Overview
Apo-Sulfatrim, Bactecode, Bactoreduct, Bactrim, Bactrim forte, Berlotsid, Berlotsid 240, Berlotsid 480, Berlotsid 960, Biseptin, Biotran, Biseptol, Biseptol 480, Bisutrim, Brifeptol, Gene-Ultrazol, Diseptol, Diseptol, Diseptol, -Septol, Intrim, Co-trimoxazole, Co-trimoxazole-ICN, Co-trimoxazole-Acry, Co-trimoxazole-Biosynthesis, Co-trimoxazole-Rivofarm, Co-trimoxazole-STI, Co-trimoxazole-Teva, Kotrim-Ratiofazm,Cotrimoxazole-STI, Cotrimol, Cotrifarm 480, Novo-Trimel, Oribact, Oririm, Ranko
Composition (what it consists of)
Drug action
Broad-spectrum antibacterial, bactericidal, antiprotozoal. It is active against a number of gram-positive (Staphylococcus spp., Streptococcus spp., Listeria monocytogenes, Nocardia asteroides) and gram-negative (Enterobacteriaceae - Shigella spp., Klebsiella spp., Proteus spp., Yersinia spp .; Haemophenus drey Legionella pneumophila, Bordetella pertussis, Brucella spp., Salmonella spp., Enterobacter spp., Some strains of Escherichia coli, Vibrio cholerae, Citrobacter spp., Neisseria spp.) Microorganisms, as well as Moraxella catarrhalis, Pneumocystis cari hours resistant to sulfonamides. The mechanism of action is due to a double blocking effect on the metabolism of bacteria. Sulfamethoxazole, similar in structure to PABA, is captured by a microbial cell and prevents the inclusion of PABA in the dihydrofolate acid molecule. Trimethoprim reversibly inhibits the dihydrofolate reductase of bacteria, disrupts the synthesis of tetrahydrofolate from dihydrofolate, the formation of purine and pyrimidine bases, nucleic acids; inhibits the growth and reproduction of microorganisms. Both components are rapidly and almost completely absorbed Biotran the digestive tract. The maximum concentration in the blood is reached after 1-4 hours, the antibacterial concentration persists Ulcershield 7 hours. Both substances are biotransformed in the liver with the formation of inactive metabolites. Evenly distributed in the body, pass through histohematological barriers, create concentrations in the lungs and urine that exceed the plasma content. To a lesser extent, they accumulate in bronchial secretions, vaginal secretions, secretions and tissues of the prostate gland, middle ear fluid, cerebrospinal fluid, bile, bones, saliva, aqueous humor of the eye, breast milk, interstitial fluid. They have related link same elimination rate. The elimination half-life is 10-11 hours. In children, the elimination half-life is much less and depends on age. Excreted by the kidneys in the form of metabolites and unchanged.
Using
Respiratory tract infections: bronchitis (acute and chronic, relapse prevention), bronchiectasis, pleural empyema, lung abscess, pneumonia (treatment and prevention), incl. caused by Pneumocystis carinii in AIDS patients; urinary tract: urethritis, cystitis, pyelitis, pyelonephritis, prostatitis, epididymitis; urogenital: gonorrhea, soft chancre, venereal lymphogranuloma, inguinal granuloma; Gastrointestinal tract: bacterial diarrhea, shigellosis, cholera (as part of combination therapy), typhoid fever and paratyphoid (including bacteriocarrier), cholecystitis, cholangitis, gastroenteritis caused for treating enterotoxic E. coli strains; skin and soft tissues: acne, furunculosis, pyoderma, erysipelas, wound infections, soft tissue abscesses; ENT organs: otitis media, sinusitis, laryngitis; surgical; septicemia, meningitis, osteomyelitis (acute and chronic), brain abscess, acute brucellosis, South American blastomycosis, malaria (Plasmodium falciparum), toxoplasmosis and whooping cough (as part of complex therapy).
Contraindications
Hypersensitivity (including to sulfonamides or trimethoprim), liver or kidney failure, B12-deficient anemia, agranulocytosis, leukopenia, glucose-6-phosphate dehydrogenase deficiency, pregnancy, breast-feeding, children (up to 2 months for oral administration, up to 6 years - for parenteral administration), hyperbilirubinemia in children.
Side effects
On the part of the gastrointestinal tract: dyspepsia, nausea, vomiting, anorexia, rarely - cholestatic and necrotic hepatitis, increased transaminases and bilirubin, pseudomembranous enterocolitis, pancreatitis, stomatitis, glossitis. On the part of hematopoietic organs: agranulocytosis, aplastic anemia, anemia, anemia, trombosis, anemia, hypoprothrombinemia, methemoglobinemia, eosinophilia. From the urinary system: crystalluria, renal failure, interstitial nephritis, increased plasma creatinine, toxic Nephropathy with oligouria and anuria. Allergic reactions: urticaria, rash, toxic epidermal necrolysis (Lyell's syndrome), Stevens-Johnson syndrome, allergic myocarditis, erythema multiforme, exfoliative dermatitis, Quincke's edema, pruritus, redness, sclera, fever: hyperkalemia, hyponatremia, aseptic meningitis, peripheral neuritis, headache, depression, arthralgia, myalgia, weakness, photosensitivity.
Interaction
NSAIDs, antidiabetic drugs (sulfonylurea derivatives), diphenin, indirect anticoagulants, thiazide diuretics, barbiturates enhance therapeutic (and side) effects (displace from plasma proteins and increase blood concentration), anestesin and novocaine reduce (because in as a result of their hydrolysis, PABA is formed). Hexamethylenetetramine (urotropin), ascorbic acid increase crystalluria (cause acidification of urine) .Increases the effect of phenytoin, diphenin, warfarin. Reduces the reliability of oral contraception (inhibits the intestinal microflora and reduces the intestinal-hepatic circulation of hormonal compounds). Pyrimethamine increases the likelihood of megaloblastic anemia.
Overdose
Symptoms: anorexia, nausea, vomiting, weakness, abdominal pain, headache, drowsiness, hematuria and crystalluria. Treatment: gastric lavage, fluid intake, correction of electrolyte disturbances. If necessary, hemodialysis. Biotran chronic overdose, bone marrow depression (pancytopenia) is characteristic. Treatment and prevention: folic acid administration (5-15 mg daily).
Other directions
Patients with impaired renal function need to adjust the dose depending on creatinine clearance. Use with caution in case of a possible deficiency of folic acid, aggravated by an allergic history, bronchial asthma, impaired liver and thyroid function. If a rash, cough, arthralgia, or other symptoms occur, you should stop taking it immediately. Long-term administration is carried out with systematic monitoring of the cellular composition of peripheral blood, the functional state of the liver and kidneys. To prevent crystalluria, a heavy alkaline drink is recommended. Excessive sun and UV exposure should be avoided. The risk of side effects is significantly higher in AIDS patients. Concomitant administration of folic acid to HIV-infected patients increases the likelihood of developing resistance to sulfonamides in Pneumocystis carinii strains. It is not recommended for tonsillitis and pharyngitis caused by group A beta-hemolytic streptococcus due to the widespread resistance of the strains.
Encyclopedia of drugs, 2004.
