Biseptol 480
Biseptol 480: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Biseptol 480
ATX code: J01EE01
Active ingredient: co-trimoxazole (sulfamethoxazole + trimethoprim)
Manufacturer: JSC "Warsaw Pharmaceutical Plant Polfa" (Poland)
Description and photo update: 2018-22-10
Prices in pharmacies: from 85 rubles.
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Biseptol 480 is an antimicrobial combined sulfonamide drug.
Release form and composition
The dosage form of Biseptol 480 is a concentrate for the preparation of a solution for infusion: a transparent, colorless or light yellow liquid with a characteristic smell of ethanol (5 ml in ampoules, in a cardboard box 2 contour packs or 10 ampoules without packaging).
The composition of the concentrate for 1 ml / 1 ampoule:
- active ingredients: sulfamethoxazole - 80/400 mg; trimethoprim - 16/80 mg;
- excipients: sodium hydroxide, sodium metabisulfite, propylene glycol, benzyl alcohol, ethanol, water for injection.
Pharmacological properties
Pharmacodynamics
Biseptol 480 is a combined antibacterial drug. The active ingredients in its composition are: sulfamethoxazole - an effective antimicrobial agent of medium duration of action that inhibits the synthesis of folic acid by competitive antagonism with para-aminobenzoic acid; Trimethoprim is a bacteriostatic antibiotic that inhibits bacterial dihydrofolic acid reductase. Their combination gives a synergistic antibacterial action, and therefore the effectiveness of such a complex is much higher in comparison with the action of other drugs.
Biseptol 480 is a broad-spectrum antibiotic; shows its activity against the following microorganisms: Streptococcus (Streptococcus pneumoniae), Neisseria gonorrhoeae (enterotoxogenic strains inclusive), Neisseria meningitidis, Staphylococcus, Klebsiella, Escherichia coli, Haemophilus influenzae, Proteus spobacter., (Salmonella typhi and Salmonella paratyphi inclusive), Vibrio cholerae, Bacillus anthracis, Listeria spp., Nocardia asteroides, Bordetella pertussis, Enterococcus faecalis, Pasteurella spp., Brucella spp., Mycobacterium spp. (Mycobacterium leprae inclusive), Enterobacter spp., Citrobacter, Legionella pneumonia, Providencia, selected Pseudomonas species (excluding P. aeruginosa), Serratia marcescens, Morganella spp., Yersinia spp., Chlamydia spp.(Chlamydia trachomatis and Chlamydia psittaci inclusive), Actinomyces israelii, Shigella, Toxoplasma gondii, Plasmodium spp., Pneumocystis carinii, Histoplasma capsulatum, Coccidioides immitis, Leishmania spp.
Microorganisms showing resistance to Biseptol 480: Corynebacterium spp., Mycobacterium tuberculosis, Pseudomonas aeruginosa, Leptospira spp., Troponema spp. and viruses.
The drug inactivates the vital activity of E. coli, leads to a decrease in the synthesis of riboflavin, thiamine, nicotinic acid, and other B vitamins in the intestine. The duration of the therapeutic effect is 7 hours.
Pharmacokinetics
Biseptol 480 penetrates into the tissues of the body and its biological fluids quickly and is well distributed in them. The drug penetrates the blood-brain barrier (BBB), the histohematogenous barrier, is excreted in breast milk. Its concentration in urine and lungs significantly exceeds plasma concentration. In vaginal secretions, bronchial secretions, bones, saliva, tissues and secretions of the prostate gland, breast milk, middle ear fluid, bile, cerebrospinal fluid, aqueous humor of the eye, interstitial fluid, sulfamethoxazole and trimethoprim accumulate to a lesser extent. Both active components are distributed in different ways: sulfamethoxazole - only in the extracellular space, and trimethoprim - both outside the cells and inside them. 66% of sulfamethoxazole and 45% of trimethoprim bind to plasma proteins.
Both drugs are metabolized in the liver. Sulfamethoxazole is metabolized to a greater extent, forming acetylated derivatives - metabolites that do not have antimicrobial activity.
Biseptol 480 is excreted by the kidneys both by glomerular filtration and by active tubular secretion. Up to 80% of the drug is excreted within 72 hours in the form of metabolites; unchanged 20% sulfamethoxazole and 50% trimethoprim are excreted. In urine, the concentration of active substances is higher than in blood plasma. Through the intestines, the drug is excreted in a small amount. The half-life (T1 / 2) for sulfamethoxazole is 9-11 hours, for trimethoprim - 10-12 hours. In children, this indicator is significantly less and depends on the child's age: in the first year of life, it is 7-8 hours, from 1 year to 10 years - 5-6 hours. T1 / 2 increases in elderly patients with impaired renal function.
Indications for use
- Gastrointestinal infections: paratyphoid fever, typhoid fever, cholera, salmonella, dysentery, cholangitis, cholecystitis caused by enterotoxic strains of Escherichia coli gastroenteritis;
- infections of the organs of the reproductive and urinary systems in acute and chronic course: pyelitis, pyelonephritis, urethritis, cystitis, epididymitis, prostatitis, chancre, gonorrhea, inguinal granuloma, lymphogranuloma venereum;
- infectious lesions of the ENT organs: tonsillitis, otitis media, laryngitis, sinusitis, scarlet fever;
- infections of the upper and lower respiratory tract: acute and chronic bronchitis, croupous pneumonia, bronchiectasis, pneumocystis pneumonia, bronchopneumonia, lung abscess, pleural empyema;
- infections of the skin and soft tissues: pyoderma, acne, furunculosis, wound infections and abscess, infection after surgery;
- other infectious diseases: sepsis, toxoplasmosis, acute brucellosis, osteoarticular infections, osteomyelitis, malaria (Plasmodium falciparum), South American blastomycosis, whooping cough (as part of complex treatment).
Contraindications
Absolute contraindications:
- liver failure;
- renal failure with creatinine clearance (CC) less than 15 ml / min;
- megaloblastic anemia due to vitamin B 9 (folic acid) deficiency, aplastic anemia, agranulocytosis, B 12 deficiency anemia, leukopenia;
- deficiency of glucose-6-phosphate dehydrogenase;
- hyperbilirubinemia in children;
- intramuscular administration of the drug to children under 6 years of age;
- neonatal period and age up to 2 months;
- period of pregnancy and lactation;
- individual hypersensitivity to sulfa drugs, trimethoprim and (or) other components of Biseptol 480.
The drug is used with caution in case of vitamin B 9 deficiency, bronchial asthma, impaired liver / kidney function, thyroid diseases.
Instructions for the use of Biseptol 480: method and dosage
The solution prepared from the Biseptol 480 concentrate must be administered intravenously (IV) by drop. Do not use the drug as a quick intravenous injection.
To dilute the Biseptol 480 concentrate, the following infusion solutions may be used: 5 and 10% dextrose solutions; 0.9% NaCl solution; 0.45% NaCl solution with 2.5% dextrose solution; Ringer's solution.
Recommended dosage:
- children under 12 years of age: the daily dose is determined at the rate of 36 mg per kg of body weight and is divided into 2 administrations in equal amounts;
- children over 12 years old and adult patients: 960 mg (10 ml or 2 ampoules) 1 time in 12 hours; if necessary, it is allowed to increase a single dose to 1440 mg (15 ml or 3 ampoules), 2-3 times a day.
It is recommended to dilute Biseptol 480 concentrate in the following proportions:
- 5 ml (1 ampoule) of the drug - 125 ml of infusion solution;
- 10 ml (2 ampoules) of the drug - 250 ml of infusion solution;
- 15 ml (3 ampoules) of the drug - 500 ml of infusion solution.
The prepared solution of Biseptol 480 should not be mixed with infusion solutions other than those listed above, or with other drugs.
For patients with renal insufficiency with CC from 15 to 30 ml / min, the dose of the drug is reduced by 1/2 of the average therapeutic dose.
Side effects
When used according to the indications in compliance with the dosage regimen, Biseptol 480 is usually well tolerated by patients, but the following side effects are possible:
- central nervous system: headaches, dizziness; in some cases - apathy, depression, tremor, aseptic meningitis, peripheral neuritis;
- Gastrointestinal tract: vomiting, nausea, diarrhea, anorexia, abdominal pain, gastritis, glossitis, stomatitis, increased activity of liver enzymes, cholestasis, hepatitis, pseudomembranous enterocolitis, liver necrosis;
- respiratory system: bronchospasm, infiltration of lung tissue;
- hematopoietic organs: rarely - leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia, hypoprothrombinemia;
- urinary system: impaired renal function, interstitial nephritis, polyuria, hematuria, crystalluria, hypocreatininemia, increased urea levels, toxic nephropathy with a decrease in urine output to oliguria and anuria;
- musculoskeletal system: myalgia, arthralgia;
- hypersensitivity reactions: rash, pruritus, erythema polymorphism, exfoliative dermatitis, photosensitivity, allergic myocarditis, hyperthermia, redness of the sclera, Quincke's edema;
- reactions at the injection site: soreness, thrombophlebitis;
- others: hypoglycemia.
Overdose
Symptoms of an overdose of Biseptol 480 are intestinal colic, nausea, vomiting, headache, dizziness, depression, fainting, drowsiness, confusion, fever, blurred vision, crystalluria, hematuria; due to prolonged overdose, leukopenia, thrombocytopenia, jaundice, megaloblastic anemia are possible.
To treat the condition, you must:
- flush the patient's stomach;
- ensure the administration of drugs that cause acidification of urine to enhance the elimination of trimethoprim;
- increase fluid intake;
- to eliminate the effect of trimethoprim on the bone marrow, inject intramuscularly calcium folinate at a dose of 5–15 mg / day;
- to stimulate erythropoiesis when trimethoprim inhibits the hematopoietic functions of the bone marrow, inject intramuscularly folic acid preparations at a dose of 3–6 mg / day, for a course of 5–7 days;
- if necessary, carry out hemodialysis.
special instructions
When using Biseptol 480 in patients with acquired immunodeficiency syndrome (AIDS) using co-trimoxazole for the treatment of pneumocystis pneumonia, such undesirable effects as hyperthermia, skin rashes, and leukopenia are more often observed.
It is advisable to determine the concentration of sulfamethoxazole in plasma every 2-3 days immediately before the next infusion; if its value is> 150 μg / ml, then therapy should be interrupted until the plasma indicator drops to 120 μg / ml.
Long-term treatment is required under the systematic monitoring of the functional state of the liver and kidneys, as well as the parameters of peripheral blood.
In order to prevent crystalluria in patients, it is necessary to maintain the volume of excreted urine in a sufficient amount.
Due to the deterioration of the filtration function of the kidneys, the likelihood of allergic and toxic complications increases significantly when using sulfonamides.
Against the background of treatment, it is inappropriate to eat foods containing para-aminobenzoic acid (PABA) in large quantities - tomatoes, carrots and green parts of vegetables (cauliflower, spinach, legumes).
Due to the possible increase in photosensitization when using Biseptol 480, excessive solar and artificial ultraviolet radiation should be avoided.
It is not recommended to use an antibiotic for pharyngitis and tonsillitis caused by group A beta-hemolytic streptococcus due to the widespread prevalence of resistant strains.
Influence on the ability to drive vehicles and complex mechanisms
The drug has no effect on the ability to perform types of work that require a high concentration of attention and speed of psychomotor reactions.
Application during pregnancy and lactation
According to the instructions, Biseptol 480 is contraindicated in pregnant and lactating women.
Pediatric use
The appointment of Biseptol 480 is contraindicated in premature babies, newborns and infants up to the 2nd month of life.
With impaired renal function
- renal failure with CC <15 ml / min - the use of Biseptol 480 is contraindicated;
- renal failure with CC 15-30 ml / min - it is recommended to use 1/2 of the average therapeutic dose.
For violations of liver function
The appointment of co-trimoxazole is contraindicated in liver failure.
Use in the elderly
Elderly patients receiving treatment with Biseptol 480 are recommended to additionally prescribe folic acid at a dose of 3–6 mg / day; the antimicrobial activity of the drug is not significantly affected by this combination. Treatment of elderly patients with suspected baseline folate deficiency requires special care.
Drug interactions
The Biseptol 480 concentrate is pharmaceutically compatible with the following solutions: 5 and 10% dextrose (glucose) solutions; 0.9% NaCl solution; 0.45% NaCl solution with 2.5% dextrose (glucose) solution; Ringer's solution.
Possible drug interactions of Biseptol 480 with other substances / drugs:
- phenytoin, oral hypoglycemic agents, warfarin derivatives: their effect is enhanced, prothrombin time and the duration of bleeding are prolonged;
- diuretics (including thiazide diuretics): the risk of thrombocytopenia increases in elderly patients;
- cyclosporine: its concentration in the blood decreases;
- medicinal products and solutions containing bicarbonates: simultaneous intravenous administration with co-trimoxazole is prohibited;
- indirect coagulants: their anticoagulant activity increases;
- hypoglycemic agents and methotrexate: their effectiveness is increased;
- rifampicin: reduces the T1 / 2 of trimethoprim;
- phenytoin and warfarin: the intensity of hepatic metabolism decreases and their effect increases; T1 / 2 of phenytoin is extended by 39%;
- pyrimethamine (at doses> 25 mg per week): increases the likelihood of megaloblastic anemia;
- diuretics (mainly thiazide): increase the risk of thrombocytopenia;
- procaine, procainamide, benzocaine, and other drugs, as a result of hydrolysis of which PABA is formed: reduce the effectiveness of co-trimoxazole;
- barbiturates, phenytoin, para-aminosalicylic acid (PASK): increase the manifestations of folic acid deficiency;
- hexamethylenetetramine, ascorbic acid, and other drugs that acidify urine: increase the likelihood of crystalluria;
- salicylates: enhance the effectiveness of the drug;
- cholestyramine: inhibits the absorption of co-trimoxazole, so it must be taken 1 hour after or 4-6 hours before using Biseptol 480;
- oral contraceptives: their reliability decreases due to the suppression of the intestinal microflora and a decrease in the intestinal-hepatic circulation of hormonal compounds.
Between diuretics (furosemide, thiazides, etc.) and hypoglycemic drugs for oral administration (sulfonylurea derivatives), on the one hand, and sulfonamides, on the other, a cross-allergic reaction may develop.
Analogs
Biseptol 480 analogues are Co-trimoxazole, Bactrim, Briefseptol, Bi-Septin, Dvaseptol, Metosulfabol, etc.
Terms and conditions of storage
Store in a dry place at a temperature not exceeding 30 ° C. Keep out of the reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Biseptol 480
For a long time, Biseptol was the drug of choice in the treatment of most infectious lesions. Today, there are numerous discussions about the relationship between the effectiveness and toxicity of the drug, both at the level of scientific discussions and among patients who used the antibiotic. Therefore, reviews of Biseptol 480 are sometimes diametrically opposite, and it is difficult to make an unambiguous conclusion about the advisability of using the drug at the moment. In such a situation, the best option would be to follow the advice of experts you trust.
Price for Biseptol 480 in pharmacies
The approximate price of Biseptol 480 for 10 ampoules of concentrate for the preparation of a solution for infusion of 5 ml is 415 rubles.
Biseptol 480: prices in online pharmacies
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Drug name Price Pharmacy |
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Biseptol 480 mg tablets 28 pcs. RUB 85 Buy |
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Biseptol 480 mg tablets 20 pcs. RUB 100 Buy |
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Biseptol 480 96 mg / ml concentrate for preparation of solution for infusion 5 ml 10 pcs. 383 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
