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 (phthalazole)

    500 mg

    Excipients:

    Lactose monohydrate (milk sugar)

    16.2 mg

    Calcium stearate monohydrate

    6 mg

    Potato starch

    77.8 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 sulfonamide preparations similar in structure to para-aminobenzoic acid, prevents the inclusion of it in the synthesis 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 there are reserves of para-amino-benzoic acid in the microbial cell.In addition, the degree of affinity of phthalazole with synthetase dihydrofolic acid, an enzyme that limits the formation of folic acid, is considerably weaker in comparison with para-aminobenzoic acid. Therefore, phthalazole must be administered at sufficiently high doses that prevent the use of parahaminobenzoic acid contained in the tissues by microorganisms. 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 exert bacteriostatic action on Streptococcus spp. (including Streptococcus pneumoniae), Staphylococcus spp :, Neisseria meningitidis, Neisseria gonorrhoeae; Escherichia coli, Pseudomonas aeruginosa, Shigella dysenteriae, Proteus vulgaris and a number of large viruses - causative agents of trachoma and follicular conjunctivitis.

    Pharmacokinetics:

    When ingested, 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 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:

    Shigellosis (acute and chronic forms in the stage of exacerbation), colitis, gastroenteritis, prevention of purulent complications in surgical interventions on the intestine.

    Contraindications:Increased individual sensitivity to sulfanilamide drugs, blood system diseases, hyperthyroidism, chronic renal failure, glomerulonephritis, acute hepatitis, intestinal obstruction, children under 3 years of age (for this dosage form), lactase deficiency, lactose intolerance, glucose-galactose malabsorption .
    Carefully:

    Use nephrite with caution.

    Pregnancy and lactation:

    The drug easily penetrates the placenta, into breast milk. Therefore, the use of the drug during pregnancy and lactation is possible only if the expected benefit for the mother exceeds the potential risk to the fetus.

    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, 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 carried out: 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 light course - 18 g.

    Higher doses for adults: single dose - 2 g, daily 7 g.

    Children over 3 years old - 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 - 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, oral lesions (stomatitis, gingivitis, glossitis and others), 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 side of the cardiovascular system: myocarditis, cyanosis.

    On the part of the blood system: in rare cases - leukopenia, thrombocytopenia, agranulocytosis, hemolysis of erythrocytes, aplastic, anemia. 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 various 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.

    If any of the side effects indicated in the manual are aggravated, or any other side effects not indicated in the instructions are noted, you should inform the doctor immediately.

    Overdose:

    Overdose phenomena are not described.

    Treatment: drug cancellation, gastric lavage with 2% sodium hydrogen carbonate solution and activated carbon suspension; abundant drink of 2% sodium bicarbonate solution, forced diuresis, hemodialysis.

    Interaction:

    When combined with other drugs, the following interactions can occur:

    - paraaminosalicylic acid and barbiturates, the activity of sulfonamides is enhanced;

    - salicylates - the activity and toxicity increase;

    - methotrexate and diphenyl - 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 drug decreases.

    Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

    Co-administration with acids and acid-binding agents, hexamethylenetetramine, epinephrine solution is impractical, since they are chemically incompatible.

    When used with preparations containing esters of para-aminobenzoic acid (epinephrine, procaine, benzocaine, tetracaine), the antibacterial activity of sulfanilamide is inactivated by a competitive mechanism.

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

    Special instructions:

    If necessary, it is possible to use simultaneously with sulfonamides or bacteriostatic antibiotics.

    Effect on the ability to drive transp. cf. and fur:

    Care should be taken when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions.

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

    10 tablets in a contour non-jawed package of paper with a polymer coating.

    10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil or paper with polyethylene coating.

    10 tablets in cans of orange glass of BTS type, sealed with plastic pull-on lids with sealing element or in polymeric banks of BP type.

    Each jar or 1 circuit pack with instructions for use is placed in a pack of cardboard.

    100 contour packs with an equal number of instructions for use are placed in a group box - a box 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 the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-002126
    Date of registration:18.07.2011
    Expiration Date:Unlimited
    The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia
    Manufacturer: & nbsp
    Representation: & nbspBIOSINTEZ JSC BIOSINTEZ JSC Russia
    Information update date: & nbsp08.01.2017
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