Sulfanilamide drugs and other antimicrobial agents (phthalazole, etazol, sulfacyl sodium, sulfadimethoxine, sulfalene, biseptol (co-trimoxazole), salazosulfopyridine, salazopyridazine, nalidixic acid, nitroxoline, ciprofloxacin, levofloxacin.

12.10.2020

SYNTHETIC ANTIBACTERIAL AGENTS

Synthetic antibacterial agents are presented in 6 main classes:

5. Sulfonamides.

6. Quinolone derivatives.

7. Nitrofuran derivatives.

8. Derivatives of 8-hydroxyquinoline.

9. Quinoxaline derivatives.

10. Oxazolidinones.

1. SULPHANYLAMIDE PREPARATIONS

Sulfanilamides 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 path)

a) Short-acting (half-life< 10 ч)

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

c) Long-term action (half-life 24-48 hours) Sulfadimethoxin, sulfamonomethoxin.

d) Ultra-long-acting (half-life\u003e 48 hours) Sulfamethoxypyrazine (Sulfalene).

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

Phthalylsulfathiazole (Phthalazole), sulfaguanidine (Sulgin).

13. Sulfonamides for topical use

Sulfacetamide (Sulfacil sodium, Albucid).

14. Combined preparations of sulfonamides and salicylic acid

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

15. Combined preparations of sulfonamides with trimethoprim

Co-trimoxazole (Bactrim, Biseptol).

Sulfonamides have a bacteriostatic effect on microorganisms. The mechanism of the bacteriostatic action 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, malaria plasmodia and actinomycetes.

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

Sulfonamides for systemic action cause a large number of side effects. When using them, violations of the blood system (anemia, leukopenia, thrombocytopenia), hepatotoxicity, allergic reactions (skin rashes, fever, agranulocytosis), dyspeptic disorders are possible. At acidic pH values \u200b\u200bof urine - crystalluria. For its prevention, sulfonamides must be washed down 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 pathogens of intestinal infections have acquired resistance to sulfonamides. To improve 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, vitamins of the B group should be prescribed, since sulfonamides inhibit the growth of E. coli, which is involved in the synthesis of B vitamins.

Sulfanilamide is one of the first antimicrobial drugs of sulfanilamide structure. Currently, the drug is practically not used due to its 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.

Sulfamethoxypyrazineused daily for acute or fast infectious processes, once every 7-10 days - for chronic, long-term current infections.

Sulfacetamide is a topical sulfonamide. The drug is usually well tolerated. It is used in eye 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, lower concentration solutions 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 of sulfamethoxazole (medium-acting sulfonamide) and 1 part of trimethoprim. The combination of trimethoprim with sulfonamides is characterized by a bactericidal effect and a broad spectrum of antibacterial action, including microflora resistant to many antibiotics and common sulfonamides. Co-trimoxazole is well absorbed from the gastrointestinal tract, penetrates into many organs and tissues, creates high concentrations in bronchial secretions, bile, urine, prostate gland. Penetrates the BBB, especially with 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 severe liver, kidney and hematopoietic disorders. The drug should not be administered during pregnancy.

Sulfamethoxazoleis part of the combined 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 (1st generation drugs)

Ciprofloxacin (Tsifran, Tsiprobay), lomefloxacin (Maxaquin), norfloxacin (Nomycin), fleroxacin (Quinodis), ofloxacin (Tarivid).

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

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

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

Side effects of dyspeptic disorders, CNS excitation, liver dysfunctions, allergic reactions. Nalidixic acid is contraindicated in renal failure.

Fluoroquinolones have general properties:

4. drugs of 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. Certain drugs (ciprofloxacin, ofloxacin, lomefloxacin) act on mycobacterium tuberculosis. Spirochetes, listeria and most anaerobes are not sensitive to fluoroquinolones;

6. fluoroquinolones act on outside and intracellularly localized microorganisms;

4. resistance of microflora to fluoroquinolones develops relatively slowly;

5. Fluoroquinolones create high concentrations in 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, prostate, etc.

Indications for appointment: infections of the urinary tract, respiratory tract, gastrointestinal tract. Oral and intravenous fluoroquinolones are prescribed.

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

fluoroquinolones can cause tendonitis (inflammation of the tendons), which can rupture with exercise.

Generation II 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 pneumococcal strains. Also, second generation drugs are highly active against chlamydia and mycoplasma.

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

4. NITROFURANES

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

The general properties of nitrofuran derivatives include the following:

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

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

7. high frequency of adverse reactions.

Nitrofurazone is used mainly as an antiseptic (for external use) for the treatment and prevention of pyoinflammatory processes.

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

Furazolidone is poorly absorbed in the gastrointestinal tract and creates

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

Furazidine is used orally for urinary tract infections and topically for washing 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 hepatic failure, pregnancy.

5. OXAZOLIDINONES

Oxazolidinones are highly active against gram-positive microorganisms.

Linezolid - it has the following properties:

5. the ability to inhibit protein synthesis in a bacterial cell. Unlike other antibiotics that act on protein synthesis, linezolid acts in 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. the type of action is 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. highly accumulates in the bronchopulmonary epithelium. Penetrates well

in skin, soft tissues, 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 (oral or intravenous) every 12 hours. When treating infections of the skin and soft tissues, 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

Sulfadimethoxin (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 0.2 g tablets Lomefloxacin 0.4 g tablets Furazolidonum 0.05 g tablets

test questions

	List the main groups of synthetic chemotherapeutic

	What sulfonamides are used for resorptive action?
	How many parts of sulfamethoxazole and trimethoprim are included
the combined sulfonamide "Co-trimoxazole"?
	What are the side effects of sulfonamides?
	Which group of quinolones are more active against gram-positive
bacteria?
	What synthetic chemotherapeutic agent is used for

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 the second generation fluoroquinolones?

TEST PROBLEMS

3) WHICH OF CHEMOTHERAPEUTIC PREPARATIONS RELATED TO SULPHANYLAMIDES:

streptomycin

erythromycin

vancomycin

sulfadimezin

4) WHICH OF THE LISTED SULPHANYLAMIDES IS USED FOR RESORPTIVE ACTION?

sulfadimidine

sulfacyl sodium

sulfaguanidine

phthalylsulfathiazole

5) THE FOLLOWING SIDE EFFECTS ARE POSSIBLE WITH THE APPLICATION OF RESORPTIVE SULPHANYLAMIDES:

hemolytic anemia, methemoglobinemia

neuritis

ototoxicity

development of addiction.

6) FOR PREVENTION OF CRYSTALLURIA CAUSED BY THE DEPOSIT OF SULPHANYLAMIDES AND THEIR METABOLITES, IT IS NECESSARY:

drinking plenty of acidified water

plentiful alkaline drink

drinking plenty of salted water

limiting fluid intake

7) SEMI-RELEASE PERIOD OF SULFAMETOXAZOLE:

5 - 6 hours

40 - 50 hours

3) 10 - 24 hours

4) 30 minutes - 1 hour

8) UROSULFAN IS USED FOR TREATMENT OF INFECTIONS:

Gastrointestinal tract

brain

urinary tract

respiratory tract

9) GENERATION II FLUORQINOLONES ARE:

Levofloxacin

Nalidixic acid

fleroxacin

ofloxacin

10) NITROFURAZONE IS USED PREVIOUSLY AS:

drugs for the treatment of tuberculosis

antiseptic

remedies for treating upper respiratory tract infections

remedies for syphilis

11) TYPE OF ACTION OF LINEZOLIDE:

bacteriostatic

bactericidal

Sulfanilamide preparations (synonym sulfonamides) - synthetic chemotherapeutic agents of a wide spectrum of action from the group of derivatives of sulfanilic acid amide (sulfanilamide).

Streptococci, and, diplococci (gonococci, meningococci, pneumococci), intestinal, dysentery, diphtheria and anthrax bacilli, brucella, cholera vibrios, actinomycetes, chlamydia (causative agents of trachudoma, ornithosis and also clostridia), some protozoal infections (malaria, a). In addition, individual pathogens of deep ovaries (nokardin, actinomycetes) are sensitive to S. of the item. Some S. p. (Sulfadimethoxine, sulfapyridazine, sulfalene) are active against mycobacterium leprosy (see. Antileprosy agents ). Salmonella, Pseudomonas aeruginosa, Mycobacterium tuberculosis, spirochetes, leptospira and viruses are among the items resistant to S. of the item. Microorganisms of S. of the item, sensitive to them, in concentrations in which they accumulate in the body in therapeutic doses, act bacteriostatically.

The mechanism of antimicrobial action of S. p. Is due to the fact that they block the process of synthesis of dihydrofolic acid at the stage of formation of dihydropteroic acid from dihydropteridine and para-aminobenzoic acid (PABA) with the participation of the enzyme dihydropteroate synthetase (dihydrofolate synthetase). It is believed that the impairment of the synthesis of dihydropteroic acid occurs primarily as a result of the inclusion of S. p. Instead of PABA as a substrate of dihydropteroate synthetase, because in terms of chemical structure, S. of the item are similar to PABA. As a result, the formation of analogs of dihydrofolic acid occurs, which do not have its inherent biological activity. In addition, during the interaction of S. of the item with dihydropteridine in the presence of ATP and magnesium ions, an intermediate metabolite is formed that inhibits dihydropteroate synthetase, which leads to inhibition of the formation of dihydrofolic acid. It is also possible that S. of the item prevent the inclusion of dihydropteridine in the synthesis of dihydrofolic acid. Ultimately, the violation of the formation of dihydrofolic acid under the influence of S. of the item leads to a decrease in the formation of tetrahydrofolic acid and the resulting inhibition of the biosynthesis of nucleotides and a delay in the development and reproduction of microorganisms. These features of the mechanism of action explain the fact that only those microorganisms in which the process of synthesis of dihydrofolic acid occurs are sensitive to S. of the item. Microorganisms and cells of a macroorganism that utilize ready-made dihydrofolic acid from the external environment are not sensitive to the action of S. of the item.

With an excess of PABA and its derivatives in the medium, for example, novocaine, anestezin, etc., as well as methionine, folic acid, purine and pyrimidine bases, the antimicrobial activity of S. p. Decreases. A decrease in S.'s activity of the item in the presence of pus and wound discharge is associated with the high content of PABA and other antagonists of sulfa drugs in these substrates.

The antimicrobial effect of S. of the item is enhanced by drugs (for example, trimethoprim), which inhibit the conversion of dihydrofolic acid to folic (tetrahydrofolic) acid by inhibiting the enzyme dihydrofolate reductase. With the simultaneous use of S. of the item with trimethoprim, the synthesis of tetrahydrofolic acid is disrupted at two successive stages - at the stage of formation of dihydrofolic acid (under the influence of S. of the item) and at the stage of transformation of the latter into tetrahydrofolic acid (under the influence of trimethoprim), as a result of which a bactericidal effect develops ...

After absorption into the blood of S. of the item is reversible, but to an unequal degree 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 degree of their binding to blood plasma proteins does not affect the rate of S.'s release of the item from the body. S. of the item is metabolized in the liver mainly by acetylation. The resulting acetylated metabolites of S. of the item do not possess antimicrobial activity and are excreted from the body through the kidneys. 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 urine reaction, since 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 orally 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 medium duration (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 streptocid, 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, ovaries, 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, salazodimethoxin and salazosulfapyridine, which are used primarily for the treatment of nonspecific ulcerative a. 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 in the intestine, 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, for the treatment of drug-resistant forms of malaria, combinations of sulfalene with chloridine are used, and for the treatment of a - combinations of sulfazine with chloridine.

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. Thus, 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, C.

the item, 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 action of 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, disturbances on the part of c.ns. (headache, dizziness, etc.), leukopenia, methemoglobinemia, etc. Due to poor solubility in water, S. p. and the products of their acetylation in the body can fall 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: powder, 0.5 tablets r... Storage: List B; in a dark place.

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

Streptocide (Streptocidum, synonym for white streptocid) 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 0.2-0.3 each r, from 6 to 12 years old, 0.3-0.5 r appointment. Higher doses for adults inside single 2 r, daily 7 r... It is used locally in the form of powders, ointments (10%) or liniment (5%). Release form: powder, tablets 0.3 and 0.5 r; 10% ointment; 5% liniment. 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

Silver sulfadiazine (Sulfadiazini argenti) is used topically. It is part of the Dermazin ointment, which is applied to the surface with a layer of 2-4 mm 2 times a day, followed by the imposition of a sterile dressing. The ointment is not prescribed for premature and newborn babies; in pregnant women, it is used for health reasons (with an 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 for the first appointment, then 0.025 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 cycle 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

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

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% solutions (eye drops) in dropper tubes, 1.5 each 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), for 5-6 days 1 r every 8 h (3 r per day). After 5-6 days, the treatment is repeated: 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 for etazole soluble) is administered intravenously (slowly) in 5-10 ml 10% or 20% solution. In pediatric practice, the drug is used orally in granules, which are dissolved in water before use and prescribed to children at the age of 1 year - 5 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.

Sulfonamides familiar to people have long established themselves, since they appeared even before the history of the discovery of penicillin. To date, these drugs in pharmacology have partially lost their significance, since they are inferior in effectiveness to modern medicines. However, in the treatment of some pathologies, they are irreplaceable.

What are sulfa drugs

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

Classification of sulfa drugs

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

Sulfonamides, rapidly absorbed from the gastrointestinal tract. They are prescribed for systemic therapy of infections that are caused by sensitive microorganisms: Etazole, Sulfadimethoxin, Sulfametizole, Sulfadimidine (Sulfadimezin), Sulfacarbamide.
Sulfonamides, not completely or slowly absorbed. They create a high concentration in the large and small intestines: Sulgin, Ftalazol, Ftazin. Etazole sodium
Topical sulfonamides. Well proven in ophthalmic therapy: Sulfacil sodium (Albucid, Sulfacetamide), Silver sulfadiazine (Dermazin), Mafenide acetate ointment 10%, Streptocide ointment 10%.
Salazosulfonamides. This classification of compounds of sulfonamides with salicylic acid: Sulfasalazine, Salazomethoxin.

The mechanism of action of sulfa drugs

The choice of a medicine for treating a patient depends on the properties of the pathogen, because the mechanism of action of sulfonamides is reduced to blocking sensitive microorganisms in the cells of folic acid synthesis. For this reason, some drugs, for example, Novocaine or Methionomyxin, are incompatible with them, since they weaken their effect. The key principle of action of sulfonamides is a violation of the metabolism of microorganisms, suppression of their reproduction and growth.

Indications for the use of sulfonamides

Depending on the structure, sulfide preparations have a general formula, but different pharmacokinetics. There are dosage forms for intravenous administration: sodium sulfacetamide, streptocid. Some drugs are injected intramuscularly: Sulfalene, Sulfadoxin. Combination drugs are used in both ways. For children, sulfonamides are used topically or in tablets: Co-trimoxazole-Rivofarm, Cotrifarm. Indications for the use of sulfonamides:

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

List of sulfa drugs

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

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

Combined sulfa drug

Time does not stand still, and many strains of microbes have mutated and adapted. Doctors have found a new way to fight bacteria - they have created a combined sulfa drug in which antibiotics are combined with trimethoprim. The list of such sulfonic drugs:

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

Sulfanilamide preparations for children

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

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

Instructions for the use of sulfonamides

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

Side effects of sulfa drugs

With prolonged or uncontrolled use, side effects of sulfonamides may appear. These are allergic reactions, nausea, dizziness, headaches, vomiting. With systemic absorption, sulfonic drugs can pass through the placenta and then be found in the fetal blood, causing toxic effects. For this reason, during pregnancy, the safety of using drugs is questionable. The physician should consider this chemotherapeutic effect when prescribing them to pregnant women and during lactation. Contraindication to the use of sulfonamides is:

hypersensitivity to the main component;
anemia;
porphyria;
hepatic or renal impairment;
pathology of the hematopoietic system;
azotemia.

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:

Video: what is sulfonamides

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

Classification of sulfa drugs

Sulfonamides, rapidly absorbed from the gastrointestinal tract. They are prescribed for systemic therapy of infections that are caused by sensitive microorganisms: Etazole, Sulfadimethoxin, Sulfametizole, Sulfadimidine (Sulfadimezin), Sulfacarbamide.
Sulfonamides, not completely or slowly absorbed. They create a high concentration in the large and small intestines: Sulgin, Ftalazol, Ftazin. Etazole sodium
Topical sulfonamides. Well proven in ophthalmic therapy: Sulfacil sodium (Albucid, Sulfacetamide), Silver sulfadiazine (Dermazin), Mafenide acetate ointment 10%, Streptocide ointment 10%.
Salazosulfonamides. This classification of compounds of sulfonamides with salicylic acid: Sulfasalazine, Salazomethoxin.

The mechanism of action of sulfa drugs

Indications for the use of sulfonamides

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

List of sulfa drugs

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

Combined sulfa drug

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

Sulfanilamide preparations for children

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

Instructions for the use of sulfonamides

Side effects of sulfa drugs

hypersensitivity to the main component;
anemia;
porphyria;
hepatic or renal impairment;
pathology of the hematopoietic system;
azotemia.

The price of sulfa drugs

Video: what is sulfonamides

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

Sulfonamides

Lecture for 3rd year students of FVM

Lecture plan

1. GENERAL CHARACTERISTIC OF SULPHANYLAMIDES

· SHORT-ACTION PREPARATIONS

· SULPHANYLAMIDES, POORLY ABSORATED FROM THE GASTROINTESTINAL TRACT

Sulfanilamide preparations - a large group of medicinal substances, the structure of which is based on sulfanilic (para-aminobenzenesulfonic) acid.

Sulfonamides are active antimicrobial agents. In recent years, interest in this group of drugs has increased in connection with the synthesis of long-acting sulfonamides and the creation of drugs combined with trimethoprim.

Sulfanilamide preparations are derivatives of white streptocide, which are very similar in physical and chemical properties.

All sulfonamides are odorless white or slightly yellowish powders, some have a bitter taste. Most of them are poorly soluble in water, better - in dilute acids and aqueous solutions of alkalis (except for sulgin). Increasing the temperature of the solvent improves the solubility of the drugs. A mixture of two or more sulfonamides dissolves somewhat better than either of its components alone. Only sulfacil has good solubility.

Sulfonamides are amphoteric, they form salts with strong alkalis (with the exception of sulgin) and with strong acids. Some sulfonamide salts are readily soluble in water; they can be used for intravenous injections when it is necessary to quickly create a high concentration of the drug in the blood and organs. Due to the fact that sodium salt in aqueous solutions have a strong alkaline reaction (pH 10.5-12.5), when administered subcutaneously and intramuscularly, they have a strong irritant effect. Infiltration of the injection site with isotonic sodium chloride solution can weaken tissue necrosis, and infiltration with novocaine solution significantly reduces the pain response. For the same reason, undiluted sodium salts should not be ingested. Intravenously, large animals are injected with 10-25%, and small - 5% solutions. The exception is the sodium salt of sulfacil, which in solution gives an almost neutral reaction, and it can be prescribed in higher concentrations.

In solutions, sulfonamides dissociate into ions. Pharmacological activity is related to their dissociation constants. For example, the bacteriostatic effect is more pronounced in alkaline solutions, since more ions are formed under these conditions. Norsulfazole and sulfacil dissociate well, streptocide is much worse. Compounds that are more capable of acid dissociation are better absorbed. Sulfanilamide preparations are readily soluble in biological fluids, including blood plasma.

Store sulfonamides according to list B in a well-sealed container, protected from light. Shelf life of drugs from 3 to 10 years

Drugs in this group belong to chemotherapeutic agents with a wide antibacterial spectrum of action, since they suppress the vital activity of many types of gram-positive and gram-negative bacteria: streptococci, staphylococci, meningococci, gonococci, bacteria of the entero-typhoid-dysentery group and many others. Difficult soluble compounds (phthalazole and its analogs, sulcimide and urosulfan) act primarily on gram-negative bacteria. Sulfonamides are active against large viruses (pathogens of trachoma, inguinal lymphogranulomatosis), coccidia, plasmodium malaria and toxoplasma, actinomycetes, etc.

Sulfanilamide drugs in small 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 most important feature of sulfonamides is their high in vivo activity with a relatively weaker in vitro effect. Under their influence, microbes swell, stop multiplying, produce toxins, and become more vulnerable to the body's defenses. The selectivity of individual drugs in relation to certain causative agents of infectious diseases has been established. So, norsulfazole and sulfazole are more active in staphylococcal infections, streptocid. - with streptococcal, and sulfapyridazine is very effective in sepsis caused by coli bacteria.

The bacteriostatic effect depends on the chemical structure of the drug, the degree and strength of binding to plasma proteins, the reaction of the environment, the dissociation constant and other factors. Of great importance is the state of the nervous system, the protective forces of the macroorganism, which play a leading role in. the final elimination of the infectious process.

The mechanism of action of sulfonamide drugs is based on the antagonism between sulfonamides and para-aminobenzoic acid (PABA). Due to the structural similarity of the molecule of para-aminobenzoic acid and sulfonamides, the latter are able to displace PABA from the enzyme systems of the microorganism. Sulfonamides disrupt the process of obtaining by microbes the "growth factors" necessary for their development - folic acid and other substances, the molecule of which includes PABA. Drugs disrupt the synthesis of methionine, purine and pyrimidine bases in the microbial cell, which in turn leads to disruption of nucleic acid synthesis and nucleoproteins.

The bacteriostatic effect of sulfonamides is manifested only at a certain concentration of drugs in the environment of microbes. This concentration should be sufficient to prevent microorganisms from using the para-aminobenzoic acid contained in the tissues. The higher the concentration of PABA, the more sulfa drug is required for the onset of the antimicrobial effect. It was found that 1600 parts of streptocide, 100 parts of sulfazine and 36 parts of norsulfazole are required to neutralize one part of PABA.

The special activity of sulfonamides in relation to some microbes (streptococci, gonococci, etc.) and the lack of activity in relation to others is explained by the fact that for the former, the presence of PABA in the environment is necessary, and for the latter, this acid is not essential. In the same way, it is possible to explain the creation of a high therapeutic effect of sulfanilamide drugs in acute processes, when the metabolism in the microbial cell is intense and the malnutrition and metabolism of microorganisms at this moment immediately affects their condition.

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

The mechanism of antimicrobial action of sulfanilamide drugs is determined not only by the competitive relationship between sulfonamides and para-aminobenzoic acid. Sulfonamides interfere with the synthesis of dihydrofolic acid in a microorganism from glutamic and para-aminobenzoic acids. Protein substances (pus, dead tissue) containing a large amount of PABA, as well as some drugs, the molecule of which contains a para-aminobenzoic acid residue (novocaine, anestezin), are inhibitors of the activity of sulfonamides. At the same time, the presence of urea increases their bacteriostatic activity.

Sulfanilamide preparations do not affect the catalase of microbes, the activity of indophenol oxidase, bacterial aspartase, do not significantly change the activity of dehydrases and do not affect proteolytic enzymes. However, with some enzymes, as well as with PABA, the drugs of this group can enter into competitive relationships. So, for example, they inhibit the activity of carboxylase of enzymes containing pikotinamide (this explains the stronger bacteriostatic effect of norsulfazole on staphylococci). Sulfonamides do not act in vitro on toxins and endotoxins of bacteria, but they are able to neutralize the effect of endotoxins on the body.

Exposure to small doses or the administration of sulfonamides at long intervals leads to the development of an adaptive reaction in microbes, a change in the pathway of formation of enzyme systems necessary for growth and reproduction. As a result, sulfonamide-resistant races of microorganisms arise. The blockade of PABA with sulfonamides does not significantly disrupt the vital activity of microbes.

The resistance of microorganisms acquired to one sulfanilamide drug extends to other drugs in this group (complete cross-resistance). The acquired resistance of bacteria to sulfonamides, associated with their increased production of PABA, can be genetically inherited.

In sulfonamide-resistant cultures, morphology, cultural and biochemical properties, antigenic structure, and virulence change. The development of sulfonamide resistance depends both on the type of microorganisms, their state, and on the state of the macroorganism (resistance, the nature of the inflammatory process, etc.).

Almost all sulfonamide-resistant strains of microorganisms remain highly sensitive to antibiotics, nitrofurans and other chemotherapeutic agents.

Sulfanilamide compounds have a wide range of action on a macroorganism and should be considered as specific nervous stimuli. They reduce the increased reactivity of the body, have an antipyretic effect. Sulfanilamide drugs act anti-inflammatory, inhibit regeneration processes when applied topically; reduce the activity of nucleophosphatase in the liver, kidneys, spleen, disrupt the normal processes of acetylation, being a specific inhibitor of carbonic anhydrase, reduce the ability of plasma to bind carbon dioxide, inhibit gas exchange, reduce the activity of other enzyme systems, stimulate the process of phagocytosis, increase the body's resistance to toxins.

Due to the combination of anti-allergic, antipyretic properties with bacteriostatic action, sulfonamides can be used for various diseases accompanied by inflammatory processes. Their impact on micro - and macroorganisms complement each other, providing a well expressed therapeutic effect.

Sulfanilamide preparations are low toxic. However, prolonged use of them in overestimated doses can lead to the development of undesirable, that is, toxic, effects: suppression of beneficial microflora in the gastrointestinal tract, cyanosis, leukopenia, anemia, B-avitaminosis, agranulocytosis, and general suppression. With insufficient renal function or with the appointment of large doses of drugs, crystalluria phenomena may occur. Correct administration of sulfonamides to animals does not cause side effects.

During the period of application of sulfonamides, animals should not be given drugs that easily split off sulfur (sodium hyposulfite, Glauber's salt, etc.).

Most sulfonamides are easily absorbed from the gastrointestinal tract (streptocid, norsulfazole, etazole, sulfazine, sulfadimezine, sulfapyridazine, sulfadimethoxine, etc.) and rapidly accumulates in the blood, organs and tissues in bacteriostatic concentrations, penetrates the blood-encephalic barrier. The bulk of the drugs are absorbed in the small intestine. The absorption rate depends on the degree of acid dissociation. The sodium salts of the preparations are very well absorbed. Some sulfonamides, such as phthalazole, sulgin, phtazin, are difficult to absorb, are in the intestine for a relatively long time in high concentrations and are excreted mainly with feces, therefore they are used mainly for diseases of the gastrointestinal tract.

In many infectious diseases, the pathogen is not in the blood for a longer time, but in various organs and tissues, therefore, the determination of the concentration of sulfanilamide preparations in organs and tissues is often more significant than the determination of their concentration in the blood.

The rate and degree of distribution of sulfonamides are influenced by the chemical structure of the drugs, the dose size, the route of administration, the activity of the pathological process, and a number of other factors. In the blood, organs and tissues, Sulfanilamide preparations are in the form of free compounds and in a state bound to plasma proteins, part of the preparation undergoes acetylation. For the manifestation of antibacterial activity, the concentration of free sulfonamide in plasma must be at least 40 μg / ml.

The strength and degree of binding of sulfa drugs with plasma proteins are of great importance in the penetration of drugs into various organs and tissues and affect the rate of their excretion from the body. Sulfonamides bind mainly to the albumin fraction, diffuse into tissues much worse, therefore, in body fluids rich in albumin, the concentration of drugs is usually higher than in fluids containing less albumin (cerebrospinal fluid, chamber water). The permeability of sulfanilamide drugs through the blood-brain barrier depends on both the properties of the drug and the state of the macroorganism. In an infected organism, sulfonamides penetrate into the cerebrospinal fluid in much larger quantities than in a healthy organism. They are unevenly distributed in various organs and tissues. The largest amount of drugs is found in the kidneys, significant amounts are found in the lungs, walls of the stomach and intestines, heart, liver, and much less in muscles, spleen, adipose tissue. Sulfonamides penetrate well through the placenta.

In humans and animals, sulfonamide compounds, like other medicinal substances, undergo splitting, oxidation, and acetylation. The acetylation process is especially important for clinical practice. It occurs mainly in the liver, both due to acetic acid coming from the outside, and due to acid formed in the body from pyruvic acid.

In a healthy body, the degree of acetylation is slightly higher than in an infected one. In addition, the degree of acetylation of sulfonamides increases with their prolonged use, decreased urine output, kidney disease, accompanied by renal failure. The intensity of acetylation is not the same in different animal species.

Acetylated derivatives of sulfonamides do not act on microorganisms and dissolve in water much worse. Due to poor solubility, especially in acidic urine, aceto products precipitate with the formation of conglomerates that clog the lumen of the renal tubules, followed by impaired diuresis.

To uniformly maintain the therapeutic concentration of sulfa drugs in the blood, organs and tissues, the rate of their elimination from the body plays an important role. Most sulfonamides (sulfacil, streptocid, norsulfazole, etc.) are relatively quickly eliminated from the body of animals. They are eliminated mainly by the kidneys as an unchanged parent compound and in a bound state with acetic and glucuronic acids. In addition to the kidneys, sulfonamides can be secreted by the mammary, sweat, salivary bronchial and intestinal glands, as well as the liver.

From a therapeutic point of view, drugs that are rapidly absorbed from the gastrointestinal tract and are slowly released from the body are especially valuable. Depending on the rate of elimination of sulfonamides from the body, I divide them into three groups:

1) fast-acting drugs (streptocid, norsulfazole etazole, sulfacil, urosulfan, sulfadimezin, etc.);

2) drugs of medium duration of action (sulfazine, methylsulfazine, etc.),

3) long-term and ultra-long-acting drugs (sulfapyridazine, sulfadimethoxine, sulfamonomethoxin, sulfalene, etc.).

The rate of elimination from the body largely determines the size of the dose and the frequency of taking the drug. The indicator of the rate of elimination is the value of T50%, or T1 / 2, - the half-life, that is, the time for a decrease in the maximum concentration in the blood by 2 times. For short-acting drugs, T1 / 2 is less than 8 hours, the average duration of action is 8-16 hours, and for long-acting and ultra-long-acting drugs, it is 24-56 hours or more.

Long-acting sulfa drugs are well absorbed from the gastrointestinal tract, creating high concentrations in the blood, and most importantly, they remain in the body for a long time. They can be administered at significantly lower doses and at longer intervals between administrations. These properties significantly expand the prospects for the use of compounds of this group in veterinary practice.

For the manifestation of bacteriostatic activity, a certain amount of the drug is required in the blood, organs and tissues of the animal. With relatively mild diseases, the concentration of drugs in the blood should be 40-80 μg / ml, with diseases of moderate severity - 80-100 μg / ml and in severe cases - 100-150 μg / ml. The creation and maintenance of the indicated concentrations of drugs in the blood depend on the scheme of sulfonamide administration.

Short-acting drugs are prescribed 4-6 times, medium-duration drugs - 2 times and long-acting drugs - 1 time per day. The first dose (initial) should be almost twice the subsequent (maintenance) doses, calculated to replenish the released drug. The course of treatment is usually 3-8 days. The value of the initial and maintenance doses depends on the sensitivity of the pathogen, the severity of the disease, the age and condition of the animal and the characteristics of the drug.

Sulfonamides are indicated for the treatment of infectious diseases of the respiratory tract (tracheitis, bronchitis, pneumonia, purulent pleurisy, etc.), gastrointestinal diseases of various etiologies (dyspepsia, coccidiosis, dysentery, gastroenterocolitis, etc.); erysipelas, myt, postpartum sepsis, pyelitis, cystitis, salmonellosis, colibacillosis, pasteurellosis, wound and other infections caused by microorganisms sensitive to sulfonamides.

Sulfanilamide drugs are prescribed externally, internally, intramuscularly, subcutaneously and intravenously. Externally used in the form of ointments, liniment, powders.

For the most rational sulfonamide therapy, it is advisable to simultaneously prescribe a mixture of two or three sulfonamide drugs with different rates of absorption and excretion. Good results are obtained by the combined use of sulfa drugs with antibiotics, organic paints and other chemotherapeutic agents. In these cases, a smaller dose of the drug is required and the possibility of the formation of sulfonamide-resistant races of microorganisms is reduced.

There are few contraindications to the use of sulfa drugs in animals: general acidosis, diseases of the hematopoietic system, hepatitis.

RESORBIVE SULPHANYLAMIDES

SHORT-ACTION PREPARATIONS

Streptocide - Streptocidum. para-aminobenzenesulfonamide. Synonyms: prontosil, white streptocid, streptamine, sulfonamide, streptozol, etc.

A white crystalline powder, odorless and tasteless. Let's slightly dissolve in water (1: 170), easily - in boiling water, solutions of acids and alkalis; hardly soluble in ethanol (1:35). Aqueous solutions are neutral, very stable (can be sterilized with flowing steam or short boiling). Incompatible with novocaine, anesthesin, barbiturates and other drugs that easily split off sulfur.

It has an antimicrobial effect on streptococci, meningococci, pneumococci, E. coli, the causative agent of gas gangrene and some other microbes, but is almost inactive against staphylococci. The drug disrupts the course of metabolic processes and inhibits the growth and reproduction of microorganisms.

Streptocid is rapidly absorbed from the gastrointestinal tract, subcutaneous tissue and from the wound surface. It is especially well absorbed from the small intestine, slightly worse - from the stomach and large intestine. When applied topically, it does not irritate tissues.

After oral administration, the maximum concentration of the drug in the blood is established after 0.5-3 hours and is maintained at approximately this level for 1-2 hours, and then decreases rather quickly. The absorbed drug easily penetrates the internal barriers. It is found in all organs and tissues in fairly high concentrations. In the body, streptocide binds to proteins up to 20% and undergoes various transformations, including acetylation. The degree of acetylation in blood is 20-25%, in urine - 25-60%. Acetylation products do not have antimicrobial activity and dissolve in water much worse. At a high concentration of the drug in the urine, they can precipitate. Streptocide is excreted in free and bound forms mainly by the kidneys (90-95%).

The toxicity of the drug is insignificant, but with prolonged use in large doses, difficultly soluble compounds can form in the kidneys, the hemoglobin content decreases, cyanosis, agranulocytosis, and leukopenia occur. Young animals are more sensitive to the drug. Contraindications to the use of streptocide are as follows: general acidosis, hepatitis, hemolytic anemia, agranulocytosis, nephritis, nephrosis.

Streptocide is used for tonsillitis, streptococcal tonsillar abscesses, washing, bronchopneumonia, postpartum sepsis and other diseases. Doses inside: horses and cattle 5-10 g, small ruminants and pigs 0.5-2, dogs 0.5-1, arctic foxes and foxes 0.3-0.5 g. The drug is prescribed in the indicated single doses 4 -6 times a day for 5-7 days. Single doses intravenously: horses and cattle 3-6, dogs 0.5-1 2-3 times a day. Outwardly, streptocide is used to treat infected wounds, ulcers, burns in the form of a powder, suspension, liniment. Dressings are carried out in 1-2 days, since pus and tissue decay products reduce the therapeutic effect of streptocide.

Produced in the form of powder, tablets of 0.3 and 0.5 g, as well as in the form of 5-10% ointment, 5% suspension and 5% liniment.

Store the streptocide powder and tablets with the precautions on list B in a well-closed container. The term of the verification analysis is 10 years.

The ointment, suspension and liniment of streptocide are stored in a cool, dark place in a carefully closed container. If a brownish film appears on the surface of the liniment, it should be removed, after which the liniment is suitable for use.

Soluble streptocide - Streptocidum solubile. sodium para-sulfamido-benzeneaminomethanesulfate.

White crystalline powder. Let's dissolve in water, practically insoluble in ether and chloroform. Aqueous solutions can be sterilized. Incompatible with novocaine, anesthesin, barbiturates.

In terms of anti-microbial action, it is similar to streptocide. Due to its good water solubility, it is suitable for parenteral administration. The pharmacokinetics of the drug is similar to the pharmacokinetics of streptocide.

Approximate streptocid soluble in septic streptococcal processes, tonsillitis, washing, bronchopneumonia, mastitis, cystitis, pyelitis. Assign intramuscularly and subcutaneously in the form of a 5% solution prepared with water for injection or isotonic sodium chloride solution. For intravenous administration, a 10% solution is prepared in isotonic sodium chloride solution or 1-5% glucose solution. Doses intravenously: horses and cattle 2-6 g, small ruminants and pigs 1-2, dogs 0.3-0.5 g. With mastitis, a 3-5% aqueous solution of the drug is injected into the affected udder lobe after milking in a volume of 25-40 ml 2-3 times a day.

Soluble streptocide can be administered not only parenterally, but also internally, as well as externally in the same doses as streptocid.

Contraindications to the use of soluble streptocide: diseases of the hematopoietic system, hepatitis, nephritis.

A soluble streptocide powder is produced. Store according to list B in a well-closed container. The term of the verification analysis is 10 years.

Norsulfazole - Norsulfazolum. 2- (para-Aminobenzenesulfamido) thiazole. Synonyms: azoseptal, pyrosulfone, sulfathiazole, thiazamide, cibazole, etc.

A white or slightly yellowish crystalline powder, odorless, very slightly soluble in water (1: 2000), little - in ethanol, soluble in dilute inorganic acids, solutions of caustic and carbonic alkalis. Incompatible with novocaine, barbiturates, orthoform.

Norsulfazole has high antimicrobial activity against streptococci, meningococci, Escherichia coli, Salmonella, Pasteurella and other microorganisms. It is one of the most active sulfa drugs, but higher doses are required to create bacteriostatic concentrations in the blood. The toxicity of norsulfazole is higher than that of streptocide, and may appear after 7-9 days. after application in the form of hematuria and agranulocytosis.

The drug is easily absorbed from the gastrointestinal tract and reaches its maximum concentration in the blood 3-6 hours after administration. The therapeutic concentration is retained in the blood for 6-12 hours. It binds to plasma proteins by 60-70%, as a result of which the penetration of the drug into organs and tissues is hampered and its excretion slows down. It is slightly acetylated and excreted in urine mainly in free form.

Norsulfazole is used for catarrhal bronchopneumonia, pleurisy, streptococcal and staphylococcal sepsis, endometritis, mastitis, gastroenteritis, necrobacteriosis, diplococcal septicemia of calves, bird pasteurellosis and other bacterial infections. Assign inside 2-3 times a day in the following doses: horses and cattle 10-25 g, small ruminants and pigs 2-5, chickens 0.5 g. The initial dose of norsulfazole should be 2 times higher.

For catarrhal bronchopneumonia of calves, norsulfazole is used intratracheally at a dose of 0.05 g / kg of body weight in the form of an 8-10% solution for 3-4 days. It is advisable to prescribe antibiotics at the same time. In case of diplococcal septicemia of calves, the drug is administered intravenously at 0.01-0.02 g / kg of weight.

In the treatment of wounds, norsulfazole is used in the form of powders and ointments in various combinations with penicillin, gramicidin, iodine, and other sulfonamides. In this case, it is necessary to cleanse the wound from pus and necrotic tissue.

Contraindications to the use of norsulfazole: nephritis, hepatitis, diseases of the blood and hematopoietic system. During the period of administration of the drug, water intake is not limited.

Norsulfazole is produced in powder and tablets of 0.25 and 0.5 g each. Store with caution according to list B in a well-sealed container. The term of the verification analysis is 5 years.

Norsulfazole sodium - Norsulfazolum-natrium. 2- (para-Aminobenzenesulfamido) thiazole sodium. Synonyms: soluble norsulfazole, sodium sulfathiazole.

Lamellar, lustrous, colorless or slightly yellowish, odorless crystals. Let's easily dissolve in water (1: 2). Aqueous solutions have a strongly alkaline reaction, withstand sterilization at 100 ° C for 30 minutes.

The drug has the same chemotherapeutic activity as norsulfazole. 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.

Indications for use are the same as for norsulfazole. It is used in septic processes when it is necessary to quickly create a high concentration of the drug in the blood, for example, with diplococcal septicemia of calves, necrobacillosis, colibacillosis, etc. Norsulfazole sodium is prescribed mainly intravenously in the form of 5-15% solutions, slowly injected. The drug can be injected under the skin and intramuscularly in solutions not exceeding 0.5-1% concentration. The penetration of stronger solutions under the skin causes irritation of tissues, up to necrosis. Doses intravenously: horses 6-12 g, cattle 6-10, sheep 1-2, dogs 0.5-1 g 2 times a day for 3-4 days.

For pasteurellosis of birds, norsulfazole sodium is used in the form of a 20% oil suspension or aqueous solution. The suspension is injected once into the upper third of the neck of chickens and ducks, 1 ml per 1 kg of bird weight. An aqueous solution is prepared immediately before use at the rate of 0.5 dry matter for chickens and 1 g for turkeys per intake. The drug is given to the bird with feed 2 times a day. For coccidiosis, chickens are given with drinking water in the form of a 0.25% aqueous solution.

In mastitis, the affected portion of the udder is removed and a 3, 5 or 10% solution of norsulfazole sodium is injected through a milk catheter in a volume of 25-40 ml. The nipple is clamped for 10-15 minutes. Treatment is carried out 1-2 times a day until recovery.

Contraindications to the use of norsulfazole sodium - diseases of the hematopoietic system, nephritis, nephrosis.

Available in powder form. Store with precautions according to list B in a package protected from moisture and light. Verification analysis period is 3 years.

Etazol - Aethazolum. 2- (para-Aminobenzenesulfamido) -5-ethyl-1,3,4-thiadiazole. Synonyms: berlofen, globucid, setadil, sulfaethidiol, etc.

White or white with a slightly yellowish sheen, odorless powder. Practically insoluble in water, hardly soluble in ethanol, slightly soluble in dilute acids, readily soluble in alkali solutions. Incompatible with peptone, para-aminobenzoic acid, novocaine, barbiturates, many sulfur derivatives.

Etazole has a high antimicrobial activity against streptococci, pneumococci, meningococci, pathogenic anaerobes, Escherichia coli, causative agents of dysentery, salmonellosis, pasteurellosis, etc. Etazole is superior to many sulfonamides in antibacterial action against a number of microorganisms.

The drug is rapidly absorbed from the gastrointestinal tract into the bloodstream. After 2-3 hours in dogs and after 5-8 hours in cattle, the maximum concentration in the blood is noted. Etazole belongs to short-acting sulfanilamide drugs, in which the maximum concentration level decreases by 50% in 5-10 hours. It penetrates well through the blood-brain barrier, is distributed unevenly in various organs and tissues: it remains the longest in the kidneys, gastrointestinal tract, liver, lungs. In dogs, the drug is not acetylated, and in other animals it is slightly acetylated (5-10%), so its use does not lead to the formation of crystals in the urinary tract. Etazole is released most rapidly in dogs, then in rabbits, and most slowly in cattle.

Used for bronchopneumonia, angina, postpartum sepsis, endometritis, dysentery, dyspepsia, swine erysipelas and other diseases of bacterial etiology, the causative agents of which are sensitive to sulfonamides.

Doses by mouth: horses 10-25 g, cattle 15-25, small ruminants 2-3, pigs 2-5, rabbits 1-1.5, poultry 0.5, dogs 0.3-0.5 g 3 -4 times a day for 4-6 days. contract. In severe cases, the initial dose is doubled. Doses for young animals are 2/3 of the dose for an adult animal.

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

Contraindications for use: severe acidosis, acute hepatitis, hemolytic anemia, agranulocytosis.

Etazole is produced in the form of powder and tablets of 0.25 and 0.5 g. Store according to list B in a well-sealed container. Verification analysis period is 3 years

Etazole sodium - Aethazolum-natrium 2 (Aminobenzene-sulfamido pair) 5 Ethyl 1,3,4 thiadiazole sodium. Synonyms: soluble etazole, sodium sulfaetidol.

White crystalline powder. Easily soluble in water; hardly soluble in ethanol. Aqueous solutions are stable and can be sterilized by boiling for 30 minutes. Incompatible with novocaine, anesthesin, drugs that easily split off sulfur.

Etazole sodium is easily absorbed by various routes of administration, quickly reaches the maximum concentration in the blood and actively penetrates into various organs and tissues. Due to its good solubility in water, it can be used not only internally, but intramuscularly and intravenously. It circulates in the body mainly in free form, is excreted quickly.

Antibacterial activity and indications for use are the same as for etazole.

Apply 10-20% solutions intramuscularly and intravenously. Doses: horses and cattle 5-10 g, small ruminants 1-2, pigs 2-3, dogs 0.1-0.3 g 2-3 times a day.

Contraindications to the use of sodium etazole are the same as for etazole.

Etazole sodium is produced in powder, as well as in ampoules 3 in the form of a 10-20% solution for injection.

Store with precautions according to list B, protected from light. The term of the verification analysis is 5 years.

Sulfacil - Sulfacylum. para-aminobenzenesulfacetamide. Synonyms: acetocide, acetosulfamine, albucid, septuron, sulamide, sulfacetamide, etc.

An odorless white or white with a yellowish tinge crystalline powder, soluble in 20 parts of cold water (dissolves much easier in hot water), in 12 parts of ethanol, in solutions of alkalis and acids. Incompatible with novocaine, anesthesin, drugs that split off sulfur.

Sulfacil has a strong antimicrobial effect against streptococci, staphylococci, pneumococci, salmonellosis and colibacillosis pathogens.

The drug is rapidly absorbed from the gastrointestinal tract of animals. The maximum concentration in the blood is established after 2-5 hours from the moment of administration. For 6-12 hours, the maximum concentration decreases by 50%. Moderately acetylated (10-15%). It binds slightly to plasma proteins, penetrates well into various organs and tissues. Relatively quickly excreted from the body, mainly in the urine.

Applied for tonsillitis, pharyngitis, bronchopneumonia, postpartum sepsis, streptococcal infections, colibacillosis, salmonellosis, dyspepsia, cystitis, etc. Locally prescribed in the form of powders and ointments in the treatment of purulent wounds, skin streptococcal diseases inside horses and staphylococcal infections. -10 g, small ruminants 2-3, pigs 1-2, dogs 0.5-1 g 3-4 times a day. The initial dose should be 2-3 times the subsequent dose.

Contraindications for use are similar to other sulfonamides.

Sulfacil is produced in powder. Store according to list B in a well-closed container, protected from light. The term of the verification analysis is 5 years.

Sulfacyl sodium - Sulfacylum-natrium. para-Aminoben-zolsulfacetamide-sodium - sodium salt of sulfacil. Synonyms: soluble sulfacil, sodium sulfacetamide, sodium albucid, etc.

Flavourless white crystalline powder. Easily soluble in water, practically insoluble in ethanol, ether. Incompatibility - similar to other sulfonamides.

In terms of antimicrobial action and characteristics of pharmacokinetics, it is similar to sulfacil.

Used for pyelitis, cystitis, colitis and postpartum sepsis. Assign inside in doses: horses and cattle 3-10 g, small ruminants and pigs 1-2, dogs 0.3-0.5 g 3-4 times a day.

Outwardly, sulfacyl sodium is used in the treatment of wounds, corneal ulcers, conjunctivitis, mastitis, endometritis. Use in the form of a powder, ointment or solutions of 10, 20 or 30% concentration. Particularly good results have been obtained with the use of sodium sulfacyl in ocular practice.

Contraindications for use: acute hepatitis, agranulocytosis, hemolytic anemia.

Available in powder. Store according to list B in a package protected from light and moisture. The term of the verification analysis is 5 years.

Sulfanthrol - Sulfanthrolum. 2- (para-Aminobenzenesulfamido) -benzoate, hydrate.

White or white with a yellowish or pink tinge, crystalline powder, readily soluble in water (1: 8), hardly soluble in ethanol. Aqueous solutions are stable, they are sterilized by boiling for 15 minutes. Incompatible with drugs that easily split off sulfur, novocaine, anesthesin, barbiturates.

Sulfanthrol is active against streptococci, pneumococci and Escherichia coli. The drug is highly toxic to nuttalia.

Applied for nuttaliasis and piroplasmosis of horses, theileriosis of cattle, bronchopneumonia, salmonellosis, colibacillosis, foulbrood of bees and other diseases. In horse nuttaliasis, sulfanthrol is administered intravenously in the form of a 4% solution at a dose of 0.005-0.01 g of pure substance per 1 kg of animal weight. The drug is administered 1-3 times with an interval of 24-38 hours. When horses are sick with nuttaliasis and piroplasmosis, a mixture of 4% sulfanthrol solution and 1% trypan blue solution is used. Administered intravenously at a dose of 0.5 ml per 1 kg of animal weight 1-2 times with an interval of 24-48 hours.

With theileriosis of cattle, sulfanthrol is administered intramuscularly in the form of a 10% solution at the rate of 0.003 g per 1 kg of animal weight.

With bronchopneumonia, the drug is administered intramuscularly and intravenously at a dose of 0.008-0.01 g per 1 kg of animal weight. With colibacillosis, salmonellosis and other gastrointestinal diseases sulfanthrol is prescribed orally on the first day 0.2 g, on the second - 0.15, on the third - 0.1 and on the fourth - 0.05 g per 1 kg of animal weight per day. The daily dose is 3-4 doses.

For foulbrood bees, the drug is added to sugar syrup in a dose of 2 g per 1 liter of syrup and fed to one bee family.

Contraindications to the use of sulfanthrol: agranulocytosis, acute hepatitis, nephritis and nephrosis

Available in powder. Store with the precaution of list B in a well-closed container, protected from light and moisture. The term of the verification analysis is 8 years.

Sulfadimezin - Sulfadimezinum. 2- (para-Aminobenzene-sulfamido) -4,6-dimethylpyrimidine. Synonyms: diazyl, diazole, dimetazyl, dimethylsulfadiazine, dimethylsulfapyrimidine, superseptyl, etc.

Flavourless white or slightly yellowish powder. Practically insoluble in water, ether and chloroform, slightly soluble in ethanol, readily soluble in diluted mineral acids and alkalis. Incompatible with novocaine, para-aminobenzoic acid, peptone, barbiturates.

It has a wide antibacterial spectrum of action: it is active against pneumococci, staphylococci, Escherichia coli, Salmonella, Pasteurella, as well as large viruses. The activity is close to sulfazine and methylsulfazine. It acts bacteriostatically, disrupts the course of metabolic processes, inhibits the growth and reproduction of microbes.

Sulfadimezin is relatively rapidly absorbed from the gastrointestinal tract. The maximum concentration of the drug in the blood is established 6-8 hours after administration. It creates higher concentrations in the blood of animals than any other. Of the commonly used sulfonamides, at the same dose. The drug penetrates well through the blood-brain barrier, creates high concentrations in many organs and tissues. It binds to proteins by 75-85%, acetylated in the blood by 5-10%, urine by 20-30%. Acetylation products of sulfadimezine dissolve better than the free form of the drug. Excreted from the body slowly, mainly by the kidneys. Due to the relatively low rate of elimination, it is safer than norsulfazole and other rapidly released drugs. Slow release provides long-term (more than 8 hours) maintenance of the therapeutic blood level. The drug is well tolerated by animals.

Sulfadimezin is used for pneumonia, catarrhal bronchopneumonia, bronchitis, laryngitis, sore throat, horse wash, sepsis, endometritis, infectious mastitis, necrobacteriosis of sheep and reindeer, dyspepsia, gastroenteritis, urinary tract infections, salmonellosis mycosis, other diseases of poultry pasteurellosis ... Assign inside in doses: horses 10-25 g, cattle 15-20, small ruminants 2-3, pigs 1-2, chickens 0.3-0.5 g 1-2 times a day. The initial dose must be doubled

To deposit sulfadimezin, it can be administered to pigs, deer, sheep under the skin or intramuscularly in the form of a 20% suspension in fish oil, peach or refined sunflower oil at a dose of 1-1.2 ml per 1 kg of animal weight. At the same time, the drug is prescribed orally at a dose of 0.05 g per 1 kg of weight.

In case of poultry pasteurellosis, sulfadimezin is used with feed at the rate of 0.05 g per 1 kg of animal weight 1-3 times a day for 2-4 days.

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

Contraindications to the use of sulfadimezin are diseases of the hematopoietic system, nephritis, nephrosis, hepatitis. With prolonged therapy, it is necessary to conduct blood tests.

Sulfadimezin is produced in powder and tablets of 0.25 and 0.5 g. Store according to list B in a dark place in a well-sealed container. The term of the verification analysis is 10 years.

Urosulfan - Urosulfanum. para-aminobenzenesulfopyl-urea. Synonyms: sulfacarbamide, sulfonylcarbamide, uramide, etc.

Flavourless white crystalline powder, sour taste. Slightly soluble in water, hardly soluble in ethanol, readily soluble in dilute acids and solutions of caustic alkalis. Incompatible with drugs that split off sulfur, novocaine, anesthesin, barbiturates.

Urosulfan has high antibacterial activity against staphylococci and Escherichia coli.

The drug is rapidly absorbed from the gastrointestinal tract, which ensures the creation of high concentrations in the blood. The maximum concentration is established in 1-3 hours from the moment of administration. Urosulfan 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. Urosulfan is low-toxic, no deposits in the urinary tract are noted.

It is used for colibacterial and staphylococcal diseases: cystitis, pyelitis, infected hydronephrosis, and other urinary tract infections. The use of urosulfan is especially effective for pyelitis and cystitis without disturbance of urination. Assign orally in doses to horses 10-30 g, cattle 10-35, small ruminants 2-5, pigs 2-4, dogs 1-2 g 3-4 times a day for at least four days in a row. For intravenous injections, soluble urosulfan is used in the form of 5, 10 and 20% solutions at a dose of 0.02-0.03 g per 1 kg of animal weight 1-2 times a day. A 25% solution is injected into the bladder.

Contraindications for use: acute hepatitis, agranulocytosis, hemolytic anemia.

Produced in powder and tablets of 0.5 g. Store with caution according to list B in a well-closed container. The term of the verification analysis is 2.5 years.

MEDIUM DURATION DRUGS

Sulfaein - Sulfazinum. 2- (Aminobenzenesulfamido pair) -pyrimidine Synonyms, adiazine, debenal, sulfadiazine, pyrimal, sulfapyrimidine, etc.

Odorless white or yellow powder. Practically insoluble in water, soluble in ethanol, solutions of alkalis and mineral acids.

It has antibacterial activity against streptococci, staphylococci, pneumococci, meningococci, Escherichia coli and other gram-positive and gram-negative bacteria. In vivo antibacterial activity is superior to norsulfazole, streptocide and some other sulfa drugs.

Sulfazine is absorbed from the gastrointestinal tract relatively slowly, the maximum concentration of the drug in the blood is established after 4-6 hours. Sulfazine binds less to plasma proteins and is released from the body more slowly than norsulfazole, which provides a higher concentration of the drug in the blood and organs. It is slightly acetylated (5-10%); acetylation products are readily soluble in water and urine.

Used for bronchopneumonia, gastroenteritis, laryngitis, sore throat, pullorosis (typhoid), coccidiosis and other diseases. Doses inside horses and cattle 10-20 g, small ruminants 2-5, pigs 2-4, dogs 0.5-1, chickens 0.5 g 2-3 times a day Sulfazine sodium salt is released for intravenous injection, which is administered in the form of a 5-10% solution at the rate of 0.02-0.03 g per 1 kg of animal weight.

The drug relatively rarely causes dysfunctions of the hematopoietic system. However, there may be complications from the urinary tract of hematuria, oliguria, anuria. To prevent these complications, it is necessary to maintain increased diuresis (abundant alkaline drinking)

Contraindications for use, nephritis, nephrosis

Produced in powder and tablets of 0.5 g. Store according to list B in a well-sealed container. The term of the verification analysis is 7 years.

LONG-LASTING PREPARATIONS

Sulfapyridazine - Sulfapyridazmum. 6 (para-aminobenzenesulfamido) 3 methoxypyridazine Synonyms aseptylex, depovernil, deposul, durasulf, kinex, lederkin, longisulf, novosulfin, quinoseptyl, retasulfin, spofadazine, sulfamethoxypyridazine, etc.

Flavourless light yellow crystalline powder, bitter taste. Soluble in cold water, slightly better in hot (1: 70). It dissolves well in dilute acids and alkalis.

Sulfapyridazine is active against many gram-positive and gram-negative microorganisms. The strength of the bacteriostatic action is equal to or somewhat inferior to etazole and sulfazine. A high sensitivity to the preparation of streptococci, staphylococci, Escherichia coli, Pasteurella and some Proteus strains was established. Microorganisms resistant to other sulfonamides are resistant to sulfa pyridazine.

The drug belongs to long-acting sulfonamides. It is rapidly absorbed from the gastrointestinal tract and creates a high concentration level in the blood, organs and tissues, which remains in the body for a long time. The maximum concentration of the drug in cattle and sheep is established after 5-12 hours, in rabbits after 2-8, in dogs and chickens after 2-5 hours from the moment of administration. The therapeutic level of concentration is maintained for 24-48 hours. Sulfapyridazine binds intensively to plasma proteins (70-95%) and is highly reabsorbed (80-90%) in the distal renal tubules. The drug penetrates well into various organs and tissues. The greatest amount of it accumulates in the kidneys, liver, walls of the stomach and intestines, lungs.

Sulfapyridazine in the body of animals undergoes the acetylation process to a small extent. The content of acetoproducts in the blood is 5-15%. Acetylated derivatives have no antimicrobial activity.

The drug is excreted from the body by the kidneys in free and acetylated form. Due to the high degree of free-form reabsorption in the renal tubules, the content of acetylated products in urine reaches 60-80%. The solubility of aceto products of sulfapyridazine in urine is good.

The drug is used for various diseases of the respiratory tract of young animals, gastrointestinal diseases of various etiologies (gastroenteritis, dyspepsia, dysentery, coccidiosis), salmonellosis, colibacillosis, pasteurellosis, for respiratory mycoplasmosis and poultry pultriosis, poultry septriosis, postpartum mastitis, postpartum urinary tract and gallbladder, for the prevention of postoperative infections. Oral doses per 1 kg of animal weight: cattle 50-75 mg, piglets 75-100, dogs 25-30, chickens 100-120, rabbits 250-500 mg once a day. The initial dose should be 1.5-2 times the indicated maintenance doses.

In case of pasteurellosis of chickens, sulfapyridazine is prescribed for therapeutic purposes in doses of 200 mg (initial) and 150 mg (maintenance) per 1 kg of body weight with a 24-hour interval between injections. The drug can be administered by a group method with food.

In order to prevent the undesirable effects of sulfapyridazine, animals should be given an abundant alkaline drink.

Contraindications for use: diseases of the hematopoietic system, kidneys, liver, severe toxic-allergic reactions.

Produced in powder and tablets of 0.5 g. Store with precautions according to list B in a tightly sealed container, protected from light. The term of the verification analysis is 2 years.

Sulfapyridazine sodium - Sulfapyridazinum-natrium. (para-aminobenzenesulfamido) -3-methoxypyridazine sodium.

Crystalline powder, white or white with a yellowish-green tinge. Let's easily dissolve in water, it is difficult - in ethanol. Gradually turns yellow on exposure to light. Aqueous solutions can be sterilized at 100 ° C for 30 minutes.

The antibacterial spectrum is similar to sulfapyridazine.

Used for severe bronchopneumonia, salmonellosis, pasteurellosis, swine erysipelas, postpartum sepsis, endometritis and other infectious diseases. Assign intravenously or intramuscularly in the form of 5%. or 10% solution. Intravenous doses per 1 kg of animal weight: cattle 25-50 mg, small ruminants 50-75 mg once a day.

With a local purulent infection, the drug is used to irrigate wounds in the form of bandages and tampons moistened with a 5-10% solution. Sulfapyridazine sodium solutions can be prepared with distilled water, isotonic sodium chloride solution, or 2-5% polyvinyl alcohol solution. With mastitis, endometritis, solutions are injected into the uterine cavity and mammary gland. When administered locally, it can be combined with oral sulfapyridazine.

When using the drug, side effects are possible: skin rashes, leukopenia. Contraindications: diseases of the hematopoietic system, kidneys, liver.

Produced in powder and in the form of a 10% solution of 7% polyvinyl alcohol in vials of 10 and 100 ml. Store according to list B in a dry, dark place. Verification analysis period is 3 years.

Sulfadimethoxine - Sulfadimethoxinum. 6- (para-Aminobenzenesulfamido) -2,6-dimethoxypyrimidine. Synonyms: depot sulfamide, madribone, madroxin, supersulfan, ultrasulfan, etc.

White crystalline powder, tasteless and odorless. Slightly soluble in water and ethanol, soluble in dilute acids and alkalis.

Sulfadimethoxine has a broad spectrum of antimicrobial activity. The most sensitive to it are meningococci, streptococci, staphylococci, various strains of Escherichia coli, Shigella, Proteus. Most strains of Pseudomonas aeruginosa, listeria, some strains of pneumococcus are resistant. Significant fluctuations in the sensitivity of the strains to the drug within the same species were noted.

Sulfadimethoxine belongs to long-acting sulfonamides. It is relatively quickly absorbed from the gastrointestinal tract into the blood, however, the absorption rate is somewhat lower than that of sulfapyridazine. The maximum concentration in the blood of cattle is established after 8-12 hours, sheep and goats - 5-8, pigs and dogs - 2-5, chickens - 3-5 hours from the moment of administration. The concentration of the drug in the blood decreases much more slowly than the concentration of sulfapyridazine. The therapeutic level is maintained for 24-48 hours. Sulfadimethoxine, somewhat worse than sulfapyridazine and sulfamonomethoxin, penetrates into various organs and tissues. The exception is bile, where the concentration of the drug can exceed its content in the blood by 1.5-4 times.

Sulfadimethoxine in the blood binds to a very large extent with plasma proteins (90-98%). According to the intensity of binding to plasma proteins, animals can be arranged in the following (decreasing) order: dogs, cattle, rabbits, rats. Acetyl production is present in the blood in small amounts (0-15%).

Sulfadimethoxine is excreted from the body very slowly, primarily due to large (93-97%) reabsorption in the tubules of the free form of the drug, and also due to a significant degree of protein binding. The acetyl form is excreted 2 times faster. In urine, sulfadimethoxine is present mainly in the form of glucuronide, which dissolves well in an acidic medium, which practically excludes the possibility of crystalluria development.

The drug is slightly toxic to animals, has a wide range of therapeutic action. Used for broncho-pneumodil of young animals, for infections of the nasopharynx, acute form of dysentery, pasteurellosis, coccidiosis, gastroenteritis, colitis, cystitis and other diseases. Sulfadimethoxin is prescribed orally in doses per 1 kg of animal weight: cattle 50-60 mg, small ruminants 75-100, pigs 50-100, dogs 20-25, rabbits 250-500, chickens 75-100 mg once a day ... The initial dose should be 2 times the indicated maintenance doses.

With pasteurellosis of chickens, Sulfadimethoxine is prescribed for therapeutic purposes in doses of 200 mg (initial) and 100 mg (maintenance) per 1 kg of body weight. For prophylactic purposes, doses of 100 mg (initial) and 50 mg (maintenance) are used once a day. The drug can be used as a group method with feed.

In order to prevent the undesirable effect of the drug, it is recommended to prescribe an abundant drink to sick animals. Sulfadimethoxine is contraindicated in case of toxic-allergic reactions, diseases of the hematopoietic system, kidneys, acute hepatitis.

Produced in powder and tablets of 0.5 g. Store with precautions according to list B in a well-sealed container, protected from light. The term of the verification analysis is 4 years.

Sulfamonomethoxin - Sulfamonomethoxinum. 6- (para-Aminobenzenesulfamido) -6-methoxypyrimidine. Synonyms: diameton, DS-36.

White or white with a yellowish sheen crystalline powder. Slightly soluble in water, better - in ethanol, easily soluble in dilute mineral acids and aqueous solutions of caustic alkalis. Incompatible with novocaine, barbiturates, preparations that easily split off sulfur.

Sulfamonomethoxin has high antibacterial activity against streptococci, meningococci, pasteurella, Escherichia coli, Toxoplasma, dysentery sticks and other microorganisms. The drug has not only a high bacteriostatic effect in vitro, but also has an extremely high chemotherapeutic activity in animal experiments. In infections caused by streptococci, staphylococci, salmonella, the activity exceeds sulfapyridazine and sulfadimethoxine.

The drug belongs to long-acting sulfonamides. It is well and quickly absorbed from the gastrointestinal tract into the blood. The maximum concentration in the blood is established in cattle after 5-8 hours, sheep and goats - after 3-5, pigs - 2-5, dogs - 1-3, chickens - 2-5 hours from the moment of administration. The concentration of sulfamonomethoxin in the blood decreases somewhat faster than with the introduction of sulfapirilazine and sulfadimethoxine. The drug diffuses quite well into organs and tissues. Higher concentrations are stopped in the kidneys, lungs, liver. Penetrates well through the blood-brain barrier. In the blood, it intensively binds to proteins (64.6-92.5%), but the forming bond is fragile. Acetyl production in blood reaches 5-14%, in urine 50-67%. It is excreted from the body slowly and mainly by the kidneys. Urine contains 50-70% acetyl derivative, 20-30% glucuronide and 10-20% free drug. The acetyl form of sulfamonomethoxin is more soluble than the free one.

Used for respiratory tract infections, purulent infections of the ear, throat, nose, dysentery, enterocolitis, infections of the bile and urinary tract, purulent meningitis. The drug is given orally in doses per 1 kg of animal weight, cattle 50-100 mg, small ruminants 75-100, pigs 50-100, dogs 25-50, rabbits 250-500, chickens 100 mg once a day. The starting dose should be doubled.

Sulfamonomethoxin is contraindicated in case of hypersensitivity to sulfonamide drugs, with hemolytic anemia, agranulocytosis, acute hepatitis, nephritis.

Produced in powder and tablets of 0.5 g. Store according to list B in a well-sealed container, protected from light. Verification analysis period is 3 years.

Sulfalen - Sulfalenum. 2- (para-Aminobenzenesulfamido) -3-methoxypyrazine. Synonyms: kelfizin, sulfametopyrazine, sulfamethoxypyrazine, sulfapyrazine methoxine.

White crystalline powder. Let's slightly dissolve in water, we will easily dissolve in solutions of alkalis. Incompatible with novocaine, barbiturates, preparations that easily split off sulfur.

In terms of its antibacterial spectrum of action, it is close to other sulfa drugs.

Sulfalene refers to ultra-long-acting sulfonamides. It is rapidly absorbed, and the maximum concentration in the blood is established after 4-6 hours. Therapeutic concentrations in the body of animals and birds can be retained in the liver for 3-5 days. Excreted from the body very slowly. Well tolerated by animals.

Applied for bronchopneumonia of young animals, colibacillosis, salmonellosis, pasteurellosis, toxoplasiosis, respiratory mycoplasmosis, as well as urethritis, mastitis and other diseases. Assign orally in doses per 1 kg of animal weight - dairy calves 20-25 mg, suckling pigs 40-50, chickens 100-150 mg 1 time per day, re-injected after 5-7 days. In severe cases, the drug is prescribed again after 3-4 days. The duration of treatment is at least 10-12 days.

In case of bronchopneumonia in calves of 2-3 months of age, sulfalene is administered orally at 50 mg (initial dose), and then 20 mg daily (maintenance dose) for 7-10 days. At the same time, it is recommended to introduce vitamin preparations (groups A, B and C), as well as to carry out intensive symptomatic therapy.

In case of colibacillosis and salmonellosis of pigs up to 2-4 months of age, sulfalene is prescribed 1 time per day per 1 kg of animal weight: on the first day, 100 mg, on the next day, 20 mg.

Possible side effects and measures to prevent them are the same as with the use of other prolonged sulfonamides.

Available in powder and tablets of 0.2, 0.5 and 2 g; in vials of 60 ml of a 5% suspension. Store according to list B in a well-closed container. The term of the verification analysis is 5 years.

Salazopyridazine - Salazopyridazinum. 5-napa- / N- (3-Methoxypyridazinyl-6) -sulfamido / -phenylazosalicylic acid.

Yellowish-orange fine crystalline powder, tasteless and odorless. Practically insoluble in water, soluble in solutions of alkalis and hydrocarbonates. Obtained as a result of azo coupling of sulfapyridazine (65%) and salicylic acid.

The antimicrobial effect of salazopyridazine is manifested only after its cleavage in the gastrointestinal tract with the release of free sulfapyridazine and 5-aminos-lycylic acid. The therapeutic effect of the drug is determined primarily by the ability of salazosulfonamides to accumulate in the connective tissue of the large intestine and have a direct effect on the inflammatory process. The metabolic products of salazopyridazine are antibacterial, anti-inflammatory and immunosuppressive. Salazopyridazine is more active than salazopyridine, however, in terms of the degree of chemotherapeutic action, it is inferior to sulfapyridazine,

As the drug breaks down, the released sulfapyridazine is gradually absorbed and reaches its maximum concentration in the blood and organs after 4-6 hours. The concentration of free sulfapyridazine in the blood and organs does not reach a high level, but it remains at the therapeutic and subtherapeutic levels for a long time. The drug is low-toxic. With long-term administration for 30-40 days. does not cause changes in blood and urine.

Recommended for the treatment of animals with various forms of colitis, enterocolitis and with the same indications as sulfapyridazine. Doses inside young farm animals are 25-50 mg per 1 kg of body weight 2 times a day.

When using salazopyridazine, side effects are possible, which are sometimes observed with the use of sulfonamides and salicylic acid: allergic reactions, leukopenia, dyspeptic disorders.If adverse reactions occur, the daily dose should be reduced or the drug should be canceled Salazopyridazip is contraindicated in the presence of severe toxic-allergic reactions to sulfonamides.

Produced in powder, tablets of 0.5 g and in the form of a 5% suspension. Store in a tightly sealed container, protected from light. The term of the verification analysis is 5 years.

Salazodimethoxin - Salazodimethoxinum. 5-napa- / N- (2,4-dimethoxypyrimidinyl-6) - sulfonamido / -phenylazo-salicylic acid.

Orange powder, tasteless and odorless. Insoluble in water, soluble in aqueous solutions of alkalis and hydrocarbons. Salazodimethoxine is a product of azo coupling of sulfadimethoxine (67.5%) and salicylic acid.

The mechanism of action, pharmacokinetics, indications and contraindications, the scheme for the use of salazodimethoxine are similar to those of salazopyridazine.

Produced in powder and tablets of 0.5 g. Store according to list B in a tightly closed package, protected from light. The term of the verification analysis is 2 years.

SULPHANYLAMIDES, POORLY ABSORATED FROM THE GASTROINTESTINAL TRACT

Sulgin - Sulginum. para-aminobenzenesulfoguanidine. Synonyms abiguanil, aseptilguanidine, ganidane, neo-sulfonamide, sulfaguanidine, etc.

Flavourless white crystalline powder. We will very little dissolve in water, in diluted mineral acids (hydrochloric, nitric), we will slightly dissolve in ethanol. Incompatible with novocaine, anesthesin, barbiturates, drugs that split off sulfur.

Sulgin has a fairly high antimicrobial activity against the intestinal group of pathogenic microorganisms and some gram-positive forms.

The drug is slowly and in small amounts absorbed from the gastrointestinal tract. Its bulk is retained in the intestines and creates a high concentration there. In the body of animals, sulgin is moderately acetylated, excreted mainly with feces. The high concentration of the drug in the digestive tract provides an effective effect on the intestinal microflora.

It is used for bacillary dysentery, colitis, enterocolitis, for the prevention of postoperative complications during bowel surgery. Assign orally in doses to horses 19-20 g, cattle 15-25, small ruminants 2-5, pigs 1-5, dairy calves 2-3, suckling piglets 0.3-0.5, chickens 0.2- 0.3 g 2 times a day. The initial dose should be twice the indicated maintenance dose.

To prevent the loss of crystals of acetylated sulgin in the kidneys, drink plenty of fluids.

Contraindications for use hypersensitivity to sulfonamides, diseases of the hematopoietic organs, acute hepatitis and nephritis,

Produced in powder and tablets of 0.5 g. Store with caution according to list B in a well-closed container. The term of the verification analysis is 5 years.

Phthalazole - Phthalazolum. 2-para- (ortho-Carboxybenzam-do) -benzenesulfamidothiazole Synonyms: sulfamidine, talazol, talazone, taledrone, talidine, talistalil, talisulfazole, phthalylsulfathiazole

White or white powder with slightly yellowish sheen. Practically insoluble in water, ether and chloroform; very slightly soluble in ethanol; we will dissolve in an aqueous solution of sodium carbonate, we will easily dissolve in an aqueous solution of sodium hydroxide. Incompatible with novocaine, anesthesin, drugs that split off sulfur.

Possesses antimicrobial activity against the causative agent of dysentery, salmonellosis, enteropathogenic strains of E. coli and some other bacteria. The mechanism of the antimicrobial action of phthalazole, like other sulfonamides, is to disrupt the process of assimilation by the microbial cell of "growth factors" - folic acid and substances close to it, which include para-aminobenzoic acid

Phthalazol is absorbed very slowly and in small quantities from the gastrointestinal tract, as a result of which a therapeutic concentration is practically not created in the blood. The bulk of the drug is retained in the gastrointestinal tract, where the active (sulfanilamide) part of the phthalazole molecule is gradually split off. The high concentration of phthalazole in the digestive tract ensures its effective effect on the intestinal microflora. The drug has low toxicity and is well tolerated by animals.

Used for dysentery, gastroenteritis, colitis, neonatal dyspepsia, coccidiosis. Assign inside in doses: horses 10-G5 g, cattle 10-20, small ruminants 2-5, pigs 1-3, dogs 0.5-1, chickens 0.1-0.2 g 2 times a day ... The initial dose can be double the subsequent dose.

Phthalazole usually does not cause side effects. Contraindication - hypersensitivity of animals to sulfa drugs

Produced in powder and tablets of 0.5 g. Store according to list B in a well-sealed container. The term of the verification analysis is 10 years.

Disulformin - Disulformmum. 1,4,4 N-Trimethylene-bis- (4-sulfanylyl-sulfanilamide)

White or slightly yellowish fine crystalline powder. Insoluble in water and dilute mineral acids, well soluble in solutions of caustic and carbonic alkalis. When heated with water, it hydrolyzes with the release of formaldehyde Incompatible with salts of heavy metals, novocaine, anesthesin, barbiturates and drugs that easily break off sulfur

Disulformin has antibacterial activity against Escherichia coli, causative agents of dysentery, salmonellosis, colibacillosis. It has a bacteriostatic effect - disrupts metabolism, inhibits the growth and reproduction of microbes.

The drug is slowly absorbed from the gastrointestinal tract and does not create high concentrations in the blood. Its bulk is retained in the intestine, where, under the influence of an alkaline medium, hydrolysis of disulformin occurs with the elimination of sulfonamide (disulfan) and formaldehyde. As a result of the high concentration of the drug in the digestive tract, combined with the activity of disulfan and formaldehyde against the intestinal microflora, it is effective in intestinal infections.

Used for bacillary dysentery, gastroenteritis of Salmonella etiology, acute colitis and enterocolitis. Assign orally in doses: horses 5-10 g, cattle 10-15, dairy calves 2-4, chickens 0.2-0.3 g 2-3 times a day.

Contraindications for use - hypersensitivity of animals to sulfonamides, acute hepatitis, nephritis, nephrosis, agranulocytosis

Produced in powder and tablets of 0.5 and 1 g. Store according to list B in a well-sealed container, protected from light. Verification analysis period 5 years

Ftazin - Phtazmum 6 (a pair of Phthalylaminobenzoylsulfanilamido) 3-methoxypyridazine

White or white with a slightly yellowish sheen, crystalline powder, odorless. Practically insoluble in water and ethanol. Easily soluble in solutions of alkalis and sodium bicarbonate. It is close in chemical structure, on the one hand, to phthalazole, and on the other, to sulfapyridazine

Ftazin has a broad antibacterial spectrum of action, is active against pneumococci, staphylococci, streptococci, Escherichia coli, Salmonella, Pasteurella, dysentery pathogens and other microorganisms. The antibacterial spectrum is close to sulfapyridazine. It acts bacteriostatically - it disrupts metabolism, the growth and reproduction of microbial cells. Bacteriostatic concentrations of phtazine are 30-300 times higher than sulfapyridazine and 2-5 times lower than phthalazole.

It is slowly absorbed from the gastrointestinal tract. In the intestine, it is gradually broken down with the release of free sulfapyridazine, which is absorbed as it is cleaved. Due to the slow elimination of sulfapyridazine in the intestine, a high concentration of the drug is maintained, which ensures good efficacy in the treatment of gastrointestinal diseases. Absorbed sulfapyridazine creates significant concentrations in the blood and has a resorptive effect, which is very important in severe forms of dysentery and other gastrointestinal diseases. It is excreted from the body slowly.

Phtazine is well tolerated by animals, does not cause noticeable disturbances in the general condition, even in cases where the dose exceeds the therapeutic one.

It is used for therapeutic and prophylactic purposes for dysentery, neonatal dyspepsia, enterocolitis, colitis, coccidiosis. The main advantage of the drug is less toxicity and longer stay in the body. Assign individually or as a group method with feed 2 times a day Doses per 1 kg of animal weight: cattle and small ruminants 10-15 mg, calves and lambs 15-20, pigs 8-12, piglets 12-16, chickens 30-50 mg ... The initial dose is increased by 1.5-2 times. In the treatment of coccidiosis of chickens, it is recommended to use a mixture of phtazin with neomycin in doses: 100-150 mg of phtazine and 500-750 μg of neomycin per chicken 2 times for 6-7 days.

For the prevention of diseases, phtazin is prescribed in half of the indicated doses, 2 times a day for 4-5 days.

Contraindications for use: hypersensitivity of animals to sulfonamides, diseases of the hematopoietic organs, acute hepatitis, nephritis, nephrosis.

Produced in powder and tablets of 0.5 g. Store according to list B in a well-sealed container, protected from light and moisture. The term of the verification analysis is 2 years.

Sulfanilamide drugs and other antimicrobial agents (phthalazole, etazol, sulfacyl sodium, sulfadimethoxine, sulfalene, biseptol (co-trimoxazole), salazosulfopyridine, salazopyridazine, nalidixic acid, nitroxoline, ciprofloxacin, levofloxacin.

13. Sulfonamides for topical use

14. Combined preparations of sulfonamides and salicylic acid

15. Combined preparations of sulfonamides with trimethoprim

6. Non-fluorinated quinolones

Fluoroquinolones have general properties:

What are sulfa drugs

Classification of sulfa drugs

The mechanism of action of sulfa drugs

Indications for the use of sulfonamides

List of sulfa drugs

Combined sulfa drug

Sulfanilamide preparations for children

Instructions for the use of sulfonamides

Side effects of sulfa drugs

The price of sulfa drugs

Video: what is sulfonamides

Classification of sulfa drugs

The mechanism of action of sulfa drugs

Indications for the use of sulfonamides

List of sulfa drugs

Combined sulfa drug

Sulfanilamide preparations for children

Instructions for the use of sulfonamides

Side effects of sulfa drugs

The price of sulfa drugs

Video: what is sulfonamides

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

Report a typo

Text to be sent to our editors:

Your comment (optional):