Active substancePhtalylsulfatiazolePhtalylsulfatiazole
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  • Phthalazole
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    BIOSINTEZ, PAO     Russia
  • Phthalazole
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  • Phthalazole
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    AVEKSIMA, JSC     Russia
  • Phthalazole
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    DALHIMFARM, OJSC     Russia
  • Phthalazole tablets 0.5 g
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  • Dosage form: & nbsptabscesses
    Composition:For one tablet:

    Active substance: phthalylsulfatiazole - 500 mg;

    Excipients: starch potato - 80 mg, talc -15 mg, calcium stearate - 5 mg.

    Description:

    Tablets are white or white with a slightly yellowish hue of color, flat-cylindrical, with a risk and a facet.

    Pharmacotherapeutic group:Antimicrobial agent - sulfonamide
    ATX: & nbsp

    A.07.A.B.02   Phtalylsulfatiazole

    Pharmacodynamics:

    Phthalazole, like other sulfanilamide preparations, similar in structure to para-aminobenzoic acid (PABA), by the principle of competitive relationships prevents its inclusion in the synthesis of folic acid microbial cells. This leads to a violation of the formation of folic acid, involved in the synthesis of purine and pyrimidine bases, on which the growth and development of microorganisms depends.

    The most pronounced bacteriostatic effect of phthalazole is on the vegetative forms of microbes.This effect develops gradually, since in the microbial cell there are some stocks of PABC. In addition, the degree of affinity of Ftalazol with dihydrophosphate acid synthetase - an enzyme limiting the formation of folic acid, in comparison with PABA is much weaker. Therefore, phthalazole must be administered at sufficiently high doses that prevent the use of microorganisms PABA contained in the tissues. Otherwise, resistant strains of pathogens can be formed, which can not be further affected by sulfanilamide preparations.

    In addition to antibacterial, Ftalazol, like other sulfonamide preparations, has an anti-inflammatory effect that is associated with its ability to limit the migration of leukocytes, reduce the total number of migrating cell elements and partially stimulate the production of glucocorticosteroids.

    The drug acts predominantly in the lumen of the intestine.

    The spectrum of antimicrobial action of Ftalazol, like that of other sulfonamides, is narrower than that of antibiotics. Sulfanilamides have a bacteriostatic effect on Streptococcus spp., Pneumococcus spp., Staphylococcus spp.; Meningococcus spp.; Gonococcus, Escherichia coli, Pseudomonas aeruginosa, Shigella dysenteriae, Proteus vulgaris.

    Pharmacokinetics:

    When ingested, the drug is slowly absorbed from the digestive tract - (only 5% of the injected substance is found in the urine), resulting in a high concentration in the lumen of the colon, where, under the influence of microorganisms, the phthalylsulfatiazole molecule undergoes cleavage into phthalic acid, amino group and norsulfazole.

    Indications:

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

    - dysentery (acute and chronic in the stage of exacerbation);

    - colitis;

    - gastroenteritis;

    - prevention of purulent complications in surgical interventions on the intestine.
    Contraindications:

    Increased individual sensitivity to sulfanilamide preparations and components of the drug, disease of the blood system, diffuse toxic goiter, chronic renal failure, glomerulonephritis, acute hepatitis, intestinal obstruction, children under 5 years.

    Dosing and Administration:

    Inside.

    With acute dysentery adults in 1-2 days - 1 g 6 times a day, 3-4 days - 1 g 4 times a day, for 5-6 days - 1 g 3 times a day. The average exchange dose is 25-30 g.

    After 5-6 days, the second course of treatment is done: 1-2 days - 1 g 5 times a day (in the daytime - every 4 hours, at night - after 8 hours), 3-4 days - 1 g 4 times a day ( at night do not give), 5 day - 1 g 3 times a day. The total dose in the second cycle is 21 g, with a mild course - 18 g. Higher doses for adults: single dose - 2 g, daily - 7 g.

    Children over 5 years - 0,5-0,75 g 4 times a day.

    With other infections adults in the first 2-3 days, appoint 1-2 g every 4-6 hours, in the next 2-3 days - half the dose; children over 5 years - 0.1 g / kg / day in equal doses after 4 hours with an overnight break, in the following days - 0.25-0.5 g every 6-8 hours.

    Side effects:

    From the central nervous system: headache, dizziness, depressed mood.

    From the gastrointestinal tract, liver, pancreas: nausea, vomiting, diarrhea, lesions of the oral mucosa (stomatitis, gingivitis, glossitis), gastritis, cholangitis, hepatitis, insufficiency of B vitamins (due to oppression of the intestinal microflora).

    From the urinary system: formation of concrements.

    From the respiratory system: eosinophilic pneumonia.

    From the side of the cardiovascular system: myocarditis, cyanosis.

    On the part of the blood system: in rare cases - leukopenia, thrombocytopenia, agranulocytosis, hemolysis of erythrocytes. With prolonged use, anemia may occur due to a deficiency of pantothenic and pteroylglutaric acids produced by microbial cells.

    Allergic and toxic-allergic reactions: drug allergy, including, skin manifestations of drug allergy in the form of a variety of rashes, up to nodular and multi-form exudative erythema, in some cases - toxic epidermal necrolysis (Lyell's syndrome). In some cases, there is an allergic edema of the lips and face, nodular periarteritis.

    Interaction:

    When using Ftalazol together with other drugs, the following interactions can be observed:

    - paraaminosalicylic acid (PASK) and barbiturates - the activity of sulfonamides is increased;

    - salicylates - the activity and toxicity of salicylates is increased;

    - methotrexate and diphenin - the toxicity of methotrexate and diphenin is increasing;

    - thioacetazone, levomycetin - the possibility of agranulocytosis increases;

    - nitrofurans - the risk of anemia and methemoglobinemia caused by nitrofurans increases;

    - anticoagulants of indirect action - the effect of the anticoagulants of indirect action is increased;

    - Oxacillin - decreases the activity of oxacillin.

    There is a chemical incompatibility in the joint use of Ftalazol with acids and acid-binding drugs, hexamethylenetetramine, epinephrine solution.

    When combined with Ftalazol with preparations containing PABA esters (procaine, benzocaine, tetracaine), the antibacterial activity of sulfanilamide is inactivated by a competitive mechanism.

    The effect of the action is enhanced by antibiotics and well-absorbed sulfonamides.

    Form release / dosage:Tablets, 500 mg.
    Packaging:

    For 10 tablets in a contour non-jellied package or in a contour mesh package.

    2 contour packs with instructions for use are placed in a pack of cardboard.

    For 600 contour non-jammed packages with instructions for use are placed in a cardboard box.

    Storage conditions:

    In a dry place protected from light.

    Keep out of the reach of children.

    Shelf life:

    4 years.

    After expiration date the drug should not be used.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-001247/10
    Date of registration:19.02.2010 / 13.08.2013
    Expiration Date:Unlimited
    The owner of the registration certificate:AVEKSIMA, JSC AVEKSIMA, JSC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp08.01.2017
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