Karaganda State Medical University

Department of General Pharmacology

Topic: Sulfanimide drugs.

Performed: Art. G.2085 Savitskaya T.

Checked: Pube Nikolaev T.L.

Karaganda 2013.

1. Introduction

2. Suulfanimide drugs (pharmacodynamics, pharmacokinetics, contraindications and testimony for use, classification)

3.Sulfanimide drugs. Name. Forms of release, average therapeutic doses, use methods.

4. Farmakology: synthetic antimicrobial agents of various chemical structure.

5. Manufacturing sulfonamide drugs.

6. Used literature.

Sulfanimide drugs are synthetic chemotherapeutic agents, derivatives of sulfanyl acid, are able to significantly suppress the development of gram-positive and gram-negative bacteria, chlamydia, some simple and pathogenic fungi. The first sulfanimide synthesized in 1908. A graduate of the Pharmaceutical Faculty of Vienna University of P. Gel. However, therapeutic properties of the new chemical compound was not investigated. In 1932, the German chemists of the Far-Benindusty company were synthesized with red paint, whose antimicrobial properties explored G. Domagk. It showed that red paint has a pronounced antimicrobial effect in mice infected with hemolytic streptococcus. Proprietary (such a name received red paint) prevented the death of mice, which was administered to a 1000-fold dose of hemolytic streptococcus. Experimental studies should be confirmed by clinical observations. The dramatic case in the family of Gosegka accelerated these observations. His daughter fell ill with a severe form of septicemia with an unfavorable forecast at that time. G. Domagk was forced to give it proposed, although this substance was not yet used to treat. The daughter was saved from imminent death. G. DomAgk agreed to test the test in different clinics of Germany. From everywhere the scientist received positive feedback. An ordinary dye turned out to be an effective antimicrobial agent. Generalizing experimental, clinical studies, G. DomAgk in 1935 printed an article "Contribution to chemotherapy of bacterial infections" in the magazine "Deutsche Medi-Cinishe Wochenschrifft". For the opening of therapeutic properties of Rartzil G. Gomgk in 1938 received the Nobel Prize. However, he was patented by Farbenindusty, which had the drug exclusive right and installed high prices for him. Employees of the Pasteur Institute in Paris showed that the effective principle of pronosil, or red streptocide, its white fraction is an aminobenzenesulfamide, which was synthesized in 1908 P. Gel. It was streptocid (white streptocid). Since white streptocid was not patented, everything could be used. The discovery of therapeutic properties of strepticide and other drugs of this group began a new stage in the treatment of patients with infectious diseases - sulfonamide therapy. The product for the synthesis of sulfanimamides is the acid sulfanyl acid obtained from the PABK. Sulfanimonds have one general formula. Today, more than 15,000 sulfanyl acid derivatives are synthesized, of which about 40 are introduced into medical practice as antibacterial agents. Under the influence of sulfonamide drugs, the bacteriostatic effect of in vivo and in vitro is observed only with respect to cells of bacteria breeding. For antimicrobial activity, the presence of a free amine group NH2 in the 4th position is required. The spectrum of antimicrobial actions of sulfonamide preparations is quite wide: gram-positive and gram-negative cocci, intestinal wand, shgella, cholera vibrion, clock-stream, protozoa (pathogens of malaria, pneumocists, toxoplasms), chlamydia (ornithosis pathogens), pathogens of Siberian ulcers, diphtheria, plague, pathogenic Mushrooms (actinomycetes, coccides), large viruses (trachoma pathogens, granuloma). The mechanism of chemotherapeutic action of sulfonamide drugs is based on the overall structure of them with a para-aminobenzoic acid (PABK), due to which they competing with it are attracted to the metabolism of bacteria. By competition with PABK, sulfonamides prevent the use of its microorganisms for the synthesis of the acid dihydrofolye. Dihydrofoliic acid with the participation of reductase turns into metabolically active coenzyme-acid tetrahydrofolya, participating in the processes of the synthesis of pyrimidine bases of DNA and RNA. The microbial cell has a certain amount of accumulated PABK, so the effect of sulfanimamides is observed after a certain latent period, during which 5.5 ± 0.5 generation occurs. Thus, competitive antagonism between sulfonamides and PABK is a significant extent prevails towards PABK. Therefore, for antimicrobial action, it is necessary that the concentration of sulfonamide in the medium exceeds the concentration of PABK in 2000 - 5000 times. Only in this case the microbial cells will absorb sulfanyamide instead of PABK. That is why sulfonamide drugs are introduced in fairly significant doses. First, 0.5 - 2 g of the drug is prescribed to create sufficient concentration in the body, and then systematically introduced in doses, which will ensure bacteriostatic concentration. As a consequence, the synthesis of purine and pyrimidine compounds, nucleoti-dov and nucleic acids is disturbed, which leads to the oppression of the exchange of proteins of microorganisms, violates the development and division of their cells. The use of sulfonamide drugs in reduced doses contributes to the formation of strains of microorganisms resistant to the action of drugs. The antibacterial effects of sulfonamide drugs decreases with pus, blood, the products of the decay of the body of the body, in which are contained in sufficient quantities of PABK and folic acid. The means that, by virtue of its biotransforphic, form a PABK (for example, Novocaine), as well as compounds containing purine and pyrimidine bases, reduce the antibacterial effect of sulfanimamides. Conversely, those compounds that are capable of suppressing dihydrofolic acid reductase are synergists of sulfanimamides, since the following stage of metabolism is violated - the synthesis of tetrahyd-rofoliyevoy acid synthesis with dihydrofolius. An example can be, for example, trimethoprium, which is used to create effective antimicrobial agents. The sensitivity of microorganisms to sulfonamide drugs is due to their ability to synthesize PABK. Hopely to streptocide hemolytic streptococcus. Microorganisms that do not require PABCs (absorb the acid dihydrofolya) are not sensitive to the action of sulfanimamides. Less sensitive to sulfonamide staphylococcus, enterococcus, protea, tularemia causative agent. In the first years of widespread use, sulfonilamide drugs showed high efficiency in terms of staphylococcus, meningococcus, gonococcal and more. Now most clinical strains of these microorganisms have gained resistance to the action of sulfonamide drugs due to the ability to synthesize PABK or as a result of mutation. Most sulfonamide preparations are obtained on the basis of the strepticide molecule by introducing aliphatic, aromatic and heterocyclic radicals. The substitution of hydrogen in the nitrogen of the sulfonamide group allows antimicrobial compounds with aliphatic groups (sulphacyl), aromatic radicals (sulfadinezin, ethazol, norsulfazole). If we replace hydrogen in the nitrogen of the amine group in the 4th position, the antibacterial activity of the compound is significantly reduced. This is due to a decrease in the similarity of sulfonamide to PABK. Phthalazole, for example, acquires antobacterial activity after the restoration of the amino group, which is occurring in the intestine. The spectrum of the antobacterial action of various sulfonamide preparations is somewhat different due to the ability to suppress them and other enzyme systems. Nisulfazol has a thiazolic ring, mimics the effect of thiamine and suppresses the synthesis of cocarbo-xylase, participating in the decarboxylli-acid pivine-grade. According to Norsulfazol acts on Gonokokk, Staphylococcus, the intestinal group of bacteria, weaker - on pneumatic, meningo and especially streptococcus. Sulfadinezin active relative to the Cockkops and gram-negative sticks, less active in relation to gono and staphylococcus. Ethane has a moderate bacteriostatic effect on most Cockkops, active in relation to intestinal flora. Sulfanimide is a white powder, a little soluble in water, soluble in aqueous substrate solutions. The selection of sulfonamide preparations is determined by the properties of the pathogen, the spectrum of antimicrobial action, as well as the peculiarities of pharmacokinetics. Classification. Depending on the features of pharmacokinetics (absorption in the gastrointestinal tract and duration of the elimination of the body), sulfonamide drugs are separated into the following groups: I. Preparations that are well absorbed from the digestive tract, and therefore they are prescribed for systemic treatment for diseases caused by sensitive microorganisms. T1 / 2 of these drugs in the blood are different, so they can be divided into separate subgroups. 1. Preparations

short-term action with T1 / 2 to 10 h (ethasol, norsulfazole, sulfadimesin). They are prescribed 4 -6 times a day, a daily dose of 4 - 6 g, term-period - 20-30 g. 2. The preparations of the average duration of the action of that / and 10 to 24 h (sulfazine, methylsulfazine). They are prescribed 1-3 g per day 2 times; Course dose 10-15 g. Preparations of short and medium duration of action are used mainly during acute infectious processes. 3. Preparations long action with T1 / 2 more than 24 hours (sulfapyridazine, sulfadimetoxin, sulfamodimeters-son). Assign the first days 1-2 g, then 0.5 - 1 g 1 time per day. 4. Preparations Increased actions with T, / 2 60 - 120 h (sulfalen). Sulfalen is prescribed in a dose of 1 g of the first day, then 2 g times a week or 0.2 g per zo mines before meals, daily in chronic diseases. II. Preparations that are practically not absorbed in the digestive channel (phthazine, phthalazole, sulgin) are prescribed with colitis, enterocolite only inside. These drugs form a significant concentration of the active substance in the intestines (phthalazole decays with the formation of norsulfazole). With long-term use of sulfonamides, the saprophitite microflora is suppressed, which plays a significant role in the synthesis of vitamin K2, whose balance sheet can lead to hypoprothrombinemia. III. Preparations local action (Strepto Cide, ethasol, sulfacyl sodium). Streptocid, ethazol as the smallest powders are used for printing, in the form of a liniment, sulphacyl sodium - for eye drops that penetrate all the fabrics of the eye. Sulfanimamides are part of many ointments. IV. Salazosulfanimamides - nitrogen compounds of sulfanimamides with salicylic acid (salazosulfapyridine, salasopyridazine, salazodimetoxin) have antibacterial and anti-inflammatory properties. In the intestines they disintegrate with the release of active sulfonamide and acid 5-aminosalcyl. Prescribed mainly by a nonspecific ulcerative colitis of 0.5 - 1 g 4 times a day. V. Combined preparations of sulfanimamides with trimethoprim (Bactrim - Biseptol). Sulfanimamides, which are well absorbed into blood, are able to form complexes with plasma albumin, and partially circulate in free state. Communication with proteins is unstable. The degree of communication increases with an increase in the hydrophobicity of molecules. Acetylated forms are more connected with proteins than free connections. With a decrease in the level of protein in a blood plasma in it significantly increases the content of the free fraction of sulfonamides. From the blood of sulfonamides, they are well penetrated into various fabrics and fluids of the body. Sulfapyridazine has the greatest permeability. In significant quantities of sulfanimamides are found in the kidneys, liver, lungs, skin, in smaller - in adipose tissue, are not detected in the bones. The concentration of sulfanimide in the pleural, peritoneal, synovial and other liquids is 50 - 80% of it in the blood. The process of inflammation greatly facilitates the penetration of sulfanimamides through the hematorencephalic barrier in the brain tissue. They are quite easy to pass through the placenta, are determined in saliva, sweat, in the milk of the mother, in the tissues of the fetus. Biotransformation of sulfonamides is different for different drugs. Sulfanimiamides in the body partially acetylates-Xia are oxidized, form inactive bonds of Ronides or do not change. Acetyluoyuvani in the liver and depends not only on the drug, but also from the acetyluyuchi liver ability. Less acetylates-Sia etazol, Urosulfan, more - sulfidine, streptocid, norsulfase, sulfadimezin. At acetylation, the activity of the drug is lost and its toxicity increases. Acetylated sulfonamides have low solubility and in an acidic environment can form concrections that are capable of falling into a precipitate (crystalluria), injury or even overlap the renal tubules. Preparations, acetyluchulus, are slightly derived from the body in an active form and have significant antimicrobial activity in the urinary tract (ethasol, worklfan). The formation of inactive glucuronides is characteristic of sulfadimetoxin. Glucuronides are well soluble and do not fall into the sediment. Sulfonamide metabolites do not have antimicrobial activity. Displays the kidneys by glomerular filtration and partially tubular secretion. Durable and enlarged drugs are small inactivated in the body and in significant quantities are reabsorbed in the tubules than and the duration of their action is explained. Side effects when using sulfonamide drugs can be different and dangerous, but with proper treatment it rarely happens. Complications common for the whole group: allergic reactions, influence on blood and the like. They are due to overdose of drugs or increased sensitivity of the patient. Overdose is more common in children and elderly, especially after the 10th day of treatment with long-term drugs. Signs of intoxication (nausea, vomiting, dizziness) may develop, damage to the epithelium of the kidney channels, the formation of crystals in them (oliguria, protein, erythrocytes in the urine), hepatitis. To prevent the formation of crystals in the urinary tract, a significant amount of alkaline drink should be prescribed (up to 3 l) or sodium hydrogencarbonate, mineral alkaline water. The purpose of sulfonamide drugs requires caution for kidney and liver diseases. Complications associated with increased sensitivity of the body may be an allergic nature (rash, dermatitis, exudative erythema, serum disease, vessel damage, sometimes anaphylactic shock). Blood lesions are observed - hemolytic anemia, leukopenia, agranulocytosis, rarely aplastic anemia, inhibiting influence on the CNS. Indications for the use of sulfonamide - Diseases caused by microorganisms sensitive to them. Sulfanimamides are well absorbed, used in infectious diseases of the urinary system, biliary tract, ear, throat, nose, lungs, prescribe a patient, actinomycosis, toxoplasmosis, malaria, meningitis, etc .. if the pathogen is sensitive to the drug, the healing effect is manifested in Flow 1 - 3 days: the signs of infectious toxicosis disappear (fever, circulatory disruption, breathing), the overall state is improved. Sulfanimamides are poorly absorbed, used in intestinal infections (enteritis, colitis, dysentery, abdominal typhoid, etc.). The antibacterial activity of sulfonamide preparations is much weaker than antibiotics. Considering this, as well as given the growth in the number of sustainable strains, recently sulfonamide drugs are applied less. They can be prescribed along with antibiotics. In order to prevent the formation of sulfanyl-dietary strains of microorganisms, combinations of sulfonamide preparations with other chemotherapeutic agents are used. For example, the combined drug Bactrim (Biseptol, Trimoxazole) contains 5 parts of sulfanilamide preparation of sulfamethoxazole and 1 part of trimethopril. Sulfamethoxazole and Timetoprix each separately carry out a bacteriostatic action. Simultaneous use in the form of a combined drug enhances antimicrobial effect and provides a high bactericidal effect even with respect to microorganisms resistant to sulfanilaminamide preparations. Sulfamethoxazole blocks the biosynthesis of acid dihydrofolya bacteria at the PABK level. Timetoprix blocks the following phase of metabolism - the recovery of the acid of dihydrofolye into the tetrahydrofolya by oppression of the dihydrofoliic acid reductase. Timetoprix at 5,000 - 10,000 times more related reductase dihydrofelting of microorganisms than with functionally similar to the reductase of mammals. Timetoprix has an antimicrobial spectrum, similar to other sulfonamides, but it is 20-100 times more active. Bactrim suppresses the development of the majority (about 95%) stamps of staphylococcus, pyrogen and green streptococcus, different species Protest, intestinal sticks, Salmonella, Shigell. Bactrim resistance is formed quite slowly. When administered inside the maximum concentration in the blood is determined after 1 - 3 hours and persisted within 7 hours. T1 / 2 Trimethopris is 16 h, sulfamethoxazole - 10 hours. In the presence of sulfamethoxazole, Timetoprix in small quantities binds to blood plasma proteins and quickly enters the tissue, where the concentration exceeds the serum concentration. Sulfamethoxazole up to 65% binds to albumin plasma blood. Sulfamethoxazole and Timetoprix in significant quantities are contained in bile, sputum, mothers milk, amniotic fluid, eye media, bone marrow, intracellularly. The current of the day with the urine is derived from the body of 60% trimethopril and 25 - 50% sulfamethoxazole, and more than 60% is derived unchanged. Indications. Bactrims are prescribed with infectious diseases of the genitourinary system, biliary tract, ear, throat, nose, upper respiratory tract, lungs, for the prevention of meningitis in groups, where there are carriers of meningococcus, for treatment with infectious diseases caused by the hemophilic stick influenza, patients with brucellosis, typhoid typhoid , cholera, etc. Therapeutic doses for adults - 1 g (2 tab.) Twice a day for 9 - 14 days and further 0.5 g twice a day in case of longer treatment. Contraindications. Sulfanilamide drugs, especially Bactrim, are contraindicated in pregnant women in connection with the possibility of disrupting the development of the fetus, women-mothers, since sulfonamides that come with milk can cause the child the development of methemoglo binemia. It should not be prescribed to children with hyper-bilirubinemia: the risk of bilirubin encephalopathy (especially in children of the first 2 months of life), as well as children with glucose-6-phosphate dehydrogenase deficiency in red blood cells. Side effect is rarely observed. These are dyspeptic phenomena of 3-4% of patients (nausea, anorexia, diarrhea, vomiting), rash on the skin, urticaria, itching (in 3-5% of patients). Sometimes heavier skin-allergic reactions are observed (Stevens - Johnson syndrome, multiform erythema, exfoliative dermatitis, etc.). Occasionally, leukopenia, agranulocytosis, thrombocytopenia, eosinophilia can develop. Possible megablast reaction bone marrow In pregnant women, patients with alcoholism (eliminated with folic acid). This reaction occurs according to the type of hypersensitivity and are usually contraindicated to the destination. Cross-reactions of allergies are possible in persons sensitized to sulfanimamides. Cases of violation of the reproductive function in men are described. Sometimes it develops candidiasis of the oral cavity and dysbacteriosis, especially in severely sick and older people. Sulfanimide preparations. Name. Forms of release, average therapeutic doses, use methods.

Sulfadimezin Sulfadimezinum Etazol Aethazolum Sulfatsil sodium Sulfacylum-natrium Sulfadimetoksin Sulfadimethoxinum Sul fap irndazin Sulfapyridazinum Ftalazol Phthalazolum Biseptolum-480 (120; 240; 960) Biseptol-480 (120; 240; 960) tablets powder of 0.25 and 0.5, the PO : 1st reception - 2 g, then take 1 g 4 - 6 times a day, sitting alkaline water. Children - 0.1 g / kg - 1st reception, further 0.025 g / kg every 4 - 6, or 4 - 8 hours. Powder tablets of 0.25 and 0.5 g. Inside 1 g 4 -6 times a day. In the wound - up to 5 g of the drug. Powder in ampoules of 5 ml of the zo% solution; in the vials of 5 and 10 ml of zo% distribution; Eye drops - a dropper tube with a 20% solution of 1, 5 ml. Inside the powder of 0.5-1 g 3 - 5 times a day, children 0.1 - 0.5 g 3 -5 times a day. Externally ointment. Powder tablets of 0.2 and 0.5 g. Inside the 1st day - 1 -2 g, then 0.5 - 1 g per day. Children: 1st day - 25 mg / kg, then 12.5 mg / kg. Powder tablets of 0.5 g. Inside the 1st day-1g, then 0.5 g; Heavy infections - 1st day - 1 g 2 times a day, then 1 -0.5 g 1 time per day Powder tablets But 0.5 g. Inside the 1st and 2nd day of 6 g per day, 3 And the 4th day - 4 g, 5th and 6th day - 3 g. Tablets for 20 pcs. Inside 2 tablets 3 times a day after eating.

Pharmacology: synthetic antimicrobial agents of various chemical structures.

This group includes various chemical compounds synthesized later than sulfonamide preparations, which differ from them and antibiotics by the structure, mechanism and spectrum of antibacterial action. All of them have high antibacterial activity and the predominant effect on pathogens intestinal infections and diseases urinary tract, including infections, difficult to treat other antimicrobial means. Preparations that are presented in this section are represented by such chemical groups 1. Hinolon derivatives of generations, derivatives of 8-oxychinoline (nitroxoline, chlorochinaldon, ranuophone, Intotrix). 2. Hinolon II generation derivatives, naphthyridine derivatives (Nalidix, oxoliniyev acid, Peipemidyev). 3. Derivatives of quinolone III generation, fluoroquinolones (ciprofloxacin, offloxacin, norfloxacin, pefloksacin, leplocksacin, sparfloxacin). 4. Hinoxalyna derivatives (chinoxydin, dioxidine). 5. Nitrofuran derivatives (Furacilin, Furazolidon, Frazolin, Furadonin, Fura-Gon, Furagin soluble). 6. The derivatives of imidazole (metronidazole). Hinolin derivatives (8-oxychinoline and 4-quinolones). Preparations of this group are presented halogen-(nitroxoline, mexazas of mexaform, quinophone) and nitro-producing compounds. They suppress the vital activity of microorganisms, forming complex compounds with metal ions, reduces their enzymatic processes and functional activity. Pipemidyev acid, for example, selectively suppresses the synthesis of bacteria DNA, has a wide range of antimicrobial action, which applies to gram-negative bacteria, pathogens of protozoal diseases (dysenteric amoeba, giardia, trichomonas, balancing). Preparations of this group are effective in relation to antibiotic-resistant bacteria due to the lack of cross-resistance. The effect of drugs are determined by the different degree of absorption in the digestive tract: enteroseptol and intestoopan are absorbed poorly, which contributes to the creation of their high concentrations in the intestine and is used in infectious diseases of the intestine. Nitroxoline, Peipemidiyev Acid and Oxoliniyev are absorbed well and are allocated by the kidneys unchanged, which ensures antibacterial effect in the urinary tract. Chlorochinaldon has antibacterial, spatimic, antiprotozoic activity. The greatest activity shows gram-positive and some gram-negative bacteria. Prescribed with intestinal infectious diseases (dysentery, salmonellosis, food toxicoinfection, infection caused by staphylococcal, proteate, enterobacteria), as well as dysbacteriosis. Intotrix for the chemical structure is close to nitroxoline and chloropaldon, contains a surface active substance. It has antimicrobial, protiamembne, spammed action. Assign in cases of acute diarrhea of \u200b\u200binfectious origin, dysbacteriosis, amebiasis. Hiniophone has no wide use. Prescribed with amoebic dysentery. Adding preparations of this group inside, it should be borne in mind that in the case of long-term use of them, as well as people with increased sensitivity, side effects may occur: peripheral neuritis, myelopathy, lesion of the optic nerve, violation of the liver, kidney function, allergic reactions. Therefore, despite their significant antibacterial activity, the treatment is carried out very limited. In case of infectious diseases of the intestines, chloropaldol and intestoopan, urinary tract - nitroxoline are used. Nitroxoline (5-Nok, Uritrol -

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

PABK is included in the structure of dihydrofoliic acid, which is synthesized by many microorganisms. Thanks to the chemical similarity with PabK, sulfanimamides prevent its inclusion in dihydrofoliic acid. In addition, they competitively oppress dihydropteroatencetase. Violation of the synthesis of dihydrofolytic acid reduces the formation of a tetrahydrofolytic acid from it, which is necessary for the synthesis of purine and pyrimidine bases.

Spectrum of action Sulfanimamides are quite wide:

a) bacteria - pathogenic cocci (gram-positive and gram-negative), intestinal wand, pathogens of dysentery, cholera vibrion, pathogens of gas gangrees, pathogens of Siberian ulcers, diphtheria, catarrhal pneumonia, influenza, plague;

b) chlamydia - pathogens of trachomas, paramathum, ornithosis, groin lymphogranulum;

c) actinomycetes;

d) the simplest - causative agent of toxoplasmosis, malaria plasmodium.

In violation of the principles of chemotherapy, stable strains of microbes are developing. Causes of resistance: Microbes produce more PABKs, workplates of protein synthesis are developed. It must be borne in mind that some medications, in whose molecule includes a PABK residue (for example, novocaine), an expressed antisulfanimine action can have a pronounced

Classification of sulfonamide

1. Sulfanimiamides, poorly absorbed from the gastrointestinal tract and slowly distinguished from the body (acting mainly in the intestine):

Sulgin - It is used in dysentery, colitis, enterocolitis, carrier of dysenteric chopsticks, chopsticks of abdominal typhoid, to prepare for intestinal operations.

Phthalazol. - split into norsulfazole and phthalic acid. Indications are the same. Less toxic than sulgin.

2. Sulfanimides with good absorption of the gastrointestinal tract:

- short-term action

Norsulfazol.- acts mainly on hemolytic streptococcus, pneumococci, gonococci, staphylococci, intestinal wand. Well penetrates the brain and lungs. It is used inside with the infections of the bronchopulmonary system, meningitis, staphylococcal and streptococcal sepsis. Causes crystallour.

long action

Sulfadimetoxin(Madribon) - Persoads badly through the BC, in other organs and fabric penetrates well. It is excreted by the kidneys in the form of soluble glucuronides, so crystallurium practically does not cause.

General principles of sulfonamide treatment

Drugs

1. Early start of treatment.

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

3. High doses of the drug.

On the first day of treatment, maximum one-time and daily doses for saturation. For short action sulfonamides, the highest one-time dose 2.0; daily 7.0; Reception frequency 4-6 times. In the following days of treatment, the daily dose is reduced by 1.0 per day. Course dose up to 30.0.

Durable preparations: on the first day they are prescribed 2.0 once, and in the following days - 0.5 - 1.0 once. Course dose up to 10.0.

4. For the prevention of crystalluria, an alkaline drink is necessary (3 liters of fluid per day).

5. Sulfonamides cause the inhibition of saprophilic bacteria in the intestine, synthesizing the vitamins of group B, so the average dose of Vitamins of group V. should be prescribed

6. Before treatment and during it, test blood.

7. Before appointing drugs to find out in the patient their portability.

8. Urine tests for microhematuria.

9. Combination with antibiotics.

Gross formula

Pharmacological group of substance Sulfanimide

Nonological Classification (ICD-10)

CAS code

Characteristics of substance Sulfanimide

Refers to a short action sulfonamide LAN. Sulfanimide is a white crystalline powder without smell, slightly bitter taste with a sweet aftertaste. Easily soluble in boiling water (1: 2), it is difficult - in ethanol (1:37), soluble in solutions of hydrochloric acid, caustic alkalis, acetone (1: 5), glycerin, propylene glycol; Practically insoluble on air, chloroform, benzene, petroleum ether. Molecular weight - 172.21.

It is also used in sodium methanesulfate (soluble streptocide) - white crystalline powder; soluble in water, practically insoluble in organic solvents.

Pharmacology

The antimicrobial action mechanism of sulfonilamide is associated with the antagonism of the PABK, with which it has chemical similarities. Sulfanimide is captured by a microbial cell, prevents the inclusion of PABK into dihydrofoliic acid and, moreover, the competitively inhibit the bacterial enzyme dihydropteroatencetase (the enzyme responsible for embedding the PABK into dihydrofoliic acid), as a result, the synthesis of dihydrofoliic acid is disrupted, the formation of metabolically active tetrahydrofolic acid is reduced. For the formation of purines and pyrimidines, the growth and development of microorganisms (bacteriostatic effect) stops.

Active with respect to gram-positive and gram-negative kokks (including streptococci, pneumococci, meningococci, gonococcal), Escherichia coli, Shigella SPP., Vibrio Cholerae, Clostridium Perfringens, Bacillus Anthracis, Corynebacterium Diphtheriae, Yersinia Pestis, Chlamydia SPP., Actinomyces Israelii, Toxoplasma Gondii.

For local application Promotes rapid healing of wounds.

When taking inside quickly absorbed from the gastrointestinal tract. C Max in the blood is created after 1-2 hours and decreases by 50% usually in less than 8 hours. Passes through histohematic, including BGB, placental barriers. It is distributed over the tissues, after 4 hours is found in the spinal cord fluid. In the liver acetylated with the loss of antibacterial properties. Displays mainly (90-95%) kidneys.

Information about carcinogenic, mutagenic action and influence on fertility during long-term use in animals and person is absent.

Previously, sulfanimide was used inside for the treatment of angina, grinding inflammation, cystitis, pylitis, enterocolitis, prevention and treatment of wound infection. Sulfanimide (soluble streptocide) in the past was used in the form of 5% aqueous solutions for in / in the introductions that were preparing ex Tempore.; Currently use only in the form of a liniment for outdoor use.

Application of substance Sulfanimide

Most: tonsillitis, purulent-inflammatory skin lesions, infected wounds of different etiology (including ulcers, cracks), furuncle, carbuncoon, pyodermium, folliculitis, face, vulgar eels, impetigo, burns (I and II degrees).

Contraindications

Hypersensitivity (including to other sulfon and sulfonamides), diseases of the hematopoietic system, anemia, renal / hepatic insufficiency, congenital deficiency of glucose-6-phosphate dehydrogenase, azotemia, porphyria.

Restrictions on application

Pregnancy, breastfeeding.

Application in pregnancy and breastfeeding

With systemic absorption, sulfanilamide can quickly pass through the placenta and detect in the blood of the fetus (the concentration in the blood of the fetus is 50-90% of the mother's blood), as well as cause toxic effects. Sulfanimide safety safety during pregnancy is not installed. It is not known whether sulfanyamide can have a harmful embryonic effect when taking pregnant women. In experimental studies in rats and mice received during pregnancy, some sulfonamides (including sulfonamide) of short, medium and long-term action inside in high doses (7-25 times greater than the therapeutic oral dose for humans), a significant increase in the frequency of development of wolf grazing and other defects of bone development in the fetus.

Penetrates into breast milk, can cause nuclear jaundice in newborns.

Side effects Substance Sulfanimide

Allergic reactions; With long-term local application in large quantities - system action: headache, dizziness, paresthesia, tachycardia, nausea, vomiting, dyspepsia, leukopenia, agranulocytosis, crystalluria, cyanosis.

Interaction

Myelotoxic LS amplify hematotoxicity.

Ways of administration

Most.

Precautions Substance Sulfanimide

With long-term use, it is necessary to periodically analyze peripheral blood.

Trade names

Sulfanimida - These are synthetic chemotherapeutic agents that are derived sulfanyl acid. Were the first highly efficient antibacterial agents.

Mechanism of action:

Sulfanimamides have a structural similarity with para-aminobenzoic acid (PABK), are its competitive antagonists.

As a result, the synthesis of nucleic acid is oppressed, as a result, the growth and reproduction of microorganisms is suppressed (bacteriostatic effect). With prolonged use of CA, the stability of microorganisms is developing. Stability Cross.

The antibacterial effect of sulfanimamides is reduced or disappears in the presence of blood, pus, the products of the decay of tissues, where there are noticeable amounts of PABK.

Antimicrobial spectrum:

Real spectrum (As a result of the resistance of microorganisms) of the antimicrobial effect of sulfonamides: Many strains of pneumococci (not all!), Dysentery pathogens, paratif, chlamydia, pneumocists.

They are practical do not work On infections caused by staphylococci, most strains of streptococci, gonococcal, meningococci, hemophilic stick, a blue rod, protemat, enterococci, klebseyella, an intestinal wand.

Sulfanimamide classification:

Depending on the pharmacokinetics, sulfonamides are divided into four groups.

1. Sulfanimamides that are well absorbed from the gastrointestinal tract (resorbing):

1.1. Preparations of short action (t 0.5 less than 10 hours):

Sulfadimesin

Sulfacyl

Norsulfazol.

Streptocid

1.2. Medium duration preparations (10 - 24 hours):

Sulfazine

Sulfamethoxazole.

1.3. Durable preparations (more than 24 hours):

Sulfadimetoxin

Sulfapyridazin

1.4. Prescription preparations (60 - 120 hours):

Sulfalen

2. Sulfanimamides, slowly and not completely absorbed in the gastrointestinal tract (non-rigging):

Phthalazol

Sulgin

3. Sulfonamides for local applications:

Sulfacyl - sodium (sulfacetamide, albucid)

Sulfapyridazin - sodium

Sulfargin (sulfadiazine, dermazin)

4. Combined sulfoniamides

A) Salazosulfanimamides

Salazopyridazin (Salazodine)

Salazosulfapyridin

Salazodimetoxin

Mesalazin (Salofalc)

B) Combined preparations with trimetaprim:

Ko-trimoxazole (Biseptol, Septrine, Bactrim, etc.)

FANCER

Pharmacokinetics:

All sulfonamides are partially absorbed in the stomach, most - in thin intestines. In the blood, peak concentrations are usually created after 2-6 hours.

In high concentrations of sulfanimamides are found in the kidneys, lungs, liver, skin; They are not detected in the bones. Sulfanimonds penetrate well through the BC. In sufficiently high concentrations (50-80% of blood content), they are present in liquid media, as well as the tissues of the fetus (the teratogenic effect is possible). Sulfanimonds are poorly soluble in conventional acidic urine reaction. In the kidney channels, they can be precipitated in the form of crystals and block lumen. This complication can be prevented and significantly accelerated the removal of drugs, artificially raising the pH of the urine by intake of soda, alkaline mineral waters.

Indications for use:

1) infections of the eyes, respiratory tract, sex tract caused by chlamydia (erythromycin and tetracyclines) remain;

2) primary (previously not treated) Acute urinary tract infections, especially in non-remote women (uroantics and antibiotics with bactericidal effects are still considered to be selected);

3) nonspecific ulcerative colitis, enteritis and other inflammatory bowel diseases, most of the strains of causative agents of dysentery have developed stability, and preference is given to antibiotics;

4) Shallow burns, wounds - only in linomies and ointments (Mafenide or Sulfadiazine of Silver).

In the treatment of pneumococcal and other pneumonia, meningitis - only after confirming the sensitivity of the flora and in combination with other chemotherapeutic agents.

Complications:

1. Overdose of the drug is more often manifested in children and older people, especially after 10 - 14 days of treatment.

Symptoms of intoxication of CNS - dizziness, headaches, oppressed state, nausea, vomiting (outpatient reception is contraindicated in transport drivers);

Kidney damage - pain in the lumbar region, oliguria, protein and red blood cells in the urine, microcrystals of drugs and their metabolites

Bloodside: hemolytic or aplastic anemia, granulocyptopenia, thrombocytopenia.

2. Hypersensitivity occurs on average in 5% of patients. Preparations can cause allergic reactions at any route of administration, but faster and brighter - after receiving well absorbing drugs. The most frequent skin manifestations of allergies (various rashes, limited dermatitis, generalized dermatitis, exudative erythema, necrotic lesions, etc.). Other manifestations include fever, vascular lesions and anaphylactic shock.

Characteristics of groups:

1. Ca, well absorbed from the GTS - are prescribed for systemic treatment of infections caused by sensitive microorganisms.

2. Sulfanimamides, slowly and not completely absorbed in the gastrointestinal tract and creating a high concentration in a thin and thick intestine - are prescribed only inside. Apply for the treatment of acute enteritis, bacterial dysentery, colitis and enterocolites caused by sensitive aerobic flora. We are prescribed according to the schemes, the course of treatment on average 5 - 7 days.

3. Sulfonamides for local applications - they are most successful in eye practice. Albucid is used in the form of 30% eye drops, eye ointment. The drug is prescribed under inflammatory diseases of conjunctivations, blufares, purulent corneal ulcers, with trachus caused by chlamydia.

For local application, a large number of soluble sodium salts of sulfonamide sodium salts is produced: streptocide, norsulfazole, ethasol, sulphapyridazine, etc. in the form of solutions, in aerosols, in lines, ointments, powders are used for the treatment of purulent wounds, long-lasting ulcers, burns, fruit diseases , breakingles, etc. Pre-wounds and the affected surface must be washed from pus and processed by an antiseptic. Most sulfanimamide solutions have a strongly alkaline reaction and, when applied to damaged tissues, they cause sharp and long-term (for 1-3 h) pain. Better than others are transferred and more efficient 10% mafenida ointmentand 1% sulfargin ointment (silver sulfadiazine, dermatain).Contraindication: Allergic reactions to sulfonamides in history. The duration of treatment is from 1 to 3 weeks.

Swipping wounds and burns with powders of sulfanimamides not only ineffectively, but also undesirable, since the pus is accumulated under the resulting crust, and the process develops deep into.

4. Salazosulfanimide - compounds of a number of preparations with salicylic acid. Most widely used salazopyridazin (Salazodine)in the form of tablets, candles, suspensions. Used to treat polyimicrobial (nonspecific) colitis, including peptic.

5. Combined CA with trimetaprim. As a result of combining, not only the mutual potentiation of antimicrobial action occurs, but also the spectrum is expanding; In high therapeutic doses, the combined drugs exhibit a bactericidal effect on a number of microbes. Sustainability of microorganisms K. combined drugs develops slowly.

Its optimal ratio in combination with sulfamethoxazole (bispetol preparation) is 1: 5. At the same time, peak concentrations of drugs in the blood are achieved after 1 to 4 h.

Indications for the use of bispetol and its analogues:

1) Bacterial infections of the respiratory tract - pneumonia, acute bronchitis and aggravation of chronic; used for the treatment and prevention of secondary infections;

2) pneumonia caused by pneumocists - Biseptol is considered to be a drug selection; In severe flow, an intravenous infusion of the solution is shown;

3) infections of the lower and upper urinary tract (in the absence of bacteriuria);

4) enteritis and enterocolites caused by a dysenteric stick, bacteria of a typhoratyphound group, cholera vibriums and another microflora, including those gained resistance to ampicillin and leftomycetin;

5) inflammation of the middle ear, meningitis (in combination with other chemotherapeutic agents), sepsis (in / c);

Side effects.

- allergic reactions.

HEMOPOOEZ VIOLATIONS.

Principles of sulfonamide therapy:

1. Begin treatment as early as possible from the use of a shock dose.

2. Assign confirmation doses to the track behind the shock according to the scheme, based on the pharmacokinetics of the drug.

3. Conduct course treatment with a duration of at least 5 - 10 days, without interrupting and without reducing the course of treatment.

Sulfanimida

Lecture for students of 3 courses FVM

Plan lectures

1. General characteristics of sulfonamide

2.

· Short action preparations

· Sulfanimonds, poorly absorbed from the gastrointestinal tract

Sulfanimide drugs - A large group of medicinal substances, the basis of the structure of which is a sulfanyl (para-aminobenzosulfonic) acid.

Sulfanimamides are active antimicrobial means. In recent years, interest in this group of drugs has increased due to the synthesis of long-acting sulfonamides and the creation of drugs combined with trimethmodium.

Sulfonamide drugs - white streptocide derivatives having a large similarity of physico-chemical properties.

All sulfonamides are white or slightly yellowish powders without smell, some are bitter taste. Most of them are poorly soluble in water, better - in dilute acids and aqueous solutions by alkalis (except Sulgin). The increase in the temperature of the solvent improves the solubility of drugs. A mixture of two or more sulfanimamides dissolves somewhat better than any of its components separately. Only sulfacyl has good solubility.

Amphoterne sulfonamides, they form salts with strong alkalis (with the exception of Sulgin) and with strong acids. Some sulfonamide salts are easily 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 solutions of aqueous solutions have a strong alkaline reaction (pH 10.5-12.5), with subcutaneous and intramuscular administration, they have a strong irritating effect. Infiltration of the place of introduction of sodium chloride isotonic solution can weaken the necrosis of tissues, and the infiltration of novocaine solution significantly reduces the painful reaction. For the same reason, undiluted sodium salts should not be given inside. An intravenously large animals introduce 10-25%, and small - 5% solutions. The exception is the sodium salt of sulfacyl, which in the solution gives an almost neutral reaction, and it can be prescribed in higher concentrations.

In sulfanylamund solutions dissociate on ions. Pharmacological activity is associated with their dissociation constants. For example, bacteriostatic effect is stronger in alkaline solutions, since ions are formed in these conditions. Norsulfazole, sulfacyl, much worse - streptocid is well dissociated. Compounds that are more capable of acid dissociation are better absorbed. Sulfanimide drugs are well soluble in biological fluids, including blood plasma.

Store sulfonamides on the list B in a well-unpaved container in a light place protected from light. The shelf life of drugs from 3 to 10 years

Preparations of this group refer to chemotherapeutic means of a wide antibacterial spectrum of action, as they suppress the vital activity of many types of gram-positive and gram-negative bacteria: streptococci, staphylococci, meningococci, gonococci, bacteria of the intestinal-typhoid-dynesentic group and many others. It is difficult for soluble compounds (phthalazole and its analogs, sulcimide and worklfan) are mainly on gram-negative bacteria. Sulfanimamides are active in relation to large viruses (pathogens of trachomas, inguinal lymphogranulation), cocidia, plasmodium malaria and toxoplasm, actinomycete, etc.

Sulfonamide drugs in small concentrations detain the growth and development of bacteria, that is, they act bacteriostatically. Bactericidal influence is only on the effects of such high concentrations that are unsafe for macroorganism. The most important feature of sulfonamide is high activity in vivo at a relatively weaker action in vitro. Under their influence, the microbes swell, cease to multiply, produce toxins, become more vulnerable to protective forces of the body. The electoral ability of individual drugs in relation to certain pathogens of infectious diseases has been established. Thus, norsulfazole and sulfazole are more active in staphylococcal infections, streptocid. - with streptococcal, and sulphapyridazine is very effective in sepsis caused by the bacterium if.

The bacteriostatic effect depends on the chemical structure of the drug, the degree and strength of binding to plasma proteins, the reaction of the medium, the dissociation constants and other factors. The condition is of great importance nervous system, the protective forces of the macroorganism, which owns the leading role in. Final elimination of the infectious process.

The mechanism of action of sulfonamide drugs is based on antagonism between sulfonilamides and para-aminobenzoic acid (PABC) due to the structural similarity of the para-aminobenzoic acid molecule and sulfanimamides, the latter are able to exhibit the PABK from the microorganism enzyme systems. Sulfanimamides violate the process of obtaining microbes necessary for their development "growth factors" - folic acid and other substances, in the molecule of which includes PABK under the influence of drugs in the microbial cell, the synthesis of methionine, purine and pyrimidine bases is disturbed, which in turn leads to a violation of nucleic acid synthesis and nucleoprotein.

The bacteriostatic effect of sulfonamides is manifested only at a certain concentration of drugs in the surrounding microbes. This concentration should be sufficient to prevent the use of para-aminobenzoic acid microorganisms contained in the tissues. The higher the PABK concentration, the greater the sulfonamide preparation is required for the antimicrobial effect. It has been established that for neutralizing one part of the PABK requires 1600 parts of the streptocide, 100 parts of sulfazine and 36 parts of the norsulfazole.

The special activity of sulfanimamides in relation to some microbes (streptococci, gonococci, etc.) and the lack of activity in respect of others is due to the fact that for the first presence of the PABK in the environment, it is necessary, and for the second, this acid has no essential value. In the same way, it is possible to explain the creation of a high therapeutic effect of sulfonamide drugs with acutely occurring processes, when the metabolism in the microbial cell passes intensively and the nutritional disorders and metabolism of microorganisms at this moment immediately affects them.

Some sulfonamides show competitive antagonism and with respect to other enzyme systems, in particular, they violate the process of decarboxylation of peeling acid, glucose oxidation

The mechanism of the antimicrobial action of sulfonamide drugs is determined not only by competitive relationship between sulfanimide and para-aminobenzoic acid. Sulfanimamides prevent the synthesis of dihydrofoliic acid in the microorganism of glutamine and para -aminobenzoic acids. Protein substances (rose, dead fabrics) containing a large amount of PABK, as well as some drugs, in the molecule of which includes the residue of para-aminobenzoic acid (novocaine, anesthesine), are inhibitors of sulfonamide activity. At the same time, the presence of urea increases their bacteriostatic activity.

Sulfanilamide drugs do not affect microbial catalase, the activity of indofenoloxidase, the absolutes of bacteria, do not significantly change the activity of dehydrangees and do not act on proteolytic enzymes. However, with some enzymes, as well as with PABK, drugs of this group can enter into competitive relationships. For example, they slow down the activity of carboxylase of enzymes containing pyotinemide (this explains the stronger bacteriostatic effect of norsulfazole on staphylococcus). Sulfanimamides do not act in vitro on toxins and endotoxins of bacteria, but they can neglece the effect of endotoxins to the body.

The effects of small doses or the purpose of sulfanimamides with large intervals leads to the development of an adaptive response in microbes, a change in the way to form them to grow and reproduction of enzyme systems. As a result, sulfanimide-sustainable races of microorganisms arise. The blockade of PABK Sulfanimidem does not significantly violate the livelihoods of microbes.

The stability of microorganisms purchased to one sulfonamide preparation is also applied to other drugs of this group (complete cross-stability). Acquired bacteria resistance to sulfonamide, associated with the increased production of PABK, can be genetically inherited.

Sulfanymido-resistant cultures change morphology, culture-biochemical properties, antigenic structure, virulence. The development of sulfanylaminilaise depends on both the type of microorganisms, their condition and the state of the macroorganism (resistance, character of the inflammatory process, etc.).

Almost all sulfanymido-stable strains of microorganisms retain high sensitivity to antibiotics, nitrofurans and other chemotherapeutic agents.

Sulfanimide compounds have a wide range of action on macroorganism and should be considered as specific nerve stimuli. They reduce the increased reactivity of the body, have an antipyretic effect. Sulfanimide drugs act anti-inflammatoryly, cause the oppression of regeneration processes under local application; Reduce the activity of nucleophosphatase liver, kidneys, spleen, violate normal acetylation processes, being a specific inhibitor of coal anhydrase, reduce the plasma ability to bind carbon dioxide, inhibit gas exchange, reduce the activity of other enzyme systems, stimulate the phagocytosis process, increase the body's stability to toxins.

Due to the combination of antiallergic, antipirelic properties with a bacteriostatic action of sulfonamides can be used in various diseases accompanied by inflammatory processes. Their effects on micro and macroorganism complement each other, providing a well-pronounced therapeutic effect.

Sulfanilamide drugs are low-toxic. However, the long-term use of them in oversized doses can lead to the development of undesirable, that is, toxic, effects: inhibition of useful microflora in the gastrointestinal tract, cyanosis, leukopenia, anemia, Avitaminosis, agranulocytosis, and shared oppression. In case of insufficient kidney function or in the appointment of large doses of drugs, crystalluria phenomena may occur. The correct appointment of sulfonamide animals does not cause side effects.

During the period of use of sulfonamide, it is impossible to give drugs, easily splitting sulfur (sodium hyposulfit, glaublers salt, etc.).

Most sulfonamides are easily absorbed from the gastrointestinal tract (streptocide, norsulfazole, ethazol, sulfazine, sulfadimesin, sulfapyridazine, sulfadimetoxin, etc.) and quickly accumulates in the blood, organs and tissues in bacteriostatic concentrations, penetrates the hematophephalic barrier. The bulk of the drugs is absorbed in the subtle intestinal department. The absorption rate depends on the degree of acid dissociation. Sodium salts of drugs are very well absorbed. Some sulfonamides, such as phthalazole, sulgin, phthazine, are difficult to be absorbed, relatively long are in the intestine in high concentrations and are allocated mainly with feces, so they are used mainly for diseases of the gastrointestinal tract.

With many infectious diseases, the causative agent is not in the blood, but in various organs and tissues, therefore the determination of the concentration of sulfonamide drugs in organs and tissues is often more significant than determining the concentration of them in the blood.

The speed and degree of distribution of sulfanimamides affect the chemical structure of drugs, the value of the dose, the method of administration, the activity of the pathological process I am a number of other factors. In the blood, organs and tissues, sulfonamide drugs are in the form of free compounds and in a plasma associated with proteins, part of the drug is subjected to acetylation. To manifest antibacterial activity, the concentration of free sulfanimide in the plasma should be no lower than 40 μg / ml.

The strength and degree of binding of sulfonamide drugs with plasma proteins are of great importance in the penetration of drugs in various organs and tissues and affect the speed of their elimination from the body. Sulfanimamides are binding mainly with albumin fraction, diffuse in tissue is much worse, therefore, in the body of the body rich in albumin, the concentration of drugs is usually higher compared to liquids containing fewer albumin (liquor, chamber water). The permeability of sulfonamide preparations through the blood-brain barrier depends on both the properties of the drug and the state of the macroorganism, in the infected organism of sulfanimamides penetrate the liquor in much large quantities than in a healthy body. In various organs and tissues, they are unevenly distributed. The greatest number of drugs are found in the kidneys, significant quantities in the lungs, walls of the stomach and intestines, heart, liver and much smaller - in the muscles, spleen, adipose tissue. Sulfanimonds penetrate well through the placenta.

In human body and animal sulfonamide compounds, like others medicinal substancesSubjected to splitting, oxidation, acetylation. Especially important for clinical practice It has acetylation process. It occurs mainly in the liver, both at the expense of acetic acid, incoming from outside, and due to the acid generated in the body of peer-grade acid.

In a healthy body, acetylation degree is slightly higher than in an infected one. In addition, the degree of acetylation of sulfonamide increases with their long-term use, decrease in diuresis, kidney diseases, accompanied by renal failure. The intensity of acetylation in various species of animals is non-etinakov.

Acetylated derivatives of sulfonamides do not act on microorganisms and are much worse dissolved in water. Due to poor solubility, especially in acidic urine, the acetoproducts fall into the sediment with the formation of conglomerates, blocking the lumen of the renal tubules, followed by a diurea violation.

To uniformly maintain the therapeutic concentration of sulfonamide drugs in the blood, organs and tissues, the speed of their removal from the body plays a major role. Most sulfanimamides (sulfacyl, streptocid, norsulfazole, etc.) are relatively quickly removed from the animal organism. They are eliminated mainly by kidneys in the form of an unchanged starting compound and in the associated state with acetic and glucuronic acids. In addition to kidneys, sulfanimamides may be isolated by milk, sweat, salivary bronchial and intestinal glands, as well as liver.

The therapeutic relations are especially valuable drugs quickly absorbed from the gastrointestinal tract and honey-standing out of the body. Depending on the rate of elimination of sulfanimamides from the body, they divide into three groups:

1) Preparations of fast-acting (streptocid, norsulfazole ethasol, sulphacyl, worklfan, sulfadimezin, etc.);

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

3) Preparations of long and superconducting actions (sulfapyridazine, sulfadimetoxin, sulfamimetoxin, sulfalen, etc.).

The rate of excretion from the body largely determines the dose value and the frequency of reception of the drug. The rate of removal is the value of T50%, or T1 / 2, the half-life period, that is, the time of reducing the maximum concentration in the blood is 2 times. In the short-acting drugs T1 / 2, less than 8 hours, the average duration of action is 8-16 hours and in long-term and super-valve drugs - 24-56 hours and more.

Sulfanimide drugs of long-term action are well absorbed from the gastrointestinal tract, creating high blood concentrations, and most importantly - long delay in the body. They can be prescribed to significantly smaller doses and through longer intervals between the introductions. These properties significantly expand the prospect of the use of connections of this group in veterinary practice.

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

Preparations of short-term type of action are prescribed 4-6 times, medium duration - 2 times and a long-term action - 1 time per day. The first dose (initial) must be almost twice as follow-up (supporting) doses, calculated on the replenishment of the separated drug. The course of treatment is usually 3-8 days. The magnitude of the initial and maintenance doses depends on the sensitivity of the pathogen, the severity of the disease, the age and the state of the animal and the features of the drug.

Sulfanimamides are shown for the treatment of infectious diseases of the respiratory tract (tracheite, bronchitis, pneumonia, purulent pleuritic, etc.), gastrointestinal diseases of various etiologies (dyspepsia, coccidiosis, dysentery, gastroenterocolites, etc.); Ground inflammation, soil, postpartum sepsis, pelitis, cystitis, salmonellosis, colibacteriosis, pastellosis, wound and other infections caused by microorganisms sensitive to sulfonamide.

Sulfanimide preparations are prescribed externally, inside, intramuscularly, subcutaneously and intravenously. Outwardly used in the form of ointments, linimes, powder.

For the most rational sulfanilamidotherapy, it is advisable to assign a mixture of two or three sulfanilaminamide preparations at the same time at a different absorption and removal rate. Good results gives the combined use of sulfonamide preparations with antibiotics, organic paints and other chemotherapeutic agents. In these cases, a smaller dose of the drug is required and the possibility of formation of sulfanimide-stable races of microorganisms is reduced.

Contraindications to the use of sulfonamide drugs Animal a bit: total acidosis, diseases of the hematopoietic system, hepatitis.

Sulfanimides of resorbative action

Short action preparations

Streptocid - Streptocidum. Para-aminobenzenesulfamide. Synonyms: ripped, streptocide white, streptamine, sulfanimide, streptozol, etc.

White crystalline powder without smell and taste. A little soluble in water (1: 170), easily - in boiling water, solutions of acids and alkalis; It is difficult to soluble in ethanol (1: 35). The aqueous solutions have a neutral reaction, very persistent (can be sterilized by fluid ferry or short boiling). Invisible with novocaine, anesthesia, barbiturates and other drugs, easy to split sulfur.

It has antimicrobial effect on Streptococcal, meningococci, pneumococci, intestinal wand, gas goggle causative agent and some other microbes, but almost inactive against staphylococci. The drug disrupts the Conduction exchange processes And inhibits the growth and reproduction of microorganisms.

Streptocid is quickly absorbed from the gastrointestinal tract, subcutaneous fiber and with a wound surface. It is especially well absorbed from the subtle intestinal department, somewhat worse - from the stomach and thick division of the intestine. When local use does not irritate the fabrics.

After oral application The maximum concentration of the drug in the blood is set in 0.5-3 hours and is held at about this level for 1-2 hours, and then decreases rather quickly. The prevailing drug easily penetrates through the internal barriers. It is found in all organs and tissues in sufficiently high concentrations. In the body, streptocid is associated with proteins up to 20% and is subjected to various transformations, including acetylation. The degree of acetylation in the blood is 20-25%, in the urine - 25-60%. Acetylation products do not have antimicrobial activity and are significantly worse dissolved in water. With a high concentration of the drug in the urine, they can fall into a precipitate. Streptocid is distinguished in free and related forms mainly by the kidneys (90-95%).

The toxicity of the drug is insignificant, but with long-term use in large doses in the kidneys, difficult soluble compounds can be formed, the hemoglobin content decreases, cyanosis, agranulocytosis, leukopenia occur. More sensitive to the preparation of young animals. Contraindications for the use of streptocide are as follows: general acidosis, hepatitis, hemolytic anemia, agranulocytosis, jade, nephrosis.

Streptocid is used in angina, streptococcal tonsillar abscesses, soe, bronchopneumonia, postpartum sepsis and other diseases. Doses inside: horses and catote 5-10 g, small cattle and pigs 0.5-2, dogs 0.5-1, sands and foxes 0.3-0.5 g. The drug is prescribed in the specified one-time doses 4 -6 times a day for 5-7 days. One-time doses Intravenously: horses and cattle 3-6, dogs 0.5-1 2-3 times a day. The externally streptocide is used to treat infected wounds, ulcers, burns in the form of powders, suspensions, liniment. Dressing is carried out after 1-2 days, since the pus and tissue decay products reduce the therapeutic effect of strepticide.

We are produced in the form of powder, tablets of 0.3 and 0.5 g, as well as in the form of 5-10% ointments, 5% suspension and 5% liniment.

Powder and pills of strepticide are stored by the list of B in a well-unpaved container. The term of check analysis is 10 years.

Ointment, suspension and streptocide liniment are stored in a cool, protected place in carefully closed packaging. When the browned film is appeared on the surface of the liniment, it should be removed, after which the line is suitable for use.

Streptocid soluble - Streptocidum Solubile. Para-sulfamido-benzene sodium benzene floor sulfate.

White crystalline powder. Soluble in water, practically insoluble on ether and chloroform. Aqueous solutions can be sterilized. Incompatible with Novocaine, anesthesia, barbiturates.

According to antphrimic crobal action, the streptocidum is similar. Due to good solubility in water is suitable for parenteral administration. The pharmacokinetics of the drug is similar to Pharmacid Pharmacokinetics.

Streptocide soluble in septic streptococcal processes, angina, soy, bronchopneumonia, mastitis, cystitis, pelitis. Prescribed intramuscularly and subcutaneously in the form of a 5% solution prepared on water for injection or isotonic sodium chloride solution. For intravenous administration, a 10% solution is prepared on a sodium chloride isotonic solution or a 1-5% glucose solution. Doses of intravenously: horses and catot 2-6 g, fine catot and pigs 1-2, dogs of 0.3-0.5 g. In mastitis in the affected share of udder after the surcharge, a 3-5% aqueous solution of the drug is introduced in a volume of 25-40 ml 2-3 times a day.

The soluble streptocid can be prescribed not only parenterally, but also inward, and also externally in the same doses as the streptocid.

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

Release soluble streptocid in powder. Store on the list b in a well-untapped container. The term of check analysis is 10 years.

Norsulfazol - Norsulfazolum. 2- (para-aminobenzenesulfamido) -Tiazol. Synonyms: Azosptal, pyrosulfophone, sulfatiasis, thiazamide, cybazole, etc.

White or slightly yellowish crystalline powder without smell, very little soluble in water (1: 2000), little - in ethanol, soluble in dilute inorganic acids, solutions of caustic and carbonic alkalis. Incompatible with novocaine, barbiturates, orthform.

Nisulfazole has a high antimicrobial activity against streptococci, meningococci, intestinal sticks, salmonella, Pastell and other microorganisms. This is one of the most active sulfonamide drugs, but higher doses are required to create bacteriostatic concentrations of it in the blood. Nisulfazole toxicity is higher than in streptocide, and can manifest itself after 7-9 days. After use in the form of hematurium and agranulocytosis.

The drug is easily absorbed from the gastrointestinal tract and reaches the maximum concentration in the blood after 3-6 hours after administration. The therapeutic concentration is held in the blood for 6-12 hours. It is binding to plasma proteins by 60-70%, as a result of which the penetration of the drug in organs and tissues is hampered and its elimination is slowed down. Acetylated slightly and stands out with urine mainly in free form.

Nisulfazole is used in catarrhal bronchopneumonia, pleurrites, streptococcal and staphylococcal sepsis, endometritis, mastitis, gastroenteritis, necrobacteriosis, diplococcal septicemia calves, pastellosis of birds and other bacterial infections. Prescribed inside 2-3 times a day in the following doses: horses and cattle 10-25 g, fine catot and pigs 2-5, a church of 0.5 g. The initial dose of norsulfazole must be 2 times higher.

Under the catarrhal bronchopneumonia, calves Nisulfazole is used intrahelectually at a dose of 0.05 g / kg of mass in the form of 8-10% solution for 3-4 days. It is advisable to simultaneously assign antibiotics. In diplococcal sepitsemia, the drug is administered intravenously at 0.01-0.02 g / kg of mass.

In the treatment of RAS, NURSULFAZOL is used in the form of powders and ointments in various combinations with penicillin, gramsicidine, iodine, as well as other sulfonamides. At the same time it is necessary to clean the wound from pus and necrotic tissues.

Contraindications for the use of Nisulfazol: jade, hepatitis, blood disease and hematopoietic system. During the prescription of the drug, the reception of water is not limited.

The norsulfazole is produced in powder and tablets of 0.25 and 0.5 g. Store with precaution on the list B in a well-visited container. The term of verification analysis is 5 years.

Norsulfazol-sodium - NORSULFAZOLUM-NATRIUM. 2- (para-aminobenzenesulfamido) -thiazol sodium. Synonyms: Nisulfazole soluble, sulfatiazol sodium.

Plate, shiny, colorless or with a slightly yellowish shade of the crystals without odor. Easily soluble in water (1: 2). The aqueous solutions have a strongly alkaline reaction, withstand sterilization at 100 ° C for 30 minutes.

The drug has the same chemotherapeutic activity as Nisulfazole. Due to the good solubility in water, it can be used not only inside, but also parenterally, as well as in the form of eye drops.

Indications for use are the same as for Nisulfazole. Used in septic processes when it is necessary to quickly create a high concentration of the drug in the blood, for example, in diplococcal septicemia of calves, necrobacteriosis, colibacteriosis, etc. Assigns norsulfazol-sodium mainly intravenously in the form of 5-15% solutions is injected slowly. Under the skin and intramuscularly, the preparation can be administered in solutions not higher than 0.5-1% concentration. Fit under the skin of faster solutions causes irritation of fabrics, up to necrosis. Doses of intravenously: horses 6-12 g, cattle 6-10, sheep 1-2, dogs 0.5-1 g 2 times a day for 3-4 days.

In the pastellosis of birds, Norsulfazol-sodium is used in the form of a 20% oil suspension or aqueous solution. The suspension is introduced once in the region of the upper third of the neck of chimes and ducks of 1 ml per 1 kg of bird weight. The aqueous solution is prepared immediately before use at the rate of 0.5 dry matter for chickens and 1 g for the intake on reception. The drug give a bird with feed 2 times a day. In coccidiosis, chickens are given with drinking water in the form of a 0.25% aqueous solution.

In the mastitis, the striking share of the udder is handed over and administered 3, 5 or 10% norsulfazole sodium solution through a milk catheter in a volume of 25-40 ml. Nipples clamp for 10-15 minutes. Treatment is carried out 1-2 times a day before recovery.

Contraindications to the use of Nisulfazol-sodium diseases of the hematopoietic system, jade, nephrosis.

Release in powder form. Store with precaution on the list b in packaging that protects moisture and light. The term of verification analysis is 3 years.

Etzol - Aethazolum. 2- (para-aminobenzenesulfamido) -5-ethyl-1,3,4-thiadiazole. Synonyms: Berfopen, Globucid, Setail, Sulphaetidiol, etc.

White or white with a slightly yellowish tint of powder without smell. Practically insoluble in water, difficult to soluble in ethanol, is not enough soluble in dilute acids, easily soluble in alkali solutions. Incompatible with pepton, para-aminobenzoic acid, novocaine, barbiturates, many sulfur derivatives.

Ethane has a high antimicrobial activity against streptococci, pneumococci, meningococci, pathogenic anaerobes, intestinal sticks, pathogens of dysentery, salmonellosis, Pastellosis, etc. Ethazol is superior to many sulfoniamides on antibacterial action against a variety of microorganisms.

The drug is quickly absorbed from the gastrointestinal tract in blood. After 2-3 hours in dogs and after 5-8 hours, the maximum concentration in the blood is noted in cattle. Ethane refers to short-acting sulfonamide drugs, in which the maximum level of concentration decreases by 50% in 5-10 hours. It penetrates well through the hematorecephalic barrier, it is unevenly distributed in various organs and tissues: longer is delayed in the kidneys, gastrointestinal tract, liver, lungs. In the body of dogs, the drug is not acetylated, and in other animals is subjected to acetylation to a small degree (5-10%), therefore its use does not lead to the formation of crystals in urinary tract. The ethazol is allocated to the most fast dogs, then rabbits and the most slowly - in cattle.

It is used for bronchopneumonia, angina, postpartum sepsis, endometritis, dysentery, dyspepsia, feel of pigs and other diseases of bacterial etiology, whose pathogens are sensitive to sulfonamide.

Doses inside: horses 10-25 g, cattle 15-25, small cattle 2-3, pigs 2-5, rabbits 1-1,5, bird 0.5, dogs 0.3-0.5 g 3 -4 times a day for 4-6 days. contract. In case of severe disease, the initial dose increases twice. Doses for youngsters make up 2 / s from a dose for an adult animal.

For the prevention of the wound infection, the ethasol is introduced into the cavity of the wound in the form of powder, 5% ointments. At the same time, the drug is prescribed inside.

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

We produce ethasol in the form of powder and tablets of 0.25 and 0.5 g. They are stored on the list B in a well-visited container. Test analysis period 3 years

Ethazol sodium - AETHAZOLUM-NATRIUM 2 (pair of aminobenzene-sulfamido) 5 ethyl 1.3,4 thiadiazole sodium. Synonyms: soluble ethazol, sodium sulphaetidol.

White crystalline powder. Easily soluble in water; It is difficult to soluble in ethanol. The aqueous solutions are stable, can be sterilized with boiling for 30 minutes. Incompatible to novocaine, anesthesia, preparations, easily swinging sulfur.

Ethane sodium is easily absorbed at different ways of administration, quickly achieves the maximum level of blood concentration and actively penetrates various organs and tissues. Due to good solubility in water, it can be used not only inside, but intramuscularly and intravenously. In the body circulates mainly in free form, it is highlighted quickly.

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

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

Contraindications to the use of etazol-sodium are the same as for the ethassol.

Ethane sodium is released in powder, as well as in ampoules 3 in the form of a 10-20% solution for injections.

Store with precaution on the list B in a place protected from light. The term of verification analysis is 5 years.

Sulfacyl - Sulfacylum. Para-aminobenzenesulfacetamide. Synonyms: acetocide, acetosulfamine, albucid, septuron, sulaud, sulfacetamide, etc.

White or white with a yellowish tint crystalline odor powder, soluble in 20 parts of cold water (in hot water dissolves much easier), in 12 parts of ethanol, in alkali solutions and acids. Incompatible with novocaine, anesthesia, preparations, sulfur swings.

Sulfacyl has a strong antimicrobial effect on streptococci, staphylococcal, pneumococci, salmonellosis pathogens and colibacteriosis.

The drug is quickly absorbed from the gastrointestinal tract of animals. The maximum concentration in the blood is set after 2-5 hours from the moment of administration. For 6-12 hours, the maximum concentration is reduced by 50%. Acetylated to moderate degree (10-15%). Slightly binds to plasma proteins, well penetrates various organs and fabrics. Relatively quickly allocated from the body, mainly with urine.

Apply with angina, pharyngitis, bronchopneumonia, postpartum sepsis, streptococcal infections, colibacteriosis, salmonellosis, dyspepsia, cystitis, etc., are deposited in the form of powder and ointments in the treatment of purulent wounds, skin streptococcal and staphylococcal diseases, dose conjunctivitis inside: horses 5-10 g, small cattle 2-3, pigs 1 -2, dogs 0.5-1 g 3-4 times a day. The initial dose must be 2-3 times the following.

Contraindications for use are similar to other sulfanimamides.

Release sulphacyl in powder. Store according to the list b in a well-baked container protecting against the action of light. The term of verification analysis is 5 years.

Sulfacyl sodium - Sulfacylum-Natrium. Para-aminoben-clastulfacetamide sodium - sodium salt sulfacyl. Synonyms: soluble sulphacyl, sulfacetamide sodium, albucid sodium, etc.

White crystalline powder without smell. Easy to soluble in water, practically insoluble in ethanol, ether. Incompatibility - similar to other sulfonamides.

According to the antimicrobial action and the peculiarities of pharmacokinetics, it is similar to sulfacyl.

Apply with pylits, cystitis, colitis and postpartum sepsis. Assigns in doses: horses and catote 3-10 g, small catot and pigs 1-2, dogs 0.3-0.5 g 3-4 times a day.

Outward sulfacyl sodium is used in the treatment of wounds, cornea, conjunctivitis, mastitis, endometritis. Use in the form of powders, ointments or solutions of 10, 20 or 30% concentration. Especially good results were obtained when using sulphacyl sodium in the eye practice.

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

Released in powder. Store on the list b in packaging that protects against the action of light and moisture. The term of verification analysis is 5 years.

Sulfantrol. - Sulfanthrolum. 2- (para-aminobenzenesulfa-mydo) -benzoate, hydrate.

White or white with a yellowish or pink crystalline powder, well soluble in water (1: 8), difficult to soluble in ethanol. Aqueous solutions are resistant, they are sterilized with boiling for 15 minutes. Incompatible with drugs, easy to split sulfur, novocaine, anesthesia, barbiturates.

Sulfantrol is active with respect to streptococci, pneumococci and intestinal sticks. The drug is high toxic for nuttal.

Used with nuttaliosis and piroplasmosis of horses, tayyluriosis of cattle, bronchopneumonia, salmonellosis, colibacteriosis, peg of bees and other diseases. Under the nuttaliosis of horses, the sulfantrol is prescribed 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 mass. The drug is administered 1-3 times with an interval of 24-38 hours. In case of horses, a mixture of 4% solution of sulfantrol and a 1% solution of tripan blue is used for horses. Input intravenously at a dose of 0.5 ml per 1 kg of animal mass 1-2 times with an interval of 24-48 hours.

With teylerium of cattle, sulfantrol is prescribed intramuscularly in the form of a 10% solution at the rate of 0.003 g per 1 kg of the mass of the animal.

In bronchopneumonia, the drug is injected intramuscularly and intravenously at a dose of 0.008-0.01 g per 1 kg of mass of the animal. With colibacteriosis, salmonellosis and other gastrointestinal diseases, sulfantrol are prescribed inside on the first day 0.2 g, in the second - 0.15, in the third - 0.1 and fourth - 0.05 g per 1 kg of animal mass per day. Daily dose gives 3-4 receptions.

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

Contraindications for the use of sulfantrogen: agranulocytosis, acute hepatitis, jade and nephrosis

Released in powder. Store with precaution on the list B in a well-visited container protecting from light and moisture. The term of verification analysis is 8 years.

Sulfadimesin - Sulfadimezinum. 2- (para-aminobenzene-sulfamido) -4,6-dimethylpyrimidine. Synonyms: diazyl, diazole, dimethazyl, dimethyl sulfadiazine, dimethyl sulphapyrimidine, supersptil, etc.

White or slightly yellow-eyed smelling powder. Practically insoluble in water, ether and chloroform, are not soluble in ethanol, easily soluble in divorced mineral acids and alkalis. Invisible with novocaine, para-aminobenzoic acid, pepton, barbiturates.

It has a wide antibacterial spectrum of action: active in relation to pneumococci, staphylococcal, intestinal wand, salmonellam, passellam, as well as large viruses. The activity is close to sulfazine and methylsulfazine. Bacteriostatically acts, disrupts the flow of metabolic processes, inhibits the growth and reproduction of microbes.

Sulfadimesin is relatively quickly absorbed from the gastrointestinal tract. The maximum concentration of the drug in the blood is set 6-8 hours after administration. In the blood of animals, it creates higher concentrations than any other. Of the usually used sulfonamides, in the same dose. The drug penetrates well through the hematorecephalic barrier, creates high concentrations in many organs and tissues. It binds to proteins by 75-85%, acetylated in the blood is 5-10%, the urine is 20-30%. Sulfadimezin acetylation products dissolve better than the free form of the drug. It allocated from the body slowly, mainly by the kidneys. Due to the relatively low rate of elimination, it is more safe as compared with Nurphazole and other rapidly released drugs. Slow selection provides long-term (more than 8 hours) maintaining the therapeutic level in the blood. The drug is well tolerated animals.

Sulfadimezin is used for pneumonia, catarrhal bronchopneumonia, bronchitis, laryngitis, angina, soy horses, sepsis, endometritis, infectious mastitis, necrobacteriosis of sheep and reindeer, dyspepsia, gastroenteritis, urinary tract, salmonellosis infections, pastellosis, respiratory mycoplasmosis, bird coccidiosis, and other diseases . Assign inside in doses: horses 10-25 g, cattle 15-20, small cattle 2-3, pigs 1-2, quarrels 0.3-0.5 g 1-2 times a day. The initial dose must be increased by 2 times

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

With pastellosis, sulfadimezin birds are used with feed at the rate of 0.05 g per 1 kg of mass of animal 1-3 times a day for 2-4 days.

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

Contraindications for the use of sulfadinezin disease of the hematopoietic system, jade, nephrosis, hepatitis. With long-term therapy, it is necessary to conduct blood tests.

Sulfadimezin is produced in powder and tablets of 0.25 and 0.5 g. They store on the list B in a place protected from light in a well-visited container. The term of check analysis is 10 years.

Urosulfan - Urosulfanum. Para-aminobenzenesulfopyl urea. Synonyms: sulfakarbamide, sulfonylcarbamide, uramis, etc.

White crystalline powder without smell, sour taste. Little soluble in water, it is difficult to soluble in ethanol, easily soluble in diluted acids and solutions of caustic alkalis. Invisible with preparations, swing sulfur, novocaine, anesthesia, barbiturates.

Wrosulfan has a high antibacterial activity in relation to staphylococci and intestinal wands.

The drug is quickly absorbed from the gastrointestinal tract, which ensures the creation of high concentrations in the blood. The maximum concentration is set after 1-3 hours from the moment of administration. Wrosulfan is slightly acetylated, circulates and stands out mainly in free, form. Fast allocation 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 the infections of the urinary tract. Wrosulfan is small-toxic, deposits in urinary tract is not marked.

Used in colibacterial and staphylococcal diseases: cystitis, pylits, infected with hydraidonphrosis, as well as other urinary tract infections. It is especially effective to use Wrosulfana with pylitis and cystitis without violation of the urinary. Prescribed in doses of horses 10-30 g, cattle 10-35, a small cattle 2-5, 2-4 pigs, pigs, 1-2 g 3-4 times a day for at least four days in a row. For intravenous injections, soluble Urosulfan is used in form 5, 10 and 20% solutions at a dose of 0.02-0.03 g per 1 kg of animal mass 1-2 times a day. IN bladder 25% solution is introduced.

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

They are produced in powder and tablets of 0.5 g. Store with precaution on the list B in a well-visited container. The term of verification analysis of 2.5 years.

Medium duration drugs

Sulfayen. - Sulfazinum. 2- (pair of aminobenzenesulfamido) -pyrimidine synonyms, adiazine, debedal, sulfadiazine, pyrimal, sulfapyrimidine, etc.

White or yellow powder without smell. Practically insoluble in water, soluble in ethanol, alkali solutions and mineral acids.

It has antibacterial activity in relation to streptococci, staphylococci, pneumococcal, meningococci, intestinal wand and other gram-positive and gram-negative bacteria. The antibacterial activity in vivo is superior to Nisulfazole, streptocid and some other sulfonilamide drugs.

Sulfazine is absorbed from the gastrointestinal tract relatively slowly, the maximum concentration of the preparation in the blood is set after 4-6 hours. Sulfazine is less binding to plasma proteins and is slowed down from the body than norsulfazole, which provides a higher concentration of the drug in blood and organs. Acetylated slightly (5-10%), acetylation products are well soluble in water and urine.

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

The drug relatively rarely causes disruption of the functions 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 reinforced diuresis (abundant alkaline drink)

Contraindications for use, jade, nephrosis

They are produced in powder and tablets of 0.5 g. Store on the list B in a well-unpaved container. The term of test analysis is 7 years.

Durable preparations

Sulfapyridazin - Sulfapyridazmum. 6 (para-aminobenzenesulfamido) 3 methoxypyridazine synonyms Aseptilex, depletion, deposit, durasulf, kines, Lederkin, Longisulf, Novosulfin, Kvosteptyl, Retasulfine, spoadazin, sulfamethoxypyridazine, etc.

Light yellow crystalline powder without smell, bitter taste. Few soluble in cold water, somewhat better in hot (1: 70). It is well soluble in diluted acids and alkalis.

Sulfapyridazine is active with respect to many gram-negative microorganisms. The power of the bacteriostatic action is equal to or somewhat inferior to the etazol and sulfazine. There is a high sensitivity to the preparation of streptococci, staphylococci, intestinal sticks, Pastell and some proto strains. Microorganisms resistant to other sulfanimamides are resistant to pyridazine sulfa.

The drug refers to long-term sulfonamides. Quickly absorbed from the gastrointestinal tract and creates a high level of concentration in the blood, organs and tissues, which is preserved in the body for a long time. The maximum concentration of the drug in cattle and sheep is installed in 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 held for 24-48 hours. Sulfapyridazine is intensively associated with plasma proteins (70-95%) and reabsorbed to a high degree (80-90%) in distal departments renal tubules. The drug penetrates well into various organs and fabrics. The greatest amount is accumulated in the kidneys, the liver, the walls of the stomach and intestines, the lungs.

Sulfapyridazine in the body of animals is slightly exposed to the process of acetylation. The content of acetoproducts in the blood is 5-15%. Acetylated derivatives do not have antimicrobial effects.

From the body, the drug is distinguished by the kidneys in a free and acetylated form. Due to the high degree of reabsorption of the free form in the renal tubules, the content of acetylated products in the urine reaches 60-80%. Sulfopyridazine acetoproducts solubility in the urine is good.

The drug is used for various diseases of the respiratory tract of young animals, gastrointestinal diseases of different etiologies (gastroenteritis, dyspepsia, dysentery, coccidiosis), salmonellosis, colibacteriosis, pastellosis, in respiratory mycoplasmosis and pullorosis-typhoid bird, with postpartum sepsis, endometritis, mastitis, infections Urinary tract and gallbladder, for the prevention of postoperative infections. Doses inside by 1 kg of animal mass: a cattle 50-75 mg, piglets 75-100, dogs 25-30, 90-120 kras, rabbits 250-500 mg 1 time per day. The initial dose must be 1.5-2 times more of the specified supportive doses.

With a pastellosis of chickens, sulphapyridazine with therapeutic goal is prescribed in doses of 200 mg (initial) and 150 mg (maintaining) per 1 kg of mass with a 24-hour interval between the introductions. The drug can be prescribed by a group method with feed.

In order to prevent the undesirable influence of sulfapyridazine, animals should be assigned abundant alkaline drink.

Contraindications for use: diseases of the hematopoietic system, kidneys, liver, pronounced toxicallergic reactions.

We are produced in powder and tablets of 0.5 g. Store with precaution on the list B in a tightly unpaid container in light-protected place. The term of the test analysis is 2 years.

Sulfapyridazin sodium - Sulfapyridazinum-Natrium. (para-aminobenzenesulfamido) -3-methoxypyridazine sodium.

White or white with yellowish green tint crystalline powder. Easy to soluble in water, difficult - in ethanol. Gradually yellow under the action of light. Aqueous solutions can be sterilized at 100 ° C for 30 minutes.

By antibacterial spectrum Similar sulfapyridazine.

Apply with severe bronchopneumonias, salmonellosis, Pastellosis, pigs, postpartum sepsis, endometritis and other infectious diseases. Prescribed intravenously or intramuscularly in the form of 5%. or 10% solution. Doses of intravenously per 1 kg of animal mass: a cattle 25-50 mg, a small cattle 50-75 mg 1 time per day.

With a local purulent infection, the drug is used for irrigation of wounds in the form of dressings and tampons, moistened with 5-10% solution. Sulfapyridazine sodium solutions can be prepared on distilled water, an isotonic solution of sodium chloride or on a 2-5% polyvinyl alcohol solution. In mastitis, endometritis solutions are injected into the uterus and milk gland. When local purpose can be combined with the purpose of sulfapyridazine inside.

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

They are produced in powder and in the form of a 10% solution on a 7% polyvinyl alcohol in bottles of 10 and 100 ml. Store on the list b in a dry, protected from light place. The term of verification analysis is 3 years.

Sulfadimetoxin - Sulfadimethoxinum. 6- (para-aminobenzenesulfamido) -2,6-dimethoxypyrimidine. Synonyms: depot-sulfamide, Madribon, Madroxin, Superfa, Ultrasulfan, etc.

White crystalline powder without taste and smell. Multulatory in water and ethanol, soluble in dilute acids and alkalis.

Sulfadimetoxin has a wide range of antimicrobial action. Meningococci, streptococci, staphylococci, various stamps of intestinal sticks, Shigella, and protein, are most sensitive to it. Most of the strains of the blue chopstick, layeries, some strains of pneumococcus are stable. Significant fluctuations in the sensitivity of strains to the drug within the same species are noted.

Sulfadimetoxin refers to long-term sulfanimides. It is relatively quickly absorbed from the joy-daily intestinal tract into blood, but the absorption intensity is somewhat lower than that of sulphapyridazine. The maximum concentration in the blood of cattle is mounted after 8-12 hours, sheep and goats - 5-8, pigs and dogs - 2-5, chickens - after 3-5 hours from the moment of administration. The concentration of the drug in the blood is reduced significantly slower than the concentration of sulfapyridazine. The therapeutic level is held for 24-48 hours. Sulfadimetoxin is somewhat worse than sulfapyridazine and sulfonimetoxin penetrates various organs and tissues. The exception is bile, where the concentration of the drug may exceed its blood content of 1.5-4 times.

Sulfadimimetoxin in the blood is very large to be associated with plasma proteins (90-98%). According to the intensity of binding with plasma proteins, animals can be positioned in the following (descending) order: dogs, cattle, rabbits, rats. Acetyl production is present in the blood in minor quantities (0-15%).

Sulfadimetoxin is derived from the body very slowly, primarily due to a large (93-97%) reabsorption in the channel of the free form of the drug, as well as due to a significant degree of binding to proteins. Acetyl form is displayed 2 times faster. In the urine, sulfadimetoxin is mainly present in the form of a glucuronide, which is well soluble in an acidic environment, which practically eliminates the possibility of crystallurium development.

The drug is little toxic for animals, has a large latitude of therapeutic action. Used with broncho-pneumody of young animals, with nasopharynx infections, acute form Dysentery, Pastellosis, Cocidize, Gastroenteritis, colitis, cystitis and other diseases. Sulfadimetoxin is prescribed inside in doses per 1 kg of animal mass: a cattle 50-60 mg, a small cattle 75-100, 50-100 pigs, 50-25 dogs, rabbits 250-500, 95-100 mg 95 times a day . The initial dose should be 2 times more of the specified supportive doses.

In case of pastellosis, sulfadimetoxin is prescribed with therapeutic goal in doses of 200 mg (initial) and 100 mg (supporting) per 1 kg of mass. With a prophylactic goal, doses of 100 mg (initial) and 50 mg - (supporting) are used 1 time per day. The drug can be used by the group method with food.

In order to prevent the undesirable influence of the drug, the patient animal is recommended to assign abundant drinking. Sulfadimetoxin is contraindicated in toxicallergic reactions, diseases of the hematopoietic system, kidneys, acute hepatitis.

We are produced in powder and tablets of 0.5 g. Store with precaution on the list B in a well-untapped container in light-protected place. The term of verification analysis is 4 years.

Sulfamonetoxin - Sulfamonomethoxinum. 6- (para-aminobenzenesulfamido) -6-methoxypyrimidine. Synonyms: Diameters, DS-36.

White or white with yellowish tint crystalline powder. Not enough soluble in water, better - in ethanol, easily soluble in diluted mineral acids and aqueous solutions of caustic alkalis. Incompatible with novocaine, barbiturates, preparations, easy to split sulfur.

Sulfamimetoxin has high antibacterial activity against streptococcal, meningococci, pastelal, intestinal sticks, toxoplasm, chopsticks of dysentery and other microorganisms. The drug has not only high bacteriostatic effect in vitro, but also has exceptionally high chemotherapeutic activity in animal experiment. In case of infections caused by streptococci, staphylococci, salmonella, exceeds the activity of sulfapyridazine and sulfadimetoxin.

The drug refers to long-term sulfonamides. Well and quickly absorbed from the gastrointestinal tract in blood. The maximum concentration in the blood is established in cattle in 5-8 h, sheep and goats - after 3-5, pigs - 2-5, dogs - 1-3, chickens - 2-5 hours from the moment of administration. The concentration of sulfonometoxin in the blood is reduced somewhat faster than with the introduction of sulfapiri-lazine and sulfadimetoxin. The drug quite well diffuses into organs and fabrics. Higher concentrations stop in the kidneys, lungs, liver. Well penetrates through the hematostephalic barrier. In the blood, intensively binds to proteins (64.6-92.5%), but the forming communication is continuing. Acetyl blood production reaches 5-14%, in the urine 50-67%. Excaped from the body slowly and mainly by the kidneys. The urine contains 50-70% acetyl derivative, 20-30% glucuronide and 10-20% free drug. Acetyl shape of sulfamonetoxin is more soluble than free.

Used in respiratory tract infections, purulent ear, throat, nose, nose, dysentery, enterocolites, infections of bile and urinary tract, purulent meningitis. The drug is given inwards in doses per 1 kg of animal mass, a cattle 50-100 mg, a small cattle 75- 100, a pig of 50-100, 25-50 dogs, rabbits 250-500, 100 mg quarrels 1 times a day. The initial dose must be enlarged twice.

Sulfamonometoxin is contraindicated with increased sensitivity to sulfonamide drugs, with hemolytic anemia, agranulocytosis, acute hepatitis, jade.

We are produced in powder and tablets of 0.5 g. Store on the list B in a well-untapped container in a dark place. The term of verification analysis is 3 years.

Sulfalen - Sulfalenum. 2- (para-aminobenzenesulfamido) -3-methoxypirazine. Synonyms: Kelfizin, sulfametopirazine, sulfamethoxypirazine, sulfapirazinmetoxin.

White crystalline powder. Little soluble in water, easily soluble in alkalis solutions. Incompatible with novocaine, barbiturates, preparations, easy to split sulfur.

According to the antibacterial spectrum of the action close to other sulfanilamide drugs.

Sulfalen refers to superclocking sulfonamides. Quickly absorbed, and the maximum concentration in the blood is set after 4-6 hours of therapeutic concentrations in the body of animals and birds can be kept in the liver 3-5 days. Displays from the body very slowly. Well tolerated animals.

Used with bronchopneumonia of young, colibacteriosis, salmonellosis, pastellosis, toxoplasiasis, respiratory mycoplasmosis, as well as urethritis, mastitis and other diseases. They are prescribed inside in doses per 1 kg of mass of the animal - calves of milking milks 20-25 mg, piglets of sausages 40-50, 90-150 mg, 1 time per day, are re-introduced in 5-7 days. In case of severe disease, the drug is prescribed again after 3-4 days. The duration of treatment is at least 10-12 days.

At bronchopneumonia, calves 2-3-month-old sulfalin is prescribed inside 50 mg (initial dose), and then daily by 20 mg (supporting dose) for 7-10 days. At the same time, it is recommended to introduce vitamin preparations (groups A, B and C), as well as carry out intense symptomatic therapy.

With colibacteriosis and salmonellosis, the pins up to 2-4 months of sulfalen are prescribed 1 time per day at the rate of 1 kg of animal mass: on the first day 100 mg, in the following - 20 mg.

Possible side effects and measures of their prevention are the same as when using other prolonged sulfonamides.

Produced in powder and tablets of 0.2, 0.5 and 2 g; In bottles of 60 ml of a 5% suspension. Store on the list b in a well-untapped container. The term of verification analysis is 5 years.

Salazopyridazin - Salazopyridazinum. 5-Napa- / N- (3-MetalSyppyridazinyl-6) -Sulfamido / -Phenylazosalicylic acid.

Yellowish-orange fine crystalline powder without taste and smell. Virtually insoluble in water, soluble in alkalis and hydrocarbonate solutions. Obtained as a result of the azosochetation of sulphapyridazine (65%) and salicylic acid.

The antimicrobial effect of salazopyridazine is manifested only after its splitting in the gastrointestinal tract with the release of free sulphapyridazine and 5-aminos-licyl acid. The therapeutic effect of the drug is determined primarily by the ability of Salazosulfanili-Dov to accumulate in the connecting tissue of the large intestine and provide direct action on the inflammatory process. Salazopyridazine metabolic products are antibacterial, anti-inflammatory and immunosuppressive. Salazopyridazine is more active than salasopyridine, however, by the degree of chemotherapeutic action, sulphapyridazin is inferior,

As the drug splits, the liberated sulfapyridazine is gradually absorbed and reaches the 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 is long held on therapeutic and subterapeutic levels. The drug is small toxic. With prolonged purpose for 30-40 days. Does not cause changes from blood and urine.

Recommended for the treatment of animals, patients with various forms of colitis, enterocolites and with the same testimony as sulfapyridazine. Doses inside the young farm animals of 25-50 mg per 1 kg of mass 2 times a day.

When using salazopyridazine, side effects are possible, observed sometimes when using sulfanimamides and salicylic acid: allergic reactions, leukopenia, dyspeptic disorders when occurring adverse Reactions Daily dose should be reduced or cancel the preparation of salazopyridazip is contraindicated in the presence of pronounced toxicallergic reactions to sulfanimamides.

We are produced in powder, tablets of 0.5 g and in the form of a 5% suspension. Store in a tightly visited container in the place protected from light. The term of verification analysis is 5 years.

Salazodimetoxin - Salazodimethoxinum. 5-Napa- / N- (2,4-dimethoxypyrimidinyl-6) - sulfonamido / -phenylase-salicylic acid.

Orange powder without taste and smell. We are insoluble in water, soluble in aqueous solutions of alkalis and hydrocarbonates. Salazodimetoxin is a product of azosochetation of sulfadimetoxin (67.5%) and salicylic acid.

The mechanism of action, pharmacokinetics, indications and contraindications, the scheme of application of salazodimetoxin is similar to that of such a salasopyridazine.

We are produced in powder and tablets of 0.5 g. Store on the list b in tightly closed packaging in a light place protected. The term of the test analysis is 2 years.

Sulfanimonds, poorly absorbed from the gastrointestinal tract

Sulgin - Sulginum. Para-aminobenzenesulfoguanidine. Synonyms of Abiguanil, Aseptilguanidine, Ganidan, Neo-Sulfonamide, Sulfaguanidine, etc.

White crystalline powder without smell. Very little soluble in water, in divorced mineral acids (hydrochloric, nitric), is not enough soluble in ethanol. Incompatible with novocaine, anesthesia, barbiturates, with preparations that swipe sulfur.

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

The drug is slowly and in small quantities is absorbed from the gastrointestinal tract. Its main mass is delayed in the intestine and creates a high concentration there. In the body of animals, Sulgin is moderately acetylated, it is highlighted mainly with feces. The large concentration of the drug in the digestive tract provides an effective impact on the intestinal microflora.

Used with bacillomic dysentery, colitis, enterocolitis, for prophylaxis postoperative complications In the intestinal operations. Prescribed in doses of horses 19-20 g, cattle 15-25, small cattle 2-5, pigs 1-5, calves of milks 2-3, piglets of Sosnes 0.3-0.5, Curass 0,2- 0.3 g 2 times a day. The initial dose must be twice as many indicated supporting doses.

To prevent the loss of the crystals of acetylated sulgin in the kidneys, it is necessary to assign abundant drink.

Contraindications to use increased sensitivity to sulfanimamides, diseases of blood-forming organs, acute hepatitis and jade,

They are produced in powder and tablets of 0.5 g. Store with precaution on the list B in a well-visited container. The term of verification analysis is 5 years.

Phthalazol. - Phthalazolum. 2-pair- (ortho-carboxybenzami-up) -benzolsulfamidiazole synonyms: sulfateydine, talazole, talazone, talledron, thalidine, talicyl, talisulfazole, phthalsulfatiazole

White or white with a slightly yellowish tint of powder. Practically insoluble in water, ether and chloroform; very little soluble in ethanol; soluble B. aqueous solution Sodium carbonate, easily soluble in an aqueous solution of caustic soda. Incompatible with novocaine, anesthesia, preparations, sulfur swings.

It has antimicrobial activity in relation to the causative agent of dysentery, salmonellosis, enteropathogenic stamps of intestinal sticks and some other bacteria. The mechanism of antimicrobial effect of phthalazole, as well as other sulfonamides, is a violation of the process of assimilation by the microbial cell "growth factors" - folic acid and substances close to it, which include para-aminobenzoic acid

Phthalazol is very slow and in minor quantities is absorbed from the gastrointestinal tract, as a result of which the therapeutic concentration is practically not created in the blood. The bulk of the drug is delayed in the gastrointestinal tract, where the clarification of the active (sulfanilamide) part of the phthalazole molecule is gradually occurs. The high concentration of phthalazole in the digestive tract ensures its effective impact on the intestinal microflora. The drug is low toxicity, well tolerated by animals.

Applied with dysentery, gastroenteritis, colitis, dyspeption of newborns, coccidiosis. Assign in doses: 10-r5 g horses, cattle 10-20, small cattle 2-5, pigs 1-3, dogs 0.5-1, chirma 0.1-0.2 g 2 times a day . The initial dose can be twice as follows.

Side phenomena phthalazole does not usually cause. Contraindication - increased sensitivity of animals to sulfanilaminamide drugs

They are produced in powder and tablets of 0.5 g. Store on the list B in a well-unpaved container. The term of check analysis is 10 years.

Disoulomba - Disulformmum. 1,4-sulfonyl-sulfonilamide)

White or slightly yellowish finely crystalline powder. Imprinable in water and diluted mineral acids, well soluble in solutions of caustic and carbonic alkalis. When heating with water is hydrolyzed with formaldehyde, incompatible with heavy metal salts, novocaine, anesthesia, barbiturates and preparations, easy to split sulfur

Disoulomba has antibacterial activity with respect to intestinal sticks, pathogens of dysentery, salmonellosis, colibacteriosis. It has a bacteriostatic action - violates the metabolism, inhibits the growth and reproduction of microbes.

The drug is slowly absorbed from the gastrointestinal tract and does not create high blood concentrations its main mass is delayed in the intestine, where under the influence alkaline environment Disulfinum hydrolysis occurs with sulfanimide (disulfan) and formaldehyde. As a result of a high concentration of the drug in the digestive tract in combination with the activity of disulfan and formaldehyde against intestinal microflora is effective in intestinal infections.

Applied with bacillomic dysentery, gastroenteritis of salinelese etiology, acute colitis and enterocolites. Prescribed inwards in doses: 5-10 g horses, cattle 10-15, calves of milks 2-4, 9-0.3 g 2-3 times a day.

Contraindications for use Increased sensitivity of animals to sulfanyamides, acute hepatitis, jade, nephrosis, agranulocytosis

We are produced in powder and tablets of 0.5 and 1 g. They are stored according to the list B in a well-visited container that protects against the action of light. The term of verification analysis is 5 years

Ftratain 3-methoxypyridazine (pair of phthalminobenzoylsulfanimide)

White or white with a slightly yellowish tint crystalline powder without smell. Practically insoluble in water and ethanol. Easily soluble in alkali and sodium bicarbonate solutions. On the chemical structure is close, on the one hand, phthalazol, and on the other - sulphapyridazin

Ftaine has a wide antibacterial spectrum of action, active in relation to pneumococci, staphylococcus, streptococci, intestinal sticks, salmonella, pastell, pathogens of dysentery and other microorganisms. According to the antibacterial spectrum is close to sulfapyridazin. Bacteriostatically acts - disrupts the metabolism, processes of growth and reproduction of microbial cells. Bacteriostatic phthazine concentrations are 30-300 times higher than sulfapyridazine and 2-5 times lower than phthalazol.

Slowly absorbed from the gastrointestinal tract. In the intestine, gradually splits with the release of free sulfapyridazine, which is absorbed as it is absorbed. Due to the slow cleavage of sulphapyridazine in the intestine, a high concentration of the drug is maintained, which provides good efficacy in the treatment of gastrointestinal diseases Sulfapyridazine, it creates significant blood concentrations and has a resortive effect, which is very important in severe forms of dysentery and other gastrointestinal diseases. Displays from the body slowly.

Phthazin is well tolerated by animals, does not cause noticeable violations in general condition Even in cases where the dose is greater than therapeutic.

Apply with therapeutic and prophylactic targets in dysentery, dyspeption of newborns, enterocolites, colitis, coccidiosis The main advantage of the drug is smaller toxicity and a longer stay in the body. Prescribed individually or group method with feed 2 times a day dose per 1 kg of animal mass: a large and small cattle 10-15 mg, calves and lambs 15-20, pigs 8-12, piglets 12-16, chickens 30-50 mg . The initial dose increases 1.5-2 times. In the treatment of cocidiosis, chickens are recommended to use a mixture of phtrugen with neomycin in doses: 100-150 mg of phthazine and 500-750 μg of neomycin on chicken 2 times for 6-7 days.

For the prevention of phthazin diseases are prescribed in half of the dimensions of the dimensions 2 times a day for 4-5 days.

Contraindications for use: Increased sensitivity of animals to sulfanyamides, diseases of blood-forming organs, acute hepatitis, jade, nephrosis.

They are produced in powder and tablets of 0.5 g. They are stored according to the list B in a well-visited container that protects against the action of light and moisture. The term of the test analysis is 2 years.