Active substanceNimesulideNimesulide
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  • Dosage form: & nbsppills
    Composition:

    Each tablet contains:

    Active substance: nimesulide 100 mg.

    Auxiliary substancesa: calcium hydrophosphate 75 mg, cellulose microcrystalline (type 114) 40 mg, corn starch 54 mg, sodium carboxymethyl starch 35 mg, magnesium stearate 3 mg, silicon dioxide colloid 2 mg, talc 1 mg.

    Description:White with a yellowish hue round biconvex tablets with a smooth surface.
    Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)
    ATX: & nbsp

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

    M.01.A.X.17   Nimesulide

    Pharmacodynamics:

    Non-steroidal anti-inflammatory drug (NSAID) from the class of sulfonanilides.It is a selective competitive inhibitor of cyclooxygenase-2 (COX-2), inhibits the synthesis of prostaglandins in the inflammatory focus. The inhibitory effect on COX-1 is less pronounced (it rarely causes side effects associated with the inhibition of prostaglandin synthesis in healthy tissues). Has anti-inflammatory, analgesic and pronounced antipyretic effect.

    Pharmacokinetics:

    Absorption when ingested - high (eating intake reduces the rate of absorption, without affecting its degree). The time to reach the maximum concentration (TСmах) - 1,5-2,5 hours. The connection with plasma proteins is 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acid alpha 1-glycoproteids - 1%. The dose change does not affect the degree of binding. The maximum concentration (Cmax) - 3,5-6,5 mg / l. The volume of distribution is 0.19-0.35 l / kg. Penetrates into the tissue of the female genital organs, where after a single intake its concentration is about 40% of the concentration in the plasma. It penetrates into the acidic environment of the inflammatory focus (40%), synovial fluid (43%). Easily penetrates through the histohematological barriers.

    Metabolized in the liver by tissue monooxygenases. The main metabolite is 4-hydroxynimidesulide (25%), has similar pharmacological activity,However, due to the decrease in the size of the molecules, it is able to rapidly diffuse over hydrophobic channel of COX-2 to the active site, binding of the methyl group. 4-hydroxynimidesulide is a water-soluble compound, for the elimination of which is not required glutathione and the conjugation reaction of the second phase of metabolism (sulfation, glucuronidation and others).

    The half-life (T1/2) nimesulide - 1.56-4.95 h, 4-hydroxynimidesulide - 2.89-4.78 h. 4-hydroxynimidesulide is excreted by the kidneys (65%) and bile (35%), subjected to enterohepatic recirculation.

    In patients with renal insufficiency (creatinine clearance of 1.84.8 l / h or 30-80 ml / min), as well as in children and the elderly, the pharmacokinetic profile of nimesulide does not change significantly.

    Indications:

    - Rheumatoid arthritis;

    - articular syndrome 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 post-traumatic inflammation soft tissues;

    - pain syndrome of different genesis (including in the postoperative period, with trauma, algodismenorea, toothache, headache, arthralgia, lumboeishalgia).

    The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, the progression of the disease is not affected.

    Contraindications:

    Hypersensitivity to the active substance or ancillary components; complete tali incomplete combination of bronchial asthma, recurrent nasal polyposis or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including, in the anamnesis); erosive-ulcerative, changes in the gastric mucosa and; duodenum (duodenum), active gastrointestinal bleeding, cerebrovascular or other bleeding; inflammatory bowel disease; (Crohn's disease, ulcerative colitis) during the exacerbation phase; hemophilia and other bleeding disorders; Decompensated heart failure;

    -hepatic insufficiency or any active liver disease; anamnestic data on the development of hepatotoxic reactions using nimesulide drugs; concomitant use of potentially hepatotoxic substances; alcoholism, drug addiction; marked renal failure (creatinine clearance less than 30 ml / min),progressive kidney disease, confirmed hyperkalemia; period after aortocoronary shunting; pregnancy, lactation; Children under 12 years of age (for this dosage form, see section "Special instructions").

    Carefully:Ischemic heart disease, cerebrovascular disease, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral arterial disease, smoking, creatinine clearance less than 60 ml / min. Anamnestic data on the development of gastrointestinal ulceration ,. infection Helicobacter pylori, old age, prolonged use of NSAIDs, frequent alcohol use, severe somatic diseases, concomitant anticoagulant therapy (eg, warfarin), antiplatelet agents (for example, acetylsalicylic acid, clopidogrel), oral glucocorticosteroids (for example, prednisolone), selective serotonin reuptake inhibitors (eg, citalopram, fluoxetan, paroxetine, sertraline).
    Pregnancy and lactation:The use of the drug may adversely affect female fertility and is not recommended for women planning pregnancy.
    Dosing and Administration:

    A minimum effective dose should be used with the minimum possible short course. Tablets are taken with a sufficient amount of water, preferably after eating. Adults and children over 12 years old inside 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 frequency of side effects is classified according to the incidence of the case: often - (1-10%), sometimes (0.1-1%), rarely (0.01-0.1%), very rarely (less than 0.01% ), including individual messages.

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

    From the central nervous system: infrequently - dizziness; rarely - a sense of fear, nervousness, nightmarish dreams; very rarely - headache, drowsiness, encephalopathy (Reye syndrome).

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

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

    From the gastrointestinal tract: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stool, gastrointestinal bleeding, ulcer and / or perforation of the stomach or duodenum.

    From the liver and bile excretory system: often - increased "liver" transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis.

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

    From the sense organs: rarely - blurred vision.

    From the side of the cardiovascular system: infrequently - arterial hypertension; rarely - tachycardia, hemorrhages, "hot flashes".

    Other: rarely - general weakness; very rarely - hypothermia.

    Overdose:

    Symptoms: apathy, drowsiness, nausea, vomiting. There may be gastrointestinal bleeding, increased blood pressure, acute renal failure, respiratory depression.

    Treatment: requires symptomatic treatment of the patient and maintenance of care for him. There is no specific antidote. In case an overdose has occurred within the last 4 hours, it is necessary to induce vomiting, to receive activated charcoal (60-100 g per adult), osmotic laxatives. Forced diuresis, hemodialysis are ineffective because of the high connection of the drug with proteins.

    Interaction:

    The effect of medications that reduce blood coagulability, increases with their simultaneous use with nimesulide.

    Nimesulide may reduce the action of furosemide. Nimesulide can increase the possibility of side effects with the simultaneous administration of methotrexate.

    The level of lithium in the plasma increases with simultaneous reception of lithium and nimesulide preparations.

    Nimesulide can enhance the action of cyclosporin on the kidneys.

    Use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of developing gastrointestinal bleeding.

    Special instructions:

    Since Nise® is partially excreted by the kidneys, its dose for patients with impaired renal function should be reduced, depending on the creatinine clearance values. Given reports of visual impairment in patients taking other NSAIDs, treatment should be stopped immediately if any visual impairment occurs and the oculist should examine the patient.

    The drug can cause fluid retention in the tissues, therefore, patients with high blood pressure and with cardiac abnormalities Nyz® should be used with extreme caution.

    Patients should undergo regular medical supervision if they take medications along with nimesulide, for which the effect on the gastrointestinal tract is characteristic.

    When there are signs of liver damage (skin itching, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of the urine,increase in the level of "liver" transaminases) should stop taking the drug and consult your doctor.

    Do not use the drug simultaneously with other NSAIDs.

    The drug can change the properties of platelets, but does not replace the preventive effect of acetylsalicylic acid in cardiovascular diseases.

    After 2 weeks of using the drug, it is necessary to monitor biochemical parameters, liver function.

    This dosage form is contraindicated for children under 12 years of age, but if nimesulide is needed in children older than 7 years, dispersible tablets of 50 mg and suspension may be used, in strict compliance with the medical instructions attached to them.

    Effect on the ability to drive transp. cf. and fur:Since the drug can cause drowsiness, dizziness and blurred vision, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:

    Tablets of 100 mg.

    Packaging:1, 2 or 10 PVC / aluminum blisters for 10 tablets together with instructions for use are packed in a cardboard box.
    Storage conditions:

    List B.

    In a dry, protected from light 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 expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012824 / 03
    Date of registration:26.05.2009 / 05.11.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India
    Manufacturer: & nbsp
    Representation: & nbspDr. Reddy`c Laboratoris Ltd.Dr. Reddy`c Laboratoris Ltd.
    Information update date: & nbsp23.05.2018
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