Biseptrim

Biseptrim is an antibacterial drug for systemic use. Contains a combination of sulfonamides and trimethoprim.

A complex bactericidal drug, which contains the element sulfamethoxazole (it is a sulfonamide with an average duration of exposure), which slows down the binding of B9-vitamin through the development of competitive antagonism with PABA. Also, the drug includes a component trimethoprim, which slows down microbial dihydrofolate reductase, which is responsible for the binding processes of bioactive tetrahydrofolate. [1]

Indications Biseptrim

It is applied in case of such violations:

• infections of the urethra associated with the action of drug-sensitive strains of Klebsiella, Morgan bacteria, Escherichia coli, common Proteus, Enterobacteriaceae and Proteus mirabilis;
• lesions in the digestive system associated with the Sonne and Flexner shigella strains (bacterial shigella);
• toxoplasmosis ;
• therapy and prevention of the development of pneumonia provoked by the influence of pneumocystis carinii (diagnosed bacteriologically);
• active stage of chronic bronchitis (in adults) and otitis media (in children), associated with drug-sensitive pneumococci and Haemophilus influenzae;
• diarrhea of travelers , provoked by E. Coli.

Release form

The release of the drug substance is realized in the form of tablets - 10 pieces inside the cell pack (inside the box - 2 such packs).

Pharmacodynamics

Co-trimoxazole demonstrates in vitro activity against Escherichia coli (this includes enteropathogenic strains), strains of the indole-positive type of Proteus (among them the common Proteus), Klebsiella, pneumococci, Morgan bacteria, Proteus mirabilis, Shigella Sonne and Flexner, enterobacteria and influenza coli. [2]

The combination of elements, acting on one of the chains of biochemical transformations, causes a synergism of the antibacterial effect and slows down the development of microbial resistance. [3]

Pharmacokinetics

Both elements of the drug are absorbed at a high rate into the blood from the gastrointestinal tract. Serum Cmax values of both components are noted after 1-4 hours from the moment of ingestion. Synthesis with whey protein is 70% (trimethoprim) and 44-62% (sulfamethoxazole).

The distribution processes of each substance are different: the distribution of sulfamethoxazole occurs only in the extracellular environment, and trimethoprim - inside all body fluids.

High values of trimethoprim are recorded inside the bronchial secretions, bile and prostate. The level of sulfamethoxazole inside fluids is slightly lower. Both elements are found in high values within sputum, middle ear fluid and vaginal secretions.

The indicator of the distribution volume of sulfamethoxazole is 360 ml / kg; trimethoprim - 2 l / kg. Both elements are involved in intrahepatic metabolic processes: sulfamethoxazole is acetylated and synthesized with glucuronic acid, while trimethoprim is oxidized and hydroxylated.

Excretion is mainly carried out through the kidneys - with the help of active secretion of the tubules and filtration. The indicator of active substances inside the urine significantly exceeds the blood values. During 72 hours, 84.5% of sulfamethoxazole and 66.8% of trimethoprim are excreted in the urine.

The half-life is 10 (sulfamethoxazole) and 8-10 hours (trimethoprim). With insufficient renal function, this indicator for both substances is prolonged.

Dosing and administration

You need to take the medicine orally, with food or after it, with plain water.

Teenagers from 12 years old and adults.

In case of inflammation in the area of the urethra, active stage of chronic bronchitis and infections of the digestive system associated with Shigella, an average of 2 tablets should be taken per day 2 times per day.

In case of inflammation in the area of the urinary tract, Biseptrim is used for 10-14 days, with infections of the gastrointestinal tract provoked by Shigella - 5 days, with the active stage of chronic bronchitis - 2 weeks.

To treat traveler's diarrhea, 2 tablets should be taken at 12-hour intervals until signs of illness disappear.

With toxoplasmosis, the drug is taken according to the schemes described below:

• 2 tablets per day during the 1st week;
• 2 tablets per day (taken every other day, 3 times a week);
• 2 tablets 2 times a day (every other day, 3 times a week).

In case of bacteriologically diagnosed pneumonia provoked by Pneumocystis carinii, 90-120 mg / kg of the drug should be used per day (divided into equal 1-fold portions). You need to take the tablets with 6-hour breaks in a period of 2-3 weeks. The same scheme is used for children 6-12 years old.

To prevent the development of pneumocystis pneumonia in people at risk, 2 tablets are used 1 time per day during the first week.

The daily serving size can be up to 1920 mg (4 tablets).

In persons with a CC level within 15-30 ml per minute, the dosage is halved.

For children 6-12 years of age.

With the active stage of otitis media, inflammation of the urethra and infection of the gastrointestinal tract associated with the activity of Shigella, 1 tablet is used 2 times a day.

In the case of inflammation of the urinary tract and otitis media, the drug is used for 10 days, and for infections in the gastrointestinal tract - 5 days.

• Application for children

The medicine in this form of release is not used in persons under the age of 6.

Use Biseptrim during pregnancy

Biseptrim should not be prescribed for HB and pregnancy.

Contraindications

The main contraindications:

• severe intolerance to the elements of the drug;
• failure of the liver / kidneys (CC indicator is below 15 ml per minute);
• anemia (megaloblastic, aplastic, folate deficient and pernicious type);
• leukopenia and agranulocytosis;
• lack of G6FD component;
• BA;
• hyperbilirubinemia in children;
• diseases in the thyroid gland.

Side effects Biseptrim

Among the side effects:

• disturbances in the activity of the National Assembly: dizziness and cephalalgia. Perhaps the development of depression, tremor, meningitis of aseptic nature, apathy and peripheral neuritis;
• problems with the work of the respiratory system: infiltrates inside the lungs, bronchial spasm;
• disorders of the digestive function: vomiting, abdominal pain, loss of appetite and nausea, gastritis, stomatitis, diarrhea and glossitis. In addition, cholestasis, hepatitis, pseudomembranous-type enterocolitis, hepatonecrosis and an increase in the activity of liver transaminases;
• lesions of hematopoietic organs: thrombocyto-, leuko- or neutropenia, megaloblastic type anemia and agranulocytosis;
• symptoms associated with the urinary system: crystalluria, polyuria, hematuria, tubulointerstitial nephritis, increased urea values, hypercreatininemia, renal dysfunction and a toxic form of nephropathy (accompanied by anuria and oliguria);
• problems with the activity of ODA: myalgia or arthralgia;
• signs of allergy: TEN, rashes, MEE (also includes SS), photosensitivity, itching, myocarditis of an allergic nature, exfoliative form of dermatitis, hyperemia affecting the sclera, Quincke's edema and fever.

Overdose

Signs of poisoning: nausea, intestinal colic and vomiting, drowsiness, dizziness, depression, cephalalgia, confusion and fainting; in addition, also crystalluria, hematuria, visual disturbances and fever. With prolonged intoxication, jaundice, leuko-, thrombocytopenia or megaloblastic type anemia develops.

It is required to perform gastric lavage and acidification of urine (increases the excretion of trimethoprim), to take oral liquid and Ca folinate - 5-15 mg per day (eliminates the effect of trimethoprim on the bone marrow). If necessary, hemodialysis is performed.

Interactions with other drugs

The drug increases the anticoagulant effect of indirect anticoagulants, methotrexate and antidiabetic drugs.

Biseptrim weakens the severity of intrahepatic metabolic processes of phenytoin (prolongs its half-life by 39%), as well as warfarin, potentiating their effect.

The drug reduces the reliability of oral contraceptives (suppresses the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal elements).

Pyrimethamine in portions of more than 25 mg per week increases the likelihood of megaloblastic anemia.

Rifampicin reduces the half-life of trimethoprim.

Diuretics (mainly thiazides) increase the likelihood of thrombocytopenia.

The therapeutic effect of the drug is weakened when combined with procaine, benzocaine, procainamide, during the hydrolysis of which PABA is formed.

Cross-allergy may occur between ingested antidiabetic substances (sulfonylurea derivatives) and diuretics (furosemide, thiazides, etc.) on the one hand, and antimicrobial sulfonamides on the other.

PASK and phenytoin barbiturates potentiate B9 deficiency symptoms.

Salicylic acid derivatives potentiate the activity of Biseptrim.

Hexamethylenetetramine and C-vitamin, which acidify urine, increase the likelihood of crystalluria.

Cholestyramine weakens absorption, which is why it is used 4-6 hours before or 1 hour after the administration of co-trimoxazole.

Medicines that suppress bone marrow hematopoietic processes increase the likelihood of myelosuppression.

Storage conditions

Biseptrim must be kept out of the reach of small children. Temperature level - no more than 25 ° С.

Shelf life

Biseptrim can be used for a 36-month term from the moment the medicinal product is sold.

Analogs

Analogues of the drug are Biseptol, Sumetrolim with B-sept, Groseptol, Bactiseptol and Oriprim.