Active substanceNimesulideNimesulide
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  • Dosage form: & nbsppills
    Composition:

    Each tablet contains:

    Active substance: nimesulide - 100.0 mg.

    Excipients: lactose monohydrate (sugar milk) - 115.0 mg; sodium carboxymethyl starch - 28.0 mg; Povidone (polyvinylpyrrolidone) 16.0 mg; magnesium stearate - 3.2 mg; cellulose microcrystalline - 52.2 mg, silicon dioxide colloid - 2.0 mg; water 3.6 mg.

    Description:cylindrical biconvex tablets of light yellow color.
    Pharmacotherapeutic group:nonsteroidal anti-inflammatory drug (NSAID).
    ATX: & nbsp

    M.01.A.X   Other non-steroidal anti-inflammatory drugs

    M.01.A.X.17   Nimesulide

    Pharmacodynamics:

    Nimesulide is a drug from the group of non-steroidal anti-inflammatory drugs. Has anti-inflammatory, analgesic and antipyretic effect. Like most NSAIDs, nimesulide shows its pharmacological action, suppressing the synthesis of prostaglandins. In contrast to classical NSAIDs, it acts in the inflammation zone and suppresses predominantly cyclooxygenase type 2 (COX 2) and a weaker COX 1, inhibiting the formation of pathogenic pro-inflammatory prostaglandins. Nimesulide blocks the release of histamine from mast cells;

    Suppresses the synthesis of elastase, metalloprotease and collagenase, protecting cartilage tissue from damage. Suppressing the release of tumor necrosis factor alpha (TNF-a), nimesulide reduces the action of kinins.

    Pharmacokinetics:

    Nimesulide is rapidly and almost completely absorbed from the gastrointestinal tract. Eating lowers the absorption rate without affecting its degree. After taking 1 tablet, 100 mg maximum concentration (Cmax) in blood plasma (about 4 μg / ml) is achieved within 2-3 hours. The dose does not affect the degree of binding. The connection with plasma proteins is more than 95%. The volume of distribution is between 0.18 and 0.39 l / kg. After oral administration, it penetrates the synovial membrane and reaches a concentration in the periarticular fluid exceeding that in the plasma, ranging from 3 to 12 hours.

    After taking 1 tablet (100 mg), the concentration of nimesulide in female reproductive organs reaches 35-50% of its plasma concentration. Binding to plasma proteins is reduced in patients with renal and hepatic insufficiency.

    Nimesulide is metabolized in the liver by tissue monooxygenases, almost completely metabolized to the active metabolite (4-hydroxynimidesulide).

    The half-life (T1/2) nimesulide is 2-5 hours, and the active metabolite is 3-6 hours.

    It is excreted by the kidneys in the form of a free or conjugated metabolite (50-71%) and bile (21-29%).

    Indications:

    For symptomatic therapy, reducing the intensity of pain and inflammation at the time of use (for the progression of the disease is not affected):

    rheumatoid arthritis;

    articular cider with exacerbation of gout;

    psoriatic arthritis;

    ankylosing spondylitis;

    osteochondrosis with radicular syndrome;

    osteoarthritis;

    myalgia of rheumatic and non-rheumatic origin;

    inflammation of ligaments, tendons, bursitis (including gystraumatic inflammation of soft tissues);

    pain syndrome of various genesis (including in the postoperative period, with trauma,

    Algodismenorea, toothache, headache, arthralgia, lumboschialgia).
    Contraindications:

    Hypersensitivity, complete or incomplete combination of bronchial asthma, recurrent polyposis of the nasal mucosa or paranasal sinuses.

    Intolerance to acetylsalicylic acid and other NSAIDs (including in history). Erosive-ulcerative lesions of the mucous membrane of the stomach and duodenum, active gastrointestinal bleeding, cerebrovascular or other bleeding, inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the phase of exacerbation.

    Hemophilia and other disorders of blood coagulability, decompensated chronic heart failure (CHF).

    Hepatic insufficiency or any active liver disease, hepatotoxic reactions when using nimesulide in anamnesis, alcoholism, drug addiction, simultaneous intake of other hepatotoxic drugs.

    Severe chronic renal failure (CRF) (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia.

    The period after the aortocoronary shunting, pregnancy, the period of breast sucking, children under 12 years.

    Lactose intolerance, lactase deficiency or glucose-galactose malabsorption.

    Carefully:

    Ischemic heart disease (IHD), cerebrovascular disease, chronic heart failure (CHF), peripheral arterial disease. Dyslipidemia / hyperlipidemia, anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of infection Helicobacter pylori. Long-term use of NSAIDs, simultaneous administration of anticoagulants (incl. warfarin), antiplatelet agents (incl. acetylsalicylic acid, clopidogrel), oral glucocorticoids, selective serotonin reuptake inhibitors (incl. citalopram, fluoxetine, paroxetine, sertraline).

    Renal failure (KK 30-60 ml / min), diabetes mellitus, severe somatic diseases, old age, smoking.

    Pregnancy and lactation:

    Pregnant

    Nimesulide is contraindicated during pregnancy (risk of atony of the uterus and premature closure of the arterial duct in the fetus).

    Breast-feeding

    Nimesulide excreted in breast milk. If it is necessary to treat the drug, breastfeeding should be discontinued.

    Dosing and Administration:

    Adults and children over 12 years of age, with sufficient water, preferably after a meal. A minimum effective dose should be used with the minimum possible short course. Adults take 1 tablet 2 times a day. In the presence of diseases of the gastrointestinal tract, the drug should be taken at the end of the meal or after eating. The maximum daily intake for adults is 200 mg. Patients with chronic renal failure require a reduction in the daily dose to 100 mg.

    Side effects:

    The incidence of side effects is distributed as follows: often - 1-10%; infrequently - 0.1-1%; rarely - 0.01-0.1%; very rarely - less than 0.001%, including individual cases.

    From the central nervous system: infrequently - dizziness; rarely - fear, nervousness, "nightmarish" dreams; very rarely - headache, drowsiness, Reye's syndrome.

    From the cardiovascular system: infrequently - lowering blood pressure; rarely - tachycardia, "hot flashes" of blood to the skin of the face and upper half of the trunk.

    From the genitourinary system: infrequently - swelling; rarely - dysuria, hematuria, urinary retention; very rarely - renal failure, oliguria, interstitial nephritis.

    From the digestive system: often - diarrhea, nausea, vomiting, increased activity of "liver" transaminases; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stool, bleeding from the gastrointestinal tract, ulcer and / or perforation of the stomach or duodenum, hepatitis, incl. fulminant, jaundice, cholestasis.

    From the skin: infrequently - itching, rash, increased sweating; rarely - erythema, dermatitis; very rarely - urticaria, angioedema, swelling of the face, multiforme exudative erythema, incl. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome).

    From the hematopoiesis: rarely - anemia, eosinophilia; very rarely - thrombocytopenia, pancytopenia, purpura, hemorrhages, lengthening bleeding time. From the respiratory system: infrequently - shortness of breath; very rarely - exacerbation of previous bronchial asthma, bronchospasm.

    From the sense organs: rarely - blurred vision.

    Allergic reactions: rarely - hypersensitivity reactions; rarely - anaphylactoid reactions.

    Other: infrequently hyperkalemia; rarely - general weakness; very rarely - hypothermia.
    Overdose:

    Symptoms: apathy, drowsiness, nausea, vomiting, bleeding from the gastrointestinal tract, increased blood pressure, acute renal failure, oppression respiration.

    Treatment: symptomatic and supportive therapy. There is no specific antidote. In the first 4 hours after an overdose, it is recommended: cause vomiting, take Activated charcoal (1 g / kg body weight). Forced diuresis, hemodialysis is ineffective.

    Interaction:

    Salicylates or other NSAIDs - It is not recommended simultaneous use with nimesulide because of the increased risk of ulceration of the gastrointestinal tract. Nimesulide displaces salicylic acid when it binds to plasma proteins.

    Oral anticoagulants - there is a higher risk of hemorrhage with simultaneous treatment with nimesulide and acenocoumarol. In the first days of treatment, prothrombin time control is necessary.

    Methotrexate - with simultaneous application nimesulide may increase the possibility of side effects.

    Heparin (parenteral) - increased risk of hemorrhage.

    Lithium - with simultaneous application nimesulide increases the concentration of lithium in blood plasma. The risk of side effects due to lithium toxicity is increasing.

    Furosemide and thiazide diuretics - NSAIDs lower natriuretic effect. With simultaneous treatment with nimesulide and furosemide, it is necessary to monitor the water-salt balance and the diuretic action of furosemide.

    ACE Inhibitors - NSAIDs reduce the antihypertensive effect. If necessary, combined treatment, this interaction should be taken into account. Ticlopidine - increased risk of hemorrhages due to synergistic antiplatelet effect.

    Beta-blockers - with simultaneous application with nimesulide, their antihypertensive effect decreases.

    Cyclosporin - There is a high risk of increased nephrotoxic action with simultaneous use with nimesulide, especially in elderly patients.

    Special instructions:

    Every 2 weeks, the functional tests of the liver should be monitored. If there are signs of liver damage (pruritus, jaundice, nausea, vomiting, abdominal pain, darkening of urine, increased activity of "liver" transaminases), stop taking the drug immediately and consult a doctor.Given reports of visual impairment in patients taking other NSAIDs, if any visual impairment occurs, treatment should be immediately discontinued and an ophthalmological examination performed. The drug may cause fluid retention, so patients with high blood pressure and heart disease nimesulide should be used with extreme caution. Patients should undergo regular medical supervision if they take medications along with nimesulide, which are characterized by an effect on the gastrointestinal tract. Do not use the drug simultaneously with other NSAIDs. Nimesulide can reduce platelet aggregation, but it does not replace the preventive effect of antiplatelet agents (incl. acetylsalicylic acid, clopidogrel, ticlopidine) in cardiovascular diseases. The use of the drug may adversely affect female fertility and is not recommended for women planning pregnancy.

    Effect on the ability to drive transp. cf. and fur:During the period of taking the drug, care must be taken when driving vehicles and occupying othersActivities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:

    Tablets of 100 mg.

    For 10, 20, 30 tablets in a contour mesh package from a polyvinyl chloride film
    and aluminum foil printed lacquered.

    By 10, 20, 30, 40, 50 or 100 tablets in cans of polymeric for medicines. One jar or 1, 2, 3, 4, 5, 6, 8 or 10 contour squares, together with the instructions for use, are placed in a cardboard package (bundle).

    Packaging:(10) - polymer cans (1) - packs cardboard
    (10) - packings, cellular, outline (1) - packs, cardboard
    (10) - packings cellular planimetric (10) - packs cardboard
    (10) - packings, cellular, outline (2) - packs, cardboard
    (10) - packings, cellular, outline (3) - packs, cardboard
    (10) - packings, cellular, outline (4) - packs, cardboard
    (10) - packings, cellular planimetric (5) - packs cardboard
    (10) - packings, cell planimetric (6) - packs cardboard
    (10) - packings, cellular planimetric (8) - packs cardboard
    (100) - polymer cans (1) - packs of cardboard
    (20) - polymer cans (1) - cardboard packs
    (20) - packings, cell planimetric (1) - packs cardboard
    (20) - packings, cellular planimetric (10) - packs cardboard
    (20) - packings, cellular, outline (2) - packs, cardboard
    (20) - packings, cellular, outline (3) - packs, cardboard
    (20) - packings cellular planimetric (4) - packs cardboard
    (20) - packings, cellular planimetric (5) - packs cardboard
    (20) - packings, cellular planimetric (6) - packs cardboard
    (20) - packings cellular planimetric (8) - packs cardboard
    (30) - polymer cans (1) - packs of cardboard
    (30) - packings cellular planimetric (1) - packs cardboard
    (30) - packings, cellular planimetric (10) - packs cardboard
    (30) - packings cellular planimetric (2) - packs cardboard
    (30) - packings, cellular planimetric (3) - packs cardboard
    (30) - packings cellular planimetric (4) - packs cardboard
    (30) - packings, cellular planimetric (5) - packs cardboard
    (30) - packings, cellular planimetric (6) - packs cardboard
    (30) - packings cellular planimetric (8) - packs cardboard
    (40) - polymer cans (1) - packs cardboard
    (50) - polymer cans (1) - cardboard packs
    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-002128
    Date of registration:05.07.2013
    The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp14.08.2015
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