Co-trimoxazole - instructions for use, analogs, reviews and release forms (tablets 120 mg and 480 mg, suspension for oral administration of 240 mg) drugs for the treatment of urethritis, cystitis and other infections in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Co-trimoxazole. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Co-trimoxazole in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Co-trimoxazole in the presence of existing structural analogs.Use for the treatment of urethritis, cystitis, bronchitis and other infectious diseases in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Co-trimoxazole - 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. (streptococcus) (haemolytic strains are more sensitive to penicillin), Staphylococcus spp. (Staphylococcus aureus), Streptococcus pneumoniae, Neisseria meningitidis, Neisseria gonorrhoeae, Escherichia coli (E. coli) (including enterotoxigenic strains), Salmonella spp. (Salmonella) (including Salmonella typhi and Salmonella paratyphi), Vibrio cholerae, Bacillus anthracis, Haemophilus influenzae (including ampicillin-resistant strains), Listeria spp. (listeria), Nocardia asteroides, Bordetella pertussis, Enterococcus faecalis, Klebsiella spp. (Klebsiella), Proteus spp. (Proteus), Pasteurella spp., Francisella tularensis, Brucella spp., Mycobacterium spp. (mycobacterium) (incl.Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumophila (Legionella), Providencia, some species of Pseudomonas (except Pseudomonas aeruginosa), Serratia marcescens, Shigella spp. (shigella), Yersinia spp., Morganella spp., Pneumocystis carinii; Chlamydia spp. (chlamydia) (including Chlamydia trachomatis, Chlamydia psittaci); protozoa: Plasmodium spp., Toxoplasma gondii, pathogens, 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.

Composition

Sulfamethoxazole + Trimethoprim + auxiliary substances.

Pharmacokinetics

When taken orally, absorption is 90%. Well distributed in the body. It penetrates the blood-brain barrier (GEB), the placental barrier and into breast milk. In the lungs and urine creates concentrations exceeding the content in the plasma. To a lesser extent, it accumulates in bronchial secretion, vaginal secretions, secretion and prostate tissue, middle ear fluid (with its inflammation), cerebrospinal fluid, bile, bones, saliva, watery eyes, breast milk, interstitial fluid. The connection with plasma proteins is 66% in sulfamethoxazole, in trimethoprim 45%. More sulfamethoxazole is metabolized 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.

Indications

• infections of the urino-genital organs: urethritis, cystitis, pyelitis, pyelonephritis, prostatitis, epididymitis, gonorrhea (male and female), mild chancroid, venereal lymphogranuloma, inguinal granuloma;
• respiratory tract infections: bronchitis (acute and chronic), bronchiectasis, croupous pneumonia, bronchopneumonia, pneumocystis pneumonia;
• infection of ENT organs: otitis media, sinusitis, laryngitis, tonsillitis; scarlet fever;
• GI tract infections: typhoid fever, paratyphoid, salmonella, 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), etc. osteoarticular infections;
• brucellosis (acute);
• South American blastomycosis;
• malaria (Plasmodium falciparum);
• toxoplasmosis (as part of complex therapy).

Forms of release

Tablets 120 mg and 480 mg.

Suspension for oral administration 240 mg.

Other dosage forms, whether capsules, ointment or cream at the time of publication of the drug in the Directory did not exist.

Instructions for use and dosing regimen

Inside, intravenously, intramuscularly. In each dosage form, the quantitative ratio of trimethoprim and sulfamethoxazole is 1: 5.

Inside (tablets), adults and children over 12 years - 960 mg once, or 480 mg 2 times a day. In severe infections - 480 mg 3 times a day, with chronic infections, a maintenance dose of 480 mg 2 times a day. Children 1-2 years - 120 mg 2 times a day, 2-6 years - 120-240 mg 2 times a day, 6-12 years - 240-480 mg 2 times a day.

Suspension: children 3-6 months - 120 mg twice 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 - 960 mg 2 times a day. Syrup for children: children 1-2 years - 120 mg 2 times a day, 2-6 years - 180-240 mg 2 times a day, 6-12 years - 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. With chronic infections, the course of treatment is longer. In acute brucellosis - 3-4 weeks, with typhoid fever and paratyphoid - 1-3 months.

For the prevention of recurrences of chronic urinary tract infections, adults and children over 12 years of age - 480 mg once a day at night, children under 12 years - 12 mg / kg per day. The duration of treatment is 3-12 months.The course of treatment of acute cystitis in children 7-16 years - 480 mg 2 times a day for 3 days.

With gonorrhea - 1920-2880 mg per day for 3 doses.

With gonorrheal pharyngitis (with hypersensitivity to penicillin) - 4320 mg once a day for 5 days. In pneumonia caused by Pneumocystis carinii, 120 mg / kg / day at intervals of 6 hours for 14 days.

Parenterally: intramuscularly to adults and children over 12 years of age - 480 mg every 12 hours, children 6-12 years - 240 mg every 12 hours.

Intravenous drip (in the form of a dropper), adults and children over 12 years - 960-1920 mg every 12 hours, children 6-12 years - 480 mg 2 times a day; 6 months-5 years - 240 mg 2 times a day; 6 weeks-5 months - 120 mg twice a day.

To achieve maximum efficacy, a constant concentration of trimethoprim in plasma or serum should be maintained at 5 μg / ml or higher.

Malaria caused by Plasmodium falciparum, is an intravenous infusion (1920 mg twice daily) for 2 days. Children will need a correspondingly reduced dose.

To achieve higher concentrations in the cerebrospinal fluid injected in / in the drip (dissolved in 200 ml of solvent) for 1 hour 2 times a day.

In case of renal insufficiency, the dose depends on the value of CC: with a QC greater than 25 ml / min - the standard dose; at 15-25 ml / min - the standard dose for 3 days, then half the standard dose.With QC less than 15 ml / min, half the standard dose is prescribed only against hemodialysis.

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

If there is clouding or crystallization of the solution before or during infusion, the mixture can not be used. The duration of administration is 1-1.5 hours (should be consistent with the needs of the patient in the liquid).

If necessary, the restriction in the volume of the injected liquid is introduced at higher concentrations - 5 ml is dissolved in 50-75 ml of a 5% solution of Dextrose in water. In severe infections in all age groups, the dose can be increased by 50%.

Side effect

• headache;
• dizziness;
• aseptic meningitis;
• depression;
• apathy;
• tremor;
• peripheral neuritis;
• bronchospasm;
• pulmonary infiltrates;
• nausea, vomiting;
• decreased appetite;
• diarrhea;
• gastritis;
• abdominal pain;
• glossitis, stomatitis;
• cholestasis;
• increased activity of hepatic transaminases;
• hepatitis;
• hepatonecrosis;
• pseudomembranous enterocolitis;
• leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia;
• polyuria;
• interstitial nephritis;
• impaired renal function;
• crystalluria;
• hematuria (blood in the urine);
• increased urea concentration;
• hypercreatininaemia;
• toxic nephropathy with oliguria and anuria;
• arthralgia;
• myalgia;
• itching;
• photosensitization;
• rash;
• multiforme exudative erythema (including Stevens-Johnson syndrome);
• toxic epidermal necrolysis (Lyell's syndrome);
• exfoliative dermatitis;
• allergic myocarditis;
• increased body temperature;
• angioedema;
• hyperemia sclera;
• thrombophlebitis (at the site of the venipuncture);
• pain in the injection site;
• hypoglycemia.

Contraindications

• hypersensitivity (including to sulfanilamides);
• liver failure;
• renal failure (CC less than 15 ml / min);
• aplastic anemia;
• B12-deficiency anemia;
• agranulocytosis, leukopenia;
• deficiency of glucose-6-phosphate dehydrogenase;
• pregnancy;
• lactation period;
• age to 6 years (for the / m introduction);
• children's age (up to 3 months - for oral administration);
• Hyperbilirubinemia in children.

Application in pregnancy and lactation

Co-trimoxazole is contraindicated in pregnancy and lactation.

Use in children

For children, the drug is prescribed according to the indications and according to the recommended dosage regimen.Intramuscular administration is contraindicated at the age of up to 6 years, ingestion for children up to 3 months.

Application in elderly patients

In the elderly and patients with impaired renal function, the elimination half-life increases.

special instructions

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

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

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 large quantities of PABC, green parts of plants (cauliflower, spinach, beans), carrots, tomatoes.

Excessive sunlight and UV irradiation should be avoided.

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

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

Drug Interactions

Pharmaceutically compatible with the following medicines: dextrose for IV infusions 5 and 10%, levulosis for IV infusions 5%, sodium chloride for IV infusions 0.9%, a mixture of 0.18% sodium chloride and 4% dextrose for IV infusions, 6% dextran 70 for IV infusions in 5% dextrose or in 0.9% sodium chloride solution, 10% dextran 40 for IV infusions in 5% dextrose or 0.9% sodium chloride solution, Ringer's 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 (prolongs its half-life by 39%) and warfarin, enhancing their effect.

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

Rifampicin reduces the half-life of trimethoprim.

Pyrimethamine in doses exceeding 25 mg per week increases the risk of megaloblastic anemia.

Diuretics (often thiazides) increase the risk of thrombocytopenia.

Reduce the effect of benzocaine, procaine, procainamide (and other medicines, as a result of hydrolysis of which formed PABC).

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

Phenytoin, barbiturates, PASC intensify manifestations of folic acid deficiency.

The derivatives of salicylic acid intensify the action.

Kolestyramine lowers absorption, so it should be taken 1 hour after or 4-6 hours before taking Co-trimoxazole.

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

Analogues of the drug Ko-trimoxazole

Structural analogs for the active substance:

• Bactrim;
• Bactrim forte;
• Berlocid 240;
• Berlocid 480;
• Bi-Septin;
• Biseptol;
• Biseptol 480;
• Briefeptol;
• Grosseptol;
• Dvseptol;
• Duo Septol;
• Co-trimoxazole Acry;
• Co-trimoxazole Rivofarm;
• Co-trimoxazole STI;
• Cotripharm 480;
• Methosulfabol;
• Oriprim;
• Septrin;
• Sinersul;
• Sulotrim;
• Sumetrolim;
• Trimezol;
• Cyplin.

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