Biseptol tablets: instructions for using the medicine, structure, Contraindications

Active material: Co-trimoxazole [Sulfamethoxazole + Trimethoprim]
When ATH: J01EE01
CCF: Antibacterial drug sulfanilamide
ICD-10 codes (testimony): A00, A01, A02, A03, A04.0, A09, A23, A38, A54, A55, A57, B40, B50, B51, B52, B58, B59, H66, J01, J02, J03, J04, J15, J20, J31, J32, J35.0, J37, J42, J47, J85, J86, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, L70, M86, N10, N11, N30, N34, N41, N45, N70, T79.3
When CSF: 06.16.01
Manufacturer: Pharmaceutical Works Polfa in Pabianice Joint-Stock Company (Poland)

Biseptol tablets: dosage form, composition and packaging

Pills white with a yellowish tint, round, flat, bevelled and engraved “Bs”.

Excipients: potato starch, talc, magnesium stearate, polyvinyl alcohol, metilparagidroksiʙenzoat, propilparagidroksibenzoat, propylene glycol.

20 PC. – blisters (1) – packs cardboard.

Pills white with a yellowish tint, round, flat, chamfered, Valium and engraving “Bs”.

Excipients: potato starch, talc, magnesium stearate, polyvinyl alcohol, metilparagidroksiʙenzoat, propilparagidroksibenzoat, propylene glycol.

20 PC. – blisters (1) – packs cardboard.

Biseptol tablets: pharmachologic effect

Combined antibacterial drug, contains sulfamethoxazole and trimethoprim.

Sulfamethoxazole, similar in structure to the PABA, It gives dihydrofolic acid synthesis in bacterial cells, preventing the inclusion of PABA in its molecule.

Trimethoprim-sulfamethoxazole enhances the action, violating recovery digidrofolievoy tetrahydrofolic acid – the active form of folic acid, responsible for protein metabolism and microbial cell division.

It is a bactericidal broad-spectrum drugs.

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 monocytogenes, Nocardia asteroids, Enterococcus faecalis, Mycobacterium spp. (including Mycobacterium leprae, excluding Mycobacterium tuberculosis); Gram-negative aerobic bacteria: Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (including strains enterotoksogennye), Salmonella spp. (including Salmonella typhi and Salmonella paratyphi); Vibrio cholerae, Haemophilus influenzae (including ampicillin resistance strains), Bordetella pertussis, Klebsiella spp., Proteus spp., Pasteurella spp., Francisella tularensis, Brucella spp., Citrobacter spp., Enterobacter spp., Legionella pneumopbila, Providence, some species Pseudomonas (other than Pseudomonas aeruginosa), Serratia wilting, Shigella spp., Yersinia spp., Morganella spp., and in regard to Chlamydia spp. (in t. no. Chlamydia trachomatis, Chlamydia psittaci); against gram-positive anaerobes: Actinomyces israelii; against protozoa: Plasmodium spp., Toxoplasma gondii; pathogenic fungi: Merciless coccidioides, Histoplasma capsulatum, Pneumocystis carinii, Leishmania spp.

C drug resistant: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira spp., viruses.

Inhibits E. coli livelihoods, which leads to reduced synthesis of thiamin, riʙoflavina, niacin and other B vitamins in the intestine.

The duration of the therapeutic effect of 7 no.

Biseptol tablets: pharmacokinetics

Absorption

After oral administration the active substance is rapidly and completely absorbed from the gastrointestinal tract.

C_max plasma levels reached within 1-4 hours after ingestion.

Distribution

Trimethoprim is well into the tissue and biological environment of the body: lungs, kidneys, prostate, bile, spittle, sputum, cerebrospinal fluid. Trimethoprim binding to plasma proteins is 50%; sulfamethoxazole – 66%.

Deduction

T_1/2 Trimethoprim – 8.6-17 no, sulfamethoxazole – 9-11 no. The main route of excretion – kidneys; while TMP output unchanged to 50%; sulfamethoxazole – 15-30%.

Biseptol tablets: testimony

Treatment of infectious and inflammatory diseases, caused by sensitive microorganisms:

• respiratory tract infections (incl. bronchitis, pneumonia, lung abscess, empyema);
• otitis, sinusitis;
• infections of the genitourinary system (incl. pyelonephritis, uretrit, salpingitis, prostatitis);
• gonorrhea;
• GI infections (incl. typhoid fever, paratif, bakterialynaya dysentery, cholera, diarrhea);
• infections of skin and soft tissue (incl. furunculosis, pyoderma).

Biseptol tablets: dosing regimen

Establish individually. The drug is taken after a meal, drinking plenty of fluids.

Children aged 3 to 5 years the drug is prescribed for 240 mg (2 tab. by 120 mg) 2 times / day; children aged 6 to 12 years – by 480 mg (4 tab. by 120 mg or 1 tab. by 480 mg) 2 times / day.

At pneumonia the drug is prescribed on the basis of 100 mg sulfamethoxazole on 1 kg body weight / day. The interval between doses – 6 no, duration of administration – 14 days.

At gonorrhea dose is 2 g (based on sulfamethoxazole) 2 times / day with an interval between doses 12 no.

Adults and children over 12 years the drug is prescribed for 960 mg 2 times / day, long-term therapy – by 480 mg 2 times / day.

The duration of treatment – from 5 to 14 days. At severe disease and / or chronic infections a single dose may be increased to 30-50%.

When the duration of a course of therapy 5 days and / or increasing the dose necessary to control the picture of peripheral blood; the appearance of pathological changes should be appointed at a dose of folic acid 5-10 mg / day.

In Patients with renal insufficiency with CC 15-30 ml / min standard dose Biseptol^® must be reduced by 50%.

Biseptol tablets: side effects

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

The respiratory system: bronchospasm, suffocation, cough, pulmonary infiltrates.

From the digestive system: nausea, vomiting, decreased appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increase in liver transaminases, hepatitis, sometimes with cholestatic jaundice, gepatonekroz, pseudomembranous enterocolitis, pancreatitis.

From the hematopoietic system: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastnaya anemia, aplastic and hemolytic anemia, eozinofilija, gipoprotrombinemii, metgemoglobinemiâ.

From the urinary system: polyuria, interstitial nephritis, impairment of renal function, kristallurija, hematuria, increasing concentrations of urea, giperkreatininemiя, toksicheskaya nephropathy oliguriey and anuriey.

On the part of the musculoskeletal system: arthralgia, myalgia.

Allergic reactions: itch, photosensitivity, hives, drug fever, rash, erythema multiforme exudative (incl. Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, allergic myocarditis, fever, angioedema, redness of the sclera.

Metabolism: gipoglikemiâ, hyperkalemia, giponatriemiya.

Preparation, usually, well tolerated.

Biseptol tablets: 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 (aplasticheskaya anemia, IN₁₂-defitsitnaya anemia, agranulocytosis, leukopenia, megaloblastnaya anemia, anemia, associated with folic acid deficiency);
• hyperbilirubinemia in children;
• deficiency of glucose-6-fosfatdegidrogenazы (the risk of hemolysis);
• pregnancy;
• lactation;
• Children up to age 3 years (for a given dosage form);
• hypersensitivity to the drug;
• hypersensitivity to sulfonamides.

FROM caution prescribers deficiency of folic acid in the body, asthma, Thyroid diseases.

Biseptol tablets: Pregnancy and lactation

Bïseptol^® contraindicated during pregnancy and lactation (breast-feeding).

Biseptol tablets: Special instructions

With care prescribe a drug for allergic history.

At long (more than a month) courses of treatment requires regular blood tests, because there is the risk of hematological changes (often asymptomatic). These changes may be reversible when assigning folic acid (3-6 mg / day), that does not significantly impair the antimicrobial activity of the drug. Particular care is required when treating elderly patients or patients with suspected initial lack of folate. Purpose of folic acid is also advisable when chronic treatment drug at high doses.

To prevent crystalluria is recommended to maintain a sufficient volume of urine. Chance of toxic and allergic complications of sulfonamides substantially increases with a decrease in kidney filtration function.

It is inappropriate and against the background of the treatment consumed foods, containing large amounts of PABA, – green parts of plants (cauliflower, spinach, pulse), carrot, tomatoes.

Avoid excessive sun and UV radiation.

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

Do not use the drug if tonsillitis and pharyngitis, caused by β-hemolytic streptococcus group A, because of widespread resistance strains.

Trimethoprim can change the results of the determination of serum levels of methotrexate, conducted by an enzymatic method, but does not affect the results when radioimmunoassay.

Co-trimoxazole may increase on 10% Results Jaffe reaction with picric acid for the quantitative determination of creatinine.

Biseptol tablets: overdose

Symptoms: anorexia, kišečnaâ how, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness, It may also have a fever, hematuria, kristallurija. Later may develop bone marrow suppression, and jaundice.

After acute poisoning trimethoprim nausea, vomiting, dizziness, headache, depression, disturbance of consciousness, suppression of bone marrow function.

Unknown, what dose of co-trimoxazole can be life-threatening.

Chronic poisoning: co-trimoxazole at high doses for prolonged periods can lead to suppression of bone marrow function, manifested by thrombocytopenia, leucopenia or anemia megaloblastic.

Treatment: removal of the drug and taking action, aimed at removing it from the blood (to gastric lavage within 2 h after ingestion or vomit), excessive drinking, If urine output is insufficient, and preserved renal function. Enter calcium folinate (5-10 mg / day). The acidic environment accelerates the excretion of urine trimethoprim, but it may also increase the risk of kidney crystallization sulfonamide.

It should monitor the blood picture, Electrolyte composition in plasma and other biochemical parameters. Hemodialysis is moderately effective, and peritoneal dialysis are not effective.

Biseptol tablets: drug interaction

In an application Biseptol^® with thiazide diuretics are at risk of thrombocytopenia and bleeding (the combination is not recommended).

Co-trimoxazole increases the anticoagulant activity of indirect anticoagulants, and the action of hypoglycemic drugs and methotrexate.

Co-trimoxazole reduces the intensity of the hepatic metabolism of phenytoin (increases egoT_1/2 on 39%) and warfarin, reinforcing their effects.

Rifampicin reduces T_1/2 Trimethoprim.

With simultaneous use of pyrimethamine at doses, exceeding 25 mg / Sun., It increases the risk of megaloblastic anemia.

With simultaneous use of diuretics (often thiazides) increase the risk of thrombocytopenia.

Benzokain, prokayn, prokaynamyd (Like other drugs, by hydrolysis which is formed PABA) reduce the effectiveness of Biseptol^®.

Between diuretics (incl. with thiazide, furosemidom) and oral hypoglycemic agents (sulfonylureas) one side, and antibacterials group sulfonamides – on the other hand, possible development of cross-allergic reaction.

Phenytoin, barbiturates, PAS increase the expression of folate deficiency while the use of Biseptol^®.

Salicylic acid derivatives enhance the effect Biseptol^®.

Vitamin C, geksametilentetramin (Like other drugs, acidifying the urine) increase the risk of crystalluria against application Biseptol^®.

Cholestyramine reduces absorption when taken with other drugs, it should be taken over 1 h after or 4-6 hours prior to receiving co-trimoxazole.

In an application with drugs, suppress bone marrow hemopoiesis, increases the risk of myelosuppression.

In some cases Biseptolum^® can increase the concentration of digoxin in the blood plasma of elderly patients.

Bïseptol^® It may decrease the effectiveness of tricyclic antidepressants.

In patients following kidney transplantation, while the use of co-trimoxazole and cyclosporin, celebrated passing the transplanted kidney dysfunction, manifested by increased serum creatinine, which is probably caused by the action of trimethoprim.

Reduces the effectiveness of oral contraceptives (It inhibits the intestinal microflora and reduce enterohepatic circulation of hormonal agents).

Biseptol tablets: terms of dispensing from pharmacies

The drug is released under the prescription.

Biseptol tablets: terms and conditions of storage

The drug should be stored out of reach of children at or above 25 ° C. Shelf life – 5 years.