Active substanceCo-trimoxazole [Sulfamethoxazole + Trimethoprim]Co-trimoxazole [Sulfamethoxazole + Trimethoprim]
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  • Dosage form: & nbsppills
    Composition:Composition per one tablet:
    active substances: sulfamethoxazole- 400 mg, trimethoprim - 80 mg;
    Excipients: starch carToffee - 98 mg, povidone (polyvinyl alcoholpyrrolidone, povidone K-17) - 5.5 mg, croscarmellose sodium - 12.0 mg, calcium stearate-4.5 mg.
    Description:Tablets are white with a creamy shade of color flat-cylindrical.Marble is allowed on the surface of the tablets.
    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 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. It accumulates to a lesser degree 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%.

    Both components are metabolized with the formation of acetylated 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; 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 sulfonamide), liver and / or renal failure (creatinine clearance - less than 15 ml / min), aplastic anemia, B 12 deficiency anemia, agranulocytosis, leukopenia, deficiency of glucose-6-phosphate dehydrogenase, pregnancy, lactation period, children under 12 years (for this dosage form), hyperbilirubinemia in children.
    Carefully:

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

    Pregnancy and lactation:Due that the safety of co-trimoxazole in pregnant women has not been established, the use of the drug during pregnancy is contraindicated.
    It is known that trimethoprim and sulfamethoxazole penetrate into breast milk, soIf you need to use the drug during lactation, you should decide whether to quit breastfeeding.
    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.

    Adults and children over 12 years of age - 960 mg once or 480 mg twice a day. In severe infections - 480 mg 3 times a day, with chronic infections, a maintenance dose of 480 mg 2 times a day.

    In uncomplicated infections appoint: over 12 years and adults 1 tablet 2 times a day.

    Duration of treatment from 5 to 14 days. In severe and / or chronic forms of infectious diseases, an increase in the single dose by 30-50% is permissible.

    The drug is taken during or after a meal. It is recommended to drink with alkaline drink (milk, mineral water).
    Side effects:

    From the nervous system: headache, dizziness, vertigo, convulsions, ataxia, paresthesia, ringing in the ears, uveitis, hallucinations, nervousness; aseptic meningitis, depression, apathy, tremor, peripheral neuritis.

    From the respiratory system: bronchospasm, pulmonary infiltrates: eosinophilic infiltrate, allergic alveolitis (cough, dyspnea).

    From the digestive system: nausea, vomiting, decreased appetite, diarrhea, gastritis, abdominal pain, glossitis, stomatitis, cholestasis, increased activity of "liver" transaminases, hepatitis incl.cholestatic, gepatonekroz, pseudomembranous colitis, "disappearing bile duct" syndrome (duktopeniya), hyperbilirubinemia, acute pancreatitis.

    From the hematopoiesis: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, anemia (megaloblastic, hemolytic / or autoimmune aplastic), methemoglobinemia, eosinophilia, hypoprothrombinemia.

    From the urinary system: polyuria, interstitial nephritis, impaired renal function, crystalluria, hematuria, increased urea concentration, hyperkreatinemia, toxic Nephropathy with oliguria and anuria.

    From the side of the locomotoriumRata: arthralgia, myalgia, rhabdomyolysis.

    Allergic reactions: itch, photosensitistion of rash, erythema multiforme (including Stivena- Johnson syndrome),toxic epidermal necrolysis (Lyell's syndrome), exfoliative dermatitis, allergic myocarditis, fever, angioedema, hyperemia sclera, urticaria, conjunctival hyperemia, anaphylactic / anaphylactoid reaction, serum sickness, hemorrhagic vasculitis (Henoch-Schonlein purpura), periarteritis nodosa, lupus-like syndrome, drug rash with eosinophilia and systemic symptoms (DRESS-syndrome).

    Other: hypoglycaemia, hyperkalemia (mainly in patients with AIDS in the treatment of pneumocystis pneumonia), hyponatremia, weakness, fatigue, insomnia, candidiasis.

    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:

    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.

    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 decreasefiltration function of the kidneys. Excessive sunlight and UV irradiation should be avoided.

    Effect on the ability to drive transp. cf. and fur:During treatment should be observed caution when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed psychomotor reactions. One should take into account the potential for the development of side effects from the nervous system, such as dizziness, vertigo, convulsions, hallucinations. If these side effects appear, you should refrain from performing these activities.
    Form release / dosage:

    Tablets 480 mg. 10 tablets in a planar cell package.

    1 or 2 packs with instructions for use in a pack of cardboard.

    Storage conditions:Store at a temperature not exceeding 25 ° C.
    Keep out of the reach of children.
    Shelf life:3 years. Do not use after the expiration date on the package.
    Terms of leave from pharmacies:On prescription
    Registration number:P N000700 / 01
    Date of registration:27.12.2007
    The owner of the registration certificate:PHARMSTANDART-FORESTRY, OJSC PHARMSTANDART-FORESTRY, OJSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp01.12.2014
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