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

active substances: sulfamethoxazole (in terms of 100 % substance) - 100 mg or 4.00 mg and trimethoprim (in terms of 100% substance) - 20 mg or 80 mg;

Excipients: potato starch, magnesium stearate, crospovidone (kollidone CL-M), carboxymethyl starch sodium (sodium starch glycolate).

Description:Tablets white or white with a creamy shade of color, flat-cylindrical, with facetcoy. Tablets with a dosage of 480 mg have risk.

Pharmacotherapeutic group:antimicrobial agent combined.

ATX: & nbsp

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

Pharmacodynamics:

Co-trimoxazole is a combined antimicrobial drug consisting of sulfamethoxazole and trimethoprim in a 5: 1 ratio.

To-triamaxazole is a chemotherapeutic agent with a wide spectrum of bactericidal action caused by blocking the biosynthesis of folates in microbial cells.

Sulfamethoxazole disrupts the synthesis of dihydrofolic acid, and trimethoprim inhibits the conversion of dihydrofolic acid to tastrahydrofolic acid. Both components, thus, violate the process of the formation of folic acid, necessary for the synthesis by microorganisms of purine compounds, and then of nucleic acids (RNA and DNA). This breaks the formation of proteins and leads to the death of bacteria.

The activity of the drug is manifested in the following microorganisms: Staphylococcus aureus, Staphylococcus saprophyticus, Streptococcus pneumoniae, Streptococcus agalactiae, Streptococcus Viridans, and Pneumocystis carinii, Salmonella spp. (including Salmonella typhi and Salmonella paratyphi), Shigella spp., Klebsiella spp., Proteus mirabilis, Proteus vulgaris, Enterobacter spp., Serratia spp., Escherichia coli, Haemophilus influenzae, Morganella morganii, Yersinia spp., Brucella spp., Neisseria meningitidis, Neisseria gonorrhoeae, Vibrio cholerae, Bacillus anthracis, Listeria spp., Nocardia asteroides, Bordetella pertussis, Enterococcus faecalis, Pasteurella spp., Francisella tularensis, Mycobacterium spp. (incl. Mycobacterium leprae), Citrobacter spp., Enterobacter spp., Legionella pneumonia, Providencia spp., some species Pseudomonas spp. (Besides Ps. aeruginosa). Chlamydia spp. (incl. Chlamydia trachomatis, Chlamydia psittaci); protozoa: Plasmodium spp., Toxoplasma gondii, pathogenic fungi: Actinomyces israelii, Coccidioides immitis, Histoplasma bapsulatum, 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 B vitamins in the intestine.

Pharmacokinetics:

When taken orally, absorption is 90%. The maximum concentration in blood plasma is reached after 1 to 4 hours.

The drug is well distributed in the body. Penetrates through the blood-brain barrier, placental barrier and into breast milk. In the lungs and urine, concentrations exceeding the plasma content are created. To a lesser extent, it accumulates in the bronchial secretion, vaginal secretions, secretion and tissue of the prostate, fluid middle ear, cerebrospinal fluid, bile, bones, saliva, watery eyes, breast milk, interstitial fluid.

The connection with plasma proteins is 66% in sulfamethoxazole, in trimethoprim 45%. Sulfamethoxazole and trimethoprim are metabolized in liver.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. The half-life (T1/2) sulfamethoxazole - 9-11 h, trimethoprim - 10-12 h, in children - significantly less and depends on age: up to 1 year - 7-8 h, 1-10 years - 5 h. In the elderly and patients with impaired functions kidney T1/2 increases.

Indications:

Infectious-inflammatory diseases caused by sensitive to the preparation by microorganisms:

- respiratory tract infections: bronchitis (acute and chronic), bronchiectasis, croupous pneumonia, bronchopneumonia, pneumocystic pneumonia, pleural empyema, lung abscess;

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

- infections of the urino-genital organs: pyelonephritis, pyelitis, epididymitis, cystitis, urethritis, salpingitis, prostatitis, gonorrhea, chancroid, inguinal granuloma

- infections of the gastrointestinal tract: dysentery, cholera, typhoid fever, paratyphoid, salmonella, cholecystitis, cholangitis, gastrohenterites caused by enterotoxic strains E. coli;

- Skin and soft tissue infections: acne, furunculosis, pyoderma, abscesses and 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 to sulfonamides, trimethoprim and / or to other components of the preparation, pregnancy, lactation, children under 3 years, lack of glucose-6-phosphate dehydrogenase, liver and / or renal failure (creatinine clearance less than 15 mL / min), aplastic anemia , B-deficiency anemia, agranulocytosis, leukopenia, hyperbilirubinemia in children.

Carefully:With a deficiency of folic acid, bronchial asthma, diseases of the thyroid gland, renal failure (creatinine clearance 15 - 30 ml / min), advanced age.

Dosing and Administration:

Inside, squeezed with enough liquid. The dose is set individually, taking into account the severity of the infection and the sensitivity of the pathogen.

Adults and children over 12 years: Co-trimoxazole-Akri® 480mg tablets: 2 tablets twice daily (every 12 hours). In severe cases - 3 tablets 2 times a day. For chronic infections, the maintenance dose is 1 tablet 2 times a day. Children under 12 years of age are prescribed Co-trimoxazole-Acry® tablets 120 mg. The average daily dose is determined from the calculation of sulfamethoxazole 0.03 g and trimethoprim 0.006 g per 1 kg of body weight. Children aged from 3 to 6 years usually administered 2 tablets twice a day (after 12 hours), aged 6 to 12 years at 4 tablets twice a day (after 12 hours). Course treatment from 7 up to 14 days. With chronic infections - longer depending on the course of the disease. Patients with impaired renal function (QC 15-30 ml / min) are recommended to take 1/2 the usual dose.

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, anorexia, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of "liver" transaminases, hepatitis, gepatonekroz, pseudomembranous enterocolitis.

From the hematopoiesis: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, megaloblastic anemia, pancytopenia, polycythemia.

Wed side of 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, rash, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, allergic myocarditis, fever, angioedema, hyperemia sclera.

Other: hypoglycaemia, hyperkalemia (with the appointment of high doses), photosensitization, ringing in the ears (rarely).

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: withdrawal of the drug, gastric lavage (no later than 2 hours after taking an excessive dose), acidification of urine increases the excretion of trimethoprim, abundant drink, intramuscularly - 5-15 mg / day of calcium folinate (eliminates the action of trimethoprim on the bone marrow), forced diuresis, with necessity - hemodialysis.

Interaction:

The drug is not recommended to be taken simultaneously with thiazide diuretics because of the risk of developing thrombocytopenia (bleeding).

The drug increases the anticoagulant activity of indirect anticoagulants, enhances the effect of hypoglycemic agents and methotrexate.

Co-trimoxazole reduces the intensity of hepatic metabolism of phenytoin (prolongs its T1/2 by 39%) and warfarin, enhancing their effect.

Co-trimoxazole 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.

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

When co-trimoxazole is used together with indomethacin, the level of sulfamethoxazole in the blood increases.

Simultaneous reception of co-trimoxazole with procainamide, amantadine promotes an increase in the concentrations in the blood plasma of these substances and trimethoprim.

Benzocaine, procaine and other drugs, as a result of hydrolysis of which paraaminobenzoic acid is formed, reduce the effect of the drug.

Between diuretics (thiazides, furosemide and others) and oral hypoglycemic drugs (sulfonylurea derivatives), on the one hand, and antimicrobial sulfonamides, on the other hand, it is possible to develop a cross-ala lethal reaction.

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

The derivatives of salicylic acid enhance the action of co-trimoxazole.

With the combined use of trimethoprim and digoxin in elderly people, an increase in the concentration of digoxin in the blood plasma can be observed.

With the simultaneous administration of co-trimoxazole and zidovudine may increase the risk of hematological disorders.

The effectiveness of tricyclic antidepressants in combination with co-trimoxazole can be reduced.

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.

The combined use of co-trimoxazole and cyclosporin increases the level of plasma creatinine in patients who underwent kidney transplantation.

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.

Special caution should be shown in the treatment of patients with a suspected initial lack of folate. The purpose of folic acid is also suitable for long-term treatment in high doses.

The appearance of a skin rash or diarrhea of severe course is an indication for the withdrawal of the drug.

For the prevention of crystalluria it is recommended to maintain a sufficient volume of excreted urine.

The likelihood of developing side effects of sulfonamides significantly increases with a decrease in the filtration function of the kidneys.

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

Excessive sunlight and ultraviolet radiation should be avoided. Co-trimoxazole can disrupt the creatinine detection reaction using the alkaline porphinate of Jaffe (increases the creatinine level by 10%).

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

It is not recommended for use in tonsillitis and pharyngitis caused by beta-hemolytic streptococcus group A, because of the widespread resistancestrains.

Y | patients with renal failure, a violation of potassium metabolism and / or combined intake of drugs that lead to the development of hyperkalemia, it is necessary to monitor the level of potassium in the blood plasma.

Form release / dosage:

Tablets 120 mg and 480 mg.

For 10 or 20 tablets in a planar cell pack.

1 or 2 contour mesh packages together with instructions for use in a pack of cardboard.

Storage conditions:In a dry, the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

4 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:P N000681 / 02

Date of registration:03.12.2009

The owner of the registration certificate:AKRIKHIN HFK, JSC AKRIKHIN HFK, JSC Russia

Manufacturer: & nbsp

AKRIKHIN HFK, JSC Russia

Information update date: & nbsp30.10.2014

Illustrated instructions

Instructions

Co-trimoxazole-Acry (Co-trimoxazole-Akri)