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

Auxiliary substances: methylparahydroxybenzoate (nipagin), propyl parahydroxybenzoate (nipazole), aspartame, acesulfame potassium (sunette), sorbitol (sorbitol), microcrystalline cellulose (avicel), glycerol (glycerin), xanthan gum (xanthan gum),cherry flavoring ("Cherry" flavor), red dyed dye, water (purified water) - up to 100 ml.

Description:Suspension light pink color, with a characteristic fruity odor, bubbles are allowed.

Pharmacotherapeutic group:antimicrobial combination

ATX: & nbsp

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

Pharmacodynamics:

Combined antimicrobial preparation, consisting ofsulfamethoxazole and trimethoprim. Sulfamethoxazole, similar in structure to para-aminobenzoic acid, disrupts the synthesis of dihydrofolic acid in bacterial cells, preventing the inclusion of para-aminobenzoic acid in 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 activity of E. coli, which leads to a decrease in the synthesis of thiamine, riboflavin, nicotinic acid and other vitamins of group B in the intestine. The duration of the therapeutic effect is 7 hours.

Pharmacokinetics:

When taken orally, absorption is 90%. Time to reach the maximum concentration of the drug in the plasma - 1-4 hours, the therapeutic level of concentration is 7 hours after a single dose. Well distributed in the body. Penetrates through the blood-brain barrier, 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 the bronchial secretion, vaginal secretions,secretion and tissue of the prostate, middle ear fluid (with its inflammation), cerebrospinal fluid, bile, bones, saliva, watery eyes, breastmilk, interstitial fluid. The connection with plasma proteins is 66% in sulfamethoxazole, in trimethoprim 45%.

Both components are metabolized with the formation of acetilated derivatives, sulfamethoxazole to a greater extent. Metabolites do not have antimicrobial activity.

It is excreted by the kidneys in the form of metabolites (80% within 72 hours) and unchanged (20% sulfamethoxazole, 50% trimethoprim); a small amount - through the intestine. The half-life of the drug sulfamethoxazole is 9-11 h, trimethoprim is 10-12 h, in children it is much less and depends on the age: up to 1 year - 7-8 h, 1-10 years - 5-6 h. In the elderly and patients with a violation of kidney function, the half-life of the drug is increased.

Indications:

- Urinary tract infections: urethritis, cystitis, pyelitis, pyelonephritis, prostatitis, epididymitis, gonorrhea, chancroid, venereal lymphogranuloma, inguinal granuloma;

- infections of the respiratory tract: bronchitis (acute and chronic), bronchoectatic disease, croupous pneumonia, bronchopneumonia, pneumocystis pneumonia;

- infection of ENT organs: otitis media, sinusitis, laryngitis, tonsillitis; scarlet fever; infections of the gastrointestinal tract: typhoid fever, paratyphoid, salmonelo-carrying, 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 sulfonamides), hepatic and / or renal insufficiency (creatinine clearance less than 15 ml / min), aplastic anemia, B 12-deficiency anemia, agranulocytosis, leukopenia, glucose-6-phosphate dehydrogenase deficiency, pregnancy, period lactation, children's age (up to 3 months), hyperbilirubinemia in children.

Carefully:

Deficiency of folic acid, bronchial asthma, thyroid gland diseases.

Dosing and Administration:

The dosage regimen is individual, depending on the severity of the disease, the sensitivity and type of pathogen, the age of the patient.At uncomplicated infections appoint:

from 3 months to 6 months of 2.5 ml suspension 2 times a day;

from 6 months to 6 years, 2.5 - 5 ml of suspension 2 times a day;

from 6 to 12 years for 5-10 ml of suspension 2 times a day;

over 12 years of age and adults 10-20 ml of suspension 2 times a day

Duration of treatment from 5 to 14 days.

The drug is taken during or after a meal. In the process of treatment, a plentiful drink is recommended.

In case of prolongation of the course of treatment for more than 5 days and / or increasing the dose, hematological control should be performed; in case of a change in the blood picture, folic acid should be prescribed at 5-10 mg per 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, megaloblastic anemia.

On the part of the urinary system: polyuria, interstitial nephritis, impaired renal function, crystalluria, hematuria,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, / m - 5-15 mg / day of calcium folinate (eliminates the effect of trimethoprim on the bone marrow), if necessary - hemodialysis.

Interaction: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 / week, increases the risk of megaloblastic anemia. Diuretics (often thiazides) increase the risk of thrombocytopenia. Reduce the effect benzocaine, procaine, procainamide (and other drugs, as a result of the hydrolysis of which paraaminobenzoic acid is formed). Between diuretics (thiazides, furosemide and others) and oral hypoglycemic drugs (sulfonylurea derivatives), on the one hand, and antimicrobial sulfonamides - with others, it is possible to develop a cross-allergic reaction. Phenytoin, barbiturates, para-aminobenzoic acid increase manifestations of folate deficiency.The derivatives of salicylic acid intensify the action. Ascorbic acid, hexamethylenetetramine (and other medicines, acidifying urine) increase the risk of developing crystalluria. Kolestyramine reduces absorption, so it should be taken 1 hour after or 4-6 hours before taking co-trimoxazole. Drugs that inhibit bone marrow hematopoies increase the risk of myelosuppression.

Special instructions:

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 / day), which does not significantly violate 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. Excessive sunlight and UV irradiation should be avoided.

Form release / dosage:

Suspension for ingestion of 240 mg / 5ml in bottles of dark glass for 50, 100 and 125 g. Each vial with instructions for use and a measuring spoon is placed in a pack of cardboard.

Storage conditions:

Store at a temperature not exceeding 15 ° C. Keep out of the reach of children.

Shelf life:

2 years. After the expiration date the drug should not be used.

Terms of leave from pharmacies:On prescription

Registration number:P N000700 / 02

Date of registration:09.11.2007

The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia

Manufacturer: & nbsp

PHARMSTANDART-FORESTRY, OJSC Russia

Information update date: & nbsp29.12.2011

Illustrated instructions

Instructions

Co-trimoxazole (Co-trimoxazol)