Nimulid pills 100 mg 20 pcs
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Active ingredients
Nimesulide
Release form
Pills
Composition
1 tablet contains: Active ingredient: Nimesulide 100 mg.
Pharmacological effect
Nimulid is a NSAID of the sulfonalide class. It has anti-inflammatory, analgesic and antipyretic effects. Nimesulide refers to NSAIDs, the mechanism of action of which is associated with selective inhibition of cyclooxygenase-2 (COX-2) and effects on a number of other factors: suppression of platelet activating factor, tumor necrosis factor alpha, suppression of proteinases and histamine. Selectively suppressing COX-2, reduces the biosynthesis of prostaglandins in the inflammation, has a less pronounced inhibitory effect on COX-1 (rarely causes side effects associated with inhibition of the synthesis of prostaglandins in healthy tissues).
Pharmacokinetics
Oral absorption is high (food intake decreases the rate of absorption without affecting its degree). Plasma protein binding - 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. Vd - 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 monooxygenases. 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, which does not require glutathione and conjugation reactions of the second phase of metabolism (sulfation, glucuronation, etc.) for nitride. T1 / 2 nimesulide - about 1.56–4.95 h, 4-hydroxyminesulide - 2.89–4.78 parts 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 nimesulide profile 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, incl.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
gastric ulcer and duodenal ulcer in the acute phase, acute bleeding from the gastrointestinal tract, moderate and severe liver failure, renal failure (CC less than 30 ml / min), hypersensitivity to nimesulide and other NSAIDs (including acetylsalicylic acid).
Precautionary measures
Do not exceed recommended doses. With caution: coronary heart disease, cerebrovascular diseases, congestive heart failure, dyslipidemia / hyperlipidemia, diabetes mellitus, peripheral artery disease, smoking, creatinine clearance less than 60 ml / min, anamnestic data on the development of gastric ulcer, infection Helicobacter pylori, 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, clopidogrel); - oral GCS (for example, prednisolone); - selective serotonin reuptake inhibitors (for example, citalopram, fluoxetine, paroxetine, sertraline).
Use during pregnancy and lactation
The drug is contraindicated in pregnancy and lactation.
Dosage and administration
The lingual tablet should be put on the tongue, where it immediately begins to dissolve, then swallow the saliva in which the tablet has dissolved. The maximum daily dose is 200 mg.
Side effects
On the part of the digestive 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 CNS side: infrequently - dizziness; rarely - a feeling of fear, nervousness, nightmares; very rarely - headache, drowsiness, encephalopathy (Reye's syndrome). On the part of the respiratory system: infrequently - shortness of breath; very rarely - bronchospasm; exacerbation of bronchial asthma is possible. From the side of the cardiovascular system: infrequently - arterial hypertension; rarely - tachycardia, hemorrhages, hot flashes. From the senses: rarely - blurred vision. Skin and mucous membranes: rarely - itching, rash, increased sweating; rarely erythema,dermatitis. Liver and biliary system: often - increased activity of hepatic transaminases; very rarely - hepatitis, fulminant hepatitis, jaundice, cholestasis. Kidneys and urinary system: infrequently - edema; rarely - dysuria, hematuria, urinary retention, hyperkalemia; very rarely - renal failure, oliguria, interstitial nephritis. On the side of the blood-forming organs: rarely - anemia, eosinophilia; very rarely - thrombocytopenia, pancytopenia, purpura, prolongation of bleeding time. Allergic reactions: rarely - hypersensitivity reactions; very rarely - anaphylactoid reactions, urticaria, angioedema, swelling of the face, erythema multiforme, including erythema. Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome). General reactions: rarely - general weakness; very rarely - hypothermia.
Overdose
Symptoms: apathy, drowsiness, nausea, vomiting. Gastrointestinal bleeding may occur, arterial hypertension, acute renal failure, respiratory depression. Treatment: symptomatic treatment of the patient is required, there is no specific antidote. If an overdose occurred during the last 4 hours, it is necessary to induce vomiting, to receive 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 effect of furosemide. Reduces the therapeutic effect of antihypertensive drugs. Nimesulide increases the onset of side effects while taking methotrexate. The level of lithium in plasma increases while taking drugs of lithium and nimesulide. Nimesulide may enhance the nephrotoxic effect of cyclosporine on the kidneys. Use with glucocorticosteroids, serotonin reuptake inhibitors increases the risk of gastrointestinal bleeding.
special instructions
Nimulid should be used with caution in patients who have a tendency to bleed, in patients with diseases of the upper GI tract or in patientsreceiving Anticoagulation , and the patient must be examined by an oculist. The drug may cause fluid retention in the tissues, therefore, patients with high blood pressure and cardiac abnormalities ty Nimulid should be used with extreme caution. To reduce the risk of adverse events from the gastrointestinal tract, a minimum effective dose should be used for the shortest possible course. Effect on the ability to drive and control machinery care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of imani and the speed of psychomotor reactions.