Biseptol tablets 480mg, No. 28

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

respiratory tract infections (including bronchitis, pneumonia, lung abscess, pleural empyema);

otitis media, sinusitis;

infections of the genitourinary system (including pyelonephritis, urethritis, salpingitis, prostatitis);

gonorrhea;

gastrointestinal tract infections (including typhoid fever, paratyphoid fever, bacterial dysentery, cholera, diarrhea);

infections of the skin and soft tissues (including furunculosis, pyoderma).

The drug is taken orally after meals with a sufficient amount of liquid. The dose is set individually.

For children aged 3 to 5 years, the drug is prescribed at 240 mg (2 tablets, 120 mg each) 2 times / day; children aged 6 to 12 years - 480 mg (4 tablets of 120 mg or 1 tablet of 480 mg) 2 times / day.

For 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 administration is 14 days.

With gonorrhea, the dose of the drug is 2 g (in terms of sulfamethoxazole) 2 times / day with an interval between doses of 12 hours.

For adults and children over 12 years of age, the drug is prescribed at 960 mg 2 times / day, with long-term therapy - 480 mg 2 times / day. The duration of the course of treatment is from 5 to 14 days.

In severe cases of the disease and / or in chronic infections, a single dose may be increased by 30-50%.

If the duration of the course of therapy is more than 5 days and / or an increase in the dose of the drug, it is necessary to control the picture of peripheral blood; when pathological changes appear, folic acid should be prescribed at a dose of 5-10 mg / day.

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, it is not recommended to use the drug.

Tablets are white with a yellowish sheen, round, flat, chamfered and engraved 'Bs'.

sulfamethoxazole, trimethoprim

• an established diagnosis of damage to the liver parenchyma;

• severe renal dysfunction in the absence of the ability to control the concentration of the drug in the blood plasma;

• severe renal failure (CC less than 15 ml / min);

• severe blood diseases (aplastic anemia, B12-deficiency anemia, agranulocytosis, leukopenia, megaloblastic anemia, anemia, hyperbilirubinemia in children associated with folic acid deficiency);

• deficiency of glucose-6-phosphate dehydrogenase (risk of hemolysis);

• simultaneous use with dofetelide, paclitaxel and amiodarone;

• simultaneous use with clozapine due to the ability of the latter to cause agranulocytosis;

• pregnancy;

• lactation;

• children under 3 years of age (for this dosage form);

• hypersensitivity to drug components;

• hypersensitivity to co-trimoxazole, trimethoprim, sulfonamides.

• The drug is prescribed with caution in case of folic acid deficiency in the body, bronchial asthma, thyroid diseases.

pharmachologic effect

Combined antibacterial drug containing sulfamethoxazole and trimethoprim. Sulfamethoxazole, which is structurally similar to PABA, disrupts the synthesis of dihydrofolic acid in bacterial cells, preventing the incorporation of PABA into its molecule. Trimethoprim enhances the effect of sulfamethoxazole, disrupting the reduction of dihydrofolic acid to tetrahydrofolic acid, the active form of folic acid, which is responsible for protein metabolism and microbial cell division. It is a broad-spectrum bactericidal drug. 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 enterotoxogenic strains), Salmonella spp. (including Salmonella typhi and Salmonella paratyphi),Vibrio cholerae, Bacillus anthracis, Haemophilus influenzae (including ampicillin-resistant strains), Listeria spp., Nocardia asteroides, Bordetella pertussis, Enterococcus faecalis, Klebsiella spp., Proteus Brucella spp., Pasteurella spp., Francispp. (including Mycobacterium leprae), Citrobacter spp., Enterobacter spp., Legionella pneumopbila, Providencia, some Pseudomonas species (except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp., Yersinia spp., Morganella spp., Pneumocystis car., Pneumocystis car. (including Chlamydia trachomatis, Chlamydia psittaci); protozoa - Plasmodium spp., Toxoplasma gondii; Actinomyces israelii; pathogenic fungi - Coccidioides immitis, Histoplasma capsulatum; Leishmania spp. Resistant to the drug: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis,Treponema spp., Leptospira spp., Viruses. It inhibits the vital activity of Escherichia coli, which leads to a decrease in the synthesis of thiamine, riboflavin, niacin and other B vitamins in the intestine. The duration of the therapeutic action is 7 hours.

Pharmacokinetics

Suction

After taking the drug inside, the active substances are completely absorbed from the gastrointestinal tract. Cmax in blood plasma is achieved within 1-4 hours after oral administration. Distribution Trimethoprim penetrates well into tissues and biological environments of the body: lungs, kidneys, prostate, bile, saliva, sputum, cerebrospinal fluid. Plasma protein binding of trimethoprim is 50%; sulfamethoxazole - 66%. Excretion of T1 / 2 trimethoprim - 8.6-17 hours, sulfamethoxazole - 9-11 hours. The main route of excretion is the kidneys; while trimethoprim is excreted unchanged up to 50%; sulfamethoxazole - 15-30% in active form. Side effects The drug is generally well tolerated. From the nervous system: headache, dizziness; in some cases - aseptic meningitis, depression, apathy, tremor, peripheral neuritis. From the respiratory system: bronchospasm,choking, cough, pulmonary infiltrates. From the digestive system: 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. From the hematopoietic system: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia, aplastic and hemolytic anemia, eosinophilia, hypoprothrombinemia, methemoglobinemia. From the urinary system: polyuria, interstitial nephritis, impaired renal function, crystalluria, hematuria, increased urea concentration, hypercreatininemia, 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, angioedema, scleral hyperemia. From the side of metabolism: hypoglycemia, hyperkalemia, hyponatremia.

Application for violations of liver function

The drug is contraindicated in case of established damage to the liver parenchyma.

Application for impaired renal function

The drug is contraindicated in severe renal impairment (CC less than 15 ml / min). In patients with renal insufficiency with a CC of 15-30 ml / min, the standard dose of the drug should be reduced by 50%.

Application in children

Contraindication: children under 3 years of age (for this dosage form).

Use in elderly patients

In elderly and senile patients, there is an increased risk of serious adverse reactions associated with the dose and duration of therapy.

special instructions

The drug should be prescribed only in cases where the advantage of such combination therapy over other antibacterial monopreparations outweighs the possible risk. Since the sensitivity of bacteria to antibacterial drugs in vitro varies in different geographic areas and over time, local characteristics of bacterial sensitivity should be taken into account when choosing a drug. Hypersensitivity and allergic reactions At the first appearance of a skin rash or any other severe adverse reaction, the drug should be discontinued. Patients with a tendency to allergic reactions and bronchial asthma should be prescribed BiseptolЃ with caution. Infiltrates in the lungs (like eosinophilic or allergic alveolitis) can present with symptoms such as cough or shortness of breath.If these symptoms appear or suddenly worsen, it is necessary to re-examine the patient and consider stopping treatment with BiseptolЃ. Renal disorders Sulfonamides, including BiseptolЃ, can increase urine output, especially in patients with edema caused by heart failure. Careful monitoring of renal function and serum potassium concentration is necessary in patients receiving high doses of BiseptolЃ (including in the treatment of pneumocystis pneumonia caused by Pneumocystis jirovecii), as well as in the following groups of patients: patients with a history of potassium metabolism disorders receiving standard doses of the drug; patients with renal insufficiency; patients receiving drugs that promote the development of hyperkalemia. Serious Adverse Reactions Fatalities have been reported.although rare, associated with such adverse reactions as blood abnormalities, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), drug rash with eosinophilia and systemic manifestations (DRESS syndrome), and fulminant liver necrosis.

Special patient groups

In elderly and senile patients, as well as in patients with concomitant diseases, for example, impaired renal and / or liver function, or while taking other drugs, there is an increased risk of severe adverse reactions; in these cases, the risk of development is related to the dose and duration of therapy. The duration of treatment with BiseptolЃ should be as short as possible, especially in elderly and senile patients. In case of impaired renal function, the dose should be adjusted according to the instructions in the section 'Dosage regimen'. Patients with severe renal impairment (CC 15-30 ml / min) receiving trimethoprim-sulfamethoxazole should be carefully monitored for the development of symptoms of toxicity (nausea, vomiting, hyperkalemia).For patients with severe hematological diseases, BiseptolЃ can be prescribed only as an exception. In elderly and senile patients, as well as in patients with pre-existing folic acid deficiency or renal failure, hematological changes characteristic of folic acid deficiency may occur. These changes disappear after folic acid administration. Due to the possibility of hemolysis, BiseptolЃ should not be prescribed to patients with glucose-6-phosphate dehydrogenase deficiency, except in the presence of absolute indications and only in minimal doses. As with any sulfonamides, caution should be exercised in patients with porphyria or thyroid dysfunction. Patients whose metabolism is characterized by 'slow acetylation'are more prone to developing idiosyncrasy towards sulfonamides.

Long-term therapy

With prolonged use of the drug BiseptolЃ, it is necessary to regularly determine the number of blood corpuscles. With a significant decrease in the number of any blood cells, BiseptolЃ should be canceled. Patients who have been receiving treatment with BiseptolЃ for a long time (especially with renal failure) should regularly do a general urine test and monitor kidney function. During treatment, sufficient fluid intake and adequate urine output should be ensured to prevent crystalluria.

Influence on the results of laboratory tests

Trimethoprim can alter the results of serum methotrexate measurements by the enzymatic method, but does not affect the results when choosing a radioimmunoassay. Co-trimoxazole can increase the results of the Jaffe reaction with picric acid for the quantitative determination of creatinine by 10%.

Influence on the ability to drive vehicles and use mechanisms

The drug, as a rule, does not affect the psychophysical abilities and the ability to service mechanisms and drive a vehicle. However, if unwanted symptoms such as headache, tremors, nervousness, feeling of fatigue appear, care should be taken when driving or servicing machinery.

Overdose

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. Bone marrow depression and jaundice may develop later. After acute poisoning with trimethoprim, nausea, vomiting, dizziness, headache, depression, disturbance of consciousness, depression of bone marrow function 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 for an extended period can lead to depression of bone marrow function, manifested by thrombocytopenia, leukopenia, or megaloblastic anemia. Treatment: withdrawal of the drug and taking action,aimed at removing it from the gastrointestinal tract (to wash the stomach no later than 2 hours after taking the drug or induce vomiting), drink plenty of fluids if diuresis is insufficient, and kidney function is preserved. Introduce calcium folinate (5-10 mg / day). The acidic environment of the urine accelerates the elimination of trimethoprim, but may also increase the risk of sulfonamide crystallization in the kidneys. The blood picture, the composition of plasma electrolytes and other biochemical parameters should be monitored. Hemodialysis is moderately effective and peritoneal dialysis is ineffective.plasma electrolyte composition and other biochemical parameters. Hemodialysis is moderately effective and peritoneal dialysis is ineffective.plasma electrolyte composition and other biochemical parameters. Hemodialysis is moderately effective and peritoneal dialysis is ineffective.

Drug interactions

With the simultaneous use of the drug 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 effect 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 effect. Rifampicin reduces the T1 / 2 of trimethoprim. With the simultaneous use of pyrimethamine in doses exceeding 25 mg / week, the risk of developing megaloblastic anemia increases. With the simultaneous use of diuretics (often thiazide), the risk of thrombocytopenia increases. Benzocaine, procaine, procainamide (like other drugs,as a result of hydrolysis of which PABA is formed) reduce the effectiveness of BiseptolЃ. Between diuretics (including thiazides, furosemide) and oral hypoglycemic agents (sulfonylurea derivatives), on the one hand, and antibacterial agents of the sulfonamide group, on the other hand, a cross-allergic reaction may develop. Phenytoin, barbiturates, PASK increase the manifestations of folic acid deficiency when used simultaneously with Biseptol. Salicylic acid derivatives enhance the effect of Biseptol. Ascorbic acid, hexamethylenetetramine (like other drugs that acidify urine) increase the risk of developing crystalluria while using Biseptol. Cholestyramine reduces absorption when taken simultaneously with other drugs,therefore, it should be taken 1 hour after or 4-6 hours before taking co-trimoxazole. With simultaneous use with drugs that inhibit bone marrow hematopoiesis, the risk of developing myelosuppression increases. BiseptolЃ may increase the concentration of digoxin in the blood plasma in some elderly patients. BiseptolЃ may decrease the effectiveness of tricyclic antidepressants. In patients after kidney transplantation with the simultaneous use of co-trimoxazole and cyclosporine, there is a passing dysfunction of the transplanted kidney, manifested by an increase in serum creatinine concentrations, which is probably caused by the action of trimethoprim. BiseptolЃ reduces the effectiveness of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal agents).With simultaneous use with drugs that inhibit bone marrow hematopoiesis, the risk of developing myelosuppression increases. BiseptolЃ can increase the concentration of digoxin in the blood plasma in some elderly patients. BiseptolЃ may decrease the effectiveness of tricyclic antidepressants. In patients after kidney transplantation with the simultaneous use of co-trimoxazole and cyclosporine, there is a passing dysfunction of the transplanted kidney, manifested by an increase in serum creatinine concentrations, which is probably caused by the action of trimethoprim. BiseptolЃ reduces the effectiveness of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal agents).With simultaneous use with drugs that inhibit bone marrow hematopoiesis, the risk of developing myelosuppression increases. BiseptolЃ may increase the concentration of digoxin in the blood plasma in some elderly patients. BiseptolЃ may decrease the effectiveness of tricyclic antidepressants. In patients after kidney transplantation with the simultaneous use of co-trimoxazole and cyclosporine, there is a passing dysfunction of the transplanted kidney, manifested by an increase in serum creatinine concentrations, which is probably caused by the action of trimethoprim. BiseptolЃ reduces the effectiveness of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal agents).the risk of developing myelosuppression increases. BiseptolЃ can increase the concentration of digoxin in the blood plasma in some elderly patients. BiseptolЃ may decrease the effectiveness of tricyclic antidepressants. In patients after kidney transplantation with the simultaneous use of co-trimoxazole and cyclosporine, there is a passing dysfunction of the transplanted kidney, manifested by an increase in serum creatinine concentrations, which is probably caused by the action of trimethoprim. BiseptolЃ reduces the effectiveness of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal agents).the risk of developing myelosuppression increases. BiseptolЃ can increase the concentration of digoxin in the blood plasma in some elderly patients. BiseptolЃ may decrease the effectiveness of tricyclic antidepressants. In patients after kidney transplantation with the simultaneous use of co-trimoxazole and cyclosporine, there is a passing dysfunction of the transplanted kidney, manifested by an increase in serum creatinine concentrations, which is probably caused by the action of trimethoprim. BiseptolЃ reduces the effectiveness of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal agents).In patients after kidney transplantation with the simultaneous use of co-trimoxazole and cyclosporine, there is a passing dysfunction of the transplanted kidney, manifested by an increase in serum creatinine concentrations, which is probably caused by the action of trimethoprim. BiseptolЃ reduces the effectiveness of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal agents).In patients after kidney transplantation with the simultaneous use of co-trimoxazole and cyclosporine, there is a passing dysfunction of the transplanted kidney, manifested by an increase in serum creatinine concentrations, which is probably caused by the action of trimethoprim. BiseptolЃ reduces the effectiveness of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal agents).