Biseptol concentrate 480mg, 5ml No. 10

• acute and chronic infections of the genitourinary organs: urethritis, pyelonephritis, cystitis, pyelitis, prostatitis, epididymitis, gonorrhea, chancre, lymphogranuloma venereum, inguinal granuloma;

• respiratory tract infections: bronchitis (acute and chronic) bronchiectasis, croupous pneumonia, bronchopneumonia, pneumocystis pneumonia, pleural empyema, lung abscess; ENT infections: otitis media, sinusitis, laryngitis, tonsillitis, scarlet fever;

• gastrointestinal tract infections: typhoid fever, paratyphoid fever, salmonella, cholera, dysentery, cholecystitis, cholangitis, gastroenteritis caused by enterotoxic strains of E. coli;

• infections of the skin and soft tissues: acne, furunculosis, pyoderma, abscess and wound infections, infections after surgery; sepsis, acute brucellosis, toxoplasmosis, osteomyelitis, osteoarticular infections, South American blastomycosis, malaria (Plasmodium falciparum), whooping cough (as part of complex therapy).

The drug should be administered intravenously drip after dilution (for example, 5% dextrose solution, 0.9% sodium chloride solution, Ringer's solution, or 0.45% sodium chloride solution with 2.5% dextrose solution). The infusion solution must be prepared immediately before administration by mixing thoroughly. After dilution, the resulting solution should be applied within 6 hours.

Do not use the drug as a rapid intravenous injection.

Adults and children over 12 years old are prescribed 960 mg (2 ampoules of 5 ml, diluted in 250 ml of solution) every 12 hours. In especially severe cases, 1440 mg (3 ampoules) should be prescribed 2-3 times / day.

For children under the age of 12, the daily dose is prescribed at the rate of 36 mg / kg of body weight in two equal doses. Patients with renal insufficiency (with creatinitis clearance of 15-30 ml / min) are prescribed 50% of the average therapeutic dose.

Concentrate for the preparation of solution for infusion in the form of a transparent, colorless or slightly yellowish liquid.

sulfamethoxazole

trimethoprim

Excipients: propylene glycol - 400 mg, ethanol 96% - 100 mg, benzyl alcohol - 15 mg, sodium disulfite (E223) - 1 mg, sodium hydroxide - 12.63 mg, sodium hydroxide 10% solution - up to pH 9.5-11.0, water d / and - up to 1 ml.

• megaloblastic anemia with folic acid deficiency, aplastic anemia, B12-deficiency anemia, agranulocytosis, leukopenia;

• deficiency of glucose-6-phosphate dehydrogenase;

• hyperbilirubinemia in children; hepatic and / or renal failure (creatinine clearance less than 15 ml / min);

• age up to 6 years (only for intramuscular injection);

• pregnancy;

• lactation period;

• increased individual sensitivity to sulfonamides or trimethoprim.

• The drug should not be used in premature babies, newborns and infants under 2 months of age.

• It is used with caution in case of folic acid deficiency, bronchial asthma, thyroid diseases, impaired liver and kidney function.

pharmachologic effect

Combined antibacterial drug containing sulfamethoxazole, which has an average duration of action, inhibits the synthesis of follic acid by competitive antagonism with para-aminobenzoic acid, as well as a trimetolrim inhibitor of bacterial reductase of dihydrofolic acid. The combination of both drugs gives an energic effect of antibacterial action, and therefore bacterial resistance is manifested less often than other drugs. Biseptol has a broad spectrum of antibacterial action. It is active against: Streptococcus (Streptococcus pneumoniae), Neisseria meningitidis, Neisseria gonorrhoeae (including enterotoxogenic strains), Staphylococcus, Escherichia coli, Klebsiella, Enterobacter, Proteus mirabilis, Proteus influenza spr., Haemella spp.(including Salmonella typhi and Salmonella paratyphi), Vibrio cholerae, Bacillus anthracis, Listeria spp., Nocardia asteroides, Bordclella pertussis, Enterococcus faecalis, Pasteurella spp., Brucella spp., Mycobacterium spp. (including Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumonia, Providencia, some Pseudomonas species (except P. aerugenosa), Serratia marcescens, Yersinia spp., Morganella spp., Chlamydia spp. (including Chlamydia trachomatis, Chlamydia psittaci), Shigella, Plasmodium spp., Toxoplasma gondii, Pneumocystis carini, Actinomyces israelii, Coccidioides immitis, Histoplasma capsulatum, Leishmania spp. Resistant to the drug: Corynebacterium spp., Pseudomonas aerugenosa, Mycobacterium tuberculosis, Troponema spp., Leptospira spp., Viruses. Suppresses the vital activity of E. coli,leads to a decrease in the synthesis of thiamine, riboflavin, niacin and other B vitamins in the intestine. The duration of the therapeutic effect is 7 hours.

Pharmacokinetics

The drug quickly penetrates into tissues and biological fluids of the body. Well distributed. Penetrates the BBB, the placental barrier and into breast milk. In the lungs and urine, it creates concentrations exceeding the content in plasma. To a lesser extent, they accumulate in bronchial secretions, vaginal secretions, secretions and tissues of the prostate gland, middle ear fluid, cerebrospinal fluid, bile, bones, saliva, aqueous humor of the eye, breast milk, interstitial fluid. The distribution of both drugs is different: sulfamethoxazole is distributed exclusively in the extracellular space, while trimethoprim is distributed both inside the cells and in the extracellular space. Plasma protein binding - 66% for sulfamethoxazole, for trimethoprim - 45%. Both drugs are metabolized in the liver.Sulfamethoxazole is metabolized to a greater extent (with the formation of acetylated derivatives), metabolites do not have antimicrobial activity. Excreted by the kidneys, both by filtration and by active secretion by the tubules, in the form of metabolites (80% within 72 hours) and unchanged (20% sulfamethoxazole, 50% trimethoprim), the concentration of active substances in the urine is much higher than in the blood ... A small amount of the drug is excreted through the intestines. T1 / 2 of sulfamethoxazole - 9-11 hours, trimethoprim - 10-12 hours, in children - significantly less and depends on age: up to the first year - 7-8 hours, 1-10 years - 5-6 hours. renal function T1 / 2 increases.in the form of metabolites (80% within 72 hours) and unchanged (20% sulfamethoxazole, 50% trimethoprim), the concentration of active substances in the urine is much higher than in the blood. A small amount of the drug is excreted through the intestines. T1 / 2 of sulfamethoxazole - 9-11 hours, trimethoprim - 10-12 hours, in children - significantly less and depends on age: up to the first year - 7-8 hours, 1-10 years - 5-6 hours. renal function T1 / 2 increases.in the form of metabolites (80% within 72 hours) and unchanged (20% sulfamethoxazole, 50% trimethoprim), the concentration of active substances in the urine is much higher than in the blood. A small amount of the drug is excreted through the intestines. T1 / 2 of sulfamethoxazole - 9-11 hours, trimethoprim - 10-12 hours, in children - significantly less and depends on age: up to the first year - 7-8 hours, 1-10 years - 5-6 hours. renal function T1 / 2 increases.In the elderly and patients with impaired renal function, T1 / 2 increases.In the elderly and patients with impaired renal function, T1 / 2 increases.

Side effect

Biseptol is usually well tolerated by patients. However, the following effects can be observed: From the gastrointestinal tract: anorexia, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of hepatic transaminases, hepatitis, pseudomembranous enterocolitis, nausea, vomiting, diarrhea, liver necrosis. From the side of the central nervous system: headaches and dizziness. In some cases - aseptic meningitis, depression, apathy, tremor, peripheral neuritis. From the respiratory system: bronchospasm, pulmonary infiltrates. From the side of hematopoiesis: rarely - neutropenia, agranulocytosis, megaloblastic anemia, leukopenia, thrombocytopenia, hypoprothrombinemia. From the urinary system: polyuria, interstitial nephritis, impaired renal function, crystalluria, hematuria, increased urea, hypocreatininemia,toxic nephropathy with oliguria and anuria. From the musculoskeletal system: arthralgia, myalgia. Allergic reactions: skin rashes and itching, photosensitivity, rash, erythema polymorphism, exfoliative dermatitis, allergic myocarditis, fever, Quincke's edema, redness of the sclera. Local reactions: thrombophlebitis (at the site of venipuncture), soreness at the injection site. Others: hypoglycemia

Application during pregnancy and lactation

The drug should not be prescribed during pregnancy and during breastfeeding.

Application for violations of liver function

Contraindicated: liver failure.

Application for impaired renal function

Contraindicated: renal failure, creatinine clearance less than 15 ml / min. Patients with renal insufficiency (with creatinitis clearance of 15-30 ml / min) are prescribed 50% of the average therapeutic dose.

Application in children

The drug should not be used in premature babies, newborns and infants under 2 months of age. For children under the age of 12, the daily dose is prescribed at the rate of 36 mg / kg of body weight in two equal doses.

Use in elderly patients

Elderly patients are recommended to additionally prescribe folic acid (3-6 mg / day), which does not significantly violate the antimicrobial activity of the drug. Particular caution should be exercised when treating elderly patients with suspected baseline folate deficiency.

special instructions

In AIDS patients treated with cotrimoxazole, due to infection with Pneumocystis carinii, undesirable effects are more often observed: skin rashes, fever, leukopenia. It is advisable to determine the plasma concentration of sulfamethoxazole every 2-3 days immediately before the next infusion. If the concentration of sulfamethoxazole exceeds 150 ?g / ml, treatment should be interrupted until it drops below 120 ?g / ml. With long-term treatment, it is necessary to systematically conduct studies of peripheral blood, the functional state of the liver and kidneys. Elderly patients are recommended to additionally prescribe folic acid (3-6 mg / day), which does not significantly violate the antimicrobial activity of the drug. Particular caution should be exercised when treating elderly patients with suspected baseline folate deficiency.For the prevention of crystalluria, it is recommended to maintain a sufficient volume of excreted urine. The likelihood of toxic and allergic complications of sulfonamides increases significantly with complications of the filtration function of the kidneys. It is also impractical to eat foods containing large amounts of PABA-green plant parts (cauliflower, spinach, legumes), carrots, and tomatoes during treatment. Excessive sun and ultraviolet radiation should be avoided. It is not recommended for use in tonsillitis, pharyngitis caused by group A beta-hemolytic streptococcus due to widespread resistance of the strains.It is also inappropriate to eat foods containing large amounts of PABA-green plant parts (cauliflower, spinach, legumes), carrots, and tomatoes during treatment. Excessive sun and ultraviolet radiation should be avoided. It is not recommended for use in tonsillitis, pharyngitis caused by group A beta-hemolytic streptococcus due to widespread resistance of the strains.It is also inappropriate to eat foods containing large amounts of PABA-green plant parts (cauliflower, spinach, legumes), carrots, and tomatoes during treatment. Excessive sun and ultraviolet radiation should be avoided. It is not recommended for use in tonsillitis, pharyngitis caused by group A beta-hemolytic streptococcus due to widespread resistance of the strains.

Influence on the ability to drive vehicles and use mechanisms

The drug does not affect the ability to drive vehicles and service moving machinery.

Overdose

Symptoms: nausea, vomiting, intestinal colic, dizziness, headache, drowsiness, depression, fainting, confusion, blurred vision, fever, hematuria, crystalluria; with prolonged overdose - thrombocytopenia, leukopenia, megaloblastic anemia, jaundice. Treatment: gastric lavage, acidification of urine increases excretion of trimethoprim, fluid intake, intramuscularly - 5-15 mg / day, calcium folinate (eliminates the effect of trimethoprim on the bone marrow), with inhibition of the hematopoietic functions of the bone marrow caused by trimethoprim, to stimulate erythropoiesis use drugs of folic acid intramuscularly (3-6 mg / day. The course of treatment - 5-7 days), if necessary - hemodialysis.

Drug interactions

Biseptol enhances the effect of phenytoin, oral hypoglycemic agents, warfarin derivatives (prolongation of prothrombin time, bleeding). In elderly patients, in combination with diuretics (in particular, with thiazide diuretics), the risk of thrombocytopenia increases. Simultaneous use with cyclosporine reduces its concentration in the blood. The drug should not be administered intravenously in combination with drugs and solutions containing bicarbonates. Biseptol is pharmaceutically compatible with the following drugs: dextrose for intravenous infusions 5%, sodium chloride for intravenous infusions 0.9%, a mixture of 0.18% sodium chloride and 4% dextrose for intravenous infusions, 6% dextran 70 for intravenous infusions in 5% dextrose or saline, 10% dextran 40 for IV infusion in 5% dextrose or saline,Ringer's solution for injection. Increases the anticoagulant activity of indirect coagulants, enhances the effect of hypoglycemic agents and methotrexate. Reduces the intensity of hepatic metabolism of phenytoin (lengthens its T1 / 2 by 39%) and warfarin, enhancing their effect. Rifampicin reduces the T1 / 2 of trimethoprim. Pyrimethamine in doses exceeding 25 mg / week increases the risk of megaloblastic anemia. Diuretics (usually thiazides) increase the risk of thrombocytopenia. Reduce the effect of benzocaine, procaine, procainamide and other drugs, as a result of hydrolysis of which PABA is formed. Between diuretics (thiazides, furosemide, etc.) and oral hypoglycemic drugs (sulfonylurea derivatives), on the one hand, and antimicrobial sulfonamides, on the other, a cross-allergic reaction may develop. Pheninoin,barbiturates, PASK increase the manifestations of folic acid deficiency. Salicylic acid derivatives enhance the effect. Ascorbic acid, hexamethylenetetramine and other drugs that acidify urine increase the risk of crystalluria. Colesteramine reduces absorption, so it should be taken 1 hour after or 4-6 hours before taking cotrimoxazole. Reduces the reliability of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal compounds).therefore, it should be taken 1 hour after or 4-6 hours before taking cotrimoxazole. Reduces the reliability of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal compounds).therefore, it should be taken 1 hour after or 4-6 hours before taking cotrimoxazole. Reduces the reliability of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal compounds).