Nimesulide Izvarino pills 100mg N20
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Active ingredients
Nimesulide
Release form
Pills
Composition
Nimesulide 100 mg.
Pharmacological effect
Nimesulide is a nonsteroidal anti-inflammatory drug (NSAID) from the sulfonanilide class. 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). Communication with plasma proteins is 95%, with erythrocytes - 2%, with lipoproteins - 1%, with acid alpha1-glycoproteins - 1%. Changing the dose does not affect the degree of binding. Cmax = 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 through the hydrophobic channel of COX-2 to the active binding site of the methyl group. 4-hydroxynimesulide is a water-soluble compound, for the elimination of which glutathione and conjugation reactions of the second phase of metabolism (sulfation, glucuronide and others) are not required. T1 / 2 nimesulide - about 1.56-4.95 h, 4-hydroxynimesulide - 2.89-4.78 hours. 4-hydroxynimesulide is excreted by the kidneys (65%) and with bile (35%), undergoes enterohepatic recirculation. 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 of soft tissues, pain syndrome of various genesis (including in the postoperative period, with injuries, algomenorrhea, toothache, headache, arthralgia, lumboischialgia), febrile syndrome in infectious and inflammatory diseases.
Contraindications
Hypersensitivity to the components of the drug, erosive and ulcerative lesions of the gastrointestinal tract (in the acute phase), bleeding from the gastrointestinal tract; a history of bronchospasm, urticaria or acute rhinitis associated with the use of acetylsalicylic acid, NSAIDs; liver failure; renal failure (creatinine clearance less than 30 ml / min, confirmed hyperkalemia), severe heart failure, pronounced coagulation disorders, the period after coronary artery bypass surgery, pregnancy, lactation, children up to 12 years. With care: ischemic heart disease, cerebrovascular diseases, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes, peripheral artery disease, smoking, creatinine clearance less than 60 ml / min. Anamnestic data on the development of ulcerative lesions of the gastrointestinal tract, the presence of Helicobacter pylori infection, old age, long-term use of NSAIDs, frequent use of alcohol, severe somatic diseases, concomitant therapy with the following drugs: anticoagulants (for example, warfarin) antiplatelet agents (for example, acetylsalicylic acid, coagidulants (for example, warfarin) antiplatelet agents (for example, acetylsalicylic acid, coagidulants (for example, warfarin) antiplatelet agents (for example, acetylsalicylic acid, coagidulants (for example, warfarin)) (for example, prednisolone) selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).
Dosage and administration
Adults and children over 12 years old (body weight more than 40 kg) are prescribed pills, 1 tablet 2 times a day. Take the pills after meals with enough water. The maximum daily dose of 200 mg.
Side effects
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. Central nervous system: infrequently - dizziness; rarely - a feeling of fear, nervousness, nightmares; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome). Respiratory: infrequently - shortness of breath; very rarely - asthma, bronchospasm.Cardiovascular system: infrequently - arterial hypertension; rarely - tachycardia, hemorrhages, "tides". Sense organs: rarely - blurred vision, very rarely - dizziness. Skin and mucous membranes: not often - itching, rash, increased sweating; rarely: erythema, dermatitis; very rarely: urticaria, angioneurotic edema , edema of the face, erythema multiforme exudative, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome). Liver and biliary system: often - increased "liver" transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis . Kidneys and m ocular system: infrequently - edema, rarely - dysuria, hematuria, urinary retention, hyperkalemia, very rarely - renal failure, oliguria, interstitial nephritis. Allergic reactions: rarely - hypersensitivity reactions; very rarely - mafialactoid reactions. General reactions: rarely - general weakness, very rarely - hypothermia. In the event of the appearance of other side effects not mentioned above or deterioration of your health, please contact your doctor immediately.
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. Reduces the therapeutic effect of antihypertensive drugs. Nimesulide may increase the possibility of side effects while taking methotrexate. The level of lithium in plasma increases while taking drugs of lithium and nimesulide. Due to the high degree of nimesulide binding to plasma proteins, patients who are simultaneously treated with hydantoin and sulfonamides should be under the supervision of a physician, undergoing examination at short intervals. Nimesulide may enhance the effect of cyclosporine on the kidneys. Use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of developing gastrointestinal bleeding.
special instructions
Nimesulide should be used with caution in patients who have a tendency to bleed, patients with diseases of the upper gastrointestinal tract or patients receiving drugs that reduce blood clotting, or drugs that inhibit platelet aggregation.Since Nimesulide is partially excreted by the kidneys, its dosage for patients with impaired renal function should be reduced, depending on the level of urination. Considering reports of visual impairment in patients taking other NSAIDs, treatment should be immediately discontinued if any visual impairment occurs and the patient should be examined by an oculist. The drug can cause fluid retention in the tissues, so patients with high blood pressure and with impaired cardiac activity Nimesulide should be used with extreme caution. Patients should undergo regular medical supervision if they, along with nimesulide, take medicines, which have an effect on the gastrointestinal tract. Patients whose work requires concentration (constant attention) should be aware that the drug may cause drowsiness or dizziness. To reduce the risk of adverse events from the gastrointestinal tract, use the minimum effective dose of the shortest possible course.