Co-trimoxazole-STI - instructions for use, dose, side effects, contraindications

Combined antimicrobial drug consisting of sulfamethoxazole and trimethoprim. Sulfamethoxazole, similar in structure to paraaminobenzoic acid (PABA), disrupts the synthesis of dihydrofolic acid in bacterial cells, preventing the incorporation of PABA into its molecule. Trimethoprim enhances the action of sulfamethoxazole, disrupting the reduction of dihydrofolic acid into a tetrahydrofolic - active form of folic acid, responsible for protein metabolism and division of the microbial cell.

It is a broad-spectrum bactericidal drug that is active against the following microorganisms: Streptococcus spp. (hemolytic strains are more sensitive to benzylpenicillin), Staphylococcus spp., Streptococcus pneumoniae, Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (including enterotoxogenic strains), Salmonella spp. (including Salmonella typhi and Salmonella paratyphi), Vibrio cholerae, Bacillus anthracis, Haemophilus influenzae (including ampicillin-resistant strains), Listeria spp., Nocardia asteroides, Bordetella pertussis, Enterococcus faecalis, Klebsiella spp., Proteus spp., Pasteurella spp., Francisella tularensis. Brucella spp., Mycobacterium spp. (incl. Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumopnia, Providencia, some species Pseudomonas (Besides Ps.aeruginosa), Serratia marcescens, Shigella (flexneri and sonnei), Yersinia spp., Morganella spp., Pneumocystis carini; Chlamydia spp. (incl. Chlamydia trachomatis, Chlamydia psittaci); protozoa: Plasmodium spp., Toxoplasma gondii, pathogenic fungi, Actinomyces israelii, Coccidioides immitis, Histoplasma capsulatum, Leishmania spp.

Resistant to the drug: Corynebacterium spp., Pseudomonas aeruginosa, Mycobacterium tuberculosis, Treponema spp., Leptospira spp., viruses.

Inhibits the vital activity of E. coli, which leads to a decrease in the synthesis of thymine, riboflavin, nicotinic acid, and other vitamins of group B in the intestine.

Pharmacokinetics: When taken orally, absorption is 90%. Time to reach the maximum concentrations in the blood (Tcmax) - 1-4 hours, the therapeutic level of concentration is maintained for 7 hours after a single dose. Well distributed in the body. Penetrates into breast milk, through the blood-brain barrier and the placenta barrier. In the lungs and urine creates concentrations, exceeding the content in the plasma. To a lesser extent, they accumulate in bronchial secretion, vaginal secretions, secretion and prostate tissue, middle ear fluid, cerebrospinal fluid, bile, bones, saliva, watery eyes, breast milk, interstitial fluid. The connection with plasma proteins is 66% in sulfamethoxazole, in trimethoprim 45%.

Sulfamethoxazole is metabolized to a greater extent with the formation of acetylated derivatives.Metabolites do not have antimicrobial activity.

It is excreted by the kidneys in the form of metabolites (80% within 72 hours) and unchanged (20% sulfamethoxazole, 50% trimethoprim); a small amount - through the intestine. The half-life (T1 / 2) of sulfamethoxazole - 9-11 hours, trimethoprim - 10-12 hours in children - significantly less depending on age: up to the first year - 7-8 hours, 1-10 years - 5-6 hours. In the elderly and patients with impaired renal function, T1 / 2 increases.

Indications: Urinary tract infections: urethritis, cystitis, pyelitis, pyelonephritis, prostatitis, epididymitis, gonorrhea (male and female), mild chancroid, venereal lymphogranuloma, inguinal granuloma; respiratory tract infections bronchitis (acute and chronic), bronchiectasis, lobar pneumonia, bronchopneumonia, pneumocystis pneumonia, empyema, lung abscess; infection of ENT organs: otitis media, sinusitis, laryngitis, tonsillitis; infections of the gastrointestinal tract: typhoid, paratyphoid, salmonellonositelstvo, cholera, dysentery, cholecystitis, cholangitis, gastroenteritis, caused by pathogenic strains of E. coli; infections of the skin and soft tissues: acne, furunculosis, pyoderma,abscess and wound infection; osteomyelitis (acute and chronic), brucellosis (acute), sepsis, peritonitis, meningitis, cerebral abscess, osteoarticular infections, South American blastomycosis, malaria (Plasmodium falciparum), toxoplasmosis and pertussis (as part of complex therapy), scarlet fever.

Contraindications: Hypersensitivity (including sulfonamides), hepatic and / or renal insufficiency (creatinine clearance less than 15 ml / min), aplastic anemia, B 12-deficiency anemia, agranulocytosis, leukopenia, glucose-6-phosphate dehydrogenase deficiency, pregnancy, period lactation, children under 2 years of age, hyperbilirubinemia in children.

Carefully:

With caution apply the drug in young children; with a deficiency of folic acid, bronchial asthma, thyroid diseases. The purpose of the drug requires monitoring the blood picture.

Pregnancy and lactation: The drug should not be used during pregnancy and breastfeeding, as the drug penetrates the placenta and is excreted with the mother's milk.

Dosing and Administration:

The drug is used orally in tablets. The dose is set individually, taking into account the severity of the infection and the sensitivity of the pathogen.

Adults and children over 12 years prescribed Co-trimoxazole-STI tablets 0.48 g: 2 tablets twice a day (after 12 hours). In severe cases - 3 tablets 2 times a day. For chronic infections - 1 tablet 2 times a day.

Children under 12 years of age are assigned Co-trimoxazole-STI 1/2 pills. The average daily dose is determined from the calculation of sulfamethoxazole 0.03 g and trimethoprim 0.006 g per 1 kg of body weight. Children aged 2 to 5 years are usually prescribed 1/2 tablet twice a day (12 hours), at the age of 6 to 12 years, 1 tablet twice a day (after 12 hours).

The course of treatment is from 7 to 14 days. With chronic infections - longer depending on the course of the disease.

Side effects:

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

On the part of the respiratory system: bronchospasm, pulmonary infiltrates.

On the part of the digestive system: nausea, vomiting, anorexia, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of "hepatic" transaminases, hepatitis, hepatonecrosis, pseudomembranous enterocolitis.

On the part of the hematopoiesis: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia.

On the part of the urinary system: polyuria, interstitial nephritis, renal dysfunction, crystalluria, hematuria, increased urea, hypercreatininaemia, toxic nephropathy with oliguria and anuria.

From the musculoskeletal system: arthralgia, myalgia.

Allergic reactions: itching, photosensitivity, rash, polymorphic erythema, exfoliative dermatitis, Stevens-Johnson syndrome, Lyell syndrome, allergic myocarditis, fever, Quincke's edema, reddening of the sclera.

Other: hypoglycemia.

Overdose:

Symptoms: nausea, vomiting, intestinal colic, dizziness, headache, drowsiness, depression, fainting, confusion, visual impairment, fever, hematuria, crystalluria; with prolonged overdose - thrombocytopenia, leukopenia, megaloblastic anemia, jaundice. Treatment: gastric lavage, urine acidification increases the excretion of trimethoprim, intake of fluid inside, / m - 5-15 mg / day of calcium folinate (eliminates the effect of trimethoprim on the bone marrow), if necessary - hemodialysis.

Interaction:

The drug is not recommended to be taken simultaneously with thiazide diuretics because of the risk of developing thrombocytopenia (bleeding).Increases the anticoagulant activity of indirect anticoagulants, the effect of hypoglycemic agents and methotrexate. Co-trimoxazole reduces the intensity of hepatic metabolism of phenytoin (prolongs its T the₂ by 39%) and warfarin, enhancing their effect. Pyrimethamine in doses exceeding 25 mg / week, increases the risk of megaloblastic anemia.

Reduce the effect benzocaine, procaine, procainamide.

Between diuretics (thiazides, furosemide and others) and oral hypoglycemic drugs (sulfanine urea derivatives) on the one hand and antimicrobial sulfonamides - on the other, it is possible to develop a cross-allergic reaction.

Phenytoin, barbiturates, paraaminosalicylic acid (PASK) increase the manifestations of folic acid deficiency. The derivatives of salicylic acid intensify the action. Ascorbic acid, hexamethylenetetramine (and other medicines, acidifying urine) increase the risk of developing crystalluria. Kolestyramine reduces absorption, so it should be taken 1 hour after or 4-6 hours before taking co-trimoxazole. Reduces the reliability of oral contraception (depresses the intestinal microflora and reduces intestinal-hepaticcirculation of hormonal compounds).

Rifampicin reduces the half-life of trimethoprim. Co-administration of co-trimoxazole and cyclosporine after kidney surgery worsens the condition of patients.

Special instructions:

With long courses of treatment, regular blood tests are necessary, since there is a possibility of hematological changes (most often asymptomatic). Care should be taken when prescribing a drug with liver or kidney deficiency (if creatinine clearance is 15-30 ml / min, it is recommended to take 1/2 of the usual dose). Particular caution should be shown in the treatment of elderly patients or patients with a suspected initial lack of folate.

With caution, take patients with allergic reactions in the anamnesis.

The appearance of a skin rash or diarrhea of severe course is an indication for the withdrawal of the drug. For the prevention of crystalluria it is recommended to maintain a sufficient volume of excreted urine. The likelihood of toxic and allergic complications of sulfonamides significantly increases with a decrease in the filtration function of the kidneys.It is also inappropriate to use food products containing paraminobenzoic acid in large amounts - green parts of plants (cauliflower, spinach, legumes), carrots, tomatoes.

Excessive sunlight and ultraviolet radiation should be avoided.

Co-trimoxazole may interfere with the determination of creatinine using alkaline picrinate Jaffe (increases the level of creatinine by about 10%).

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

It is not recommended for use in tonsillitis and pharyngitis caused by beta-hemolytic streptococcus group A because of the widespread resistance of strains.

Form release / dosage:For 10 tablets in a planar cell package or a contiguous, cell-free package. For 20 tablets in a can of polymer or polymer bottles. For 1 and 2 contour packs and jar, or vial with instructions for medical use in a pack of cardboard.

Storage conditions:List B. In a dry, dark place, inaccessible to children, at a temperature of no higher than 25 C.

Shelf life:2 years. Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002559 / 01-2003

Date of registration:29.01.2009

The owner of the registration certificate:AVVA RUS, OJSC AVVA RUS, OJSC Russia

Manufacturer: & nbsp

AVVA RUS, OJSC Russia

Information update date: & nbsp24.06.2010

Illustrated instructions

Instructions

Co-trimoxazole-STI (Co-trimoxazol-STI)