Biseptol, 480 mg tablets 28 pcs

A combined antibacterial drug, contains sulfamethoxazole and trimethoprim.

Sulfamethoxazole, 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 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.

The drug is resistant to: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira spp., 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

Assimilation

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

Pdistribution

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Trimethoprim penetrates well into body tissues and biological media: 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 the kidneys; trimethoprim is excreted unchanged up to 50%; sulfamethoxazole – 15-30% in the 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

1 tablet contains:

Active substances:sulfamethoxazole – 400 mg, trimethoprim – 80 mg.

Excipients: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 of 120 mg) 2 times a day; in children aged 6 to 12 years 480 mg (4 tablets of 120 mg or 1 tablet of 480 mg) 2 times a day.

In case of pneumonia the drug is indicated 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 use 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, with long-term therapy at 480 mg 2 times a day.

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

If the course of therapy lasts more than 5 days and/or the dose is increased the peripheral blood picture must be controlled; in case of pathological changes it is necessary to administer folic acid in the dose of 5-10 mg/day.

If a dose is missed, the drug should be taken as soon as possible. If the time for 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

In concomitant use of Biseptol with thiazide diuretics there is a risk of thrombocytopenia and bleeding (combination is not recommended).

Co-trimoxazole increases anticoagulant activity of indirect anticoagulants as well as the effect of hypoglycemic drugs and methotrexate.

Co-trimoxazole decreases intensity of hepatic metabolism of phenytoin (increases its T1/2 by 39%) and warfarin, increasing their action.
Rifampicin decreases T1/2 of trimethoprim.

Concurrent use of pyrimethamine in doses greater than 25 mg/week increases the risk of megaloblastic anemia.

When used concomitantly, diuretics (often thiazides) increase the risk of thrombocytopenia.

Benzocaine, procaine, procainamide (as well as other drugs whose hydrolysis produces PABA) reduce the effectiveness of Biseptol.
Between diuretics (including
A cross-allergic reaction may develop between diuretics (including thiazides, furosemide) and oral hypoglycemic agents (sulfonylurea derivatives) on the one hand, and antibacterial agents of sulfonamide group on the other hand.
Phenytoin, barbiturates, PASC increase manifestations of folic acid deficiency when used simultaneously with Biseptol.

Salicylic acid derivatives increase the effect of Biseptol.

Ascorbic acid, hexamethylantetramine (as well as other drugs that acidify the urine) increase the risk of crystalluria with Biseptol.

Colestiramine reduces absorption when taken simultaneously with other drugs, so it should be taken 1 h after or 4-6 h before taking co-trimoxazole.

Concurrent use with drugs that inhibit bone marrow hematopoiesis increases the risk of myelosuppression.
In some cases, Biseptol® may increase the plasma concentration of digoxin in elderly patients.
Biseptol® may decrease the effectiveness of tricyclic antidepressants.

In patients after kidney transplantation, when concomitant use of co-trimoxazole and cyclosporine, there is a transient impairment of transplanted kidney function manifested by increased serum creatinine concentrations, which is probably caused by the action of trimethoprim.
Reduces the effectiveness of oral contraception (inhibits intestinal microflora and reduces intestinal hepatic circulation of hormones).

Special Instructions

Biseptol is prescribed with caution in a history of allergic reactions.

With long (more than a month) courses of treatment regular blood tests are required, 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 impair 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 reasonable during long-term treatment with the drug in high doses.

For prevention of crystalluria it is recommended to maintain sufficient volume of urine excreted. The likelihood of toxic and allergic complications of sulfonamides increases significantly with decreased renal filtration function.

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

Excessive sunlight and UV exposure should be avoided.
The risk of side effects is much higher in AIDS patients.

Biseptol is not recommended for tonsillitis and pharyngitis caused by group A β-haemolytic streptococcus because of widespread resistance of the strains.

Trimethoprim can change the results of enzyme-linked serum methotrexate levels, but does not affect the results when a radioimmunoassay is chosen.

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

Contraindications

– established damage to the liver parenchyma;

– marked renal dysfunction when there is no possibility to control the drug concentration in the blood plasma;

– 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 prescribed with caution in case of folic acid deficiency in the body, 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.

Digestive system disorders: Nausea, vomiting, decreased appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of liver transaminases, hepatitis, sometimes with cholestatic jaundice, hepatonecrosis, pseudomembranous enterocolitis, pancreatitis.

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

Urinary system disorders: polyuria, interstitial nephritis, renal dysfunction, crystalluria, hematuria, increased concentration of urea, hypercreatininemia, toxic nephropathy with oliguria and anuria.

Muscular system: arthralgia, myalgia.

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

Metabolism: 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 trimethoprim poisoning, 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), plenty of drinking 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