Translation of the instructions can be
Sulfadimezin tablets 500 mg
Instruction
For medical use of the medicinal product
Composition:
Active ingredient: sulfadimidine;
1 tablet contains sulfadimidine 500 mg;
Excipients: potato starch, gelatin, colloidal anhydrous silicon dioxide, calcium stearate.
Dosage form.
Pills.
Main physicochemical properties: round tablets with a flat surface, beveled edges and a score, white or slightly yellowish in color.
Pharmacotherapeutic group.
Antimicrobials for systemic use. Short-acting sulfonamides. Sulfadimidine. ATC code j01e B03.
Pharmacological properties.
Pharmacodynamics.
Sulfadimezin is a short-acting sulfonamide drug. Active against gram-positive and gram-negative cocci, Escherichia coli, Shigella, Klebsiella, Vibrio cholerae, causative agents of gas gangrene, anthrax, diphtheria, catarrhal pneumonia, plague, as well as chlamydia, actinomycetes, 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 tetrahydrofolic acid, necessary for the synthesis of purines and pyrimidines.
Pharmacokinetics.
Rapidly absorbed in the gastrointestinal tract (mainly in the small intestine), 75-86% bound to plasma proteins. Well penetrates into tissues and body fluids (including lungs, cerebrospinal fluid), quickly excreted from the body, 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 can precipitate when concentrated in the urine. The solubility of metabolites improves when alkalizing the urine.
Clinical characteristics.
Indication.
Infections caused by microorganisms sensitive to the drug:
respiratory tract and ENT infections (bronchitis, pneumonia, tonsillitis, sinusitis, otitis); inflammatory diseases of the biliary and urinary tracts; skin and soft tissue infections (wound infection, pyoderma, erysipelas); gonorrhea, trachoma; shigellosis; toxoplasmosis.
Contraindication.
Hypersensitivity to sulfadimidine or other components of the drug; history of toxic-allergic reactions to other sulfonamides or their derivatives; systemic blood diseases, suppression of bone marrow hematopoiesis, including anemia, leukopenia; severe liver and/or kidney function disorders, renal and/or hepatic failure; acute porphyria; hyperthyroidism; azotemia; glucose-6-phosphate dehydrogenase deficiency (hemolysis is possible).
Interaction with other drugs and other types of interactions.
Cyclosporine - possible decrease in plasma concentrations of the latter; increased risk of nephrotoxicity.
Antithrombotic agents, indirect anticoagulants (including phenindione, warfarin) - with simultaneous use, their anticoagulant effect is enhanced.
General anesthetics (thiopental) - increased effects of thiopental.
Pyrazolone derivatives, indomethacin and salicylates: increased activity and toxicity of sulfonamides.
Other nonsteroidal anti-inflammatory drugs, sulfonylurea derivatives (including oral antidiabetic agents), phenytoin - their plasma concentrations may increase, the therapeutic effect may be enhanced and the risk of side effects may increase. It may be necessary to adjust the dose of these drugs, including oral antidiabetic agents.
Clozapine and other potentially hematotoxic drugs (e.g. chloramphenicol, thiamazole, mercazolil) - increased risk of hematotoxicity, including agranulocytosis, leukopenia. Their simultaneous use with sulfonamides should be avoided.
Hexamethylenetetramine (urotropine), high doses of ascorbic acid, diuretics - increased risk of crystalluria. Joint use is not recommended.
Erythromycin, lincomycin, tetracycline, trimethoprim, pyrimethamine - mutual enhancement of antibacterial activity, expansion of the spectrum of action. Risk of pancytopenia and megaloblastic anemia when used simultaneously with pyrimethamine (inhibition of folic acid synthesis increases).
Folic acid, bactericidal antibiotics (including penicillins, cephalosporins), rifampicin - the effectiveness of sulfadimidine is reduced.
Methotrexate - sulfonamides increase the toxicity of methotrexate.
PASK preparations, barbiturates, local anesthetics (benzocaine, tetracaine, procaine), preparations containing paraaminobenzoic acid - reduced antimicrobial activity of sulfadimidine. There is an increased risk of methemoglobinemia with simultaneous use of sulfonamides with prilocaine.
Oral estrogen-containing contraceptives - their contraceptive effect is reduced when used simultaneously. Additional contraceptive measures should be used during treatment and for 7 days after discontinuation of sulfonamide treatment.
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.
Diagnostic tests: Sulfonamides may cause a false-positive Benedict's test for glucose in urine; may interfere with the results of the urine urobilinogen test.
Application features.
Given the similarity of chemical structure, sulfonamides should not be used in individuals with hypersensitivity to furosemide, thiazide diuretics, carbonic anhydrase inhibitors, and sulfonylurea derivatives.
Sulfonamides, including sulfadimidine, are not used to treat infectious diseases caused by group A beta-hemolytic streptococcus, since they do not contribute to its eradication and, therefore, cannot prevent complications such as rheumatism and glomerulonephritis.
Fatalities associated with the use of sulfonamides have been observed extremely rarely and have 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.
Sulfonamides should be discontinued at the first appearance of skin and/or mucous membrane rash or any other sign of adverse reaction. In very rare cases, severe adverse reactions may develop after the appearance of a skin rash. Patients should be informed of the signs of Stevens-Johnson syndrome and toxic epidermal necrolysis and of the need for immediate and permanent discontinuation of sulfonamide treatment at the first appearance. The greatest risk of Stevens-Johnson syndrome and toxic epidermal necrolysis occurs during the first weeks of treatment. The best results in the treatment of Stevens-Johnson syndrome or toxic epidermal necrolysis are associated with early diagnosis and immediate discontinuation of the suspected drug. Immediate discontinuation of the drug is associated with a better prognosis. If a patient develops Stevens-Johnson syndrome or toxic epidermal necrolysis during treatment with sulfonamides, including Sulfadimidine, any drugs containing sulfonamides, should not be re-administered by this patient throughout his life.
Hematologic disorders also require immediate and permanent discontinuation of sulfonamide therapy. Rash, sore throat, fever, joint pain, pale skin, purpura, or jaundice may be early signs of a serious hematologic reaction to sulfonamides, including sulfadimidine.
Pseudomembranous colitis, which can range from mild to life-threatening, is a risk associated with the use of virtually all antibacterial agents, including sulfonamides (due to overgrowth of Clostridium difficile). Therefore, it is important to consider this complication in patients with diarrhea when determining further treatment.
Sulfonamides, including sulfadimidine, should be used with caution in patients with impaired renal or hepatic function, severe allergic diseases or bronchial asthma, and diabetes mellitus (sulfonamides may affect blood sugar levels). If possible, sulfonamides should be avoided in patients over 65 years of age due to the increased risk of severe adverse reactions.
During treatment with the drug, especially long-term treatment, it is necessary to systematically monitor the state of kidney function (creatinine clearance), liver (serum transaminase levels), peripheral blood picture (complete blood count, platelet and reticulocyte levels), and blood glucose levels.
Patients should consume sufficient fluids to maintain a high diuresis (minimum 1200 ml/day) to prevent crystalluria and the development of urolithiasis. For the same purpose, if necessary, sulfadimidine can be prescribed in combination with urine alkalizing drugs.
It is recommended to avoid exposure to direct sunlight and artificial ultraviolet radiation, given the possibility of developing photosensitivity reactions when using sulfonamides.
Since sulfonamides are bacteriostatic, not bactericidal drugs, a full course of therapy is necessary to prevent recurrence of infection and the development of resistant forms of microorganisms.
During treatment with the drug, it is necessary to adhere to the dosage regimen, do not miss a dose. In case of missing a dose, double the next dose.
Use during pregnancy or breastfeeding.
The use of the drug during pregnancy is contraindicated.
If it is necessary to use the drug in women during lactation, breastfeeding should be discontinued.
The ability to influence the reaction speed when driving vehicles or other mechanisms.
Until the patient's individual reaction to the drug is determined, one should refrain from driving or operating other mechanisms, given that during treatment with sulfadimidine, such adverse reactions from the nervous system as dizziness, convulsions, drowsiness, and hallucinations are possible.
Method of administration and doses.
Sulfadimezin should be taken orally.
Average doses for adults - 2 g (4 tablets) for the first dose, then - 1 g (2 tablets) 4-6 times a day. Higher 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 for the first dose, then 0.025 g/kg of body weight every 4-6-8 hours.
1-2nd day - 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).
Total for the course of treatment - 25-30 g of the drug.
After a 5-6-day break, a second course of therapy should be prescribed:
1-2nd day - 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 sulfadimezine is taken. In mild cases 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 for 5-7 days. For most infectious diseases, treatment continues for at least another 48-72 hours after the disappearance of symptoms of the disease and confirmation of recovery by the results of bacteriological analysis.
Children.
The drug should be used in children from 3 years of age.
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 overdose. The development of methemoglobinemia is possible.
Treatment: immediate discontinuation of the drug, gastric lavage, increased drinking regimen of solutions that alkalize urine is indicated; with reduced diuresis and normal kidney function - intravenous administration of solutions. Further treatment is symptomatic.
If methemoglobinemia is confirmed, intravenous administration of 1% methylene blue is indicated.
Peritoneal dialysis is ineffective, and hemodialysis is only moderately effective in treating sulfonamide overdose.
Adverse reactions.
The same adverse reactions are possible as with other sulfonamides.
Digestive system: abdominal pain, dyspeptic phenomena, including nausea, vomiting, diarrhea, anorexia; stomatitis, sialadenitis, pancreatitis, pseudomembranous colitis.
Hepatobiliary system: increased serum levels of hepatic transaminases, hepatomegaly, rarely jaundice, hepatitis, possible hepatonecrosis.
Nervous system: headache, neurological reactions including aseptic meningitis, ataxia, benign intracranial hypertension, convulsions, dizziness, vertigo, drowsiness/insomnia, fatigue, peripheral or optic neuropathies, tinnitus.
Mental disorders: depression, psychosis, hallucinations.
Immune system: hypersensitivity reactions, including pruritus, skin rashes (including urticaria), drug fever, chills, photosensitivity reactions, exfoliative dermatitis, toxic epidermal necrolysis (Lyell's syndrome), erythema nodosum, erythema multiforme, erythroderma, fixed drug erythema, Stevens-Johnson syndrome, serum sickness-like syndrome, periorbital edema, anaphylactic reactions, including angioedema, very rarely - anaphylactic shock. In addition, cases of allergic myocarditis, nodular periarteritis, 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 glucose-6-phosphate dehydrogenase deficiency, purpura, hypoprothrombinemia, methemoglobinemia.
Human anatomical models: crystalluria (possibly with lumbar pain, hematuria, oliguria, anuria), the risk of which can be reduced by using the drug with sufficient fluid, treated by alkalinizing urine; nephrotoxic reactions: interstitial nephritis, tubular necrosis, renal failure. Increased levels of urea and creatinine in the blood serum.
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, the drug should be discontinued immediately.
Expiration date.
5 years.
Do not use after the expiry date stated on the packaging.
Storage conditions.
Store in a dry, dark place at a temperature not exceeding 25 ºС.
Keep out of reach of children.
Packaging.
10 tablets in a blister.
Vacation category.
According to the recipe.
Producer.
OOO "AGROFARM".
Location of the manufacturer and address of the place of business.
Ukraine, 08200, Kyiv region, Irpin city, Centralna st., 113-a.
