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

Excipients: microcrystalline cellulose, potato starch, povidone (low molecular weight medical polyvinylpyrrolidone 12600 ± 2700), crospovidone (kollidone CL), magnesium stearate.

Description:Tablets are white or almost white, flat-cylindrical with a bevel, tablets 120 mg without risks, tablets 480 mg with a risk.

Pharmacotherapeutic group:Antimicrobial combination.

ATX: & nbsp

J.01.E.E.01 Co-trimoxazole [sulfamethoxazole in combination with trimethoprim]

Pharmacodynamics:Combined antimicrobial drug consisting of sulfamethoxazole and trimethoprim. Sulfamethoxazole, similar in structure to paraminobenzoic acid (PABA), disrupts the synthesis of dihydrofolic acid in bacterial cells, preventing the release 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 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. (incl. Mycobacterium leprae), Citrobacter, Enterobacter spp., Legionella pneumophila, Providencia, some species Pseudomonas (Besides Pseudomonas aeruginosa), Serratia marcescens. Shigella spp., Yersinia spp., Morganella spp., Pneumocystis carinii; 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. The duration of the therapeutic effect is 7 hours.

Pharmacokinetics:

When ingestion, both components of the drug are completely absorbed from the gastrointestinal tract. The maximum concentration of the active components of the drug is observed after 1-4 hours.

Trimethoprim penetrates well into cells and through tissue barriers - into the lungs, kidneys, prostate gland, bile, saliva, sputum, liquor. Binding to proteins 50%. The half-life period is normally 8.6-17 hours. It is excreted mainly by the kidneys, 50% - unchanged.

Sulfamethoxazole binds to plasma proteins 66%, the half-life in the norm is 9-11 hours. It is excreted mostly by the kidneys, 15-30% - in active form.

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, croupous pneumonia, bronchopneumonia, pneumocystis pneumonia;

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

gastrointestinal tract infections: typhoid fever, paratyphoid, salmonella, cholera, dysentery, cholecystitis, cholangitis, gastroenteritis caused by enterotoxic strains 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).

Contraindications:

Hypersensitivity (including to trimethoprim and sulfonamides), severe cardiovascular diseases, hepatic, renal failure, aplastic anemia, B12-deficiency anemia, agranulocytosis, leukopenia, glucose-6-phosphate dehydrogenase deficiency, pregnancy, lactation period, children under 3 years, hyperbilirubinemia in children.

Carefully:With a deficiency of folic acid, bronchial asthma, thyroid gland diseases.

Dosing and Administration:

Inside, after eating, with enough liquid.

The dose is set individually.

Children: from 3 to 5 years - 240 mg (2 tablets of 120 mg) 2 times a day; from 6 to 12 years - 480 mg (4 tablets of 120 mg or 1 tablet of 480 mg) 2 times a day.

Adults and children over 12 years: 960 mg 2 times a day, with prolonged therapy - 480 mg 2 times a day. The course of treatment 5-14 days, with severe course and / or chronic form of the disease, a single dose can be increased by 30-50%.

For pneumonia, 0.1 g / kg / day (calculated for sulfamethoxazole), the interval between doses is 6 hours, the course is 14 days.

With gonorrhea - 2 g (calculated on sulfamethoxazole) 2 times a day with an interval of 12 h. If the course of treatment exceeds 5 days and / or an increase in dose is necessary, therapy should be carried out under hematological control; when changing the blood picture, folic acid should be prescribed at 5-10 mg / day.

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, decreased appetite, 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, interregional anemia.

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

From the musculoskeletal system: arthralgia, myalgia.

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

Local reactions: thrombophlebitis (in place of venipuncture), tenderness at the site of administration. 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, acidification of urine increases the excretion of trimethoprim, intake of fluid inside, intramuscularly - 5-15 mg / day of calcium folinate (eliminates the effect of trimethoprim on the bone marrow), if necessary - hemodialysis.

Interaction:

It is not recommended to use with thiazide diuretics because of the risk of thrombocytopenia (bleeding).

It is not recommended simultaneous administration of the drug with salicylates, butadione, naproxen and paraaminobenzoic acid derivatives.

Enhances the anticoagulant activity of warfavin and anti-sarcoid phenytoin. Potentiates (trimethoprim) the effect of hypoglycemic drugs, derivatives of sulfonylureas.

Rifampicin reduces T₁_/2 trimethoprim.

Co-administration of Co-trimoxazole and cyclosporine after kidney surgery worsens the condition of patients.

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

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

Reduce the effect benzocaine, procaine, procainamide (and other drugs, as a result of hydrolysis towhich forms a PABC).

Between diuretics (thiazides, furosemide and others) and oral hypoglycemic drugs (sulfonylureas derivatives), on the one hand, and antimicrobial sulfonamides - with others, 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.

Ascorbic acid, hexamethylenetetramine (and other drugs that acidify urine) increase the risk of developing crystalluria.

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

Drugs that depress bone marrow hematopoies, increase the risk of myelosuppression.

Special instructions:

Excessive sunlight and UV irradiation should be avoided.

With caution appoint a drug with a deficiency of folic acid in the body, bronchial asthma, a burdened allergic anamnesis.

Form release / dosage:

Tablets 120 mg and 480 mg.

20 tablets in a jar of orange glass or in a jar of polymer type BP.

10 tablets in a contour non-cellular package of paper with a polymer coating or in a contour cell packaging of a polyvinylchloride film and aluminum foil.

Each jar or 1, 2, 3, 4, or 5 contour mesh packages together with instructions for the use of the drug are placed in a pack of cardboard.

100 contour packs with the application of 3-5 instructions for the use of the drug are placed in a box of cardboard (for hospitals).

Storage conditions:

List B. In a dry, protected from light and out of reach of children, at a temperature of no higher than 25 ° C.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N000908 / 01

Date of registration:13.04.2009

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Information update date: & nbsp13.04.2009

Illustrated instructions

Instructions

Co-trimoxazole (Co-trimoxazole)