Expiration date: 04/2025

Composition and form of issue:

Tablets for children, 1 tablet contains:

sulfamethoxazole 100 mg

trimethoprim 20 mg

auxiliary substances: potato starch talc magnesium StartSmart polyvinyl methyl parahydroxybenzoate parahydroxybenzoate propylene glycol 

in a contour cell package 20 PCs. in a pack of cardboard 1 blister.

Tablets, 1 tablet contains:

sulfamethoxazole 400 mg

trimethoprim 80 mg

auxiliary substances: potato starch talc magnesium StartSmart polyvinyl methyl parahydroxybenzoate parahydroxybenzoate propylene glycol 

in a contour cell package 20 PCs. in a pack of cardboard 1 blister.

Description of dosage form:

120 mg tablets: flat, round, white with a yellowish tinge of color, with chamfer and engraving "BS".

Pills 480 mg: flat, round, white with a yellowish sheen color, with facet, scored and engraved "Bs".

Pharmacokinetics:

When administered, both components of the drug are completely absorbed from the gastrointestinal tract. Cmax active components of the drug is observed in 1-4 hours.

Trimethoprim penetrates well into cells and through tissue barriers — into the lungs, kidneys, prostate, bile, saliva, sputum, liquor. The binding of trimethoprim to plasma proteins is 50%, T1/2 is the norm 8, from 6 to 17 h. the Main route of excretion is through the kidneys (50% in unmodified form).

Sulfamethoxazole: plasma protein binding is 66%, T1/2 in the norm — 9-11 h. the Main route of elimination is via the kidneys, and 15-30% in the active form.

Description of pharmacological action:

Combined antibacterial drug consisting of sulfamethoxazole and trimethoprim. Sulfametoxazole, similar in structure to pabc, disrupts the synthesis of dihydrofolic acid in bacterial cells, preventing the inclusion of pabc in its molecule. Trimethoprim enhances the action of sulfamethoxazole, disrupting the recovery of dihydrofolic acid in tetrahydrofolic-active form of folic acid, responsible for protein metabolism and division of microbial cells.

It is a broad-spectrum bactericidal preparation, active against the following microorganisms: Streptococcus spp. (hemolytic strains are more sensitive to penicillin), Staphylococcus spp., Streptococcus pneumoniae, Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (including enterotoxigenic strains), Salmonella spp. (including Salmonella typhi and Salmonella paratyphi), Vibrio cholerae, Bacillus anthracis, Haemophilus influenzae (including ampicillin-resistant strains), Listeria spp., Nocardia asteroids, Bordetella pertussis, Enterococcus faecalis, Klebsiella spp., Proteus spp., Pasteurella spp., Francisella tularensis, Brucella spp., Mycobacterium spp. (including Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumophila, Providencia, some species of Pseudomonas (except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp., Yersinia spp., Morganella spp., Pneumocystis carinii, Chlamydia spp., (including Chlamydia trachomatis, Chlamydia psittaci) protozoa: Plasmodium spp., Toxoplasma gondii, pathogenic fungi, Actinomyces israelii, Coccidioides immitis, Histoplasma capsulatum, Leishmania spp.

Resistant to the drug: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira spp., viruses.

Inhibits the life of the E. coli, which leads to a decrease in the synthesis of thiamine, Riboflavin, nicotinic acid and other b vitamins in the intestine.

The duration of the therapeutic effect is 7 hours.

Indications:

• respiratory infections (bronchitis, pneumonia, lung abscess, pleural empyema, otitis media, sinusitis)
  
• infections of the genitourinary system (pyelonephritis, urethritis, salpingitis, prostatitis), including gonorrheal nature
  
• infection of the gastrointestinal tract (dysentery, cholera, typhoid, paratyphoid, diarrhea)
  
• infections of the skin and soft tissues (pyoderma, furunculosis, etc.).
  

Contraindications:

• hypersensitivity to co-trimoxazole, trimethoprim, sulfonamides, or any component of the drug
  
• pregnancy
  
• lactation
  
• children up to 3 years (for this dosage form)
  
• established diagnosis of damage to the liver parenchyma severe renal failure, if it is not possible to determine the concentration of the drug in the blood plasma (not recommended for use in Cl creatinine <15 ml / min)
  
• severe hematological diseases (aplastic anemia, B12-deficiency anemia, agranulocytosis, leukopenia, megaloblastic anemia, hyperbilirubinemia in children associated with folic acid deficiency)
  
• the deficit glukozo-6-fosfatdegidrogenaza (the risk of hemolysis).
  

With caution: folic acid deficiency bronchial asthma thyroid disease.

Side effect:

Usually the drug is well tolerated.

From the nervous system: headache, dizziness, in some cases, aseptic meningitis, depression, apathy, tremor, peripheral neuritis.

Respiratory system: bronchospasm, choking, cough, pulmonary infiltrates.

From the digestive tract: nausea, vomiting, decreased appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of hepatic transaminases, hepatitis, sometimes with cholestatic jaundice, hepatonecrosis, pseudomembranous enterocolitis, pancreatitis.

Organs of hematopoiesis: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anaemia, aplastic and hemolytic anemia, eosinophilia, hypoprothrombinemia, methemoglobinemia.

From the urinary system: polyuria, interstitial nephritis, impaired renal function, crystalluria, hematuria, increased concentrations of urea, hypercreatinemia, toxic nephropathy with oliguria and anuria.

From the musculoskeletal system: arthralgia, myalgia.

Allergic reactions: itching, photosensitivity, urticaria, drug fever, rash, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, allergic myocarditis, fever, angioneurotic edema, hyperemia of the sclera.

Other: hypoglycemia, hyperkalemia, hyponatremia.

Drug interaction:

The drug is not recommended to take simultaneously with thiazide diuretics due to the risk of thrombocytopenia (bleeding). Co-trimoxazole increases anticoagulant activity of indirect anticoagulants, as well as the effect of hypoglycemic drugs and methotrexate. Reduces the intensity of liver metabolism of phenytoin (lengthens its T1 / 2 39%) and warfarin, increasing their effect.

Rifampicin reduces T1/2 of trimethoprim.

Pyrimethamine in doses exceeding 25 mg / week increases the risk of megaloblastic anemia.

Diuretics (usually thiazides) increase the risk of developing thrombocytopenia.

Benzocaine, procaine, procainamide and other drugs, as a result of hydrolysis of which PABK is formed, reduce the effect of the drug.

Between diuretics (including thiazides, furosemide) and oral hypoglycemic drugs (sulfonylurea derivatives) — on the one hand and antimicrobial sulfanilamides — on the other may develop cross-allergic reaction.

Phenytoin, barbiturates, PAS, increase the manifestations of deficiency folievoy acid.

Derivatives of salicylic acid enhance the effect of the drug.

Ascorbic acid, hexamethylentetramine and other drugs, acidifying urine, increase the risk of crystalluria.

Colestyramine reduces absorption, so it should be taken 1 h after or 4-6 h before taking co-trimoxazole.

Drugs that inhibit bone marrow hematopoiesis increase the risk of myelosuppression.

May increase plasma concentrations of digoxin in some elderly patients.

May reduce the effectiveness of tricyclic antidepressants.

In patients after kidney transplantation, taking co-trimoxazole and cyclosporine, there is a transient violation of the function of the transplanted kidney, manifested by an increase in the concentration of creatinine in the blood serum, which is likely caused by the action of trimethoprim.

Reduces the reliability of oral contraception (inhibits intestinal microflora and reduces intestinal-hepatic circulation of hormonal compounds).

Dosage and administration:

Inside, after eating, with enough liquid. The dose is set individually.

Children: from 3 to 5 years-2 table. (120 mg) 2 times a day from 6 to 12 years — 4 table. (120 mg) or 1 table. (480 mg) 2 times a day.

In pneumonia-100 mg/kg / day (per sulfamethoxazole), the interval between doses — 6 h, the course of treatment — 14 days.

With gonorrhea - 2 g (per sulfametoxazole) 2 times a day, with an interval of 12 hours.

Adults and children over 12 years — 960 mg twice a day with long — term therapy-480 mg twice a day. The duration of treatment-5-14 days in severe and / or chronic form of infectious disease single dose can be increased by 30-50%.

In case of extension of the course of treatment for more than 5 days and/or increase in the dose, hematological control is necessary in case of changes in the blood picture, folic acid should be prescribed at 5-10 mg per day.

Patients with renal failure: patients with Cl creatinine 15-30 ml / min should apply 1/2 standard dose with Cl creatinine <15 ml / min — co-trimoxazole is not recommended.

Overdose:

It is not known what dose of co-trimoxazole can be life-threatening.

Symptoms: sulfonamide overdose - lack of appetite, intestinal colic, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness. Perhaps the development of fever, hematuria, crystalluria, later-the oppression of the bone marrow and jaundice.

In case of an overdose of trimethoprim-nausea, vomiting, dizziness, headache, depression, consciousness disorder, bone marrow function oppression.

Treatment: withdrawal of the drug, gastric lavage (not later than 2 hours after taking the drug) or induction of vomiting, abundant drinking (if diuresis is insufficient, and kidney function is preserved). Introduction of calcium folinate-5-10 mg / day. Acidic urine environment accelerates the excretion of trimethoprim, but may also increase the risk of crystallization of sulfonamide in the kidneys.

Control of blood picture, composition of electrolytes in plasma and other biochemical parameters.

Hemodialysis is moderately effective, and peritoneal dialysis is ineffective.

Chronic overdose of co-trimoxazole (with high doses for a long period ) — inhibition of bone marrow function, manifested by thrombocytopenia, leukopenia or megaloblastic anemia.

Special instruction:

With caution, the drug is prescribed for folic acid deficiency in the body, bronchial asthma, burdened with an allergic history.

With long-term (over 1 month) courses of treatment, regular blood tests are necessary, since there is a probability of hematological changes (most often asymptomatic). These changes can be reversible in the appointment of folic acid at a dose of 3-6 mg/day, which does not significantly violate the antimicrobial activity of the drug. Particular care should be taken in the treatment of elderly patients or patients with suspected initial folate deficiency. The appointment of folic acid is also advisable for long-term treatment in high doses.

For the prevention of crystalluria is recommended to maintain a sufficient amount of urine. The probability of toxic and allergic complications from sulfonamides increases significantly with a decrease in the filtration function of the kidneys.

It is impractical to use food products containing large amounts of pabq — green parts of plants (cauliflower, spinach, legumes), carrots, tomatoes during treatment.

Excessive sun and UV radiation should be avoided.

The risk of side effects is much higher in AIDS patients.

It is not recommended for use in tonsillitis and pharyngitis caused by beta-hemolytic Streptococcus group A, because of the widespread resistance of strains.

Effects on laboratory results: trimethoprim may alter the results of determination of serum methotrexate levels by the enzymatic method, but does not affect the result when choosing a radioimmunological method. Co-trimoxazole may increase the 10% results of the reaction of Jaffe with picric acid (for quantitative determination of creatinine).