Sulfamethoxazole (sulfamethoxazole)
- trimethoprim (trimethoprim)

Composition and form of release of the drug

20 pcs. - cans (1) - packs of cardboard.
10 pieces. - cellular contour packings (3) - packs of cardboard.
10 pieces. - non-cell packing contour (100) - cardboard boxes.

pharmachologic effect

The combined means of a wide spectrum of activity.

Sulfamethoxazole has a bacteriostatic effect, which is associated with inhibition of the process of PABA utilization and disruption of the synthesis of dihydrofolic acid in bacterial cells.

Trimethoprim inhibits an enzyme that is involved in metabolism by converting dihydrofolate to tetrahydrofolate. Thus, 2 consecutive stages of the biosynthesis of purines and, consequently, nucleic acids, which are necessary for the growth and reproduction of bacteria, are blocked. High concentrations are created in the tissues of the lungs, kidneys, prostate gland, cerebrospinal fluid, bile, bones.

Combination sulfamethoxazole + trimethoprim is active against gram-positive bacteria: Staphylococcus spp. (including strains producing penicillinase), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae; Gram-negative bacteria: Neisseria gonorrhoeae, Escherichia coli, Shigella spp., Salmonella spp., Proteus spp., Enterobacter spp., Klebsiella spp., Yersinia spp., Vibrio cholerae, Haemophilus influenzae; anaerobic non-spore-forming bacteria- Bacteroides spp. Also is also active in relation to Chlamydia spp.

For this combination resistant Pseudomonas aeruginosa, Treponema spp., Mycoplasma spp., Mycobacterium tuberculosis, as well as viruses and fungi.

Pharmacokinetics

When taken orally, absorption is 90%. T Cmax - 1-4 hours, the therapeutic level of concentration is maintained for 7 hours after a single dose. Well distributed in the body. Penetrates through the BBB, the placental barrier and into breast milk. In the lungs and urine creates concentrations exceeding the content in. To a lesser extent, it accumulates in bronchial secretions, vaginal secretions, secretions and prostate tissue, middle ear fluid (with inflammation), cerebrospinal fluid, bile, bones, saliva, aqueous humor of the eye, breast milk, interstitial fluid. Communication with plasma proteins - 66% for sulfamethoxazole, for trimethoprim - 45%.

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

Excreted by the kidneys as metabolites (80% within 72 hours) and unchanged (20% sulfamethoxazole, 50% trimethoprim); a small amount - through the intestines. T 1/2 sulfamethoxazole - 9-11 hours, trimethoprim - 10-12 hours, in children - significantly less and depends on age: up to 1 year - 7-8 hours, 1-10 years - 5-6 hours. In the elderly and patients with impaired renal function T 1/2 increases.

Indications

Infectious and inflammatory diseases caused by susceptible microorganisms, including: urinary tract infections (urethritis, cystitis, pyelitis, pyelonephritis), genital infections (prostatitis, epididymitis, gonorrhea, chancroid, lymphogranuloma venereum, inguinal granuloma); respiratory tract infections (acute and chronic bronchitis, bronchiectasis, lobar pneumonia, bronchopneumonia, pneumocystis pneumonia); infections of ENT organs (otitis media, sinusitis, laryngitis, tonsillitis); scarlet fever; gastrointestinal infections (typhoid fever, paratyphoid, salmonellosis, cholera, dysentery, cholecystitis, cholangitis, gastroenteritis caused by enterotoxic strains of Escherichia coli); skin and soft tissue infections (acne, furunculosis, pyoderma, wound infections); osteomyelitis (acute and chronic) and other osteoarticular infections; brucellosis (acute), South American blastomycosis, malaria (Plasmodium falciparum), toxoplasmosis (as part of complex therapy).

Contraindications

Damage to the liver parenchyma; severe renal dysfunction in the absence of the ability to control the concentration of sulfamethoxazole and trimethoprim in the blood plasma; severe renal insufficiency (KK<15 мл/мин); тяжелые заболевания крови (апластическая анемия, В 12 -дефицитная анемия, агранулоцитоз, лейкопения, мегалобластная анемия, анемия, связанная с дефицитом фолиевой кислоты); гипербилирубинемия у детей; дефицит глюкозо-6-фосфатдегидрогеназы; беременность; период лактации (грудного вскармливания); детский возраст до 2 месяцев или до 6 недель (рожденных от матерей с ВИЧ-инфекцией) - для суспензии и в/в инфузии; детский возраст до 2 лет - для таблеток; одновременное применение с дофетилидом; повышенная чувствительность к сульфаниламидам и триметоприму.

Carefully

Folic acid deficiency in the body, bronchial asthma, thyroid disease.

Dosage

Installed individually. Doses are given based on sulfamethoxazole. Inside for adults and children over 12 years of age, the average dose is 0.4-2 g every 12 hours (2 times / day), the course of treatment is 5-14 days. Inside for children aged 2-5 months - 100 mg 2 times / day; from 6 months to 5 years - 200 mg 2 times / day; from 6 to 12 years - 400 mg 2 times / day.

If necessary, apply in / in the drip of 0.8-1.6 g every 12 hours (2 times / day) for 5 days. For children over the age of 6 weeks, the dose is set individually, depending on body weight and the clinical situation.

After parenteral therapy, if necessary, they switch to oral administration.

Maximum daily dose for adults when taken orally is 3.6 g.

Side effects

From the digestive system: nausea, vomiting, diarrhea, glossitis, pseudomembranous colitis, cholestatic hepatitis.

Allergic reactions: skin rash, angioedema, Stevens-Johnson syndrome, Lyell's syndrome.

From the hematopoietic system: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia.

From the urinary system: crystalluria, hematuria, interstitial nephritis.

Local reactions: phlebitis (with a / in the introduction).

Others: purpura, thyroid dysfunction.

drug interaction

With the simultaneous use of this combination, the effect of indirect action is significantly enhanced due to the slowdown in the inactivation of the latter, as well as their release from the association with plasma proteins.

With simultaneous use with some sulfonylurea derivatives, an increase in the hypoglycemic effect is possible.

The simultaneous use of this combination can lead to an increase in the toxicity of the latter (in particular, to the appearance of pancytopenia) due to its release from its association with plasma proteins.

Under the influence of indomethacin, naproxen, salicylates and some other NSAIDs, it is possible to enhance the action of this combination with the development of undesirable effects, since the active substances are released from the connection with blood proteins and their concentration increases.

The simultaneous use of diuretics and this combination increases the likelihood of developing thrombocytopenia caused by the latter, especially in elderly patients.

In the case of simultaneous administration of chloridine with this combination, the antimicrobial effect is enhanced, since chloridine inhibits the formation of tetrahydrofolic acid, which is necessary for the synthesis of nucleic acids and proteins. In turn, sulfonamides inhibit the formation of dihydrofolic acid, which is a precursor of tetrahydrofolic acid. This combination is widely used in the treatment of toxoplasmosis.

The absorption of sulfamethoxazole and trimethoprim when taken together with cholestyramine is reduced as a result of the formation of insoluble complexes, which leads to a decrease in their concentration in the blood.

Reduces the intensity of hepatic metabolism of phenytoin (extends its T 1/2 by 39%), enhancing its effect and toxic effects.

With the simultaneous use of this combination with pyrimethamine in doses exceeding 25 mg / week, the risk of developing megaloblastic anemia increases.

May increase serum concentrations of digoxin, especially in elderly patients, monitoring of serum digoxin concentrations is necessary.

The effectiveness of tricyclic antidepressants when taken with this combination may be reduced.

In patients receiving this combination and after kidney transplantation, there may be a reversible deterioration in kidney function, manifested by an increase in creatinine levels.

With simultaneous use with ACE inhibitors, especially in elderly patients, hyperkalemia may develop.

Trimethoprim, by inhibiting the transport system of the kidneys, increases dofetilide AUC by 103% and dofetilide Cmax by 93%. With increasing concentrations, dofetilide can cause ventricular arrhythmias with prolongation of the QT interval, including torsades de pointes. Simultaneous use is contraindicated.

special instructions

Children should be prescribed only those preparations of sulfamethoxazole in combination with trimethoprim, which are intended for use in pediatrics.

It is desirable to determine the concentration of sulfamethoxazole in plasma every 2-3 days immediately before the next infusion. If the concentration of sulfamethoxazole exceeds 150 µg/ml, treatment should be interrupted until it drops below 120 µg/ml.

With long-term (over a month) courses of treatment, regular blood tests are necessary, since there is a possibility of hematological changes (most often asymptomatic). These changes can be reversible with the appointment of folic acid (3-6 mg / day), which does not significantly impair the antimicrobial activity of the drug. Particular caution should be exercised in the treatment of elderly patients or patients with suspected initial folate deficiency. The appointment of folic acid is also advisable for long-term treatment in high doses.

It is also inappropriate to use food products containing large amounts of PABA during treatment - green parts of plants (cauliflower, spinach, legumes), carrots, tomatoes.

Excessive sun and UV exposure should be avoided.

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

Pregnancy and lactation

Use during pregnancy and lactation (breastfeeding) is contraindicated.

Application in childhood

For children, the drug is prescribed according to the indications and according to the recommended dosing regimen. V / m administration is contraindicated under the age of 6 years, ingestion is contraindicated in children under 3 months.

For impaired renal function

At kidney failure the dose depends on the size of the CC: with QC over 25 ml / min- standard dose; at 15-25 ml/min- the standard dose for 3 days, then half the standard dose. At CC less than 15 ml/m in appoint half of the standard dose only on the background of hemodialysis.

For impaired liver function

Contraindicated in liver failure.

Use in the elderly

In the elderly and patients with impaired renal function T 1/2 increases.

Clinical and pharmacological group

06.035 (Antibacterial sulfa drug)

pharmachologic effect

Combined antimicrobial drug consisting of sulfamethoxazole and trimethoprim. Sulfamethoxazole, similar in structure to para-aminobenzoic 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 to tetrahydrofolic acid, the active form of folic acid, which is responsible for protein metabolism and microbial cell division.

It is a broad-spectrum bactericidal preparation, active against the following microorganisms: Streptococcus spp. (hemolytic strains are more sensitive to penicillin), 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. (including Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumophila, Providencia, some species of Pseudomonas (except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp., Yersinia spp., Morganella spp., Pneumocystis carinii; Chlamydia spp. (including 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.

It inhibits the vital activity of Escherichia coli, which leads to a decrease in the synthesis of thymine, riboflavin, nicotinic acid and other B vitamins in the intestine.

Pharmacokinetics

When taken orally, absorption is 90%. T Cmax - 1-4 hours, the therapeutic level of concentration is maintained for 7 hours after a single dose. Well distributed in the body. Penetrates through the BBB, the placental barrier and into breast milk. In the lungs and urine creates concentrations exceeding those in plasma. To a lesser extent, it accumulates in bronchial secretions, vaginal secretions, secretions and prostate tissue, middle ear fluid (with inflammation), cerebrospinal fluid, bile, bones, saliva, aqueous humor of the eye, breast milk, interstitial fluid. Communication with plasma proteins - 66% for sulfamethoxazole, for trimethoprim - 45%.

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

Dosage

Inside, in / in, in / m. In each dosage form, the quantitative ratio of trimethoprim and sulfamethoxazole is 1:5.

Inside ( pills), - 960 mg once, or 480 mg 2 times a day. With severe the course of infections- 480 mg 3 times a day, with chronic infections maintenance dose - 480 mg 2 times a day. Children 1-2 years old- 120 mg 2 times a day, 2-6 years old- 120-240 mg 2 times a day, 6-12 years old- 240-480 mg 2 times a day.

Suspension: children 3-6 months - 120 mg 2 times a day, 7 months-3 years - 120-240 mg 2 times a day, 4-6 years - 240-480 mg 2 times a day, 7-12 years - 480 mg 2 times a day, adults and children over 12 years old - 960 mg 2 times a day. Syrup for children: children 1-2 years old - 120 mg 2 times a day, 2-6 years old - 180-240 mg 2 times a day, 6-12 years old - 240-480 mg 2 times a day.

The minimum duration of treatment is 4 days; after the disappearance of symptoms, therapy is continued for 2 days. For chronic infections, the course of treatment is longer. At acute brucellosis- 3-4 weeks, with typhoid and paratyphoid- 1-3 months

For prevention of recurrence of chronic urinary tract infections adults and children over 12 years old- 480 mg 1 time per day at night, children under 12 years old- 12 mg / kg / day. Duration of treatment - 3-12 months. The course of treatment of acute cystitis in children aged 7-16 years - 480 mg 2 times a day for 3 days.

At gonorrhea- 1920-2880 mg / day for 3 doses.

At gonorrheal pharyngitis(with increased sensitivity to penicillin) - 4320 mg 1 time per day for 5 days. At pneumonia caused by Pneumocystis carinii, - 120 mg / kg / day with an interval of 6 hours for 14 days.

Parenterally: i/m adults and children over 12 years old - 480 mg every 12 hours, children 6-12 years old - 240 mg every 12 hours.

In/in drip, adults and children over 12 years old - 960-1920 mg every 12 hours, children 6-12 years old - 480 mg 2 times a day; 6 months-5 years - 240 mg 2 times a day; 6 weeks-5 months - 120 mg 2 times a day.

For maximum efficacy, a constant plasma or serum concentration of trimethoprim should be maintained at or above 5 µg/mL.

Malaria due to Plasmodium falciparum, - IV infusion (1920 mg 2 times a day) for 2 days. Children will need a correspondingly reduced dose.

To achieve higher concentrations in the CSF, it is administered intravenously (dissolved in 200 ml of solvent) for 1 hour 2 times a day.

Dissolve in the following proportions immediately before administration: 480 mg (5 ml solution for infusion) per 125 ml, 960 mg (10 ml) per 250 ml, 1440 mg (15 ml) per 500 ml infusion solution.

If turbidity or crystallization of the solution appears before or during the infusion, the mixture should not be used. The duration of administration is 1-1.5 hours (should be consistent with the patient's fluid needs).

If necessary, restrictions on the volume of fluid administered are administered at higher concentrations - 5 ml is dissolved in 50-75 ml of a 5% dextrose solution in water. In severe infections in all age groups, the dose may be increased by 50%.

Overdose

Symptoms: nausea, vomiting, intestinal colic, dizziness, headache, drowsiness, depression, fainting, confusion, blurred vision, fever, hematuria, crystalluria; with prolonged overdose - thrombocytopenia, leukopenia, megaloblastic anemia, jaundice.

Treatment: gastric lavage, acidification of urine increases the excretion of trimethoprim, oral fluid intake, i / m - 5-15 mg / day of calcium folinate (eliminates the effect of trimethoprim on the bone marrow), if necessary - hemodialysis.

drug interaction

Pharmaceutically compatible with the following drugs: dextrose for IV infusion 5 and 10%, levulose for IV infusion 5%, sodium chloride for IV infusion 0.9%, a mixture of 0.18% sodium chloride and 4% dextrose for IV infusion, 6% dextran 70 for IV infusion in 5% dextrose or 0.9% sodium chloride solution, 10% dextran 40 for IV infusion in 5% dextrose or 0.9% sodium chloride solution, Ringer's solution for injection.

Increases the anticoagulant activity of indirect anticoagulants, as well as the effect of hypoglycemic drugs and methotrexate.

Reduces the intensity of hepatic metabolism of phenytoin (extends its T 1/2 by 39%) and warfarin, enhancing their effect.

Reduces the reliability of oral contraception (inhibits the intestinal microflora and reduces the enterohepatic circulation of hormonal compounds).

Rifampicin shortens the half-life of trimethoprim.

Pyrimethamine at doses greater than 25 mg/week increases the risk of megaloblastic anemia.

Diuretics (more often thiazides) increase the risk of thrombocytopenia.

Reduce the effect of benzocaine, procaine, procainamide (and other drugs, the hydrolysis of which produces PABA).

Between diuretics (thiazides, furosemide, etc.) and oral hypoglycemic drugs (sulfonylurea derivatives), on the one hand, and antimicrobial sulfonamides, on the other, a cross-allergic reaction may develop.

Phenytoin, barbiturates, PAS increase the manifestations of folic acid deficiency.

Derivatives of salicylic acid enhance the action.

Kolestiramin reduces absorption, so it should be taken 1 hour after or 4-6 hours before taking co-trimoxazole.

Drugs that inhibit bone marrow hematopoiesis increase the risk of myelosuppression.

Pregnancy and lactation

Contraindicated in pregnancy and lactation.

Side effects

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

From the respiratory system: bronchospasm, pulmonary infiltrates.

From the digestive system: nausea, vomiting, loss of appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of "liver" transaminases, hepatitis, hepatonecrosis, pseudomembranous enterocolitis.

From the side of the hematopoietic organs: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia.

From the urinary system: polyuria, interstitial nephritis, impaired renal function, crystalluria, hematuria, increased urea concentration, hypercreatininemia, toxic nephropathy with oliguria and anuria.

From the musculoskeletal system: arthralgia, myalgia.

Allergic reactions: itching, photosensitivity, rash, erythema multiforme exudative (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, allergic myocarditis, fever, angioedema, scleral hyperemia.

Local reactions: thrombophlebitis (at the site of venipuncture), pain at the injection site.

Others: hypoglycemia.

Indications

- infections of the genitourinary organs: urethritis, cystitis, pyelitis, pyelonephritis, prostatitis, epididymitis, gonorrhea (male and female), soft chancre, venereal lymphogranuloma, inguinal granuloma;

- respiratory tract infections: bronchitis (acute and chronic), bronchiectasis, lobar pneumonia, bronchopneumonia, pneumocystis pneumonia;

- infections of ENT organs: otitis media, sinusitis, laryngitis, tonsillitis; scarlet fever;

- gastrointestinal infections: typhoid fever, paratyphoid, salmonella carriers, cholera, dysentery, cholecystitis, cholangitis, gastroenteritis caused by enterotoxic strains of Escherichia coli;

- infections of the skin and soft tissues: acne, furunculosis, pyoderma, wound infections;

- osteomyelitis (acute and chronic) and other osteoarticular infections, brucellosis (acute), South American blastomycosis, malaria (Plasmodium falciparum), toxoplasmosis (as part of complex therapy).

Contraindications

- hypersensitivity (including to sulfonamides);

- liver failure;

- renal failure (CC less than 15 ml / min);

- aplastic anemia;

- B 12 -deficiency anemia;

- agranulocytosis, leukopenia;

- deficiency of glucose-6-phosphate dehydrogenase;

- pregnancy;

- lactation period;

- age up to 6 years (for i / m administration);

- children's age (up to 3 months - for oral administration);

- hyperbilirubinemia in children.

WITH caution: folic acid deficiency, bronchial asthma, thyroid disease.

special instructions

It is also inappropriate to use food products containing large amounts of PABA during treatment - green parts of plants (cauliflower, spinach, legumes), carrots, tomatoes.

Excessive sun and UV exposure should be avoided.

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

It is not recommended for use in tonsillitis and pharyngitis caused by group A beta-hemolytic streptococcus, due to the widespread resistance of strains .. tab. 480 mg: 20, 30, 40, 50 or 100 pcs. P No. 013806/02-2002 (2018-03-02 - 2018-03-07)
. tab. 480 mg: 20 pcs. P No. 014257/02-2002 (2015-10-02 - 2015-10-07)
. tab. 480 mg: 20, 30 or 1000 pcs. R No. 000908/01 (2013-04-09 - 2013-04-14)
. tab. 480 mg: 1000 pcs. P No. 014522/01-2002 (2019-11-02 - 2019-11-07)
. susp. for oral administration 480 mg/5 ml: vial. 60 ml or 120 ml P No. 013806/01-2002 (2018-03-02 - 2018-03-07)
. tab. 480 mg: 20 or 50 pcs. P No. 014141/01-2002 (2018-06-02 - 2018-06-07)
. susp. for oral administration for children 240 mg: vial. 100 ml P No. 014257/01-2002 (2015-10-02 - 2015-10-07)
. tab. 480 mg: 20 pcs. R No. 002616/01-2003 (2030-06-03 - 2030-06-08)
. tab. 480 mg: 20 pcs. P No. 014658/01-2002 (2020-12-02 - 2020-12-07)
. tab. 120 mg: 20 pcs. P N013420/01 (2012-12-07 - 0000-00-00)
. tab. 480 mg: 10, 20, 30 or 40 pcs. R No. 003300/01 (2023-12-05 - 2023-12-10)
. concentrate for preparation. r-ra d / inf. 96 mg/1 ml: amp. 5 ml 10 pcs. P N015943/01 (2005-02-10 - 2005-02-15)
. rr d / inf. concentrated 480 mg/5 ml: amp. 10 pieces. R N001575/01-2002 (2026-07-02 - 2026-07-07)
. susp. oral 240 mg/5 ml: vial. 80 ml P N014891/01-2003 (2024-06-08 - 0000-00-00)
. susp. for oral administration 240 mg/5 ml: vial. 100 ml in set. with measuring spoon Р №001227/02-2002 (2020-08-02 - 2020-08-07)
. tab. 480 mg: 20 pcs. R No. 000908/01-2001 (2017-11-08 - 2017-11-13)
. tab. 120 mg: 20 pcs. R N000681/02-2003 (2016-03-09 - 0000-00-00)
. tab. 120 mg: 2, 4, 6, 12, 14 or 20 pcs. P N014348/01 (2029-12-06 - 2029-12-11)
. tab. 480 mg: 20 pcs. R N000743/01 (2017-10-07 - 0000-00-00)
. tab. 120 mg: 20, 30 or 1000 pcs. R No. 000908/01 (2013-04-09 - 2013-04-14)
. susp. for oral administration for children 240 mg/5 ml: vial. 50 ml or 100 ml P No. 014378/01-2002 (2017-09-02 - 2017-09-07)
. tab. 480 mg: 10, 20, 30 or 100 pcs. P No. 014378/02-2002 (2017-09-02 - 2017-09-07)
. tab. 480 mg: 20 pcs. R N000681/02-2003 (2016-03-09 - 0000-00-00)
. tab. 960 mg: 20, 30, 40, 50 or 100 pcs. P No. 013806/02-2002 (2018-03-02 - 2018-03-07)
. tab., cover shell, 960 mg: 10, 20 or 50 pcs. P N014158/01 (2012-09-08 - 0000-00-00)
. susp. for oral administration 240 mg/5 ml: vial. 50 ml or 100 ml P N014160/01 (2029-09-08 - 0000-00-00)
. tab. 480 mg: 20 pcs. P No. 014628/02-2003 (2001-04-03 - 2001-04-08)
. tab. 120 mg: 20 pcs. R No. 002616/01-2003 (2030-06-03 - 2030-06-08)
. syrup 120 mg/4 ml: vial. 100 ml in set. with dosing cap P No. 014628/01-2002 (2018-12-02 - 2018-12-07)
. tab. 480 mg: 10 or 20 pcs. Р №000700/01 (2027-12-07 - 2027-12-12)
. tab. 960 mg: 10 pcs. P No. 014260/01-2002 (2015-10-02 - 2015-10-07)
. susp. for oral administration 240 mg/5 ml: vial. 60 ml or 120 ml P No. 013806/01-2002 (2018-03-02 - 2018-03-07)
. tab. 480 mg: 20 pcs. R No. 001227/01-2002 (2025-03-02 - 2025-03-07)

SULFAMETOXAZOLE + TRIMETHOPRIM - description and instructions provided by the Vidal medicines guide.

Co-trimoxazole: instructions for use and reviews

Latin name: Co-trimoxazole

ATX Code: J01EE01

Active substance: co-trimoxazole [sulfamethoxazole + trimethoprim] (co-trimoxazole)

Producer: OJSC "Biosintez", OJSC "Pharmstandard-Leksredstva", Russia

Description and photo update: 31.07.2017

Co-trimoxazole is a combined antimicrobial sulfanilamide drug.

Release form and composition

Dosage forms of Co-trimoxazole:

Tablets 120 mg (10 pcs in blister packs, 3 packs in a carton pack; 20 pcs in jars, 1 jar in a carton pack; 10 pcs in blister packs, 100 packs in a carton box);
Tablets 480 mg (10 pcs in blisters, 1 or 2 blisters in a carton pack; 10 pcs in blister packs, 3 packs in a carton pack; 20 pcs in jars, 1 jar in a carton pack; 10 pcs . in non-cell contour packs, 100 packs in a cardboard box);
Tablets 960 mg (in packs of 10, 20, 100 or 500 pieces);
Suspension for oral administration (50, 100 or 125 mg in dark glass bottles, 1 bottle complete with a dosing spoon in a cardboard pack);
Granules for the preparation of a suspension for oral administration (4.8 g each in 100 ml vials, in a package of 1 or 20 vials).

Active substances in the composition of Co-trimoxazole:

1 tablet 120 mg: sulfamethoxazole - 100 mg and trimethoprim - 20 mg;
1 tablet 480 mg: sulfamethoxazole - 400 mg and trimethoprim - 80 mg;
1 tablet 960 mg: sulfamethoxazole - 800 mg and trimethoprim - 160 mg;
5 ml suspension: sulfamethoxazole - 200 mg and trimethoprim - 40 mg;
5 ml suspension prepared from granules: sulfamethoxazole - 200 mg and trimethoprim - 40 mg.

Pharmacological properties

Pharmacodynamics

Sulfamethoxazole is similar in structure to para-aminobenzoic acid and prevents the production of dihydrofolic acid in bacterial cells, preventing the inclusion of para-aminobenzoic acid in its molecule. Trimethoprim enhances the properties of sulfamethoxazole, disrupting the process of reduction of dihydrofolic acid to tetrahydrofolic acid. The latter is the active form of folic acid, which is responsible for the division of microbial cells and protein metabolism in them.

Co-trimoxazole is a broad-spectrum bactericidal agent. It is characterized by high activity against the following microorganisms: Chlamydia spp. (including Chlamydia psittaci, Chlamydia trachomatis), Streptococcus pneumoniae, Streptococcus spp. (especially hemolytic strains with increased sensitivity to penicillin), Pneumocystis carinii, Staphylococcus spp., Morganella spp., Neisseria gonorrhoeae, Neisseria meningitidis, Yersinia spp., Escherichia coli (including enterotoxigenic strains), Shigella spp., Salmonella spp . (including Salmonella paratyphi and Salmonella typhi), Serratia marcescens, Vibrio cholerae, some varieties of Pseudomonas (excluding Pseudomonas aeruginosa), Bacillus anthracis, Providencia, Haemophilus influenzae (including ampicillin-resistant strains), Legionella pneumophila, Listeria spp. , Enterobacter spp., Nocardia asteroides, Citrobacter, Bordetella pertussis, Mycobacterium spp. (including Mycobacterium leprae), Enterococcus faecalis, Brucella spp., Francisella tularensis, Klebsiella spp., Pasteurella spp., Proteus spp.

Co-trimoxazole also acts on protozoa: Leishmania spp., Plasmodium spp., Histoplasma capsulatum, Toxoplasma gondii, Coccidioides immitis, Actinomyces israelii, pathogenic fungi. Viruses, Corynebacterium spp., Leptospira spp., Pseudomonas aeruginosa, Treponema spp., Mycobacterium tuberculosis show resistance to the drug.

The drug suppresses the vital activity of Escherichia coli, which causes a decrease in the production of thiamine, nicotinic acid, riboflavin and other B vitamins in the intestine. The therapeutic effect lasts at least 7 hours.

Pharmacokinetics

When taken orally, Co-trimoxazole is absorbed by approximately 90%. The maximum level of the substance in plasma is recorded 1-4 hours after administration, and therapeutic concentrations remain at the required level for 7 hours after a single dose. Co-trimoxazole is well distributed throughout the tissues and systems of the body, penetrates through the placental and blood-brain barriers, as well as into breast milk. During treatment in the urine and lungs, concentrations of the substance exceeding those in plasma are maintained.

To a lesser extent, Co-trimoxazole accumulates in interstitial fluid, bronchial secretions, breast milk, vaginal secretions, aqueous humor of the eye, prostate tissue and secretion, saliva, middle ear fluid (during an inflammatory process), bones, bile, cerebrospinal fluid. Sulfamethoxazole binds to plasma proteins by 66%, trimethoprim - by 45%.

Both active components of Co-trimoxazole are metabolized, forming acetylated derivatives (to a greater extent this is typical for sulfamethoxazole). Metabolites do not have antibacterial activity.

Co-trimoxazole is excreted through the kidneys unchanged (trimethoprim - 50% of the dose taken, sulfamethoxazole - 20% of the dose taken) and in the form of metabolites (80% of the dose taken over 72 hours). A small amount of the substance is excreted through the intestines. The half-life of trimethoprim is 10-12 hours, sulfamethoxazole - 9-11 hours. In children, it turns out to be significantly less and is determined by age: up to 1 year, the half-life is 7-8 hours, from 1 year to 10 years - 5-6 hours. In elderly patients and patients with renal dysfunction, the half-life of co-trimoxazole increases.

Indications for use

Monotherapy:

Respiratory tract infections: acute and chronic bronchitis, bronchopneumonia, lobar and pneumocystis pneumonia, bronchiectasis;
Infections of the gastrointestinal tract: cholera, salmonella, cholangitis, dysentery, paratyphoid, cholecystitis, typhoid fever and gastroenteritis caused by enterotoxic strains of Escherichia coli;
ENT infections: tonsillitis, laryngitis, sinusitis, scarlet fever, otitis media;
Urinary tract infections: gonorrhea (male and female), inguinal granuloma, venereal lymphogranuloma, soft chancre, epididymitis, prostatitis, pyelitis, cystitis, pyelonephritis, urethritis;
Soft tissue and skin infections: wound infections, furunculosis, acne, pyoderma.

Complex therapy:

Acute brucellosis;
Toxoplasmosis;
Malaria (Plasmodium falciparum);
South American blastomycosis;
Acute and chronic osteomyelitis;
Other osteoarticular infections.

Contraindications

Absolute:

Renal failure (creatinine clearance less than 15 ml / min);
B12 deficiency anemia;
aplastic anemia;
Liver failure;
Deficiency of glucose-6-phosphate dehydrogenase;
Agranulocytosis, leukopenia;
Hyperbilirubinemia in children;
Children's age up to 3 months;
Pregnancy and lactation;
Hypersensitivity to Co-trimoxazole or other sulfonamides.

Relative:

Bronchial asthma;
folic acid deficiency;
Thyroid diseases;
Impaired kidney and liver function;
Allergic reactions in history.

Instructions for use Co-trimoxazole: method and dosage

According to the instructions, Co-trimoxazole should be taken orally during or after meals.

A suspension is prepared from the granules. To do this, add 100 ml of boiled water to the vial and mix thoroughly.

Adults and children over 12 years old: 960 mg 1 time / day or 480 mg 2 times / day, in severe cases - 480 mg 3 times / day, for chronic infections - 480 mg 2 times / day;
Children 6-12 years old: 240-480 mg 2 times / day;
Children 2-6 years old: 120-240 mg 2 times / day;
Children 1-2 years old: 120 mg 2 times / day.

Adults and adolescents over 12 years of age: 960 mg 2 times / day;
Children 7-12 years old: 480 mg 2 times / day;
Children 4-6 years old: 240-480 mg 2 times / day;
Children from 7 months to 6 years: 120-240 mg 2 times / day;
Children 3-6 months: 120 mg 2 times / day.

The duration of treatment depends on the indication and the overall clinical picture, usually ranging from 5 to 10 days. After the clinical symptoms of the disease disappear, the drug should be continued for another 2 days. Therapy for acute brucellosis lasts 3-4 weeks, paratyphoid and typhoid fever - 1-3 months. Treatment of chronic infections is longer.

To prevent recurrence of chronic infections of the urinary system, Co-trimoxazole is prescribed to adults and adolescents over 12 years of age, 480 mg once a day at night, to children under 12 years of age - 12 mg / kg / day. The course can last from 3 to 12 months.

In acute cystitis in children aged 7-16 years, 480 mg is prescribed 2 times / day for 3 days.

The initial dose for typhoid fever is 960 mg 3 times / day, after the fever subsides, the dose is reduced to 960 mg 2 times / day, treatment is continued for at least 2 weeks. For children, the dose is reduced by 2 times.

Patients with gonorrheal pharyngitis Co-trimoxazole is prescribed in case of hypersensitivity to penicillin: at a dose of 4320 mg once a day for 5 days.

For some diseases in adults, the doctor may recommend a single dose of the drug or short-term courses. Eg:

Uncomplicated cystitis in women: 2400 mg once with plenty of water;
Chancroid: 3840 mg once with plenty of water;
Uncomplicated acute gonorrhea: 2400 mg once, after 8 hours - taking a similar dose.

Patients with renal insufficiency with a creatinine clearance (CC) of more than 25 ml / minute do not require dose adjustment of Co-trimoxazole, with CC from 15 to 25 ml / minute, a standard dose is prescribed during the first 3 days of therapy, then - ½ of the standard dose. Patients with CC less than 15 ml / minute can use ½ of the standard dose only if the patient is undergoing hemodialysis.

Side effects

On the part of the hematopoietic organs: agranulocytosis, thrombocytopenia, megaloblastic anemia, neutropenia, leukopenia;
From the nervous system: vertigo, headache; in some cases - tremor, apathy, peripheral neuritis, depression, aseptic meningitis;
From the respiratory system: pulmonary infiltrates, bronchospasm;
From the digestive system: stomatitis, glossitis, gastritis, diarrhea, abdominal pain, loss of appetite, cholestasis, nausea, vomiting, increased activity of hepatic transaminases, pseudomembranous enterocolitis, hepatonecrosis, hepatitis;
From the urinary system: hematuria, crystalluria, hypercreatininemia, polyuria, increased urea concentration, impaired renal function, interstitial nephritis, toxic nephropathy with oliguria and anuria;
From the musculoskeletal system: myalgia, arthralgia;
Allergic reactions: rash, itching, exfoliative dermatitis, scleral hyperemia, angioedema, fever, allergic myocarditis, photosensitivity, toxic epidermal necrolysis, erythema multiforme exudative;
Other: hypoglycemia.

Overdose

Symptoms of an overdose of Co-trimoxazole include crystalluria, hematuria, intestinal colic, nausea, vomiting, fever, headache, dizziness, visual disturbances, drowsiness, clouded consciousness, depression, fainting. Long-term use of the drug in high doses can also provoke jaundice, megaloblastic anemia, leukopenia, thrombocytopenia.

Emergency measures for overdose include gastric lavage. Trimethoprim is excreted from the body faster when urine is acidified. Oral fluid intake and intramuscular administration of calcium folinate at a daily dose of 5–15 mg are also recommended (it neutralizes the effect of trimethoprim on the bone marrow). If necessary, hemodialysis is carried out.

special instructions

With long-term treatment (more than 1 month), it is necessary to regularly do a blood test, because. there is a risk of hematological changes (including asymptomatic). These changes can be reversible due to the intake of folic acid (at a daily dose of 3-6 mg), while the antimicrobial activity of the drug is not significantly impaired. Particular caution should be observed in the treatment of the elderly and patients with suspected initial folate deficiency. The additional appointment of folic acid is also advisable for long-term treatment with Co-trimoxazole in high doses. In addition, with long-term treatment, it is necessary to monitor the functional state of the liver and kidneys.

To avoid the development of crystalluria, an adequate water load should be ensured and a sufficient volume of urine should be maintained. With a decrease in the filtration function of the kidneys, the risk of developing allergic and toxic complications of sulfonamides increases significantly.

During treatment, it is recommended to avoid excessive solar and ultraviolet exposure, as well as to exclude from the diet foods that contain large amounts of para-aminobenzoic acid (PABA), such as tomatoes, carrots, green parts of plants (spinach, cauliflower and legumes).

Patients with acquired immune deficiency syndrome (AIDS) have a significantly higher risk of side effects.

Due to the widespread resistance of strains, Co-trimoxazole is not recommended for pharyngitis and tonsillitis caused by group A beta-hemolytic streptococcus.

Influence on the ability to drive vehicles and complex mechanisms

During therapy, care must be taken when driving and performing potentially hazardous types of work that require increased concentration and immediate psychomotor reactions. The possibility of side effects from the central nervous system should be taken into account: dizziness, hallucinations, convulsions, vertigo. With their development, it is recommended to abandon the activities indicated above.

drug interaction

Derivatives of salicylic acid: the effect of Co-trimoxazole is enhanced;
Methotrexate: its toxicity increases;
Hypoglycemic drugs: their effect is enhanced;
Indirect anticoagulants: their activity increases;
Phenytoin, warfarin: the intensity of their hepatic metabolism decreases, the effects increase;
Oral contraceptives: their effectiveness decreases;
Procaine, benzocaine, procainamide and other drugs, as a result of the hydrolysis of which PABA is formed: reduce the effect of Co-trimoxazole;
Rifampicin: shortened half-life of trimethoprim;
Pyrimethamine at doses greater than 25 mg/week: increased risk of megaloblastic anemia;
Diuretics (especially thiazides): increased risk of thrombocytopenia, especially in the elderly;
Para-aminosalicylic acid, phenytoin, barbiturates: manifestations of folic acid deficiency increase;
Colestyramine: absorption of Co-trimoxazole is reduced (in this regard, the drug should be taken 1 hour before or 4-6 hours after taking colestyramine);
Drugs that inhibit bone marrow hematopoiesis: the risk of myelosuppression increases;
Indomethacin, butadione, naproxen, salicylates and some other non-steroidal anti-inflammatory drugs: it is possible to increase the action of Co-trimoxazole with the development of undesirable effects;
Chloridine: the antimicrobial effect of the drug is enhanced.

Between diuretics (furosemide, thiazides, etc.) and oral hypoglycemic drugs (sulfonylurea derivatives), on the one hand, and antimicrobial sulfonamides, on the other hand, a cross-allergic reaction may develop.

Analogues

Analogues of Co-trimoxazole are: Berlocid 240, Biseptol, Bactrim, Groseptol, Brifeseptol, Duo-Septol, Dvaseptol, Co-trimoxazole-Acri, Cotrifarm 480, Co-trimoxazole-STI, Oriprim, Co-trimoxazole-Biosynthesis, Trimezol, Metosulfabol, Polseptol, Sinersul, Septrin, Sumetrolim, Sulotrim, Tsiplin.

Terms and conditions of storage

Store in a dry, dark place and out of the reach of children. Tablets and granules - at a temperature of 15-25 ºС, suspension - at a temperature of up to 15 ºС.

The shelf life of tablets is 5 years, suspensions and granules - 2 years. The suspension prepared from granules can be stored for 2 weeks at room temperature, up to 4 weeks in the refrigerator.

Co-trimoxazole [Sulfamethoxazole + Trimethoprim]

Latin name

Co-trimoxazole

chemical name

Trimethoprim* and sulfamethoxazole* in a mass ratio of 1:5

Pharmacological group

Sulfonamides

Nosological classification (ICD-10)

Pharmacology

Pharmacological action - broad spectrum antibacterial, bactericidal, antiprotozoal.

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.; Haemophilus ducreyi, some strains of H.influenzae, 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 carinii, Toxoplasma gondii, incl. h. 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 the microbial cell and prevents the incorporation of PABA into the dihydrofolic acid molecule. Trimethoprim reversibly inhibits bacterial dihydrofolate reductase, disrupts the synthesis of tetrahydrofolic acid from dihydrofolic acid, the formation of purine and pyrimidine bases, nucleic acids; inhibits the growth and reproduction of microorganisms.

In connection with the inhibition of the vital activity of Escherichia coli, the synthesis of thiamine, riboflavin, nicotinic acid and other B-complex vitamins in the intestine decreases.

After oral administration, both components are rapidly and almost completely absorbed in the gastrointestinal tract. Cmax in the blood is reached after 1-4 hours, the antibacterial concentration persists for 7 hours; 24 hours after a single dose in plasma, small amounts are determined. Equilibrium plasma concentration is recorded after 2-3 days. 44% of trimethoprim and 70% of sulfamethoxazole are bound to plasma proteins. Both substances are biotransformed in the liver (acetylation) with the formation of inactive metabolites. They are evenly distributed in the body, pass through histohematic barriers, create concentrations in the lungs and urine that exceed those in plasma. To a lesser extent, they accumulate in bronchial secretions, vaginal secretions, secretions and prostate tissue, middle ear fluid, cerebrospinal fluid, bile, bones, saliva, aqueous humor of the eye, breast milk, interstitial fluid. They have the same elimination rate, T 1/2 - 10-11 hours. In children, T 1/2 is significantly less and depends on age: up to the 1st year - 7-8 hours, 1-10 years - 5-6 hours. elderly and patients with impaired renal function T 1/2 increases. Excreted by the kidneys in the form of metabolites and unchanged (50-70% trimethoprim and 10-30% sulfamethoxazole) through glomerular filtration and tubular secretion.

Application

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, chancre, venereal lymphogranuloma, inguinal granuloma; Gastrointestinal tract: bacterial diarrhea, shigellosis, cholera (as part of combination therapy), typhoid fever and paratyphoid fever (including bacteria carrier), cholecystitis, cholangitis, gastroenteritis caused by enterotoxic strains of E. coli; 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 (as part of complex therapy).

Contraindications

Hypersensitivity (including to sulfonamides or trimethoprim), liver or kidney failure, B 12 deficiency anemia, agranulocytosis, leukopenia, glucose-6-phosphate dehydrogenase deficiency, pregnancy, breast-feeding, children's age (up to 2 months - for oral, up to 6 years - for parenteral administration), hyperbilirubinemia in children.

Application restrictions

It is used with caution in case of a possible deficiency of folic acid (including in the elderly, patients with chronic alcoholism, with malabsorption syndrome - in these cases, additional folate is indicated for low body weight), aggravated allergic history, bronchial asthma, impaired liver and thyroid function glands.

Use during pregnancy and lactation

Side effects

From the nervous system and sensory organs: aseptic meningitis, headache, convulsions, peripheral neuritis, ataxia, vertigo, tinnitus, headache, hallucinations, depression, apathy, nervousness, weakness, fatigue, insomnia.

From the digestive tract: nausea, vomiting, diarrhea, abdominal pain, anorexia, cholestatic and necrotic hepatitis, increased serum levels of transaminases and bilirubin, pseudomembranous enterocolitis, pancreatitis, stomatitis, glossitis.

From the respiratory system: allergic cough and shortness of breath, infiltrates in the lungs.

On the part of the hematopoietic organs: agranulocytosis, aplastic anemia, thrombocytopenia, leukopenia, neutropenia, hemolytic anemia, megaloblastic anemia, hypoprothrombinemia, methemoglobinemia, eosinophilia.

From the urinary system: renal failure, interstitial nephritis, increased plasma creatinine, toxic nephropathy with oliguria and anuria.

Allergic reactions: urticaria, rash, toxic epidermal necrolysis (Lyell's syndrome), Stevens-Johnson syndrome, anaphylaxis, allergic myocarditis, erythema multiforme, exfoliative dermatitis, angioedema, drug fever, chills, Henoch-Schonlein disease, serum sickness, generalized allergic reactions , generalized skin rash, photosensitivity, itching, redness of the sclera; there are reports of periarteritis nodosa and systemic lupus erythematosus.

Others: hyperkalemia, hyponatremia, arthralgia, myalgia, isolated cases of rhabdomyolysis (mainly in AIDS patients).

Interaction

NSAIDs, antidiabetic drugs (sulfonylurea derivatives), diphenin, indirect anticoagulants, thiazide diuretics, barbiturates enhance therapeutic (and side) effects (displace from plasma protein binding and increase blood concentration). Hexamethylenetetramine (urotropine), ascorbic acid increase crystalluria (cause urine acidification).

Co-trimoxazole increases serum concentrations of digoxin, especially in elderly patients (control of serum digoxin concentrations is necessary). With simultaneous administration, the effectiveness of tricyclic antidepressants decreases.

With simultaneous use with indomethacin, an increase in the concentration of sulfamethoxazole in the blood is possible.

Co-trimoxazole reduces the intensity of hepatic metabolism of phenytoin (extends its T 1/2 by 39% and reduces metabolic clearance by 27%); against the background of co-trimoxazole, the antiepileptic activity of phenytoin increases. Enhances the effect of oral hypoglycemic agents. Against the background of co-trimoxazole, which competes for renal secretion, excretion slows down, tissue levels increase and the risk of developing the toxic effects of amantadine increases; described a case of acute psychosis in an 84-year-old patient, which arose after the combined administration of co-trimoxazole and amantadine. With simultaneous use with ACE inhibitors, especially in elderly patients, hyperkalemia may develop.

Co-trimoxazole may prolong PT in patients concomitantly treated with warfarin (dose adjustment of warfarin required). Reduces the reliability of oral contraception (inhibits the intestinal microflora and reduces the enterohepatic circulation of hormonal compounds). Pyrimethamine (more than 25 mg/week) increases the likelihood of developing megaloblastic anemia.

Patients taking co-trimoxazole and cyclosporine after kidney transplantation may experience a reversible deterioration in kidney function, manifested by hypercreatininemia.

Overdose

Symptoms of acute overdose: anorexia, nausea, vomiting, weakness, abdominal pain, dizziness, headache, drowsiness, confusion; pyrexia, hematuria and crystalluria are possible.

Treatment: gastric lavage, fluid administration, correction of electrolyte disturbances. If necessary, hemodialysis.

Symptoms of chronic overdose: bone marrow depression (thrombocytopenia, leukopenia and / or megaloblastic anemia).

Treatment and prevention: the appointment of folic acid (5-15 mg daily).

Dosage and administration

Inside, in / m, in / in drip. 2 times a day (after 12 hours). Single dose: adults and children over 12 years old - 960 mg each; children 2-6 months - 120 mg (or 2.5 ml of children's suspension), 6 months - 5 years - 240 mg (or 5 ml of children's suspension), 6-12 years - 480 mg (or 10 ml of children's suspension) ).

Treatment of acute infections is continued until the disappearance of clinical symptoms and for the next 2 days, the average duration is at least 5 days; course duration for urinary tract infections, exacerbation of chronic bronchitis, acute otitis media, chancre, inguinal lymphogranulomatosis - 10-14 days; shigellosis, travelers' diarrhea - 5 days; uncomplicated infections of the lower urinary tract - 1-3 days; acute brucellosis - 3-4 weeks; typhoid and paratyphoid - 1-3 months; chronic prostatitis - 3 months. Parenterally (for severe infections): adults and children over 12 years old - 3 ml intramuscularly 2 times a day; children 6-12 years old - 1.5 ml intramuscularly 2 times a day, or intravenously drip 10-20 ml in 250 ml of 0.9% sodium chloride solution or 5% glucose solution 2 times a day, children 6-12 years - 18 mg (15 mg of sulfamethoxazole and 3 mg of trimethoprim) per 1 kg of body weight 2 times a day. The average duration is 5 days, then oral administration.

For the prevention of recurrence of chronic infections of the urinary system without bacteriuria: adults and children over 12 years old - 480 mg once a day at night, children under 12 years old - 2 mg / kg body weight trimethoprim per day and 10 mg / kg sulfamethoxazole per day , duration - 3-12 months.

In the treatment of pneumonia caused by Pneumocystis carinii, the highest doses are used: 15-20 mg / kg of trimethoprim and 75-100 mg / kg of sulfamethoxazole per day in 4 doses, for 14-21 days orally or parenterally. For the prevention of pneumocystis pneumonia - the usual doses during the period of possible relapse.

Uncomplicated gonorrhea - 480 mg 2 times a day, 2 days, or at the first dose - 2.4 g (table 5) and after 8 hours another 2.4 g, or a single dose of 3.84 g (table 8) .

With gonococcal infection of the nasopharynx - 960 mg 3 times / day for 7 days.

In case of malaria caused by Plasmodium falciparum, 1.92 g (4 tablets) are prescribed 2 times / day for 2 days.

Precautionary measures

Patients with impaired renal function with Cl creatinine 15-25 ml / min are administered orally in medium doses for 3 days, then 50% of the average daily dose; with values of Cl creatinine less than 15 ml / min, apply (1/2 of the average dose) only against the background of hemodialysis. When administered parenterally to patients with renal insufficiency, the concentration of sulfamethoxazole in plasma should be determined every 2-3 days in samples taken before the next administration (at a concentration above 150 μg / ml, treatment is stopped until a level of 120 μg / ml is reached).

If a rash, cough, arthralgia and other symptoms appear, the use should be stopped 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, an abundant alkaline drink (2-3 liters of fluid per day) is recommended.

Excessive sun and UV exposure should be avoided. The risk of side effects is much higher in AIDS patients. The simultaneous administration of folic acid to HIV-infected patients increases the likelihood of developing resistance to sulfonamides in strains of Pneumocystis carinii.

Year of last adjustment

2011

Interactions with other active substances

Sulfamethoxazole is an effective antimicrobial agent.

Presented are analogues of the drug co-trimoxazole [sulfamethoxazole + trimethoprim] (co-trimoxazole), in accordance with medical terminology, called "synonyms" - drugs that are interchangeable in terms of effects on the body, containing one or more identical active substances. When choosing synonyms, consider not only their cost, but also the country of origin and the reputation of the manufacturer.

Description of the drug

Co-trimoxazole [Sulfamethoxazole + Trimethoprim] (Co-trimoxazole)- Combined antimicrobial drug consisting of sulfamethoxazole and trimethoprim. Sulfamethoxazole, similar in structure to para-aminobenzoic 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 to tetrahydrofolic acid, the active form of folic acid responsible for protein metabolism and microbial cell division.

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

It inhibits the vital activity of Escherichia coli, which leads to a decrease in the synthesis of thymine, riboflavin, nicotinic acid and other B vitamins in the intestine.

List of analogues

Note! The list contains synonyms Co-trimoxazole [Sulfamethoxazole + Trimethoprim] (Co-trimoxazole), which have a similar composition, so you can choose a replacement yourself, taking into account the form and dose of the medicine prescribed by your doctor. Give preference to manufacturers from the USA, Japan, Western Europe, as well as well-known companies from Eastern Europe: Krka, Gedeon Richter, Actavis, Egis, Lek, Geksal, Teva, Zentiva.

Release form(by popularity)	price, rub.
Bactrim
Suspension for oral administration 240mg / 5ml 100ml (Seneksi S.a.S. (France)	162.50
Bactrim forte
Berlocid 240
Berlocid 480
Bi-Septin
Biseptol
Tab 120mg N20 Poland (POLFA Pabyanitsky za - d (Poland)	35.20
480mg No. 28 tab (POLFA Pabyanitsky za - d (Poland)	96.80
Suspension 80ml Poland (MEDANA Farma (Poland)	138.50
Biseptol 480
Brifeseptol
Groseptol
Dvaseptol
Duo-Septol
Co-trimoxazole
480mg No. 10 tab FST - LS (Pharmstandard - Leksredstva OAO (Russia)	25.20
Co-trimoxazole (Co-trimoxazole)
Co-trimoxazole [Sulfamethoxazole + Trimethoprim] (Co-trimoxazole)
Co-trimoxazole-Acri
480mg No. 20 tab (Akrikhin HFC OJSC (Russia)	36.90
Co-trimoxazole-Biosynthesis
Co-trimoxazole-Rivopharm
Co-trimoxazole-STI
Cotrifarm 480
Methosulfabol
Oriprim
Halfseptol
Septrin
Sinersul
Sulothrim
Sumetrolim
trimezol
Ziplin

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Official instructions for use

There are contraindications! Before use, read the instructions

SUMETROLIM ®

The active ingredients of Sumetrolim - sulfamethoxazole and trimethoprim - affect the metabolism of folic acid in bacteria. Sulfamethoxazole inhibits the incorporation of para-aminobenzoic acid into dihydrofolic acid in the bacterial cell. In addition, sulfamethoxazole competitively inhibits dihydropteroate synthetase. Trimethoprim specifically inhibits dihydrofolate reductase, which catalyzes the conversion of dihydrofolic acid to tetrahydrofolic acid. That is, sulfamethoxazole and trimethoprim affect the same chain of biochemical reactions at different stages, potentiating each other's action.

Active substance:
sulfamethoxazole 2500 mg
trimethoprim 500 mg
in one bottle of syrup (100 ml)

sulfamethoxazole 400 mg
trimethoprim 80 mg
in one tablet

Indications for use:

Diseases of the upper and lower respiratory tract:
acute and chronic bronchitis, bronchiectasis, pneumonia, tonsillitis, sinusitis, pharyngitis.
Kidney and urinary tract infections:
acute and chronic cystitis, pyelitis, pyelonephritis, urethritis.
Inflammatory diseases of the gallbladder and biliary tract:
cholecystitis, cholangitis.
Infections of the gastrointestinal tract:
enteritis, typhoid fever, paratyphoid, dysentery.
Skin infections: pyoderma, furunculosis, abscess, wound infections.
Diseases of the urinary tract:
urethritis caused by gonococcus, prostatitis.

Contraindications:

Liver and kidney failure, blood disorders, hypersensitivity to sulfanilamide drugs, pregnancy (first trimester and period before childbirth).

Dosage:
In cases of acute infection, it is necessary to prescribe for at least 4 days, and then at a maintenance dose until an asymptomatic clinical picture is achieved for at least 2 days.
For adults- the initial daily dose is 2 tablets 2 times a day (maximum 3 tablets 2 times a day) in the morning and evening after meals; maintenance dose is 1 tablet 2 times a day.
For children: at the age of 1 year - 1/4 tablet 2 times a day or 1 ml of syrup 2 times a day; at the age of 2-6 years - 1/4-1/2 tablets 2 times a day or 6-8 ml of syrup 2 times a day; at the age of 7-12 years - 1/2-1 tablet 2 times a day or 8-16 ml of syrup 2 times a day after meals.
1/4 tablet or 4 ml syrup contains 20 mg trimethoprim and 100 mg sulfamethoxazole.

Side effects

Feeling unwell, headaches, drug rash, complaints from the stomach (to prevent the latter, it is advisable to prescribe a small amount of hydrochloric acid). Transient disorders of the hematopoietic system (leukopenia, a decrease in the number of platelets and folic acid) are rarely noted, which disappear when folic acid is prescribed. Impaired liver function.

drug interaction

Avoid co-administration with:

oral anticoagulants (increased anticoagulant action)

phenytoin (an increase in the content of phenytoin in the blood serum to toxic is possible)

oral antidiabetic agents (danger of hypoglycemia)

methotrexate (its content in blood serum can reach toxic levels)

salicylates, phenylbutazone and naproxen (they can increase the content of sulfanilamide in the blood serum to toxic)
Warning:
It is forbidden to prescribe the drug to premature newborns, newborns and infants up to 6 weeks of age! Up to 3 months of age, the drug can be prescribed only in exceptional cases!
With limited renal function - in order to avoid cumulation - it is allowed to prescribe the drug only in reduced doses (it is recommended to determine the concentration in the blood plasma).
With long-term administration of the drug, systematic monitoring of the blood picture (including the number of platelets!) is necessary. If during the use of the drug exanthema is noted, the reception should be stopped immediately!
During treatment with Sumetrolim, care must be taken to take enough fluids.
Care must be taken when prescribing the drug: in cases of anemia caused by folic acid deficiency, when prescribed in patients with alcoholism and in patients taking immunosuppressive agents.
During lactation - in the first 6 weeks - the appointment of the drug should be avoided. However, if the infection is caused by pathogens resistant to all antibiotics, but pathogens sensitive to sulfonamides, then during the treatment of the mother and in the next 3 months, the newborn should receive milk from another mother or, as a last resort, it is necessary to transfer it to artificial feeding.

Package:
1 bottle of syrup (100 ml)
20 tablets

The information on the page was verified by the therapist Vasilyeva E.I.

Azathioprine*	Against the background of co-trimoxazole, leukopenia may be exacerbated, especially in patients with a transplanted kidney.
Azithromycin*	When combined, the effect is summed up.
Amantadine*	Against the background of co-trimoxazole, which competes for renal secretion, excretion slows down, tissue levels increase and the risk of developing the toxic effects of amantadine increases; described a case of acute psychosis in an 84-year-old patient, which arose after the combined administration of co-trimoxazole and amantadine.