Biseptol, pills 120mg, 20pcs

Composition

Active ingredients:  

Sulfamethoxazole 100 mg,

Trimethoprim 20 mg;

Auxiliary substances:  

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

Pharmacological action

Clinical and pharmacological group: Antibacterial sulfonamide preparation

Pharmaco-therapeutic group: Antimicrobial combined agent

Pharmacological action

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 action 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.

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 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., Legionella pneumopbila, Providencia, some species of Pseudomonas (except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp., Yersinia spp., Morganella spp., as well as Chlamydia spp. (including Chlamydia trachomatis, Chlamydia psittaci); against gram-positive anaerobes: Actinomyces israelii; against 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., viruses.

Inhibits the vital activity of Escherichia 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

Suction

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

Distribution

Trimethoprim penetrates well into the tissues and biological environments of the body: lungs, kidneys, prostate, bile, saliva, sputum, cerebrospinal fluid. The binding of trimethoprim to plasma proteins is 50%; sulfamethoxazole-66%.

Elimination

of T1 / 2 trimethoprim – 8.6-17 hours, sulfamethoxazole-9-11 hours. The main route of elimination is the kidneys; trimethoprim is excreted unchanged up to 50%; sulfamethoxazole-15-30% in active form.

Indications

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

— respiratory tract infections (including bronchitis, pneumonia, lung abscess, empyema);

— otitis media, sinusitis,

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

gonorrhoea;

infection of the gastrointestinal tract (including typhoid fever, paratyphoid fever, shigellosis, cholera, diarrhea);

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

Contraindications

— set damage of the liver parenchyma;

— severe renal dysfunction in the absence of control of drug concentration in plasma;

— renal failure severe (CC less than 15 ml/min);

severe blood disorders (aplastic anemia,12 deficiency anemia, agranulocytosis, leukopenia, megaloblastic anemia, anemia associated with folic acid deficiency);

— hyperbilirubinemia in children;

— deficiency of glucose-6-phosphate dehydrogenase (risk of hemolysis);

— pregnancy;

— lactation;

— children’s age up to 3 years (for this dosage form);

— hypersensitivity to the components of the drug;

— hypersensitivity to sulfonamides.

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

Side effects

The drug is generally well tolerated.

From the nervous system: headache, dizziness; in some cases-aseptic meningitis, depression, apathy, tremor, peripheral neuritis.

From the respiratory system: bronchospasm, choking, cough, pulmonary infiltrates.

From the digestive system: nausea, vomiting, decreased appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of hepatic transaminases, hepatitis, sometimes with cholestatic jaundice, hepatonecrosis, pseudomembranous enterocolitis, pancreatitis.

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

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

Musculoskeletal disorders: arthralgia, myalgia.

Allergic reactions: pruritus, photosensitivity, urticaria, drug fever, rash, erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), exfoliative dermatitis, allergic myocarditis, fever, angioedema, scleral hyperemia.

From the side of metabolism: hypoglycemia, hyperkalemia, hyponatremia.

Interaction

Biseptol may reduce the effectiveness of tricyclic antidepressants. In patients after kidney transplantation, with the simultaneous use of co-trimoxazole and cyclosporine, there is a passing violation of the function 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 hormones). When Biseptol is co-administered 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 of phenytoin (increases its T 1/2 by 39%) and warfarin, increasing their effect. Rifampicin reduces T 1/2 of trimethoprim. Simultaneous use of pyrimethamine in doses exceeding 25 mg / week increases the risk of megaloblastic anemia. Concomitant use of diuretics (most commonly thiazides) increases the risk of thrombocytopenia. Benzocaine, procaine, procainamide (as well as other drugs that hydrolyze PABA) reduce the effectiveness of Biseptol. Between diuretics (including thiazides, furosemide ) and oral hypoglycemic agents (sulfonylureas), on the one hand, and antibacterial agents of the sulfonamide group, on the other hand, a cross – allergic reaction may develop. Phenytoin, barbiturates, and PASC increase the manifestations of folic acid deficiency when used concomitantly with Biseptol. Salicylic acid derivatives enhance the effect of Biseptol. Ascorbic acid, hexamethylenetetramine (as well as other drugs that acidify the urine) increase the risk of crystalluria during the use of Biseptol. Colestyramine reduces absorption when taken concomitantly with other medications, so it should be taken 1 hour after or 4-6 hours before taking co-trimoxazole. When used concomitantly with drugs that inhibit bone marrow hematopoiesis, the risk of developing myelosuppression increases. In some cases, Biseptol may increase the plasma concentration of digoxin in elderly patients.

How to take it, course of use and dosage

The drug is taken orally after a meal, washed down with a sufficient amount of liquid. The dose is set individually.

Children aged 3 to 5 years are prescribed 240 mg (2 tablets of 120 mg) 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.

For 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 admission 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 severe cases of the 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 of the drug is increased, it is necessary to monitor the picture of peripheral blood; if pathological changes occur, folic acid should be prescribed at a 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 compensate for the missed one.

In patients with renal insufficiency with a creatinine clearance of 15-30 ml/min, the standard dose of the drug should be reduced by 50%, with a creatinine clearance of less than 15 ml/min, it is not recommended to use the drug.

Overdose

Symptoms: with an overdose of sulfonamide – 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, confusion, and bone marrow suppression are possible.

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

Chronic poisoning: the use of co-trimoxazole in high doses for an extended period of time can lead to bone marrow suppression, manifested by thrombocytopenia, leukopenia or megaloblastic anemia.

Treatment: discontinue the drug and take measures aimed at its removal from the gastrointestinal tract (perform gastric lavage no later than 2 hours after taking the drug or induce vomiting), drink plenty of water if diuresis is insufficient, and kidney function is preserved. Enter calcium folinate (5-10 mg / day). The acidic environment of the urine accelerates the elimination of trimethoprim, but may also increase the risk of crystallization of sulfonamide in the kidneys.

It is necessary to monitor the blood picture, the composition of electrolytes in plasma and other biochemical parameters. Hemodialysis is moderately effective, while peritoneal dialysis is ineffective.

Special instructions

With caution, the drug is prescribed for folic acid deficiency in the body, bronchial asthma, thyroid diseases, a burdened allergic history.

It is not recommended to use the drug for tonsillitis and pharyngitis caused by ?- group A hemolytic streptococcus, due to widespread strain resistance.

For long-term (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 reversed with folic acid (3-6 mg/day), which does not significantly affect the antimicrobial activity of the drug. Special care should be taken when treating elderly patients or patients with suspected initial folate deficiency. use of folic acid is also advisable for long-term treatment with the drug in high doses.

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

Excessive sun and UV exposure should be avoided.

The risk of side effects is significantly higher in patients with AIDS.

Trimethoprim can change the results of determining the level of methotrexate in serum, given by the enzymatic method, but does not affect the result when choosing a radioimmunological method.

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

– Use in patients with impaired liver function, the drug is contraindicated in cases of established liver parenchyma damage.

– Use in patients with impaired renal function The drug is contraindicated in patients with severe renal impairment ( creatinine clearance (CC) is less than 15 ml / min). In patients with renal insufficiency with creatinine clearance of 15-30 ml/min, the standard dose of Biseptol should be reduced by 50%. To prevent crystalluria, it is recommended to maintain a sufficient volume of urine excreted. The probability of toxic and allergic complications of sulfonamides increases significantly with a decrease in the filtration function of the kidneys.

Form of production

Tablets

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Co-trimoxazole Sulfamethoxazole, Trimethoprim

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

Children as prescribed by a doctor, Children over 3 years of age

Indications

Otitis media, Infectious Diseases, Boils, Salmonellosis, Bronchitis, Pneumonia, Urethritis, Prostatitis