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Active ingredients
Co-trimoxazole [Sulfamethoxazole + Trimethoprim]
Release form
Pills
Composition
Active ingredient: Co-trimoxazole [Sulfamethoxazole + Trimethoprim] (Co-trimoxazolum [Sulfamethoxazolum + Trimethoprimum]) Active ingredient concentration (mg): Sulfamethoxazole 400 mg, trimethoprim 80 mg
Pharmacological effect
Combined antibacterial drug contains sulfamethoxazole and trimethoprim. Sulfamethoxazole, similar in structure to PABA, disrupts the synthesis of dihydrofolic acid in bacterial cells, preventing the incorporation of PABA into its molecule. for protein metabolism and division of microbial cells. It is a bactericidal agent with a broad spectrum of action. It is active against gram olozhitelnyh aerobic bacteria: Streptococcus spp, including Streptococcus pneumoniae (hemolytic strains are more sensitive to penicillin), Staphylococcus spp, Bacillus anthracis, Listeria monocytogenes, 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, Klebs spp., Proteus spp., Pasteurella spp., Francisella tularensis, Brucella spp., Citrobacter spp., Spp. Spp., Citrobacter spp., Sis. except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp., Yersinia spp., Morganella spp., as well as for Chlamydia spp. (including Chlamydia trachomatis, Chlamydia psittaci); against gram-positive anaerobes: Actinomyces israelii; for the simplest: Plasmodium spp., Toxoplasma gondii; pathogenic fungi: Coccidioides immitis, Histoplasma capsulatum, Pneumocystis carinii, Leishmania spp. The drug is resistant to: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira with apt. , riboflavin, nicotinic acid and other B vitamins in the intestine. The duration of therapeutic action is 7 hours.
Pharmacokinetics
AbsorptionAfter taking the drug inside, the active substances are quickly and completely absorbed from the gastrointestinal tract. Cmax in the blood plasma is reached within 1-4 hours after ingestion. Distribution Trimethoprim penetrates well into the body tissues and biological media: lungs, kidneys, prostate, bile, saliva, sputum, cerebrospinal fluid. The binding of trimethoprim to plasma proteins is 50%; sulfamethoxazole - 66%. Excretion of T1 / 2 of trimethoprim - 8.6-17 h, sulfamethoxazole - 9-11 h. The main route of elimination is the kidneys; while trimethoprim is displayed unchanged up to 50%; sulfamethoxazole - 15-30% in active form.
Indications
Treatment of infectious and inflammatory diseases caused by microorganisms that are susceptible to the drug: - respiratory tract infections (including bronchitis, pneumonia, lung abscess, pleural empyema); - otitis, sinusitis; - urinary tract infections (including pyelonephritis, urethritis, salpingitis, prostatitis); - gonorrhea; - gastrointestinal infections (including typhoid fever, paratyphoid fever, bacterial dysentery, cholera, diarrhea); - skin and soft tissue infections (including furunculosis, pyoderma).
Contraindications
- established damage to the liver parenchyma; - pronounced renal dysfunction in the absence of the possibility to control the concentration of the drug in the blood plasma; - severe renal failure (CC less than 15 ml / min); - severe blood diseases (aplastic anemia, B12-deficient 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 under 3 years old ( dosage form) - hypersensitivity to the drug; - hypersensitivity to sulfonamides.
Precautionary measures
Do not exceed the recommended dose. With caution, prescribe a drug with a deficiency of folic acid in the body, bronchial asthma, diseases of the thyroid gland.
Use during pregnancy and lactation
Biseptolum is contraindicated for use during pregnancy and lactation (breastfeeding).
Dosage and administration
Install individually. The drug is taken after a meal, drinking down with a sufficient amount of liquid. For children aged 3 to 5 years, the drug is prescribed 240 mg (2 pills. 120 mg) 2 times / day; children aged 6 to 12 years old - 480 mg each (4 pills of 120 mg or 1 tablet of 480 mg) 2 times / day. In 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 taking 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. For adults and children over 12 years old, the drug is prescribed in 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. With severe disease and / orchronic infections may increase the single dose by 30-50%. In the course of therapy for more than 5 days and / or increasing the dose of the drug, it is necessary to monitor the picture of peripheral blood; when pathological changes occur, folic acid should be prescribed in a dose of 5-10 mg / day. In patients with renal insufficiency with a CC of 15-30 ml / min, the standard dose of Biseptol should be reduced by 50%.
Side effects
From the side of the central nervous system and peripheral nervous system: headache, dizziness; in some cases - aseptic meningitis, depression, apathy, tremor, peripheral neuritis. On the respiratory system: bronchospasm, asphyxiation, cough, pulmonary infiltrates. On the part of the digestive system: nausea, vomiting, loss of 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, agranulocyte oz, megaloblastic anemia, aplastic and hemolytic anemia, eposinia, hypoprothrombinemia, methemoglobinemia.Our urinary system: polyuria, interstitial nephritis, renal failure, crystalluria, hematuria, increased urea concentration, hypercreatinenemia, octopia - muscular system: arthralgia, myalgia. Allergic reactions: itching, photosensitization, urticaria, drug fever, rash, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, allergic myocarditis, fever, angioedema, scleral hyperemia. Metabolism: hypoglycemia, hyperkalemia, hyponatremia.
Overdose
Symptoms: lack of appetite, intestinal colic, nausea, vomiting, dizziness, headache, drowsiness, loss of consciousness, fever, hematuria, crystalluria are also possible. Later, bone marrow depression and jaundice may develop. After acute poisoning with trimethoprim, nausea, vomiting, dizziness, headache, depression,disorder of consciousness, suppression of bone marrow function. It is not known what dose of co-trimoxazole can be life-threatening. Chronic poisoning: the use of co-trimoxazole in high doses for an extended period can lead to a depression of bone marrow function, manifested by thrombocytopenia, leukopenia or megaloblastic anemia . Treatment: removal of the drug and taking measures aimed at its removal from the gastrointestinal tract (gastric lavage no later than 2 hours after taking the drug or cause vomiting), drink plenty of water, if I have diuresis is insufficient, and the kidney function is preserved. Introduce calcium folinate (5-10 mg / day). Acid urine accelerates the excretion of trimethoprim, but may also increase the risk of sulfonamide crystallization in the kidneys. The blood picture, plasma electrolyte composition and other biochemical parameters should be monitored. Hemodialysis is moderately effective, and peritoneal dialysis is not effective.
Interaction with other drugs
With the simultaneous use of Biseptol 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. 2 to 39%) and warfarin, enhancing their effect. Rifampicin reduces T1 / 2 of trimethoprim. With simultaneous use of pyrimethamine in doses exceeding 2 5 mg / week., Increases the risk of megaloblastic anemia. With simultaneous use of diuretics (often thiazides) increase the risk of thrombocytopenia. Benzocaine, procaine, procainamide (like other drugs, as a result of hydrolysis of PABK) reduce the effectiveness of Biseptol. (including with thiazides, furosemide) and oral hypoglycemic agents (sulfonylurea derivatives), on the one hand, and antibacterial agents of the sulfonamide group, on the other hand, may develop The term cross-allergic reaktsii.Fenitoin, barbiturates, PASK increase the expression of folate deficiency while the use of salicylic acid Biseptolom.Proizvodnye reinforcing effect Biseptola.Askorbinovaya acid, hexamethylenetetramine (as well as other drugs,acidifying urine) increase the risk of crystalluria on the background of Biseptol use. Colestiramine reduces absorption while taking with other drugs, so it should be taken 1 h after or 4-6 h before taking co-trimoxazole. When used simultaneously with drugs that depress bone marrow hematopoiesis, increases the risk of myelosuppression. In some cases, Biseptol may increase the concentration of digoxin in the blood plasma in elderly patients. Biseptol may reduce the effect tricyclic antidepressants. Patients after kidney transplantation, with simultaneous use of co-trimoxazole and cyclosporine, show a dysfunction of transplanted kidney, manifested by increased serum creatinine concentrations, which is probably caused by trimethoprim. -hepatic circulation of hormonal drugs).
special instructions
A drug is prescribed with caution when allergic history is aggravated. For long (more than a month) courses of treatment, regular blood tests are necessary, since there is a likelihood of hematological changes (usually asymptomatic). These changes may be reversible with the appointment of folic acid (3-6 mg / day), which does not significantly violate the antimicrobial activity of the drug. Special care is needed in the treatment of elderly patients or patients with suspected initial folate deficiency. Appointment of folic acid is also advisable with long-term drug treatment in high doses. To prevent crystalluria, it is recommended to maintain a sufficient amount of urine. The likelihood of toxic and allergic complications of sulfonamides increases significantly with a decrease in the filtration function of the kidneys. It is also inappropriate to eat foods containing large amounts of PABA — green plant parts (cauliflower, spinach, legumes), carrots, and tomatoes during treatment. Avoid excessive sun and UV exposure. The risk of side effects is significantly higher in AIDS patients. It is not recommended to use the drug for tonsillitis and pharyngitis,caused by β-hemolytic streptococcus group A, due to the widespread resistance of strains. Trimethoprim can change the results of serum methotrexate determination carried out by the enzymatic method, but does not affect the result when choosing the radioimmunological method. Co-trimoxazole can increase by 10% Jaffe with picric acid for the quantitative determination of creatinine.
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