does not affect enterococci, Pseudomonas aeruginosa, gonococci and anaerobes.

Pharmacokinetics

It is quickly and almost completely absorbed from the gastrointestinal tract, is well distributed in the body, creates high concentrations in bronchial secretions, bile, inner ear, urine, prostate gland. Penetrates through the BBB, especially during inflammation of the meninges. It is excreted mainly in the urine. T1/2 sulfamethoxazole - 10-12 hours, trimethoprim - 8-10 hours.

Adverse reactions

• Hives.
• Stevens-Johnson syndrome.
• Lyell's syndrome.
• Hyperkalemia.
• Aseptic meningitis (more often in patients with collagenosis).
• Dyspeptic symptoms (nausea, vomiting), diarrhea.

Indications

• Pneumocystis pneumonia (treatment and prevention for AIDS).
• Community-acquired infections of MVP (at the level of resistance E.coli in the region less than 15%).
• Intestinal infections(shigellosis, salmonellosis) in regions with low level resistance.
• Staphylococcal infections(second line drug).
• Infections caused by S. maltophilia, B. cepacia.
• Nocardiosis.
• Brucellosis.
• Toxoplasmosis.

Dosage

Adults

Orally - for mild/moderate infections, 0.96 g every 12 hours; for the prevention of Pneumocystis pneumonia - 0.96 g once a day.

Intravenous drip - for severe infections (including those caused by S.aureus, S.maltophilia, B.cepacia) 10 mg/kg/day (trimethoprim) in 2-3 administrations; for Pneumocystis pneumonia - 20 mg/kg/day for 3 weeks.

Children over 2 months

Orally - for mild/moderate infections 6-8 mg/kg/day (trimethoprim) in 2 divided doses; for the prevention of Pneumocystis pneumonia - 10 mg/kg/day in 2 divided doses for 3 days every week.

Intravenous drip - for severe infections (including Pneumocystis pneumonia) - 15-20 mg/kg/day in 3-4 administrations.

Release forms

Tablets of 0.12 g (0.1 g sulfamethoxazole, 0.02 g trimethoprim), 0.48 g (0.4 g sulfamethoxazole, 0.08 g trimethoprim) and 0.96 g (0.8 g sulfamethoxazole, 0 ,16 g trimethoprim).

Syrup 0.2 g sulfamethoxazole and 0.04 g trimethoprim/5 ml. Solution in ampoules: 0.4 g of sulfamethoxazole and 0.08 g of trimethoprim/5 ml.

SULFAMONOMETHOXINE/TRIMETHOPRIM

Sulfatone

A drug with basic characteristics similar to co-trimoxazole. 1 tablet contains 0.25 g of sulfamonomethoxine (long-acting sulfonamide) and 0.1 g of trimethoprim.

The dosage is similar to co-trimoxazole, but on the 1st day a loading (double) dose is prescribed - adults, 2 tablets 2 times a day.

You should remember high risk development of Stevens-Johnson or Lyell syndromes due to the presence of sulfamonomethoxine.

SULFAMETROL/TRIMETHOPRIM

Lidaprim

Its main characteristics are similar to co-trimoxazole. Consists of sulfametrol (sulfanilamide average duration action close to sulfamethoxazole) and trimethoprim in a ratio of 5:1.

Release forms

Tablets of 0.12 g (0.1 g sulfamethoxazole, 0.02 g trimethoprim), 0.48 g (0.4 g sulfamethoxazole, 0.08 g trimethoprim) and 0.96 g (0.8 g sulfamethoxazole, 0 ,16 g trimethoprim); suspension, 0.2 g sulfamethoxazole and 0.04 g trimethoprim/5 ml; solution in ampoules: 0.8 g of sulfamethoxazole and 0.16 g of trimethoprim/250 ml.

The mechanism of the bacteriostatic effect of sulfonamides is associated with their competitive antagonism with para-aminobenzoic acid (PABA).

PABA is included in the structure of dihydrofolic acid, which is synthesized by many microorganisms. Due to their chemical similarity to PABA, sulfonamides prevent its inclusion in dihydrofolic acid. In addition, they competitively inhibit dihydropteroate synthetase. Impaired synthesis of dihydrofolic acid reduces the formation of tetrahydrofolic acid from it, which is necessary for the synthesis of purine and pyrimidine bases.

Spectrum of action sulfonamides is quite broad:

a) bacteria - pathogenic cocci (gram-positive and gram-negative), Escherichia coli, pathogens of dysentery, Vibrio cholerae, pathogens of gas gangrene, pathogens of anthrax, diphtheria, catarrhal pneumonia, influenza, plague;

b) chlamydia - causative agents of trachoma, paratrachoma, ornithosis, inguinal lymphogranuloma;

c) actinomycetes;

d) protozoa - the causative agent of toxoplasmosis, malarial plasmodium.

When the principles of chemotherapy are violated, resistant strains of microbes develop. Reasons for resistance: microbes produce more PABA, bypass pathways for protein synthesis develop. It must be taken into account that some drugs that contain a PABA residue in their molecule (for example, novocaine) can have a pronounced antisulfonamide effect,

Classification of sulfonamides

1. Sulfonamides, poorly absorbed from the gastrointestinal tract and slowly released from the body (acting mainly in the intestines):

Sulgin- used for dysentery, colitis, enterocolitis, carriage of dysentery bacilli, bacilli typhoid fever, to prepare for intestinal operations.

Phthalazole- splits into norsulfazole and phthalic acid. The indications are the same. Less toxic than sulgin.

2. Sulfonamides with good absorption from the gastrointestinal tract:

- short-term action

Norsulfazole- acts primarily on hemolytic streptococcus, pneumococci, gonococci, staphylococci, E. coli. Penetrates well into the brain and lungs. It is used orally for infections of the bronchopulmonary system, meningitis, staphylococcal and streptococcal sepsis. Causes crystalluria.

long acting

Sulfadimethoxine(Madribon) - penetrates poorly through the BBB, but penetrates well into other organs and tissues. It is excreted by the kidneys in the form of soluble glucuronides, so it practically does not cause crystalluria.

GENERAL PRINCIPLES OF SULFANAMIDE TREATMENT

DRUGS

1. Early start of treatment.

2. The course of treatment is at least 7 days.

3. High doses of the drug.

On the first day of treatment, the maximum single and daily doses are given for saturation. For short-acting sulfonamides, the highest single dose is 2.0; daily 7.0; reception frequency 4-6 times. On subsequent days of treatment daily dose reduced by 1.0 per day. The course dose is up to 30.0.

Long-acting drugs: on the first day, 2.0 is prescribed once, and on subsequent days - 0.5 - 1.0 once. Course dose up to 10.0.

4. To prevent crystalluria, alkaline drinking is necessary (3 liters of liquid per day).

5. Sulfonamides cause inhibition of saprophytic bacteria in the intestines that synthesize B vitamins, so medium doses of B vitamins should be prescribed.

6. Before and during treatment, conduct a blood test.

7. Before prescribing drugs, find out from the patient their tolerance.

8. Urine tests for the presence of microhematuria.

9. Combination with antibiotics.