Sulfadimezin

Instruction manual

For medical use of the drug

Structure:

Active substance: sulfadimidine;

1 tablet contains 500 mg sulfadimidine;

excipients: potato starch, gelatin, colloidal anhydrous silicon dioxide, calcium stearate.

Dosage form.

Tablets.

Basic physical and chemical properties: round tablets with a flat surface, beveled edges and notch, white or slightly yellowish.

Pharmacotherapeutic group.

Antimicrobial agents for systemic use. short-acting sulfonamides. sulfadimidine. code atx j01e b03.

Pharmacological properties.

Pharmacodynamics

Sulfadimezin is a short-acting sulfanilamide drug. It is active against gram-positive and gram-negative cocci, Escherichia coli, Shigella, Klebsiella, cholera vibrio, causative agents of gas gangrene, anthrax, diphtheria, catarrhal pneumonia, plague, as well as chlamydia, actinomycetes, and causative agents of toxoplasmosis. It acts bacteriostatically. The mechanism of action is associated with para-aminobenzoic acid (PABA) and competitive inhibition of dihydropteroate synthetase, which leads to impaired synthesis of tetrahydrofolate acid, necessary for the synthesis of purines and pyrimidines.

Pharmacokinetics

It is rapidly absorbed in the gastrointestinal tract (mainly in the small intestine), binds to plasma proteins by 75–86%. It penetrates well into tissues and body fluids (including lungs, cerebrospinal fluid), is rapidly excreted from the body, the half-life is 7 hours; elimination is carried out mainly by the kidneys by glomerular filtration. In the liver it undergoes biotransformation (acetylation), acetylated metabolites when concentrated in the urine may precipitate. The solubility of metabolites improves with alkalization of urine.

Clinical characteristics.

Indications.

Infections caused by drug-sensitive microorganisms:

• infections of the respiratory tract and ENT organs (bronchitis, pneumonia, tonsillitis, sinusitis, otitis media);
• inflammatory diseases of the biliary and urinary tract;
• infections of the skin and soft tissues (wound infection, pyoderma, erysipelas);
• gonorrhea, trachoma;
• shigellosis;
• toxoplasmosis.

Contraindications

• Hypersensitivity to sulfadimidine or to other components of the drug; the presence of a history of toxic-allergic reactions to other sulfonamides or their derivatives; systemic blood diseases, inhibition of bone marrow hematopoiesis, including anemia, leukopenia; severe impaired liver and / or kidney function, renal and / or liver failure; acute porphyria; hyperthyroidism; azotemia; glucose-6-phosphate dehydrogenase deficiency (hemolysis is possible).

Interaction with other drugs and other types of interactions.

Cyclosporine - a decrease in plasma concentrations of the latter is possible; increased risk of nephrotoxicity.

Antithrombotic agents, indirect anticoagulants (including phenindione, warfarin) - with simultaneous use, their anticoagulant effect is enhanced.

General anesthetics (thiopental) - enhancing the effects of thiopental.

Pyrazolone derivatives, indomethacin and salicylates: increased activity and toxicity of sulfonamides.

Other non-steroidal anti-inflammatory drugs, sulfonylurea derivatives (including oral antidiabetic agents), phenytoin - it is possible to increase their concentration in blood plasma, increase the therapeutic effect and increase the risk of side effects. It may be necessary to adjust the dose of these drugs, including oral antidiabetic agents.

Clozapine and other potentially hematotoxic drugs (for example, chloramphenicol, Thiamazole, mercazolil) - the risk of hematotoxicity increases, includingagranulocytosis, leukopenia. Their simultaneous use with sulfonamides should be avoided.

Hexamethylenetetramine (urotropin), high doses of ascorbic acid, diuretics - an increased risk of crystalluria. Combined use is not recommended.

Erythromycin, lincomycin, tetracycline, trimethoprim, pyrimethamine - mutual enhancement of antibacterial activity, expansion of the spectrum of action. The risk of pancytopenia and megaloblastic anemia with simultaneous use with pyrimethamine (inhibition of folic acid synthesis increases).

Folic acid, bactericidal antibiotics (including penicillins, cephalosporins), rifampicin - the effectiveness of sulfadimidine decreases.

Methotrexate - sulfonamides increase the toxicity of methotrexate.

PASK preparations, barbiturates, local anesthetics (benzocaine, tetracaine, procaine), preparations containing paraaminobenzoic acid - a decrease in the antimicrobial activity of sulfadimidine. There is an increased risk of methemoglobinemia with the simultaneous use of sulfonamides with prilocaine.

Oral estrogen-containing contraceptives - with simultaneous use, their contraceptive effect is reduced. Additional contraceptive measures should be used during treatment and within 7 days after discontinuation of treatment with sulfonamides.

Oral typhoid vaccine - sulfonamides as antibacterial drugs inactivate the vaccine. The use of antibacterial drugs should be avoided for 3 days before and after oral vaccination.

Antacids - The absorption of sulfadimidine in the intestine decreases under their influence.

Diagnostic tests: sulfonamides can be the cause of a false positive test result of Benedict when determining glucose in the urine; may affect the results of a urine urobilinogen test.

Features of the application.

Given the similarity of the chemical structure, sulfonamides cannot be used by individuals with hypersensitivity to furosemide, thiazide diuretics, carbonic anhydrase inhibitors and sulfonylurea derivatives.

Sulfanilamides, including sulfadimidine, are not used to treat infectious diseases caused by beta-hemolytic group A streptococcus, since they do not contribute to its eradication and, therefore, cannot prevent complications such as rheumatism and glomerulonephritis.

Fatal cases due to the use of sulfanilamides were extremely rare and occurred as a result of serious adverse reactions, including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatonecrosis, agranulocytosis, aplastic anemia and other pathological conditions of the blood system.

The intake of sulfonamides must be stopped when the first rashes appear on the skin and / or mucous membranes or with any other signs of a negative reaction. In very rare cases, after the appearance of a rash on the skin, severe adverse reactions can develop. Patients should be informed about the signs of Stevens-Johnson syndrome and toxic epidermal necrolysis and the need for an immediate and final cessation of treatment with sulfonamides at their first manifestations. The greatest risk of Stevens-Johnson syndrome and toxic epidermal necrolysis occurs in the first weeks of treatment. The best results in treating Stevens-Johnson syndrome or toxic epidermal necrolysis are associated with early diagnosis and immediate discontinuation of the suspected drug. Immediate withdrawal of the drug is associated with a better prognosis. If the patient has developed Stevens-Johnson syndrome or toxic epidermal necrolysis in the treatment of sulfonamides, incl. sulfadimidine, any drugs containing sulfanilamides should not be reused by this patient throughout his life.

Hematologic disorders also require immediate discontinuation of sulfonamide treatment forever. A rash, sore throat, fever, joint pain, pallor of the skin, purpura, or jaundice can be early signs of a serious pathological reaction from the blood system when using sulfonamides, including sulfadimidine.

The risk of pseudomembranous colitis, which can vary from mild to life-threatening, exists with the use of almost all antibacterial agents, including sulfonamides (as a result of the excessive growth of Clostridium difficile). Therefore, it is important to consider the possibility of this complication in patients with diarrhea in order to determine further treatment tactics.

Sulfanilamides, including sulfadimidine, should be used with caution in patients with impaired renal, liver, severe allergic diseases or bronchial asthma, in patients with diabetes mellitus (sulfonamides can affect blood sugar). If possible, sulfanilamides should be avoided in patients over 65 due to the increased risk of serious adverse reactions.

When treating with a drug, especially a long one, it is necessary to systematically monitor the state of renal function (creatinine clearance), liver (serum transaminase level), peripheral blood picture (general blood count, platelet count, reticulocytes), and blood glucose level.

Patients should consume enough fluid to maintain high urine output (at least 1200 ml / day) to prevent crystalluria and the development of urolithiasis. For the same purpose, if necessary, sulfadimidine can be prescribed in combination with drugs that alkalinize urine.

It is recommended to avoid exposure to direct sunlight and artificial ultraviolet radiation, given the possibility of developing photosensitization reactions when using sulfonamides.

Since sulfonamides are bacteriostatic and not bactericidal, a full-fledged course of therapy is required to prevent recurrence of infection and the development of resistant forms of microorganisms.

During treatment with the drug, it is necessary to observe the dosage regimen, do not skip the dose. In case of missing a dose, do not double the next dose.

Use during pregnancy or lactation.

The use of the drug during pregnancy is contraindicated.

If it is necessary to use the drug for women during breast-feeding, breast-feeding should be discontinued.

The ability to influence the reaction rate when driving vehicles or other mechanisms.

Until the patients individual reaction to the drug is clarified, one should refrain from driving vehicles or other mechanisms, given that during treatment with sulfadimidine, adverse reactions from the nervous system, such as dizziness, convulsions, drowsiness, hallucinations, are possible.

Dosage and administration.

Take sulfadimezin orally.

The average dose for adults is 2 g (4 tablets) at the first dose, then 1 g (2 tablets) 4-6 times a day. Highest doses for adults: single - 2 g, daily - 7 g.

Children from 3 years of age should be prescribed 0.1 g / kg of body weight at the first dose, then 0.025 g / kg of body weight every 4-6-8 hours.

In the treatment of shigellosis, the drug should be prescribed to adults according to the scheme:

1-2 days - 1 g 6 times a day (every 4 hours);

3-4th day - 1 g 4 times a day (every 6 hours);

5-6th day - 1 g 3 times a day (every 8 hours).

In total, 25-30 g of the drug per course of treatment.

After a 5-6-day break, a second course of therapy should be prescribed:

1-2 days - 1 g 5 times a day (every 4 hours, and at night - after 8 hours);

3-4th day - 1 g 4 times a day (do not take at night);

5th day - 1 g 3 times a day.

During the second course, 21 g of sulfadimezin are taken.With a mild course of shigellosis, the dose can be reduced to 18 g.

Doses for the treatment of shigellosis in children from 3 years: a single dose - from 0.4 g to 0.75 g, which should be taken 4 times a day. The drug must be taken within 5-7 days. For most infectious diseases, treatment continues for at least another 48–72 hours after the disappearance of the disease symptoms and confirmation of recovery by the results of bacteriological analysis.

Children.

The drug is used for children from 3 years.

Overdose.

Symptoms: anorexia, spastic abdominal pain, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness. hyperthermia, hematuria, crystalluria are possible. pathological changes in the blood (leukopenia, agranulocytosis, hemolytic anemia) and jaundice are later manifestations of an overdose. possible development of methemoglobinemia.

Treatment: immediate discontinuation of the drug, gastric lavage, an enhanced drinking regimen of solutions alkalizing urine is indicated; with a decrease in diuresis and normal kidney function - intravenous administration of solutions. In the future, symptomatic treatment.

When methemoglobinemia is confirmed, intravenous administration of 1% methylene blue is indicated.

Peritoneal dialysis is not effective, hemodialysis is only moderately effective in the treatment of an overdose of sulfonamides.

Adverse Reactions

The same adverse reactions are possible as with other sulfonamides.

Digestive system: pain in the abdomen, dyspeptic phenomena, including nausea, vomiting, diarrhea, anorexia; stomatitis, sialadenitis, pancreatitis, pseudomembranous colitis.

Hepatobiliary system: increased serum levels of hepatic transaminases, hepatomegaly, occasionally jaundice, hepatitis, hepatonecrosis is possible.

Nervous system: headache, neurological reactions, including aseptic meningitis, ataxia, benign intracranial hypertension, cramps, dizziness, vertigo, drowsiness / insomnia, feeling tired, peripheral or optical neuropathies, tinnitus.

Mental disorders: depression, psychoses, hallucinations.

Immune system: hypersensitivity reactions, incl. itching, rashes (including urticaria), drug fever, chills, photosensitivity reactions, exfoliative dermatitis, toxic epidermal necrolysis (Lyells syndrome), erythema nodosum, erythema multiforme, erythroderma, fixed drug erythema, Stevens-Johnson syndrome, syvorotochnopodobny syndrome, periorbital edema anaphylactic reactions, including angioedema, very rarely - anaphylactic shock. In addition, cases of the development of allergic myocarditis, periarteritis nodosa, systemic lupus erythematosus / lupus-like syndrome have been reported.

Blood and lymphatic system: very rarely - agranulocytosis, aplastic anemia, thrombocytopenia, leukopenia, neutropenia, eosinophilia, acute hemolytic anemia with a deficiency of glucose-6-phosphate dehydrogenase, purpura, hypoprothrombinemia, methemoglobinemia.

Urinary system: crystalluria (possibly with lumbar pain, hematuria, oliguria, anuria), which is possible to reduce the risk of using the drug with a sufficient amount of liquid, is treated by alkalization of urine; nephrotoxic reactions: interstitial nephritis, tubular necrosis, renal failure. Increased levels of urea, serum creatinine.

Endocrine system: hypothyroidism, hypoglycemia.

Respiratory system: cough, sore throat, shortness of breath, pulmonary eosinophilic infiltrates, fibrosing alveolitis.

Other: tachycardia, arteritis, vasculitis, joint pain, muscle pain.

If adverse reactions occur, stop taking the drug immediately.

Shelf life.

5 years.

Do not use after the expiration date indicated on the package.

Storage conditions.

Store in a dry, dark place at a temperature not exceeding 25 °С.

Keep out of the reach of children.

Packaging.

10 tablets in a blister.

Vacation category.

On prescription.

Manufacturer.

LLC "agrofarm".

The location of the manufacturer and the address of the place of business.

Ukraine, 08200, Kiev region, Irpin city, st. central, 113-a.