Sulfonamides and sulfonamides. How sulfa drugs work.

ANTRIMA (Antrima)

pharmachologic effect. Combined sulfa drug. Sulfadiazine and trimethoprim have a bacteriostatic (preventing the growth of bacteria) and bactericidal (destroying bacteria) action, in combination, their antimicrobial effect is enhanced. Highly sensitive to the drug: E. coli, Klebsiella, Enterobacter, Proteus, Citrobacter, Salmonella, Shigella, Haemophilus, Vibriocholerae, Listeria, Pneu-mocystiscarinii.

Indications for use. Bacterial infections caused by microorganisms sensitive to the drug, including infections respiratory tract, infections urinary tract, infections gastrointestinal tract (especially typhoid fever).

Method of administration and dosage. Before prescribing a drug to a patient, it is advisable to determine the sensitivity of the microflora to it that caused the disease in this patient. Adults are prescribed 1 tablet 2 times a day with meals. For children, the drug is usually prescribed in the form of a suspension (suspension of solid particles of the drug in a liquid) - 1 attached measuring spoon (2.5 ml) per 5 kg of body weight 2 times a day with meals. The maximum daily dose is 8 scoops. For patients with creatinine clearance (the rate of blood cleansing from the end product of nitrogen metabolism - creatinine) from 30 to 15 ml / min, the drug is prescribed only in the case of hemodialysis (blood purification method), once a day.

In the case of prolonged treatment with the drug, systematic monitoring of the peripheral blood picture, kidney and liver function is necessary. In the case of using the drug in patients with diabetes mellitus it should be borne in mind that 2.5 ml of the drug contains 1 g of sucrose.

Side effect. Nausea, abdominal pain, thrombocytopenia (decrease in the number of platelets in the blood),

neutropenia (a decrease in the number of neutrophils in the blood), allergic reactions.

Contraindications. Deficiency of the enzyme glucose-6-phosphate dehydrogenase in erythrocytes (risk of increased hemolysis / destruction of erythrocytes /); pregnancy, breastfeeding; hypersensitivity to the components of the drug. The drug is not prescribed for premature and newborn babies.

Release form. Tablets containing 0.4 g of sulphadiazine and 0.08 g of trimethoprim; oral suspension for Children (2.5 ml - 0.1 g of sulfadiazine and 0.02 g of trimethoprim) in 50 ml vials.

Storage conditions. List B. In a cool, dry, dark place.

BISEPTOL (Biseptol)

Synonyms: Bactrim, Septrin, Abacin, Abaktrim, Andoprim, Bacterial, Bacticel, Bactifer, Bactramine, Bactramel, Bactrizol, Berlocid, Hemitrin, Doktonil, Ectapprim, Expectrin, Falprin, Gantrin, Infektrim, Metomid, Microcetimrad, Nola "Psakt" Potecept, Primazol, Resprim, Septocid, Sumetrolim, Trimexazole, Trixazole, Uroxen, Vanadil, Aposulfatrin, Bactekod, Bactreduct, Blekson, Groseptol, Kotribene, Cotrim, Cotrimol, Eriprim, Applied, Rancotrim, Sulfatrim, Exprimazol Sinersul, Cotrimaxol, Cotrimaxazole, Sulotrim, Trimosul, etc.

Combined preparation containing two active ingredients: sulfanilamide preparation sulfamethoxazole and a diaminopyrimidine derivative - trimethoprim.

Pharmachologic effect. The combination of these two drugs, each of which has a bacteriostatic (inhibiting the growth of bacteria) effect, provides a high bactericidal (destroying

bacteria) activity against gram-positive and gram-negative microorganisms, including bacteria resistant to sulfa drugs.

The bactericidal effect is associated with the double blocking effect of bactrim on the metabolism (metabolism) of bacteria. Sulfamethoxazole disrupts the biosynthesis of dihydro folic acid, and trimethoprim blocks the next stage of metabolism - the reduction of dihydrofolic acid to tetrahydrofolic acid, which is necessary for the development of microorganisms. The choice of sulfamethoxazole as a component of bactrim is due to the fact that it has the same elimination rate (elimination rate) with trimethoprim.

The drug is effective against streptococci, staphylococci, pneumococci, dysentery sticks, typhoid fever, colibacillus, protea; ineffective against mycobacterium tuberculosis, spirochetes, Pseudomonas aeruginosa.

The drug is rapidly absorbed when taken orally. The maximum concentration in the blood is observed 1-3 hours after ingestion and lasts for 7 hours. High concentrations are created in the lungs and kidneys. It is excreted in significant quantities in the urine (within 24 hours, 40-50% of trimethoprim and about 60% of sulfamethoxazole are excreted, mainly in the acetylated form).

Indications for use. Biseptol is used for respiratory tract infections: acute and chronic bronchitis (inflammation of the bronchi), pleural empyema (accumulation of pus between the membranes of the lungs), bronchiectasis (disease of the bronchi associated with the expansion of their lumen), abscess (abscess) of the lung, pneumonia (inflammation of the lungs) ; urinary tract: urethritis (inflammation urethra), cystitis (inflammation of the bladder), pyelitis (inflammation of the renal pelvis), chronic pyelonephritis (inflammation of the tissue of the kidney and renal pelvis), prostatitis (inflammation of the prostate gland), gonococcal urethritis. Also used for infections of the gastrointestinal tract, surgical infection and others infectious diseases... The drug is also effective for septicemia (a form of blood poisoning by microorganisms) caused by bacteria sensitive to the drug. The high efficacy of the drug was established in uncomplicated gonorrhea.

Method of administration and dosage. Before prescribing a drug to a patient, it is advisable to determine the sensitivity of the microflora to it that caused the disease in this patient. Adults and children over 12 years of age are usually prescribed in a daily dose of 4 tablets (or 2 forte tablets, or 8 scoops of syrup). The minimum daily dose for long-term therapy (more than 14 days) is 2 tablets (or 1 tablet forte, or 4 scoops of syrup). The maximum daily dose (for the treatment of especially severe cases) is 6 tablets (or 3 forte tablets, or 12 scoops of syrup). The daily dose is divided into 2 doses (morning and evening). The drug is taken after meals with enough liquids. When acute infections drug treatment is carried out for 5 days or until the patient has no symptoms of an infectious disease for 2 days.

With gonorrhea, the drug is prescribed for one day in a daily dose of 10 tablets (5 tablets forte, or 20 measuring beds of syrup), divided into 2 doses (morning and evening). For acute uncomplicated urinary tract infections in women, it is recommended to prescribe 2-3 tablets forte once. It is advisable to take the tablets in the evening after meals or before going to bed.

With pneumocystosis ( acute form pneumonia; observed more often in weakened children of the first months of life), caused by Pneumocystiscarinii, is prescribed in a daily dose of sulfamethoxazole up to 0.1 g / kg of body weight and

trimethoprim up to 0.02 g / kg. Assign every 6 hours. The course of treatment is 14 days.

For children under 12 years of age, the drug is prescribed in the form of a syrup in a daily dose of 0.03 g sulfamethoxazole and 0.006 g of trimethoprim. The syrup is taken 2 times a day (morning and evening). For severe infections, the daily dose can be increased by about 50%.

For patients with impaired renal function, the dose is set depending on the value of creatinine clearance (the rate of blood cleansing from the end product of nitrogen metabolism - creatinine). When creatinine clearance is more than 30 ml / min, dose adjustment is not required; at 15-30 ml / min apply half the usual dose; when creatinine clearance is less than 15 ml / min, it is not recommended to use the drug. In elderly patients, dose adjustment may also be required.

The drug should be used under close medical supervision.

Side effect. Possible nausea, vomiting, diarrhea (diarrhea), allergic reactions, nephropathy (a common name for some kidney diseases). Leukopenia (a decrease in the level of leukocytes in the blood) and agranulocytosis (a sharp decrease in the number of granulocytes in the blood) may develop.

Contraindications. Hypersensitivity to sulfonamides, diseases of the hematopoietic system, impaired liver and kidney function, pregnancy. The drug should not be prescribed premature babies and newborns. Bactrim should be used with caution in children. early age... When treating with the drug, it is necessary to carefully monitor the blood picture.

Release form. Tablets in a package of 20 pieces. The drug is available in tablets in two dosages: for adults, containing 0.4 g (400 mg) of sulfamethoxazole and 0.08 g (80 mg) of trimethoprim in one tablet; for children containing 100 mg of sulfamethoxazole and 20 mg of trimethoprim in one tablet.

For adults, Bactrim Forte tablets are also produced, containing 800 mg of sulfamethoxazole and 160 mg of trimethoprim, and for children, a syrup, 1 ml of which contains 40 mg of sulfamethoxazole and 8 mg of trimethoprim (suspension of white with a yellowish tinge of color in 100 ml vials ).

Storage conditions.

BACTRIM SUSPENSION (Bactrim)

Synonyms: Biseptol, Septrin, etc.

Pharmachologic effect. Combined drug. The combination of sulfamethoxazole and trimethoprim provides high efficiency against gram-positive and gram-negative microorganisms, including those resistant to sulfa drugs. Bactrim is rapidly absorbed when taken orally. The maximum concentration in the blood is observed after 1-3 hours and lasts for 7 hours.

Indications for use. Septicemia (a form of blood poisoning by microorganisms), infections of the respiratory, urinary tract and gastrointestinal tract caused by microorganisms sensitive to the drug, etc.

Method of administration and dosage. Before prescribing a drug to a patient, it is advisable to determine the sensitivity of the microflora to it that caused the disease in this patient. Assign inside after meals (morning and evening). Doses are set depending on the age of the child: from 6 weeks. up to 5 months - "/ 2 teaspoons 2 times a day; from 6 months to 5 years - 1 teaspoon 2 times a day; from 5 to 12 years - 2 teaspoons 2 times a day.

Side effect. Nausea, vomiting, allergic reactions, leukopenia (a decrease in the level of leukocytes in the blood) and agranulocytosis (a sharp decrease in the number of granulocytes in the blood). Treatment is carried out under the control of the blood picture.

Contraindications.

Release form. Suspension (syrup) in bottles of 100 ml. The suspension (per 5 ml) contains the following substances: sulfamethoxazole-3 (paminobenzenesulfamido) -5-methylisoxazole - 0.2 g; trimethoprim - 2,4-diamino-5- (3,4,5-trimethoxybenzyl) -pyrimidine - 0.04 g.

Storage conditions. List B. In a cool, dry dark place.

LIDAPRIM (Lidaprim)

Pharmachologic effect. Combined preparation containing sulfamethrol and trimethoprim. Sulfametrol has high antibacterial activity, and in combination with trimethoprim (see Biseptol provides bactericidal (destroying bacteria) action against gram-positive and gram-negative microorganisms, including bacteria resistant to conventional sulfa drugs.

Indications for use. Indications for the use of lidaprim basically coincide with the indications for the use of Biseptol.

Lidaprim is effective for infections of the respiratory tract, ear, throat and nose of the kidneys and urinary tract and gastrointestinal tract, for prostatitis (inflammation of the prostate gland), gonorrhea, gynecological infectious diseases and other infections caused by pathogens sensitive to the drug.

Method of administration and dosage. Before prescribing a drug to a patient, it is advisable to determine the sensitivity of the microflora to it that caused the disease in this patient. Adults and children over 12 years of age are prescribed the drug by mouth, usually starting with 2 tablets of lidaprim or 1 tablet of lidaprim forte 2 times a day (morning and evening). Take until the acute manifestations of the infection disappear (at least 5 days); then 1 tablet or U2 tablets of Lidaprim forte 2 times a day.

Sick chronic pyelonephritis (inflammation of the tissue of the kidney and renal pelvis) and in chronic salmonella, 2 tablets of lidaprim or 1 tablet of lidaprim forte are prescribed 2 times a day for a long time (on average 3 months).

With gonorrhea, usually 4 tablets of Lidaprim Forte are prescribed once a day.

For acute infections, an intravenous infusion of lidaprim solution can be started; injected slowly in 250 ml (1 bottle) 2 times a day.

Children under 2 years of age are prescribed "/ 2 teaspoons of the suspension 2 times a day, from 2 to 3 years - 1 teaspoon of the suspension or 2 tablets for children 2 times a day; 3-6 years - 1" / 2 teaspoon or 3 tablets per day for children; 6-12 years old - 2 teaspoons or 4 tablets for children 2 times a day.

Side effects and contraindications are the same as biseptol.

Release form. Lidaprim is available in different dosage forms: a) lidaprim tablets containing 400 mg of sulfametrol and 80 mg of trimethoprim, in a package of 20 or 100 pieces; b) coated tablets of lidaprim forte containing 800 mg of sulfametrol and 160 mg of trimethoprim, in a package of 10; 25 or 50 pieces; c) Lidaprim tablets for children, containing 100 mg of sulfametrol and 20 mg of trimethoprim, in a package of 20 pieces; d) suspension of lidaprim (for children), containing 5 ml (1 teaspoon) of 200 mg of sulfamethrol and 40 mg of trimethoprim, in bottles of 50 and 100 ml; e) solution for injection (infusion) in glass bottles of 250 ml, containing 800 mg of sulfametrol and 160 mg of trimethoprim.

Storage conditions.

MAPHENID (Maphenidum)

Synonyms: Ambamide, Bensulfamidine, Homosulfamidine, Sulfamilon, Mafenide acetate, etc.

Sulfanilamide antibacterial drug for external use. Available as Acetate Mafenide.

Pharmachologic effect. Mafenide acetate has a wide spectrum of action, is effective against gram-positive and gram-negative bacteria and pathogenic (pathogenic) anaerobes (microorganisms that can exist in the absence of oxygen), causative agents of gas gangrene. It is not inactivated by para-aminobenzoic acid and does not change the activity in acidic environment.

Indications for use. Used to treat infected burns, purulent wounds, bedsores (tissue necrosis caused by prolonged pressure on them due to lying), trophic ulcers (slowly healing skin defects).

Method of administration and dosage. Before prescribing a drug to a patient, it is advisable to determine the sensitivity of the microflora to it that caused the disease in this patient. Ointment (10%) is applied directly to the affected surface, tampons soaked in ointment are introduced into the cavity, wipes are also applied to the wounds, smeared with ointment with a layer of 2-3 mm. Usually, 30-70 g of ointment is consumed per bandage. Before applying a bandage, the wound is cleaned of purulent-necrotic masses (inflamed necrotic / dead / tissue). Dressings are changed daily or 2-3 times a week, depending on the amount of purulent discharge. The duration of treatment is from 1 to 4-5 weeks.

In case of II degree burns, a single bandage application is possible.

Side effect. When applying the ointment to the burn or wound surface, there may be a burning sensation, pain lasting from "/ 2 to 1-3 hours; with severe pain analgesics (pain relievers) are prescribed.

Contraindications. The use of the ointment is contraindicated if there is a history (medical history) of data on toxic-allergic reactions to sulfa drugs.

Release form. 10% ointment in 50 g and 2 kg light-shielded glass jars.

Storage conditions.

ALGIMAF (Algimafum)

Lyophilized gel (iron-like dosage form, dehydrated by freezing in a vacuum) of sodium-calcium salt of alginic acid containing mafenide and other substances.

Pharmachologic effect. Shows adsorbent (absorbing) and antimicrobial activity, cleanses wounds, promotes tissue regeneration (restoration).

Indications for use. Applied for superficial burns of 2 and 3 degrees, long-term non-healing ulcers and wounds.

Method of administration and dosage. Apply a plate of the appropriate size to the affected surfaces (after processing). Fix with a gauze bandage or bandage. Can be left in the wound until the end of epithelialization (recovery skin surface or mucous).

Side effect. A passing burning sensation.

Release form. Sterile porous sheets from 50x50 to 135x250 mm in size and 10 mm thick in bags,

Storage conditions. List B. In a dry, dark place, without bending the bags and protecting them from mechanical damage.

NORSULFAZOL (Norsulfazolum)

Synonyms: Sulfathiazole, Amidothiazole, Aseptozil, Azoseptal, Cybazol, Eleudron, Poliseptil, Pirisulfone, Thiazamide, etc.

Pharmachologic effect. Sulfanilamide drug. Effective for infections caused by hemolytic streptococcus, pneumococcus, gonococcus, staphylococcus, and Escherichia coli.

Indications for use. Pneumonia (inflammation of the lungs), cerebral meningitis (purulent inflammation of the membranes of the brain), gonorrhea, staphylococcal and streptococcal sepsis (infection of the blood by microbes / streptococci / from the focus of purulent inflammation), dysentery, etc.

Method of administration and dosage. Before prescribing a drug to a patient, it is advisable to determine the sensitivity of the microflora to it that caused the disease in this patient. Is taken internally. With pneumonia and meningitis, the first dose is 2 g, then 1 g every 4-6 g (course dose 20-30 g); for staphylococcal infections, the first dose is 3-4 g, then 1 g 4 times a day for 3-6 days. In the treatment of dysentery, 6-4-3 g per day according to a special scheme.

For children, norsulfazole is prescribed every 4-6-8 hours in the following single doses: at the age of 4 months. up to 2 years old - 0.1-0.25 g each, from 2 to 5 years old - 0.3-0.4 g each, from 6 to 12 years old - 0.4-0.5 g each. double dose.

Side effect. Possible dyspeptic disorders (digestive disorders), allergic reactions, leukopenia (a decrease in the level of leukocytes in the blood), neuritis (inflammation of the nerve), impaired renal function (crystalluria - the presence of salt crystals in the urine).

Contraindications. Hypersensitivity to sulfa drugs.

Release form. Powder; tablets in packs of 10 pieces of 0.25 g each and 0.5 g each with a line.

Storage conditions. List B. In a dry, dark place.

Norsulfazole is also a part of Ingalipt preparations, Sunoref ointment.

NORSULFAZOL-SODIUM (Norsulfazolum-natrium)

Synonyms: Sulfathiazole sodium, Sulfathiazole sodium, Norsulfazole soluble.

Norsulfazole sodium salt.

Indications for use. The same as for norsulfazole. In addition, for infectious eye diseases.

Method of administration and dosage. Before prescribing a drug to a patient, it is advisable to determine the sensitivity of the microflora to it that caused the disease in this patient. It is administered intravenously in cases where the possibility of introducing nosulfazole into the stomach is excluded (for example, after surgery on the gastrointestinal tract, with vomiting and unconsciousness of the patient) and if it is necessary to quickly create a high concentration of the drug in the blood. As soon as the patient's condition allows, they switch to taking the drug inside.

A 5% or 10% solution is injected into a vein; appoint at the rate of 0.5-1.0-2.0 g per infusion (10-20 ml of 5% or 10% solution; pour in slowly). It is advisable to additionally dilute solutions of norsulfazole soluble in 5% glucose solution or in isotonic sodium chloride solution. When using concentrated solutions, one should take into account the possibility of phlebitis (inflammation of the vein) at the injection site. Subcutaneous and intramuscular solutions are not prescribed, since they can cause tissue irritation up to necrosis (tissue necrosis).

They are also used in the form of eye drops (10% solution, 2 drops 3-4 times a day) for conjunctivitis (inflammation of the outer membrane of the eye), blepharitis (inflammation of the edges of the eyelids) and other infectious eye diseases. Can be taken internally.

Higher doses for adults inside: single - 2 g, daily - 7 g.

Side effects and contraindications. The same as for norsulfazole.

Release form. Powder.

Storage conditions. List B. In a dry, dark place.

SALAZODIMETOXIN (Salazodimethoxintun)

Pharmachologic effect. Sulfanilamide of prolonged (long-acting) action. -Like salazopyridazine, the drug breaks down in the intestine, with the formation of 5-aminosalicylic acid and sulfadimethoxin, which have anti-inflammatory and antibacterial effects. The drug is low-toxic.

Indications for use. Nonspecific ulcerative colitis (chronic inflammation of the colon with ulceration caused by unclear causes) in the active stage, mainly in lungs and moderate severe forms diseases, poor tolerance or ineffectiveness of salazopyridazine.

Method of administration and dosage. Assign orally (after meals) in approximately the same doses and for the same period as salazopyridazine. Usually adults are given 0.5 g 4 times a day (1 g 2 times a day) for 3-4 weeks, and then (if during this period therapeutic effect) 0.5 g 2-3 times a day for the next 2-3 weeks. In severe forms of the disease, the daily dose is increased in the first days to 4 g, and after a decrease in stool frequency, the dose is reduced. In milder forms of the disease, you can start with a dose of 1.5 g per day, and if there is no effect, go to 2 g per day.

Children aged 3 to 5 years in the first 7-14 days are prescribed 0.5 g per day, in the next 2 weeks. - 0.25 g per day, on other days (up to the 40th - 50th day from the start of treatment) - 0.125 g per day; children from 5 to 7 years old - respectively, 0.8-1.0 g each; 0.4-0.5 g and 0.2-0.25 g; from 7 to 15 years old - 1.0-1.5 g; 0.5-0.75 g and 0.25-0.375 g. Daily doses are given in 2-3 doses.

If during the first 14 days from the start of treatment it is not possible to obtain a therapeutic effect, salazodimethoxin is canceled; you can switch to the use of salazopyridazine or salazosulfapyridine.

To prevent relapses ( reappearance signs of the disease) ulcerative colitis and Crohn's disease (a disease of an unclear cause, characterized by inflammation and narrowing of the lumen of certain parts of the intestine) salazodimethoxin is prescribed for a long time in gradually decreasing doses: for adults, 0.5 g 1-2 times a day daily for 2-6 months ., then 0.25-0.5 g daily or every other day for 6-12 months. For children, the drug is prescribed in smaller

doses, taking into account age and doses used in acute period disease. In case of deterioration of health, the dose of salazodimethoxin is increased,

Side effect. Allergic reactions, leukopenia (a decrease in the level of leukocytes in the blood), dyspeptic disorders (digestive disorders).

Contraindications. Hypersensitivity to sulfonamides.

Release form.

Storage conditions. List B. In the dark place.

SALAZOPIRIDAZIN (Salazopyridazinum)

Synonyms: Salazodin.

Pharmachologic effect. Sulfanilamyl drug. It has anti-inflammatory and immunosuppressive (suppressing the body's defenses) effect.

Indications for use. Ulcerative colitis (chronic inflammation of the colon with the formation of ulcers, caused by unclear reasons), as well as in diseases occurring with autoimmune disorders (disorders based on allergic reactions to their own tissues or waste products of the body), including as a baseline agents in the treatment of rheumatoid arthritis (infectious-allergic disease from the group of collagenoses, characterized by chronic progressive inflammation of the joints).

Method of administration and dosage. In case of ulcerative colitis, salazopyridazine is prescribed for adults inside (after meals) in tablets of 0.5 g 4 times a day for 3-4 weeks. If a therapeutic effect appears during this period, the daily dose is reduced to 1.0-1.5 g (0.5 g 2-3 times a day) and treatment is continued for another 2-3 weeks. If there is no effect, the drug is stopped. Patients with mild forms of the disease are prescribed the drug first in a daily dose of 1.5 g, and in the absence of an effect, the dose is increased to 2 g per day.

For children aged 3 to 5 years, salazopyridazine is prescribed starting with a dose of 0.5 g per day (2-3 doses). In the absence of effect within 2 weeks. the drug is canceled, and if there is a therapeutic effect, treatment is continued at this dose for 5-7 days, then the dose is reduced by 2 times and treatment is continued for another 2 weeks. In the case of clinical remission (temporary weakening or disappearance of the manifestations of the disease), the daily dose is again halved and it is prescribed until the 40-50th day, counting from the start of treatment.

Children aged 5 to 7 years are prescribed the drug, starting from 0.75-1.0 g per day; from 7 to 15 years old - with a dose of 1.0-1.2-1.5 g per day. Treatment and dose reduction is carried out according to the same scheme as in children from 3 to 5 years old.

The use of salazopyridazine is combined with general methods treatment and diet recommended for ulcerative colitis.

Salazopyridazine can also be used for ulcerative colitis and Crohn's disease (a disease of unknown cause, characterized by inflammation and narrowing of the lumen of certain parts of the intestine) rectally (into the rectum) in the form of suspensions (suspension of solid particles in a liquid) and suppositories.

A suspension of salazopyridazine 5% is used for rectal administration with lesions of the rectum and sieve, in the preoperative period and after subtogal colectomy (after removal of a part of the colon), with poor tolerance of the drug in the form of tablets. The suspension is slightly warmed up and injected in the form of an enema into the rectum or into the stump of the intestine, 20-40 ml

1-2 times a day. Children are injected with 10-20 ml (depending on age). Rectal administration can be combined with oral administration of the drug.

Suppositories are used rectally. In the acute stage of the disease, 1 suppository is prescribed 2-4 times a day for 2 weeks. up to 3 months The duration of the course depends on the effectiveness of treatment and the tolerability of the drug. The maximum daily dose is 4 suppositories (2 g). At the same time, you can take salazopyridazine tablets (not exceeding the total daily dose of 3 g) and other drugs for the treatment of ulcerative colitis.

In order to prevent relapses (reappearance of signs of the disease), 1-2 suppositories are prescribed per day for 2-3 months.

Doses and prescribing regimen for other forms of colitis with ulcerative lesions are the same as for ulcerative colitis.

Side effect. When taking salazopyridazine tablets inside, the same side reactions are possible as when using sulfonamides and salicylates: allergic phenomena, leukopenia (a decrease in the level of leukocytes in the blood), dyspeptic disorders (digestive disorders), sometimes a slight decrease in the level of hemoglobin (the functional structure of an erythrocyte that ensures its interaction with oxygen). IN similar cases the dose should be reduced or the drug should be discontinued. After the introduction of the suspension, a burning sensation in the rectum and the urge to defecate (bowel emptying) may appear, especially with rapid administration. When using salazopyridazine in suppositories, a burning sensation and soreness in the rectum is possible, and sometimes stool becomes more frequent. In case of severe pain with rectal administration of salazopyridazine in suppositories, it is recommended to prescribe the drug rectally in the form of a 5% suspension and inside in tablets.

Contraindications. The drug is contraindicated if there is a history (medical history) of data on toxic-allergic reactions during treatment with sulfonamides and salicylates.

Forms of release. 0.5 g tablets in a package of 50 pieces; 5% suspension in 250 ml vials containing salazopyridazine, tween-80, benzyl alcohol and polyvinyl alcohol (the preparation after shaking is a suspension orangewhich then settles); candles ( brown color) 0.5 g in a package of 10 pieces.

Storage conditions. List B. In the dark place at room temperature.

SALAZOSULFALIRIDIN (Salazosulfapyridinum)

Synonyms: Sulfasalazine, Azopyrin, Azufidin, Salazopyridine, Salazopyrin, Salicylazosulfapyridine, Salisulf.

Pharmachologic effect. The drug has an antibacterial effect against diplococci, streptococci, gonococci, Escherichia coli. A feature of the drug is that it has a pronounced healing effect in patients with ulcerative colitis (chronic inflammation of the colon with the formation of ulcers caused by unclear reasons). The mechanism of this action is not fully understood. A certain role is played by the drug's ability to accumulate in connective tissue (including intestinal tissue) and gradually separate 5-aminosalicylic acid and sulfapyridine, which have anti-inflammatory and antibacterial properties.

Indications for use. Ulcerative colitis, rheumatoid arthritis (infectious-allergic disease from the group of collagenoses, characterized by chronic progressive inflammation of the joints).

Method of administration and dosage. Before prescribing a drug to a patient, it is advisable to determine the sensitivity of the microflora to it that caused the disease in this patient. Assign inside. Recommended on the 1st day for adults 1 tablet (0.5 g) Phrase per day (at regular intervals), on the 2nd day - 2 tablets 4 times and on the following days in case of good drug tolerance - 3-4 times tablets 4 times a day. After subsiding clinical symptoms diseases are prescribed maintenance doses (1.5-2.0 g per day) for several months.

For children, salazosulfapyridine is prescribed in smaller doses: at the age of 5-7 years - on! / 2-1 tablet (0.25-0.5 g) 3-6 times a day, over 7 years old - 1 tablet (0.5 g ) 3-6 times a day.

Salazosulfapyridine is also effective in mild to moderate forms of Crohn's disease (a disease of unknown cause, characterized by inflammation and narrowing of the lumen of certain parts of the intestine)

Salazosulfapyridine is also used as a basic agent in the treatment of rheumatoid arthritis due to the presence of immunocorrecting properties in the drug (restoring immunity / body defenses /). Assign 2-3 g per day (40 mg / kg per day) for 2-6 months.

Treatment should be carried out under close medical supervision; it is necessary to systematically monitor the blood picture.

Side effect. Nausea, vomiting may occur, headache, dizziness. In such cases, the drug is canceled, and after 2 days, gradually, within 3 days, the dose is again increased. Allergic reactions in the form of skin rashes, drug fever (a sharp rise in body temperature in response to taking the drug); leukopenia (a decrease in the level of leukocytes in the blood). In these cases, the drug should be discontinued. The drug is excreted in the urine and alkaline reaction paints it yellow-orange.

Contraindications. Severe toxic-allergic reactions in history (formerly) to sulfonamides.

Release form. 0.5 g tablets in a package of 50 pieces.

Storage conditions. List B. In a dry, dark place.

STREPTOCID (Streptocidum)

Synonyms: Sulfanilamide, Streptocid white, Ambezid, Deseptil, Dipron, Prontalbin, Prontoin, Prontoin, Prontosil white, Streptamine, Streptozol, Sulfamidil, etc.

Pharmachologic effect. Sulfanyl amide preparation. Has antimicrobial effect against streptococci, meningococci., Gonococci, pneumococci, Escherichia coli and some other bacteria.

Indications for use. Erysipelas, tonsillitis, epidemic cerebrospinal meningitis (purulent inflammation of the meninges of the brain), cystitis (inflammation of the bladder), pyelitis (inflammation of the renal pelvis), colitis (inflammation of the colon :), wound infection.

Method of administration and dosage. Before prescribing a drug to a patient, it is advisable to determine the sensitivity to it of the microflora that caused the disease in this patient. Inside 0.5-1 g 5-6 times a day. Dose for children

reduce according to age. Higher doses for adults inside: single - 2 g, daily - 7 g.

Topically injected into the wound 5-15 g of sterile powder; externally in the form of 5% liniment or 10% ointment.

Side effect. Headache, dizziness, nausea, vomiting, cyanosis (blue skin and mucous membranes), allergic reactions, leukopenia (a decrease in the level of leukocytes in the blood), agranulocytosis (a sharp decrease in the number of granulocytes in the blood), paresthesia (feeling of numbness in the limbs), tachycardia ( heart palpitations).

Contraindications. Diseases of the hematopoietic system, kidneys, Graves' disease (disease thyroid gland), hypersensitivity to sulfonamides.

Release form. Powder; tablets in a package of 10 pieces of 0.3 g each and 0.5 g each; 5% liniment in a package of 50 g; ointment 10% in a package of 30 g.

Storage conditions. List B. In a dry, dark place.

STREPTOCIDA LINIMENT 5% (Linimentum Streptocidi5%)

Indications for use. To accelerate the healing of infected wounds, degree I and II burns, boils (purulent inflammation of the hair follicle of the skin that has spread to the surrounding tissues), carbuncles (acute diffuse purulent-necrotic inflammation of several nearby sebaceous glands and hair follicles), with superficial pyoderma (purulent inflammation of the skin), acne vulgaris, impetigo (superficial inflammation of the skin, characterized by the appearance of abscesses, drying up with the formation of crusts) and other purulent-inflammatory skin diseases.

Method of administration and dosage. Before prescribing the drug to the patient, it is advisable to determine the sensitivity of the microflora to it that caused the disease in this patient, Liniment is applied to the lesion (under gauze bandage) 1-2 times a day.

Side effects and contraindications are the same as for streptocide.

Release form. In tubes or glass jars to 30 g.

Storage conditions. In a cool, dry place; banks - in a dark place.

"SUNOREF" OINTMENT (Unguentum "Sunoreph")

Indications for use. Sharp and chronic rhinitis (inflammation of the nasal mucosa).

Method of administration and dosage. Topically (lubricate the mucous membranes of the nose).

Side effect. Allergic reactions are possible.

Contraindications. Hypersensitivity to sulfa drugs.

Release form. Ointment composition: streptocide - 5 g, norsulfazole - 5 g, sulfadimezin - 5 g, ephedrine hydrochloride - 1 g, camphor - 3 g, eucalyptus oil - 5 drops, ointment base - up to 100 g, in a package of 15 g.

Storage conditions. In a cool place.

Streptocide is also part of the drug osarcid.

SOLUBLE STREPTOCID (Streptocidumsolubile)

Pharmachologic effect. Sulfanilamide drug. (See Streptocide).

Indications for use. Epidemic, cerebrospinal meningitis (purulent inflammation of the membranes of the brain), erysipelas, tonsillitis, cystitis (inflammation of the bladder), pyelitis (inflammation of the renal pelvis), colitis (inflammation of the colon), wound infection. The appointment of the drug is especially indicated for vomiting or unconsciousness of the patient.

Method of administration and dosage. Before prescribing a drug to a patient, it is advisable to determine the sensitivity of the microflora to it that caused the disease in this patient. Subcutaneously, intramuscularly up to 100 ml of 1-1.5% solution 2-3 times a day; intravenously up to 20-30 ml of 2%, 5% or 10% solution.

Side effects and contraindications are the same as for streptocide.

Release form. Powder.

Storage conditions. List B. In a dry, dark place.

Soluble streptocid is also part of the inhalipt preparation.

SULGIN (Sulginum)

Synonyms: Sulfaguanidine, Abiguanil, Aseptiguamidine, Ganidan, Guamid, Guanicil, Guasept, Neosulfonamide, Resulfone, Sulfaguanisan, etc.

Pharmachologic effect. Sulfanilamide drug. Sulgin is absorbed very slowly. The main amount of the drug taken orally is retained in the intestines and excreted in the feces. Is an effective remedy for the treatment of intestinal infections. The action is similar to phthalazole.

Indications for use. Bacterial dysentery, colitis (inflammation of the colon) and enterocolitis (inflammation of the small and large intestine) with diarrhea, carriage of Shigella and typhoid fever sticks, preparation for bowel surgery.

Method of administration and dosage. Inside, 1-2 g 6-5-4-3 times a day (on the first day - 6 times; 2 and 3 - 5; 4 - 4, and 5 - 3 times a day).

Children under 3 years old - 0.2 g / kg per day in 3 doses for 7 days; children over 3 years old - 0.4-0.75 g (depending on age) 4 times a day.

For prevention postoperative complications on the intestine, 0.05 g / kg every 8 hours for 5 days before surgery and 7 days after surgery.

Higher doses for adults inside: single 2 g, daily 7 g.

Side effect. Possible nausea, vomiting, crystalluria (the presence of salt crystals in the urine).

Contraindications. Hypersensitivity to sulfonamides, impaired renal function.

Release form.

Storage conditions. List B. In a dry, dark place.

SULFADIMEZIN (Sulfadimezinum)

Synonyms: Sulfadimidine, Diazil, Diazol, Dimetazil, Dimethyldebenal, Dimethylsulfadiazine, Dimethyl-sulfapyrimidine, Primazin, Sulfadimerazine, Sulfamethazine, Sulfamezatil, Sulfamezatin, Sulmet, Sulfadimethyl-pyrimidine, Superseptyl.

Pharmachologic effect. Sulfanilamide drug. It is active against pneumococci, meningococci, streptococci, gonococci, Escherichia coli and some other microorganisms.

Method of administration and dosage. Before prescribing the drug to the patient, it is advisable to determine the sensitivity

to him the microflora that caused the disease in this patient. Inside, 1 g 4-6 times a day. With pneumonia and meningitis, 2 g is prescribed for the first dose; children at the rate of 0.1 g / kg for the first dose, then 0.25 g / kg every 4, 6, 8 hours. Higher doses for adults inside: single 2 g, daily 7 g.

For the treatment of dysentery in adults on the 1-2 nd day - 1 g 6 times; on the 3-4th day - 1 g 4 times; on the 5-6th day - 1 g 3 times a day. The course dose is 25-30 g. After a 5-6 days break, repeat the course of treatment for 5 days, the course dose is 21 g of the drug. With dysentery, children under 3 years old - up to 0.2 g / kg per day in 4 doses for 7 days; children over 3 years old - 0.4-0.75 g (depending on age) 4 times a day.

Side effect. Possible nausea, vomiting, allergic reactions, leukopenia (a decrease in the level of leukocytes in the blood), agranulocytosis (a sharp decrease in the number of granulocytes in the blood), crystalluria (the presence of salt crystals in the urine).

Contraindications. Hypersensitivity to sulfonamides, diseases of the hematopoietic system, impaired renal function.

Release form. Powder; tablets of 0.5 g in a package of 10 pieces.

Storage conditions. List B. In a place protected from light.

Sulfanilamide drugs are antibacterial agents that have shown nice results in the treatment of diseases caused by bacteria in humans. Sulfonamides familiar to many have long established themselves with positive side, because they were invented even before the appearance penicillin antibiotics, as well as fluoroquinols.

In connection with the release modern drugs sulfanilamide are produced in a smaller volume, but their importance in practical official medicine did not shake at all. Still, with sensitivity to sulfonamides of bacterial flora and harmful microorganisms, which are shown by tests, they choose this active ingredient, which has been tested over the years.

How sulfa drugs work

It was revealed that sulfa drugs cope with certain types bacteria, including:

• gram-positive and negative bacteria;
• protozoa that cause malaria and toxoplasma;
• chlamydia.

Effective action is achieved by disrupting the formation process necessary conditions for reproduction and the existence of infection in human body... The microbial cell lives by feeding on para-aminobenzoic acid, with which sulfa drugs are similar in structure. As a result, the bacterium begins to feed on another substance that destroys the metabolic processes of the microbe, after which the latter dies.

Types of sulfa drugs

Sulfonamides are distinguished by the circulation period:

• short action;
• medium action;
• long acting;
• ultra-long.

Time does not stand still, and, unfortunately, many strains of microbes were able to mutate and adapt to sulfonamides. IN this case doctors have found the next effective way out, how to deal with bacteria - by combining the sulfanilamide group of antibiotics with trimethoprim. Combined medicines also help, which also include a sulfanilamide component.

What types of sulfonamides are currently used to treat microbial ailments:

1. Co-trimoxazole.
2. Sulfadimethoxine.
3. Sulfalen.
4. Sulfaetidol.

In terms of chemical content, the agents are similar to sulfones, which exhibit excellent activity against leprosy mycobacteria, and therefore are used to treat a serious disease - leprosy.

Sulfaminamide preparations in pure form: list

It is impossible to list absolutely all sulfa drugs found in pharmacies, so we have compiled a list of the most basic medicines used in modern times to cure many strains of bacteria:

1. Argidin.
2. Argosulfan.
3. Bactrim.
4. Berlocid.
5. Biseptol.
6. Dermazin.
7. Duo-Septol.
8. Co-trimoxazole-Rivopharm.
9. Kotrifarm.
10. Mafenide acetate ointment 10%.
11. Oriprim.
12. Septrine
13. Sinersul.
14. Streptocide.
15. Streptocide ointment 10%.
16. Sulgin.
17. Sulfadimezin.
18. Sulfadimethoxine.
19. Sulfalen.
20. Sulfargin.
21. Sulfacetamide.
22. Sulfacetamide sodium.
23. Sumetrolim.
24. Trimezole.
25. Phthalazol.
26. Tsiplin.
27. Etazole sodium.
28. Etazole tablets.

Sulfonamides in combinations

There are not so many sulfa drugs in combinations:

1. Ingalipt - used as a remedy for inflammation of the tonsils, which is characterized by sore throat, swelling, pain. An otolaryngologist (ENT) prescribes Ingalipt if patients, including children, are diagnosed with one of the following ailments: tonsillitis, pharyngitis, laryngitis, stomatitis, expressed in ulcers. The pharmacological action of the spray is based on anti-inflammatory and antimicrobial principles. Plant extracts not only are powerful antiseptics, but also refresh the larynx. Children can be taken from the age of 12, because medicated oils can cause an allergic reaction in babies.
2. A variation of Ingalipt is another sulfa drug - Ingalipt-Vial.
3. Lidaprim - helps in the treatment of many bacterial diseases, complete list which can be found in the instructions for use. They are mainly associated with inflammatory ailments of the throat, nose and ear, complicated by infections of the skin, urinary system. The antibiotic is also useful as a maintenance therapy after surgery. To prevent the bacteria from Candida, it is shown to orally consume tablets to maintain the intestinal microflora, women can insert suppositories into the vagina.
4. Streptonitol - helps cleanse the skin and organs from bacteria. Doctors prescribe a drug for the treatment of wounds, burns from 1 to 4 degrees, bedsores, trophic ulcers, gangrene formed against the background of diabetes. The remedy saves from erysipelas, dermatitis of various etiologies and pyoderma. Also attributed to acne. However, with the use of Streptonitol, you need to be careful in patients who have wounds with profuse purulent discharge.

Indications for the use of basic sulfa drugs

Doctors note the following features of the main sulfa drugs:

1. Argosulfan - acts not only against bacteria, but also against microbes of different strains. It can be applied openly or with an occlusive wound dressing. If a bandage is applied, it is important to cleanse the affected area with particular care. The thickness of the application of the ointment is at least 2-3 mm, it is allowed to use it 3 times a day.

It is considered impractical to leave individual areas uncovered, the cream must be placed tightly so that it is not visible skin... You can cover the wound or leave it uncovered with a bandage, the cream will not spread.

How long does Argosulfan treatment last? Before complete healing area or before a skin graft is planned. Do not be afraid if exudate appears in the wound - this is normal phenomenon with internal infection. Before use, doctors recommend washing the wound from ichor and other secretions with Chlorhexidine 0.1%.

The ointment must not be frozen, otherwise it will lose its medicinal properties.

1. Biseptol is an antibiotic of the sulfanilamide class, which is directed against bacteria, the advantage is that today it is effective against many types of microbes. Therefore, the course of Biseptol will relieve such ailments as bronchitis, sinusitis, whooping cough, scarlet fever, syphilis, gonorrhea, chlamydia, malaria, meningitis, otitis media, pneumonia, peritonitis, osteomyelitis, cystitis and urethritis, both chronic and primarily indicated.

Biseptol can be stored for up to 5 years at a temperature not exceeding 25 degrees with a plus sign.

1. Berlocid - the unique composition of the drug allows you to fight microorganisms that are resistant to other representatives of the sulfanilamide group. Berlocid is prescribed for infections involving the respiratory tract, ear, throat and nose. The antibiotic is active against microbes found in the kidneys, genitourinary tract and organs of the gastrointestinal tract. Among the contraindications in the instructions, the manufacturer indicated: hypersensitivity to individual components of the medication, Stevens-Johnson syndrome, severe complicationsassociated with kidney and liver dysfunction, prematurity. Pregnant women should not use the active ingredient in this composition in the 1st trimester of pregnancy.
2. Dermazin - helps to heal burns, bedsores and wounds that have affected the deep layers of the skin. Among side effects itching, burning and baking of the treated area may occur. The ointment is applied no more than 2 times a day after surgical treatment of the wound and disinfection. The remedy is not applicable to newborns. Dermazin is designed for external use only.
3. Co-trimoxazole-Rivopharm. Tablets are available with content active substance volume of 120 mg, 480 mg, 960 mg. Also on sale are suspensions for oral administration, packaged in 100 ml vials. With the help of an antibiotic, therapy is carried out for streptococci, staphylococci, pathogens of gonorrhea, salmonella, which cause severe forms of poisoning in people.
4. With the help of Streptocide, wounds are treated; for this, the tablets should be rubbed into powder. The powder is applied both wet and dry alone. Allergic reactions may occur very rarely.

Karaganda State Medical University

Department of General Pharmacology

Topic: Sulfanilamide preparations.

Completed: Art. group 2085 Savitskaya T.

Checked by: teacher Nikolaeva T.L.

Karaganda 2013

1. Introduction

2.sulfanilamide drugs (pharmacodynamics, pharmacokinetics, contraindications and indications for use, classification)

3. Sulfanilamide preparations. Name. Forms of release, average therapeutic doses, methods of administration.

4.

5. Derivatives of sulfa drugs.

6. Used literature.

Sulfanilamide drugs are synthetic chemotherapeutic agents, derivatives of sulfanilic acid, capable of significantly inhibiting the development of gram-positive and gram-negative bacteria, chlamydia, and some protozoa and pathogenic fungi. The first sulfonamide was synthesized in 1908 by P. gel, a graduate of the pharmaceutical faculty of the University of Vienna. However, the medicinal properties of the new chemical compound have not been investigated. In 1932 German chemists of the Far-Benindustri company synthesized red paint, the antimicrobial properties of which were investigated by G. Domagk. He showed that red dye has a pronounced antimicrobial effect in mice infected with hemolytic streptococcus. Proptosil (this is the name given to the red paint) prevented the death of mice, which were injected with a 1000-fold dose of hemolytic streptococcus. Experimental studies had to be confirmed by clinical observations. A dramatic incident in the family of G. Domagka accelerated these observations. His daughter fell ill with a severe form of septicemia with an unfavorable prognosis at the time. Mr. Domagk was forced to give her proptosil, although this substance has not yet been used for treatment. The daughter was saved from certain death. G. Domagk agreed to test prontosil in different clinics in Germany. The scientist received positive reviews from everywhere. The common dye has proven to be an effective antimicrobial agent. Summarizing the experimental, clinical studies, G. Domagk in 1935 published in the magazine "Deutsche medi-cinishe wochenschrifft" an article "Contribution to the chemotherapy of bacterial infections." For the discovery of the medicinal properties of prontosil, G. Domagk received the Nobel Prize in 1938. However, prontosil was patented by Farbenindustri, which had an exclusive right to the drug and established high prices... Employees of the Pasteur Institute in Paris showed that the effective principle of prontosil, or red streptocide, is its white fraction - aminobenzenesulfamide, which was synthesized in 1908 by P. gel. It was streptocide (white streptocide). Since white streptocide was not patented, everyone could use it. The discovery of the medicinal properties of streptocide 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 sulfonamides is sulfanilic acid obtained from PABA. Sulfonamides have one general formula. To date, more than 15,000 derivatives of sulfanilic acid have been synthesized, of which about 40 have been introduced into medical practice as antibacterial agents. Under the influence of sulfa drugs, a bacteriostatic effect is observed in vivo and in vitro only in relation to bacterial cells that multiply. Antimicrobial activity requires the presence of a free amine group NH2 at the 4-position. The spectrum of antimicrobial action of sulfa drugs is quite wide: gram-positive and gram-negative cocci, Escherichia coli, Shigella, Vibrio cholerae, clostridia, protozoa (causative agents of malaria, pneumocystis, toxoplasma), chlamydia (causative agents of psittacosis), causative agents, diphtheria pathogens, plague fungi (actinomycetes, coccidia), large viruses (causative agents of trachoma, inguinal granulomas). The mechanism of the chemotherapeutic action of sulfa drugs is based on overall structure them with para-aminobenzoic acid (PABA), due to which they, competing with it, are attracted to the metabolism of bacteria. By competing with PABA, sulfonamides prevent its use by microorganisms for the synthesis of dihydrofolic acid. Dihydrofolic acid with the participation of reductase is converted into a metabolically active coenzyme tetrahydrofolic acid, which is involved in the synthesis of pyrimidine bases of DNA and RNA. The microbial cell has a certain amount of accumulated PABA; therefore, the effect of sulfonamides is observed after a certain latency period, during which 5.5 ± 0.5 generation occurs. Thus, the competitive antagonism between sulfonamides and PABA largely predominates towards PABA. Therefore, for antimicrobial action, the concentration of sulfanilamide in the medium must exceed the concentration of PABA by a factor of 2000 - 5000. Only in this case will microbial cells absorb sulfanilamide instead of PABA. That is why sulfa drugs are administered in rather significant doses. First, 0.5 - 2 g of the drug is prescribed to create a sufficient concentration in the body, and then it is systematically administered in doses that will provide a bacteriostatic concentration. As a result, the synthesis of purine and pyrimidine compounds, nucleotides and nucleic acids is disrupted, which leads to inhibition of the exchange of proteins of microorganisms, disrupts the development and division of their cells. The use of sulfa drugs in reduced doses promotes the formation of strains of microorganisms that are resistant to the action of drugs. The antibacterial effect of sulfa drugs is reduced in the presence of pus, blood, decay products of body tissues, which contain sufficient amounts of PABA and folic acid. Means that, due to their biotransformation in the body, form PABA (for example, novocaine), as well as compounds containing purine and pyrimidine bases, reduce the antibacterial effect of sulfonamides. Conversely, those compounds that are capable of inhibiting dihydrofolic acid reductase are synergists of sulfonamides, since they disrupt the next stage of metabolism - the synthesis of tetrahydrofolic acid with dihydrofolic acid. An example is, for example, trimethoprim, which is used to create effective antimicrobial agents. The sensitivity of microorganisms to sulfa drugs is due to their ability to synthesize PABA. Nichutlnvish to streptocid hemolytic streptococcus. Microorganisms that do not require PABA (assimilate dihydrofolic acid) are not sensitive to the action of sulfonamides. Staphylococcus, enterococcus, proteus, tularemia causative agent are less sensitive to sulfonamides. In the early years widespread use sulfa drugs were highly effective against staphylococcus, meningococcus, gonococcus, etc. Now, most clinical strains of these microorganisms have acquired resistance to the action of sulfa drugs due to the ability to synthesize PABA or as a result of mutation. Most sulfa drugs are obtained on the basis of a streptocide molecule by introducing aliphatic, aromatic and heterocyclic radicals. Substitution of hydrogen at the nitrogen of the sulfanilamide group makes it possible to obtain antimicrobial compounds with aliphatic groups (sulfacil), aromatic radicals (sulfadimezine, etazole, norsulfazole). If we replace hydrogen at the nitrogen of the amine group in the 4-position, the antibacterial activity of the compound is significantly reduced. This is due to a decrease in the similarity of sulfonamides to PABA. Phthalazole, for example, acquires antibacterial activity after the reduction of the amino group, which occurs in the intestine. The spectrum of antibacterial action of various sulfanilamide drugs is somewhat different due to the ability to suppress them and others. enzyme systems... Norsulfazole has a thiazole ring, mimics the action of thiamine and inhibits the synthesis of cocarboxylase, which is involved in the decarboxylation of pyruvic acid. According to norsulfazole acts on gonococcus, staphylococcus, intestinal group of bacteria, weaker - on pneumo-, meningo- and especially streptococcus. Sulfadimezin is active against cocci and gram-negative rods, less active against gono-and staphylococcus. Etazole has a moderate bacteriostatic effect on most cocci, active against the intestinal flora. Sulfanilamide is a white powder, slightly soluble in water, soluble in aqueous solutions of bases. The choice of sulfa drugs is determined by the properties of the pathogen, the spectrum of antimicrobial action, as well as the characteristics of pharmacokinetics. Classification. Depending on the characteristics of pharmacokinetics (absorption in the gastrointestinal tract and the duration of excretion from the body), sulfa drugs are divided into the following groups: I. Drugs 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 is different, so they can be divided into separate subgroups. 1. Preparations

short-term action from T1 / 2 to 10 hours (etazole, norsulfazole, sulfadimezin). they are prescribed 4-6 times a day, the daily dose is 4-6 g, the course dose is 20-30 g. 2. Preparations average duration action of TU / and 10 - 24 hours (sulfazine, methylsulfazine). they are prescribed 1-3 g per day 2 times; course dose of 10 - 15 g. Preparations of short and medium duration of action are used mainly in acute infectious processes. 3. Long-acting drugs with T1 / 2 more than 24 hours (sulfapyridazine, sulfadimethoxine, sulfamonodimethox-son). Appoint the first days 1-2 g, then 0.5 - 1 g 1 time per day. 4. Drugs Increased action with T, / 2 60 - 120 h (sulfalene). Sulfalene is prescribed in a dose of 1 g of the first day, then 2 g once a week or 0.2 g per 30 minutes before meals, daily for chronic diseases. II. Drugs that are practically not absorbed in the alimentary canal (phtazin, phthalazol, sulgin) are prescribed for colitis, enterocolitis only inside. These drugs form a significant concentration of the active substance in the intestine (phthalazole decomposes to form norsulfazole). With prolonged use, sulfonamides suppress saprophytic microflora, which plays a significant role in the synthesis of vitamin K2, an imbalance of which can lead to hypoprothrombinemia. III. Topical preparations (streptocid, etazole, sodium sulfacyl). Streptocide, etazole as the smallest powders are used for powders, in the form of liniment, sodium sulfacyl - for eye drops, which penetrate well into all eye tissues. Sulfonamides are found in many ointments. IV. Salazosulfonamides - nitrogen compounds of sulfonamides with salicylic acid (salazosulfapyridine, salazopyridazine, salazodimethoxin) have antibacterial and anti-inflammatory properties. In the intestine, they break down with the release of active sulfonamides and 5-aminosalicylic acid. Prescribed mainly to patients with ulcerative colitis, 0.5 - 1 g 4 times a day. V. Combined preparations of sulfonamides with trimethoprim (bactrim - biseptol). Sulfonamides, which are well absorbed into the blood, are able to form complexes with plasma albumin, and partially circulate in a free state. The connection with proteins is unstable. The degree of bond increases with an increase in the hydrophobicity of the molecules. Acetylated forms are more associated with proteins than free compounds. With a decrease in the level of protein in the blood plasma, the content of the free fraction of sulfonamides in it significantly increases. From the blood, sulfonamides penetrate well into various fabrics and body fluids. Sulfapyridazine has the highest permeability. Sulfonamides are found in significant quantities in the kidneys, liver, lungs, skin, in smaller quantities in adipose tissue, and in bones they are not detected. The concentration of sulfonamide in the pleural, peritoneal, synovial and other fluids is 50 - 80% of it in the blood. The process of inflammation greatly facilitates the penetration of sulfonamides through the blood-brain barrier into the brain tissue. Quite easily, they pass through the placenta, are determined in saliva, sweat, in the mother's milk, in the tissues of the fetus. The biotransformation of sulfonamides is different for different drugs. Sulfonamides in the body are partially acetylated, oxidized, form inactive glucaronides or do not change. Acetylation in the liver and depends not only on the drug, but also on the acetylative ability of the liver. Etazole, urosulfan are less acetylated, and sulfidine, streptocid, norsulfazole, sulfadimezine are more acetylated. With acetylation, the activity of the drug is lost and its toxicity increases. Acetylated sulfonamides have low solubility and in an acidic environment can form calculi that can precipitate (crystalluria), injure or even block the renal tubules. Drugs that are slightly acetylated are excreted from the body in active form and have significant antimicrobial activity in the urinary tract (etazole, urosulfan). The formation of inactive glucuronides is characteristic of sulfadimethoxine. Glucuronides are highly soluble and do not precipitate. Sulfonamide metabolites have no antimicrobial activity. Excreted by the kidneys by glomerular filtration and partly tubular secretion. Long-term and increased-action drugs are little inactivated in the body and are reabsorbed in significant quantities in the tubules, which explains the duration of their action. Side effects when using sulfa drugs can be different and dangerous, but with proper treatment, it rarely happens. Complications are common for the entire group: allergic reactions, effects on the blood, and the like. They are caused by an overdose of drugs or hypersensitivity of the patient. Overdose is more common in children and the elderly, especially after 10-14 days of treatment with long-acting drugs. Signs of intoxication (nausea, vomiting, dizziness), damage to the epithelium of the renal tubules, the formation of crystals in them (oliguria, protein, erythrocytes in the urine), hepatitis may develop. To prevent the formation of crystals in the urinary tract, a significant amount of alkaline drink (up to 3 liters) or sodium hydrogencarbonate, mineral alkaline waters should be prescribed. Prescribing sulfa drugs requires caution in kidney and liver diseases. Complications associated with increased sensitivity of the body can be of an allergic nature (rash, dermatitis, exudative erythema, serum sickness, vascular damage, sometimes anaphylactic shock). There are blood lesions - hemolytic anemia, leukopenia, agranulocytosis, rarely - aplastic anemia, a depressing effect on the central nervous system. Indications for the use of sulfonamides - diseases caused by microorganisms sensitive to them. Sulfonamides, are well absorbed, are used for infectious diseases of the urinary system, biliary tract, ear, throat, nose, lungs, patients are prescribed trachoma, actinomycosis, toxoplasmosis, malaria, meningitis, etc. If the pathogen is sensitive to the drug, the therapeutic effect is manifested in within 1 - 3 days: signs of infectious toxicosis (fever, impaired blood circulation, respiration) disappear, the general condition improves. Sulfonamides, poorly absorbed, used for intestinal infections (enteritis, colitis, dysentery, typhoid fever, etc.). The antibacterial activity of sulfa drugs is much weaker than antibiotics. Taking this into account, and also taking into account the increase in the number of resistant strains, in recent times sulfa drugs are used less. they can be given along with antibiotics. To prevent the formation of sulfanil-midostiic strains of microorganisms, combinations of sulfa drugs with other chemotherapeutic agents are used. For example, the combined preparation Bactrim (Biseptol, Trimoxazole) contains 5 parts of the sulfa drug sulfamethoxazole and 1 part of trimethoprim. Sulfamethoxazole and trimethoprim each separately carry out a bacteriostatic effect. Simultaneous use in the form of a combined preparation enhances the antimicrobial effect and provides a high bactericidal effect even against microorganisms resistant to sulfa drugs. Sulfamethoxazole blocks the biosynthesis of the acid of dihydrofolic bacteria at the PABA level. Trimethoprim blocks the next phase of metabolism - the reduction of dihydrofolic acid to tetrahydrofolic by inhibition of dihydrofolic acid reductase. Trimethoprim is 5,000 - 10,000 times more related to microorganism dihydrofelate reductase than with functionally analogous mammalian reductases. Trimethoprim has an antimicrobial spectrum similar to other sulfonamides, but it is 20-100 times more active. Bactrim inhibits the development of most (about 95%) strains of staphylococcus, pyogenic and green streptococcus, different types protea, Escherichia coli, Salmonella, Shigella. Resistance to Bactrim develops rather slowly. When administered orally, the maximum concentration in the blood is determined after 1 to 3 hours and lasts for 7 hours. T1 / 2 of trimethoprim is 16 hours, sulfamethoxazole - 10 hours. In the presence of sulfamethoxazole, trimethoprim in a small amount binds to plasma proteins and quickly enters the tissues, where the concentration exceeds the concentration in the blood serum. Sulfamethoxazole binds up to 65% to blood plasma albumin. Sulfamethoxazole and trimethoprim are found in significant quantities in bile, sputum, mother's milk, amniotic fluid, eye media, bone marrow, intracellularly. During the day, 60% of trimethoprim and 25 - 50% of sulfamethoxazole are excreted in the urine, and more than 60% is excreted unchanged. Indications. Bactrim is prescribed for 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 the treatment of infectious diseases caused by hemophilus influenzae, patients with brucellosis, typhoid fever , cholera, etc. Therapeutic doses for adults - 1 g (2 tab.) Twice a day for 9-14 days and then 0.5 g twice a day in case of longer treatment. Contraindications. Sulfanilamide drugs, especially bactrim, are contraindicated in pregnant women due to the possibility of impaired fetal development, for mothers, since sulfonamides that come with milk can cause the development of methemoglobinemia in a child. Should not be prescribed to children with hyper-bilirubinemia: the risk of bilirubin encephalopathy (especially in children in the first 2 months of life), as well as children with a deficiency of glucose-6-phosphate dehydrogenase in erythrocytes. Side effects are rare. These are dyspeptic symptoms in 3-4% of patients (nausea, anorexia, diarrhea, vomiting), skin rash, urticaria, itching (in 3-5% of patients). Sometimes there are also severe skin-allergic reactions (Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis, etc.). Occasionally, leukopenia, agranulocytosis, thrombocytopenia, eosinophilia may develop. Possible megablastic reaction of the bone marrow in pregnant women with alcoholism (eliminated by folic acid). This reaction occurs as a hypersensitivity and is usually a contraindication to the appointment. Possible allergy cross-reactions in persons sensitized to sulfonamides. Cases of reproductive dysfunction in men are described. Sometimes candidiasis develops oral cavity and dysbiosis, especially in seriously ill and elderly people. Sulfanilamide preparations. Name. Forms of release, average therapeutic doses, methods of administration.

Sulfadimezin Sulfadimezinum Etazole Aethazolum Sulfacil sodium Sulfacylum-natrium Sulfadimethoxin Sulfadimethoxinum Sul lfap irndazin Sulfapyridazinum Phthalazol Phthalazolum Biseptol-480 (120; 240; 960) Pills 4805 each (120; 240; 960) : 1st intake - 2 g, then take but 1 g 4 - 6 times a day, with alkaline water. Children - 0.1 g / kg - 1st dose, then 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 30% solution; in vials of 5 and 10 ml ZO% difference; eye drops - a dropper tube with a 20% solution of 1.5 ml. Inside powder, 0.5-1 g 3 - 5 times a day, children 0.1 - 0.5 g 3-5 times a day, externally ZO% 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, 0.5 g. Inside the 1st day-1 g, then 0.5 g; severe 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, 6 g per day, 3 th and 4 th day - 4 g, 5 th and 6 th day - 3 g. Tablets, 20 pcs. Inside, 2 tablets 3 times a day after meals.

Pharmacology: Synthetic antimicrobial agents of various chemical structures.

This group includes various chemical compounds synthesized later than sulfa drugs, which differ from them and antibiotics in structure, mechanism and spectrum of antibacterial action. All of them have high antibacterial activity and a predominant effect on pathogens of intestinal infections and diseases. urinary tract, including infections that are difficult to treat with other antimicrobial agents. The drugs presented in this section are represented by the following chemical groups 1. Quinolone derivatives of the 1st generation, derivatives of 8-hydroxyquinoline (nitroxoline, chlorquinaldone, quiniophone, intetrix). 2. Quinolone derivatives of the II generation, derivatives of naphthyridine (nalidixic acid, oxolinium acid, pipemidium acid). 3. Quinolone derivatives of the third generation, fluoroquinolones (ciprofloxacin, ofloxacin, norfloxacin, pefloxacin, lomefloxacin, sparfloxacin). 4. Quinoxaline derivatives (quinoxidine, dioxidine). 5. Derivatives of nitrofuran (furacilin, furazolidone, furazolin, furadonin, fura-gon, soluble furagin). 6. Derivatives of imidazole (metronidazole). Quinoline derivatives (8-hydroxyquinoline and 4-quinolones). The drugs of this group are represented by halogen- (nitroxoline, mexazand mexaform, quiniophone) and nitro-derivatives. They suppress the vital activity of microorganisms, forming complex compounds with metal ions, reducing their enzymatic processes and functional activity. Pipemidic acid, for example, selectively inhibits the synthesis of bacterial DNA, has a wide spectrum of antimicrobial action, which spreads to gram-negative bacteria, causative agents of protozoal diseases (dysentery amoeba, lamblia, Trichomonas, balantidia). Drugs in this group are effective against antibiotic-resistant bacteria due to their lack of cross-resistance. The effect of the drugs is determined by varying degrees of absorption in the digestive tract: enteroseptol and intestopan are poorly absorbed, which contributes to their high concentration in the intestine and is used for infectious intestinal diseases. Nitroxoline, pipemidium and oxolinium acids are well absorbed and excreted by the kidneys unchanged, which provides an antibacterial effect in the urinary tract. Chlorquinaldone has antibacterial, protimycosis, antiprotozoal activity. The greatest activity is shown by gram-positive and some gram-negative bacteria. It is prescribed for intestinal infectious diseases (dysentery, salmonellosis, foodborne diseases, infections caused by staphylococcus, proteus, enterobacteria), as well as for dysbiosis. Intetrix by chemical structure close to Nitroxoline and Chlorquinaldone, contains a surfactant. Possesses antimicrobial, antiamebna, antimycotic action. Prescribed in cases of acute infectious diarrhea, dysbiosis, amebiasis. Hiniophone is not widely used. Prescribed for amoebic dysentery. Prescribing drugs of this group inside, it should be borne in mind that in the case of prolonged use of them, as well as in people with increased sensitivity to them, side effects may occur: peripheral neuritis, myelopathy, damage to the optic nerve, impaired liver and kidney function, allergic reactions. Therefore, despite their significant antibacterial activity, their treatment is very limited. For infectious diseases of the intestine, Chlorquinaldol and Intestopan are used, for the urinary tract, nitroxoline. Nitroxoline (5-NOK, uritrol -

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

Sulfonamides are active antimicrobial agents. IN last years interest in this group medicines increased in connection with the synthesis of long-acting sulfonamides and the creation of drugs combined with trimethoprim.

Sulfanilamide preparations - derivatives of white streptocide, having great similarity by physical and chemical properties.

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

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

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

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

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

Sulfanilamide preparations in low concentrations retard the growth and development of bacteria, that is, they act bacteriostatically. They have a bactericidal effect only when exposed to such high concentrations that are unsafe for the macroorganism. The most important feature sulfonamides - high activity in vivo with a relatively weaker effect in vitro. Under their influence, microbes swell, stop multiplying, produce toxins, and become more vulnerable to the body's defenses. The selectivity of individual drugs in relation to certain pathogens of infectious diseases has been established. So, norsulfazole and sulfazole are more active in staphylococcal infections, streptocid. - with streptococcal, and sulfapyridazine is very effective in sepsis caused by coli bacteria.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

In many infectious diseases, the pathogen is not in the blood for a longer time, but in various organs and tissues, therefore, the determination of the concentration of sulfa drugs in organs and tissues often has more essentialthan determining their concentration in the blood.

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

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

In humans and animals, sulfonamide compounds, like others medicinal substances, undergo cleavage, oxidation, acetylation. The acetylation process is especially important for clinical practice. It occurs mainly in the liver as a result of acetic acidcoming from the outside, and due to the acid formed in the body from pyruvic acid.

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

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

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

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

1) drugs quick action (streptocid, norsulfazole etazole, sulfacil, urosulfan, sulfadimezin, etc.);

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

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

The rate of elimination from the body largely determines the size of the dose and the frequency of taking the drug. The indicator of the rate of elimination is T50%, or T 1/2, - the half-life, that is, the time of decrease maximum concentration in the blood 2 times. For short-acting drugs, T 1/2 is less than 8 hours, the average duration of action is 8-16 hours, and for long-acting and super-long-acting drugs, 24-56 hours or more.

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

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

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

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

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

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

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

RESORPTIVE SULPHANYLAMIDES

SHORT-ACTION PREPARATIONS

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

For conjunctivitis, blepharitis and other infectious, eye diseases, 10% solutions are used in the form of eye drops 3-4 times a day.

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

Available in powder form. Store with precautions according to list B in a package protected from moisture and light. The term of the verification analysis is 3 years.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

White or white with a yellowish sheen, odorless crystalline powder, soluble in 20 parts of cold water (in hot water dissolves much easier), in 12 parts of ethanol, in solutions of alkalis and acids. Incompatible with novocaine, anesthesin, sulfur-splitting drugs.

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

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

Used for tonsillitis, pharyngitis, bronchopneumonia, postpartum sepsis, streptococcal infections, colibacillosis, salmonellosis, dyspepsia, cystitis, etc. Locally prescribed in the form of powders and ointments for the treatment of purulent wounds, skin streptococcal and staphylococcal diseases, conjunctivitis Doses inside: horses 5-10 g, small cattle 2-3, pigs -2, dogs 0.5-1 g 3-4 times a day. The initial dose should be 2-3 times the subsequent dose.

Contraindications for use are similar to other sulfonamides.

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Flavourless white crystalline powder, sour taste. We will slightly dissolve in water, it is difficult to dissolve in ethanol, we will easily dissolve in diluted acids and solutions of caustic alkalis. Incompatible with drugs that split off sulfur, novocaine, anesthesin, barbiturates.

Urosulfan has high antibacterial activity against staphylococci and Escherichia coli.

The drug is rapidly absorbed from the gastrointestinal tract, which ensures the creation of high concentrations in the blood. The maximum concentration is established in 1-3 hours from the moment of administration. Urosulfan is slightly acetylated, circulates and is excreted mainly in free form. The rapid release ensures the creation of high concentrations of the free form of the drug in the urine, which contributes to the manifestation of its antimicrobial properties in urinary tract infections. Urosulfan is low-toxic, no deposits in the urinary tract are noted.

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

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

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

MEDIUM DURATION OF ACTION PREPARATIONS

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

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

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

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

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

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

Contraindications for use, nephritis, nephrosis

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

LONG-ACTION PREPARATIONS

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

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

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

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

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

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

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

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

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

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

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

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

Crystalline powder, white or white with a yellowish-green tinge. Easily soluble in water, difficult in ethanol. Gradually turns yellow on exposure to light. Aqueous solutions can be sterilized at 100 ° C for 30 minutes.

The antibacterial spectrum is similar to sulfapyridazine.

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

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

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

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

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

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

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

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

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

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

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

In case of pasteurellosis of chickens, Sulfadimethoxine is prescribed for therapeutic purposes in doses of 200 mg (initial) and 100 mg (maintenance) per 1 kg of body weight. FROM preventive purpose apply doses of 100 mg (initial) and 50 mg - (maintenance) 1 time per day. The drug can be used as a group method with feed.

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

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

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

Crystalline powder, white or white with a yellowish sheen. We will slightly dissolve in water, better - in ethanol, we will easily dissolve in dilute mineral acids and aqueous solutions of caustic alkalis. Incompatible with novocaine, barbiturates, drugs that easily split off sulfur.

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

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

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

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

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

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

White crystalline powder. We will slightly dissolve in water, we will easily dissolve in solutions of alkalis. Incompatible with novocaine, barbiturates, drugs that easily split off sulfur.

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

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

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

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

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

Possible side effects and measures for their prevention are the same as with the use of other prolonged sulfonamides.

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

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

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

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

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

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

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

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

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

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

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

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

SULPHANYLAMIDES, POORLY ABSORATED FROM THE GASTROINTESTINAL TRACT

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

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

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

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

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

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

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

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

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

White or white powder with a slightly yellowish sheen. Practically insoluble in water, ether and chloroform; very slightly soluble in ethanol; soluble in aqueous solution sodium carbonate, easily soluble in an aqueous solution of sodium hydroxide. Incompatible with novocaine, anesthesin, sulfur-splitting drugs.

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

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

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

Side effects phthalazole usually does not cause. Contraindication - hypersensitivity of animals to sulfa drugs

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Mechanism of action

Sulfonamides have a bacteriostatic effect. Being analogs of PABA in chemical structure, they competitively inhibit the bacterial enzyme responsible for the synthesis of dihydrofolic acid, a precursor of folic acid, which is the most important factor vital activity of microorganisms. In environments containing a large amount of PABA, such as pus or tissue degradation products, the antimicrobial effect of sulfonamides is significantly weakened.

Some topical sulfonamide preparations contain silver (silver sulfadiazine, silver sulfathiazole). As a result of dissociation, silver ions are slowly released, providing a bactericidal effect (due to binding to DNA), which does not depend on the concentration of PABA at the site of application. Therefore, the effect of these drugs persists in the presence of pus and necrotic tissue.

Spectrum of activity

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

Currently, many strains of staphylococci, streptococci, pneumococci, gonococci, meningococci, enterobacteria are characterized by high level acquired resistance. Enterococci, Pseudomonas aeruginosa and most anaerobes are naturally resistant.

Preparations containing silver are active against many pathogens of wound infections - Staphylococcus spp., P.aeruginosa, E.coli, Proteus spp., Klebsiella spp., mushrooms Candida.

Pharmacokinetics

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

They are widely distributed in tissues and body fluids, including pleural effusion, peritoneal and synovial fluids, middle ear exudate, chamber moisture, and tissues of the urogenital tract. Sulfadiazine and sulfadimethoxine pass through the BBB, reaching 32-65% and 14-30% serum concentrations in the CSF, respectively. Pass through the placenta and enter breast milk.

Metabolized in the liver, mainly by acetylation, with the formation of microbiologically inactive, but toxic metabolites. Excreted by the kidneys about half unchanged, with an alkaline reaction of urine, excretion is enhanced; small quantities excreted in the bile. With renal failure, the accumulation of sulfonamides and their metabolites in the body is possible, leading to the development of toxic effects.

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

Adverse reactions

Systemic drugs

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

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

Liver: hepatitis, toxic dystrophy.

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

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

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

Thyroid: dysfunction, goiter.

Others: photosensitivity (increased sensitivity of the skin to sunlight).

Local preparations

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

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

Indications

Systemic drugs

Local preparations

Trophic ulcers.

Bedsores.

Contraindications

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

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

Renal failure

Warnings

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

Pneumocystis pneumonia (treatment and prevention).

Contraindications

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

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

Pregnancy.

Severe renal failure.

Severe liver dysfunction.

Megaloblastic anemia associated with folate deficiency.

Warnings

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

Pregnancy. The use of co-trimoxazole during pregnancy (especially in I and III trimesters) is not recommended, since the sulfanilamide component can cause kernicterus and hemolytic anemia, and trimethoprim interferes with folate metabolism.

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

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

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

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

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

Thyroid dysfunction. Caution is required when using due to the possible aggravation of thyroid dysfunction.

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

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

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

Porphyria. Development of an acute attack of porphyria is possible.

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

Drug interactions

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

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

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

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

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

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

Patient information

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

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

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

A doctor should be consulted if there is no improvement within a few days or new symptoms appear.

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

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

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

INN	Lecform LS	T ½, h *	Dosage regimen	Features of drugs
Sulfadimidine	Tab. 0.25 g and 0.5 g	3-5	Inside Adults: 2.0 g for the first dose, then 1.0 g every 4-6 hours Children older than 2 months: 100 mg / kg for the first dose, then 25 mg / kg every 4-6 hours For the prevention of plague (adults and children): 30-60 mg / kg / day in 4 divided doses	The drug is highly soluble, therefore it was previously widely used for infections with MEP
Sulfadiazine	Tab. 0.5 g	10	Inside Adults: 2.0 g for the first dose, then 1.0 g every 6 hours Children older than 2 months: 75 mg / kg for the first dose, then 37.5 mg / kg every 6 hours or 25 mg / kg every 4 hours (but not more than 6.0 g per day) For the prevention of plague (adults and children): 30-60 mg / kg / day in 4 steps	Better than other sulfonamides it penetrates the BBB, therefore it is preferable for toxoplasmosis. Not recommended for use in MEP infections, as it is poorly soluble
Sulfadimethoxine	Tab. 0.2 g	40	Inside Adults: 1.0-2.0 g on the first day, on the next 0.5-1.0 g, at one time Children over 2 months of age: 25-50 mg / kg on the first day, then 12.5-25 mg / kg	High risk of developing Stevens-Johnson and Lyell's syndrome
Sulfalen	Tab. 0.2 g	80	Inside Adults: 1.0 g on the first day, on the next 0.2 g; or 2.0 g once a week	High risk of developing Stevens-Johnson and Lyell's syndrome. Not assigned to children
Silver sulfadiazine	Ointment 1% in tubes of 50 g	ND	Locally Apply to the affected surface 1-2 times a day	Indications: burns, trophic ulcers, bedsores
Silver sulfathiazole	Cream 2% in tubes of 40 g and in jars of 400 g	ND	Also	The same
Co-trimoxazole (Trimethoprim / sulfamethoxazole)	Tab. 0.12 g; 0.48 g and 0.96 g Sir., 0.24 g / 5 ml in a bottle. Rr d / in. 0.48 g in amp. 5 ml each	Trime- toprim 8-10 Sulfa- tags- sazol 8-12	Inside Adults: at {!LANG-b77461716e38be0dcf6c51747189d015!} and {!LANG-7e168db5eb439ca5440a83c542ddab11!}{!LANG-6c9324fdfd6a51867e7b42946cc7e260!} {!LANG-65e17ed758abdc070abf966c8fff3e8d!} {!LANG-74640e6a41397e92463771df44075942!} {!LANG-2f4ab1409a838c0e53f29c04dd567fb4!} {!LANG-d3a2881cb8f9516f8e9f777a95479fb6!} {!LANG-a9d6e8881efa8e062e4bf2980675f2e1!} {!LANG-a71ad62ad2494d6cd7c18523f5163dde!} {!LANG-94d4d379431d739e33f5e6b688e5f6fa!} {!LANG-7f71d1318787526e5000c5acd3d6f915!} {!LANG-3bdb640dfdc6a6b08f7a07036b20d3fc!}	{!LANG-3ad416fbbb2bb83e03e55f54401a754f!} {!LANG-b98a3f1622cf0c86f3c3c6d6b7746d33!}

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