- sulfamethoxazole 400 mg
- Trimethoprim 80 mg
Excipients: potato starch, talc, magnesium stearate, polyvinyl alcohol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, propylene glycol.
Clinico-pharmacological group: Antibacterial sulfanilamide drug
Pharmaco-therapeutic group: Antimicrobial combined agent
The combined antibacterial drug contains sulfamethoxazole and trimethoprim.
Sulfamethoxazole, similar in structure to PABA, disrupts the synthesis of dihydrofolic acid in bacterial cells, preventing the inclusion of PABA in its molecule.
Trimethoprim enhances the action of sulfamethoxazole by disrupting the reduction of dihydrofolic acid to tetrahydrofolic acid, the active form of folic acid responsible for protein metabolism and the division of microbial cells.
Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug:
- respiratory tract infections (including bronchitis, pneumonia, lung abscess, pleural empyema);
- otitis, sinusitis;
- infections of the genitourinary system (including pyelonephritis, urethritis, salpingitis, prostatitis);
- gastrointestinal infections (including typhoid fever, paratyphoid fever, bacterial dysentery, cholera, diarrhe
- infections of the skin and soft tissues (including furunculosis, pyoderma).
Active against gram-positive aerobic bacteria: Streptococcus spp., Including Streptococcus pneumoniae (hemolytic strains are more susceptible to penicillin), Staphylococcus spp., Bacillus anthracis, Listeria spp., Nocardia asteroides, Enterococcus faeceecerosis Icerosis Icerosis Icerosis, Ibero ster., Listeria spp., Nocardia ster. (including Mycobacterium leprae, excluding Mycobacterium tuberculosis); Gram-negative aerobic bacteria: Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (including enterotoxogenic strains), Salmonella spp. (including Salmonella typhi and Salmonella paratyphi);
Vibrio cholerae, Haemophilus influenzae (including ampicillin-resistant strains), Bordetella pertussis, Klebsiella spp., Proteus spp., Pasteurella spp., Francisella tularensis, Brucella spp., Citrobacter spp., Enterobacter spp. some species of Pseudomonas (except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp., Yersinia spp., Morganella spp., as well as for Chlamydia spp. (including Chlamydia trachomatis, Chlamydia psittaci); against gram-positive anaerobes: Actinomyces israelii; for the simplest: Plasmodium spp., Toxoplasma gondii; pathogenic fungi: Coccidioides immitis, Histoplasma capsulatum, Pneumocystis carinii, Leishmania spp.
Resistant to the drug: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira spp., Viruses.
Inhibits the vital activity of Escherichia coli, which leads to a decrease in the synthesis of thiamine, riboflavin, nicotinic acid and other B vitamins in the intestine.
The duration of therapeutic action is 7 hours.
After taking the drug inside the active substances are completely absorbed from the gastrointestinal tract. Cmax in plasma is reached within 1-4 hours after ingestion.
Trimethoprim penetrates well into the tissues and biological environment of the body: lungs, kidneys, prostate, bile, saliva, sputum, cerebrospinal fluid. The binding of trimethoprim to plasma proteins is 50%; sulfamethoxazole - 66%.
T1 / 2 trimethoprim - 8.6-17 h, sulfamethoxazole - 9-11 h. The main route of elimination is the kidneys; while trimethoprim is displayed in unchanged form up to 50%; sulfamethoxazole - 15-30% in active form.
- established damage to the liver parenchyma;
- pronounced renal dysfunction in the absence of the ability to control the drug concentration in the blood plasma;
- renal failure severe (CC less than 15 ml / min);
- severe blood diseases (aplastic anemia, B12-deficient anemia, agranulocytosis, leukopenia, megaloblastic anemia, anemia associated with folic acid deficiency);
- hyperbilirubinemia in children;
- deficiency of glucose-6-phosphate dehydrogenase (risk of hemolysis);
- children's age up to 3 years (for this dosage form);
- hypersensitivity to the drug;
- Hypersensitivity to sulfonamides.
With caution prescribed with a folic acid deficiency in the body, asthma, diseases of the thyroid gland.
The drug is usually well tolerated.
Of the nervous system: headache, dizziness; in some cases - aseptic meningitis, depression, apathy, tremor, peripheral neuritis.
On the part of the respiratory system: bronchospasm, asphyxiation, cough, pulmonary infiltrates.
On the part of the digestive system: nausea, vomiting, loss of appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of hepatic transaminases, hepatitis, sometimes with cholestatic jaundice, hepatonecrosis, pseudomembranous enterocolitis, pancreatitis.
On the part of the hematopoietic system: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia, aplastic and hemolytic anemia, eosinophilia, hypoprothrombinemia, methemoglobinemia.
On the part of the urinary system: polyuria, interstitial nephritis, renal dysfunction, crystalluria, hematuria, increased urea concentration, hypercreatininemia, toxic nephropathy with oliguria and anuria.
From the musculoskeletal system: arthralgia, myalgia.
Allergic reactions: pruritus, photosensitization, urticaria, drug fever, rash, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome), exfoliative dermatitis, allergic myocarditis, elevation of the organism, elevation of the body mass, elevation of the organism, erythema; hyperemia sclera.
Metabolism: hypoglycemia, hyperkalemia, hyponatremia.
With the simultaneous use of Biseptol with thiazide diuretics, there is a risk of thrombocytopenia and bleeding (the combination is not recommended). Co-trimoxazole increases the anticoagulant activity of indirect anticoagulants, as well as the action of hypoglycemic drugs and methotrexate. Co-trimoxazole reduces the intensity of hepatic metabolism of phenytoin (increases its T1 / 2 by 39%) and warfarin, enhancing their action. Rifampicin reduces T1 / 2 trimethoprim.
With simultaneous use of pyrimethamine in doses exceeding 25 mg / week., Increases the risk of megaloblastic anemia.
With simultaneous use of diuretics (often thiazides) increase the risk of thrombocytopenia.
Benzocaine, procainum, procainamide (like other drugs, the hydrolysis of which produces PABA) reduces the effectiveness of Biseptol.
Between diuretics (including thiazides, furosemide) and oral hypoglycemic agents (sulfonylurea derivatives), on the one hand, and sulfonamide antibacterial agents, on the other hand, a cross-allergic reaction is possible.
Phenytoin, barbiturates, PAS increase the manifestations of folic acid deficiency while using with Biseptol.
Derivatives of salicylic acid enhance the effect of Biseptol.
Ascorbic acid, hexamethylenetetramine (like other urinary acidifying drugs) increase the risk of crystalluria during the use of Biseptol.
Kolestiramin reduces absorption while taking it with other drugs, so it should be taken 1 h after or 4-6 h before taking co-trimoxazole.
With simultaneous use with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases.
In some cases, Biseptol® can increase the concentration of digoxin in the blood plasma of elderly patients.
Biseptol® can reduce the effectiveness of tricyclic antidepressants.
Patients after kidney transplantation, with simultaneous use of co-trimoxazole and cyclosporine, show a dysfunction of the transplanted kidney, manifested by an increase in serum creatinine concentrations, which is probably caused by the action of trimethoprim.
It reduces the effectiveness of oral contraception (inhibits the intestinal microflora and reduces the enterohepatic circulation of hormonal drugs).
How to take, the course of administration and dosage
The drug is taken orally after a meal, drinking a sufficient amount of liquid. Dose set individually.
Children aged 3 to 5 years, the drug is prescribed 240 mg (2 tab. 120 mg) 2 times / day; children aged 6 to 12 years old - 480 mg each (4 tablets of 120 mg or 1 tablet of 480 mg) 2 times / day.
In pneumonia, the drug is prescribed at the rate of 100 mg of sulfamethoxazole per 1 kg of body weight / day. The interval between doses is 6 hours, the duration of treatment is 14 days.
In gonorrhea, the dose of the drug is 2 g (in terms of sulfamethoxazole) 2 times / day with an interval between doses of 12 hours.
Adults and children over 12 years old are prescribed 960 mg 2 times / day, with long-term therapy, 480 mg 2 times / day.
Duration of treatment is from 5 to 14 days. In severe cases of the disease and / or in chronic infections, a single dose may increase by 30-50%.
With the duration of the course of therapy for more than 5 days and / or increasing the dose of the drug, it is necessary to monitor the picture of peripheral blood; when pathological changes occur, folic acid should be administered at a dose of 5-10 mg / day.
In case of missing a dose, the drug should be taken as soon as possible. If the time of the next dose is coming, the previous dose should be skipped. Do not take a double dose in order to compensate for the missed.
In patients with renal insufficiency with a CC of 15-30 ml / min, the standard dose of the drug should be reduced by 50%, with a CC of less than 15 ml / min, the drug is not recommended.
Symptoms: in case of an overdose of sulfonamide - lack of appetite, intestinal colic, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness, fever, hematuria, crystalluria are also possible. Later, bone marrow depression and jaundice may develop.
After acute poisoning with trimethoprim, nausea, vomiting, dizziness, headache, depression, disorder of consciousness, and bone marrow function depression are possible.
It is not known what dose of co-trimoxazole can be life threatening.
Chronic poisoning: the use of co-trimoxazole in high doses over a prolonged period can lead to inhibition of bone marrow function, manifested by thrombocytopenia, leukopenia or megaloblastic anemia.
Treatment: removal of the drug and taking measures aimed at its removal from the gastrointestinal tract (gastric lavage should be performed no later than 2 hours after taking the drug or cause vomiting), drink plenty of water if diuresis is insufficient, and the kidney function is preserved. Introduce calcium folinate (5-10 mg / day). Acid urine accelerates excretion of trimethoprim, but may also increase the risk of sulfonamide crystallization in the kidneys.
The blood picture, electrolyte composition in plasma and other biochemical parameters should be monitored. Hemodialysis is moderately effective, and peritoneal dialysis is ineffective.
Be wary prescribed drug Biseptol with burdened allergic history.
With long (more than a month) courses of treatment, regular blood tests are necessary, since there is a likelihood of hematological changes (most often asymptomatic). These changes may be reversible with the appointment of folic acid (3-6 mg / day.), Which does not significantly violate the antimicrobial activity of the drug. Special care is needed in the treatment of elderly patients or patients with suspected initial folate deficiency. Appointment of folic acid is also advisable with long-term drug treatment in high doses.
For the prevention of crystalluria, it is recommended to maintain a sufficient amount of excreted urine. The probability of toxic and allergic complications of sulfonamides increases significantly with a decrease in the filtration function of the kidneys.
Against the background of treatment, it is also inappropriate to eat foods containing a large amount of PABA — green parts of plants (cauliflower, spinach, legumes), carrots, and tomatoes.
Excessive solar and UV radiation should be avoided.
The risk of side effects is significantly higher in AIDS patients.
It is not recommended to use the drug Biseptol for tonsillitis and pharyngitis caused by β-hemolytic streptococcus group A, due to the widespread resistance of the strains.
Trimethoprim can change the results of the determination of the level of methotrexate in serum, carried out by the enzymatic method, but does not affect the result when choosing a radioimmunological method.
Co-trimoxazole can increase by 10% the results of the reaction of Jaffe with picric acid for the quantitative determination of creatinine.
|Active substance||Trimethoprim / Sulfamethoxazole|
|Pills in 1 package||28|
|Expiration Date (in months)||60|
|Country of origin||Russia|