Sulfadimethoxine

I N S T R U C T I O N for medical use of the medicinal product SULFADIMETHOXINE (SULFADIMETHOXINUM)

Composition:

Active substance: sulfadimethoxine;

1 tablet contains sulfadimethoxine 500 mg (0.5 g);

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

Medicinal form. Tablets.

Main physicochemical properties: tablets are white or white with a creamy shade, with a flat surface, a score line and beveled edges.

Pharmacotherapeutic group. Antimicrobial agents for systemic use. Long-acting sulfonamides.

ATC code J01E D01.

Pharmacological Properties.

Pharmacodynamics.

A long-acting sulfonamide. Sulfadimethoxine exhibits antibacterial activity against gram-negative and gram-positive bacteria: pneumococci, staphylococci, streptococci, Escherichia coli, Klebsiella pneumoniae, and Shigella species; less active against Proteus. Active against the causative agent of trachoma. Sulfadimethoxine does not affect bacterial strains resistant to other sulfonamides.

Pharmacokinetics.

Sulfadimethoxine is absorbed relatively slowly from the gastrointestinal tract. After oral administration, it appears in the blood within 30 minutes, with maximum concentration reached within 8–12 hours. The required therapeutic blood concentration (in adults) is achieved with an initial dose of 1–2 g on the first day and 500 mg–1.0 g on subsequent days. The drug is 90–98% bound to plasma proteins. Compared to other long-acting sulfonamides, sulfadimethoxine penetrates the blood-brain barrier poorly (thus, its use in purulent meningitis is inappropriate). The drug is excreted mainly in the form of metabolites, primarily via urine. Elimination half-life is 41 hours.

Clinical characteristics.

Indications.

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug: tonsillitis, bronchitis, pneumonia, sinusitis, otitis, dysentery, inflammatory diseases of the biliary and urinary tracts, gonorrhea, dysentery, pyoderma, meningitis, wound infections, trachoma, toxoplasmosis, shigellosis, resistant forms of malaria (in combination with antimalarial agents).

Contraindications.

Increased individual sensitivity to the components of the drug; history of severe toxic-allergic reactions to sulfonamides; bone marrow suppression; chronic heart failure; renal and/or hepatic insufficiency; hepatitis; glucose-6-phosphate dehydrogenase deficiency; porphyria; azotemia; agranulocytosis; hemolytic anemia; drug-induced jaundice; severe dermatitis.

Interaction with other medicinal products and other types of interactions.

When used simultaneously:

• with nonsteroidal anti-inflammatory drugs, sulfonylurea derivatives, antithrombotic agents, vitamin K antagonists – the effect of these drugs is enhanced;
• with folic acid, bactericidal antibiotics (including penicillins, cephalosporins) – the activity of sulfadimethoxine is reduced;
• with bactericidal antibiotics, oral contraceptives – the effect of these drugs is reduced;
• with para-aminosalicylic acid and barbiturates – the activity of sulfadimethoxine is enhanced;
• with pyrazolone derivatives, indomethacin, and salicylates – the activity and toxicity of sulfadimethoxine are enhanced;
• with methotrexate and phenytoin – the toxicity of sulfadimethoxine is enhanced;
• with erythromycin, lincomycin, tetracycline – mutual enhancement of antibacterial activity and broadening of the spectrum of action;
• with rifampicin, streptomycin, monomycin, kanamycin, gentamicin, oxquinoline derivatives (nitroxoline) – antibacterial activity of the drugs remains unchanged;
• with chloramphenicol, nitrofurans – reduced overall effect;
• with nalidixic acid (neviramone) – antagonism may occasionally occur.

Sulfadimethoxine should not be prescribed simultaneously with hexamethylenetetramine (urotropine), antidiabetic agents (sulfonylurea derivatives), phenytoin, neodicoumarin, and other indirect anticoagulants.

Special precautions for use.

During treatment with the drug, regular monitoring of kidney function, peripheral blood parameters, and blood glucose levels is necessary.

Sulfonamides, including sulfadimethoxine, should not be used for the treatment of infections caused by group A beta-hemolytic streptococci, as they do not eradicate this pathogen and therefore cannot prevent complications such as rheumatic fever and glomerulonephritis.

The drug should be prescribed with caution to patients with chronic heart failure, liver diseases, or impaired kidney function. Sulfadimethoxine should be administered cautiously to patients with severe forms of allergic disorders or bronchial asthma, as well as those with blood system disorders. Sulfonamides, including sulfadimethoxine, should be used with caution in patients with diabetes mellitus, since sulfonamides may affect blood glucose levels.

Since sulfonamides are bacteriostatic rather than bactericidal agents, a full course of therapy is required to prevent infection recurrence and the development of resistant microbial strains. Patients should maintain adequate fluid intake to prevent crystalluria and the development of urolithiasis.

The use of the drug in patients over 65 years of age should be avoided due to an increased risk of severe adverse reactions.

Exposure to direct sunlight and artificial ultraviolet radiation should be avoided due to the possibility of photosensitization during sulfonamide therapy.

During treatment, the prescribed dosing regimen must be strictly followed, using the recommended dose at 24-hour intervals, without missing doses. If a dose is missed, the next dose should not be doubled.

Use during pregnancy or breastfeeding.

Sulfadimethoxine is not recommended during pregnancy or breastfeeding.

Ability to influence reaction rate when driving or operating machinery.

There is no available information regarding the effect of the drug on the ability to drive or operate machinery.

Until the individual patient's response to the drug has been established, driving vehicles or operating machinery should be avoided, considering that adverse reactions of the nervous system such as dizziness, seizures, ataxia, drowsiness, depression, and psychosis may occur during sulfadimethoxine therapy.

Administration and Dosage.

Sulfadimethoxine is administered orally once daily with 24-hour intervals between doses.

Adults: On the first day, administer 1–2 g of sulfadimethoxine (2–4 tablets); in subsequent days, 500 mg–1 g of sulfadimethoxine (1–2 tablets) per day.

Children aged 12 years and older: On the first day, administer 1 g of sulfadimethoxine (2 tablets); in subsequent days, 500 mg of sulfadimethoxine (1 tablet) per day.

Children aged 3 to 12 years: Administer sulfadimethoxine at a dose of 25 mg/kg body weight on the first day and 12.5 mg/kg body weight per day in subsequent days.

After temperature normalization, the drug should be continued at maintenance doses for another 2–3 days.

The duration of treatment depends on the nature and severity of the disease. On average, the treatment course lasts 7–14 days.

Children.

The drug is indicated for the treatment of children aged 3 years and older.

Overdose.

Symptoms: Thirst, dry mouth, anorexia, pain in the right hypochondrium and lumbar region, spasmodic abdominal pain, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness, oliguria, change in urine color (intense yellow-brown). Hyperthermia, hematuria, and crystalluria may occur. Biochemical analysis may reveal increased activity of liver enzymes (alanine aminotransferase (ALT), aspartate aminotransferase (AST), alkaline phosphatase). Pathological blood changes (leukopenia, agranulocytosis, hemolytic anemia) and jaundice are later manifestations of overdose. Methemoglobinemia, tachycardia, paresthesia, dermatitis, diarrhea, and cholestasis may also develop.

Treatment: Discontinue the drug. If necessary, induce vomiting, perform gastric lavage, administer activated charcoal, and cleansing enema, and provide alkaline fluids. In confirmed cases of methemoglobinemia, intravenous administration of 1% methylene blue is indicated. In severe cases, forced diuresis is recommended. Peritoneal dialysis is ineffective; hemodialysis is only moderately effective in treating sulfonamide overdose.

Adverse Reactions

Blood and lymphatic system disorders: leukopenia, agranulocytosis, aplastic anemia, thrombocytopenia, hypoprothrombinemia, eosinophilia, hemolytic anemia in glucose-6-phosphate dehydrogenase deficiency.

Nervous system disorders: headache, neurological reactions including aseptic meningitis, ataxia, mild intracranial hypotension, seizures, dizziness, somnolence/insomnia, fatigue, depression, peripheral or optic neuropathies, psychosis.

Respiratory system disorders: pulmonary infiltrates, fibrosing alveolitis.

Gastrointestinal disorders: thirst, dry mouth, dyspeptic symptoms, nausea, vomiting, diarrhea, anorexia, pancreatitis, pseudomembranous colitis.

Renal and urinary system disorders: change in urine color (intense yellow-brown), crystalluria; possible nephrotoxic reactions – interstitial nephritis, tubular necrosis, renal failure.

Skin and subcutaneous tissue disorders: skin rashes, urticaria, allergic dermatitis, photosensitization, exfoliative dermatitis, nodular erythema.

Allergic reactions: toxic epidermal necrolysis (Lyell's syndrome), Stevens-Johnson syndrome, systemic lupus erythematosus, serum sickness-like syndrome, anaphylactic reactions, swelling of the tongue, upper lip, swallowing difficulties.

General disorders: drug fever, pain in the right hypochondrium and lumbar region.

Hepatobiliary disorders: increased liver enzyme activity (ALT, AST, alkaline phosphatase), cholestatic hepatitis, hepatonecrosis, hepatomegaly, jaundice.

Other: myocarditis, polyarteritis nodosa, hypothyroidism, hypoglycemia.

Shelf life.

5 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25°C.

Keep out of reach of children.

Packaging.

10 tablets in strips or blisters;
10 tablets in a strip or blister; 2 or 10 strips or blisters per cardboard pack.

Prescription status.

Prescription only.

Manufacturer. JSC " Monfarm ".

Manufacturer's address and location of business operations.

8, Zavodska St., Avramivka, Uman district, Cherkasy region, 19161, Ukraine.