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: & nbsppills
    Composition:

    Active ingredient: phthalylsulfatiazole 0.5 g;

    Excipients: potato starch, calcium stearate, talc.

    Description:

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

    Pharmacotherapeutic group:Antimicrobial agent - sulfonamide
    ATX: & nbsp

    A.07.A.B.02   Phtalylsulfatiazole

    Pharmacodynamics:

    Phthalazole, like other sulfanilamide preparations, similar in structure to PABA (para-aminobenzoic acid), by the principle of competitive interrelation prevents its inclusion in the synthesis of folic acid of the microbial cell. 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 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 phthalazole with dihydrofolic acid synthetase, an enzyme that limits the formation of folic acid, is significantly weaker in comparison with PABA. Therefore, phthalazole must be administered at sufficiently high doses that prevent the use of microorganisms PABA contained in tissues. Otherwise, resistant strains of pathogens can be formed, which can not be further affected by sulfanilamide preparations.

    In addition to antibacterial, phthalazole, 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 cellular elements and partially stimulate the production of glucocorticosteroids.

    The spectrum of antimicrobial action of phthalazole, like other sulfonamides, is narrower than antibiotics. Sulfanilamides have a bacteriostatic effect on Streptococcus, Pneumococcus, Staphylococcus, Meningococcus, Gonococcus, Escherichia coli, Pseudomonas aeruginosa, Shigella dysenteriae, Proteus vulgaris and a number of large viruses - causative agents of trachoma and follicular conjunctivitis.

    Pharmacokinetics:

    When administered orally, the drug is slowly adsorbed from the digestive tract - (only 5% of the injected substance is found in the urine),resulting in a high concentration of it in the lumen of the colon, where, under the influence of microorganisms, the phthalazole molecule undergoes cleavage into phthalic acid, amino group and norsulfazole. The latter has a bacteriostatic effect on the causative agents of intestinal infections (bacillary dysentery, colitis, gastroenterocolitis). Acts mainly in the lumen of the intestine.

    Indications:Dysentery (acute and chronic at the stage of exacerbation), colitis, gastroenteritis, prevention of purulent complications in surgical interventions on the intestine.
    Contraindications:

    Increased individual sensitivity to sulfanilamide drugs, diseases of the blood system, diffuse toxic goiter, chronic renal failure, glomerulonephritis, acute hepatitis, intestinal obstruction.

    Dosing and Administration:

    Inside, with acute dysentery adults 1-2 days - 1 g 6 times a day, 3-4 days - 1 g 4 times a day, 5-6 days - 1 g 3 times a day. The average course 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 h), 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 light course - 18 g.Higher doses for adults: single dose - 2 g, daily -7 g.

    Children up to 3 let - 0.2 g / kg in 3 divided doses for 7 days, over 3 years old - 0.4-0.75 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 - 0.1 g / kg / day in equal doses after 4 hours with an overnight break, in the following days - 0.2-0.5 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, oral lesions (stomatitis, gingivitis, glossitis, etc.), gastritis, cholangitis, hepatitis, insufficiency of B vitamins (due to oppression of the intestinal microflora).

    From the urinary system: urolithiasis disease.

    From the respiratory system: eosinophilic pneumonia.

    From 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, incl. cutaneous manifestations of drug allergy in the form of a variety of rashes, up to nodular and multiforme exudative erythema, in some cases - epidermal necrolysis (Lyell's syndrome). In some cases, there is an allergic edema of the lips and face, nodular periarteritis.
    Interaction:

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

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

    - salicylates - increased activity and toxicity;

    - methotrexate and diphenin - toxicity is increased;

    - thioacetazone, levomycetin - the possibility of agranulocytosis increases;

    - nitrofurans - the risk of anemia and methemoglobinemia increases;

    - anticoagulants of indirect action - anticoagulant effect is increased;

    - Oxacillin - the activity of the antibiotic decreases.

    The combined use of phthalazole with acids and acid-binding drugs, hexamethylenetetramine, adrenaline solution is inadvisable, since they are chemically incompatible.

    With the combined use of phthalazole with preparations containing esters of para-aminobenzoic acid (novocaine, anesthesin, dicaine), the antibacterial activity of sulfanilamide is inactivated by a competitive mechanism.

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

    Form release / dosage:Tabletki, 0.5 g.
    Packaging:

    For 10 tablets in a contiguous cell-free or contiguous cell package.

    2 contour mesh packages along with the instruction for use are placed in a cardboard pack.

    Storage conditions:

    In a dry, dark place, out of the reach of children.

    Shelf life:

    4 years.

    Do not use after the expiration date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:P N003869 / 01
    Date of registration:10.12.2009 / 13.05.2014
    Expiration Date:Unlimited
    The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspDALHIMFARM, OJSCDALHIMFARM, OJSC
    Information update date: & nbsp09.01.2017
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