Can Biseptol be given to children? What helps Biseptol Biseptol active substance.

How often can you give

Microflora restoration

Probiotics

Among sulfa drugs, Biseptol can be called the most popular. Such a drug is produced in suspension, which can be given to even the smallest children. In addition, Biseptol is available in tablets. Is it allowed to give this dosage form to children and in what dosage is it used?

Release form

Biseptol tablets are distinguished by their round flat shape, white (sometimes yellow) color, as well as the presence of risks and engraving Bs. They are packed in blisters of 20 pieces and sold in 1 blister per pack.

Composition

The substance that provides Biseptol with a therapeutic effect is called co-trimoxazole. This name combines two active compounds, the ratio of which in one tablet is 5 to 1. Depending on the amount of such active substances, the drug is presented in two dosages:

1. 120 mg tablets, containing 100 mg of sulfamethoxazole supplemented with 20 mg of trimethoprim.
2. 480 mg tablets,of which the patient receives 400 mg of sulfamethoxazole and 80 mg of trimethoprim.

To make the drug solid and keep the tablet in shape, talc, Mg stearate, propyl and methyl parahydroxy benzoate, potato starch, propylene glycol and polyvinyl alcohol are added to the composition.

Operating principle

The active substances in Biseptol have a bactericidal effect... They affect the synthesis of proteins in bacterial cells, disrupting it, as a result of which microbes die. The drug is active in infection with E. coli, enterococci, Klebsiella, Salmonella, pneumococcus, Proteus, Shigela, Pneumocystis and many other bacteria. In relation to pseudomonads, mycobacteria, leptospira, viruses, treponemas and some other microorganisms, Biseptol is ineffective.

Indications

Biseptol helps with infections caused by pathogens that are sensitive to it.It is prescribed for:

• Purulent otitis media.
• Sinusitis.
• Typhoid fever.
• Cholera.
• Salmonellosis.
• Brucellosis.
• Bronchitis.
• Bacterial diarrhea.
• Pneumocystosis.
• Typhoid fever.
• Scarlet fever.
• Angina.
• Pharyngitis.
• Gonorrhea.
• Whooping cough.
• Laryngitis.
• Pneumonia.
• Bronchiectasis.
• Peritonitis.
• Cholangitis.
• Osteomyelitis.
• Skin abscesses.
• Furunculosis.
• Urethritis.
• Orchite.
• Cystitis and many other infections.

Doctor Komarovsky devoted one of his programs to infectious diseases in children:

From what age is it allowed to take?

Instructions for the use of the Biseptol tablet form include information that the remedy is recommended for children over three years old. If you want to prescribe a medicine to babies who have not yet turned 3 years old, use a suspension. It can be given from 2 months of age.

Contraindications

The use of Biseptol is prohibited:

• If a child has an intolerance to such a drug or other sulfonamide drugs.
• If the analyzes of a small patient showed renal failure.
• If the child's liver is damaged and its work is severely impaired.
• If deficiency of glucose 6 phosphate dehydrogenase is detected.
• If a blood test reveals agranulocytosis, aplastic anemia, or leukopenia.

The use of the drug with caution implies that the child has an allergic disease, thyroid pathology, lack of vitamins B9 and B12, or porphyria.

Side effects

The child's body often reacts to treatment with Biseptol with allergies or disruption of the digestive tract. In addition, the drug can cause:

• Suppression of hematopoiesis.
• Dizziness, apathetic or depressive state, convulsions, headaches.
• Shortness of breath and cough.
• Impaired renal function.
• Joint or muscle pain.

Instructions for use and dosage

The tablets should be taken after meals with plenty of water.The dosage is best determined individually based on the clinical picture, the condition of the child, the sensitivity of the pathogen and other factors. Usually Biseptol tablets are prescribed in such a single dose:

In this single dosage, Biseptol should be taken twice a day., and the break between doses should be 12 hours.

The duration of use is determined depending on the pathology. The drug is prescribed for at least 5 days, and when the symptoms of infection disappear, it should be taken for another two days. The average duration of treatment with Biseptol is 5 to 14 days.If the infection is severe, single dosages can be increased by 30-50%.

Overdose

If you take more pills than the doctor has prescribed, your child will develop headaches, nausea, abdominal pain, drowsiness, fever, and other negative symptoms. Prolonged excess of the dosage leads to the appearance of anemia, leukopenia, jaundice and thrombocytopenia.

Interaction with other drugs with food

• Biseptol tablets should not be taken with milk, as this will reduce their effect.
• Before taking the drug, you should not eat foods that are quickly absorbed and removed from the intestines, for example, baked goods or dried fruits.
• During treatment, it is advisable to limit fatty animal products in the patient's diet, as well as peas, cabbage, carrots, beans and tomatoes.
• Biseptol enhances the therapeutic effect of the use of indirect anticoagulants, hypoglycemic drugs, phenytoin and methotrexate.
• Co-administration with diuretic drugs will increase the risk of thrombocytopenia.
• The medicine should not be used together with aspirin or drugs that can inhibit hematopoiesis.

Terms of sale

To buy a tablet form of Biseptol, you need to present a prescription from a doctor. The average price of a pack of tablets with 120 mg of active compound is 30 rubles.

Storage conditions and shelf life

Biseptol tablets should be stored away from moisture and sunlight, at temperatures below +25 degrees. Babies should not have free access to the drug. The shelf life of this form of medicine is 5 years.

Few facts about the product:

Instructions for use

Online pharmacy price website: from 35

Pharmacological properties

The drug Biseptol is a medicine with a targeted bactericidal and bacteriostatic effect. The active components of the drug are trimethoprim and sulfamethoxazole. Sulfamethoxazole has a similar structure to para-aminobenzoic acid. Its action is aimed at interfering with the synthesis of dihydrofolate reductase in infected cells, which limits the ingress of para-aminobenzoic acid into the molecules of these cells. Trimetroprim stops the conversion of dihydrofolate reductase to tetrahydrofolate, which prevents the infected cell from dividing. Also, one of the qualities of trimethoprim is an increase in the pharmacological action of the sulfamethoxazole substance.

The drug is most active against bacteria such as pneumococcus, staphylococcus, listeria monocytogenes, bacillus anthrax, nocardia asteroides, mycobacteria, fecal enterococcus, meningococcus, Escherichia coli, gonococcus, salmonella, cholerae colibacillus, haemopluoroma coli, citrobacter freundi, proteus mirabilis, brucellosis, providence, enterobacter, legionella pneumophilus, pseudomonas, shigella flexner, serration marcessens, coli pseudotuberculosis, chlamydia, Morgan's bacteria, toxoplasma, pneumocystisis, pneumoniae, leushmoidosis immitis

Bacteria such as corynebacteria, Koch's bacillus, Pseudomonas aeruginosa, leptospirosis, treponema pale remain unchanged when interacting with Biseptol.

The drug has almost one hundred percent bioavailability, is absorbed from the digestive system. It reaches its maximum blood content within four hours from the moment of use. The drug is distributed in tissues and organs in approximately the same ratio. Elimination is carried out by the kidneys unchanged.

Composition and form of release

The release of the drug Biseptol is carried out in the form of tablets and suspension.

The following components are used for the production of tablets:

• auxiliary substances in the form of potato starch, polyvinyl alcohol, preservative E128, para-hydroxybenzoic acid propyl ester, propane-1,2-diol.

The tablets are round in shape without bulges. The color of the tablets ranges from pure white to white with yellowish tints. A chamfer and an abbreviation indicating the name of the preparation are applied on each side along the diameter. Their primary packaging is polyvinyl chloride blister packs that hold twenty tablets. One blister plate, together with instructions for use, is packed in a cardboard box.

The following components are used for the production of the suspension:

• the active ingredients are trimethoprim and sulfamethoxazole;
• excipients in the form of citric acid monohydrate, methyl parahydroxybenzoate, saccharin, sweetener maltitol E965, strawberry aldehyde, purified water, propane-1,2-diol, carmellose sodium, macrogol glyceryl hydroxystearate, magnesium aluminum silicate, sodium orthophosphate dodecahydrate.

The suspension has a uniform consistency with a characteristic strawberry aroma. The color ranges from pure white to creamy white. Its primary packaging is a dark glass bottle with a screw cap. The bottle, along with the instructions, is placed in a cardboard box.

Indications for use

Prescription of the drug Biseptol is carried out for the treatment of the following diseases:

• bronchitis in the acute stage;
• pneumonia;
• inflammation of the middle ear;
• inflammation of the lymph nodes and ulcers on the genitals;
• infectious diseases of the genitourinary system;
• bowel disease caused by salmonella bacteria;
• dysentery;
• frequent loose stools caused by E. coli;
• disorders of the digestive tract;
• other diseases caused by infectious microbacteria.

Side effects

Side effects after using the drug can occur from various body systems. These include:

• spasm of the muscles of the bronchi;
• a feeling of nausea, turning into vomiting;
• cough, shortness of breath;
• frequent loose stools;
• dizziness, migraine;
• weakness, loss of strength;
• depressive state;
• limb cramps;
• change in appetite;
• inflammation of the pancreas;
• pain in the abdomen;
• inflammation of the oral mucosa;
• cholestatic syndrome;
• increased activity of liver enzymes;
• inflammation of the liver;
• chronic liver disease;
• intestinal inflammation;
• inflammation of the stomach lining;
• lowering the level of leukocytes, platelets, neutrophils;
• anemia;
• blood clotting disorders;
• increased levels of methemoglobin in the blood;
• increased urine production;
• kidney inflammation;
• an increase in the blood content in the urine above the physiological norm;
• pain in the joints;
• muscle pain;
• photosensitivity;
• allergic reactions in the form of itching, burning, dermatitis;
• swelling of the subcutaneous tissue;
• lowering blood sugar;
• an increase in the content of potassium in the blood.

Contraindications

You should not use the drug Biseptol if you have one of the following contraindications:

• hypersensitivity to individual components present in the composition of the medication;
• severe kidney disease;
• severe blood diseases;
• damage to the liver tissue;
• increased bilirubin levels in childhood;
• lack of ether Robison.

Pregnancy and lactation

Biseptol tablets should not be taken during pregnancy. The suspension should be administered with caution in cases where the expected benefit to the mother is higher than the potential threat to the embryo.

It has been clinically established that the active ingredient of the drug is excreted in breast milk. In this regard, it is recommended to suspend breastfeeding for the period of using the medication.

Application: method and features

The drug Biseptol is administered orally. The therapy regimen, as well as the dosage, varies depending on the age of the patient.

Tablets are prescribed:

• adults and children over twelve years old, two tablets with a dosage of four hundred and eighty milligrams in the morning and in the evening;
• children from six years to twelve, one tablet with a dosage of four hundred and eighty milligrams in the morning and evening;
• children from three to six years old, two tablets with a dosage of two hundred and forty milligrams in the morning and evening.

The average duration of a therapeutic course with tablets is from one to two weeks.

The suspension is prescribed:

• for adults and children over twelve years old, four measuring spoons in the morning and in the evening;
• children from six to twelve, two measuring spoons in the morning and in the evening;
• children from three to six years old, one or two measuring spoons in the morning and in the evening.
• children from six months to three years, one measuring spoon in the morning and in the evening.
• children from three months to six months, half a measuring spoon in the morning and in the evening.

The average duration of a therapeutic course with a suspension is from ten days to two weeks.

Alcohol compatibility

It is not recommended to consume alcoholic beverages during a therapeutic course. Alcohol can reduce the pharmacological properties of the drug. In some cases, disturbances in the work of various body systems are possible.

Interaction with other medicinal products

With the combined use of the drug Biseptol with diuretics, a decrease in the level of platelets is possible.

With simultaneous use with anticoagulants, blood clotting may decrease.

Medicines that promote the formation of para-aminobenzoic acid reduce the effectiveness of the active components of Biseptol.

When using tricyclic antidepressants, their effectiveness may decrease.

Overdose

In case of an overdose, the following symptoms occur:

• change in appetite;
• feeling of nausea with vomiting;
• dizziness, migraine;
• impotence, loss of strength;
• temperature increase;
• increased blood levels in the urine;
• fainting;
• depressive state;
• violation of concentration.

To eliminate these symptoms, it is necessary to immediately stop taking the medication, wash the stomach in order to quickly remove the remnants of the drug from the body. Frequent fluid absorption and competent supportive care are recommended.

special instructions

Side effects most often occurred in patients with acquired immunodeficiency syndrome.

It does not affect driving or engaging in activities that require increased attention.

Analogs

The drug has the following analogue agents similar in spectrum of action: Bactiseptol, Bebitrim, Bactrim, Bi-Sept-Farmak, Oriprim, Raseptol, Soluseptol, Sumetrolim, Triseptol.

International Classification of Diseases (ICD-10)

According to the international classification of diseases (ICD-10), the diagnoses in which this medication is used have the following coding:

• typhoid fever (A01.0);
• brucellosis (A23.9);
• whooping cough (A37);
• scarlet fever (A38);
• pneumocytosis (B59);
• otitis externa (H60);
• acute sinusitis (J01);
• acute laryngitis (J04.0);
• acute bronchitis (J20).

Terms of sale

In pharmacies, Biseptol is sold in accordance with the prescriptions of the attending physician.

Storage rules, shelf life

According to the instructions, the drug should be stored in a place protected from sunlight at a temperature of less than twenty-five degrees Celsius for no more than three years.

thanks

The site provides background information for informational purposes only. Diagnosis and treatment of diseases must be carried out under the supervision of a specialist. All drugs have contraindications. A specialist consultation is required!

Biseptol drug

Biseptol Is a combined preparation from the sulfonamide group. It contains sulfamethoxazole and trimethoprim. Biseptol is a drug with a wide spectrum of action. This is a bactericidal drug (it causes the death of a microbial cell), but it does not belong to antibiotics. The effect of the drug is due to the fact that it blocks the synthesis of folic acid, without which the microbial cell cannot divide. Sulfamethoxazole and trimethoprim complement and reinforce each other in this mechanism.

Biseptol is active against the following pathogens: staphylococci, streptococci, pneumococci, dysentery bacillus, typhoid bacillus, proteus, Escherichia coli, salmonella, pneumocystis, plasmodium, the causative agent of leishmaniasis, meningococci, cholera vibrio, chleracoccus, actinomycetea mushrooms.

The drug is ineffective against Pseudomonas aeruginosa, the causative agent of leptospirosis, the causative agent of tuberculosis, spirochetes and viruses.
Biseptol also has an effect on microorganisms that are resistant to other sulfa drugs.

Biseptol is rapidly and well absorbed from the stomach and reaches its maximum concentration in the blood 1-3 hours after ingestion. The therapeutic concentration of the drug is kept up to 7 hours.

The drug penetrates well into biological fluids and body tissues: bile, saliva, cerebrospinal fluid, sputum, prostate gland, kidneys, lungs. It is excreted from the body mainly in the urine.

Release forms

Biseptol is available in the form of tablets, suspension and concentrate for injection:

• 120 mg tablets (100 mg sulfamethoxazole and 20 mg trimethoprim);
• 480 mg tablets (400 mg sulfamethoxazole and 80 mg trimethoprim);
• Bactrim Forte tablets 960 mg (800 mg sulfamethoxazole and 160 mg trimethoprim);
• Syrup (or suspension) - for oral administration 100 ml (in 1 ml - 40 mg of sulfamethoxazole and 8 mg of trimethoprim);
• Concentrate for preparation of solution for injection 480 mg (in 1 ml of concentrate - 80 mg of sulfamethoxazole and 16 mg of trimethoprim).

The drug should be stored in a dry place and at a temperature of no more than +25 o C.

Instructions for the use of Biseptol

Indications for use

Biseptol is used to treat infections caused by microorganisms sensitive to this drug:

• diseases of the respiratory tract (bronchitis in acute and chronic form; pneumonia; pleural empyema - purulent inflammation of the membranes of the lungs; abscess or abscess of the lung; bronchiectasis - expansion of the lumen of the bronchi due to disease);
• ENT pathology (otitis media, or ear inflammation; sinusitis, or inflammation of the paranasal sinuses);
• intestinal infections (dysentery, paratyphoid fever A and B, cholera, typhoid fever);
• infections of the genitourinary organs (urethritis - inflammation of the urethra; prostatitis - inflammation of the prostate gland; pyelonephritis - inflammation of the renal pelvis and the kidney tissue itself; salpingitis - inflammation of the uterine appendages);
• gonorrhea (sexually transmitted disease);
• infections of soft tissues and skin (pyoderma, or pustular skin lesions; acne; boil, or boil);
• meningitis (inflammation of the meninges) and abscess (abscess) of the brain;
• septicemia (a form of blood "infection");
• infectious diseases: brucellosis, malaria, toxoplasmosis, borreliosis, scarlet fever;
• wound infections and osteomyelitis;
• prevention and treatment of Pneumocystis pneumonia in HIV-infected patients.

Contraindications

Biseptol is not used for treatment in such cases:

• with severe cardiovascular failure;
• with diseases of the hematopoietic organs;
• with severe renal failure;
• mothers while breastfeeding;
• with a deficiency of glucose-6-phosphate dehydrogenase (hereditary disease);
• children under the age of 3 months and premature babies;
• with an increased level of bilirubin in children;
• with hypersensitivity to the components that make up the drug, or to other sulfa drugs.

With caution, Biseptol can be used if the patient has previously had an allergy to other drugs; with bronchial asthma; patients with a lack of folic acid; with diseases of the thyroid gland; in early childhood and old age.

Treatment with Biseptol should be carried out under medical supervision and the blood test should be carefully monitored.

Side effects

Biseptol is generally well tolerated. But, like any drug, it can have side reactions:

• From the digestive system: in rare cases - diarrhea, abdominal pain, loss of appetite, nausea, vomiting; in isolated cases - colitis (intestinal inflammation); reactive inflammation of the liver with stagnation of bile - cholestatic hepatitis; glossitis - inflammation of the tongue; stomatitis - inflammation of the oral mucosa; pancreatitis is an inflammation of the pancreas.
• From the side of the nervous system in some cases: dizziness, headache, depression, small tremors of the fingers of the extremities.
• From the side of the kidneys in rare cases: an increase in the volume of urine, inflammation of the kidneys (nephritis), excretion of blood in the urine.
• From the respiratory system: bronchospasm, cough, choking or feeling short of breath.
• On the part of the hematopoietic organs in isolated cases: a decrease in the number of leukocytes in the blood, a decrease in the number of neutrophils (a type of leukocytes that protect the body from infections), a decrease in platelets (platelets involved in blood clotting), folate deficiency anemia.
• From the side of the skin: rash on the skin in the form of urticaria; itching; in isolated cases - Lyell's syndrome and Stevens-Johnson syndrome (the most severe variants of allergic manifestations on the skin and mucous membranes with necrosis and rejection); Quincke's edema (local or diffuse edema of the subcutaneous tissue and mucous membranes); hypersensitivity to ultraviolet rays.
• There have been isolated cases of chills and fever after taking Biseptol (drug fever).
• Pain in joints and muscles.
• Thrombophlebitis (at the injection site).
• Decreased levels of potassium, sodium, and blood sugar.

Side effects, as a rule, are mild and disappear after drug withdrawal.

With prolonged use (more than 5 days) and when using higher dosages, as well as when changes appear in the blood test during treatment, folic acid should be taken at 5-10 mg per day.

Drug interactions
Biseptol should not be taken simultaneously with Aspirin, Butadion, Naproxen.

Biseptol enhances the effect of drugs that reduce blood clotting, for example, Warfarin.

Biseptol enhances the effect of some antidiabetic drugs (Glickvidone, Glibenclamide, Glipizide, Chlorpropamide, Gliclazide).

Biseptol increases the activity of the anticancer drug Methotrexate and the anticonvulsant drug Phenytoin.

Biseptol is not recommended to be prescribed simultaneously with thiazide diuretics (Chlorothiazide, Diuril, Naturetin, Metolazone, Diukardin, Furosemide, etc.) - this contributes to increased bleeding.

Biseptol in combination with diuretics, as well as with the antidiabetic agents listed above, can cause cross-allergic reactions.

Hexamethylenetetramine, ascorbic acid and other drugs that acidify the urine increase the risk of "sand" formation in the urine when used simultaneously with Biseptol.

Biseptol may increase the concentration of digoxin in the blood in elderly patients.

The simultaneous use of Biseptol and Pyrimethamine (an anti-malarial agent) increases the risk of anemia.

Benzocaine, Procaine (drugs for local anesthesia) reduce the effectiveness of Biseptol.

Biseptol dosage
The dose of the drug and the duration of administration are prescribed by the doctor individually, depending on the severity of the condition and concomitant diseases.

Adult patients are usually prescribed 960 mg 2 times a day (2 tablets of 480 mg or 1 tablet forte 2 times) every 12 hours for 5-14 days.

If necessary, long-term treatment is prescribed 480 mg 2 times a day (1 tablet 480 mg 2 times).

Suspension of Biseptol is prescribed for adults at 20 ml every 12 hours.

In the case of a severe course of the disease (sometimes with a chronic disease), the dose may be increased up to 50%.

And with a duration of treatment more than 5 days, and with an increase in the dose of Biseptol, it is necessary to control a complete blood count.

But microbes adapt to drugs that are often used, and over time, they lose sensitivity to these drugs; medications stop working. So it happened with Biseptol. Therefore, the attitude towards the appointment of Biseptol for cystitis is very restrained at the present time.

The correct tactics for the treatment of cystitis is the selection of medications in accordance with their sensitivity. For this purpose, urine culture is prescribed for microflora and its sensitivity to drugs. The doctor will receive the result 3-4 days after the test and will select the correct treatment.

In some cases, the doctor initially prescribes Biseptol, and after receiving the result of the sensitivity of the flora to drugs, if necessary, changes the treatment. Sometimes Biseptol is prescribed because of intolerance to antibiotics or other drugs. Biseptol is prescribed in the usual dosage (2 tablets 2 times a day) for 5-10 days.

Analogs and synonyms of Biseptol

It is necessary to distinguish between drug analogues and drug synonyms.

Analogs are drugs that have different active ingredients in their composition, differ in names, but are used in the treatment of the same diseases, because have the same effect. Analogs may differ in strength of action, drug tolerance, contraindications, side effects.

Antibiotics of different groups are analogs of Biseptol. they also have antimicrobial effects. Depending on the sensitivity of the pathogen and the spectrum of action, antibiotics are used to treat the same diseases as Biseptol.

Biseptol's analogs are other sulfa drugs:

• Asakol (active ingredient: mesalazine);
• Dermazin (active ingredient: sulfadiazine);
• Ingalipt (active ingredients: streptocid, sodium sulfathiazole);
• Ingaflu (active ingredient: streptocide) and other sulfa drugs.

Synonymous drugs are drugs with the same active ingredients, but having different names, because produced by different companies. These are generic drugs. They may differ in dosage forms, but have the same pharmacological properties.

Synonyms for Biseptol: Bactrim, Bacterial, Bactramine, Abacin, Andoprim, Bactifer, Abactrim, Bactramel, Hemitrin, Bactrizol, Ectapprim, Berlocid, Bacticel, Doktonil, Expectrin, Gantrin, Falprin, Metomid, Infektrim, Primazol, Microcetim, Oradin, Oradin, Poteseakt Sumetrolim, Septocid, Uroxen, Baktekod, Trixazole, Trimexazol, Blexon, Vanadil, Aposulfatrin, Bactreduct, Groseptol, Cotrimol, Kotribene, Eriprim, Priotremed, Sulfatrim, Rancotrim, Expazol, Novotrimed, Oriprimaxazul, Trimexol.

Release form

Pills

Composition

Active ingredient: Co-trimoxazole [Sulfamethoxazole + Trimethoprim] (Co-trimoxazolum) Concentration of active ingredient (mg): Sulfamethoxazole 400 mg, trimethoprim 80 mg

Pharmacological effect

Combined antibacterial drug, contains sulfamethoxazole and trimethoprim. Sulfamethoxazole, which is similar in structure to PABA, disrupts the synthesis of dihydrofolic acid in bacterial cells, preventing the inclusion of PABA in its molecule. Trimethoprim enhances the effect of sulfamethoxazole, which is responsible for the reduction of dihydrofolic acid - phymic acid. for protein metabolism and division of microbial cells. It is a bactericidal drug with a wide spectrum of activity. It is active against gram-positive aerobic bacteria: Streptococcus spp., including Streptococcus pneumoniae (hemolytic strains are more sensitive to penicillin), Staphylococcus spp., Bacillus anthracoides asteroides as , Enterococcus faecalis, Mycobacterium spp. (including Mycobacterium leprae, excluding Mycobacterium tuberculosis); gram-negative aerobic bacteria: Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (including enterotoxogenic strains), Salmonella spp. (including Salmonella typhi and Salmonella paratyphi); Vibrio cholerae, Haemophilus influenzae (including ampicillin-resistant strains), Bordetella pertussis, Klebsiella spp., Proteus spp., Pasteurella spp., Francisella tularensis, Brucella spp., Citrobacter spp., Enterobacter spp., Some except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp., Yersinia spp., Morganella spp., as well as for Chlamydia spp. (including Chlamydia trachomatis, Chlamydia psittaci); in relation to gram-positive anaerobes: Actinomyces israelii; for protozoa: Plasmodium spp., Toxoplasma gondii; pathogenic fungi: Coccidioides immitis, Histoplasma capsulatum, Pneumocystis carinii, Leishmania spp. Resistant to the drug: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira spp., leads to the synthesis of bacteria. , riboflavin, nicotinic acid and other B vitamins in the intestine. The duration of the therapeutic effect is 7 hours.

Pharmacokinetics

Absorption After taking the drug inside, the active substances are quickly and completely absorbed from the gastrointestinal tract. Cmax in the blood plasma is achieved within 1-4 hours after ingestion. Distribution Trimethoprim penetrates well into tissues and biological environments of the body: lungs, kidneys, prostate, bile, saliva, phlegm, cerebrospinal fluid. The 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.

Indications

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); - skin and soft tissue infections (including furunculosis, pyoderma).

Contraindications

Established 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 associated with a deficiency of folic acid); - hyperbilirubinemia in children; - deficiency of glucose-6-phosphate dehydrogenase (risk of hemolysis); - pregnancy; - lactation; - children under 3 years of age (for this dosage form); - hypersensitivity to the components of the drug; - hypersensitivity to sulfonamides.

Precautionary measures

Application during pregnancy and lactation

Biseptol is contraindicated for use during pregnancy and lactation (breastfeeding).

Method of administration and dosage

Set individually. The drug is taken after meals with a sufficient amount of liquid. 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 In case of 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. In gonorrhea, the dose of the drug is 2 g (in terms of sulfamethoxazole) 2 times / day with an interval between doses of 12 hours. Adults and children over 12 years of age are prescribed the drug 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 a severe course of the disease and / or in chronic infections, a single dose may be increased by 30-50%. If the course of therapy lasts more than 5 days and / or an increase in the dose of the drug, it is necessary to monitor the peripheral blood picture; 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 Biseptol should be reduced by 50%.

Side effects

From the side of the central nervous system and peripheral nervous system: headache, dizziness; in some cases - aseptic meningitis, depression, apathy, tremor, peripheral neuritis. On the part of the respiratory system: bronchospasm, choking, cough, pulmonary infiltrates. On the part of the digestive system: nausea, vomiting, loss of appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of hepatic transaminases, hepatitis, sometimes with cholestatic jaundice, hepatonecrosis, pseudomembranous enterocolitis, pancreatitis. On the part of the hematopoietic system: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic hemorrhage 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: allergic reactions. , urticaria, medicinal fever, rash, erythema multiforme exudative (incl. Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, allergic myocarditis, fever, angioedema, hyperemia of the sclera. From the metabolic side: hypoglycemia, hyperkalemia, hyponatremia. The drug is generally well tolerated.

Overdose

Symptoms: lack of appetite, intestinal colic, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness, fever, hematuria, crystalluria are also possible. Later, bone marrow depression and jaundice may develop. After acute poisoning with trimethoprim, nausea, vomiting, dizziness, headache, depression, 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: use co-trimoxazole in high doses for a long period can lead to depression of bone marrow function, manifested by thrombocytopenia, leukopenia or megaloblastic anemia. Treatment: discontinuation of the drug and taking measures aimed at removing it from the gastrointestinal tract (wash the stomach no later than 2 hours after ingestion drug or induce vomiting), drinking plenty of fluids if diuresis is insufficient, and kidney function is preserved. Introduce calcium folinate (5-10 mg / day). The acidic environment of urine accelerates the excretion of trimethoprim, but may also increase the risk of crystallization of sulfonamide in the kidneys. The blood picture, the composition of electrolytes in plasma and other biochemical parameters should be monitored. Hemodialysis is moderately effective and peritoneal dialysis is not effective.

Interaction with other drugs

With the simultaneous use of Biseptol with thiazide diuretics, there is a risk of thrombocytopenia and bleeding (the combination is not recommended). Co-trimoxazole increases the anticoagulant activity of indirect anticoagulants, as well as the effect of hypoglycemic drugs and methotrexate. Co-trimoxazole reduces the intensity of hepatic metabolism T1 / 2 by 39%) and warfarin, increasing their effect. Rifampicin reduces the T1 / 2 of trimethoprim. With the simultaneous use of pyrimethamine in doses exceeding 25 mg / week, increases the risk of megaloblastic anemia. With the simultaneous use of diuretics (usually thiazides) increase the risk of developing thrombocytopenia. Benzocaine, procaine, procainamide (as well as other drugs, as a result of hydrolysis of which PABA is formed) reduce the effectiveness of Biseptol. Between diuretics (including thiazides, furosemide) and oral hypoglycemic agents (sulfonylurea derivatives) on the one hand, and anti-tank on the other hand, the development of a cross-allergic reaction is possible. 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 (as well as other acidifying drugs urine) increase the risk of crystalluria during the use of Biseptol. Colestyramine reduces absorption when taken simultaneously with other drugs, so it should be taken 1 hour after or 4-6 hours before taking co-trimoxazole. When used simultaneously with drugs that inhibit bone marrow hematopoiesis, the risk of myelosuppression increases. In some cases, Biseptol may increase the concentration of digoxin in the blood plasma in elderly patients. Biseptol may decrease the effectiveness of tricyclic antidepressants. In patients after kidney transplantation, with one With the temporary 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. Reduces the effectiveness of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal agents).

special instructions

The drug is prescribed with caution in case of a burdened allergic history. With prolonged (more than a month) courses of treatment, regular blood tests are necessary, since there is a possibility of hematological changes (most often asymptomatic). These changes can be reversible when folic acid is prescribed (3-6 mg / day), which does not significantly violate the antimicrobial activity of the drug. Particular care is needed when treating elderly patients or patients with suspected baseline folate deficiency. Prescribing folic acid is also advisable for long-term treatment with the drug in high doses.To prevent crystalluria, it is recommended to maintain a sufficient volume of urine excreted. The likelihood of toxic and allergic complications of sulfonamides significantly increases with a decrease in the filtration function of the kidneys. It is also inappropriate during treatment to eat foods containing a large amount of PABA - green parts of plants (cauliflower, spinach, legumes), carrots, tomatoes. Excessive sun exposure and UV radiation. The risk of side effects is significantly higher in AIDS patients. It is not recommended to use the drug for tonsillitis and pharyngitis caused by β-hemolytic group A streptococcus, due to widespread resistance of strains. method, however, does not affect the result when choosing a radioimmunological method. Co-trimoxazole can increase the results of Jaffe's reaction with picric acid for the quantitative determination of creatinine by 10%.

Composition

One tablet contains

active substances: trimethoprim 20 mg, 80 mg;

sulfamethoxazole 100 mg, 400 mg,

excipients: potato starch, talc, magnesium stearate, polyvinyl alcohol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, propylene glycol.

Description

Tablets from white to white with a yellowish sheen, round, with a flat surface, beveled, engraved with "Bs" on one side, with a diameter of 7.8 to 8.3 mm (for a dosage of 120 mg).

Tablets from white to white with a yellowish sheen, round, with a flat surface, beveled, scored and engraved "Bs" above the score on one side, with a diameter of 12.80 to 13.40 mm (for a dosage of 480 mg).

Pharmacotherapeutic group

Antibacterial drugs for systemic use. Sulfonamides and trimethoprim. Sulfonamides in combination with trimethoprim and its derivatives. Co-trimoxazole.

ATX code J01EE 01

Pharmacological properties

Pharmacokinetics

Both components of the drug are rapidly absorbed from the digestive tract; the maximum concentration of both components in the blood serum is reached within 1-4 hours after ingestion. The volume of distribution of trimethoprim is about 130 liters, sulfamethoxazole - about 20 liters. 45% of trimethoprim and 66% of sulfamethoxazole are bound to plasma proteins.

The distribution of both compounds is different; sulfanilamide is distributed exclusively in the extracellular space, trimethoprim is distributed in all body fluids. A high concentration of trimethoprim is observed, including in the secretions of the bronchial glands, prostate gland and bile. Sulfamethoxazole concentrations in biological fluids are lower. Both compounds appear at effective concentrations in sputum, vaginal secretions, and middle ear fluid.

The volume of distribution of sulfamethoxazole is 0.36 dm3kg, trimethoprim - 2.0 dm3kg.

Both drugs are metabolized in the liver, sulfonamide by acetylation and binding with glucuronic acid, trimethoprim by oxidation and hydroxylation.

Both drugs are excreted from the body mainly through the kidneys, both by filtration and by active tubular secretion. The concentration of active compounds in urine is significantly higher than in blood. Within 72 hours, 84.5% of the accepted dose of sulfonamide and 66.8% of trimethoprim are excreted in the urine.

The serum half-life is 10 hours for sulfamethoxazole and 8-10 hours for trimethoprim, respectively.

Both sulfamethoxazole and trimethoprim enter human milk and the fetal circulatory system.

Pharmacokinetics in special clinical situations

Elderly and senile patients

With normal renal function, the half-life of both components of the drug changes slightly.

Patients with impaired renal function

In patients with renal insufficiency (creatinine clearance 15-30 ml / min), the half-lives of both components of the drug increase, which requires dose adjustment.

Pharmacodynamics

Combined bactericidal preparation containing sulfamethoxazole, an intermediate-acting sulfonamide that inhibits the synthesis of folinic acid by competitive antagonism with para-aminobenzoic acid, and trimethoprim, an inhibitor of the bacterial reductase of dehydrofolinic acid, which is responsible for the synthesis of biologically active tetrahydrofolinic acid. The combination of components acting on the same chain of biochemical transformations leads to a synergistic antibacterial action; believe that due to the combination of two active substances, the development of bacterial resistance is slower than in the case of using one active substance.

Co-trimoxazole is a broad-spectrum bactericidal agent, active against almost all groups of microorganisms - gram-negative bacteria: Salmonella spp., Shigella spp., Neisseria spp., Proteus vulgaris, Vibrio cholerae, Yersinia spp., Escherichia coli, Corynebacterium spp .; gram-positive bacteria: Staphylococcus spp. and others. Chlamydia spp., Actinomyces spp., Klebsiella spp .. are also sensitive to the drug.

Indications for use

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

Acute otitis media in children due to drug-sensitive strains of Str. pneumoniae and H. influenzae

Exacerbation of chronic bronchitis in adults caused by susceptible strains of Streptococcus pneumoniae

or H. influenzae if the combination drug is more effective than monotherapy in the opinion of the clinician

Microbiologically confirmed pneumonia due to Pneumocystis carinii and prevention of infection with this microorganism in high-risk patients (such as those with AIDS)

Urinary tract infections in adults and children caused by susceptible strains of E. coli, Klebsiella sp., Enterobacter sp., Morganella morganii, Proteus mirabilis and Proteus vulgaris (except for uncomplicated infections)

Gastrointestinal tract infections in adults and children caused by the sticks Shigella flexneri and Shigella sonnei, if antibiotic therapy is indicated), travelers' diarrhea caused by enterotoxic strains of Escherichia coli, cholera (in addition to fluid and electrolyte replacement).

Method of administration and dosage

The drug is administered orally after meals with a sufficient amount of liquid.

Children from 6 to 12 years old: 240-480 mg 2 times a day after 12 hours.

Adults and children over 12 years old: 960 mg once, or 480 mg 2 times a day. The daily dose should not exceed 1920 mg (4 tablets of 480 mg).

The course of treatment is 7 to 10 days. In chronic infections, the course of treatment is longer and depends on the severity of the disease.

In acute infectious diseases, the course of treatment is 5 days, if after 7 days there is no clinical improvement, it is necessary to consider correcting the treatment in connection with the possible resistance of the pathogen.

Dosing in special cases:

Pneumocystis carinii pneumonia in adults and children:

The maximum daily dose for patients with diagnosed infection is 90-120 mg / kg body weight of Biseptol, divided into parts, taken every 6 hours for 14 days.

Prevention of Pneumocystis carinii infection and toxoplasmosis:

Adults and children over 12 years of age: 960 mg Biseptol (two 480 mg tablets) once a day.

Children from 6 to 12 years old: Biseptol 960 mg per day, divided into two equal doses after 12 hours for three days. The daily dose should not exceed 1920 mg (4 tablets of 480 mg).

For patients with creatinine clearance of 15-30 cm3 / min, the dose should be halved, with creatinine clearance less than 15 cm3 / min, the use of co-trimoxazole is not recommended.

Elderly patients

The drug should be taken with caution in elderly patients due to the increased risk of side effects, especially in patients with renal / hepatic impairment or taking other drugs at the same time.

Unless otherwise indicated, standard doses of the drug should be taken.

Side effects

Nausea, vomiting

Rash, itching

Agranulocytosis, aplastic anemia, hemolytic anemia, megaloblastic anemia, eosinophilia, hypoprothrombinemia, leukopenia, methemoglobinemia, neutropenia, thrombocytopenia, autoimmune or aplastic pancytopenia, granulocytopenia

Allergic myocarditis, chills, drug fever, colliquation necrosis of the skin, photosensitivity, anaphylactic reactions, vasomotor edema, pruritus, allergic rash, Schönlein-Henoch disease, urticaria, polymorphic erythema, generalized skin reactions, Steve's syndrome, exfoliation syndrome Johnson's syndrome, Lyell's syndrome (toxic epidermal necrolysis, symptoms of hypersensitivity of the respiratory system, periarteritis nodosa, lupus-like syndrome, conjunctival and scleral hyperemia

Diarrhea, abdominal pain, lack of appetite, nausea, pseudo-diphtheria inflammation of the intestine, vomiting, increased serum transaminases and creatinine levels, inflammation of the oral cavity, inflammation of the tongue, pancreatitis, hepatitis, sometimes with cholestatic jaundice or liver necrosis

Crystalluria, renal failure, interstitial nephritis, nephrotoxic syndrome with oliguria or anuria, an increase in non-protein nitrogen and serum creatinine, increased urine output (in patients with cardiac edema)

Hypokalemia, hyponatremia, hyperglycemia

Apathy, aseptic meningitis, coordination disorder, headache, depression, convulsions, hallucinations, nervousness, tinnitus, inflammation of the peripheral nerves, dizziness, weakness, fatigue, insomnia

Joint pain, muscle pain, rhabdomyolysis

Choking, coughing, lung infiltrates.

Contraindications

Hypersensitivity to the drug, its components, drugs from the co-trimoxazole group

Severe damage to the liver parenchyma, hyperbilirubinemia (in children)

Acute renal failure, in which it is impossible to determine the concentration of the drug in the blood plasma

Blood diseases (aplastic anemia, B12-deficiency anemia, agranulocytosis, leukopenia)

Simultaneous reception with dofetilide

Lack of glucose-6-phosphate dehydrogenase (the likelihood of hemolysis)

Pregnancy and lactation.

Children under 6 years old

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

Drug interactions

Dofetilide can cause ventricular arrhythmias with prolongation of the QT interval, including torsades de pointes, which are directly related to the concentration of dofelitide in the blood plasma.

With the simultaneous use of certain diuretics (mainly thiazides), the risk of thrombocytopenia increases, especially in elderly and senile patients.

Biseptol may enhance the effect of anticoagulants to the extent that dose modification is required.

Biseptol inhibits the metabolism of phenytoin. In patients taking both drugs, the elimination half-life of phenytoin is increased by about 39% and the clearance of phenytoin is reduced by about 27%.

Biseptol increases the concentration of the free fraction of methotrexate in serum by displacing it from the bonds with proteins.

Influence on the results of laboratory tests.

Trimethoprim can interfere with the results of the determination of the concentration of methotrexate in serum by the enzymatic method, but does not affect them if the determination is carried out by radioimmunoassay methods.

Biseptol can overestimate by about 10% the results of the Jaffe test with basic picrate for creatinine.

Biseptol can potentiate the effect of simultaneously taken hypoglycemic drugs, derivatives of sulfonylureas, and thus increase the risk of hypoglycemia.

Biseptol may increase the plasma concentration of digoxin in some elderly patients.

Biseptol may reduce the effectiveness of tricyclic antidepressants.

In patients after kidney transplantation treated with Biseptol and cyclosporine, transient dysfunctions of the transplanted kidney are observed, manifesting an increase in serum creatinine, which is probably due to the action of trimethoprim.

Biseptol with pyrimethamine can cause megaloblastic anemia.

Sulfonamides show chemical similarities to some antithyroid drugs, diuretics (acetazolamide and thiazides), and oral antidiabetic drugs, which can cause cross-allergy.

special instructions

Rare cases of life-threatening complications associated with sulfonamides have been described, including Stevens-Johnson syndrome, Lyell's syndrome, acute liver necrosis, aplastic anemia, other bone marrow injuries, and airway sensitization.

If, during treatment with Biseptol, symptoms appear that indicate the possibility of complications, especially a rash, sore throat, fever, joint pain, cough, choking or hepatitis, you should stop taking the drug and immediately consult a doctor.

Use with caution is necessary when prescribing co-trimoxazole to patients with a deficiency of folic acid (the elderly, persons suffering from alcohol dependence, malabsorption syndrome), porphyria, thyroid dysfunction, bronchial asthma and a history of allergic reactions. If a skin rash or diarrhea occurs during treatment with Biseptol, it should be stopped immediately.

In patients with glucose-6-phosphate dehydrogenase deficiency, Biseptol may cause hemolysis.

In elderly patients, the risk of severe side effects of Biseptol increases, including kidney or liver damage. The most commonly reported severe side effects of Biseptol in elderly patients are severe skin reactions, bone marrow suppression, and thrombocytopenia with or without purpura. Taking Biseptol and diuretics together increases the risk of purpura.

AIDS patients taking Biseptol for diseases caused by Pneumocystis carinii are more likely to have undesirable effects, especially rash, fever, leukopenia, increased serum aminotransferase levels, hypokalemia and hyponatremia.

When prescribing Biseptol to patients who are already receiving anticoagulants, one should remember about the possible increase in the anticoagulant effect. In such cases, it is necessary to re-determine the blood clotting time.

The drug should not be administered to patients with hereditary fructose intolerance.

Care must be taken in patients with porphyria or thyroid dysfunction.

In patients taking high doses of Biseptol, serum potassium should be monitored regularly. Large doses of Biseptol, which are used in the treatment of Pneumocystis pneumonia, can lead to a progressive but reversible increase in serum potassium in a significant number of patients. Even taking the recommended doses of the drug can cause hyperkalemia if it is prescribed against a background of potassium metabolism disorders, renal failure, or the simultaneous administration of drugs that provoke hyperkalemia.

When treating with large doses of Biseptol, the possibility of hypoglycemia should be considered, usually a few days after starting treatment. The risk of hypoglycemia is higher in patients with impaired renal function, liver disease, and malnutrition.

While taking Biseptol (as well as while taking other antibacterial agents), pseudomembranous enterocolitis of varying severity from mild to life-threatening can develop, therefore, timely diagnosis of this disease in patients who develop diarrhea during the use of an antibacterial drug is important.

Treatment with antibacterial agents alters the physiological flora of the colon and can cause an excessive increase in the number of anaerobic rods. Toxins produced by Clostridium difficile are one of the main causes of enterocolitis.

In cases of a mild course of pseudomembranous enterocolitis, discontinuation of the drug is usually sufficient; in more severe cases, correction of the water-electrolyte balance, the introduction of proteins and antibacterial agents active against Clostridium difficile (metronidazole or vancomycin) is necessary. Do not administer drugs that inhibit peristalsis or other drugs that have an astringent effect. The product contains parahydroxybenzoates, which can cause allergic reactions (rash, itching) and propylene glycol, which can cause symptoms similar to those after drinking.

Excessive sun and UV exposure should be avoided.

Features of the influence of the drug on the ability to drive a vehicle and potentially dangerous mechanisms.

When using the drug, side effects such as headache, dizziness, convulsions, nervousness and fatigue may occur, therefore, care should be taken when driving a vehicle and potentially dangerous machinery.

Overdose

Symptoms: lack of appetite, colic pain, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness. Fever, hematuria, and crystalluria may appear. In a later period, bone marrow damage and hepatitis may develop. Long-term use of large doses of Biseptol for a long time can cause bone marrow depression, which manifests itself as thrombocytopenia, leukopenia, or megaloblastic anemia.

Treatment: gastric lavage (no later than 2 hours after taking the drug), drinking plenty of fluids, forced diuresis. Acidification of urine speeds up the elimination of trimethoprim, but may increase the risk of sulfonamide crystallization in the kidneys. The blood picture, serum electrolytes and other biochemical parameters of the patient should be monitored. Hemodialysis is moderately effective; peritoneal dialysis is ineffective.

Storage period

Do not use after the expiration date.

Terms of dispensing from pharmacies

On prescription

Manufacturer

Pabyanitsk pharmaceutical plant Polfa JSC

st. march. Pilsudski 5, 95-200 Pabianice, Poland