Biseptol, tablets 120 mg 20 pcs

Pharmacological group: Antibacterial sulfonamide drug

Pharmacotherapeutic group: Antimicrobial combination drug

Pharmacological action

A 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 incorporation of PABA into its molecule.

Trimethoprim enhances the effect of sulfamethoxazole by disrupting the reduction of dihydrofolic acid to tetrahydrofolic acid, the active form of folic acid responsible for protein metabolism and microbial cell division.

It is a broad-spectrum bactericidal drug.

It is active against Gram-positive aerobic bacteria: Streptococcus spp. including Streptococcus pneumoniae (hemolytic strains are more sensitive to penicillin), Staphylococcus spp, Bacillus anthracis, Listeria spp, Nocardia asteroides, Enterococcus faecalis, Mycobacterium spp. (including Mycobacterium leprae, excluding Mycobacterium tuberculosis); Gram-negative aerobic bacteria: Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (including enterotoxigenic 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., Legionella pneumopbila, Providencia, some Pseudomonas species (except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp, Yersinia spp., Morganella spp. as well as against Chlamydia spp. (including Chlamydia trachomatis, Chlamydia psittaci); against Gram-positive anaerobes: Actinomyces israelii; against protozoa: Plasmodium spp., Toxoplasma gondii; against pathogenic fungi: Coccidioides immitis, Histoplasma capsulatum, Pneumocystis carinii, Leishmania spp.

Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira spp. are resistant to the drug, viruses.

Depresses the activity of E. coli, which leads to a decrease in the synthesis of thiamine, riboflavin, nicotinic acid and other B vitamins in the intestine.

The duration of therapeutic action is 7 hours.

Pharmacokinetics

absorption

After oral administration the active substances are completely absorbed from the gastrointestinal tract. Cmax in plasma is reached within 1-4 hours after oral administration.

Distribution

Trimethoprim penetrates well into tissues and biological media of the body: lungs, kidneys, prostate, bile, saliva, sputum, cerebrospinal fluid. Binding of trimethoprim with plasma proteins is 50%; sulfamethoxazole – 66%.

Elimation

T1/2 of trimethoprim is 8.6-17 h, of sulfamethoxazole 9-11 h. The main route of excretion is renal; 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, sinusitis;

– urinary tract infections (including

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

– gonorrhea;

– gastrointestinal infections (including

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

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

Active ingredient

Composition

Active ingredients:

Sulfamethoxazole 100 mg,

Trimethoprim 20 mg;

Auxiliary substances:

Potato starch, talc, magnesium stearate, polyvinyl alcohol, methyl parahydroxybenzoate, propyl parahydroxybenzoate, propylene glycol.

How to take, the dosage

The drug is taken orally after a meal with plenty of fluid. The dose is set individually.

In children aged 3 to 5 years, 240 mg (2 tablets 120 mg) 2 times a day; in children aged 6 to 12 years 480 mg (4 tablets 120 mg or 1 tablet 480 mg) 2 times a day.

In case of pneumonia the drug is indicated at the rate of 100 mg sulfamethoxazole per 1 kg of body weight/day. The interval between doses is 6 hours; duration of therapy is 14 days.

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

In adults and children over 12 years of age the drug is prescribed at 960 mg 2 times a day; if prolonged therapy, 480 mg 2 times a day.

The course of treatment is from 5 to 14 days. In case of severe disease and/or chronic infections it is possible to increase a single dose by 30-50%.

If the course of therapy lasts more than 5 days and/or if the dose is increased the peripheral blood count should be monitored; in case of pathological changes the folic acid should be prescribed in the dose of 5-10 mg/day.

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

In patients with renal impairment with a CK of 15-30 ml/min, the standard dose of the drug should be reduced by 50%; in CK less than 15 ml/min, the drug is not recommended.

Interaction

Special Instructions

The drug is prescribed with caution in folic acid deficiency in the body, bronchial asthma, thyroid disease, with a history of allergies.

The drug is not recommended for tonsillitis and pharyngitis caused by ?-hemolytic streptococcus group A because of widespread resistance of strains.

In long (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 may be reversed with folic acid (3-6 mg/day), which does not significantly compromise the antimicrobial activity of the drug. Particular caution is required when treating elderly patients or patients with suspected underlying folate deficiency. Administration of folic acid is also advisable during long-term treatment with the drug in high doses.

It is also inadvisable to use foods containing large amounts of PABA, such as green parts of plants (cauliflower, spinach, legumes), carrots, and tomatoes.

Overexposure to sunlight and UV radiation should be avoided.

The risk of side effects is much higher in AIDS patients.

Trimethoprim may change the results of determining methotrexate levels in serum given by the enzymatic method, but does not affect the result when a radioimmunoassay is chosen.

Co-trimoxazole can increase by 10% the results of the Jaffe reaction with picric acid for the quantification of creatinine.

– Use in liver dysfunction The drug is contraindicated if liver parenchyma damage is established.

– Use in renal dysfunction The drug is contraindicated in severe renal dysfunction (creatinine clearance (CK) less than 15 ml/min). In patients with renal insufficiency at a CKR of 15-30 ml/min the standard dose of Biseptol should be reduced by 50%. To prevent crystalluria, it is recommended to maintain an adequate volume of urine excreted. The likelihood of toxic and allergic complications of sulfonamides increases significantly with decreased renal filtration function.

Contraindications

– established damage to the liver parenchyma;

– marked impairment of renal function in the absence of the possibility to control plasma concentrations of the drug;

– severe renal insufficiency (CK less than 15 ml/min);

– severe blood disorders (aplastic anemia, B12-deficiency anemia, agranulocytosis, leukopenia, megaloblastic anemia, anemia associated with folic acid deficiency);

– hyperbilirubinemia in children;

– glucose-6-phosphate dehydrogenase deficiency (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.

The drug is used with caution in folic acid deficiency, bronchial asthma, thyroid diseases.

Side effects

The drug is generally well tolerated.

Nervous system disorders:headache, dizziness; in some cases – aseptic meningitis, depression, apathy, tremor, peripheral neuritis.

Respiratory system: bronchospasm, choking, cough, pulmonary infiltrates.

The digestive system: nausea, vomiting, decreased appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased liver transaminase activity, hepatitis, sometimes with cholestatic jaundice, hepatonecrosis, pseudomembranous enterocolitis, pancreatitis.

Hematopoietic system:Leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia, aplastic and hemolytic anemia, eosinophilia, hypoprothrombinemia, methemoglobinemia.

With regard to the urinary system: polyuria, interstitial nephritis, impaired renal function, crystalluria, hematuria, increased concentration of urea, hypercreatininemia, toxic nephropathy with oliguria and anuria.

Muscular system disorders: arthralgia, myalgia.

Allergic reactions:Itching, photosensitization, urticaria, drug fever, rash, erythema multiforme (including erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell syndrome), exfoliative dermatitis, allergic myocarditis, increased body temperature, angioedema, sclera hyperemia.

Metabolic disorders: hypoglycemia, hyperkalemia, hyponatremia.

Overdose

Symptoms: in sulfonamide overdose – lack of appetite, intestinal colic, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness, fever, hematuria, crystalluria are also possible. Bone marrow depression and jaundice may develop later.

After acute poisoning with trimethoprim, nausea, vomiting, dizziness, headache, depression, impaired consciousness, depressed bone marrow function may occur.

It is not known what dose of co-trimoxazole may be life-threatening.

Chronic poisoning: use of co-trimoxazole in high doses over a prolonged period may lead to suppression of bone marrow function, manifested by thrombocytopenia, leukopenia, or megaloblastic anemia.

Treatment: discontinue the drug and take measures to remove it from the gastrointestinal tract (perform gastric lavage within 2 hours of taking the drug or induce vomiting), drink copiously if diuresis is insufficient and renal function is preserved. Administer calcium folinate (5-10 mg/day). An acidic urine environment accelerates excretion of trimethoprim, but may also increase the risk of sulfonamide crystallization in the kidneys.

The blood count, plasma electrolyte composition and other biochemical parameters should be monitored. Hemodialysis is moderately effective and peritoneal dialysis is ineffective.

Similarities