Co-trimoxazole [Sulfamethoxazole + Trimethoprim] - instructions for use, dose, side effects, contraindications

Its structure is similar to paraminobenzoic acid, involved in the synthesis of folic acid, without which the growth of microorganisms stops. Competitively inhibits dihydropteroate synthetase, and also prevents the inclusion of para-aminobenzoic acid in dihydrophosphate. Violation of the synthesis of dihydrofolic acid reduces the formation of tetrahydrofolic acid from it, which is necessary for the synthesis of purine and pyrimidine bases. As a result, the synthesis of nucleic acids is suppressed, which leads to inhibition of growth and reproduction of microorganisms.

It does not break the structure of the cells of the macroorganism, since they already recycle the already prepared dihydrofolic acid.

Trimethoprim

Oppresses dihydrofolate reductase involved in the synthesis of tetrahydrofolic acid in microbial cells.

Co-trimoxazole

Effective against many pathogens resistant to one of its components.

Active with a number of Gram-positive (Staphylococcus spp., Streptococcus spp., Nocardia asteroides, Listeria monocytogenes) and Gram-negative (Enterobacteriaceae - Shigella spp., Haemophilus ducreyi, Klebsiella spp., Proteus spp., Yersinia spp.; some strains Bordetella pertussis, Brucella spp., H. influenzae, Legionella pneumophila, Salmonella spp., Enterobacter spp., some strains Escherichia coli, Vibrio cholerae, Citrobacter spp., Neisseria spp.) of microorganisms, and Moraxella catarrhalis, Pneumocystis carinii, Toxoplasma gondii, including those resistant to sulfonamides.

Pharmacokinetics:

After ingestion, up to 90% is absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 1.4 hours and remains for 7 hours. The connection with plasma proteins is 66% in sulfamethoxazole, in trimethoprim - 45%.

Metabolism in the liver to inactive metabolites.

Half-life sulfamethoxazole - 9-11 hours, trimethoprim - 10-12 hours. Elimination of the kidney form of metabolites for 72 hours.

Indications:

It is used to treat infections of the urogenital organs: pyelonephritis, pyelitis, cystitis, urethritis, epididymitis, prostatitis, gonorrhea, venereal granuloma, lymphogranuloma, inguinal granuloma; respiratory tract infections: acute and chronic bronchitis, bronchiectasis, croupous pneumonia, pneumocystis pneumonia; infections of the ENT organs: otitis media, laryngitis, sinusitis, scarlet fever, angina; infections of the gastrointestinal tract: typhoid fever, paratyphoid, cholera, salmonella, dysentery, cholera, gastroenteritis, shigellosis; osteomyelitis, toxoplasmosis, malaria, skin and soft tissue infections: pyoderma, acne, furunculosis, wound infections.

ICD-10

I.A00-A09.A00 Cholera

I.A00-A09.A01.0 Typhoid fever

I.A00-A09.A01.4 Paratyphus, unspecified

I.A00-A09.A09 Diarrhea and gastroenteritis of allegedly infectious origin

I.A50-A64.A54 Gonococcal infection

X.J00-J06.J06 Acute upper respiratory tract infections of multiple and unspecified sites

XIV.N10-N16.N15 Other tubulo-interstitial diseases of the kidneys

XIV.N30-N39.N39.0 Urinary tract infection without established localization

XIV.N40-N51.N41 Inflammatory diseases of the prostate

XIV.N70-N77.N74.3 * Gonococcal inflammatory diseases of female pelvic organs (A54.2 +)

XIX.T79.T79.3 Post-traumatic wound infection, not elsewhere classified

Contraindications:

Anemia, leukemia, hepatic and renal insufficiency, deficiency of glucose-6-phosphate dehydrogenase, porphyria, individual intolerance, neonatal period.

Carefully:

Deficiency of folic acid, bronchial asthma, thyroid disease, hypersensitivity.

Pregnancy and lactation:

Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Use in children

5-12 years: inside at the rate of 400/160 mg of sulfamethoxazole and trimethoprim 2 times a day.

Intravenously drip:

from 6 weeks to 5 months - 120 mg times per day;

from 6 months to 5 years - 240 mg times per day;

6-12 years - 480 mg 2 times per day.

Adults

Inside after eating 800/160 mg 2 times per day.

Intravenously drip: 800/160 mg 2 times per day, in severe cases - 1200 mg of sulfamethoxazole / 240 mg of trimethoprim 2-3 times a day for 3 days.

The highest daily dose: 1200 mg of sulfamethoxazole / 240 mg of trimethoprim.

The highest single dose: 800/160 mg.

Side effects:

Central and peripheral nervous system: headache, dizziness, aseptic meningitis, apathy, depression, peripheral neuritis, tremor.

Respiratory system: pulmonary infiltrates, bronchospasm.

Hemopoietic system: megaloblastic anemia, agranulocytosis, pancreatemia.

Digestive system: decreased appetite, nausea, vomiting, gastritis, diarrhea, stomatitis, glossitis, hepatonecrosis, pseudomembranous enterocolitis.

Musculoskeletal system: myalgia, arthralgia.

Dermatological reactions: photosensitivity, exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis.

Sense organs: hyperemia sclera.

Urinary system: polyuria, crystalluria, interstitial nephritis, toxic Nephropathy with oliguria and anuria.

Allergic reactions.

Overdose:

Headache, drowsiness, depression, fainting, confusion, visual impairment, fever, hematuria, crystalluria; with prolonged overdose - thrombocytopenia, leukopenia, megaloblastic anemia, jaundice.

Treatment: intramuscularly: 5-15 mg per day of calcium folinate (eliminates the effect of trimethoprim on the bone marrow), if necessary - hemodialysis.

Interaction:

Increases the activity of indirect anticoagulants, the effect of methotrexate and hypoglycemic agents.

Reduces the effectiveness of oral contraception, reducing the intestinal-hepatic circulation of hormonal drugs.

Thiazide diuretics increase the risk of thrombocytopenia.

Rifampicin shortens the elimination half-life.

Medicinal products, as a result of hydrolysis of which paraaminobenzoic acid is formed (procaine, benzocaine, procainamide) reduce the effect of co-trimoxazole.

Increase manifestations of folic acid deficiency: phenytoin, para-aminosalicylic acid, barbiturates.

Reduces absorption colestramine, it is recommended to take it 1 hour after or 5 hours before taking co-trimoxazole.

Increased risk of myelosuppression drugs that oppress bone marrow hematopoiesis.

Special instructions:

It is not recommended during the treatment to eat foods that contain paraminobenzoic acid in large quantities: green parts of plants (cauliflower, spinach, beans), carrots, tomatoes.

Excessive sunlight and ultraviolet radiation should be avoided.

In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

Instructions

Co-trimoxazole [Sulfamethoxazole + Trimethoprim] (Co-trimoxazolum [Sulfamethoxazolum + Trimethoprimum])