Biseptol - complete instructions for the use of tablets and suspensions. Biseptol - a modern look at a long-familiar antibacterial drug

In this medical article, you can get acquainted with the drug Biseptol. The instructions for use will explain in which cases you can take a syrup, suspension or tablets, what the medicine helps with, what are the indications for use, contraindications and side effects. The annotation presents the form of release of the drug and its composition.

In the article, doctors and consumers can only leave real reviews about Biseptol, from which you can find out if the medicine helped in the treatment of sore throats, colds, cystitis and other infectious pathologies in adults and children, for which it is also prescribed. The instructions list Biseptol analogues, drug prices in pharmacies, as well as its use during pregnancy.

The combined antibacterial drug is Biseptol. Instructions for use recommends taking 120 mg and 480 mg tablets, suspension or syrup for the treatment of tonsillitis, pneumonia, prostatitis, chronic pyelonephritis, dysentery.

Release form and composition

Pharmacies receive:

1. Biseptol tablets 120 and 480 mg: flat, round, yellowish (in blisters of 20 pcs., 1 blister in a carton box);
2. oral suspension: light cream, with the smell of strawberries (in dark glass bottles of 80 ml, 1 bottle in a cardboard box);
3. concentrate for solution for infusions (injections) - Biseptol 480.

The active substances are sulfamethoxazole and trimethoprim.

pharmachologic effect

Biseptol, instructions for use informs about it, has bactericidal (destruction of bacteria) and bacteriostatic (obstruction of bacteria growth) properties. The drug is effective against staphylococci, streptococci, Escherichia coli, pneumococci, typhoid fever, dysentery and protea.

It is not used in the fight against tuberculosis microbacteria, spirochetes and Pseudomonas aeruginosa. The drug is rapidly absorbed when taken orally. The maximum content of Biseptol components in the blood is reached within 3 hours after ingestion. The effect persists for 7 hours.

The highest content of the components of the drug is noted in the lungs and kidneys. It is excreted from the body during the day with urine.

What helps Biseptol?

Indications for the use of the drug include the treatment of infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• skin and soft tissue infections (including furunculosis, pyoderma);
• infections of the genitourinary system (including pyelonephritis, urethritis, salpingitis, prostatitis);
• gonorrhea;
• otitis, sinusitis;
• respiratory tract infections (including bronchitis, pneumonia, lung abscess, pleural empyema);
• gastrointestinal infections (including typhoid fever, paratyphoid fever, bacillary dysentery, cholera, diarrhea).

Instructions for use

Biseptol (tablets)

Taken orally after meals. Washed down with a sufficient amount of liquid. The dosage is determined by the doctor, taking into account the individual indications of the patient.

• Children 3-5 years old are prescribed 240 mg 2 times a day.
• Children 6-12 years old - 480 mg 2 times a day.

In the treatment of pneumonia, the daily dose is calculated: 100 mg of sulfamethoxazole per 1 kg of body weight. The drug should be taken every 6 hours. The duration of therapy is 2 weeks.

For the treatment of gonorrhea, 2 g of sulfamethoxazole is prescribed 2 times a day with an interval of 12 hours between doses. Adults and children over 12 years of age take 960 mg 2 times a day. With a long course of treatment - 480 mg 2 times a day.

The duration of therapy is from 5 to 14 days. In severe cases or in chronic infections, an increase in a single dose by 30-50% may be required.

If therapy lasts more than 5 days or the patient takes higher doses of the drug, monitoring of peripheral blood is necessary. In case of pathological changes, folic acid is prescribed at a dose of 5-10 mg per day.

If you miss a dose, the drug should be taken as soon as possible. If a double dose is required, the previous dose should be skipped. Do not take a double dose to make up for the missed one.

In case of renal insufficiency (CC 15-30 ml / min), the recommended dose is reduced by 2 times. With CC less than 15 ml / min, the drug is not recommended.

Syrup

Biseptol in the form of a suspension is taken orally, after a meal with a sufficient amount of liquid. Adults and children over 12 years of age take 960 mg every 12 hours. In severe infections, the dose is increased to 1440 mg every 12 hours.

The duration of therapy for urinary tract infections is 10-14 days, exacerbation of chronic bronchitis - 2 weeks, traveler's diarrhea and shigellosis - 5 days. The minimum dose is 480 mg every 12 hours. With a duration of treatment of more than 14 days, the minimum dose is used.

Children from 2 months (or 6 weeks at birth from mothers with HIV infection) to 5 months take 120 mg 2 times a day. Children from 6 months to 5 years old take 240 mg with an interval of 12 hours. Children 6-12 years old are prescribed 480 mg every 12 hours.

The duration of therapy for urinary tract infections and acute otitis media is 10 days, for shigellosis - 5 days. In the treatment of severe infections in children, the dose can be increased by 2 times.

The minimum duration of therapy for acute infections is 5 days. After the disappearance of symptoms, therapy should be continued for another 2 days. If after 2 weeks there is no improvement, you need to re-examine.

In the treatment of pneumonia caused by Pneumocystis carinii, 30 mg per 1 kg of body weight is prescribed 4 times a day with an interval of 6 hours. The duration of therapy is 2-3 weeks.

For adults and children over 12 years of age, 960 mg per day is prescribed. The total daily dose for children under 12 years of age should not exceed 1920 mg. Reception is carried out for 3 consecutive days every week.

Soft chancre - 960 mg every 12 hours. If after 7 days the skin element does not heal, you can extend the drug for another 7 days. The lack of effect may indicate the resistance of the pathogen.

In acute uncomplicated urinary tract infections in women, a single dose is 1920-2880 mg. It is recommended to take the drug in the evening after meals or at bedtime.

In other bacterial infections, the dose is selected individually, taking into account age, body weight, kidney function and severity of the disease. With nocardiosis, adults take 2880-3840 mg per day for at least 3 months. The course of treatment for acute brucellosis is 3-4 weeks.

Contraindications

Biseptol children are not prescribed:

• suspension - up to 2 months (or up to 1.5 months if the child was born from a mother with HIV infection);
• tablets - up to 3 years.

Side effects

• apathy;
• angioedema;
• arthralgia;
• abdominal pain;
• bronchospasm;
• gastritis;
• hematuria;
• headache;
• hyperemia of the sclera;
• hypoglycemia, hyperkalemia, hyponatremia;
• dizziness;
• diarrhea;
• depression;
• interstitial nephritis;
• cough;
• leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia, aplastic and hemolytic anemia, eosinophilia;
• medicinal fever;
• hives;
• myalgia;
• erythema multiforme exudative (including Stevens-Johnson syndrome);
• impaired renal function;
• increase in body temperature;
• polyuria;
• loss of appetite;
• rash;
• stomatitis;
• tremor;
• nausea, vomiting;
• suffocation;
• photosensitivity.

Children, during pregnancy and lactation

Suspension Biseptol can be prescribed to children older than 2 months. Tablets - from 3 years. Children born to mothers with HIV infection may be given the drug after 6 weeks of age. With jaundice in children, the use of the drug is prohibited. During pregnancy and lactation, the drug is contraindicated.

special instructions

Caution in the use of Biseptol should be observed in people suffering from alcoholism, with nutritional deficiencies and malabsorption.

To prevent crystalluria during therapy, it is recommended to drink enough liquids, this will also prevent blockage of the kidney tubules. While taking Biseptol, it is recommended to avoid being in direct sunlight.

drug interaction

With the simultaneous use of Biseptol with thiazide diuretics, there is a risk of developing 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, and also reduces the intensity of hepatic metabolism of phenytoin (increases its T1 / 2 by 39%) and warfarin, enhancing their effect.

Biseptol's analogs

According to the structure, analogues are determined:

Holiday conditions and price

The average price of Biseptol (80 ml suspension) in Moscow is 136 rubles. In Kyiv, you can buy medicine for 117 hryvnia, in Kazakhstan - for 680 tenge. In Minsk, pharmacies offer an analogue of Co-trimoxazole (tablets 480 mg No. 20) for 2-3 bel. ruble. It is released from pharmacies by prescription.

According to the pharmacological classification, Biseptol refers to antimicrobial combined agents containing sulfamethoxazole and trimethoprim. The antibacterial drug is produced by the Polish pharmaceutical company Polfa.

Composition and form of release

Biseptol (Biseptol) has three forms of release:

Biseptol - an antibiotic or not

The drug belongs to the combined antibiotics. It contains co-trimoxazole, a 5:1 mixture of sulfamethoxazole and trimethoprim. Sulfomethoxazole inhibits the synthesis of dihydrofolic acid, is a competitive antagonist with para-aminobenzoic acid, and exhibits a bacteriostatic effect. Trimethoprim is an inhibitor of the bacterial enzyme dihydrofolate reductase, has a bactericidal or bacteriostatic effect.

Biseptol is active against streptococci, staphylococci, neisseria, E. coli, salmonella, listeria, enterococci, klebsiella, proteus, mycobacteria, shigella, chlamydia, protozoa, pathogenic fungi. Corynebacteria, Pseudomonas, mycobacteria, treponemas, viruses are resistant to the drug. Within an hour after taking the medicine, the maximum concentrations of both active substances are observed.

Trimethoprim is a weak alkali with lipophilic properties, accumulates in bile, sputum. Half of its dose combines with plasma proteins, has a 13-hour half-life. Trimethoprim is excreted by the kidneys in the urine. Sulfamethoxazole is a weak acid that accumulates in bile, cerebrospinal, synovial and intracellular fluid. The active component is excreted by the kidneys, its clearance is reduced in the elderly.

Indications for Biseptol's use

Instructions for use indicate the following indications for the use of Biseptol:

• otitis media;
• typhoid fever, paratyphoid, gastroenteritis, dysentery, cholera;
• tonsillitis, bronchitis, bronchopneumonia, laryngitis, stomatitis;
• malaria, meningitis;
• pyelitis, pyelonephritis;
• sinusitis;
• cholangitis;
• scarlet fever;
• nocardiosis, brucellosis, toxoplasmosis;
• actinomycosis, South American blastomycosis.

Method of application and dosage

The concentrate for the preparation of the infusion solution is administered intravenously, shaken thoroughly before use. The formation of sediment or the appearance of crystals is unacceptable. 5 ml of the concentrate is diluted in 125 ml of solution for infusion. Solvents are dextrose 5 or 10%, Ringer's solution, saline, 0.45% sodium chloride solution with 2.4% dextrose solution. The infusion lasts 1-1.5 hours. If the patient cannot be administered a lot of liquid, it is allowed to mix 5 ml of the concentrate with 75 ml of 5% dextrose.

Dosages for patients older than 12 years, depending on the disease:

The drug is taken after meals, washed down with water. For pneumonia, 100 mg of sulfamethoxazole per kg of body weight is prescribed with a 6-hour interval. The course of treatment does not exceed 2 weeks. For gonorrhea, take 2 g twice a day with a 12-hour interval. Adults and children over 12 years old are prescribed 960 mg twice a day for a course of 5-14 days.

In severe cases of the disease, the dose is increased by 30-50%. With prolonged therapy, manifestations of the pathological type are possible, in which case folic acid is prescribed. If a dose is missed, the drug is taken as soon as possible. In renal failure, the dosage is halved.

Biseptol for cough in the form of a suspension is taken at a dose of 6 mg of trimethoprim and 30 mg of sulfamethoxazole per kg of body weight per day. Patients over 12 years old are prescribed 20 ml every 12 hours. Therapy lasts 10-14 days, with shigillosis - 5. For infections of the lungs, the dose is 120 mg / kg of body weight per day with a 6-hour interval for a course of 2-3 weeks. In case of impaired renal function, the dose is halved.

special instructions

It is useful to study the special instructions section in the instructions for use:

1. With long-term therapy, regular blood tests are recommended, there is a risk of folic acid deficiency.
2. After taking the remedy, diarrhea may develop. Sometimes it serves as a symptom of pseudomembranous colitis. In this case, antidiarrheal drugs are canceled.
3. When a skin rash appears, the injections are canceled.
4. The drug is not used during pregnancy, breastfeeding.
5. During therapy, driving and operating machinery should be avoided.

Biseptol for children

1 ml of solution accounts for 15 mg of benzyl alcohol, so the drug in this form is not used in premature babies, infants, children under 3 years old.

Biseptol for prostatitis

Biseptol can be prescribed for prostatitis by a doctor after tests and diagnostics. Treatment eliminates the inflammatory process in the tissues of the prostate, prevents the transition of the acute stage to the chronic one. The therapy lasts 3 weeks, repeats in a month. At the initial stage, an increased dosage is used: for 3 days the patient takes 6 tablets of the drug (divided into two doses). After 2-3 days of treatment, the first result is visible. Then take 2 tablets per day.

To prevent the development of recurrence of prostatitis, take 1 tablet per day for a course of 2 weeks. The daily dose of the drug should not exceed 960 mg. The components do not affect inflammation, but reduce the amount of pathogenic microflora. Tablets are allowed in the primary and chronic course of the disease.

drug interaction

The instructions for use describe the drug interaction of the drug:

1. The agent lowers the concentration of Cyclosporine in the blood, this combination leads to a transient deterioration in kidney function.
2. The solution is incompatible with bicarbonates.
3. The agent enhances the effect of Methotrexate, hypoglycemic agents, barbiturates, reduces the intensity of the metabolism of Phenytoin, Warfarin, reduces the half-life of Rifampicin, increases the concentration of Digoxin.
4. Caution should be exercised when taking potassium-sparing diuretics, other drugs that can cause hyperkalemia.
5. The combination of the drug with the antimalarial pyrimethamine can lead to megaloblastic anemia.
6. Benzocaine, Procainamide, Procaine are able to reduce the therapeutic effect of the drug.
7. Between diuretics, hypoglycemic sulfonylurea derivatives and antimicrobial sulfonamides there is a risk of cross-allergy.
8. The agent increases the concentration in the blood of Procainamide, Amantadine.
9. Salicylates can enhance the effect of the drug.
10. Hexamethylenetetramine, ascorbic acid can increase the risk of developing crystalluria.

Side effects

The antibiotic Biseptol can lead to the development of side effects:

• hallucinations, headache, depression, apathy, tinnitus, tremor, dizziness, convulsions, ataxia, neuritis;
• pulmonary infiltrates, bronchospasm, shallow breathing, cough;
• pancreatitis, gastritis, glossitis, cholestasis, liver necrosis, abdominal pain, hyperbilirubinemia, nausea, vomiting, hepatitis;
• hemolysis, leukopenia, eosinophilia, neutropenia, purpura, thrombocytopenia, methemoglobinemia, hypoprothrombinemia, anemia, agranulocytosis;
• hepatonecrosis, granuloma;
• nephritis, polyuria, anuria, crystalluria, oliguria, hematuria, nephropathy, hypercreatininemia;
• myalgia, arthralgia;
• systemic lupus erythematosus, serum sickness, periarteritis nodosa, allergic myocarditis, anaphylactic reactions, vasomotor rhinitis, hemorrhagic vasculitis, drug-induced fever;
• skin rash, photosensitivity, angioedema, allergies, dermatitis, erythema, necrolysis, redness of the sclera;
• hypoglycemia, anorexia, hyperkalemia, hyponatremia;
• candidiasis;
• thrombophlebitis.

Overdose

Symptoms of an overdose of the drug are vomiting, confusion, nausea. In severe cases, bone marrow depression is possible. With the development of such symptoms, treatment is canceled, liquid, electrolytes are introduced, if necessary, hemodialysis is performed.

Contraindications

The drug is prescribed with caution for alcohol dependence, bronchial asthma, in old age. Contraindications:

• intolerance to the components of the composition;
• damage to the liver parenchyma;
• porphyria;
• age up to 3 years for concentrate and tablets, up to 3 months for suspension;
• pregnancy, lactation.

  Medication type

  Price, rubles

  Tablets 480 mg 28 pcs.

  Concentrate 5 ml 10 ampoules

  Tablets 120 mg 20 pcs.

  Suspension 80 ml

  Video

120 mg per day or 2 tablets of 240 mg after meals with plenty of liquid. In especially severe cases, 6 tablets per day are prescribed. Reception should be divided into two parts - in the morning and in the evening. Therapy, as a rule, is no more than 5 days. With long-term treatment, 2 tablets of 120 mg per day are taken.

For children, the drug is prescribed in the form of a suspension, twice a day. Each suspension bottle has a measuring cap with divisions of 2.5, 5 and 7.5 ml. For aged less than a year, 2.5 ml of medication is prescribed every 12 hours. If the child is between 1 and 3 years of age, 5 ml is usually given twice a day. From the age of 4, you can take 10 ml of the drug, depending on the intensity of the course of the disease and the recommendations of the pediatrician.

Biseptol has a number of side effects that can occur with an overdose or improper use: muscle spasms of the respiratory system, digestive disorders, diarrhea, jaundice, inflammation of the mucous membranes of the mouth. It is also possible deterioration of kidney function and the appearance of allergic reactions. Before taking the drug, you should consult with your doctor and pass the necessary tests. The medication is taken under the supervision of a specialist.

note

Do not use biseptol with intolerance to sulfonamides, which are part of the tablets. It is also recommended to be carefully treated with medicine if there are problems in the functioning of the kidneys and liver. Patients with kidney disease are prescribed a dose depending on current creatinine levels.

Biseptol is a broad-spectrum antimicrobial agent. This drug provides inhibition of pathogenic microorganisms that cause the disease, has a bactericidal effect. You can take "Biseptol" in the form of tablets, suspensions and infusion solutions.

Instruction

The drug "Biseptol" is prescribed for a number of diseases of an infectious and inflammatory nature. This remedy is used in the treatment of respiratory tract infections, in particular, Biseptol is indicated for the treatment of bronchitis, pneumonia, as well as pleural empyema and lung abscesses. The drug is used in the treatment of infectious diseases of the genitourinary system: urethritis, prostatitis, pyelonephritis, salpingitis, gonorrhea. Also, "Biseptol" is used in the treatment of dysentery, diarrhea, cholera, typhoid fever and paratyphoid. The drug is effective in infectious lesions of the skin and tissues, including it is prescribed for furunculosis and purulent formations. Also, "Biseptol" is used to treat sinusitis, otitis and meningitis.

Tablets "Biseptol" should be drunk after meals, 2 times a day. Children 2-5 years old are prescribed 240 mg, 5-12 years old - 480 mg per dose. Children from 12 years of age and adults use a dosage of 960 mg. With long-term treatment, the amount of the drug must be reduced to 480 mg, taking the drug also twice a day. The duration of therapy depends on the complexity of the disease and is 5-14 days. In the treatment of chronic infections and severe disease, a single dose can be increased by 30-50%. In the treatment of pneumonia, the drug is taken at the rate of 100 mg of sulfamethoxazole per kg of the patient's weight per day. The drug should be drunk for 2 weeks, the interval between doses should be 6 hours. For gonorrhea, 2 g of sulfamethoxazole is indicated 2 times a day at intervals of 12 hours.

Suspension "Biseptol" is indicated for adults and children from 3 months. The drug is taken every 12 hours. Babies 3-6 months old are given 2.5 ml each, 7 months - 3 years old - 2.5-5 ml each. Children 4-6 years old are prescribed 5-10 ml, 7-12 years old - 10 ml of suspension. Adults and adolescents should drink the medicine 20 ml at a time. Treatment should be carried out within 1.5-2 weeks, with dysentery - 5 days. Shake the vial with the suspension well before use.

Biseptol solution is administered intravenously. For and children from 12 years of age, a single dosage is 10 ml of the drug. Before administration, the drug should be diluted in 250 ml of dextrose or sodium chloride solution. Intravenous "Biseptol" is used every 12 hours for 5 days. With particularly severe symptoms, the dosage can be increased to 3 ampoules with a frequency of administration 2-3 times a day. The pediatric daily dose of sulfamethoxazole is 30 mg/kg body weight. This amount of medicine should be used for 2 times. Infusion should be done no longer than 1.5 hours.

Biseptol is a potent combined antibacterial agent. The drug actively destroys the coccal flora, including gram-positive and gram-negative pathogens. Let's consider how to take Biseptol correctly for adults and children, what diseases it helps with, and in what cases it is better to wait a little with its use.

Biseptol - composition, dosage forms

The bactericidal agent Biseptol contains two active ingredients - sulfamethoxazole and trimethoprim. The concentration of these substances in one therapeutic dose depends on the form of release of the drug.

Biseptol is produced in three pharmaceutical forms:

• Tablets - round flat-shaped tablets with a smooth surface, on one side there is an engraving "-Bs". The amount of sulfamethoxazole varies from 100 to 400 ml, and trimethoprim from 20 to 80 ml. The composition additionally includes starch, alcohol, talc, propylene glycol.
• Suspension is a cream-colored syrup for children with a light strawberry flavor. The product is recommended for children from 2 months to 12 years old weighing no more than 80 kg. Premature babies Biseptol is contraindicated.
• The concentrate for infusion is a colorless liquid in ampoules that requires preliminary dilution before intravenous administration. The substance is diluted directly in front of the dropper. The contents of the ampoule are intensively mixed with the solution for infusion.

Biseptol is active against streptococci, pneumococci, staphylococci, chlamydia, Escherichia coli, meningococci. The drug is not effective for tuberculosis, leptospirosis and viral diseases. The medicinal effect of the drug is due to its ability to stop the synthesis of folic acid, without which the coccal flora is not able to multiply.

Biseptol - indications and contraindications

Biseptol is prescribed for infectious diseases caused by microbes sensitive to the drug:

• Bronchitis (all forms).
• Pneumonia (except viral).
• Bronchiectasis.
• Angina.
• Urethritis.
• Otitis.
• Pyelonephritis.
• Sinusitis.
• Cystitis.
• Pharyngitis.
• Prostatitis.
• Brucellosis.
• Typhoid fever.
• Toxoplasmosis.
• Cholera.
• bacterial diarrhea.
• Osteomyelitis.

Biseptol is not used in such cases:

• Intolerance to the components of the drug.
• Liver damage (hepatitis, porphyria, liver failure).
• Blood diseases.
• Renal failure.
• Passing a course of chemotherapy.

Dosage and duration of treatment with Biseptol in adults and children

The regimen for taking Biseptol depends on age, body weight and dosage form.

Tablets. For the age category "12+", 2 tablets at a dose of 400 mg / 80 ml or 8 tablets of 100 ml / 20 ml are taken twice a day. In the case of a severe course of the inflammatory process, the daily dose is increased to 3 or 12 tablets twice a day. The course of treatment is 14 days. For children from 6 to 12 years old, the daily dose is calculated taking into account body weight - 30 ml of sulfamethoxazole per kg.

Suspension. The dose for a child is measured in a measuring cup according to age and taken every 12 hours:

• 2 to 5 months - 2.5 mg.
• From 6 months up to 5 years - 5 mg.
• From 6 to 12 years - 10 mg.

The duration of antibiotic therapy depends on the type of disease and is 5-14 days.

Biseptol - possible complications after treatment

Side effects are rarely recorded and, as a rule, are allergic in nature or manifest as digestive disorders. In addition, the following complications can rarely occur:

• Changes in the blood formula and disorders of the lymphatic system (anemia, leukopenia).
• Allergic processes (rash, bronchospasm, drug-induced fever, urticaria, edema).
• Metabolic disorders (hyperkalemia, hypercalcemia, sodium deficiency, anorexia).
• Mental disorders (psychosis, insomnia, anxiety, fatigue).
• Problems with the nervous system (tinnitus, convulsions, dizziness, migraine).
• Digestive disorders (diarrhea, gastritis).

The use of Biseptol should be monitored by a doctor, since an incorrectly selected dosage can provoke the transition of the disease into a chronic form or cause a number of serious complications.

Catad_pgroup Sulfonamides

Biseptol 480 mg - official instructions for use

MINISTRY OF HEALTH AND SOCIAL DEVELOPMENT OF THE RUSSIAN FEDERATION

INSTRUCTIONS
on the use of the medicinal product
for medical use

Registration number:

Tradename
Biseptol 480

International non-proprietary name of active substances
Co-trimoxazole [Sulfamethoxazole + Trimethoprim]

Dosage form
Concentrate for solution for infusion

Composition 1 ml concentrate
Active substances: sulfamethoxazole 80.00 mg + trimethoprim 16.00 mg
Excipients: propylene glycol 400.00 mg, ethyl alcohol 96% 100.00 mg. benzyl alcohol 15.00 mg, sodium disulfite (E223) 1.00 mg. sodium hydroxide 12.63 mg, sodium hydroxide 10% solution to pH 9.5 - 11.0, water for injection up to 1 ml. 1 ampoule (5 ml) contains 400 mg of sulfamethoxazole and 80 mg of trimethoprim.

Description
Clear colorless or slightly yellowish liquid.

Pharmacotherapeutic group
Combined antimicrobial agent.

Code ATX: J01EE01

Pharmacological properties
Pharmacodynamics
Biseptol is a combined antibacterial agent containing co-trimoxazole, a 5:1 mixture of sulfamethoxazole and trimethoprim. Sulfamethoxazole inhibits the synthesis of folic acid by competitive antagonism with para-aminobenzoic acid, i.e. has a bacteriostatic effect.
Trimethoprim is an inhibitor of bacterial dihydrofolate reductase. Depending on the conditions, it can have a bactericidal or bacteriostatic effect. Thus, trimethoprim and sulfamethoxazole block two successive steps in the biosynthesis of purines, and then nucleic acids necessary for numerous bacteria.
Biseptol is a broad-spectrum bactericidal drug active against the following microorganisms: Streptococcus spp. (Streptococcus pneumoniae), Staphylococcus spp., 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 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.
Pharmacokinetics
The maximum concentration of sulfamethoxazole and trimethoprim, determined after one hour, is higher and is reached more quickly when administered intravenously, compared with the concentration obtained when the drug is taken orally. Significant differences regarding plasma concentration, half-life and elimination after administration of co-trimoxazole in oral and intravenous form have not been established. Trimethoprim is a weak base (pKa = 7.3) with lipophilic properties. The concentration of trimethoprim in tissues is higher than the concentration determined in plasma, it is especially high in the lungs and kidneys. Higher concentrations of trimethoprim compared with plasma are observed in bile, fluid and tissues of the prostate gland, sputum, and vaginal discharge. The concentrations of trimethoprim in breast milk, cerebrospinal fluid, middle ear secretion, synovial fluid, intracellular fluid (interstitial) correspond to the concentrations necessary for antibacterial action. Trimethoprim penetrates into the amniotic fluid and fetal tissues, reaching a concentration there close to the concentration observed in the mother's blood serum.
Approximately 50% of trimethoprim binds to plasma proteins. The elimination half-life in individuals with normal renal function ranges from 8.6 to 17 hours. There were no significant differences in the elderly compared with younger patients. Trimethoprim is excreted mainly by the kidneys - approximately 50% unchanged within 24 hours in the urine. Several metabolites of trimethoprim have been identified in urine.
Sulfamethoxazole is a weak acid with pKa = 6.0. The concentration of the active form of sulfamethoxazole in amniotic fluid, bile, cerebrospinal fluid, middle ear secretion, sputum, synovial fluid, intracellular fluid is from 20 to 50% of sulfamethoxazole in plasma. Approximately 66% of sulfamethoxazole binds to plasma proteins. The elimination half-life in individuals with normal renal function is 9 to 11 hours. In persons with impaired renal function, no changes in the half-life of the active form of sulfamethoxazole have been established, but an increase in the half-life of the main acetylated metabolite is observed if the creatinine clearance is less than 25 ml / min.
Sulfamethoxazole is excreted primarily by the kidneys, from 15 to 30% of the administered dose is found in the urine in the active form. In elderly patients, there is a decrease in the renal clearance of sulfamethoxazole.

Indications for use
Infectious and inflammatory diseases caused by microorganisms sensitive to co-trimoxazole:

• urinary tract infections: urinary tract infections, soft chancre;
• respiratory tract infections: chronic bronchitis, treatment and prevention of pneumonia caused by Pneumocystis jiroveci (formerly P. carinii) (PCP);
• infections of ENT organs: otitis media (in children);
• gastrointestinal infections: typhoid fever and paratyphoid fever, cholera, dysentery, gastroenteritis caused by enterotoxic strains of Escherichia coli;
• other bacterial infections: nocardiosis, brucellosis, actinomycosis, South American blastomycosis, toxoplasmosis.

Contraindications

• Hypersensitivity to sulfonamides, trimethoprim, co-trimoxazole or any auxiliary component of the drug;
• serious damage to the liver parenchyma;
• severe renal failure (CC less than 15 ml / min);
• liver failure;
• severe hematological disorders: aplastic anemia, B12 deficiency anemia, agranulocytosis, leukopenia, deficiency of glucose-6-phosphate dehydrogenase;
• administering the drug to diagnosed porphyria or to patients who are at risk of developing acute porphyria should be avoided. the drug may increase the symptoms of this disease;
• children under 3 years of age (with the exception of the treatment or prevention of pneumonia caused by Pneumocystis jiroveci);
• pregnancy and lactation.

Carefully
Care must be taken when prescribing Biseptol 480 to patients with a deficiency of folic acid (for example, people with alcohol dependence, treatment with anticonvulsants, malabsorption syndrome and the elderly); patients with bronchial asthma and severe allergies; patients with diseases of the circulatory and respiratory systems, tk. after the introduction of high doses, excessive hydration may occur; patients with thyroid disease. Special care is advised in elderly patients, as this group is more susceptible to side effects and feels more pronounced side effects, especially with concomitant diseases, such as renal failure and / or liver dysfunction and taking other drugs.

Dosage and administration
Biseptol 480, a concentrate for solution for infusion, is intended for intravenous administration only and should be diluted immediately before use.
After the introduction of the drug Biseptol 480 into the solution for infusion, the resulting mixture must be vigorously shaken in order to completely mix. If sediment or crystals appear before mixing or during infusions, the mixture should be discarded and a new one prepared.
The following dilution scheme for Biseptol 480 is recommended:
1 ampoule (5 ml) of Biseptol 480 in 125 ml of solution for infusion;
2 ampoules (10 ml) of Biseptol 480 in 250 ml of solution for infusion;
3 ampoules (15 ml) of Biseptol 480 in 500 ml of solution for infusion.
It is allowed to use the following solutions for infusions to dilute the drug Biseptol 480:

• 5% and 10% dextrose solution;
• 0.9% NaCl solution;
• Ringer's solution;
• 0.45% NaCl solution with 2.5% dextrose solution.

• children aged 3 to 5 years: 2.5 ml every 12 hours.
• children aged 6 to 12 years: 5 ml every 12 hours.

Overdose
Symptoms: nausea, vomiting, dizziness, headache, confusion. In severe overdose of trimethoprim, bone marrow depression was noted.
Treatment: if side effects occur, the drug should be discontinued immediately. Fluid administration, correction of electrolyte disturbances. If necessary - hemodialysis.

Interaction with other drugs
Co-trimoxazole is compatible with the following drugs: 5% dextrose for IV infusion, 0.9% sodium chloride for IV infusion, a mixture of 0.18% sodium chloride and 4% dextrose for IV infusion, 6% dextran 70 for IV infusion in 5% dextrose or saline, 10% dextran 40 for IV infusion in 5% dextrose or saline, Ringer's solution for injection.
In elderly patients, biseptol in combination with diuretics, in particular with thiazide diuretics, increases the risk of thrombocytopenia. Simultaneous use with cyclosporine reduces its concentration in the blood.
Do not administer the drug intravenously in combination with drugs and solutions containing bicarbonates.
Increases the anticoagulant activity of indirect anticoagulants, enhances the effect of hypoglycemic agents and methotrexate. Reduces the intensity of hepatic metabolism of phenytoin (extends its T1 / 2 by 39%) and warfarin, enhancing their effect. With the simultaneous use of co-trimoxazole and rifampicin for a week, the half-life of trimethoprim is reduced.
In patients taking prophylactic pyrimethamine (an antimalarial drug) in doses exceeding 25 mg / week, cases of megaloblastic anemia have been noted during treatment with co-trimoxazole. This type of combination therapy is not recommended.
With the simultaneous use of co-trimoxazole and zidovudine, the risk of developing hematological disorders increases, and therefore blood tests should be performed.
Increases serum concentrations of digoxin, especially in elderly patients (control is necessary) of serum digoxin concentrations.
Reduce the therapeutic effect of co-trimoxazole benzocaine, procaine, procainamide and other drugs, as a result of the 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.
Phenytoin, barbiturates, PAS increase the manifestations of folic acid deficiency.
In patients taking cyclosporins (for example, after kidney transplantation), a transient deterioration in renal function was observed during treatment with co-trimoxazole.
With the simultaneous use of co-trimoxazole and procainamide or amantadine, an increase in the serum concentration of the listed drugs may occur.
Derivatives of salicylic acid enhance the effect of co-trimoxazole.
Ascorbic acid, hexamethylenetetramine, and other drugs that acidify urine increase the risk of crystalluria.
Co-trimoxazole reduces the reliability of oral contraception (inhibits the intestinal microflora and reduces the enterohepatic circulation of hormonal compounds).

special instructions
During the use of the drug, proper diuresis should be maintained. In malnourished patients, the risk of sulfonamide crystals is increased. In the case of prolonged administration of the drug, regular laboratory blood tests are recommended, since there is a possibility of hematological changes associated with folic acid deficiency.
After using the drug, diarrhea may occur, which may be a symptom of pseudomembranous colitis. It is necessary to stop the use of the drug and cancel antidiarrheal agents.
Biseptol 480 should not be used in the treatment of pharyngitis caused by group A beta-hemolytic streptococci.
Caution should be exercised in patients taking other medicinal products that may cause hyperkalemia, including potassium-sparing diuretics.
It is recommended to monitor the concentration of potassium in the serum, given the risk of an increase in its concentration (hyperkalemia).
If the first symptoms of a skin rash appear, the drug should be discontinued.
Given the content of benzyl alcohol in Biseptol 480 (15 mg of benzyl alcohol in 1 ml of solution), the drug should not be used in premature and infants. Benzyl alcohol can cause intoxication and anaphylactoid reactions in infants and children under 3 years of age.

Use during pregnancy and during breastfeeding
Do not prescribe the drug during pregnancy and during breastfeeding.

Influence on the ability to drive a car and other mechanisms
During the period of treatment, care must be taken when driving vehicles and engaging in potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Release form and packaging
Concentrate for solution for infusion (80.00 mg + 16.00 mg)/ml. 5 ml in colorless hydrolytic glass ampoules (class 1, Evr. Pharm.). Above the notch of the ampoule there is a dot of white or red color, as well as a strip in the form of a yellow ring. 5 ampoules are placed in a PVC ampoule tray. Two pallets in a cardboard box with instructions for use.

Storage conditions
Store in a place protected from light at a temperature not exceeding 25°C. Do not freeze!

Best before date
5 years.
Do not use after the expiry date stated on the packaging.

Holiday conditions
On prescription.

Manufacturer and holder of the registration certificate
JSC Warsaw Pharmaceutical Plant Polfa
st. Karolkova 22/24, 01-207 Warsaw, Poland.

Representation in the Russian Federation:
121248 Moscow, Kutuzovsky prospect, 13, office 85