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Active ingredients
Nimesulide
Release form
Pills
Composition
Each tablet contains: Active ingredient: nimesulide 100 mg. Excipients: calcium hydrophosphate 75 mg, cellulose; microcrystalline (type 114) 40 mg, corn starch 54 mg, carboxymethyl starch sodium 35 mg, magnesium stearate 3 mg, colloidal silicon dioxide 2 mg, talc 1 mg.
Pharmacological effect
Nonsteroidal anti-inflammatory drug (NSAIDs) from the class of sulfonanilides. It is a selective competitive inhibitor of cyclooxygenase-2 (COX-2), inhibits the synthesis of prostaglandins in the focus of inflammation. The inhibitory effect on COX-1 is less pronounced (less likely to cause side effects associated with inhibition of prostaglandin synthesis in healthy tissues). It has anti-inflammatory, analgesic and pronounced antipyretic effect.
Pharmacokinetics
Oral absorption is high (food intake decreases the rate of absorption without affecting its degree). The time to reach the maximum concentration (Tmax) is 1.5-2.5 hours. Communication with plasma proteins is 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acid alpha-glycoproteins - 1%. Changing the dose does not affect the degree of binding. The maximum concentration (Smah) is 3.5-6.5 mg / l. The volume of distribution is 0.19-0.35 l / kg. It penetrates the tissue of the female genital organs, where, after a single dose, its concentration is about 40% of the concentration in plasma. It penetrates well into the acidic environment of the focus of inflammation (40%), synovial fluid (43%). Easily penetrates histohematogenous barriers .; Metabolized in the liver by tissue mono-oxygenases. The main metabolite, 4-hydroxynimesulide (25%), has similar pharmacological activity, but due to a decrease in the size of molecules, it is able to quickly diffuse the hydrophobic channel of COX-2 to the active binding site of the methyl group. 4-hydroxynimesulide is a water-soluble compound, the elimination of which does not require glutathione and conjugation reactions of the second phase of metabolism (sulfation, glucuronide and others) .; The half-life (T1 / 2) of nimesulide is 1.56-4.95 h, 4-hydroxynimesulide - 2.89- 4.78 h. 4-hydroxynimesulide is excreted by the kidneys (65%) and with bile (35%), is subjected to enterohepatic recycling .; In patients with renal insufficiency (creatinine clearance 1.8-4.8 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 genesis; - inflammation of ligaments, tendons, bursitis, including post-traumatic inflammation, soft tissues; - pain syndrome of various genesis (including in the postoperative period, with; injuries, algomenorrhea, toothache, headache, arthralgia, lumboischialgia) .; The drug is intended for symptomatic therapy, reducing pain and inflammation at the time of use, does not affect the progression of the disease.
Contraindications
Hypersensitivity to the active substance or auxiliary components; complete or incomplete combination of asthma, recurrent polyposis of the nose or paranasal sinuses and intolerance to acetylsalicylic acid and other NSAIDs (including a history of); erosive and ulcerative changes of the mucous membrane of the stomach and duodenum (WPC), active gastrointestinal bleeding, cerebrovascular or other bleeding; inflammatory bowel disease (Crohn's disease, ulcerative colitis) in the acute phase; hemophilia and other bleeding disorders; decompensated heart failure; liver failure or any active liver disease; anamnestic data on the development of hepatotoxic reactions with the use of nimesulide preparations; concomitant use of potentially hepatotoxic substances; alcoholism, drug addiction; severe renal failure (creatinine clearance less than 30 ml / min), progressive kidney disease, confirmed hyperkalemia; the period after coronary artery bypass surgery; pregnancy, lactation; children's age up to 12 years (for this dosage form, see the section "Special instructions").
Use during pregnancy and lactation
Contraindicated
Dosage and administration
The minimum effective dose should be used with the shortest possible short course. Tablets are taken with a sufficient amount of water, preferably after meals. Adults and children over 12 years old with 1 tablet 2 times a day.In the presence of diseases of the gastrointestinal tract, it is desirable to take the drug at the end of a meal or after a meal. 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 depending on the frequency of occurrence 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 side of the central nervous system: infrequently - dizziness; rarely - a feeling of fear, nervousness, nightmares; very rarely - headache, drowsiness, encephalopathy (Reis syndrome) .; On the part of the skin: infrequently - itching, rash, increased sweating; rarely: erythema, dermatitis; very rarely: urticaria, angioedema, facial swelling, erythema multiforme exudative, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome) .; From the urinary system: infrequently - edema; rarely - dysuria, hematuria, urinary retention, hyperkalemia; very rarely - renal failure, oliguria, interstitial nephritis .; On the part of the gastrointestinal tract: often - diarrhea, nausea, vomiting; infrequently - constipation, flatulence, gastritis; very rarely - abdominal pain, stomatitis, tarry stools, gastrointestinal bleeding, ulcers and / or perforation of the stomach or duodenum. On the part of the liver and biliary system: often - increased “liver” transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis. From the side of blood-forming organs: rarely - anemia, eosinophilia; very rarely, thrombocytopenia, pancytopenia, purpura, lengthening of bleeding time On the part of the respiratory system: infrequently - shortness of breath; very rarely - exacerbation of asthma, bronchospasm. From the senses: rarely - blurred vision .; Since 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: the patient needs symptomatic treatment and supportive care. There is no specific antidote.If an overdose occurred during the last 4 hours, it is necessary to induce vomiting, to ensure the intake of activated carbon (60-100 g per adult), osmotic laxatives. Forced diuresis, hemodialysis are ineffective due to the high association of the drug with proteins.
Interaction with other drugs
The effect of drugs that reduce blood clotting, increases with their simultaneous use with nimesulide .; Nimesulide may reduce the effects of furosemide. Nimesulide may increase the possibility of side effects while taking methotrexate .; The level of lithium in the plasma increases while taking drugs of lithium and nimesulide .; Nimesulide may increase the effects of cyclosporine on the kidneys .; Use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of 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 indicators of creatinine clearance. Considering reports of visual impairment in patients taking other NSAIDs, treatment should be immediately discontinued if any visual impairment occurs and the eye doctor must be examined by the patient .; The drug can cause fluid retention in the tissues, so for patients with high blood pressure and with impaired cardiac activity, nise should be used with extreme caution .; Patients should undergo regular medical supervision if they, along with nimesulide, take medicines that have an effect on the gastrointestinal tract .; If there are signs of liver damage (itching, yellowing of the skin, nausea, vomiting, abdominal pain, darkening of the urine, increased levels of liver transaminases), you should stop taking the drug and contact your doctor. Do not use the drug simultaneously with other NSAIDs .; The drug can change the properties of platelets, but does not replace the prophylactic action of acetylsalicylic acid in cardiovascular diseases. Use of the drug may adversely affect female fertility and is not recommended for women.planning a pregnancy .; After 2 weeks of use of the drug, monitoring of the biochemical parameters of liver function is necessary .; This dosage form is contraindicated for children up to 12 years old, but if necessary, use nimesulide in children over 7 years old, dispersible 50 mg pills and suspension can be used, in strict accordance with the instructions for medical use attached to them .; Since the drug can cause drowsiness, dizziness and blurred vision, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.